EA200702048A1 - Фармакокинетически улучшенные соединения - Google Patents
Фармакокинетически улучшенные соединенияInfo
- Publication number
- EA200702048A1 EA200702048A1 EA200702048A EA200702048A EA200702048A1 EA 200702048 A1 EA200702048 A1 EA 200702048A1 EA 200702048 A EA200702048 A EA 200702048A EA 200702048 A EA200702048 A EA 200702048A EA 200702048 A1 EA200702048 A1 EA 200702048A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- improved compounds
- pharmacokinetically improved
- compounds
- pharmacokinetically
- rock2
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 2
- 101000669917 Homo sapiens Rho-associated protein kinase 1 Proteins 0.000 abstract 2
- 101000669921 Homo sapiens Rho-associated protein kinase 2 Proteins 0.000 abstract 2
- 102100039313 Rho-associated protein kinase 1 Human genes 0.000 abstract 2
- 102100039314 Rho-associated protein kinase 2 Human genes 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 230000003285 pharmacodynamic effect Effects 0.000 abstract 1
Classifications
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- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
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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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
-
- 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
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- 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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
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- 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
- A61P25/08—Antiepileptics; Anticonvulsants
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- 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
- A61P25/28—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
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
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- 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]
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- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- 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
- A61P7/08—Plasma substitutes; Perfusion solutions; Dialytics or haemodialytics; Drugs for electrolytic or acid-base disorders, e.g. hypovolemic shock
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- 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
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- 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
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- B—PERFORMING OPERATIONS; TRANSPORTING
- B82—NANOTECHNOLOGY
- B82Y—SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
- B82Y30/00—Nanotechnology for materials or surface science, e.g. nanocomposites
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
-
- 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
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
- C07D405/14—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
- C07D419/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Nanotechnology (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Crystallography & Structural Chemistry (AREA)
- Materials Engineering (AREA)
- General Physics & Mathematics (AREA)
- Condensed Matter Physics & Semiconductors (AREA)
- Composite Materials (AREA)
- Physics & Mathematics (AREA)
- Cardiology (AREA)
- Pain & Pain Management (AREA)
- Urology & Nephrology (AREA)
- Ophthalmology & Optometry (AREA)
- Heart & Thoracic Surgery (AREA)
- Pulmonology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Psychiatry (AREA)
- Endocrinology (AREA)
- Gynecology & Obstetrics (AREA)
- Hematology (AREA)
Abstract
Изобретение относится к ингибиторам ROCK1 и ROCK2 и способам модулирования фармакокинетических и/или фармакодинамических свойств таких соединений. Также представлены способы ингибирования ROCK1 и/или ROCK2, применимые для лечения заболеваний.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US66516505P | 2005-03-25 | 2005-03-25 | |
PCT/US2006/011271 WO2006105081A2 (en) | 2005-03-25 | 2006-03-27 | Pharmacokinetically improved compounds |
Publications (2)
Publication Number | Publication Date |
---|---|
EA200702048A1 true EA200702048A1 (ru) | 2008-04-28 |
EA022875B1 EA022875B1 (ru) | 2016-03-31 |
Family
ID=37054004
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA200702048A EA022875B1 (ru) | 2005-03-25 | 2006-03-27 | Производные 4-(индазол-5-ил-амино)-2-фенилхиназолина |
Country Status (21)
Country | Link |
---|---|
US (6) | US8357693B2 (ru) |
EP (1) | EP1865958B1 (ru) |
JP (2) | JP2008534518A (ru) |
KR (1) | KR20080081122A (ru) |
CN (1) | CN101208094B (ru) |
AU (1) | AU2006230159A1 (ru) |
BR (1) | BRPI0622285A2 (ru) |
CA (1) | CA2602254C (ru) |
CR (1) | CR9465A (ru) |
EA (1) | EA022875B1 (ru) |
EC (1) | ECSP077836A (ru) |
ES (1) | ES2549397T3 (ru) |
GE (1) | GEP20105029B (ru) |
IL (1) | IL186299A0 (ru) |
MX (1) | MX2007011859A (ru) |
NO (1) | NO20075145L (ru) |
NZ (1) | NZ562083A (ru) |
SG (1) | SG155163A1 (ru) |
UA (1) | UA96126C2 (ru) |
WO (1) | WO2006105081A2 (ru) |
ZA (1) | ZA200708858B (ru) |
Families Citing this family (63)
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US7846915B2 (en) | 2004-10-20 | 2010-12-07 | Resverlogix Corporation | Stilbenes and chalcones for the prevention and treatment of cardiovascular diseases |
CR9465A (es) | 2005-03-25 | 2008-06-19 | Surface Logix Inc | Compuestos mejorados farmacocineticamente |
JP5368792B2 (ja) | 2005-07-29 | 2013-12-18 | レスバーロジックス コーポレイション | 複合疾患の予防および処置のための薬学的組成物および挿入可能な医療用デバイスによるその送達 |
JP2009534458A (ja) | 2006-04-26 | 2009-09-24 | キャンサー・リサーチ・テクノロジー・リミテッド | アミノ−エチル−アミノ−アリール(aeaa)化合物およびそれらの使用 |
CN101528042A (zh) * | 2006-08-24 | 2009-09-09 | 表面线段公司 | 药代动力学改进的化合物 |
CA2707449A1 (en) | 2006-12-01 | 2009-06-12 | President And Fellows Of Harvard College | Compounds and methods for enzyme-mediated tumor imaging and therapy |
NZ579355A (en) | 2007-02-01 | 2012-03-30 | Resverlogix Corp | 2-(Aryl)-4-oxo-quinazoline derivatives |
WO2008106692A1 (en) | 2007-03-01 | 2008-09-04 | Novartis Vaccines And Diagnostics, Inc. | Pim kinase inhibitors and methods of their use |
RU2010101416A (ru) * | 2007-06-19 | 2011-07-27 | Такеда Фармасьютикал Компани Лимитед (Jp) | Профилактическое/лекарственное средство от рака |
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JP5412519B2 (ja) | 2008-09-02 | 2014-02-12 | ノバルティス アーゲー | キナーゼ阻害剤としてのピコリンアミド誘導体 |
CA2747417C (en) | 2009-01-08 | 2017-01-03 | Resverlogix Corp. | Compounds for the prevention and treatment of cardiovascular disease |
CA2755095A1 (en) * | 2009-03-09 | 2010-09-16 | Surface Logix, Inc. | Rho kinase inhibitors |
EP2408454B1 (en) | 2009-03-18 | 2024-07-24 | Resverlogix Corp. | Novel anti-inflammatory agents |
EP3431086B1 (en) | 2009-04-22 | 2020-06-17 | Resverlogix Corp. | Novel anti-inflammatory agents |
US8658676B2 (en) * | 2010-10-12 | 2014-02-25 | The Medicines Company | Clevidipine emulsion formulations containing antimicrobial agents |
CN103945848B (zh) | 2011-11-01 | 2016-09-07 | 雷斯韦洛吉克斯公司 | 被取代的喹唑啉酮的口服即释制剂 |
AU2013264831B2 (en) | 2012-05-21 | 2016-04-21 | Novartis Ag | Novel ring-substituted N-pyridinyl amides as kinase inhibitors |
WO2013191244A1 (ja) * | 2012-06-21 | 2013-12-27 | 大正製薬株式会社 | ピリドピリミジン-4-オン誘導体 |
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JP6464139B2 (ja) | 2013-03-14 | 2019-02-06 | コンバージーン・リミテッド・ライアビリティ・カンパニーConvergene Llc | ブロモドメイン含有タンパク質の阻害のための方法および組成物 |
CN111285813A (zh) | 2013-08-23 | 2020-06-16 | 润新生物公司 | 化学实体、组合物和方法 |
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JP6903585B2 (ja) | 2015-03-13 | 2021-07-14 | レスバーロジックス コーポレイション | 補体関連疾患の治療のための組成物および治療方法 |
JP6480025B2 (ja) | 2015-06-24 | 2019-03-06 | 日東電工株式会社 | イオン性化合物及び組成物並びにその使用 |
JP6882289B2 (ja) | 2015-11-25 | 2021-06-02 | コンバージーン・リミテッド・ライアビリティ・カンパニーConvergene Llc | 二環式betブロモドメイン阻害剤及びその使用 |
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US11071735B2 (en) | 2017-04-28 | 2021-07-27 | Kadmon Corporation, Llc | Treatment of inflammatory conditions and autoimmune diseases with glucose uptake inhibitors |
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KR102469161B1 (ko) | 2017-06-30 | 2022-11-23 | 베이징 타이드 파마슈티컬 코퍼레이션 리미티드 | Rho-관련 단백질 키나아제 억제제, Rho-관련 단백질 키나아제 억제제를 함유하는 약학 조성물, 제조 방법 및 약학 조성물의 용도 |
CN110573501B (zh) | 2017-06-30 | 2023-09-29 | 北京泰德制药股份有限公司 | Rho相关蛋白激酶抑制剂、包含其的药物组合物及其制备方法和用途 |
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MA71430A (fr) | 2022-07-14 | 2025-04-30 | Kadmon Corporation, Llc | Méthodes d'administration du belumosudil pour le traitement de la maladie du greffon contre l'hôte chronique chez des sous-populations de patients |
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