Provided is a pharmaceutical composition containing compound 1, the pharmaceutical composition having excellent disintegratability and bioavailability. The pharmaceutical composition comprises: a granulated product containing 3-ethyl-4-{4-[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl}benzamide or a pharmaceutically acceptable salt thereof; and crystalline cellulose, and has a disintegration time of within 360 seconds in a coated tablet form.
A61K 9/28 - DragéesPilules ou comprimés avec revêtements
A61K 31/437 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec un azote comme seul hétéro-atome d'un cycle condensés en ortho ou en péri avec des systèmes hétérocycliques le système hétérocyclique contenant un cycle à cinq chaînons ayant l'azote comme hétéro-atome du cycle, p. ex. indolizine, bêta-carboline
The invention provides biomarkers to predict effective treatment of cancer using an IAP antagonist. Identifying one or more of the identified biomarkers in a cancer patient allows a determination to be made whether the patient's cancer is likely to be successfully treated using an IAP antagonist. Accordingly, the invention relates generally to a companion diagnostic for IAP antagonist therapy. In particular, the biomarkers include IL-2Rα, IL-6r, CRP, EPO, CD27, CD40, TN-C, IL-18, PLGF, TNFrl and MCP-4.
Provided is a crystal of a compound having EGFR inhibition ability or a salt thereof, said crystal being excellent in one or more characteristics of stability, hygroscopicity and oral absorbability. One aspect of the present invention provides a crystal form of N-(4-(4-amino-6-ethynyl-5-(quinolin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)bicyclo[2.2.1]heptan-1-yl)-5-methylpyrazine-2-carboxamide the diffraction angle (2θ±0.2°) of which has a peak at a preset angle in the X-ray powder diffraction spectrum.
The present invention provides a method for producing a compound represented by formula (I) suitable for mass synthesis as API. Provided according to one aspect of the present invention is a method for producing a compound represented by formula (I) or a salt thereof, the method including deprotecting a protecting group represented by R1 in formula (II) under basic conditions to thereby form a compound represented by formula (I) or a salt thereof.
The present invention provides a method for producing a compound represented by formula (I) suitable for mass synthesis as API. Provided according to one aspect of the present invention is a method for producing a compound represented by formula (I) or a salt thereof, the method including deprotecting a protecting group represented by R1 in formula (II) under basic conditions to thereby form a compound represented by formula (I) or a salt thereof.
The problem addressed is to provide an agent for preventing or treating steroid osteoporosis. The problem is solved by an agent for preventing or treating steroid osteoporosis that contains a Piezo1 and/or an Hes1 enhancer.
A61K 45/00 - Préparations médicinales contenant des ingrédients actifs non prévus dans les groupes
A61K 31/497 - Pyrazines non condensées contenant d'autres hétérocycles
A61K 31/573 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrèneLeurs dérivés, p. ex. stéroïdes substitués en position 17 bêta par une chaîne à deux atomes de carbone, p. ex. prégnane ou progestérone substitués en position 21, p. ex. cortisone, dexaméthasone, prednisone ou aldostérone
A61P 19/10 - Médicaments pour le traitement des troubles du squelette des maladies osseuses, p. ex. rachitisme, maladie de Paget de l'ostéoporose
C12N 15/12 - Gènes codant pour des protéines animales
C12N 15/52 - Gènes codant pour des enzymes ou des proenzymes
6.
2'-DEOXY-2',2'-DIFLUOROTETRAHYDROURIDINES WITH HIGH PURITY AND METHODS OF MAKING THE SAME
The invention relates to methods of synthesizing 2′-deoxy-2′,2′-difluorotetrahydrouridine with increased purity and uniform particle size distribution. In particular, methods of the invention include crystallization and isolation procedures rendering synthetic reaction intermediates. The invention further includes compositions comprising the final compound in highly pure form, including lower number of impurities and lower levels of individual and total impurities.
The present disclosure relates to novel crystalline forms of sulfonamide compounds, pharmaceutical compositions containing the crystalline form compounds and methods of preparing and using the same.
C07D 271/113 - Oxadiazoles-1, 3, 4Oxadiazoles-1, 3, 4 hydrogénés avec des atomes d'oxygène, de soufre ou d'azote, liés directement aux atomes de carbone du cycle, les atomes d'azote ne faisant pas partie d'un radical nitro
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
8.
ANTI-TUMOR AGENT CONTAINING TAXANE COMPOUND, AND ANTI-TUMOR EFFECT ENHANCER
In order to provide a novel cancer treatment method using a FTD-TPI combination drug that exhibits markedly excellent anti-tumor effects with fewer side effects, the present invention provides an anti-tumor agent characterized in that the FTD.TPI combination drug and a taxane compound are administered in combination.
A61K 31/7072 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p. ex. cytidine, acide cytidylique ayant deux groupes oxo liés directement au cycle pyrimidine, p. ex. uridine, acide uridylique, thymidine, zidovudine
A61K 31/337 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à quatre chaînons, p. ex. taxol
A61K 31/513 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime ayant des groupes oxo liés directement à l'hétérocycle, p. ex. cytosine
9.
BRAIN-MIGRATING TUMOR TREATMENT AGENT CONTAINING, AS ACTIVE INGREDIENT, N-(4-(4-AMINO-6-ETHYNYL-5-(QUINOLIN-3-YL)-7H-PYRROLO[2,3-D]PYRIMIDIN-7-YL) BICYCLO[2.2.1]HEPTAN-1-YL)-5-METHYLPYRAZINE-2-CARBOXAMIDE OR SALT THEREOF
The present invention provides a brain-migrating anti-tumor agent that exhibits brain migration ability and EGFR inhibitory activity. One embodiment of the present invention provides a brain-migrating anti-tumor agent comprising, as an active ingredient, N-(4-(4-amino-6-ethynyl-5-(quinolin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl) bicyclo[2.2.1]heptan-1-yl)-5-methylpyrazine-2-carboxamide or a salt thereof.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations, namely, pharmaceutical preparations for the treatment of inflammation
11.
METHODS OF TREATING CANCER WITH IAP ANTAGONIST COMPOUNDS AND COMBINATION THERAPIES
The present disclosure relates generally to use of a compound of formula (I), also named ASTX660 in combination therapies for treating cancer, in particular leukemia.
A61K 31/5377 - 1,4-Oxazines, p. ex. morpholine non condensées et contenant d'autres hétérocycles, p. ex. timolol
A61K 31/573 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrèneLeurs dérivés, p. ex. stéroïdes substitués en position 17 bêta par une chaîne à deux atomes de carbone, p. ex. prégnane ou progestérone substitués en position 21, p. ex. cortisone, dexaméthasone, prednisone ou aldostérone
A61K 31/635 - Composés contenant des groupes para-N-benzènesulfonyl-N-, p. ex. sulfanilamide, p-nitrobenzènesulfonohydrazide contenant un hétérocycle, p. ex. sulfadiazine
A61P 35/02 - Agents anticancéreux spécifiques pour le traitement de la leucémie
12.
COMBINATION DECITABINE AND CEDAZURIDINE SOLID ORAL DOSAGE FORMS
Embodiments of the present invention provide solid oral dosage forms that upon daily administration to a subject provide plasma levels of decitabine with a 5-day AUC for decitabine that is equivalent to the 5-day AUC for a daily IV dose of decitabine of 20 mg/m2 administered as a one hour (1 h) infusion. Also provided according to embodiments of the present invention are solid oral dosage forms wherein upon daily administration to a subject provides a pharmacodynamic effect that is equivalent to the pharmacodynamic effect for a daily intravenous dose of decitabine of 20 mg/m2 administered as a one hour (1 h) infusion. Also provided are methods of treatment using a solid oral dosage form according to an embodiment of the invention.
A61K 31/706 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
A61K 9/48 - Préparations en capsules, p. ex. de gélatine, de chocolat
A61K 31/20 - Acides carboxyliques, p. ex. acide valproïque ayant un groupe carboxyle lié à une chaîne acyclique d'au moins sept atomes de carbone, p. ex. acides stéarique, palmitique ou arachidique
A61K 31/7016 - Disaccharides, p. ex. lactose, lactulose
An object of the present disclosure is to provide a crystalline form of 3-(15-methoxypentadecyl)-2, 4, 4-trimethylcyclohex-2-en-1-one, the crystalline form having excellent stability and being preferable in terms of production. The present disclosure provides a crystalline form having characteristic peaks at diffraction angles) (2θ+0.2° of 7.0°, 14.0°, 17.5°, 19.5°, 21.0°, 23.7°, and 24.8° in a powder X-ray diffraction spectrum (CuKα).
C07C 49/753 - Composés non saturés comportant un groupe cétone faisant partie d'un cycle contenant des groupes éther, des groupes , des groupes ou des groupes
Provided are a novel cancer treatment method and immunostimulant which exhibit a remarkably excellent antitumor effect with little side effects. An antitumor agent and an immunostimulant include an azabicyclo compound and an immune checkpoint molecule regulator which are administered in combination.
A61K 31/437 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec un azote comme seul hétéro-atome d'un cycle condensés en ortho ou en péri avec des systèmes hétérocycliques le système hétérocyclique contenant un cycle à cinq chaînons ayant l'azote comme hétéro-atome du cycle, p. ex. indolizine, bêta-carboline
A61K 39/395 - AnticorpsImmunoglobulinesImmunsérum, p. ex. sérum antilymphocitaire
Provided is a method of treating malignant tumor by an azabicyclic compound, particularly, with eye disorder reduced. The present invention provides a method for treating malignant tumor, comprising administering an effective amount of 3-ethyl-4-[3-(1-methylethyl)-4-[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-1H-pyrazolo[3,4-b]pyridin-1-yl]benzamide (compound 1) or a salt thereof to a patient in need thereof according to a dosing regimen, wherein the dosing regimen comprises administering the compound 1 or the salt thereof at a dose from 40 mg/body/day to 240 mg/body/day in terms of the amount of the compound 1 for consecutive days, and then providing a withdrawal period of at least 2 days.
A61K 31/437 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec un azote comme seul hétéro-atome d'un cycle condensés en ortho ou en péri avec des systèmes hétérocycliques le système hétérocyclique contenant un cycle à cinq chaînons ayant l'azote comme hétéro-atome du cycle, p. ex. indolizine, bêta-carboline
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
This invention provides an antibody that binds specifically to sulfated glycosaminoglycan (sGAG) in a pH-dependent manner. The antibody that binds specifically to sulfated glycosaminoglycan is at least one antibody selected from the group consisting of (1) to (3): (1) an antibody comprising a heavy chain that comprises CDR1 consisting of the amino acid sequence represented by SEQ ID NO: 1, CDR2 consisting of the amino acid sequence represented by SEQ ID NO: 2, and CDR3 consisting of the amino acid sequence represented by SEQ ID NO: 3 and a light chain that comprises CDR1 consisting of the amino acid sequence represented by SEQ ID NO: 4, CDR2 consisting of the amino acid sequence represented by LGS, and CDR3 consisting of the amino acid sequence represented by SEQ ID NO: 6; (2) an antibody comprising a heavy chain that comprises CDR1 consisting of the amino acid sequence represented by SEQ ID NO: 7, CDR2 consisting of the amino acid sequence represented by SEQ ID NO: 8, and CDR3 consisting of the amino acid sequence represented by SEQ ID NO: 9 and a light chain that comprises CDR1 consisting of the amino acid sequence represented by SEQ ID NO: 10, CDR2 consisting of the amino acid sequence represented by AAS, and CDR3 consisting of the amino acid sequence represented by SEQ ID NO: 12; and (3) an antibody comprising a heavy chain that comprises CDR1 consisting of the amino acid sequence represented by SEQ ID NO: 13, CDR2 consisting of the amino acid sequence represented by SEQ ID NO: 14, and CDR3 consisting of the amino acid sequence represented by SEQ ID NO: 15 and a light chain that comprises CDR1 consisting of the amino acid sequence represented by SEQ ID NO: 16, CDR2 consisting of the amino acid sequence represented by WAS, and CDR3 consisting of the amino acid sequence represented by SEQ ID NO: 18.
C07K 16/30 - Immunoglobulines, p. ex. anticorps monoclonaux ou polyclonaux contre du matériel provenant d'animaux ou d'humains contre des récepteurs, des antigènes de surface cellulaire ou des déterminants de surface cellulaire provenant de cellules de tumeurs
A61K 39/00 - Préparations médicinales contenant des antigènes ou des anticorps
A61K 47/68 - Préparations médicinales caractérisées par les ingrédients non actifs utilisés, p. ex. les supports ou les additifs inertesAgents de ciblage ou de modification chimiquement liés à l’ingrédient actif l’ingrédient non actif étant chimiquement lié à l’ingrédient actif, p. ex. conjugués polymère-médicament l’ingrédient non actif étant un agent de modification l’agent de modification étant un anticorps, une immunoglobuline ou son fragment, p. ex. un fragment Fc
Provided is a novel method for treating cancer using an HSP90 inhibitor which exhibits a markedly superior antitumor effect and has a reduced side effect.
Provided is a novel method for treating cancer using an HSP90 inhibitor which exhibits a markedly superior antitumor effect and has a reduced side effect.
An antitumor agent is characterized in that an azabicyclo compound of the following Formula (1) or a salt thereof is administered in combination with other antitumor agent (s).
Provided is a novel method for treating cancer using an HSP90 inhibitor which exhibits a markedly superior antitumor effect and has a reduced side effect.
An antitumor agent is characterized in that an azabicyclo compound of the following Formula (1) or a salt thereof is administered in combination with other antitumor agent (s).
A61K 31/437 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec un azote comme seul hétéro-atome d'un cycle condensés en ortho ou en péri avec des systèmes hétérocycliques le système hétérocyclique contenant un cycle à cinq chaînons ayant l'azote comme hétéro-atome du cycle, p. ex. indolizine, bêta-carboline
A61K 31/337 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à quatre chaînons, p. ex. taxol
A61K 31/454 - Pipéridines non condensées, p. ex. pipérocaïne contenant d'autres systèmes hétérocycliques contenant un cycle à cinq chaînons avec l'azote comme hétéro-atome du cycle, p. ex. pimozide, dompéridone
A61K 31/506 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime non condensées et contenant d'autres hétérocycles
A61K 31/517 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des systèmes carbocycliques, p. ex. quinazoline, périmidine
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
A61K 31/5377 - 1,4-Oxazines, p. ex. morpholine non condensées et contenant d'autres hétérocycles, p. ex. timolol
A61K 31/555 - Composés hétérocycliques contenant des métaux lourds, p. ex. hémine, hématine, mélarsoprol
A61K 31/704 - Composés ayant des radicaux saccharide liés à des composés non-saccharide par des liaisons glycosidiques liés à un composé carbocyclique, p. ex. phloridzine liés à un système carbocyclique condensé, p. ex. sennosides, thiocolchicosides, escine, daunorubicine, digitoxine
A61K 31/7048 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'oxygène comme hétéro-atome d'un cycle, p. ex. leucoglucosane, hespéridine, érythromycine, nystatine
A61K 31/7068 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p. ex. cytidine, acide cytidylique
The present invention provides an antitumor agent for treating a malignant tumor patient expressing EGFR having at least one mutation selected from the group consisting of L718X mutation in exon 18 and L792X mutation in exon 20, wherein X represents an arbitrary amino-acid residue, the antitumor agent comprising (S)-N-(4-amino-6-methyl-5-(quinolin-3-yl)-8,9-dihydropy-rimido[5,4-b]indolizin-8-yl)acrylamide (Compound (A)) or a salt thereof.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of immune diseases and disorders; immunomodulators; immunosuppressive agents; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of immune diseases and disorders; immunomodulators; immunosuppressive agents; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders, pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood, pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders, pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood, pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders, pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood, pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders, pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood, pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders, pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood, pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders, pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood, pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; chemical reagents for medical purposes in the field of oncology
29.
CRYSTALS OF 7H-PYRROLO[2,3-D]PYRIMIDIN-4-AMINE DERIVATIVES
Crystalline forms of N-(4-(4-amino-6-ethynyl-5-(quinolin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-7- yl)bicyclo[2.2.1]heptan-1-yl)-5-methylpyrazine-2-carboxamide (TAS3351), a compound having an inhibitory effect against EGFR and an acid. The crystalline forms have advantageous physical properties including stability, hygroscopicity, and oral absorption. The crystalline forms have peaks in a powder X-ray diffraction spectrum at specific diffraction angles (2θ ± 0.2°).
A61K 31/395 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines
A61K 31/505 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
A61K 31/166 - Amides, p. ex. acides hydroxamiques ayant des cycles aromatiques, p. ex. colchicine, aténolol, progabide ayant l'atome de carbone d'un groupe carboxamide lié directement au cycle aromatique, p. ex. procaïnamide, procarbazine, métoclopramide, labétalol
The present disclosure relates to methods of treating a cancer in a subject in need thereof, comprising administering to the subject futibatinib or a pharmaceutically acceptable salt thereof, pembrolizumab or a pharmaceutically acceptable salt thereof, and at least one additional anti-cancer therapy agent or a pharmaceutically acceptable salt thereof. In some embodiments, the at least one additional anti-cancer therapy agent is a chemotherapeutic agent.
A61K 31/4025 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil non condensés et contenant d'autres hétérocycles, p. ex. cromakalim
A61K 31/407 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil condensés avec des systèmes hétérocycliques, p. ex. kétorolac, physostigmine
A61K 31/7115 - Acides nucléiques ou oligonucléotides ayant des bases modifiées, c.-à-d. autres que l'adénine, la guanine, la cytosine, l'uracile ou la thymine
The present disclosure relates to methods of treating a cancer in a subject in need thereof, comprising administering to the subject futibatinib or a pharmaceutically acceptable salt thereof, pembrolizumab or a pharmaceutically acceptable salt thereof, and at least one additional anti-cancer therapy agent or a pharmaceutically acceptable salt thereof. In some embodiments, the at least one additional anti-cancer therapy agent is a chemotherapeutic agent.
A61K 31/4025 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil non condensés et contenant d'autres hétérocycles, p. ex. cromakalim
A61K 31/407 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil condensés avec des systèmes hétérocycliques, p. ex. kétorolac, physostigmine
A61K 31/7115 - Acides nucléiques ou oligonucléotides ayant des bases modifiées, c.-à-d. autres que l'adénine, la guanine, la cytosine, l'uracile ou la thymine
The present disclosure relates to a juniper pollen protein selected from (a)-(c) below. (a) A protein comprising an amino acid sequence represented by SEQ ID NO: 2. (b) A protein comprising an amino acid sequence represented by SEQ ID NO: 2 with one or several amino acids substituted, deleted, or added, and having a juniper pollen allergen activity. (c) A protein having at least 90% amino acid identity with the amino acid sequence represented by SEQ ID NO: 2, and having a juniper pollen allergen activity.
C07K 16/16 - Immunoglobulines, p. ex. anticorps monoclonaux ou polyclonaux contre du matériel provenant de végétaux
C12N 15/63 - Introduction de matériel génétique étranger utilisant des vecteursVecteurs Utilisation d'hôtes pour ceux-ciRégulation de l'expression
C12P 21/02 - Préparation de peptides ou de protéines comportant une séquence connue de plusieurs amino-acides, p. ex. glutathion
G01N 33/68 - Analyse chimique de matériau biologique, p. ex. de sang ou d'urineTest par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligandsTest immunologique faisant intervenir des protéines, peptides ou amino-acides
33.
CANCER THERAPY USING 3,5-DISUBSTITUTED BENZENE ALKYNYL COMPOUND AND IMMUNE CHECKPOINT INHIBITOR
The problem to be solved by the present invention is to provide a novel combination therapy exhibiting an excellent antitumor effect. The present invention provides an antitumor agent (that does not contain pemblolizumab as an active ingredient) that contains, as an active ingredient, futibatinib or a salt thereof that is administered to a cancer patient in combination with an immune checkpoint inhibitor (excluding CD155/TIGIT pathway antagonist) and at least one or more other antitumor agents.
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
A61K 31/337 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à quatre chaînons, p. ex. taxol
A61K 31/357 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant plusieurs atomes d'oxygène dans le même cycle, p. ex. éthers en couronne, guanadrel
A61K 31/4745 - QuinoléinesIsoquinoléines condensées en ortho ou en péri avec des systèmes hétérocycliques condensées avec des systèmes cycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. phénanthrolines
A61K 31/475 - QuinoléinesIsoquinoléines ayant un cycle indole, p. ex. yohimbine, réserpine, strychnine, vinblastine
A61K 31/506 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime non condensées et contenant d'autres hétérocycles
A61K 31/513 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime ayant des groupes oxo liés directement à l'hétérocycle, p. ex. cytosine
A61K 31/7048 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'oxygène comme hétéro-atome d'un cycle, p. ex. leucoglucosane, hespéridine, érythromycine, nystatine
A61K 31/7068 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p. ex. cytidine, acide cytidylique
A61K 31/7072 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p. ex. cytidine, acide cytidylique ayant deux groupes oxo liés directement au cycle pyrimidine, p. ex. uridine, acide uridylique, thymidine, zidovudine
A61K 31/7076 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées contenant des purines, p. ex. adénosine, acide adénylique
A61K 39/395 - AnticorpsImmunoglobulinesImmunsérum, p. ex. sérum antilymphocitaire
The present invention addresses the problem of providing a novel combination therapy having an excellent antitumor effect. The present invention provides an antitumor agent that is administered to a cancer patient in combination with an immune checkpoint inhibitor (other than CD155/TIGIT pathway antagonist) and at least one other antitumor agent and that contains futibatinib or a salt thereof as an active ingredient (but does not contain pembrolizumab as an active ingredient).
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
A61K 31/337 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à quatre chaînons, p. ex. taxol
A61K 31/357 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant plusieurs atomes d'oxygène dans le même cycle, p. ex. éthers en couronne, guanadrel
A61K 31/4745 - QuinoléinesIsoquinoléines condensées en ortho ou en péri avec des systèmes hétérocycliques condensées avec des systèmes cycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. phénanthrolines
A61K 31/475 - QuinoléinesIsoquinoléines ayant un cycle indole, p. ex. yohimbine, réserpine, strychnine, vinblastine
A61K 31/506 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime non condensées et contenant d'autres hétérocycles
A61K 31/513 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime ayant des groupes oxo liés directement à l'hétérocycle, p. ex. cytosine
A61K 31/7048 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'oxygène comme hétéro-atome d'un cycle, p. ex. leucoglucosane, hespéridine, érythromycine, nystatine
A61K 31/7068 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p. ex. cytidine, acide cytidylique
A61K 31/7072 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p. ex. cytidine, acide cytidylique ayant deux groupes oxo liés directement au cycle pyrimidine, p. ex. uridine, acide uridylique, thymidine, zidovudine
A61K 31/7076 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées contenant des purines, p. ex. adénosine, acide adénylique
A61K 39/395 - AnticorpsImmunoglobulinesImmunsérum, p. ex. sérum antilymphocitaire
The present invention attempts to solve the problem of providing a novel combination therapy that exhibits an excellent antitumor effect. The present invention provides an antitumor agent (the antitumor agent does not contain pembrolizumab as an active ingredient) containing, as an active ingredient, futibatinib or a salt thereof that is administered to a cancer patient in combination with an immune checkpoint inhibitor (excluding CD155/TIGIT pathway antagonists) and at least one other antitumor agent.
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
A61K 31/337 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à quatre chaînons, p. ex. taxol
A61K 31/357 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant plusieurs atomes d'oxygène dans le même cycle, p. ex. éthers en couronne, guanadrel
A61K 31/475 - QuinoléinesIsoquinoléines ayant un cycle indole, p. ex. yohimbine, réserpine, strychnine, vinblastine
A61K 31/506 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime non condensées et contenant d'autres hétérocycles
A61K 31/513 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime ayant des groupes oxo liés directement à l'hétérocycle, p. ex. cytosine
A61K 31/4745 - QuinoléinesIsoquinoléines condensées en ortho ou en péri avec des systèmes hétérocycliques condensées avec des systèmes cycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. phénanthrolines
A61K 31/7048 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'oxygène comme hétéro-atome d'un cycle, p. ex. leucoglucosane, hespéridine, érythromycine, nystatine
A61K 31/7068 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p. ex. cytidine, acide cytidylique
A61K 31/7072 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p. ex. cytidine, acide cytidylique ayant deux groupes oxo liés directement au cycle pyrimidine, p. ex. uridine, acide uridylique, thymidine, zidovudine
A61K 31/7076 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées contenant des purines, p. ex. adénosine, acide adénylique
A61K 39/395 - AnticorpsImmunoglobulinesImmunsérum, p. ex. sérum antilymphocitaire
Provided is a novel method for treating castration resistant prostate cancer (CRPC), particularly CRPC that has acquired resistance to antiandrogen agents. This antitumor agent is characterized by the co-administration of an antiandrogen agent and 3-ethyl-4-{4-[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl}benzamide or a salt thereof.
A61K 31/437 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec un azote comme seul hétéro-atome d'un cycle condensés en ortho ou en péri avec des systèmes hétérocycliques le système hétérocyclique contenant un cycle à cinq chaînons ayant l'azote comme hétéro-atome du cycle, p. ex. indolizine, bêta-carboline
A61K 31/568 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrèneLeurs dérivés, p. ex. stéroïdes non substitués en position 17 bêta par un atome de carbone, p. ex. œstrane, œstradiol substitués en positions 10 et 13 par une chaîne ayant au moins un atome de carbone, p. ex. androstane, testostérone
A61K 31/4155 - 1,2-Diazoles non condensés et contenant d'autres hétérocycles
A61K 31/4439 - Pyridines non condenséesLeurs dérivés hydrogénés contenant d'autres systèmes hétérocycliques contenant un cycle à cinq chaînons avec l'azote comme hétéro-atome du cycle, p. ex. oméprazole
A61K 45/00 - Préparations médicinales contenant des ingrédients actifs non prévus dans les groupes
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; immunomodulators and immunosuppressive agents being pharmaceutical preparations for the treatment of immune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines being anti-emetic preparations; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; immunomodulators and immunosuppressive agents being pharmaceutical preparations for the treatment of immune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines being anti-emetic preparations; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; immunomodulators and immunosuppressive agents being pharmaceutical preparations for the treatment of immune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines being anti-emetic preparations; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; immunomodulators and immunosuppressive agents being pharmaceutical preparations for the treatment of immune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines being anti-emetic preparations; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; immunomodulators and immunosuppressive agents being pharmaceutical preparations for the treatment of immune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines being anti-emetic preparations; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; immunomodulators and immunosuppressive agents being pharmaceutical preparations for the treatment of immune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines being anti-emetic preparations; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; immunomodulators and immunosuppressive agents being pharmaceutical preparations for the treatment of immune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines being anti-emetic preparations; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of immune diseases and disorders; immunomodulators; immunosuppressive agents; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of immune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of immune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of immune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology.
48.
PROCESS FOR PREPARING A BENZOATE SALT OF A 1-(3-AMINOPYRROLIDINE-1-CARBONYL)-3,4-DIPHENYLBENZENE COMPOUND
A process for preparation of benzoate salt of 4-[5-[(3S)-3-aminopyrrolidine-1-carbonyl]-2-[2-fluoro-4-(2-hydroxy-2-methyl-propyl)phenyl]phenyl]-2-fluoro-benzonitrile, designated herein as Compound (A), and methods of using Compound (A) are provided. (I)
A process for preparation of benzoate salt of 4-[5-[(3S)-3-aminopyrrolidine-1-carbonyl]-2-[2-fluoro-4-(2-hydroxy-2-methyl-propyl)phenyl]phenyl]-2-fluoro-benzonitrile, designated herein as Compound (A), and methods of using Compound (A) are provided. (I)
A61K 31/40 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil
A61K 31/4025 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil non condensés et contenant d'autres hétérocycles, p. ex. cromakalim
C07C 67/52 - SéparationPurificationStabilisationEmploi d'additifs par modification de l'état physique, p. ex. par cristallisation
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of immune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology..
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Anti-cancer preparations; pharmaceutical preparations for the treatment of tumor; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of immune disorders; pharmaceutical preparations for the treatment of hematological disorders.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Anti-cancer preparations; pharmaceutical preparations for the treatment of tumor; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of immune disorders; pharmaceutical preparations for the treatment of hematological disorders
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Anti-cancer preparations; pharmaceutical preparations for the treatment of tumor; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of immune disorders; pharmaceutical preparations for the treatment of hematological disorders
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Anti-cancer preparations; pharmaceutical preparations for the treatment of tumor; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of immune disorders; pharmaceutical preparations for the treatment of hematological disorders.
54.
TREATMENT METHODS FOR SUBJECTS WITH NON-SMALL CELL LUNG CANCER HAVING AN ABERRATION IN EGFR
A method of treating a subject with a cancer having at least one aberration in EGFR, whereby the subject is administered (S)-N-(4-amino-6-methyl-5-(quinolin-3-yl)-8,9-dihydropyrimido[5,4-b]indolizin-8-yl)acrylamide (also known as zipalertinib and as TAS6417) or a pharmaceutically acceptable salt thereof, to a subject who has previously been treated with a molecularly targeted therapeutic. The molecularly targeted therapeutic may be an EGFR-targeting therapeutic other than Compound (1) or a non-EGFR-targeting therapeutic. The method may optionally involve administering to the subject an additional therapeutic agent.
A method of treating a subject with cancer having a dysregulated MAPK and/or PI3K pathway, whereby the subject is administered an effective amount of 4-(4-(3-((2-(tert-butylamino)ethyl)amino)-6-(5-(trifluoromethyl)-1,3,4-oxadiazol-2-yl)pyridin-2-yl)piperidin-1-yl)-5,5-dimethyl-5H-pyrolo[2,3-d]pyrimidin-6(7H)-one or a pharmaceutically acceptable salt thereof.
The present invention addresses the problem of providing a crystal of a compound having EGFR inhibition ability or a salt thereof, said crystal being excellent in the characteristic of stability (heat, purity) and/or low hygroscopicity. One aspect of the present invention provides a crystal form of (S)-N-(4-amino-6-methyl-5-(quinolin-3-yl)-8,9-dihydropyrimido[5,4-b]indolizin-8-yl)acrylamide that has a peak at a prescribed angle as the diffraction angle (2θ±0.2°) in a powder X-ray diffraction spectrum.
In one embodiment, the present invention provides an antibody specifically binding to human GH or an antigen-binding fragment thereof. In one embodiment, the present invention relates to an antibody specifically binding to human GH or an antigen-binding fragment thereof, comprising a heavy chain variable region (VH) and a light chain variable region (VL), wherein the VH comprises an amino acid sequence set forth in SEQ ID NO: 5 as a VH complementarity-determining region (CDR) 1 (VHCDR1), an amino acid sequence set forth in SEQ ID NO: 6 as a VHCDR2, and an amino acid sequence set forth in SEQ ID NO: 7 as a VHCDR3, and the VL comprises an amino acid sequence set forth in SEQ ID NO: 8 as a VL complementarity-determining region (CDR) 1 (VLCDR1), an amino acid sequence set forth in SEQ ID NO: 9 as a VLCDR2, and an amino acid sequence set forth in SEQ ID NO: 10 as a VLCDR3.
The purpose of the present invention is to provide a pharmaceutical composition containing naproxen or a salt thereof and acetaminophen or a salt thereof and having excellent storage stability. For this purpose, provided is a composition in which at least one selected from the group consisting of a specific basic compound and glycine or a salt thereof is used.
A61K 31/192 - Acides carboxyliques, p. ex. acide valproïque ayant des groupes aromatiques, p. ex. sulindac, acides 2-aryl-propioniques, acide éthacrynique
A61K 31/167 - Amides, p. ex. acides hydroxamiques ayant des cycles aromatiques, p. ex. colchicine, aténolol, progabide ayant l'atome d'azote d'un groupe carboxamide lié directement au cycle aromatique, p. ex. lidocaïne, paracétamol
A61K 47/18 - AminesAmidesUréesComposés d’ammonium quaternaireAcides aminésOligopeptides ayant jusqu’à cinq acides aminés
A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; chemical reagents for medical purposes in the field of oncology
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for use in dermatology, treating wounds, treating diabetes, skincare, treating cold symptoms, and treating athlete's foot; Pharmaceutical preparations in the nature of preparations for the treatment of wounds, for the purposes of being applied to plasters for medical purposes; Pharmaceutical preparations in the nature of analgesics, medicated eye wash, febrifuges, hemorrhoid preparations, and digestives for pharmaceutical purposes; medicinal drinks; tonics in the nature of medicines for the improvement of poor appetite, gastroenteric weakness, poor blood circulation, chills, fatigue, weak constitution and weakness following disease; vitamin preparations; nutritional preparations for medical use in the nature of nutritional supplements; nutritional additives for medical purposes; nutritional food supplements for medical purposes in the nature of natural food extracts derived from fish, meat and vegetables; food supplements for medical purposes for humans; dental materials in the nature of medicated toothpastes; bracelets for medical purposes; oiled paper for medical purposes; sanitary masks; pharmaceutical wafer in the nature of drug delivery agents in the form of edible wafers for wrapping powdered pharmaceuticals; gauze for dressings; capsules sold empty for pharmaceutical purposes; capsules for medicines for the treatment of cardiovascular disorders; eye patches for medical purposes; ear bandages; incontinence diapers; semen for artificial insemination; menstruation bandages; menstruation tampons; sanitary napkins; menstruation pads; sanitary pads; sanitary panties; sanitary knickers; menstruation knickers; absorbent cotton for medical purposes; absorbent wadding for medical purposes; lacteal flour for babies; milk sugar for medical purposes being lactose; fly catching paper; adhesive plaster for medical purposes; court plaster; sticking plasters for medical use; bandages for dressings; collodion for pharmaceutical purposes; mothproofing paper; breast-nursing pads; dietetic foods adapted for medical purposes; dietetic beverages adapted for medical purposes
61.
SMALL MOLECULE INHIBITORS OF KRAS MUTATED PROTEINS
Compounds of Formula (I) or their pharmaceutically acceptable salts can inhibit the G12C, G12D and/or G12V mutants of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
A61K 31/541 - Thiazines non condensées contenant d'autres hétérocycles
A61K 31/551 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à sept chaînons, p. ex. azélastine, pentylènetétrazole ayant deux atomes d'azote comme hétéro-atomes d'un cycle, p. ex. clozapine, dilazèpe
A61K 31/553 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à sept chaînons, p. ex. azélastine, pentylènetétrazole ayant au moins un azote et au moins un oxygène comme hétéro-atomes d'un cycle, p. ex. loxapine, staurosporine
A61K 31/554 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à sept chaînons, p. ex. azélastine, pentylènetétrazole ayant au moins un azote et au moins un soufre comme hétéro-atomes d'un cycle, p. ex. clothiapine, diltiazem
C07D 519/00 - Composés hétérocycliques contenant plusieurs systèmes de plusieurs hétérocycles déterminants condensés entre eux ou condensés avec un système carbocyclique commun non prévus dans les groupes ou
62.
PROPHYLACTIC DRUG/THERAPEUTIC DRUG FOR PROGRESSIVE SUPRANUCLEAR PALSY
Provided is a novel prophylactic drug and/or a novel therapeutic drug useful for progressive supranuclear palsy (PSP), the prophylactic drug and/or the therapeutic drug containing, as an active ingredient, a growth arrest and DNA damage-inducible protein 34 (GADD34) inhibitor including guanabenz that is a compound represented by formula [I-1].
A61K 31/4706 - 4-Aminoquinoléines8-Aminoquinoléines, p. ex. chloroquine, primaquine
A61P 25/00 - Médicaments pour le traitement des troubles du système nerveux
A61P 25/14 - Médicaments pour le traitement des troubles du système nerveux pour traiter les mouvements anormaux, p. ex. chorée, dyskinésie
A61P 25/28 - Médicaments pour le traitement des troubles du système nerveux des troubles dégénératifs du système nerveux central, p. ex. agents nootropes, activateurs de la cognition, médicaments pour traiter la maladie d'Alzheimer ou d'autres formes de démence
Provided is an antibody-drug conjugate (ADC) that specifically binds to CD138 and exhibits an excellent antitumor effect. In the ADC, monomethyl auristatin E is bound via a linker to an anti-CD138 antibody having a specific amino acid sequence.
A61K 47/68 - Préparations médicinales caractérisées par les ingrédients non actifs utilisés, p. ex. les supports ou les additifs inertesAgents de ciblage ou de modification chimiquement liés à l’ingrédient actif l’ingrédient non actif étant chimiquement lié à l’ingrédient actif, p. ex. conjugués polymère-médicament l’ingrédient non actif étant un agent de modification l’agent de modification étant un anticorps, une immunoglobuline ou son fragment, p. ex. un fragment Fc
A61K 38/08 - Peptides ayant de 5 à 11 amino-acides
A61K 39/395 - AnticorpsImmunoglobulinesImmunsérum, p. ex. sérum antilymphocitaire
Provided are: an anti-tumor agent having a high anti-tumor effect and fewer side effects; and others. The present invention relates to: a combination preparation containing trifluridine and tipiracil hydrochloride at a molar ratio of 1:0.5; an anti-tumor agent containing a PD-1 pathway antagonist, which is used in such a manner that the anti-tumor agent is administered in combination with a VEGF pathway antagonist; and others.
A61K 31/7072 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p. ex. cytidine, acide cytidylique ayant deux groupes oxo liés directement au cycle pyrimidine, p. ex. uridine, acide uridylique, thymidine, zidovudine
A61P 43/00 - Médicaments pour des utilisations spécifiques, non prévus dans les groupes
C07D 403/06 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une chaîne carbonée ne contenant que des atomes de carbone aliphatiques
C07H 19/073 - Radicaux pyrimidine avec un désoxy-2 ribosyle comme radical saccharide
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
66.
TREATMENT METHODS FOR SUBJECTS WITH CANCER HAVING AN ABERRATION IN EGFR AND/OR HER2
A method of treating a subject with cancer having an aberration in EGFR and/or HER2, whereby the subject is administered 7-((3R,5S)-1-acryloyl-5-methylpyrrolidin-3-yl)-4-amino-6-(cyclopropylethynyl)-N—((R)-1-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carboxamide or a pharmaceutically acceptable salt thereof.
Forms of 4-[5-[(3S)-3-aminopyrrolidine-1-carbonyl]-2-[2-fluoro-4-(2-hydroxy-2-methyl-propyl)phenyl]phenyl]-2-fluoro-benzonitrile, designated herein as Compound I, were prepared and characterized in the solid state. Also provided are processes of manufacture and methods of using the forms of Compound I.
C07D 207/14 - Atomes d'azote ne faisant pas partie d'un radical nitro
A61K 31/40 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil
The present invention provides I form crystals of 4-piperidinyl 2,2-diphenyl-2-(propoxy-1,1,2,2,3,3,3-d7)acetate hydrochloride having at least one diffraction angle (2θ±0.2°) selected from group (a) below and at least one diffraction angle (2θ±0.2°) selected from group (b) below in a powder x-ray diffraction spectrum (CuKα). (a) 11.3°, 11.4°, and 17.2° (b) 12.7°, 15.9°, 16.1°, 20.5°, 20.7°, 23.1°, 23.2°, 25.9°, and 28.4°
The present invention provides a substituted polypeptide having the effect of inhibiting MMP2 and represented by formula [I′], or a pharmaceutically acceptable salt thereof.
The present invention provides a substituted polypeptide having the effect of inhibiting MMP2 and represented by formula [I′], or a pharmaceutically acceptable salt thereof.
A61K 38/08 - Peptides ayant de 5 à 11 amino-acides
C07K 5/02 - Peptides ayant jusqu'à quatre amino-acides dans une séquence entièrement déterminéeLeurs dérivés contenant au moins une liaison peptidique anormale
70.
TREATING CANCER IN PATIENT HAVING CO-OCCURRING GENETIC ALTERATION IN FGFR2 AND A CANCER DRIVER GENE
A method of treating a subject with cholangiocarcinoma having a co-occurring genetic alteration in FGFR2 and a cancer driver gene selected from TP53, BAP1, ARID1A, MLL2, PIK3C2B, IKBKE, MCL1, MDM4, and MYC, whereby the subject is administered (S)-1-[(3)-[4-amino-3-[(3,5-dimethoxyphenyl)ethynyl]-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-pyrrolidinyl]-2-propen-1-one or a pharmaceutically acceptable salt thereof.
C12Q 1/6886 - Produits d’acides nucléiques utilisés dans l’analyse d’acides nucléiques, p. ex. amorces ou sondes pour les maladies provoquées par des altérations du matériel génétique pour le cancer
71.
COMBINATION THERAPY USING AZABICYCLO COMPOUND FOR CANCER
Provided is a novel method for treating cancer using an HSP90 inhibitor which exhibits a markedly superior antitumor effect and has a reduced side effect.
Provided is a novel method for treating cancer using an HSP90 inhibitor which exhibits a markedly superior antitumor effect and has a reduced side effect.
An antitumor agent is characterized in that an azabicyclo compound of the following Formula (1) or a salt thereof is administered in combination with other antitumor agent(s).
Provided is a novel method for treating cancer using an HSP90 inhibitor which exhibits a markedly superior antitumor effect and has a reduced side effect.
An antitumor agent is characterized in that an azabicyclo compound of the following Formula (1) or a salt thereof is administered in combination with other antitumor agent(s).
A61K 31/437 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec un azote comme seul hétéro-atome d'un cycle condensés en ortho ou en péri avec des systèmes hétérocycliques le système hétérocyclique contenant un cycle à cinq chaînons ayant l'azote comme hétéro-atome du cycle, p. ex. indolizine, bêta-carboline
A61K 31/337 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à quatre chaînons, p. ex. taxol
A61K 31/454 - Pipéridines non condensées, p. ex. pipérocaïne contenant d'autres systèmes hétérocycliques contenant un cycle à cinq chaînons avec l'azote comme hétéro-atome du cycle, p. ex. pimozide, dompéridone
A61K 31/506 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime non condensées et contenant d'autres hétérocycles
A61K 31/517 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des systèmes carbocycliques, p. ex. quinazoline, périmidine
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
A61K 31/5377 - 1,4-Oxazines, p. ex. morpholine non condensées et contenant d'autres hétérocycles, p. ex. timolol
A61K 31/555 - Composés hétérocycliques contenant des métaux lourds, p. ex. hémine, hématine, mélarsoprol
A61K 31/704 - Composés ayant des radicaux saccharide liés à des composés non-saccharide par des liaisons glycosidiques liés à un composé carbocyclique, p. ex. phloridzine liés à un système carbocyclique condensé, p. ex. sennosides, thiocolchicosides, escine, daunorubicine, digitoxine
A61K 31/7048 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'oxygène comme hétéro-atome d'un cycle, p. ex. leucoglucosane, hespéridine, érythromycine, nystatine
A61K 31/7068 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p. ex. cytidine, acide cytidylique
An antitumor agent comprising a compound selected from the group consisting of Compounds A to D described in the specification, or a salt thereof, for treating a malignant tumor patient expressing EGFR having exon 20 insertion mutation.
A method for treating cancer in patients with creatinine clearance of 15 mL/min or more and less than 30 mL/min, including dividing a combination drug containing α,α,α-trifluorothymidine (FTD) and 5-chloro-6-[(2-iminopyrrolidine-1-yl)methyl]pyrimidine-2,4(1H,3H)-dione hydrochloride in a molar ratio of 1:0.5, in a dose of 30 to 40 mg/m2/day as FTD-equivalent, into two to four times a day, and orally administering it to the patient.
A61K 31/513 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime ayant des groupes oxo liés directement à l'hétérocycle, p. ex. cytosine
A61K 31/506 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime non condensées et contenant d'autres hétérocycles
A61K 31/7072 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p. ex. cytidine, acide cytidylique ayant deux groupes oxo liés directement au cycle pyrimidine, p. ex. uridine, acide uridylique, thymidine, zidovudine
A61P 13/12 - Médicaments pour le traitement des troubles du système urinaire des reins
A method of treating a subject with a cancerous tumor exhibiting an inactivating mutation in the PTEN gene including administering to the subject trans-3-amino-1-methyl-3-(4-(3-phenyl-5H-imidazo[1,2-c]pyrido[3,4-e][1,3]oxazin-2-yl)phenylcyclobutanol or a pharmaceutically acceptable salt thereof.
A61K 31/5365 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec au moins un azote et au moins un oxygène comme hétéro-atomes d'un cycle, p. ex. 1,2-oxazines condensées en ortho ou en péri avec des systèmes hétérocycliques
A61K 31/706 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle
A61K 31/5377 - 1,4-Oxazines, p. ex. morpholine non condensées et contenant d'autres hétérocycles, p. ex. timolol
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
84.
BRAIN-MIGRATING TUMOR THERAPEUTIC AGENT CONTAINING FUSED PYRIMIDINE COMPOUND AS ACTIVE INGREDIENT
An object to be solved of the present invention is to provide a brain-penetrable antitumor agent showing an excellent brain penetration property and RET inhibitory activity.
An object to be solved of the present invention is to provide a brain-penetrable antitumor agent showing an excellent brain penetration property and RET inhibitory activity.
The present invention provides brain-penetrable antitumor agent including a compound represented by Formula (I) below or a salt thereof as an active ingredient:
An object to be solved of the present invention is to provide a brain-penetrable antitumor agent showing an excellent brain penetration property and RET inhibitory activity.
The present invention provides brain-penetrable antitumor agent including a compound represented by Formula (I) below or a salt thereof as an active ingredient:
An object to be solved of the present invention is to provide a brain-penetrable antitumor agent showing an excellent brain penetration property and RET inhibitory activity.
The present invention provides brain-penetrable antitumor agent including a compound represented by Formula (I) below or a salt thereof as an active ingredient:
wherein R1, R2, and R3 are as described in Specification.
Crystalline Forms of 4-amino-N-[4-(methoxymethyl)phenyl]-7-(1-methylcyclopropyl)-6-(3-morpholinoprop-1-yn-1-yl)-7H-pyrrolo[2,3-d]pyrimidine-5-carboxamide
Provided herein are various crystalline forms of 4-amino-N-[4-(methoxymethyl)phenyl]-7-(1-methylcyclopropyl)-6-(3-morpholinoprop-1-yn-1-yl)-7H-pyrrolo[2,3-d]pyrimidine-5-carboxamide, methods of producing same, and methods of using same to for RET inhibition.
Provided is a type-I crystal of a free form of 4-(4-(3-((2-(tert-butylamino)ethyl)amino)-6-(5-(trifluoromethyl)-1,3,4-oxadiazol-2-yl)piperidin-2-yl)piperidin-1-yl)-5,5-dimethyl-5H-pyrrolo[2,3-d]pyrimidin-6(7H)-one that has, in a powder X-ray diffraction spectrum (CuKα), peaks at at least two diffraction angles (2θ±0.2°) selected from the following (a) and at least two diffraction angles (2θ±0.2°) selected from the following (b). (a) 6.2°, 9.3°, 9.7°, 11.1°, 15.4°, and 25.1° (b) 6.7°, 8.3°, 8.7°, 13.0°, 13.7°, 16.3°, 16.9°, 17.7°, 18.7°, 19.4°, 20.3°, 25.9°, and 26.5°
Methods of Using 4-Amino-N-[4-(Methoxymethyl)Phenyl]-7-(1-Methylcyclopropyl)-6-(3-Morpholinoprop-1-YN-1-YL)-7H-Pyrrolo[2,3-D]Pyrimidine-5-Carboxamide for the Treatment of Tumors
The present invention relates to compositions and methods for treating patients with cancer having a RET gene abnormality comprising administering HM06/TAS0953, for example patients with non-small cell lung cancer (NSCLC), and that may also have brain and/or leptomeningeal metastases, or another solid tumor; where the patient is administered an effective amount of HM06/TAS0953, where the HM06/TAS0953 can be formulated in a composition and administered orally in a single or multiple doses; and where the patients may have previously received and/or have developed resistance to another RET-selective or multi-kinase inhibitor.
Provided are novel compounds which are analogues to be removed from APIs and formulations. Also provided are standard products of analogues to be used in controlling the qualities of medicines. Analogue 1: 3-ethyl-4-\{4-[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-3,3'-di(propan-2-yl)-1'H-[1,4'-bipyrazolo[3,4-b]pyridin]-1'-yl\}benzamide. Analogue 2: 3-ethyl-4-fuluorobenzamide. Analogue 3: N-[1-(4-carbamoyl-2-ethylphenyl)-3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin-4-yl]-3-ethyl-4-\{4-[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl\}benzamide. Analogue 4: 3-ethyl-4-\{14-[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-13,23,33-tri(propan-2-yl)-31H-[11,24:21, 34-terpyrazolo[3,4-b]pyridin]-31-yl\}benzamide. Analogue 5: 4,4'-(1H,1'H-[4,4'-biimidazol]-1,1'-diylbis\{[3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin-4,1-diyl]\})bis(3-ethylbenzamide). Analogue 6: 4-\{4,6-bis[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin]-1-yl\}-3-ethylbenzonitrile. Analogue 7: 4-\{4,6-bis[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl\}-3-ethylbenzamide. Analogue 8: 4-[4-ethoxy-3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl]-3-ethylbenzamide. Analogue 9: 3-ethyl-4-[4-methoxy-3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl]benzamide.
C07C 233/65 - Amides d'acides carboxyliques ayant des atomes de carbone de groupes carboxamide liés à des atomes de carbone de cycles aromatiques à six chaînons ayant les atomes d'azote des groupes carboxamide liés à des atomes d'hydrogène ou à des atomes de carbone de radicaux hydrocarbonés non substitués
A61K 31/166 - Amides, p. ex. acides hydroxamiques ayant des cycles aromatiques, p. ex. colchicine, aténolol, progabide ayant l'atome de carbone d'un groupe carboxamide lié directement au cycle aromatique, p. ex. procaïnamide, procarbazine, métoclopramide, labétalol
A61K 31/437 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec un azote comme seul hétéro-atome d'un cycle condensés en ortho ou en péri avec des systèmes hétérocycliques le système hétérocyclique contenant un cycle à cinq chaînons ayant l'azote comme hétéro-atome du cycle, p. ex. indolizine, bêta-carboline
C07D 519/00 - Composés hétérocycliques contenant plusieurs systèmes de plusieurs hétérocycles déterminants condensés entre eux ou condensés avec un système carbocyclique commun non prévus dans les groupes ou
Provided is a pharmaceutical composition containing compound 1 and having excellent disintegrability and bioavailability. This pharmaceutical composition contains crystalline cellulose and a granulated substance containing 3-ethyl-4-{4-[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridine-1-yl}benzamide or a pharmaceutically acceptable salt thereof, and has a disintegration time of 360 seconds or less in a coated tablet state.
A61K 31/437 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec un azote comme seul hétéro-atome d'un cycle condensés en ortho ou en péri avec des systèmes hétérocycliques le système hétérocyclique contenant un cycle à cinq chaînons ayant l'azote comme hétéro-atome du cycle, p. ex. indolizine, bêta-carboline
A61K 9/36 - Revêtements organiques contenant des hydrates de carbone ou leurs dérivés
The present invention provides a pharmaceutical composition for preventing and/or treating an RNR-related disease in a patient in need thereof, wherein the pharmaceutical composition comprises 5-chloro-2-(N-((1S,2R)-2-(6-fluoro-2,3-dimetylphenyl)-1-(5-oxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)propyl)sulfamoyl)benzamide or a salt thereof, and is administered to the patient on an intermittent administration schedule for two weeks comprising dosing 1 to 5 days per week. The present invention also provides a method of treating an RNR-related diseases in a patient in need thereof, the method comprising administering an effective amount of 5-chloro-2-(N-((1S,2R)-2-(6-fluoro-2,3-dimetylphenyl)-1-(5-oxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)propyl)sulfamoyl)benzamide or a salt thereof to the patient on an intermittent administration schedule for two weeks comprising dosing 1 to 5 days per week.
The present invention relates to a compound having inhibitory activity against KRAS G12D mutation or a salt thereof, and relates to a pharmaceutical composition comprising the compound as an active ingredient.
C07D 519/00 - Composés hétérocycliques contenant plusieurs systèmes de plusieurs hétérocycles déterminants condensés entre eux ou condensés avec un système carbocyclique commun non prévus dans les groupes ou
A method of synthesizing anhydrous lactic acid is provided by reacting a compound of formula (Ia): with an acid compound of formula HnX in a first solvent to produce a reaction mixture comprising a compound of formula (Ib) and a lactic acid compound of formula (I) in solution with the first solvent and/or water. n is an integer other than 0, x is 0, or an integer other than 0, M is an alkali metal or alkaline earth metal and X is the conjugate base of the acid compound of formula HnX. The resulting reaction mixture is filtered to produce a filtrate containing lactic acid in solution. The filtrate is crystalized from a second solvent to produce anhydrous lactic acid.
A method of synthesizing anhydrous lactic acid is provided by reacting a compound of formula (Ia): with an acid compound of formula HnX in a first solvent to produce a reaction mixture comprising a compound of formula (Ib) and a lactic acid compound of formula (I) in solution with the first solvent and/or water. n is an integer other than 0, x is 0, or an integer other than 0, M is an alkali metal or alkaline earth metal and X is the conjugate base of the acid compound of formula HnX. The resulting reaction mixture is filtered to produce a filtrate containing lactic acid in solution. The filtrate is crystalized from a second solvent to produce anhydrous lactic acid.
C07C 51/46 - SéparationPurificationStabilisationEmploi d'additifs par changement de l'état physique, p. ex. par cristallisation par distillation azéotropique
The present invention provides a pharmaceutical composition for preventing and/or treating an RNR-related disease in a patient in need thereof, wherein the pharmaceutical composition comprises 5-chloro-2-(N-((1S,2R)-2-(6-fluoro-2,3-dimetylphenyl)-1-(5-oxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)propyl)sulfamoyl)benzamide or a salt thereof, and is administered to the patient on an administration schedule comprising continuous, daily dosing for one week, followed by a resting period of one week. The present invention also provides a method of treating an RNR-related diseases in a patient in need thereof, the method comprising administering an effective amount of 5-chloro-2-(N-((1S,2R)-2-(6-fluoro-2,3-dimetylphenyl)-1-(5-oxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)pr opyl)sulfamoyl)benzamide or a salt thereof to the patient on an administration schedule comprising daily dosing for one week, followed by a resting period of one week.
Provided is a novel therapeutic agent useful for the prevention or treatment of lung inflammation and fibrosis, the agent containing, as an active ingredient, a compound which has an MMP2 inhibitory activity and is represented by formula [IX], or a pharmaceutically acceptable salt thereof.
Provided is a crystal of a compound having EGFR inhibition ability or a salt thereof, said crystal being excellent in one or more characteristics of stability, hygroscopicity and oral absorbability. One aspect of the present invention provides a crystal form of N-(4-(4-amino-6-ethynyl-5-(quinolin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)bicyclo[2.2.1]heptan-1-yl)-5-methylpyrazine-2-carboxamide the diffraction angle (2θ±0.2°) of which has a peak at a preset angle in the X-ray powder diffraction spectrum.
A crystal of 7-((3R,5S)-1-acryloyl-5-methylpyrrolidin-3-yl)-4-amino-6-(cyclopropylethynyl)-N-((R)-1-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carboxamide (compound (I)), and a crystal thereof with an acid (salt crystal or co-crystal) are provided.
A crystal of 7-((3R,5S)-1-acryloyl-5-methylpyrrolidin-3-yl)-4-amino-6-(cyclopropylethynyl)-N-((R)-1-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carboxamide (compound (I)), and a crystal thereof with an acid (salt crystal or co-crystal) are provided.
There are provided: a type II crystal of compound (I) with fumaric acid, having characteristic peaks at three or more diffraction angles (2θ ± 0.2 °) selected from 5.5°, 6.8°, 9.3°, 13.4°, 15.3°, 16.3°, 18.5°, 19.8°, 22.0°, and 24.5° in a powder X-ray diffraction spectrum;
a (free-form) type II crystal of compound (I) having characteristic peaks at three or more diffraction angles selected from 8.3°, 14.8°, 17.3°, 18.0°, 19.1°, 20.3°, 21.0°, 22.5°, 23.0°, and 26.2° in a powder X-ray diffraction spectrum;
a (free-form) type I crystal of compound (I) having characteristic peaks at three or more diffraction angles selected from 9.9°, 11.7°, 13.2°, 17.7°, 18.1°, 18.8°, and 20.8° in a powder X-ray diffraction spectrum;
a type V crystal of compound (I) with fumaric acid, having characteristic peaks at four or more diffraction angles selected from 6.9°, 9.4°, 10.2°, 13.7°, 21.1°, 23.6°, and 26.5° in a powder X-ray diffraction spectrum; and
a type I crystal of compound (I) with fumaric acid, having characteristic peaks at four or more diffraction angles selected from 6.4°, 10.3°, 12.8°, 15.0°, 20.7°, 23.4°, and 26.6° in a powder X-ray diffraction spectrum.
Provided is an antibody that exhibits pH dependence and specifically binds to a sulfated glycosaminoglycan (sGAG). An antibody specifically binding to a sulfated glycosaminoglycan that is at least one selected from the group consisting of the following (1) to (3): (1) an antibody that contains a heavy chain having CDR1 comprising an amino acid sequence represented by SEQ ID NO: 1, CDR2 comprising an amino acid sequence represented by SEQ ID NO: 2 and CDR3 comprising an amino acid sequence represented by SEQ ID NO: 3, and a light chain having CDR1 comprising an amino acid sequence represented by SEQ ID NO: 4, CDR2 comprising an amino acid sequence represented by LGS and CDR3 comprising an amino acid sequence represented by SEQ ID NO: 6; (2) an antibody that contains a heavy chain having CDR1 comprising an amino acid sequence represented by SEQ ID NO: 7, CDR2 comprising an amino acid sequence represented by SEQ ID NO: 8 and CDR3 comprising an amino acid sequence represented by SEQ ID NO: 9, and a light chain having CDR1 comprising an amino acid sequence represented by SEQ ID NO: 10, CDR2 comprising an amino acid sequence represented by AAS and CDR3 comprising an amino acid sequence represented by SEQ ID NO: 12; and (3) an antibody that contains a heavy chain having CDR1 comprising an amino acid sequence represented by SEQ ID NO: 13, CDR2 comprising an amino acid sequence represented by SEQ ID NO: 14 and CDR3 comprising an amino acid sequence represented by SEQ ID NO: 15, and a light chain having CDR1 comprising an amino acid sequence represented by SEQ ID NO: 16, CDR2 comprising an amino acid sequence represented by WAS and CDR3 comprising an amino acid sequence represented by SEQ ID NO: 18.
C07K 16/30 - Immunoglobulines, p. ex. anticorps monoclonaux ou polyclonaux contre du matériel provenant d'animaux ou d'humains contre des récepteurs, des antigènes de surface cellulaire ou des déterminants de surface cellulaire provenant de cellules de tumeurs
A61K 39/395 - AnticorpsImmunoglobulinesImmunsérum, p. ex. sérum antilymphocitaire
A61K 47/68 - Préparations médicinales caractérisées par les ingrédients non actifs utilisés, p. ex. les supports ou les additifs inertesAgents de ciblage ou de modification chimiquement liés à l’ingrédient actif l’ingrédient non actif étant chimiquement lié à l’ingrédient actif, p. ex. conjugués polymère-médicament l’ingrédient non actif étant un agent de modification l’agent de modification étant un anticorps, une immunoglobuline ou son fragment, p. ex. un fragment Fc
The invention relates to methods of synthesizing 2′-deoxy-2′,2′-difluorotetrahydrouridine with increased purity and uniform particle size distribution. In particular, methods of the invention include crystallization and isolation procedures rendering synthetic reaction intermediates. The invention further includes compositions comprising the final compound in highly pure form, including lower number of impurities and lower levels of individual and total impurities.
