AR033683A1 - Compuestos de ciclobutendiona , procedimiento para su preparacion y composiciones farmaceuticas que los contienen - Google Patents
Compuestos de ciclobutendiona , procedimiento para su preparacion y composiciones farmaceuticas que los contienenInfo
- Publication number
- AR033683A1 AR033683A1 ARP010104769A ARP010104769A AR033683A1 AR 033683 A1 AR033683 A1 AR 033683A1 AR P010104769 A ARP010104769 A AR P010104769A AR P010104769 A ARP010104769 A AR P010104769A AR 033683 A1 AR033683 A1 AR 033683A1
- Authority
- AR
- Argentina
- Prior art keywords
- branched
- linear
- group
- heterocycle
- optionally substituted
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D417/14—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 three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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
-
- 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
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D211/20—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms
- C07D211/22—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms by oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Hydrogenated Pyridines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Indole Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Compuestos de ciclobutendiona de la fórmula (1) en los cuales X representa: un heterociclo, monocíclico o bicíclico, saturado, parcialmente insaturado, o un aromático de 5 a 12 eslabones, que contiene de 1 a 3 heteroátomos seleccionados entre oxígeno, nitrógeno y azufre pero que contienen al menos un átomo de nitrógeno, y dicho heterociclo, está unido al resto de la molécula por dicho átomo de nitrógeno y dicho heterociclo ha sido opcionalmente sustituido, o un grupo de fórmula -NR2R3 en la cual R2 representa un átomo de hidrógeno o un grupo alquilo (C1-6) lineal o ramificado, y R3 representa un grupo arilo opcionalmente sustituido un grupo 1,3-dihidro-2H-bencimidazolil-2-ona, o un grupo alquilo (C1-6) lineal o ramificado, sustituido por un heterociclo monocíclico o bicíclico, saturado, parcialmente insaturado o aromático, que tiene de 5 a 12 eslabones, que contiene de 1 a 3 heteroátomos seleccionados entre oxígeno, nitrógeno y azufre, pero que contiene al menos un átomo de nitrógeno, y dicho heterociclo ha sido opcionalmente sustituido, n representa cero o 1, R1 representa un átomo de hidrógeno o un grupo alquilo (C1-6) lineal o ramificado, Ra representa un enlace simple o una cadena alquileno (C1-6) lineal o ramificada, A representa un átomo de nitrógeno o un grupo CH, pero A solo representa un grupo CH cuando Ra representa un enlace simple, y A representa solo un átomo de nitrógeno cuando n representa cero, E representa un átomo de nitrógeno o un grupo CRe, en el cual Re representa también un átomo de hidrógeno, o un enlace a un átomo de carbono de W, y se entiende que al menos uno de los grupos A y E representa un átomo de nitrógeno, Rb representa un enlace simple o una cadena alquileno (C1-6) lineal o ramificada, uno de cuyos átomos de carbono se reemplaza opcionalmente por un átomo de oxígeno o un átomo de azufre, W representa un grupo arilo o heteroarilo, y cada uno de esos grupos ha sido opcionalmente sustituido, sus isómeros ópticos, sus hidratos, sus solvatos y sales de adición de los mismos con un ácido farmacéuticamente aceptable, y se entiende que: se entiende por "grupo arilo", un grupo seleccionado entre fenilo, bifenilo, biciclo[4.2.0]octa-1,3,5-trienilo, naftilo, dihidronaftilo, tetrahidronaftilo, indanilo e indenilo, se entiende por "grupo heteroarilo" un grupo arilo tal como se ha definido anteriormente que contiene de 1 a 3 heteroátomos idénticos o diferentes, seleccionados entre oxígeno, nitrógeno o azufre, se entiende por "opcionalmente sustituido", cuando esta asociado a "heterociclo", "grupo arilo" o "grupo heteroarilo" opcionalmente sustituido por uno o más grupos idénticos o diferentes, seleccionados entre halógeno, alquilo (C1-6) lineal o ramificado, hidroxi, alcoxi (C1-6) lineal o ramificado, mercapto, alquiltio, (C1-6) lineal o ramificado, trihaloalquilo (C1-6) lineal o ramificado, ciano, nitro amino, alquilamino (C1-6) lineal o ramificado, dialquilamino en el cual cada grupo alquilo tiene de 1 a 6 átomos de carbono y es lineal o ramificado, y metilendioxi, se entiende por "isómeros ópticos", los enantiómeros y diastereoisómeros. Experimentos in vitro han permitido demostrar que los compuestos de referencia son capaces de limitar la disfunción endotelial y disminuir la disponibilidad vascular de NO que fueron inducidas por pruebas que implican los dos mecanismos fisiopatológicos ya citados: inhibición de la NO sintetasa endotelial y un estrés oxidativo por producción de O2. Los compuestos debido, a su actividad farmacológica específica que es capaz de limitar el desarrollo de la disfunción endotelial, son útiles para la prevención del desarrollo, extensión y complicaciones de las lesiones ateroescleróticas, especialmente en pacientes que presentan un factor de riesgo vascular (dislipidemia, diabetes, hipertensión arterial), y para tratar las distintas formas clínicas de isquemia de miocardio o periférica, la insuficiencia y las distintas formas de hipertensión arterial pulmonar. Los compuestos también son útiles para prevenir complicaciones vasculares (espasmo, trombosis, restenosis, ateroesclerosis acelerada) en pacientes sometidos a un by-pass, a una dilatación vascular con o sin stent u otras formas de repermeabilización vascular así como a un trasplante cardíaco. También se divulgan un procedimiento para la preparación de los compuestos y composiciones farmacéuticas que los contienen.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR0013072A FR2815345B1 (fr) | 2000-10-12 | 2000-10-12 | Nouveaux derives de cyclobutene-dione, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR033683A1 true AR033683A1 (es) | 2004-01-07 |
Family
ID=8855275
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP010104769A AR033683A1 (es) | 2000-10-12 | 2001-10-11 | Compuestos de ciclobutendiona , procedimiento para su preparacion y composiciones farmaceuticas que los contienen |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US6696469B2 (es) |
| EP (1) | EP1197485B1 (es) |
| JP (1) | JP3566685B2 (es) |
| KR (1) | KR100511132B1 (es) |
| CN (1) | CN1274675C (es) |
| AR (1) | AR033683A1 (es) |
| AT (1) | ATE273276T1 (es) |
| AU (1) | AU781002B2 (es) |
| BR (1) | BR0104471A (es) |
| CA (1) | CA2358724C (es) |
| DE (1) | DE60104791T2 (es) |
| DK (1) | DK1197485T3 (es) |
| EA (1) | EA004268B1 (es) |
| ES (1) | ES2227092T3 (es) |
| FR (1) | FR2815345B1 (es) |
| HK (1) | HK1045517B (es) |
| HU (1) | HUP0104272A3 (es) |
| MX (1) | MXPA01010049A (es) |
| NO (1) | NO320702B1 (es) |
| NZ (1) | NZ514758A (es) |
| PL (1) | PL350104A1 (es) |
| PT (1) | PT1197485E (es) |
| SI (1) | SI1197485T1 (es) |
| TR (1) | TR200402070T4 (es) |
| ZA (1) | ZA200108404B (es) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2005264996A1 (en) | 2004-06-17 | 2006-01-26 | Wyeth | Gonadotropin releasing hormone receptor antagonists |
| EP1756093A1 (en) | 2004-06-17 | 2007-02-28 | Wyeth | Processes for preparing gonadotropin releasing hormone receptor antagonists |
| CN101048383A (zh) * | 2004-11-23 | 2007-10-03 | 惠氏公司 | 促性腺激素释放激素受体拮抗剂 |
| EP2096107A1 (en) * | 2004-12-23 | 2009-09-02 | GPC Biotech AG | Derivatives of squaric acid with anti-proliferative activity |
| US7582634B2 (en) | 2005-02-18 | 2009-09-01 | Wyeth | 7-substituted imidazo[4,5-c]pyridine antagonists of gonadotropin releasing hormone receptor |
| US7534796B2 (en) | 2005-02-18 | 2009-05-19 | Wyeth | Imidazo[4,5-b]pyridine antagonists of gonadotropin releasing hormone receptor |
| US7538113B2 (en) | 2005-02-18 | 2009-05-26 | Wyeth | 4-substituted imidazo[4,5-c]pyridine antagonists of gonadotropin releasing hormone receptor |
| US20060189619A1 (en) * | 2005-02-24 | 2006-08-24 | Wyeth | 3-({4-[2-(4-Tert-butylphenyl)-1h-benzimidazol-4-yl]piperazin-1-yl}methyl)pyrido[2,3-b]]pyrazi ne compounds |
| US7531542B2 (en) | 2005-05-18 | 2009-05-12 | Wyeth | Benzooxazole and benzothiazole antagonists of gonadotropin releasing hormone receptor |
| US7582636B2 (en) | 2005-05-26 | 2009-09-01 | Wyeth | Piperazinylimidazopyridine and piperazinyltriazolopyridine antagonists of Gonadotropin Releasing Hormone receptor |
| US8450348B2 (en) * | 2007-02-21 | 2013-05-28 | Forma Tm, Llc | Derivatives of squaric acid with anti-proliferative activity |
| JP5816082B2 (ja) | 2008-06-24 | 2015-11-17 | トポターゲット・アクティーゼルスカブＴｏｐｏＴａｒｇｅｔ Ａ／Ｓ | ニコチンアミドの阻害剤としてのスクアリン酸誘導体 |
| MX359259B (es) | 2011-09-02 | 2018-09-20 | Novartis Ag | Sal de colina de un compuesto anti - inflamatorio de ciclobutenodiona sustituida. |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE69911980T2 (de) * | 1998-08-21 | 2004-09-09 | Smithkline Beecham P.L.C., Brentford | Pyrimidinonderivate zur behandlung von atheroscleros |
| CA2351464A1 (en) * | 1998-12-14 | 2000-06-22 | Joan E. Sabalski | 3,4-diamino-3-cyclobutene-1,2-dione derivatives which inhibit leukocyte adhesion mediated by vla-4 |
| US6432960B2 (en) * | 2000-05-10 | 2002-08-13 | Bristol-Myers Squibb Company | Squarate derivatives of dihydropyridine NPY antagonists |
-
2000
- 2000-10-12 FR FR0013072A patent/FR2815345B1/fr not_active Expired - Fee Related
-
2001
- 2001-10-05 MX MXPA01010049A patent/MXPA01010049A/es active IP Right Grant
- 2001-10-09 JP JP2001311565A patent/JP3566685B2/ja not_active Expired - Fee Related
- 2001-10-09 BR BR0104471-0A patent/BR0104471A/pt not_active IP Right Cessation
- 2001-10-11 DE DE60104791T patent/DE60104791T2/de not_active Expired - Fee Related
- 2001-10-11 DK DK01402623T patent/DK1197485T3/da active
- 2001-10-11 NZ NZ514758A patent/NZ514758A/xx unknown
- 2001-10-11 ES ES01402623T patent/ES2227092T3/es not_active Expired - Lifetime
- 2001-10-11 SI SI200130164T patent/SI1197485T1/xx unknown
- 2001-10-11 AT AT01402623T patent/ATE273276T1/de not_active IP Right Cessation
- 2001-10-11 TR TR2004/02070T patent/TR200402070T4/xx unknown
- 2001-10-11 PT PT01402623T patent/PT1197485E/pt unknown
- 2001-10-11 CA CA002358724A patent/CA2358724C/fr not_active Expired - Fee Related
- 2001-10-11 NO NO20014945A patent/NO320702B1/no not_active IP Right Cessation
- 2001-10-11 EP EP01402623A patent/EP1197485B1/fr not_active Expired - Lifetime
- 2001-10-11 AR ARP010104769A patent/AR033683A1/es unknown
- 2001-10-12 US US09/976,572 patent/US6696469B2/en not_active Expired - Fee Related
- 2001-10-12 KR KR10-2001-0062988A patent/KR100511132B1/ko not_active IP Right Cessation
- 2001-10-12 AU AU79386/01A patent/AU781002B2/en not_active Ceased
- 2001-10-12 EA EA200100969A patent/EA004268B1/ru unknown
- 2001-10-12 HU HU0104272A patent/HUP0104272A3/hu unknown
- 2001-10-12 ZA ZA200108404A patent/ZA200108404B/xx unknown
- 2001-10-12 PL PL01350104A patent/PL350104A1/xx not_active Application Discontinuation
- 2001-10-12 CN CNB011412968A patent/CN1274675C/zh not_active Expired - Fee Related
-
2002
- 2002-09-26 HK HK02107053.7A patent/HK1045517B/zh not_active IP Right Cessation
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