The present disclosure relates to novel salts, particularly crystalline salts of 2-(5-methoxyisochroman-1-yl)-4,5-dihydro-1H-imidazole (I) which are suitable for use in the manufacture of pharmaceutical compositions. Compound (I) is selective alpha2A adrenoceptor agonist and is useful in the treatment of anxiety, and for use as a sedative or analgesic agent, and other diseases were alpha2A agonism is desired.
C07D 405/04 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
The present invention relates to a pharmaceutical composition for oral administration, particularly in the form of a tablet or a powder suitable to be filled into a capsule shell, comprising 2-(isoindolin-2-ylmethyl)-5-((1-(methylsulfonyl)-piperidin-4-yl)methoxy)-4H-pyran-4-one (I) or a pharmaceutically acceptable salt thereof as an active ingredient. Compound (I) or a pharmaceutically acceptable salt thereof is a selective inhibitor of CYP11A1 enzyme and is useful in the treatment of hormonally regulated diseases such as cancer including prostate cancer and breast cancer.
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
03 - Cosmetics and toiletries; cleaning, bleaching, polishing and abrasive preparations
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Shampoos and hair lotions for the treatment and prevention of head lice.. Anti-lice preparations; medicated shampoos for treatment and prevention of head lice..
03 - Cosmetics and toiletries; cleaning, bleaching, polishing and abrasive preparations
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Dermatological creams [non-medicated] for skin or mucous
membrane irritation, abrasions, cracks or wounds. Medicated creams for the treatment of skin or mucous
membrane irritation, abrasions, cracks or wounds.
The present invention relates to an improved process for the preparation of carboxamide structured androgen receptor (AR) antagonists such as N-((S)-1-(3-(3- chloro-4-cyanophenyl)-1H-pyrazol-1-yl)-propan-2-yl)-5-(1-hydroxyethyl)-1H- pyrazole-3-carboxamide (1A) and key intermediates thereof such as (S)-4-(1-(2- aminopropyl)-1H-pyrazol-3-yl)-2-chlorobenzonitrile (VII). AR antagonists are useful in the treatment of cancer, particularly prostate cancer and other diseases where AR antagonism is desired.
C07D 231/12 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
The present invention relates to a pharmaceutical composition for oral administration, for example in the form of a tablet or a powder suitable to be filled into a capsule shell, comprising 2-(isoindolin-2-ylmethyl)-5-((1-(methylsulfonyl)- piperidin-4-yl)methoxy)-4H-pyran-4-one (I) or a pharmaceutically acceptable salt thereof as an active ingredient. Compound (I) or a pharmaceutically acceptable salt thereof is a selective inhibitor of CYP11A1 enzyme and is useful in the treatment of hormonally regulated diseases such as cancer including prostate cancer and breast cancer.
03 - Cosmetics and toiletries; cleaning, bleaching, polishing and abrasive preparations
05 - Pharmaceutical, veterinary and sanitary products
31 - Agricultural products; live animals
Goods & Services
Dental care preparations for animals; non-medicated hair
shampoos; shampoos for pets [non-medicated grooming
preparations]; non-medicated cosmetics; non-medicated oils;
non-medicated toiletries; non-medicated toilet soaps. Medicated shampoos for pets; sanitary preparations for
veterinary use; probiotic bacterial formulations for
veterinary use; diagnostic preparations for medical or
veterinary purposes; reagent paper for medical or veterinary
purposes; veterinary preparations and substances;
anti-infective products for veterinary use; dietary
supplements for pets; vitamins for animals; vitamins and
vitamin preparations; mineral nutritional supplements;
disinfectants for veterinary use; lotions for veterinary
purposes; diagnostic preparations for veterinary purposes;
bacterial preparations for veterinary purposes; food
supplements for veterinary use; feed supplements for
veterinary use; nutritional supplements for veterinary use;
antiparasitic preparations for pets; antiparasitic collars
for animals; pharmaceutical preparations for animal
skincare. Fodder; beverages for pets.
The present invention relates to a compound of formula (I) wherein A, B, R1, R2, R3, R4 and R5 are as defined in claim 1, or pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as cytochrome P450 monooxygenase 11A1 (CYP11A1) inhibitors. The compounds are useful as medicaments in the treatment of steroid receptor, for example androgen receptor or estrogen receptor, dependent diseases and conditions, such as cancer including prostate cancer and breast cancer.
The present invention relates to a compound of formula (I) wherein A, B, R1, R2, R3, R4 and R5 are as defined in claim 1, or pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as cytochrome P450 monooxygenase 11A1 (CYP11A1) inhibitors. The compounds are useful as medicaments in the treatment of steroid receptor, for example androgen receptor or estrogen receptor, dependent diseases and conditions, such as cancer including prostate cancer and breast cancer.
A61K 31/423 - Oxazoles condensed with carbocyclic rings
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C07D 209/46 - Iso-indolesHydrogenated iso-indoles with an oxygen atom in position 1
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
25.
2-PHENOXY-1-(4-(ALKYLSULFONYL)PIPERIDIN-1-YL)ETHAN-1-ONE AND 3-PHENYL-1-(4-(ALKYLSULFONYL)PIPERIDIN-1-YL)PROP-2-EN-1-ONE DERIVATIVES AS GPR183 ANTAGONISTS FOR THE TREATMENT OF CHRONIC PAIN
144, n, and m have the meaning given in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula I exhibit GPR 183 antagonistic activity and are thus useful in the treatment or prevention of disorder, condition, or disease where GRP183 antagonist is indicated to be useful, such as e.g. chronic pain e.g osteoarthritis, chronic low back pain, neuropathic pain and immune system diseases e.g inflammatory bowel diseases e.g. Colitis and Chron's diseases, multiple sclerosis, rheumatoid arthritis, inflammatory pulmonary diseases e.g. asthma and psoriasis.
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
A61K 31/453 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61P 25/04 - Centrally acting analgesics, e.g. opioids
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment of parkinson's
disease and syndrome; transdermal patches for use in the
treatment of parkinson's disease and syndrome.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment of Parkinson's
disease and syndrome; transdermal patches for use in the
treatment of Parkinson's disease and syndrome.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment of Parkinson's
disease and syndrome; transdermal patches for use in the
treatment of Parkinson's disease and syndrome.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations for the treatment of parkinson's disease and syndrome; transdermal patches for use in the treatment of parkinson's disease and syndrome.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations for the treatment of Parkinson's disease and syndrome; transdermal patches for use in the treatment of Parkinson's disease and syndrome.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations for the treatment of Parkinson's disease and syndrome; transdermal patches for use in the treatment of Parkinson's disease and syndrome.
35.
PROCESS FOR THE PREPARATION OF A CYP11A1 INHIBITOR AND INTERMEDIATES THEREOF
The present invention relates to an improved process for the preparation of 4H-pyranone structured CYP11A1 inhibitors such as 5-((1-(methylsulfonyl)-piperidin-4-yl)methoxy)-2-((5-(trifluoromethyl)isoindolin-2-yl)methyl)-4H-pyran-4-one (1A) and key intermediates thereof including 5-(trifluoromethyl)isoindoline (V) and 5-hydroxy-2-((5-(trifluoromethyl)isoindolin-2-yl)methyl)-4H-pyran-4-one (III). CYP11A1 inhibitors are useful in the treatment of hormonally regulated cancers, such as prostate cancer and breast cancer.
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
36.
ANDROGEN RECEPTOR ANTAGONISTS FOR THE TREATMENT OF PATIENTS WITH BIOCHEMICAL RECURRENCE OF HORMONE SENSITIVE PROSTATE CANCER
Described herein are methods of treating patients with biochemical recurrence of hormone-sensitive prostate cancer using a drug product comprising an androgen receptor inhibitor, such as darolutamide.
A61K 31/4155 - 1,2-Diazoles not condensed and containing further heterocyclic rings
A61K 31/4166 - 1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
Compounds of formula (I) wherein R1, R2,R3,R4,R5,R23,R24,L, A and B are as defined in claim 1, or pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as cytochrome P450 monooxygenase 11A1(CYP11A1) inhibitors. The compounds are useful as medicaments in the treatment of steroid receptor, particularly androgen receptor, dependent diseases and conditions, such as—prostate cancer.
Compounds of formula (I) wherein R1, R2,R3,R4,R5,R23,R24,L, A and B are as defined in claim 1, or pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as cytochrome P450 monooxygenase 11A1(CYP11A1) inhibitors. The compounds are useful as medicaments in the treatment of steroid receptor, particularly androgen receptor, dependent diseases and conditions, such as—prostate cancer.
C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 451/02 - Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamineCyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring systems, e.g. tropaneCyclic acetals thereof
C07D 491/056 - Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
03 - Cosmetics and toiletries; cleaning, bleaching, polishing and abrasive preparations
05 - Pharmaceutical, veterinary and sanitary products
31 - Agricultural products; live animals
Goods & Services
Dental care preparations for animals; Non-medicated hair shampoos; Shampoos for pets [non-medicated grooming preparations]; Non-medicated cosmetics; Non-medicated oils; Non-medicated toiletries; Non-medicated toilet soaps. Medicated shampoos for pets; Sanitary preparations for veterinary use; Probiotic bacterial formulations for veterinary use; Diagnostic preparations for medical or veterinary purposes; Reagent paper for medical or veterinary purposes; Veterinary preparations and substances; Anti-infective products for veterinary use; Dietary supplements for pets; Vitamins for animals; Vitamins and vitamin preparations; Mineral nutritional supplements; Disinfectants for veterinary use; Lotions for veterinary purposes; Diagnostic preparations for veterinary purposes; Bacterial preparations for veterinary purposes; Food supplements for veterinary use; Feed supplements for veterinary use; Nutritional supplements for veterinary use; Antiparasitic preparations for pets; Antiparasitic collars for animals; Pharmaceutical preparations for animal skincare. Fodder; Beverages for pets.
123 3 are as defined in claim 1, or a pharmaceutically acceptable salt thereof. The compounds of formula (I) possess utility as inhibitors of Cbl-b. The compounds are useful as medicaments in the treatment of diseases or conditions wherein inhibition of CBl-b is desired, such as cancer.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
C07D 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/4995 - Pyrazines or piperazines forming part of bridged ring systems
A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
The present invention relates to a compound of formula (I)
The present invention relates to a compound of formula (I)
wherein A, Z, L, R1, R2, R3, R4, R5 and R33 are as defined in claim 1, or a pharmaceutically acceptable salt thereof. The compounds of formula (I) possess utility as inhibitors of TEAD. The compounds are useful as medicaments in the treatment of diseases or conditions wherein inhibition of TEAD is desired, such as cancer and chronic pain.
C07D 207/277 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
A61K 31/197 - Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
A61K 31/382 - Heterocyclic compounds having sulfur as a ring hetero atom having six-membered rings, e.g. thioxanthenes
A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
A61K 31/4015 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
A61K 31/4025 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
A61K 31/4155 - 1,2-Diazoles not condensed and containing further heterocyclic rings
A61K 31/4166 - 1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
A61K 31/421 - 1,3-Oxazoles, e.g. pemoline, trimethadione
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
A61K 31/429 - Thiazoles condensed with heterocyclic ring systems
A61K 31/4412 - Non-condensed pyridinesHydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/45 - Non-condensed piperidines, e.g. piperocaine having oxo groups directly attached to the heterocyclic ring, e.g. cycloheximide
A61K 31/4525 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
A61K 31/453 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
C07C 237/04 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
C07D 205/08 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams
C07D 207/16 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 207/263 - 2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms
C07D 211/78 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
C07D 263/24 - Oxygen atoms attached in position 2 with hydrocarbon radicals, substituted by oxygen atoms, attached to other ring carbon atoms
C07D 275/03 - Heterocyclic compounds containing 1, 2-thiazole or hydrogenated 1,2-thiazole rings not condensed with other rings with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
C07D 285/00 - Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups
C07D 333/48 - Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings substituted on the ring sulfur atom by oxygen atoms
C07D 335/02 - Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/04 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
The present disclosure relates to a process for the preparation of 3-(4,5-dichloro-2-(4- (trifluoromethoxy)phenoxy)benzamido)pyridine 1-oxide, to a compound which is 3-(4,5- dichloro-2-fluorobenzamido)pyridine 1-oxide and use thereof in the preparation of 3-(4,5- dichloro-2-(4-(trifluoromethoxy)phenoxy)benzamido)pyridine 1-oxide as well as to a compound which is 3-(5-chloro-2,4-bis(4-(trifluoromethoxy)phenoxy)benzamido)pyridine 1-oxide and use thereof as a reference substance in the control of impurities in the manufacture of 3-(4,5-dichloro-2-(4-(trifluoromethoxy)phenoxy)benzamido)pyridine 1- oxide. 3-(4,5-Dichloro-2-(4-(trifluoromethoxy)phenoxy)benzamido)pyridine 1-oxide is a NaV 1.8 blocker.
C07D 213/89 - Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to the ring nitrogen atom
A61K 31/4412 - Non-condensed pyridinesHydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
03 - Cosmetics and toiletries; cleaning, bleaching, polishing and abrasive preparations
05 - Pharmaceutical, veterinary and sanitary products
31 - Agricultural products; live animals
Goods & Services
Dental care preparations for animals; non-medicated hair
shampoos; shampoos for pets [non-medicated grooming
preparations]; non-medicated cosmetics; non-medicated oils;
non-medicated toiletries; non-medicated toilet soaps. Medicated shampoos for pets; sanitary preparations for
veterinary use; probiotic bacterial formulations for
veterinary use; diagnostic preparations for medical or
veterinary purposes; reagent paper for medical or veterinary
purposes; veterinary preparations and substances;
anti-infective products for veterinary use; dietary
supplements for pets; vitamins for animals; vitamins and
vitamin preparations; mineral nutritional supplements;
disinfectants for veterinary use; lotions for veterinary
purposes; diagnostic preparations for veterinary purposes;
bacterial preparations for veterinary purposes; food
supplements for veterinary use; feed supplements for
veterinary use; nutritional supplements for veterinary use;
antiparasitic preparations for pets; antiparasitic collars
for animals; pharmaceutical preparations for animal
skincare. Fodder; beverages for pets.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment of Parkinson's disease and syndrome; transdermal patches for use in the treatment of Parkinson's disease and syndrome..
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment of Parkinson's disease and syndrome; transdermal patches for use in the treatment of Parkinson's disease and syndrome..
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment of Parkinson's disease and syndrome; transdermal patches for use in the treatment of Parkinson's disease and syndrome..
The present invention relates to an improved process for the preparation of 4H-pyranone structured CYP11A1 inhibitors such as 2-(isoindolin-2-ylmethyl)-5-((1-(methylsulfonyl)piperidin-4-yl)methoxy)-4H-pyran-4-one (1A) and key intermediates thereof such as 2-(chloromethyl)-5-hydroxy-4H-pyran-4-one (II), 5-hydroxy-2-(isoindolin-2-ylmethyl)-4H-pyran-4-one (III), (1-(methylsulfonyppiperidin-4-yHmethyl methane sulfonate (V) and (1-(methyl-sulfonyppiperidin-4-yHmethyl 4-methylbenzene fonate (V″). CYP11A1 inhibitors are useful in the treatment of hormonally regulated cancers, such as prostate cancer and breast cancer.
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 309/32 - Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
The present disclosure relates to a pharmaceutical composition in the form of an orally deliverable liquid composition comprising tasipimidine, or a pharmaceutically acceptable salt thereof, as an active ingredient and to the use thereof in the treatment and prevention of a disorder, condition or disease where an alpha2A agonist is indicated to be useful, for example, for use as a sedative or analgesic agent, and for use in the treatment of anxiety or agitation. The composition is stable at the pH range from about 2.0 to about 5.0.
The present disclosure relates to a pharmaceutical composition in the form of an orally deliverable liquid composition comprising tasipimidine, or a pharmaceutically acceptable salt thereof, as an active ingredient and to the use thereof in the treatment and prevention of situational anxiety and fear in companion animals, such as dogs. The composition is stable at the pH range from about 2.0 to about 5.0 and it can be easily administered by the pet owners.
The present invention relates to novel salts, particularly crystalline salts, of 2-(isoindolin-2-ylmethyl)-5-((1-(methyl sulfonyl)piperidin-4-yl)methoxy)-4H-pyran-4-one (I) which are particularly suitable for use in the manufacture of pharmaceutical 5 compositions. Furthermore, the invention relates to pharmaceutical compositions comprising such novel salts. Compound (I) is a selective inhibitor of CYP11A1 enzyme and is useful in the treatment of hormonally regulated cancers, such as prostate cancer and breast cancer.
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
63.
SOLID FORMS OF A 4H-PYRAN-4-ONE STRUCTURED CYP11A1 INHIBITOR
The present invention relates to novel solid forms, particularly crystalline forms, of 2-(isoindolin-2-ylmethyl)-5-((1-(methylsulfonyl)piperidin-4-yl)methoxy)-4H-pyran-4-one (I). Compound (I) is a selective inhibitor of CYP11A1 enzyme and is useful in the treatment of hormonally regulated cancers, such as prostate cancer and breast cancer.
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations containing pregabalin; medical
and veterinary preparations containing pregabalin.
70.
2,3-DIHYDRO-4H-BENZO[B][1,4]OXAZIN-4-YL)(5-(PHENYL)-PYRIDIN-3-YL)METHANONE DERIVATIVES AND SIMILAR COMPOUNDS AS CYP11A1 INHIBITORS FOR THE TREATMENT OF PROSTATE CANCER
The present invention relates to compounds of formula (I),
The present invention relates to compounds of formula (I),
The present invention relates to compounds of formula (I),
wherein A is a 3-10 membered carbocyclyl or a 4-12 membered heterocyclyl containing 1-4 heteroatoms selected from O, N, or S; B is any of the following groups (1), (2), or (3); C is any of the following groups (1′), (2′), (3′), or (4′); G1 is CH2, NH, or O; G2 and G3 are, independently, CH or N; Z is —C(O)—, —SO2—, —C1-3 alkyl-, or —CH2—C(O)—; L is a bond, —C1-7 alkyl-, or —C1-7 alkenyl-. The compounds of formula (I) are cytochrome P450 monooxygenase 11A1 (CYP11A1) inhibitors. The compounds are useful as medicaments in the treatment of steroid receptor, for example, androgen receptor or estrogen receptor, dependent diseases and conditions, such as cancer including prostate cancer and estrogen cancer.
C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
05 - Pharmaceutical, veterinary and sanitary products
10 - Medical apparatus and instruments
Goods & Services
Pharmaceutical preparations; pharmaceutical preparations for the treatment and alleviation of asthma and other respiratory diseases or ailments. Medical apparatus and instruments; drug delivery devices and inhalers; inhalers filled with pharmaceutical preparations for the treatment and alleviation of respiratory disorders.
The present invention relates to chimeric antigen receptors (CAR) comprising an inert and modifiable spacer that evades the off-target binding by Fc receptor (FcR) expressing cells in CAR T cell therapy. The spacer is based on Ig-like C1 domain of signal-regulatory protein alpha.
C07K 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
A61K 39/00 - Medicinal preparations containing antigens or antibodies
The invention relates to co-administration a CYP2D6 inhibitor with tasipimidine, or a pharmaceutically acceptable salt thereof, in order to improve the pharmacokinetic profile of tasipimidine by decreasing its clearance and inter-individual variation. The invention also relates to a combination of tasipimidine, or a pharmaceutically acceptable salt thereof, and a CYP2D6 inhibitor, and the use of such a combination for the treatment of a disorder, condition or disease where an alpha2A agonist is indicated to be useful, for example, for use in the treatment of neuropsychiatric disorders.
A61K 31/137 - Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine
A61K 31/138 - Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
A61K 31/36 - Compounds containing methylenedioxyphenyl groups, e.g. sesamin
A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
A61K 31/4433 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
A61K 31/4525 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 25/00 - Drugs for disorders of the nervous system
A method to introduce a mutation to a variable domain of an antibody or its fragment by introducing at least one peptide linker to close proximity of the variable domain, wherein the peptide linker is encoded by a nucleic acid forming a G quadruplex (G4) structure and the G4 structure promotes activity of activation-induced cytidine deaminase (AID).
03 - Cosmetics and toiletries; cleaning, bleaching, polishing and abrasive preparations
05 - Pharmaceutical, veterinary and sanitary products
31 - Agricultural products; live animals
Goods & Services
Dental care preparations for animals; Non-medicated hair shampoos; Shampoos for pets [non-medicated grooming preparations]; Non-medicated cosmetics; Non-medicated oils; Non-medicated toiletries; Non-medicated toilet soaps. Medicated shampoos for pets; Sanitary preparations for veterinary use; Probiotic bacterial formulations for veterinary use; Diagnostic preparations for medical or veterinary purposes; Reagent paper for medical or veterinary purposes; Veterinary preparations and substances; Anti-infective products for veterinary use; Dietary supplements for pets; Vitamins for animals; Vitamins and vitamin preparations; Mineral nutritional supplements; Disinfectants for veterinary use; Lotions for veterinary purposes; Diagnostic preparations for veterinary purposes; Bacterial preparations for veterinary purposes; Food supplements for veterinary use; Feed supplements for veterinary use; Nutritional supplements for veterinary use; Antiparasitic preparations for pets; Antiparasitic collars for animals; Pharmaceutical preparations for animal skincare. Fodder; Beverages for pets.
83.
USE OF LEVODOPA, CARBIDOPA AND ENTACAPONE FOR TREATING PARKINSON'S DISEASE
The present disclosure provides a method for the treatment of Parkinson's disease comprising simultaneously or sequentially administering to a patient in need of treatment of Parkinson's disease a dosage form comprising
(i) levodopa in an amount ranging from 50 mg to 300 mg,
(ii) carbidopa in an amount ranging from 25 mg to 150 mg or a therapeutically equivalent amount of another aromatic amino acid decarboxylase inhibitor, and
(iii) entacapone in an amount ranging from 50 mg to 300 mg, wherein the proportion of entacapone to carbidopa in said dosage form ranges from 0.3:1.0 to 3.2:1.0 by weight, a moderately potent COMT inhibitor in an amount ranging from 25 mg to 200 mg, wherein the proportion of said COMT inhibitor to carbidopa in said dosage form ranges from 0.16:1.0 to 3.08:1.0 by weight, or a highly potent COMT inhibitor in an amount ranging from 1 mg to 100 mg, wherein the proportion of said COMT inhibitor to carbidopa in said dosage form ranges from 0.006:1.0 to 1.54:1.0 by weight. Pharmaceutical dosage form used in said method are also disclosed.
A61K 31/198 - Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceuticals, medical and veterinary preparations; sanitary preparations for medical purposes; dietetic food and substances adapted for medical or veterinary use; dietary supplements for human beings and animals..
05 - Pharmaceutical, veterinary and sanitary products
10 - Medical apparatus and instruments
Goods & Services
Drug delivery systems in the nature of drug delivery agents in the form of capsules that provide controlled release of the active ingredients for a wide variety of pharmaceuticals; inhalers for medical purposes, sold filled with pharmaceutical preparations for the treatment and alleviation of asthma and other respiratory diseases and ailments; drug delivery systems in the nature of transdermal patches for use in the treatment of pain, allergies, inflammation, viral, metabolic, endocrine, musculoskeletal, cardiovascular, cardiopulmonary, genitourinary, sexual dysfunction, oncological, hepatological, ophthalmic, respiratory, neurological, gastrointestinal, hormonal, dermatological, psychiatric and immune system related diseases and disorders Medical apparatus for facilitating the inhalation of pharmaceutical preparations; inhalers for medical purposes, sold empty; drug delivery systems in the nature of drug delivery patches sold without medication
05 - Pharmaceutical, veterinary and sanitary products
10 - Medical apparatus and instruments
Goods & Services
Chemical preparations for medical purposes, namely, for sanitary purposes; chemical reagents for medical purposes; chemical preparations for veterinary use in the nature of chemical reagents for veterinary use; house mark for a full line of pharmaceutical, veterinary and sanitary products; dietetic preparations adapted for medical purposes; dietetic foods adapted for veterinary purposes; vitamins; medical and surgical plasters; dressings for medical purposes; disinfectants for hygiene purposes; diagnostic preparations for in vitro laboratory use in the nature of in vitro preparations for predicting ovulation; diagnostic preparations for medical and veterinary use; inhaled pharmaceutical preparations for the treatment of respiratory diseases and disorders; inhalers for medical purposes sold filled with pharmaceutical preparations for treating respiratory diseases and disorders; drug delivery systems in the nature of drug delivery agents in the form of capsules that provide controlled release of the active ingredients for a wide variety of pharmaceuticals; inhalers for medical purposes, sold filled with pharmaceutical preparations for the treatment and alleviation of asthma and other respiratory diseases or ailments; drug delivery systems in the nature of transdermal patches for use in the treatment of pain, neurological diseases, menopause, allergies and inflammation Surgical apparatus and instruments for medical, and veterinary use; medical apparatus and instruments for diagnosing or treating respiratory conditions and for monitoring respiratory events; medical apparatus for introducing pharmaceutical preparations into the human body; veterinary apparatus and instruments in the nature of surgical apparatus and instruments for veterinary use; suture materials; medical apparatus for facilitating the inhalation of pharmaceutical preparations; inhalers for medical purposes, sold empty; drug delivery systems in the nature of drug delivery patches sold without medication and inhalers for medical use sold empty; sanitary products being sanitary masks
