AR040472A1 - Derivado de 2-(fenil)-2h-pirazol-3-carboxilico-n-4(tioxo-heterociclil)fenil-amida e imino-heterociclil derivados y compuestos relacionados, procedimiento, medicamentos, kit - Google Patents
Derivado de 2-(fenil)-2h-pirazol-3-carboxilico-n-4(tioxo-heterociclil)fenil-amida e imino-heterociclil derivados y compuestos relacionados, procedimiento, medicamentos, kitInfo
- Publication number
- AR040472A1 AR040472A1 AR20030102321A ARP030102321A AR040472A1 AR 040472 A1 AR040472 A1 AR 040472A1 AR 20030102321 A AR20030102321 A AR 20030102321A AR P030102321 A ARP030102321 A AR P030102321A AR 040472 A1 AR040472 A1 AR 040472A1
- Authority
- AR
- Argentina
- Prior art keywords
- atoms
- mono
- hal
- con
- coor2
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—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 being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—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 being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—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 being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—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 being nitrogen, e.g. tetrazole
- A61K31/433—Thidiazoles
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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
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- A61P9/08—Vasodilators for multiple indications
-
- 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
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—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 C07D415/00
- C07D417/02—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 C07D415/00 containing two hetero rings
- C07D417/12—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 C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pain & Pain Management (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Oncology (AREA)
- Vascular Medicine (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Los compuestos 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. Reivindicación 1: Compuestos de la fórmula (1) donde: D está ausente o es una cadena de alquileno saturada, total o parcialmente no saturado de 3 a 4 miembros, en la cual 1 a 3 átomos de C pueden estar reemplazados por un átomo de N y/o 1 a 2 átomos de C pueden estar reemplazados por 1 a 2 átomos de O y/o 1 a 2 átomos de S, pero donde se reemplazan a lo sumo hasta 3 átomos de C y donde adicionalmente puede aparecer un mono, di o trisustitución de la cadena de alquileno y/o de un nitrógeno que se encuentra allí por Hal, A, -[C(R3)2]n-Ar, -[C(R3)2]n-Het, -[C(R3)2]n-cicloalquilo, OR2, N(R2)2, NO2, CN, COOR2, CON(R2)2, NR2COA, NR2SO2A, COR2, SO2NR2, y / o S(O)mA, y donde además un grupo CH2 de la cadena de alquileno puede estar reemplazado por un grupo C=O; M es un anillo de fenilo o un heterociclo aromático que puede contener 1-2 átomos de N, O y/o S; R1, R1' son en cada caso, independientemente entre sí, H, Hal, A, OR2, N(R2)2, NO2, CN, COOR2, CON(R2)2, C(=S)N(R2)2, -[C(R3)2]n-Ar, -[C(R3)2]n-Het o -[C(R3)2]n-cicloalquilo, -[C(R3)2]n-N(R3)2, CN, -C(=NH)-NH2 insustituido o monosustituido por C(=O)R3, COOR3, OR3, OCOR3, OCOOR3 o sustituido por un grupo de protección amino convencional, y de fórmula (2); R2 es H, A, -[C(R3)2]n-Ar, -[C(R3)2]n-Het, -[C(R3)2]n-cicloalquilo, -[C(R3)2]n-N(R3)2 o -[C(R3)2]n-OR3; R2' es H, A, -[C(R3)2]n-Ar', -[C(R3)2]n-Het', -[C(R3)2]n-cicloalquilo, -[C(R3)2]n-N(R3)2 o -[C(R3)2]n-OR3; R2'' es H, A, -[C(R3)2]n-Ar' o -[C(R3)2]n-cicloalquilo, -[C(R3)2]n-N(R3)2 o -[C(R3)2]n-OR3; R3 es H o A; W es un carbociclo o heterociclo mono o bicíclico saturado, no saturado o aromático con 1 a 4 átomos de N, O y/o S, que puede estar mono o disustituido por R2; X es CONR2, CONR2C(R3)2, -C(R3)2NR2 o -C(R3)2NR2C(R3)2, -C(R3)2O-, -C(R3)2OC(R3)2- o NR2CO; Y es alquileno, cicloalquileno, Het-diilo o Ar-diilo; T es un carbociclo o heterociclo mono o bicíclico saturado, no saturado o aromático con 1 a 4 átomos de N, O y/o S, que está mono o disustituido por =S, =NR2, =N-CN, =N-NO2, =NOR2, =NCOR2, =NCOOR2, =NOCOR2 y que además pueda estar mono, disustituido o trisustituido por Hal, A, -[C(R3)2]n-Ar, -[C(R3)2]n-Het -[C(R3)2]n-cicloalquilo, -OR3, N(R3)2, NO2, CN, COOR2, CON(R2)2, NR2COA, NR2CON(R2)2, NR2SO2A, COR2, SO2NR2 y/o S(O)mA; A es alquilo no ramificado o ramificado C1-10, donde uno o dos grupos CH2 pueden estar reemplazados por átomos de O o S y/o por grupos -CH=CH y/o también 1-7 átomos de H pueden estar reemplazados por F; Ar es fenilo, naftilo o bifenilo insustituido o mono, di o trisustituido por Hal, A, OR3, N(R3)2, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3CON(R3)2, NR3SO2A, COR3, SO2N(R3)2, S(O)mA, -[C(R3)2]n-COOR2', u -O-[C(R3)2]o-COOR2'; Ar' es fenilo o bencilo insustituido o mono o disustituido por Hal; Het es un heterociclo mono o bicíclico saturado, no saturado o aromático con 1 a 4 átomos de N, O y/o S, que puede estar insustituido o mono, di o trisustituido por el oxígeno del carbonilo, =S, =N(R3)2, Hal, A, -[C(R3)2]n-Ar, -[C(R3)2]n-Het1, -[C(R3)2]n-cicloalquilo, -[C(R3)2]n-OR2', -[C(R3)2]n-N(R2')2, NO2, CN, -[C(R3)2]n-COOR2', -[C(R3)2]n-CON(R2')2, -[C(R3)2]n-NR2'COA, NR2'CON(R2')2, -[C(R3)2]n-NR2'SO2A, COR2', SO2NR2' y/o S(O)mA; Het1 es un heterociclo mono o bicíclico saturado, no saturado o aromático con 1 a 2 átomos de N, O y/o S, que puede estar insustituido o mono o disustituido por el oxígeno del carbonilo, =S, =N(R3)2, Hal, A, OR2'', N(R2'')2, NO2, CN, COOR2'', CON(R2'')2, NR2''COA, NR2''CON(R2'')2, NR2''SO2A, COR2'', SO2NR2'' y/o S(O)mA; Hal es F, Cl, Br o I; n es 0, 1 ó 2; m es 0, 1 ó 2; o es 1, 2 ó 3; así como los derivados, solvatos estereoisómeros de los mismos de uso farmacéutico, incluyendo las mezclas de los mismos en todas las proporciones.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE10229070A DE10229070A1 (de) | 2002-06-28 | 2002-06-28 | Phenylderivate 5 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR040472A1 true AR040472A1 (es) | 2005-04-06 |
Family
ID=29723536
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
AR20030102321A AR040472A1 (es) | 2002-06-28 | 2003-06-27 | Derivado de 2-(fenil)-2h-pirazol-3-carboxilico-n-4(tioxo-heterociclil)fenil-amida e imino-heterociclil derivados y compuestos relacionados, procedimiento, medicamentos, kit |
Country Status (8)
Country | Link |
---|---|
US (1) | US20050203127A1 (es) |
EP (2) | EP1517685A1 (es) |
JP (1) | JP2005535630A (es) |
AR (1) | AR040472A1 (es) |
AU (1) | AU2003238475A1 (es) |
CA (1) | CA2491271A1 (es) |
DE (1) | DE10229070A1 (es) |
WO (1) | WO2004002477A1 (es) |
Families Citing this family (17)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU2001269531A1 (en) * | 2000-07-17 | 2002-01-30 | Takeda Chemical Industries Ltd. | Sulfone derivatives, process for their production and use thereof |
EP1564213A4 (en) * | 2002-11-22 | 2009-05-27 | Takeda Pharmaceutical | IMIDAZOLE DERIVATIVES, PROCESS FOR THE PRODUCTION AND USE THEREOF |
TWI396686B (zh) | 2004-05-21 | 2013-05-21 | Takeda Pharmaceutical | 環狀醯胺衍生物、以及其製品和用法 |
DE102004051277A1 (de) * | 2004-10-21 | 2006-04-27 | Merck Patent Gmbh | Heterocyclische Carbonylverbindungen |
CN101087609B (zh) | 2004-10-26 | 2012-11-14 | 詹森药业有限公司 | 因子Xa化合物 |
DE102005038947A1 (de) | 2005-05-18 | 2006-11-30 | Grünenthal GmbH | Substituierte Benzo[d]isoxazol-3-yl-amin-Verbindungen und deren Verwendung in Arzneimitteln |
DE102005045115A1 (de) * | 2005-09-21 | 2007-04-05 | Siemens Ag | Verfahren und Vorrichtung zum Betrieb eines Kommunikationsendgeräts |
US8338367B2 (en) | 2008-10-15 | 2012-12-25 | Boehringer Ingelheim International Gmbh | Fused heteroaryl diamide compounds useful as MMP-13 inhibitors |
JP5529876B2 (ja) | 2008-10-17 | 2014-06-25 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Mmp−13阻害剤として有用なヘテロアリール置換インドール化合物 |
RU2017144535A (ru) | 2010-03-30 | 2019-02-18 | Версеон Корпорейшн | Мультизамещенные ароматические соединения в качестве ингибиторов тромбина |
AU2014238478B2 (en) | 2013-03-15 | 2018-07-19 | Verseon Corporation | Halogenopyrazoles as inhibitors of thrombin |
AU2014232308B2 (en) | 2013-03-15 | 2017-11-09 | Verseon Corporation | Multisubstituted aromatic compounds as serine protease inhibitors |
ES2773303T3 (es) | 2013-10-14 | 2020-07-10 | Eisai R&D Man Co Ltd | Compuestos de quinolina sustituidos selectivamente |
US9663486B2 (en) | 2013-10-14 | 2017-05-30 | Eisai R&D Management Co., Ltd. | Selectively substituted quinoline compounds |
CN113307772B (zh) | 2014-03-07 | 2024-06-28 | 拜奥克里斯特制药公司 | 人类血浆激肽释放酶抑制剂 |
AU2015317522A1 (en) | 2014-09-17 | 2017-03-23 | Verseon Corporation | Pyrazolyl-substituted pyridone compounds as serine protease inhibitors |
ES2931460T3 (es) | 2015-02-27 | 2022-12-29 | Verseon Int Corporation | Compuestos de pirazol sustituido como inhibidores de serina proteasa |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
SK86699A3 (en) * | 1996-12-23 | 2000-11-07 | Du Pont Pharm Co | Nitrogen containing heteroaromatics as factor xa inhibitors |
US6020357A (en) * | 1996-12-23 | 2000-02-01 | Dupont Pharmaceuticals Company | Nitrogen containing heteroaromatics as factor Xa inhibitors |
ZA985247B (en) * | 1997-06-19 | 1999-12-17 | Du Pont Merck Pharma | Guanidine mimics as factor Xa inhibitors. |
IL133526A0 (en) * | 1997-06-19 | 2001-04-30 | Du Pont Pharm Co | Inhibitors of factor xa with a neutral p1 specificity group |
US5998424A (en) * | 1997-06-19 | 1999-12-07 | Dupont Pharmaceuticals Company | Inhibitors of factor Xa with a neutral P1 specificity group |
-
2002
- 2002-06-28 DE DE10229070A patent/DE10229070A1/de not_active Withdrawn
-
2003
- 2003-06-05 US US10/519,356 patent/US20050203127A1/en not_active Abandoned
- 2003-06-05 JP JP2004516575A patent/JP2005535630A/ja active Pending
- 2003-06-05 WO PCT/EP2003/005898 patent/WO2004002477A1/de not_active Application Discontinuation
- 2003-06-05 CA CA002491271A patent/CA2491271A1/en not_active Abandoned
- 2003-06-05 EP EP03732540A patent/EP1517685A1/de not_active Withdrawn
- 2003-06-05 EP EP06000157A patent/EP1679073A1/de not_active Withdrawn
- 2003-06-05 AU AU2003238475A patent/AU2003238475A1/en not_active Abandoned
- 2003-06-27 AR AR20030102321A patent/AR040472A1/es not_active Application Discontinuation
Also Published As
Publication number | Publication date |
---|---|
DE10229070A1 (de) | 2004-01-15 |
US20050203127A1 (en) | 2005-09-15 |
EP1679073A1 (de) | 2006-07-12 |
WO2004002477A8 (de) | 2004-04-15 |
WO2004002477A1 (de) | 2004-01-08 |
EP1517685A1 (de) | 2005-03-30 |
JP2005535630A (ja) | 2005-11-24 |
CA2491271A1 (en) | 2004-01-08 |
AU2003238475A1 (en) | 2004-01-19 |
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