The invention relates to anhydrides, solvates and ethanol hetero-solvates and hydrates of dimethoxy docetaxel or (2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenyl-propionate of 4-acetoxy-2α-benzoyloxy-5β,20-epoxy-1-hydroxy-7β, 10β-dimethoxy-9-oxo-tax-11-ene-13α-yle, and to the preparation thereof.
C07D 305/14 - Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
The present invention relates to the compound having the following formula (I): which may be in base form or in the form of a hydrate or a solvate, for its use as a medicament in the treatment of cancer in patients with hepatic impairment.
The invention relates to a compound of formula (I) which may be in base form or in the form of a hydrate or a solvate, for its use as a medicament in the treatment of advanced gastric adenocarcinoma, especially for patients who have failed prior chemotherapy regimens.
The invention relates to a compound of formula: which may be in base form or in the form of a hydrate or a solvate, for its use as a medicament in the treatment of metastatic NSCLC, especially for patients who are not catered for by a taxane-based treatment. In particular, the present invention relates to the use of cabazitaxel in the treatment of patients with metastatic NSCLC, who have been previously treated with a docetaxel based regimen.
The present invention relates to a novel crystalline ethyl acetate solvate form of cabazitaxel or 4α-acetoxy-2α-benzoyloxy-5β,20-epoxy-1β-hydroxy-7β,10β-dimethoxy-9-oxo-11-taxen-13α-yl(2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate and process for preparing the same.
C07D 305/14 - Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
6.
CABAZITAXEL AND ITS USE FOR TREATING METASTATIC PROSTATE CANCERS
The present invention relates to the compound having the following formula: (I), which may be in base form or in the form of a hydrate or a solvate, in combination with prednisone or prednisolone, for its use for the treatment of castration resistant or hormone-refractory metastatic prostate cancer in patients not at risk of developing gastrointestinal disorders chosen from the group consisting of: gastrointestinal bleeding and perforation, gastritis, enterocolitis, neutropenic enterocolitis, colitis, intestinal obstruction, and ileus.
The present invention relates to the compound of formula (I): which may be in the form of an anhydrous base, a hydrate or a solvate, for its use for the treatment of pediatric cancers.
The invention relates to anhydrides, solvates and ethanol hetero-solvates and hydrates of dimethoxy docetaxel or (2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenyl-propionate of 4-acetoxy-2α-benzoyloxy-5β,20-epoxy-1-hydroxy-7β,10β-dimethoxy-9-oxo-tax-11-ene-13α-yle, and to the preparation thereof.
C07D 305/14 - Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
9.
CRYSTALLINE FORM OF CABAZITAXEL AND PROCESS FOR PREPARING THE SAME
The present invention relates to a novel crystalline ethyl acetate solvate form of cabazitaxel or 4α-acetoxy-2α-benzoyloxy-5β,20-epoxy-1β-hydroxy-7β,10β-dimethoxy-9-oxo-11-taxen-13α-yl(2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3- phenylpropionate and process for preparing the same.
C07D 305/14 - Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
The invention relates to an ultra-low molecular weight heparin with an average molecular weight of 2000 to 3000 Daltons, an anti-FXa activity of about 160 U/mg and an anti-Flla activity of about 2 U/mg, in particular semuloparin, for use as a prophylactic antithrombotic agent in cancer patients receiving chemotherapy for locally advanced solid tumors, wherein said use is accompanied by an improval of the survival of patients with locally advanced cancer of the lungs or with a venous thromboembolism risk score equal to or greater than 3.
The present invention relates to a pharmaceutical formulation of ketoprofen sodium salts in a hydrophilic solvent system suitable as a liquid fill composition. In another aspect, the invention also relates to a process for the preparation of the said pharmaceutical formulation and the use of the said formulation for preparing a medicament to treat inflammatory pains.
The invention relates to an ultra-low molecular weight heparin with an average molecular weight of 2000 to 3000 Daltons, an anti-FXa activity of about 60 U/mg and an anti-FIIa activity of about 2 U/mg, in particular semuloparin, for use as an antithrombotic agent for the prophylaxis of venous thromboembolism in cancer patients receiving chemotherapy for locally advanced or metastatic solid tumors, more specifically in patients receiving chemotherapy for locally advanced or metastatic pancreatic or lung cancer, or for locally advanced or metastatic solid tumors with a VTE risk score equal to or greater than 3.
The present invention relates to a combination comprising cabazitaxel and cisplatin. The present invention relates also to a pharmaceutical composition containing such a combination and to a pharmaceutical kit comprising: (i) a first galenic formulation comprising cabazitaxel; and (ii) a second galenic formulation comprising cisplatin. The invention relates also to the use of this combination and/or pharmaceutical composition and/or pharmaceutical kit in the treatment of neoplastic diseases, more particularly in the treatment of cancer.
The invention relates to the use of semuloparin or a pharmaceutically acceptable salt thereof as an antithrombotic treatment in a patient undergoing major abdominal surgery, wherein said use is effective and safe in the prevention of major venous thromboembolism events, such as proximal deep vein thrombosis.
SEMULOPARIN FOR USE AS AN ANTITHROMBOTIC TREATMENT IN MAJOR ABDOMINAL SURGERY WITH IMPROVED SAFETY IN TERMS OF CLINICALLY RELEVANT BLEEDINGS AND MAJOR BLEEDINGS
The invention relates to the use of semuloparin or a pharmaceutically acceptable salt thereof as an antithrombotic treatment in patients undergoing major abdominal surgery, wherein said use involves an improved safety in terms of clinically relevant bleedings and of major bleedings compared to a standard antithrombotic treatment.
The invention relates to the use of semuloparin or a pharmaceutically acceptable salt thereof as an antithrombotic treatment in patients undergoing major orthopaedic surgery, wherein said use involves an improved benefit-risk profile, compared to a standard antithrombotic treatment.
The invention relates to the use of semuloparin or a pharmaceutically acceptable salt thereof for the prevention of a mortality and/or morbidity event, more specifically venous thromboembolism and death, in a patient undergoing major orthopaedic surgery, such as hip replacement, knee replacement or hip fracture surgery.
The invention relates to the use of semuloparin or a pharmaceutically acceptable salt thereof for the extended prevention of a mortality and/or morbidity event, more specifically venous thromboembolism and death, in a patient having undergone hip fracture surgery.
The invention relates to the use of semuloparin or a pharmaceutically acceptable salt thereof as an antithrombotic treatment in patients undergoing hip replacement surgery, wherein said use involves an improved safety in terms of clinically relevant bleedings and of major bleedings compared to a standard antithrombotic treatment.
The invention relates to anhydrides, solvates and ethanol hetero-solvates and hydrates of dimethoxy docetaxel or (2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenyl-propionate of 4-acetoxy-2α-benzoyloxy-5β,20-epoxy-1-hydroxy-7β, 10β-dimethoxy-9-oxo-tax-11-ene-13α-yl, and to the preparation thereof.
C07D 305/14 - Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
The invention relates to a compound of Formula (I): which may be in base form or in the form of a hydrate or a solvate, in combination with prednisone or prednisolone, for its use as a medicament in the treatment of prostate cancer, particularly metastatic prostate cancer, especially for patients who are not catered for by a taxane-based treatment.
A01N 43/02 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atom
A61K 31/335 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
C07D 305/00 - Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms
C07D 407/00 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group
C07D 493/00 - Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
24.
CRYSTALLINE FORMS OF DIMETHOXY DOCETAXEL AND METHODS FOR PREPARING SAME
The invention relates to anhydrides, solvates and ethanol hetero-solvates and hydrates of dimethoxy docetaxel or (2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenyl-propionate of 4-acetoxy-2α-benzoyloxy-5β,20-epoxy-l-hydroxy-7β,10β-dimethoxy-9-oxo-tax-l l- ene-13α-yle, and to the preparation thereof.
C07D 305/14 - Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
The present invention relates to novel taxoid-based compositions comprising injectable formulations of these derivatives in the form of an emulsion. These formulations are for direct intravenous injection.
A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
A61K 47/44 - Oils, fats or waxes according to two or more groups of Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
A61K 9/00 - Medicinal preparations characterised by special physical form
Compounds of formula (I):
2 are as defined in the disclosure, pharmaceutical compositions comprising said compounds, processes for making and methods of using the same are provided.
A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
A61K 38/16 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof
The invention relates to the solubilisation of docetaxel in an organic solvent, to the mixture thereof with polysorbate 80 and to the evaporation of the solvent.
This invention relates to compounds of formula (I)
to processes for the preparation of such compounds, to pharmaceutical compositions comprising such compounds, and to methods of treatment comprising administering of such compounds.
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (C.N.R.S) (France)
Inventor
Bacque, Eric
El-Ahmad, Youssef
Billard, Thierry
Langlois, Bernard
Ferry, Aurélien
Abstract
The invention relates to a method for preparing polyfluorinated sulphanylamides of formula (I) and polyfluorinated sulphinamidines of formula (II), wherein R1-R4 are defined as in the claims, and for preparing the precursors of same.
C07C 311/48 - Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups having nitrogen atoms of sulfonamide groups further bound to another hetero atom
C07C 313/20 - Sulfenamides having sulfur atoms of sulfenamide groups bound to acyclic carbon atoms
C07C 313/32 - X and Y not being nitrogen atoms, e.g. N-sulfenylcarbamic acid
C07C 319/14 - Preparation of thiols, sulfides, hydropolysulfides or polysulfides of sulfides
C07C 321/18 - Sulfides, hydropolysulfides, or polysulfides having thio groups bound to acyclic carbon atoms of an acyclic unsaturated carbon skeleton
C07C 321/22 - Thiols, sulfides, hydropolysulfides, or polysulfides having thio groups bound to carbon atoms of rings other than six-membered aromatic rings
C07C 323/12 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and singly-bound oxygen atoms bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
C07C 323/49 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton having at least one of the nitrogen atoms, not being part of nitro or nitroso groups, further bound to other hetero atoms to sulfur atoms
C07C 381/00 - Compounds containing carbon and sulfur and having functional groups not covered by groups
C07C 381/06 - Compounds containing sulfur atoms only bound to two nitrogen atoms
C07D 233/74 - Two oxygen atoms, e.g. hydantoin with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to other ring members
The disclosure relates to compounds of formula (I):
which modulate the activity of proteins, particularly kinases, and to compositions containing the same, and to the use thereof as medicaments, in particular as anticancer agents.
C07D 491/02 - Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups , , or in which the condensed system contains two hetero rings
32.
Fluorene derivatives, composition containing said derivatives and the use thereof
This invention relates to derivatives of 4-(benzimidazol-2-yl)fluorene and 4-(azabenzimidazol-2-yl)fluorene, to pharmaceutical compositions comprising such derivatives, and to methods of treatment of disorders related to Hsp90 protein activity, comprising administering such derivatives.
C07D 401/10 - 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 aromatic rings
A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
C07D 239/02 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
33.
Isoindole derivatives, compositions containing same, preparation thereof and pharmaceutical uses thereof in particular as inhibitors of chaperone protein Hsp90 activities
This invention relates to isoindole derivates of Formula I
to pharmaceutical compositions comprising such derivatives, and to methods of treatment comprising administering of such derivatives.
C07D 221/04 - Ortho- or peri-condensed ring systems
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
34.
USE OF ENOXAPARIN SODIUM FOR TREATING PATIENTS WITH ACUTE ISCHEMIC STROKE
Methods for treating acute ischemic stroke in a patient in need thereof comprising administering an effective amount of enoxaparin sodium to the patient for a therapeutic dosing period are described. Also described are methods for preventing or treating thrombosis, such as thrombotic episodes, in a human patient with acute ischemic stroke by treating that patient with enoxaparin.
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
35.
Substituted pyrazolopyridines, compositions containing them, method for the production thereof, and their use
The disclosure relates to substituted pyrazolo-pyridines, compositions containing them, methods for the production thereof, and to their use as medicaments, in particular, as anticancer agents.
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
The invention relates to compounds having the following general formula (I): in which formula (I): R1 and R4 are independently selected from the group consisting of: H, Me, Et, CO2Rc, CH2ORc, ORc, F, Cl and C(=O)NHRd ; in which Rc is chosen from H, (C1-C6)alkyl, substituted (C1-C6)alkyl, (C3-C7)cycloalkyl; substituted (C3-C7)cycloalkyl, aryl, substituted aryl, heteroaryl and substituted heteroaryl; and in which Rd is chosen from H, (C1-C6)alkyl, substituted (C1-C6)alkyl, (C3-C7)cycloalkyl, substituted (C3-C7)cycloalkyl, and (C3- C7)heterocycloalkyl comprising from 1 to 3 heteroatoms chosen from N, O and S, optionally substituted; R2 and R3 are selected from the group consisting of H, F, ORe and NReRf, with the exception of methoxy and ethoxy, in which: (i) Re and Rf are independently selected from the group consisting of: H, (C1-C6)alkyl, (C1-C6)alkyl substituted with a substituent selected from the group consisting of: ORg, NRhRj, (C3-C7)cycloalkyl and substituted (C3-C7)cycloalkyl, in which: (a) Rg, Rh and Rj are independently selected from the group consisting of: H, (C1-C6)alkyl and substituted (C1-C6)alkyl, or (b) Rg is selected from the group consisting of: H, (C1-C6)alkyl and substituted (C1-C6)alkyl, and Rh and Rj form a ring containing one to three heteroatoms chosen from N, O and S, or (ii) Re and Rf form an optionally substituted heterocycle containing from one to three heteroatoms chosen from N, O and S; R5 is selected from the group consisting of: NMeEt, NH(iPr), NEt2, N(iPr2), NEt(iPr), pyrrolidinyl, piperidinyl, morpholinyl, N-methylpiperazinyl, NHCy, NCy2, NMe(iPr), NH(tBu), NH(iBu), N(nBu)2, piperazinyl, NH(Et), N(nPr)2 and NEt(iPr).
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 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 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
A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
The invention relates to the novel products of formula (I): in which n is 0 or 2; R is pyridyl or pyrimidinyl substituted with an NR1R2 radical, in which one of R1 and R2 is hydrogen or alkyl and the other of R1 and R2 is hydrogen or optionally substituted alkyl, cycloalkyl, heterocycloalkyl, phenyl, pyrimidinyl, pyridyl, and CO-R3 with R3 chosen in particular from amino, alkoxy, heterocycloalkyl, aryl, aryloxy and heteroaryl radicals; all these radicals being optionally substituted; and the salts thereof.
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 401/14 - 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 403/06 - 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 403/14 - 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
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 31/4439 - 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 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
38.
NOVEL CYCLIC UREA DERIVATIVES, PREPARATION THEREOF AND PHARMACEUTICAL USE THEREOF AS KINASE INHIBITORS
The invention relates to the novel products of formula (I): in which X1 and X2 represent: either one hydrogen and the other alkyl; or one -OCF3 or -SCF3 and the other NH-CO-alkyl-R3; or X1 and X2 form, with the phenyl radical to which they are attached, an optionally substituted dihydro-indole radical; R represents pyridyl or pyrimidinyl substituted with NR1R2, with R1 representing hydrogen or alkyl, and R2 representing optionally substituted alkyl, cycloalkyl, heterocycloalkyl, phenyl, pyrimidinyl, pyridyl, and CO-R3 with R3 representing in particular amine, alkoxy, heterocycloalkyl, aryl, aryloxy and heteroaryl; all these radicals being optionally substituted; and salts thereof.
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 401/14 - 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 403/06 - 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 403/14 - 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
A61K 31/4166 - 1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
39.
COMBINATION COMPRISING COMBRETASTATIN AND ANTICANCER AGENTS
An antitumour combination comprising a stilbene derivative and an anticancer compound chosen from VEGF inhibitors, and more particularly VEGF Trap. Also provided are methods for using these pharmaceutical preparations for the treatment of solid carcinomas and the like.
A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 31/136 - Amines, e.g. amantadine having aromatic rings, e.g. methadone having the amino group directly attached to the aromatic ring, e.g. benzeneamine
NOVEL BENZIMIDAZOLE AND BENZOTHIAZOLE DERIVATIVES, METHOD FOR PREPARING SAME, USE THEREOF AS DRUGS, PHARMACEUTICAL COMPOSITIONS AND NOVEL USE IN PARTICULAR AS C-MET INHIBITORS
The invention concerns novel products of formula (I), wherein: A represents NH or S; R1, R2 and R3 represent H, NH2, Hal or Alk, one at least of R1, R2 and R3 being other than hydrogen; R represents in particular: cycloalkyl, alkyl, alkoxy or NR4R5, R4 representing H or Alk and R5 representing cycloalkyl or alkyl optionally substituted by hydroxyl, alkoxy, heteroaryl, heterocycloalkyl, NR6R7, phenyl, phenyl-NR6R7 and CONR6R7, R6 and R7 representing H or Alk or phenyl and R6 and R7 may form together with H a cyclic radical; R4 and R5 may also form together with N a cyclic radical; all the above heterocycloalkyl, heteroaryl and phenyl radicals being optionally substituted, said products being in all the isomeric forms and their salts, as medicines in particular as Met inhibitors.
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 417/12 - 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 two hetero rings linked by a chain containing hetero atoms as chain links
41.
USE OF ENOXAPARIN FOR PERFORMIMG PERCUTANEOUS CORONARY INTERVENTION
Methods for performing percutaneous coronary intervention in a patient in need thereof comprising administering intravenously a bolus comprising an effective amount of enoxaparin sodium to the patient after sheath insertion and prior to the percutaneous coronary intervention are described. Also described are methods for preventing or treating thrombosis, such as thrombotic episodes, in a human percutaneous coronary intervention patient by treating that patient with enoxaparin.
A61K 31/4365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
A61K 31/616 - Salicylic acidDerivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid by carboxylic acids, e.g. acetylsalicylic acid
The invention relates to specific novel 7-aza-indazoles having formula (I), which modulate the activity of proteins, particularly kinases, compositions containing same and the use thereof as a medicament, in particular as anticancer agents.
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
The invention concerns an affinity chromatography column comprising the ATIII protein bound to a solid support, characterized in that the ATIII protein has been first activated by incubation with an unmodified low-molecular weight heparin rich in active species, and in that it is covalently bound to a resin in a ratio less than about 2 mg of protein per ml of hydrated resin.
B01D 15/38 - Selective adsorption, e.g. chromatography characterised by the separation mechanism involving specific interaction not covered by one or more of groups , e.g. affinity, ligand exchange or chiral chromatography
B01J 20/28 - Solid sorbent compositions or filter aid compositionsSorbents for chromatographyProcesses for preparing, regenerating or reactivating thereof characterised by their form or physical properties
B01J 20/22 - Solid sorbent compositions or filter aid compositionsSorbents for chromatographyProcesses for preparing, regenerating or reactivating thereof comprising organic material
44.
1,4-DIHYDROPYRIDINE-FUSED HETEROCYCLES, PROCESS FOR PREPARING THE SAME, USE AND COMPOSITIONS CONTAINING THEM
1,4-Dihydropyridine-fused heterocycles, process for preparing the same, use and compositions containing them. The invention is about substituted dihydropyridine-fused heterocycles useful for the treatment of cancer disease, especially for preventing cancerous cells to divide. These compounds act as inhibitors of Aurora A and/or B kinases. Formula (I).
The invention relates to novel products of formula (1), wherein A1, A2, A3 and A4 are CRa or N, R1 and R1' are such that one represents H, Hal, C1C3-alkyl, C1C3-alkoxy, alkyl-OH, CF3, cyano, carboxy or carboxamido and the other represents Hal; CF3 ; OH ; SH; nitro; amino ; NH-OH ; NH-CO-H ; NH-CO-OH, NH-CO-O alkyl , NH-CO-NH2 ; carboxy ; CN ; CO-NH2 ; X-(CH2)m-alkyl; X-(CH2)m-cycloalkyl ; X-(CH2)m-heterocycloalkyl ; X-(CH2)m-aryl or X-(CH2)m-heteroaryl with X = simple bond, CH2, CH=CH, CH2-O, CH2-NH, CH2-C(O), CH2-C(O)-O, CH2-C(O)-NH, CH2-NH-(CO), CH2-NH-S(O), CH2-NH-S(O)2, O, S, NH, O-C(O), C(O)-NH, -NH-C(O), -NH-C(O)-C(O)-, -NH-C(O)-NH-, ; NH-CS, NH-S(O) or NH-S(O)2 ; m = 0, 1 or 2, or R1 and R'1 form with C to which they are bound either a radical =O ; =S ; =N-OH ; =N-NH2 ; =N-NH-CO-NH2, =CH-OH ; =Y1-(CH2)m-aryl or =Y1-(CH2)m heteroaryl, wherein Y1 represents CH, CH-CO-, CH-CO-NH, N, N-O or N-NH-, where m = 0, 1 or 2, or a cycle, R2 et R'2 represent H, halogen, CF3, nitro, cyano, alkyl, hydroxy, mercapto, amino, alkylamino, dialkylamino, alkoxy, alkylthio, free or esterified carboxy, carboxamide, CO-NH(alkyl) et CO N(alkyl)2, p= 1 à 3 et p'= 1 à 4; Ra represents H ; halogen ; CF3 ; hydroxy ; mercapto ; nitro ; amino ; NH-OH ; NH-CO-H ; NH-CO-NH2 ; carboxy ; CN ; CO-NH2 ; Y-(CH2)n-alkyl ; Y-(CH2)n-cycloalkyl, Y-(CH2)n-heterocycloalkyl, Y-(CH2)n-aryl or Y-(CH2)n-heteroaryl, with Y = O, S, NH, O-C(O), C(O)-NH, NH-C(O), NH-S(O) or NH-S(O)2, with n = 0, 1, 2 or 3, wherein all alkyl, alkoxy, alkylthio, cycloalkyl, heterocycloalkyl, aryl and heteroaryl radicals are optionally substituted and all products in any forms are tautomers and isomers and the salts, which are used in the form of drugs.
The invention relates to substituted pyrrolo-pyridines, compositions containing them, a method for their production and use thereof. The invention particularly relates to the preparation of pyrrolo-pyridines, compositions containing them, their production method and their use as a medicament, in particular, as anticancer agents. Formula (I).
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
The invention relates to triazine derivatives of general formula (I) in which R1 represents a heteroaryl group or aryl group; R2 represents a hydrogen atom or a group (C1-C4) alkyl; R3 represents a group -(CH2)n-NR4R5 in which n is equal to 2, 3 or 4 and R4 and R5, independent of one another, represent a (C1-C4) alkyl group or (C3-C7) cycloalkyl, or R4 and R5, together with the nitrogen atom that carries them, form a (C3-C9) heterocycloalkyl group or; R3 represents a group -(CH2)m-NR4R5 in which m is equal to 0, 1, 2, 3 or 4, and; R6 represents a (C3-C9) heterocycloalkyl group comprising at least one nitrogen atom and bound to the triazine nucleus by a carbon atom; R2 and R3, together with the nitrogen atom carrying them, form a (C5-C9) heterocycloalkyl comprising 2 nitrogen atoms; in the form of a base or of an acid addition salt, as well as in the form of a hydrate or solvate. The invention also relates to a method for preparing these triazine derivatives and their use as ligands of α7 nicotinic acetylcholine receptors.
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 453/02 - Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
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 409/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
48.
NOVEL ISOINDOLE DERIVATIVES, COMPOSITIONS CONTAINING SAME, PREPARATION THEREOF AND PHARMACEUTICAL USES THEREOF IN PARTICULAR AS INHIBITORS OF CHAPERONE PROTEIN HSP90 ACTIVITIES
The invention concerns novel products of formula (I), wherein: A1, A2, A3 and A4 represent CRa or N; n represents 1 or 2; R1 represents O, S or NRb; R2 represents H, halogen, CF3, nitro, cyano, methyl, ethyl, hydroxy, mercapto, amino, methoxy, thiomethoxy, methylamino, dimethylamino, acetylamino, carboxy and carboxamido; Ra represents in particular H, halogen, CF3, hydroxy, mercapto, nitro, amino, NH-OH, NH-CO-H, NH-CO-OH, NH-CO-NH2, carboxy, cyano, carboxamido, Y-(CH2)p-alkyl, Y (CH2)p-cycloalkyl, Y-(CH2)p-heterocycloalkyl, Y-(CH2)p-aryl or Y-(CH2)p-heteroaryl, with Y = O, S, NH, O-C(O), C(O)-NH, NH-C(O), NH-S(O) or NH-S(O)2, and p = 1, 2, or 3; Rb represents H, (CH2)m-cycloalkyl, (CH2)m-heterocycloalkyl, (CH2)m-aryl or (CH2)m-heteroaryl, with m = 0, 1, 2; said products being in all isomeric forms and the salts thereof, as medicines.
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
The invention concerns hydrazinocarbonyl-thieno[2,3-c]pyrazoles, their preparation method, compositions containing same and use thereof. In particular, the invention concerns the preparation of hydrazinocarbonyl-thieno[2,3-c]pyrazoles, their preparation method, compositions containing same, and their use as medicine, in particular as anticancer agents.
The invention concerns novel products of formula (I), wherein: A1 and A2 represent CH or N; X represents Cra or N; Y represents CRb or N; R1, R2, R3 and R4 identical or different represent in particular hydrogen, halogen, cyano, nitro, trifluoromethyl, OR5, SR5, NR5R6, C(O)R5, C(O)OR5, C(O) NR5R6, S(O)R5, S(O)2R5, S(O)NR5R6, S(O)2NR5R6, NR6C(O)R5, NR6C(O)OR5, alkyls, alkenyls, alkynyls, aryls, heteroaryls, aralkyls or heteroaralkyls, all optionally substituted; Ra represents in particular halogen, hydroxyl, alkoxy, nitro; Rb represents in particular hydrogen, halogen, cyano, nitro, trifluoromethyle, -W-(C1- C3 alkyl)m- R5; R5 and R6 represent in particular alkyl, aralkyl or heteroaralkyls optionally substituted; said products being all in the form of isomers and salts, and their use as medicines.
The invention relates to a solid pharmaceutical composition comprising telithromycin or one of the addition salts thereof with a pharmaceutically-acceptable acid as an active principle. The invention is characterised in that the composition comprises the following components in relation to the total weight of the composition: between 0.1 and 80 wt.- % telithromycin or one of the addition salts thereof with a pharmaceutically-acceptable acid, and between 10 and 50 wt.- % of at least one diluent with a plastic behaviour. Advantageously, the invention takes the form of a telithromycin tablet having a noticeably-reduced size but providing an identical dosage of telithromycin and displaying improved mechanical properties.
A61K 31/704 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin, digitoxin
The invention concerns substituted pyrroles, compositions containing same, a method for making same and use thereof. In particular, the invention concerns the preparation of substituted pyrroles, compositions containing same, a method for making same and use thereof, in particular as anti-cancer agents. Formula.
C07D 207/34 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members 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
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
05 - Pharmaceutical, veterinary and sanitary products
42 - Scientific, technological and industrial services, research and design
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Pharmaceutical products. Pharmaceutical, medical and scientific research and
development services for new products. Medical and pharmaceutical services.
The invention relates to a process for preparing compounds of formula (I):
3, n and X are as defined in the description, and to the intermediate compounds for implementing this process.
C07J 43/00 - Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
C07J 1/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, not substituted in position 17 beta by a carbon atom, e.g. oestrane, androstane
A pharmaceutical composition comprised of acetocyclorpropyl taxotere or a derivative thereof, and at least one of an alkylating agent, an antimetabolite, a spindle poison, an epidophyllotoxin, an antibiotic, and enzyme, a topoisomerase inhibitor, a plantinum coordination complex, a biological response modifier or a growth factor inhibitor is described.
A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
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 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
A61K 31/555 - Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
A61K 31/565 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol
A61K 31/704 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin, digitoxin
A61K 31/7064 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical, veterinary and sanitary products; dietetic
substances adapted for medical use, food for babies;
plasters, materials for dressings; material for stopping
teeth and dental wax; disinfectants; products for
destroying vermin; fungicides, herbicides.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Produits pharmaceutiques, vétérinaires et hygiéniques;
substances diététiques à usage médical, aliments pour
bébés; emplâtres, matériel pour pansements; matières
pour plomber les dents et pour empreintes dentaires;
désinfectants; produits pour la destruction des
animaux nuisibles; fongicides, herbicides.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Produits pharmaceutiques et hygiéniques; produits
diététiques pour enfants et malades; emplâtres, matériel
pour pansements; matières pour plomber les dents et pour
empreintes dentaires; désinfectants.
PRECIS DE LA DIVULGATION: L'invention concerne des compositions pharmaceuti- ques contenant, à titre de principe actif, au moins un des produits de formule (I"): (I") dans laquelle peuvent représenter selon une combinaison déterminée, R un alkyle (1-4C), R1 un méthyle ou éthyle, R2 un hydrogène, acétyle, benzoyle, t-butyle ou méthoxyméthyle, R3 un hydrogène, méthyle, éthyle, propargyle ou isobutényle, et R4 un hydrogène, les pointillés symbolisant une éventuelle seconde liaison et le trait ondulé une liaison .alpha. ou .beta.. Les compositions de l'invention s'avèrent utile pour le traitement d'affections locales liées à une hyperandrogénocité, telles que l'acné, l'hirsutisme, la séborrhée et l'hyperpilosité.
