AR037342A1 - Sulfonamidas ciclicas, inhibidores del factor xa de la coagulacion - Google Patents
Sulfonamidas ciclicas, inhibidores del factor xa de la coagulacionInfo
- Publication number
- AR037342A1 AR037342A1 ARP020104288A ARP020104288A AR037342A1 AR 037342 A1 AR037342 A1 AR 037342A1 AR P020104288 A ARP020104288 A AR P020104288A AR P020104288 A ARP020104288 A AR P020104288A AR 037342 A1 AR037342 A1 AR 037342A1
- Authority
- AR
- Argentina
- Prior art keywords
- het
- trisubstituted
- hal
- con
- cycloalkyl
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D275/00—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings
- C07D275/02—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings not condensed with other 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
- A61K31/425—Thiazoles
-
- 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
-
- 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
-
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Heart & Thoracic Surgery (AREA)
- Neurology (AREA)
- Epidemiology (AREA)
- Neurosurgery (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Pain & Pain Management (AREA)
- Biomedical Technology (AREA)
- Rheumatology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Thiazole And Isothizaole Compounds (AREA)
Abstract
Compuestos que responden a la fórmula (1), en donde: E es Ar o Het no sustituido o monosustituido por R1; R1 es CN, CON(R3)2, [C(R3)2]nN(R2)2, C(=NH)-NH2, que también puede estar monosustituido por -COR2, -COOR2, OR2, OCOR2, OCOOR2 o por un grupo amino-protector convencional, o se selecciona de los restos representados por el grupo de fórmulas (2); R2 es H, A, -[C(R3)2]n-Ar', -[C(R3)2]n-Het' o -[C(R3)2]n-cicloalquilo; R3 es H ó A; W es -C(R2)2-, -[C(R2)2]2-, -OC(R2)2-, -NR2C(R2)2-, -NR2COOC(R2)2-, -NR2CONR2C(R2)2-, un carbociclo o heterociclo con uno o dos núcleos, saturado o insaturado con 1 a 4 átomos de N-, O- y/o S, que está mono-, di- o trisustituido por carboniloxi y/o que puede estar mono, di- o trisustituido por Hal, A, -[C(R3)2]n-Ar, -[C(R3)2]n-Het, -[C(R3)2]n-cicloalquilo, OR2, N(R2)2, NO2, CN, [C(R3)2]nCOOR2, O[C(R3)2]oCOOR2, CON(R2)2, NR2COA, NR2CON(R2)2, NR2SO2A, COR2, SO2NR2 y/o S(O)mA; X es CONR2, CONR2C(R3)2, -C(R3)2NR2, -C(R3)2NR2C(R3)2, C(R3)2O- o C(R3)2OC(R3)2; Y es alquileno, cicloalquileno, Het-diilo o Ar-diilo, T es (CH2)p no sustituido o mono-, di- o trisustituido por R4, en donde 1 a 2 grupos CH2 pueden estar sustituidos por átomos de N-, O- y/o S; R4 es Hal, A, -[C(R3)2]n-Ar, -[C(R3)2]n-Het, -[C(R3)2]n-cicloalquilo, OR2, N(R2)2, NO2, CN, [C(R3)2]nCOOR2, CON(R2)2, NR2COA, NR2SO2A, COR2, SO2NR2, S(O)mA o carboniloxi; A es alquilo lineal o ramificado con 1 a 6 átomos de carbono, en donde uno o dos grupos CH2 pueden estar sustituidos por átomos de O- o S- y/o por grupos -CH=CH- y/o también 1-7 átomos de H pueden estar sustituidos por F; Ar es fenilo, naftilo o bifenilo no sustituido o mono-, di- o trisustituido por Hal, A -[C(R3)2]n-Het, -[C(R3)2]n-cicloalquilo, OR2, N(R2)2, NO2, CN, [C(R3)2]nCOOR2, O[C(R3)2]oCOOR2, CON(R2)2, NR2COA, NR2SO2A, COR2, SO2N(R2)2, S(O)mA; Ar' es fenilo, naftilo o bifenilo no sustituido o mono-, di- o trisustituido por Hal, A, -[C(R3)2]n-Het, -[C(R3)2]n-cicloalquilo, OR3, N(R3)2, NO2, CN, [C(R3)2]nCOOR3, O[C(R3)2]oCOOR3, CON(R3)2, NR3COA, NR3SO2A, COR3, SO2N(R3)2, S(O)mA; Het es un heterociclo de uno o dos núcleos, saturado, insaturado o aromático con 1 a 4 átomos de N-, O- y/o S-, que puede estar no sustituido o mono-, di- o trisustituido por carboniloxi, Hal, A, [C(R3)2]n-Ar, -[C(R3)2]n-cicloalquilo, OR2, N(R2)2, NO2, CN, [C(R3)2]nCOOR2, O[C(R3)2]oCOOR2, CON(R2)2, NR2COA, NR2SO2A, COR2, SO2NR2 y/o S(O)mA; Het' es un heterociclo de uno o dos núcleos, saturado, insaturado o aromático con 1 a 4 átomos de N-, O- y/o S-, que puede estar no sustituido o mono-, di- o trisustituido por carboniloxi, Hal, A, -[C(R3)2]n-Ar, -[C(R3)2]n-cicloalquilo, OR3, N(R3)2, NO2, CN, C(R3)2]nCOOR3, O[C(R3)2]oCOOR3, CON(R3)2, NR3COA, NR3SO2A, COR3, SO2NR3 y/o S(O)mA; Hal es F, CI, Br ó I; n es 0, 1 ó 2; m es 0, 1 ó 2; o es 1, 2 ó 3; p es 1, 2, 3, 4, 5 ó 6; y sus derivados, solvatos y estereoisómeros de uso farmacéutico, incluyendo sus mezclas en todas las proporciones. Son inhibidores del factor Xa de la coagulación y se pueden usar para la prevención y/o el tratamiento de enfermedades tromboembólicas y para el tratamiento de tumores.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10155075A DE10155075A1 (de) | 2001-11-09 | 2001-11-09 | Cyclische Sulfonamide |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR037342A1 true AR037342A1 (es) | 2004-11-03 |
Family
ID=7705183
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP020104288A AR037342A1 (es) | 2001-11-09 | 2002-11-08 | Sulfonamidas ciclicas, inhibidores del factor xa de la coagulacion |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US7199133B2 (es) |
| EP (1) | EP1441726B1 (es) |
| JP (1) | JP4447909B2 (es) |
| KR (1) | KR20050035165A (es) |
| CN (1) | CN1582148A (es) |
| AR (1) | AR037342A1 (es) |
| AT (1) | ATE348611T1 (es) |
| AU (1) | AU2002363366B2 (es) |
| BR (1) | BR0213680A (es) |
| CA (1) | CA2465713A1 (es) |
| DE (2) | DE10155075A1 (es) |
| DK (1) | DK1441726T3 (es) |
| ES (1) | ES2277623T3 (es) |
| HU (1) | HUP0401983A2 (es) |
| MX (1) | MXPA04004307A (es) |
| MY (1) | MY134079A (es) |
| PL (1) | PL369737A1 (es) |
| PT (1) | PT1441726E (es) |
| RU (1) | RU2301228C2 (es) |
| WO (1) | WO2003039543A1 (es) |
| ZA (1) | ZA200404549B (es) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1302462A4 (en) * | 2000-07-17 | 2007-07-18 | Takeda Pharmaceutical | Sulphonic derivatives, process for their preparation and their use |
| US20040152741A1 (en) * | 2002-09-09 | 2004-08-05 | Nps Allelix Corporation | Arylglycine derivatives and their use as glycine transport inhibitors |
| WO2004048363A1 (ja) * | 2002-11-22 | 2004-06-10 | Takeda Pharmaceutical Company Limited | イミダゾール誘導体、その製造法および用途 |
| US7371743B2 (en) | 2004-02-28 | 2008-05-13 | Boehringer Ingelheim International Gmbh | Carboxylic acid amides, the preparation thereof and their use as medicaments |
| 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 |
| DE102004054847A1 (de) * | 2004-11-13 | 2006-05-24 | Sanofi-Aventis Deutschland Gmbh | Substituierte Benzoylguanidine, Verfahren zu ihrer Herstellung, ihre Verwendung als Medikament oder Diagnostikum sowie sie enthaltendes Medikament |
| KR101009594B1 (ko) * | 2007-05-09 | 2011-01-20 | 주식회사 레고켐 바이오사이언스 | Ｐ4 위치에 사이클릭 아미딘을 가지는 ＦＸａ 저해제, 이의유도체, 제조방법 및 이를 함유하는 의약 조성물 |
| BRPI0816837B1 (pt) * | 2007-09-28 | 2022-10-18 | Portola Pharmaceuticals, Inc | Composições farmacêuticas, polipeptídeo isolado de duas cadeias e uso de uma composição farmacêutica |
| KR20150105302A (ko) | 2012-11-05 | 2015-09-16 | 난트 홀딩스 아이피, 엘엘씨 | 헤지 호그 신호 경로의 억제제로서 환상 술폰아미드 함유 유도체 |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3901814A1 (de) | 1988-07-28 | 1990-02-01 | Bayer Ag | Substituierte aminomethylzetraline sowie ihre heterocyclischen analoga |
| US5300523A (en) | 1988-07-28 | 1994-04-05 | Bayer Aktiengesellschaft | Substituted aminomethyltetralins and their heterocyclic analogues |
| AU4224993A (en) * | 1992-08-19 | 1994-03-15 | Pfizer Inc. | Substituted benzylamino nitrogen containing non-aromatic heterocycles |
| US5550139A (en) | 1994-01-03 | 1996-08-27 | The Wichita State University | Serine protease inhibitors |
| GB9715895D0 (en) * | 1997-07-29 | 1997-10-01 | Zeneca Ltd | Heterocyclic compounds |
| US6489300B1 (en) | 1997-07-31 | 2002-12-03 | Eugene D. Thorsett | Carbamyloxy compounds which inhibit leukocyte adhesion mediated by VLA-4 |
| AR016133A1 (es) | 1997-07-31 | 2001-06-20 | Wyeth Corp | Compuesto de carbamiloxi que inhiben la adhesion de leucocitos mediada por vla-4, compuestos que son prodrogas de dichos compuestos, composicionfarmaceutica, metodo para fijar vla-4 a una muestra biologica, metodo para el tratamiento de una condicion inflamatoria |
| DE19751949A1 (de) | 1997-11-24 | 1999-05-27 | Bayer Ag | Verwendung von substituierten Aminomethyl-Chromanen zur Verhinderung der neuronalen Degeneration und zur Förderung der neuronalen Regeneration |
| DE19754573A1 (de) * | 1997-12-09 | 1999-06-10 | Bayer Ag | Pharmazeutische Zusammensetzung zur Behandlung von Schlaganfall und Schädel-Hirn-Trauma |
| US6114532A (en) | 1998-02-03 | 2000-09-05 | Boehringer Ingelheim Pharma Kg | Bicyclic heterocycles, the preparation thereof, and their use as pharmaceuticals |
| DE19804085A1 (de) | 1998-02-03 | 1999-08-05 | Boehringer Ingelheim Pharma | 5-Gliedrige heterocyclische kondensierte Benzoderivate, deren Herstellung und deren Verwendung als Arzneimittel |
| BR0009083B1 (pt) | 1999-03-17 | 2011-11-01 | derivado de amida compreendendo um núcleo de quinazolinona, processo para a preparação de um derivado de amida, composição farmacêutica, e, uso de um derivado de amida. | |
| US20030065176A1 (en) * | 2000-01-29 | 2003-04-03 | Myung-Gyun Kang | Factor xa inhibitors with aryl-amidines and derivatives, and prodrugs thereof |
| KR100423899B1 (ko) | 2000-05-10 | 2004-03-24 | 주식회사 엘지생명과학 | 세포 증식 억제제로 유용한 1,1-디옥소이소티아졸리딘을갖는 인다졸 |
| IL155089A0 (en) * | 2000-10-12 | 2003-10-31 | Merck & Co Inc | Aza and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors |
| US6488154B1 (en) * | 2000-10-16 | 2002-12-03 | Ming-Chuan Yeh | Chip tray |
-
2001
- 2001-11-09 DE DE10155075A patent/DE10155075A1/de not_active Withdrawn
-
2002
- 2002-10-10 MX MXPA04004307A patent/MXPA04004307A/es unknown
- 2002-10-10 US US10/495,254 patent/US7199133B2/en not_active Expired - Fee Related
- 2002-10-10 JP JP2003541834A patent/JP4447909B2/ja not_active Expired - Fee Related
- 2002-10-10 WO PCT/EP2002/011349 patent/WO2003039543A1/de active IP Right Grant
- 2002-10-10 BR BR0213680-5A patent/BR0213680A/pt not_active IP Right Cessation
- 2002-10-10 PL PL02369737A patent/PL369737A1/xx unknown
- 2002-10-10 DE DE50209031T patent/DE50209031D1/de not_active Expired - Lifetime
- 2002-10-10 DK DK02802623T patent/DK1441726T3/da active
- 2002-10-10 CA CA002465713A patent/CA2465713A1/en not_active Abandoned
- 2002-10-10 HU HU0401983A patent/HUP0401983A2/hu unknown
- 2002-10-10 AU AU2002363366A patent/AU2002363366B2/en not_active Ceased
- 2002-10-10 PT PT02802623T patent/PT1441726E/pt unknown
- 2002-10-10 CN CNA028219198A patent/CN1582148A/zh active Pending
- 2002-10-10 EP EP02802623A patent/EP1441726B1/de not_active Expired - Lifetime
- 2002-10-10 RU RU2004117594/04A patent/RU2301228C2/ru not_active IP Right Cessation
- 2002-10-10 AT AT02802623T patent/ATE348611T1/de not_active IP Right Cessation
- 2002-10-10 KR KR1020047005508A patent/KR20050035165A/ko not_active Application Discontinuation
- 2002-10-10 ES ES02802623T patent/ES2277623T3/es not_active Expired - Lifetime
- 2002-11-06 MY MYPI20024148A patent/MY134079A/en unknown
- 2002-11-08 AR ARP020104288A patent/AR037342A1/es unknown
-
2004
- 2004-06-08 ZA ZA200404549A patent/ZA200404549B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN1582148A (zh) | 2005-02-16 |
| CA2465713A1 (en) | 2003-05-15 |
| PT1441726E (pt) | 2007-03-30 |
| BR0213680A (pt) | 2004-10-26 |
| KR20050035165A (ko) | 2005-04-15 |
| DE50209031D1 (de) | 2007-02-01 |
| PL369737A1 (en) | 2005-05-02 |
| ATE348611T1 (de) | 2007-01-15 |
| AU2002363366B2 (en) | 2007-11-22 |
| EP1441726B1 (de) | 2006-12-20 |
| DK1441726T3 (da) | 2007-04-10 |
| US7199133B2 (en) | 2007-04-03 |
| RU2301228C2 (ru) | 2007-06-20 |
| ZA200404549B (en) | 2005-02-04 |
| DE10155075A1 (de) | 2003-05-22 |
| WO2003039543A1 (de) | 2003-05-15 |
| US20040254175A1 (en) | 2004-12-16 |
| HUP0401983A2 (hu) | 2005-01-28 |
| ES2277623T3 (es) | 2007-07-16 |
| JP2005522412A (ja) | 2005-07-28 |
| EP1441726A1 (de) | 2004-08-04 |
| JP4447909B2 (ja) | 2010-04-07 |
| RU2004117594A (ru) | 2006-01-10 |
| MY134079A (en) | 2007-11-30 |
| MXPA04004307A (es) | 2004-08-11 |
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