AR034692A1 - Inhibidores de la integrina alfavbeta3, un procedimiento para su preparacion, los medicamentos a base de estos compuestos, las composiciones farmaceuticas que los contienen y el uso de los mismos para preparar un medicamento destinado a combatir enfermedades que se basan en la expresion y funcion pa - Google Patents
Inhibidores de la integrina alfavbeta3, un procedimiento para su preparacion, los medicamentos a base de estos compuestos, las composiciones farmaceuticas que los contienen y el uso de los mismos para preparar un medicamento destinado a combatir enfermedades que se basan en la expresion y funcion paInfo
- Publication number
- AR034692A1 AR034692A1 ARP000104353A ARP000104353A AR034692A1 AR 034692 A1 AR034692 A1 AR 034692A1 AR P000104353 A ARP000104353 A AR P000104353A AR P000104353 A ARP000104353 A AR P000104353A AR 034692 A1 AR034692 A1 AR 034692A1
- Authority
- AR
- Argentina
- Prior art keywords
- substituted
- compounds
- unsubstituted
- inhibitors
- ocf3
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 5
- 102000006495 integrins Human genes 0.000 title abstract 4
- 108010044426 integrins Proteins 0.000 title abstract 4
- 239000003814 drug Substances 0.000 title abstract 3
- 229940079593 drug Drugs 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 208000030499 combat disease Diseases 0.000 title 1
- 229940126601 medicinal product Drugs 0.000 title 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 3
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 239000003446 ligand Substances 0.000 abstract 2
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 102000005962 receptors Human genes 0.000 abstract 2
- 108020003175 receptors Proteins 0.000 abstract 2
- 125000004400 (C1-C12) alkyl group Chemical group 0.000 abstract 1
- 206010003210 Arteriosclerosis Diseases 0.000 abstract 1
- 206010016654 Fibrosis Diseases 0.000 abstract 1
- 206010061218 Inflammation Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 208000001132 Osteoporosis Diseases 0.000 abstract 1
- 208000007536 Thrombosis Diseases 0.000 abstract 1
- 208000011775 arteriosclerosis disease Diseases 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 1
- 208000029078 coronary artery disease Diseases 0.000 abstract 1
- 230000004761 fibrosis Effects 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 208000015181 infectious disease Diseases 0.000 abstract 1
- 230000004054 inflammatory process Effects 0.000 abstract 1
- 230000003993 interaction Effects 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 208000010125 myocardial infarction Diseases 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 230000001575 pathological effect Effects 0.000 abstract 1
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 abstract 1
- 125000006239 protecting group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 230000029663 wound healing Effects 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/72—Nitrogen atoms
- C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
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- 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
- A61K31/435—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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4402—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
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- 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)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Physical Education & Sports Medicine (AREA)
- Cardiology (AREA)
- Oncology (AREA)
- Rheumatology (AREA)
- Communicable Diseases (AREA)
- Ophthalmology & Optometry (AREA)
- Heart & Thoracic Surgery (AREA)
- Diabetes (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Dermatology (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Virology (AREA)
- Pain & Pain Management (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Pulmonology (AREA)
- Biomedical Technology (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
Abstract
Se describen inhibidores de la integrina alfavbeta3 de fórmula (1): X-Y-Z-R1-CH2-R2(R4)-CH2-CO-R5, en donde: X significa H2N-C(=NH)-, H2N-C(=NH)-NH, A-C(=NH)-NH-, Het1- ó Het1-NH-, donde los grupos amino primarios también pueden estar provistos con grupos protectores de amino convencionales; Y significa -(CH2)n, ó un compuesto de fórmula (2) donde 1, 2, 3 ó 4 grupo metileno pueden estar reemplazados por N, O y/o S; Z está ausente o significa -O-, -NH-, -NA-, -CH(OH)-, -CH(OA)-, -CHA-, -CA2- ó -S-; R1 significa fenileno no sustituido o sustituido 1, 2 ó 3 veces con F, Cl, Br, A, OA, OCF3 ó CN; R2 significa N, CH ó CA; R3 significa H, F, Cl, Br, A, OA ó OCF3; R4 significa fenilo, naftilo o Het2 no sustituido o sustituido una o varias veces con A, arilo ó CF3; R5 significa OH, OA, NH2, NHA ó NA2; Het1 significa un heterociclo de 1 ó 2 núcleos con 1 a 4 átomos de N, que puede estar no sustituido o sustituido 1-2 veces con NH2; Het2 significa un heterociclo aromático de 1 ó 2 núcleos con 1 a 3 átomos de N, O y/o S, que puede estar no sustituido o sustituido 1 ó 2 veces con F, Cl, Br, A, OA, SA, OCF3, -CO-A, CN, COOA, CONH2, CONHA, CONA2 ó NO2; Arilo significa fenilo no sustituido o sustituido 1, 2 ó 3 veces con Hal, A u OA; A significa alquilo C1-12; n significa de 1 a 12; m y o independientemente entre sí significan de 1 a 12; así como sus sales y solvatos fisiológicamente inofensivos. Estos compuestos inhiben especialmente las interacciones de los receptores alfav con los ligando, siendo especialmente efectivos como ligandos de la integrina alfavbeta3. También se describe un procedimiento para preparar los compuestos de fórmula (1), los medicamentos a base de estos compuestos, las composiciones farmacéuticas que los contienen y el uso de los mismos para la preparación de un medicamento para combatir las enfermedades que se basan en la expresión y la función patológica de receptores de integrina alfavbeta3, en particular, para combatir la trombosis, el infarto de miocardio, las enfermedades cardíacas coronarias, la arteriosclerosis, los tumores, la osteoporosis, la fibrosis, las inflamaciones, las infecciones, lapsoriasis, así como para influir sobre los procesos de curación de heridas.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19939980A DE19939980A1 (de) | 1999-08-24 | 1999-08-24 | Inhibitoren des Integrins alphavbeta¶3¶ |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR034692A1 true AR034692A1 (es) | 2004-03-17 |
Family
ID=7919342
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP000104353A AR034692A1 (es) | 1999-08-24 | 2000-08-23 | Inhibidores de la integrina alfavbeta3, un procedimiento para su preparacion, los medicamentos a base de estos compuestos, las composiciones farmaceuticas que los contienen y el uso de los mismos para preparar un medicamento destinado a combatir enfermedades que se basan en la expresion y funcion pa |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US6645991B1 (es) |
| EP (1) | EP1206455A1 (es) |
| JP (1) | JP2003507457A (es) |
| KR (1) | KR20020086849A (es) |
| CN (1) | CN1370146A (es) |
| AR (1) | AR034692A1 (es) |
| AU (1) | AU6992500A (es) |
| BR (1) | BR0013502A (es) |
| CA (1) | CA2382561A1 (es) |
| CZ (1) | CZ2002525A3 (es) |
| DE (1) | DE19939980A1 (es) |
| HK (1) | HK1049667A1 (es) |
| HU (1) | HUP0203212A3 (es) |
| MX (1) | MXPA02001862A (es) |
| NO (1) | NO20020885D0 (es) |
| PL (1) | PL352987A1 (es) |
| SK (1) | SK2272002A3 (es) |
| WO (1) | WO2001014337A1 (es) |
| ZA (1) | ZA200202284B (es) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0008696D0 (en) | 2000-04-07 | 2000-05-31 | Merck Sharp & Dohme | Therapeutic agents |
| WO2001096307A2 (en) | 2000-06-15 | 2001-12-20 | Pharmacia Corporation | Cycloalkyl alkanoic acids as integrin receptor antagonists |
| US6531494B1 (en) | 2001-08-29 | 2003-03-11 | Pharmacia Corporation | Gem-substituted αvβ3 antagonists |
| DE10063173A1 (de) * | 2000-12-18 | 2002-06-20 | Merck Patent Gmbh | Harnstoff- und Urethanderivate |
| AU783516B2 (en) | 2001-04-30 | 2005-11-03 | Warner-Lambert Company | Methods, kits and compositions for using pyrrole derivatives |
| ES2384235T3 (es) * | 2001-10-22 | 2012-07-02 | The Scripps Research Institute | Compuestos dirigidos a integrinas |
| JP2007502300A (ja) * | 2003-08-13 | 2007-02-08 | カイロン コーポレイション | Ｇｓｋ−３インヒビターおよびその使用 |
| PT1765362E (pt) | 2004-06-04 | 2012-06-04 | Scripps Research Inst | Composições e métodos para o tratamento de doenças neovasculares |
| WO2006111925A2 (en) * | 2005-04-18 | 2006-10-26 | Sloan-Kettering Institute For Cancer Research | Inhibition of tumorigenesis by inhibition of a6b4 integrin |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5234936A (en) * | 1991-10-24 | 1993-08-10 | American Home Products Corporation | Pyrimidocycloalkanes as a ii antagonists |
| US5654322A (en) * | 1992-08-11 | 1997-08-05 | Wakunaga Seiyaku Kabushiki Kaisha | Biphenylmethane derivatives and pharmaceuticals containing the same |
| EP0628559B1 (en) * | 1993-06-10 | 2002-04-03 | Beiersdorf-Lilly GmbH | Pyrimidine compounds and their use as pharmaceuticals |
| KR19990076877A (ko) | 1995-12-29 | 1999-10-25 | 스티븐 베네티아너 | 비트로넥틴 수용체 길항제 |
| WO1997036862A1 (en) * | 1996-03-29 | 1997-10-09 | G.D. Searle & Co. | META-SUBSTITUTED PHENYLENE DERIVATIVES AND THEIR USE AS ALPHAvBETA3 INTEGRIN ANTAGONISTS OR INHIBITORS |
| EP0891340B1 (en) | 1996-04-03 | 2002-11-13 | Takeda Chemical Industries, Ltd. | Oxazole derivatives, their production and use |
| DZ2741A1 (fr) | 1998-03-10 | 2003-09-08 | Smithkline Beecham Corp | Composés nouveaux antagonistes des récepteurs de vitronectine procédé pour leur préparation et compositions. |
| AP1654A (en) | 1999-03-24 | 2006-09-01 | Anormed Inc | Chemokine receptor binding heterocyclic compounds. |
-
1999
- 1999-08-24 DE DE19939980A patent/DE19939980A1/de not_active Withdrawn
-
2000
- 2000-08-04 CA CA002382561A patent/CA2382561A1/en not_active Abandoned
- 2000-08-04 WO PCT/EP2000/007590 patent/WO2001014337A1/de not_active Ceased
- 2000-08-04 CN CN00811880A patent/CN1370146A/zh active Pending
- 2000-08-04 MX MXPA02001862A patent/MXPA02001862A/es unknown
- 2000-08-04 AU AU69925/00A patent/AU6992500A/en not_active Abandoned
- 2000-08-04 CZ CZ2002525A patent/CZ2002525A3/cs unknown
- 2000-08-04 HK HK03101817.6A patent/HK1049667A1/zh unknown
- 2000-08-04 PL PL00352987A patent/PL352987A1/xx unknown
- 2000-08-04 US US10/069,187 patent/US6645991B1/en not_active Expired - Fee Related
- 2000-08-04 KR KR1020027001418A patent/KR20020086849A/ko not_active Withdrawn
- 2000-08-04 BR BR0013502-0A patent/BR0013502A/pt not_active IP Right Cessation
- 2000-08-04 SK SK227-2002A patent/SK2272002A3/sk unknown
- 2000-08-04 JP JP2001518426A patent/JP2003507457A/ja active Pending
- 2000-08-04 EP EP00958381A patent/EP1206455A1/de not_active Withdrawn
- 2000-08-04 HU HU0203212A patent/HUP0203212A3/hu unknown
- 2000-08-23 AR ARP000104353A patent/AR034692A1/es not_active Application Discontinuation
-
2002
- 2002-02-22 NO NO20020885A patent/NO20020885D0/no not_active Application Discontinuation
- 2002-03-20 ZA ZA200202284A patent/ZA200202284B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| HUP0203212A2 (hu) | 2003-02-28 |
| KR20020086849A (ko) | 2002-11-20 |
| AU6992500A (en) | 2001-03-19 |
| PL352987A1 (en) | 2003-09-22 |
| NO20020885L (no) | 2002-02-22 |
| ZA200202284B (en) | 2003-08-27 |
| MXPA02001862A (es) | 2002-10-23 |
| NO20020885D0 (no) | 2002-02-22 |
| CN1370146A (zh) | 2002-09-18 |
| CA2382561A1 (en) | 2001-03-01 |
| DE19939980A1 (de) | 2001-03-01 |
| WO2001014337A1 (de) | 2001-03-01 |
| CZ2002525A3 (cs) | 2002-05-15 |
| EP1206455A1 (de) | 2002-05-22 |
| HK1049667A1 (zh) | 2003-05-23 |
| SK2272002A3 (en) | 2002-06-04 |
| US6645991B1 (en) | 2003-11-11 |
| BR0013502A (pt) | 2002-05-07 |
| JP2003507457A (ja) | 2003-02-25 |
| HUP0203212A3 (en) | 2005-02-28 |
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