AR020121A1 - Derivados de 1,3-oxazol, composicion farmaceutica que los comprende, procedimiento para la preparacion de dichos derivados y el uso de los mismospara la elaboracion de medicamentos utiles como antagonistas del receptor de vitronectina. - Google Patents
Derivados de 1,3-oxazol, composicion farmaceutica que los comprende, procedimiento para la preparacion de dichos derivados y el uso de los mismospara la elaboracion de medicamentos utiles como antagonistas del receptor de vitronectina.Info
- Publication number
- AR020121A1 AR020121A1 ARP990103914A ARP990103914A AR020121A1 AR 020121 A1 AR020121 A1 AR 020121A1 AR P990103914 A ARP990103914 A AR P990103914A AR P990103914 A ARP990103914 A AR P990103914A AR 020121 A1 AR020121 A1 AR 020121A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- het
- cycloalkyl
- derivatives
- crg2
- Prior art date
Links
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical class C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 239000003814 drug Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 17
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 9
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 4
- 102100025248 C-X-C motif chemokine 10 Human genes 0.000 abstract 4
- 101000858088 Homo sapiens C-X-C motif chemokine 10 Proteins 0.000 abstract 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 229910052760 oxygen Inorganic materials 0.000 abstract 3
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000004005 formimidoyl group Chemical group [H]\N=C(/[H])* 0.000 abstract 2
- 125000001475 halogen functional group Chemical group 0.000 abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 abstract 1
- 102100022337 Integrin alpha-V Human genes 0.000 abstract 1
- 208000001132 Osteoporosis Diseases 0.000 abstract 1
- 108010048673 Vitronectin Receptors Proteins 0.000 abstract 1
- 125000002837 carbocyclic group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- -1 methylenedioxy Chemical group 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 239000002464 receptor antagonist Substances 0.000 abstract 1
- 229940044551 receptor antagonist Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
-
- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Physical Education & Sports Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Rheumatology (AREA)
- Engineering & Computer Science (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Pain & Pain Management (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Se describen compuestos derivados de la 1,3-oxazol de formula (1) que son antagonistas del receptor de vitronectina y son utiles en el tratamientode la osteoporosis, en la que: Y es CRR o NRC(O); R1 es -(alquilo C0-6)-Het, -(alquilo C0-6)-Ar, H, -(alquilo C1-6), -CN o -S(O)kRg; R2 esformulas (2); W es -(CHRg)a-U-(CHRg)b-; U está ausente o es CO, CRg2, C(=CRg2), S(O)k, O, NRg, CRgORg, CRg(ORk)CRg2, CRg2CRg(ORk), C(O)CRg2, CRg2C(O), CONRl,NRlCO,OC(O),C(O)O,C(S)O,OC(S),C(S)NRg,NRgC(S),S(O)2NRg,NRgS(O)2N=N, NRgNRg,NRgCRg2,CRg2NRg,CRg2O,OCRg2, CRg=CRg, Ar o Het; G es NRe, S o O; Rg es H,alquilo C1-6, Het-alquilo C0-6, (cicloalquilo C3-7)-alquilo C0-6 o Ar-alquilo C0-6; Rk es Rg, -C(O)Rg o -C(O)ORf; Ri es H, alquilo C1-6, Het-alquilo C0-6,(cicloalquilo C3-7)-alquilo C0-6, Ar-alquilo C0-6 o alquilo C1-6 sustituido con uno a tres grupos elegidos entre halogeno, CN, NRg2, ORg, SRg, CO2Rg yCON(Rg)2; Rf es H, alquilo C1-6 o Ar-alquilo C0-6; Re es H, alquilo C1-6, Ar-alquilo C0-6, Het-alquilo C0-6, (cicloalquilo C3-7)-alquilo C0-6, o (CH2)kCO2Rg;Rb y Rc se eligen independientemente entre H, alquilo C1-6, Ar-alquilo C0-6, Het-alquilo C0-6, o (cicloalquilo C3-7)-alquilo C0-6, halogeno, CF3, ORf, S(O)kRf,CORf, NO2, N(Rf)2, CO(NRf)2, CH2N(Rf)2,o Rb y Rc se juntan formando un anillo heterocíclico o carbocíclico de 5-6 miembros, aromático o no aromático,opcionalmente sustituido con hasta tres sustituyentes elegidos entre halogeno, CF3, alquilo C1-4, ORf, S(O)kRf, CORf, CO2Rf, OH, NO2, N(Rf)2, CO(NRf)2 yCH2N(Rf)2; o metilendioxi; Q1, Q2, Q3 y Q4 son independientemente N o C-Ry, con la condicion de que no más de uno de los grupos Q1, Q2, Q3 y Q4 sea N; R es H,alquilo C1-6, Ar-alquilo C0-6, o (cicloalquilo C3-6)-alquilo C0-6; R es R, -C(O)R o -C(O)OR; Ry es H, halo, -ORg, -SRg, -CN, -NRgRk, -NO2, -CF3,-CF3-S(O)r-, -CO2Rg, -CORg o -CONRg2, o alquilo C1-6 opcionalmente sustituido con halo, -ORg, -SRg, -CN, -NRgR, -NO2, -CF3, RS(O)r-, -CO2Rg, -CORg o-CONRg2; a es 0-2; b es 0-2; k es 0-2;r es 0-2; s es 0-2; u es 0-1; y v es 0-1; o una sal del mismo aceptable farmacéuticamente; un procedimiento para su
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US9570398P | 1998-08-07 | 1998-08-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR020121A1 true AR020121A1 (es) | 2002-04-10 |
Family
ID=22253229
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP990103914A AR020121A1 (es) | 1998-08-07 | 1999-08-05 | Derivados de 1,3-oxazol, composicion farmaceutica que los comprende, procedimiento para la preparacion de dichos derivados y el uso de los mismospara la elaboracion de medicamentos utiles como antagonistas del receptor de vitronectina. |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US6458814B1 (es) |
| EP (1) | EP1102587A4 (es) |
| JP (1) | JP2002522360A (es) |
| KR (1) | KR20010086355A (es) |
| CN (1) | CN1322133A (es) |
| AR (1) | AR020121A1 (es) |
| AU (1) | AU5336299A (es) |
| BR (1) | BR9912638A (es) |
| CA (1) | CA2339666A1 (es) |
| CO (1) | CO5170532A1 (es) |
| CZ (1) | CZ2001447A3 (es) |
| HU (1) | HUP0103090A3 (es) |
| IL (1) | IL141163A0 (es) |
| NO (1) | NO20010620D0 (es) |
| PL (1) | PL346157A1 (es) |
| TR (1) | TR200100363T2 (es) |
| WO (1) | WO2000007544A2 (es) |
| ZA (1) | ZA200100935B (es) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9805655D0 (en) | 1998-03-16 | 1998-05-13 | Celltech Therapeutics Ltd | Chemical compounds |
| GB9826174D0 (en) | 1998-11-30 | 1999-01-20 | Celltech Therapeutics Ltd | Chemical compounds |
| JP2003531141A (ja) | 2000-04-17 | 2003-10-21 | セルテック アール アンド ディ リミテッド | エナミン誘導体 |
| US7119098B2 (en) | 2000-06-15 | 2006-10-10 | Pharmacia Corporation | Heteroarylakanoic acids as intergrin receptor antagonists |
| FR2847254B1 (fr) * | 2002-11-19 | 2005-01-28 | Aventis Pharma Sa | Nouveaux derives antagonistes du recepteur de la vitronectine, leur procede de preparation, leur application comme medicaments et les compositions pharmaceutiques les refermant |
| JP2006516144A (ja) | 2002-12-20 | 2006-06-22 | ファルマシア・コーポレーション | インテグリン受容体アンタゴニスト誘導体としてのチアゾール化合物 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS59108771A (ja) * | 1982-12-13 | 1984-06-23 | Taiho Yakuhin Kogyo Kk | オキサゾール誘導体 |
| FI922867A7 (fi) | 1991-06-21 | 1992-12-22 | Tanabe Seiyaku Co | Dikarbonsyraderivat och foerfarande foer framstaellning av dem |
| ATE181735T1 (de) * | 1993-05-01 | 1999-07-15 | Merck Patent Gmbh | Substituierte 1-phenyl-oxazolidin-2-on derivate, deren herstellung und deren verwendung als adhäsionsrezeptor-antagonisten |
| US5756466A (en) * | 1994-06-17 | 1998-05-26 | Vertex Pharmaceuticals, Inc. | Inhibitors of interleukin-1β converting enzyme |
| AU702661B2 (en) * | 1994-06-29 | 1999-02-25 | Smithkline Beecham Corporation | Vitronectin receptor antagonists |
-
1999
- 1999-08-03 AU AU53362/99A patent/AU5336299A/en not_active Abandoned
- 1999-08-03 WO PCT/US1999/017665 patent/WO2000007544A2/en not_active Ceased
- 1999-08-03 CZ CZ2001447A patent/CZ2001447A3/cs unknown
- 1999-08-03 BR BR9912638-9A patent/BR9912638A/pt not_active Application Discontinuation
- 1999-08-03 PL PL99346157A patent/PL346157A1/xx not_active Application Discontinuation
- 1999-08-03 HU HU0103090A patent/HUP0103090A3/hu unknown
- 1999-08-03 CA CA002339666A patent/CA2339666A1/en not_active Abandoned
- 1999-08-03 TR TR2001/00363T patent/TR200100363T2/xx unknown
- 1999-08-03 CN CN99811933A patent/CN1322133A/zh active Pending
- 1999-08-03 KR KR1020017001583A patent/KR20010086355A/ko not_active Withdrawn
- 1999-08-03 EP EP99938993A patent/EP1102587A4/en not_active Withdrawn
- 1999-08-03 IL IL14116399A patent/IL141163A0/xx unknown
- 1999-08-03 JP JP2000563230A patent/JP2002522360A/ja not_active Withdrawn
- 1999-08-03 US US09/762,406 patent/US6458814B1/en not_active Expired - Fee Related
- 1999-08-05 AR ARP990103914A patent/AR020121A1/es unknown
- 1999-08-06 CO CO99049955A patent/CO5170532A1/es not_active Application Discontinuation
-
2001
- 2001-02-02 ZA ZA200100935A patent/ZA200100935B/en unknown
- 2001-02-06 NO NO20010620A patent/NO20010620D0/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| PL346157A1 (en) | 2002-01-28 |
| CO5170532A1 (es) | 2002-06-27 |
| CN1322133A (zh) | 2001-11-14 |
| HUP0103090A3 (en) | 2002-12-28 |
| CA2339666A1 (en) | 2000-02-17 |
| NO20010620L (no) | 2001-02-06 |
| NO20010620D0 (no) | 2001-02-06 |
| WO2000007544A3 (en) | 2000-05-18 |
| WO2000007544A2 (en) | 2000-02-17 |
| HUP0103090A2 (hu) | 2002-01-28 |
| CZ2001447A3 (cs) | 2001-08-15 |
| IL141163A0 (en) | 2002-02-10 |
| JP2002522360A (ja) | 2002-07-23 |
| BR9912638A (pt) | 2001-05-02 |
| AU5336299A (en) | 2000-02-28 |
| EP1102587A2 (en) | 2001-05-30 |
| EP1102587A4 (en) | 2003-03-12 |
| US6458814B1 (en) | 2002-10-01 |
| KR20010086355A (ko) | 2001-09-10 |
| TR200100363T2 (tr) | 2001-06-21 |
| ZA200100935B (en) | 2002-05-14 |
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| AR020121A1 (es) | Derivados de 1,3-oxazol, composicion farmaceutica que los comprende, procedimiento para la preparacion de dichos derivados y el uso de los mismospara la elaboracion de medicamentos utiles como antagonistas del receptor de vitronectina. | |
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