PE20070181A1 - DERIVADOS DE CICLOHEXILAMINISOQUINOLONA COMO INHIBIDORES DE Rho-QUINASA - Google Patents
DERIVADOS DE CICLOHEXILAMINISOQUINOLONA COMO INHIBIDORES DE Rho-QUINASAInfo
- Publication number
- PE20070181A1 PE20070181A1 PE2006000895A PE2006000895A PE20070181A1 PE 20070181 A1 PE20070181 A1 PE 20070181A1 PE 2006000895 A PE2006000895 A PE 2006000895A PE 2006000895 A PE2006000895 A PE 2006000895A PE 20070181 A1 PE20070181 A1 PE 20070181A1
- Authority
- PE
- Peru
- Prior art keywords
- alkylene
- alkyl
- halogen
- isoquinolin
- rho
- Prior art date
Links
- 102000000568 rho-Associated Kinases Human genes 0.000 title abstract 2
- 108010041788 rho-Associated Kinases Proteins 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title 1
- 229910052736 halogen Inorganic materials 0.000 abstract 5
- 150000002367 halogens Chemical class 0.000 abstract 5
- 206010019668 Hepatic fibrosis Diseases 0.000 abstract 1
- 206010020772 Hypertension Diseases 0.000 abstract 1
- 208000001145 Metabolic Syndrome Diseases 0.000 abstract 1
- 102000003505 Myosin Human genes 0.000 abstract 1
- 108060008487 Myosin Proteins 0.000 abstract 1
- 102000004160 Phosphoric Monoester Hydrolases Human genes 0.000 abstract 1
- 108090000608 Phosphoric Monoester Hydrolases Proteins 0.000 abstract 1
- 108091000080 Phosphotransferase Proteins 0.000 abstract 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-M hydroxide Chemical class [OH-] XLYOFNOQVPJJNP-UHFFFAOYSA-M 0.000 abstract 1
- VDBNYAPERZTOOF-UHFFFAOYSA-N isoquinolin-1(2H)-one Chemical group C1=CC=C2C(=O)NC=CC2=C1 VDBNYAPERZTOOF-UHFFFAOYSA-N 0.000 abstract 1
- AWJUIBRHMBBTKR-UHFFFAOYSA-N isoquinoline Chemical group C1=NC=CC2=CC=CC=C21 AWJUIBRHMBBTKR-UHFFFAOYSA-N 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 208000004296 neuralgia Diseases 0.000 abstract 1
- 208000021722 neuropathic pain Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000026731 phosphorylation Effects 0.000 abstract 1
- 238000006366 phosphorylation reaction Methods 0.000 abstract 1
- 102000020233 phosphotransferase Human genes 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
- C07D217/24—Oxygen atoms
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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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
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- A61P11/16—Central respiratory analeptics
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P15/06—Antiabortive agents; Labour repressants
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
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- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A—HUMAN NECESSITIES
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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
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
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- 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
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- 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
- C07D405/12—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 chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Diabetes (AREA)
- Pulmonology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Endocrinology (AREA)
- Biomedical Technology (AREA)
- Rheumatology (AREA)
- Ophthalmology & Optometry (AREA)
- Oncology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Urology & Nephrology (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Obesity (AREA)
- Reproductive Health (AREA)
- Gynecology & Obstetrics (AREA)
- Vascular Medicine (AREA)
- Hematology (AREA)
- Gastroenterology & Hepatology (AREA)
- Immunology (AREA)
Abstract
SE REFIERE A COMPUESTOS DE ISOQUINOLONA O ISOQUINOLINAS SUSTITUIDOS CON 6-CICLOHEXILAMINAS, DE FORMULAS (I) O (I'), EN DONDE R1 ES H, ALQUILO(C1-C6), ALQUENILO O ALQUINILO(C2-C6), [ALQUILENO(C1-C6)0-1-CICLOALQUILO(C3-C8), ENTRE OTROS; R2 ES H, ALQUILO(C1-C6), [ALQUILENO(C1-C6)]0-1-R', ENTRE OTROS; R3 ES H, HALOGENO, CN, ENTRE OTROS; R4 ES H, HALOGENO, HIDROXI, ENTRE OTROS; R5 ES H, HALOGENO, NO2, ENTRE OTROS; R6 Y R6' SON INDEPENDIENTEMENTE H, R', ALQUILO(C1-C8), ALQUILENO(C1-C6)-O-ALQUILO(C1-C6), CICLOALQUILO(C3-C8), ALQUILENO(C1-C4)-HETEROCICLILO, ENTRE OTROS; R7 Y R8 SON INDEPENDIENTEMENTE H, HALOGENO, ALQUILO(C1-C6), ENTRE OTROS; R9 ES HALOGENO O ALQUILO(C1-C6); n ES 0,1,2,3 o 4; L ES O o O-ALQUILENO(C1-C6). SON PREFERIDOS: 6-(CIS-4-DIETILAMINO-CICLOHEXILOXI)-7-METIL-2H-ISOQUINOLIN-1-ONA, 6-(CIS-4-ISOPROPILAMINO-CICLOHEXILOXI)-7-METIL-2H-ISOQUINOLIN-1-ONA, 2-(TRANS-4-METOXI-BENCIL9-6-(4-METILANIMO-CICLOHEXILOXI)-2H-ISOQUINOLIN-1-ONA, ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA Y UN PROCEDIMIETO DE PREPARACION. ESTOS COMPUESTOS SON INHIBIDORES DE LA Rho-QUINASA Y/O SOBRE LA FOSFORILACION MEDIADA POR LA Rho.QUINASA DE LA FOSFATASA DE LA CADENA LIGERA DE MIOSINA, Y SON UTILES PARA EL TRATAMIENTO HIPERTENSION OCULAR, FIBROSIS HEPATICA, DOLOR NEUROPATICO, SINDROME METABOLICO
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP05016153 | 2005-07-26 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20070181A1 true PE20070181A1 (es) | 2007-03-07 |
Family
ID=35115842
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2006000895A PE20070181A1 (es) | 2005-07-26 | 2006-07-25 | DERIVADOS DE CICLOHEXILAMINISOQUINOLONA COMO INHIBIDORES DE Rho-QUINASA |
Country Status (37)
| Country | Link |
|---|---|
| US (2) | US8609691B2 (es) |
| EP (1) | EP1912949B1 (es) |
| JP (1) | JP5049970B2 (es) |
| KR (1) | KR101336678B1 (es) |
| CN (1) | CN101228132B (es) |
| AR (1) | AR057082A1 (es) |
| AT (1) | ATE521595T1 (es) |
| AU (1) | AU2006274246B2 (es) |
| BR (1) | BRPI0614063A2 (es) |
| CA (1) | CA2615663C (es) |
| CR (1) | CR9604A (es) |
| CY (1) | CY1112085T1 (es) |
| DK (1) | DK1912949T3 (es) |
| DO (1) | DOP2006000177A (es) |
| EC (1) | ECSP088136A (es) |
| ES (1) | ES2372067T3 (es) |
| GT (1) | GT200600327A (es) |
| HK (1) | HK1123036A1 (es) |
| HN (1) | HN2008000130A (es) |
| HR (1) | HRP20110839T1 (es) |
| IL (1) | IL188949A (es) |
| MA (1) | MA29639B1 (es) |
| MX (1) | MX2008000956A (es) |
| MY (1) | MY146644A (es) |
| NI (1) | NI200800024A (es) |
| NO (1) | NO20080965L (es) |
| NZ (1) | NZ565669A (es) |
| PE (1) | PE20070181A1 (es) |
| PL (1) | PL1912949T3 (es) |
| PT (1) | PT1912949E (es) |
| RS (1) | RS52241B (es) |
| RU (1) | RU2440988C2 (es) |
| SI (1) | SI1912949T1 (es) |
| TN (1) | TNSN08038A1 (es) |
| TW (1) | TWI412521B (es) |
| WO (1) | WO2007012422A1 (es) |
| ZA (1) | ZA200710952B (es) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101327780B1 (ko) | 2005-06-28 | 2013-11-11 | 사노피 | Ｒｈｏ 키나제 억제제로서의 이소퀴놀린 유도체 |
| NZ565669A (en) | 2005-07-26 | 2010-05-28 | Sanofi Aventis | Cyclohexylamin isoquinolone derivatives as Rho-kinase inhibitors |
| MX2008001053A (es) | 2005-07-26 | 2008-03-19 | Sanofi Aventis | Derivados de isoquinolona sustituidos con piperidinilo en calidad de inhibidores de rho-quinasa. |
| US7893088B2 (en) | 2006-08-18 | 2011-02-22 | N.V. Organon | 6-substituted isoquinoline derivatives |
| US7906504B2 (en) * | 2006-09-11 | 2011-03-15 | N.V. Organon | 2-(1-oxo-1H-isoquinolin-2-yl)acetamide derivatives |
| CA2673920C (en) * | 2006-12-27 | 2015-03-24 | Sanofi-Aventis | Cycloalkylamine substituted isoquinoline derivatives |
| CN101595094B (zh) * | 2006-12-27 | 2013-02-20 | 塞诺菲-安万特股份有限公司 | 环烷基胺取代的异喹诺酮衍生物 |
| WO2008077555A2 (en) | 2006-12-27 | 2008-07-03 | Sanofi-Aventis | Substituted isoquinolines and their use as rho-kinase inhibitors |
| KR20090094338A (ko) | 2006-12-27 | 2009-09-04 | 사노피-아벤티스 | 치환된 이소퀴놀린 및 이소퀴놀리논 유도체 |
| WO2008077556A1 (en) | 2006-12-27 | 2008-07-03 | Sanofi-Aventis | Cycloalkylamine substituted isoquinoline and isoquinolinone derivatives |
| RU2455302C2 (ru) | 2006-12-27 | 2012-07-10 | Санофи-Авентис | ЗАМЕЩЕННЫЕ ИЗОХИНОЛИНОВЫЕ И ИЗОХИНОЛИНОНОВЫЕ ПРОИЗВОДНЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ Rho-КИНАЗЫ |
| CL2008000973A1 (es) | 2007-04-05 | 2009-01-02 | Astrazeneca Ab | Compuestos derivados de 1-oxo-isoquinolina; procedimiento de preparación; composición farmacéutica; y su uso en el tratamiento de enfermedades pulmonares obstructvas crónicas (epoc) y asma. |
| WO2009054984A1 (en) * | 2007-10-24 | 2009-04-30 | Merck & Co., Inc. | Heterocycle phenyl amide t-type calcium channel antagonists |
| ES2436531T3 (es) | 2008-06-24 | 2014-01-02 | Sanofi | Isoquinolinas e isoquinolinonas sustituidas en posición 6 |
| SI2303845T1 (sl) * | 2008-06-24 | 2013-12-31 | Sanofi | Bi- in policiklični substituirani izokinolin in izokinolinski derivati kot inhibitorji rho-kinaze |
| CN102131784B (zh) * | 2008-06-24 | 2014-08-27 | 赛诺菲-安万特 | 作为rho激酶抑制剂的取代的异喹啉和异喹啉酮 |
| WO2010027746A2 (en) | 2008-08-25 | 2010-03-11 | Irm Llc | Hedgehog pathway modulators |
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