AR041024A1 - Derivados de benzimidazol como inhibidores del factor de coagulacion xa - Google Patents
Derivados de benzimidazol como inhibidores del factor de coagulacion xaInfo
- Publication number
- AR041024A1 AR041024A1 ARP030103008A ARP030103008A AR041024A1 AR 041024 A1 AR041024 A1 AR 041024A1 AR P030103008 A ARP030103008 A AR P030103008A AR P030103008 A ARP030103008 A AR P030103008A AR 041024 A1 AR041024 A1 AR 041024A1
- Authority
- AR
- Argentina
- Prior art keywords
- hal
- coor2
- con
- atoms
- het
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/02—Inorganic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0048—Eye, e.g. artificial tears
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/02—Suppositories; Bougies; Bases therefor; Ovules
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/282—Organic compounds, e.g. fats
- A61K9/2826—Sugars or sugar alcohols, e.g. sucrose; Derivatives thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/06—Antimigraine agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—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
- C07D409/04—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—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
Abstract
Los nuevos compuestos de la fórmula (1) en la cual D es un anillo carbocíclico o heterocíclico aromático que tiene de 0 a 4 átomos de N, O y/o S, que está insustituido o monosustituido o polisustituido por Hal, A, OR2, N(R2), NO2, CN, COOR2 o CON(R2)2, X y X' son cada uno, en forma independiente entre sí, H, Hal, A, OR2, N(R2)2, NO2, CN, COOR2 o CON(R2)2, R1 es H o A, R2 es H, A, -[C(R1)2]n-Ar', -[C(R1)2]n-Het', -[C(R1)2]n-cicloalquilo, -[C(R1)2n-N(R1)2 o -[C(R1)2]n-OR1, W es _[C(R2)2]nCONR2[C(R2)2]n-, [C(R")2]nNR2CO[C(R2)2]-, [C(R2)2]nO[C(R2)2]-, -[C(R2)2]NNR2[C(R2)2]n-, -[C(R2)2]O[C(R2)2]nCONR2[C(R2)2]n-, -[C(R2)2]nNR2[C(R2)2]n-, -[C(R2)2]nNR2COO[C(R2)2]n- o -[C(R2)2]nS(O)m[C(R2)2]nCONR2[C(R2)2]n-, Y es alqiuleno, cicloalquileno, Het-diilo o Ar-diilo, es un anillo carbocíclico o heterocíclico monocíclico o bicíclico, saturado, no saturado o aromático que tiene de 0 a 4 átomos de N, O y/o S que está insustituido o monosustituido, disustituido o trisustituido por =O, =S, =NR2, =N-CN, =N-NO2, =NOR2, NCOR2, =NCOOR2, NOCOR2, R2,Hal, -[C(R1)2]n- Ar, -[C(R1)2]n-Het, [C(R1)2]n - cicloalquilo, OR2, N(R2)2, NO2, CN, COOR2, CON(R2)2, NR2COA, NR2SO2A, COR y/o S(O)mA, A es alquilo no ramificado o ramificado que tiene 1-10 átomos de carbono, en uno o dos grupos CH2 pueden estar reemplazados por átomos de O o S y/o por grupos -CH=CH- y/o además 1-7 átomos de H pueden estar reemplazados por F, Ar es fenilo, naftilo o bifenilo, cada uno de los cuales está insustituido o monosustituido, disustituido o trisustituido por Hal, A, OR2, N(R2)2, NO2, CN, COOR2, CON(R2)2, NR2COA, NR2CON(R2)2, NR2SO2A, COR2, SO2N(R2)2, S(O)mA, -[(R1)2]n-COOR2 u -O-[C(R1)2]o -COOR2, Ar' es fenilo que está insustituido o monosustituido, disustituido o trisustituido por Hal, A, OR1, N(R1)2, NO2, CN, COOR1, CON(R1)2, NR1COA, NR1SO2A, COR1, SO2N(R1)2, S(O)mA, -[C(R1)2]n, COOR1 u -O-[C(R1)2]o-COOR1, Het es un anillo heterocíclico monocíclico o bicíclico, saturado, no saturado o aromático que tiene de 1 a 4 átomos de N, O y/o S que está insustituido o monosustituido, disustituido o trisustituido por el oxígeno del carbonilo, =S, =N(R1)2, Hal, A, -[C(R1)2]n-Ar, -[C(R1)2]n-Het', -[C(R1)2]n-cicloalquilo, -[C(R1)2]n-OR2, -[C(R1)2]n-N(R2)2, NO2, CN, -[C(R1)2]n-.COOR2, -[C(R1)2]n-CON(R2)2, -[C(R1)2]nNR2COA, NR2CON(R2)23, -[C(R1)2]n-NR2SO2A, COR2, SO2N(R2)2 y/o S(O)mA, Het' es un anillo heterocíclico monocíclico o bicíclico, saturado, no saturado o aromático que tiene de 1 a 4 átomos de N, O y/o S que está insustituido o monosustituido o disustituido por el oxígeno del carbonilo, =S, =N(R1)2, Hal, A, OR1, N(R1)2, NO2, CN, COOR1, CON(R1)2, NR1SO2A, COR1, SO2N(R1)2 y/o S(O)mA, Hal es F, Cl, Br o I, m es 0, 1 ó 2, n es 0, 1 ó 2, o es 1, 2 o 3, y derivados, solvatos y estereoisómeros de ellos de uso farmacéutico, incluyendo sus mezclas en todas las proporciones. Son inhibidores del factor de coagulación Xa y pueden emplearse para la profilaxis y/o la terapia de enfermedades tromboembólicas y para el tratamiento de tumores.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE10238002A DE10238002A1 (de) | 2002-08-20 | 2002-08-20 | Benzimidazolderivate |
Publications (1)
Publication Number | Publication Date |
---|---|
AR041024A1 true AR041024A1 (es) | 2005-04-27 |
Family
ID=31197107
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP030103008A AR041024A1 (es) | 2002-08-20 | 2003-08-20 | Derivados de benzimidazol como inhibidores del factor de coagulacion xa |
Country Status (13)
Country | Link |
---|---|
US (1) | US7566789B2 (es) |
EP (1) | EP1558247B1 (es) |
JP (1) | JP4668614B2 (es) |
CN (1) | CN1674893A (es) |
AR (1) | AR041024A1 (es) |
AT (1) | ATE386518T1 (es) |
AU (1) | AU2003250890B2 (es) |
BR (1) | BR0313634A (es) |
CA (1) | CA2496139C (es) |
DE (2) | DE10238002A1 (es) |
ES (1) | ES2303606T3 (es) |
RU (1) | RU2005108042A (es) |
WO (1) | WO2004017963A1 (es) |
Families Citing this family (28)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
PT3000810T (pt) * | 2002-03-13 | 2017-10-25 | Array Biopharma Inc | Derivados de benzimidazole alquilado n3 como inibidores de mek |
WO2004031145A2 (en) * | 2002-10-02 | 2004-04-15 | Bristol-Myers Squibb Company | Lactam-containing diaminoalkyl, beta-aminoacids, alpha-aminoacids and derivatives thereof as factor xa inhibitors |
EP1702919B1 (en) * | 2003-12-29 | 2012-05-30 | Msd K.K. | Novel 2-heteroaryl-substituted benzimidazole derivative |
US20060160799A1 (en) | 2004-04-23 | 2006-07-20 | Alekshun Michael N | Transcription factor modulating compounds and methods of use thereof |
TW200720255A (en) | 2005-07-13 | 2007-06-01 | Taiho Pharmaceutical Co Ltd | Benzoimidazole compound capable of inhibiting prostaglandin d synthetase |
AU2006295645B2 (en) * | 2005-09-30 | 2011-09-29 | Msd K.K. | 2-heteroaryl-substituted indole derivative |
WO2008076805A2 (en) * | 2006-12-15 | 2008-06-26 | Bristol-Myers Squibb Company | Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor xia inhibitors |
US20110166132A1 (en) * | 2007-12-13 | 2011-07-07 | Amgen Inc. | Gamma Secretase Modulators |
MX2010011920A (es) * | 2008-05-05 | 2010-11-26 | Amgen Inc | Compuestos de urea como moduladores de gamma secretasa. |
PA8854101A1 (es) | 2008-12-18 | 2010-07-27 | Ortho Mcneil Janssen Pharm | Derivados de imidazol bicíclicos sustituidos como moduladores de gamma secretasa |
WO2010089292A1 (en) | 2009-02-06 | 2010-08-12 | Ortho-Mcneil-Janssen Pharmaceuticals, Inc | Novel substituted bicyclic heterocyclic compounds as gamma secretase modulators |
TWI461425B (zh) | 2009-02-19 | 2014-11-21 | Janssen Pharmaceuticals Inc | 作為伽瑪分泌酶調節劑之新穎經取代的苯并唑、苯并咪唑、唑并吡啶及咪唑并吡啶衍生物類 |
JP5559309B2 (ja) | 2009-05-07 | 2014-07-23 | ジヤンセン・フアーマシユーチカルズ・インコーポレーテツド | γ分泌酵素調節物質としての新規置換インダゾールおよびアザインダゾール誘導体 |
EP2454239B1 (en) | 2009-07-15 | 2014-08-13 | Janssen Pharmaceuticals Inc. | Substituted triazole and imidazole derivatives as gamma secretase modulators |
MX2012006994A (es) * | 2009-12-18 | 2012-07-03 | Mitsubishi Tanabe Pharma Corp | Agente antiplaquetas novedoso. |
CA2784765A1 (en) | 2010-01-15 | 2011-07-21 | Janssen Pharmaceuticals, Inc. | Novel substituted bicyclic triazole derivatives as gamma secretase modulators |
ES2536442T3 (es) | 2011-03-24 | 2015-05-25 | Janssen Pharmaceuticals, Inc. | Derivados novedosos de triazolil piperazina y triazolil piperidina como moduladores de la gamma secretasa |
WO2013010904A1 (en) | 2011-07-15 | 2013-01-24 | Janssen Pharmaceuticals, Inc. | Novel substituted indole derivatives as gamma secretase modulators |
WO2013019682A1 (en) * | 2011-07-29 | 2013-02-07 | Tempero Pharmaceuticals, Inc. | Compounds and methods |
CN104583208B (zh) | 2012-05-16 | 2016-09-28 | 杨森制药公司 | 可用于治疗(尤其是)阿尔茨海默病的取代的3,4-二氢-2H-吡啶并[1,2-a]吡嗪-1,6-二酮衍生物 |
ES2608356T3 (es) | 2012-12-20 | 2017-04-10 | Janssen Pharmaceutica Nv | Novedosos derivados tricíclicos de 3,4-dihidro-2H-pirido[1,2-a]pirazin-1,6-diona como moduladores de la secretasa gamma |
AU2014206834B2 (en) | 2013-01-17 | 2017-06-22 | Janssen Pharmaceutica Nv | Novel substituted pyrido-piperazinone derivatives as gamma secretase modulators |
CN103396405A (zh) * | 2013-08-21 | 2013-11-20 | 中国药科大学 | 具有parp抑制作用的苯并咪唑-4-甲酰胺衍生物 |
US10562897B2 (en) | 2014-01-16 | 2020-02-18 | Janssen Pharmaceutica Nv | Substituted 3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-diones as gamma secretase modulators |
US10011585B2 (en) | 2014-07-28 | 2018-07-03 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
SG11201702142UA (en) * | 2014-10-08 | 2017-04-27 | Redx Pharma Plc | N-pyridinyl acetamide derivatives as wnt signalling pathway inhibitors |
CN105712937B (zh) * | 2016-02-28 | 2019-02-22 | 河北宁格生物医药科技有限公司 | 一种治疗转移性肿瘤的化合物及其用途 |
IL309666A (en) | 2021-07-09 | 2024-02-01 | Plexium Inc | Aryl compounds and pharmaceutical preparations that modulate IKZF2 |
Family Cites Families (15)
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DE2641060A1 (de) * | 1976-09-11 | 1978-03-16 | Hoechst Ag | Beta-lactamverbindungen und verfahren zu ihrer herstellung |
JP2869561B2 (ja) * | 1989-05-22 | 1999-03-10 | 大塚製薬株式会社 | 血小板粘着抑制剤 |
JPH06759B2 (ja) | 1989-09-22 | 1994-01-05 | ファイザー製薬株式会社 | 新規なベンゾイミダゾール化合物 |
GB9225141D0 (en) * | 1992-12-01 | 1993-01-20 | Smithkline Beecham Corp | Chemical compounds |
DE4330959A1 (de) | 1993-09-09 | 1995-03-16 | Schering Ag | Neue Benzimidazolderivate, Verfahren zu ihrer Herstellung und ihre pharmazeutische Verwendung |
PE27997A1 (es) | 1994-04-29 | 1997-09-20 | Lilly Co Eli | Antagonistas de receptores de taquicininas |
US5849759A (en) | 1995-12-08 | 1998-12-15 | Berlex Laboratories, Inc. | Naphthyl-substituted benzimidazole derivatives as anti-coagulants |
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WO2000071510A2 (en) * | 1999-05-24 | 2000-11-30 | Cor Therapeutics, Inc. | INHIBITORS OF FACTOR Xa |
MXPA01012283A (es) * | 1999-06-23 | 2002-07-30 | Aventis Pharma Gmbh | Bencimidazoles sustituidos. |
ATE290865T1 (de) * | 1999-10-19 | 2005-04-15 | Merck & Co Inc | Tyrosin kinase inhibitoren |
AP1666A (en) * | 2000-09-11 | 2006-09-29 | Chiron Corp | Quinolinone derivatives as tyrosine kinase inhibitors. |
US7064215B2 (en) | 2001-07-03 | 2006-06-20 | Chiron Corporation | Indazole benzimidazole compounds |
DE10139060A1 (de) * | 2001-08-08 | 2003-02-20 | Merck Patent Gmbh | Phenylderivate |
-
2002
- 2002-08-20 DE DE10238002A patent/DE10238002A1/de not_active Withdrawn
-
2003
- 2003-07-04 BR BR0313634-5A patent/BR0313634A/pt not_active IP Right Cessation
- 2003-07-04 WO PCT/EP2003/007180 patent/WO2004017963A1/de active IP Right Grant
- 2003-07-04 DE DE50309217T patent/DE50309217D1/de not_active Expired - Lifetime
- 2003-07-04 CA CA2496139A patent/CA2496139C/en not_active Expired - Fee Related
- 2003-07-04 ES ES03792176T patent/ES2303606T3/es not_active Expired - Lifetime
- 2003-07-04 AU AU2003250890A patent/AU2003250890B2/en not_active Ceased
- 2003-07-04 RU RU2005108042/04A patent/RU2005108042A/ru not_active Application Discontinuation
- 2003-07-04 US US10/525,001 patent/US7566789B2/en not_active Expired - Fee Related
- 2003-07-04 JP JP2004529997A patent/JP4668614B2/ja not_active Expired - Fee Related
- 2003-07-04 EP EP03792176A patent/EP1558247B1/de not_active Expired - Lifetime
- 2003-07-04 CN CNA038198355A patent/CN1674893A/zh active Pending
- 2003-07-04 AT AT03792176T patent/ATE386518T1/de not_active IP Right Cessation
- 2003-08-20 AR ARP030103008A patent/AR041024A1/es unknown
Also Published As
Publication number | Publication date |
---|---|
DE50309217D1 (en) | 2008-04-03 |
AU2003250890B2 (en) | 2009-07-16 |
BR0313634A (pt) | 2005-06-21 |
ATE386518T1 (de) | 2008-03-15 |
US20050272740A1 (en) | 2005-12-08 |
CN1674893A (zh) | 2005-09-28 |
ES2303606T3 (es) | 2008-08-16 |
AU2003250890A1 (en) | 2004-03-11 |
JP2006500369A (ja) | 2006-01-05 |
US7566789B2 (en) | 2009-07-28 |
EP1558247B1 (de) | 2008-02-20 |
CA2496139C (en) | 2011-12-13 |
CA2496139A1 (en) | 2004-03-04 |
WO2004017963A1 (de) | 2004-03-04 |
RU2005108042A (ru) | 2005-11-20 |
DE10238002A1 (de) | 2004-03-04 |
JP4668614B2 (ja) | 2011-04-13 |
EP1558247A1 (de) | 2005-08-03 |
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