CN103764655A - 作为alk5和/或alk4抑制剂的经2-吡啶基取代的咪唑 - Google Patents
作为alk5和/或alk4抑制剂的经2-吡啶基取代的咪唑 Download PDFInfo
- Publication number
- CN103764655A CN103764655A CN201280034416.4A CN201280034416A CN103764655A CN 103764655 A CN103764655 A CN 103764655A CN 201280034416 A CN201280034416 A CN 201280034416A CN 103764655 A CN103764655 A CN 103764655A
- Authority
- CN
- China
- Prior art keywords
- imidazo
- alkyl
- dihydro
- pyridine
- imidazoles
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 0 C*1C=*c2nc(-c3ccccn3)c(*)[n]2CC1(C)* Chemical compound C*1C=*c2nc(-c3ccccn3)c(*)[n]2CC1(C)* 0.000 description 4
- SGVNXGNPLLXNFL-UHFFFAOYSA-N Cc1nc(-c2c(-c(cc3)ccc3N3CCOCC3)[n](CCN3)c3n2)ccc1 Chemical compound Cc1nc(-c2c(-c(cc3)ccc3N3CCOCC3)[n](CCN3)c3n2)ccc1 SGVNXGNPLLXNFL-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- 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
-
- 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
- A61P11/08—Bronchodilators
-
- 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
-
- 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
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- 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
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
- A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
-
- 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
-
- 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
-
- 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
-
- 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
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
-
- 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
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
-
- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Health & Medical Sciences (AREA)
- Cardiology (AREA)
- Neurology (AREA)
- Physical Education & Sports Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Rheumatology (AREA)
- Reproductive Health (AREA)
- Dermatology (AREA)
- Pulmonology (AREA)
- Hospice & Palliative Care (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Urology & Nephrology (AREA)
- Obesity (AREA)
- Gastroenterology & Hepatology (AREA)
- Immunology (AREA)
- Vascular Medicine (AREA)
- Ophthalmology & Optometry (AREA)
- Psychiatry (AREA)
- Oncology (AREA)
- Gynecology & Obstetrics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
实施例 | IC50(nM) |
2 | 6.6 |
3 | 31.6 |
4 | 12.1 |
6 | 6.1 |
7 | 10.3 |
9 | 11.5 |
15 | 38.1 |
Claims (12)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201161507305P | 2011-07-13 | 2011-07-13 | |
US61/507,305 | 2011-07-13 | ||
PCT/KR2012/005617 WO2013009140A2 (en) | 2011-07-13 | 2012-07-13 | 2-pyridyl substituted imidazoles as alk5 and/or alk4 inhibitors |
Publications (2)
Publication Number | Publication Date |
---|---|
CN103764655A true CN103764655A (zh) | 2014-04-30 |
CN103764655B CN103764655B (zh) | 2017-04-12 |
Family
ID=47506748
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN201280034416.4A Active CN103764655B (zh) | 2011-07-13 | 2012-07-13 | 作为alk5和/或alk4抑制剂的经2‑吡啶基取代的咪唑 |
Country Status (17)
Country | Link |
---|---|
US (1) | US10155763B2 (zh) |
EP (1) | EP2731949B1 (zh) |
JP (1) | JP6094975B2 (zh) |
KR (1) | KR101938368B1 (zh) |
CN (1) | CN103764655B (zh) |
AU (1) | AU2012281281B2 (zh) |
BR (1) | BR112014000774B1 (zh) |
CA (1) | CA2841252C (zh) |
DK (1) | DK2731949T3 (zh) |
ES (1) | ES2671581T3 (zh) |
MX (1) | MX369576B (zh) |
NO (1) | NO2861601T3 (zh) |
PL (1) | PL2731949T3 (zh) |
PT (1) | PT2731949T (zh) |
RU (1) | RU2612958C2 (zh) |
TR (1) | TR201808033T4 (zh) |
WO (1) | WO2013009140A2 (zh) |
Cited By (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN107207531A (zh) * | 2014-11-21 | 2017-09-26 | 里格尔药品股份有限公司 | 作为TGF‑β抑制剂的稠合的咪唑衍生物 |
CN107663206A (zh) * | 2016-07-29 | 2018-02-06 | 上海璎黎药业有限公司 | 含氮芳香杂环化合物、其制备方法、药物组合物和应用 |
WO2018171611A1 (zh) * | 2017-03-22 | 2018-09-27 | 江苏恒瑞医药股份有限公司 | 6-吡唑-[1,2,4]三唑并[4,3-a]吡啶-3-酰胺类衍生物、其制备方法及其在医药上的应用 |
CN110563735A (zh) * | 2019-09-27 | 2019-12-13 | 江苏好收成韦恩农化股份有限公司 | 制备双氟磺草胺的方法 |
CN112759592A (zh) * | 2021-02-01 | 2021-05-07 | 无锡鸣鹭医药科技有限公司 | 一种6-碘[1,2,3]三唑并[1,5-a]吡啶的合成方法 |
CN113272281A (zh) * | 2019-01-10 | 2021-08-17 | 大日本住友制药肿瘤公司 | 用于治疗骨髓增生异常综合征的alk5抑制剂 |
CN114787145A (zh) * | 2019-11-28 | 2022-07-22 | 奥里戈生物制药有限公司 | 作为转化生长因子-β受体I/ALK5抑制剂的苯甲酰胺衍生物 |
Families Citing this family (18)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US10233170B2 (en) * | 2014-04-08 | 2019-03-19 | Rigel Pharmaceuticals, Inc. | 2,3-disubstituted pyridine compounds as TGF-beta inhibitors and methods of use |
US10071079B2 (en) * | 2016-06-29 | 2018-09-11 | Bristol-Myers Squibb Company | [1,2,4]triazolo[1,5-a]pyridinyl substituted indole compounds |
JP2019534266A (ja) | 2016-10-14 | 2019-11-28 | 江蘇恒瑞医薬股▲ふん▼有限公司 | 5員ヘテロアリール環の架橋した環誘導体、その製造方法およびその医学的使用 |
JP2020500177A (ja) | 2016-11-14 | 2020-01-09 | ジエンス ヘンルイ メデイシンカンパニー リミテッドJiangsu Hengrui Medicine Co.,Ltd. | 3,4−ビピリジルピラゾール誘導体、およびその製造方法およびその医療応用 |
JP2020512400A (ja) | 2017-03-23 | 2020-04-23 | クラヴィウス ファーマシューティカルズ,エルエルシー | TGFβの阻害のための三置換イミダゾールおよび治療方法 |
GB201718285D0 (en) * | 2017-11-03 | 2017-12-20 | Discuva Ltd | Antibacterial Compounds |
EP3826684A4 (en) | 2018-07-26 | 2022-04-06 | Sumitomo Dainippon Pharma Oncology, Inc. | METHODS FOR TREATING DISEASES ASSOCIATED WITH ABNORMAL ACVR1 EXPRESSION AND ACVR1 INHIBITORS FOR USE THEREOF |
WO2020041562A1 (en) * | 2018-08-22 | 2020-02-27 | Clavius Pharmaceuticals, Llc | Substituted imidazoles for the inhibition of tgf-beta and methods of treatment |
EP3894401A2 (en) | 2018-12-11 | 2021-10-20 | Theravance Biopharma R&D IP, LLC | Naphthyridine and quinoline derivatives useful as alk5 inhibitors |
CN114728941A (zh) | 2019-11-22 | 2022-07-08 | 施万生物制药研发Ip有限责任公司 | 作为alk5抑制剂的经取代的1,5-萘啶或喹啉 |
WO2021142086A1 (en) | 2020-01-08 | 2021-07-15 | Synthis Therapeutics, Inc. | Alk5 inhibitor conjugates and uses thereof |
BR112023000588A8 (pt) | 2020-07-15 | 2023-05-09 | Chiesi Farm Spa | Derivados de piridazinil amino como inibidores de alk5 |
EP4182322B1 (en) | 2020-07-15 | 2024-04-24 | Chiesi Farmaceutici S.p.A. | Pyrido oxazine derivatives as alk5 inhibitors |
BR112023000592A2 (pt) | 2020-07-15 | 2023-01-31 | Chiesi Farm Spa | Derivados de pirido oxazina amino como inibidores de alk5 |
EP4267584A1 (en) | 2020-12-23 | 2023-11-01 | Chiesi Farmaceutici S.p.A. | Pyrido oxazine derivatives as alk5 inhibitors |
CN117999077A (zh) | 2021-07-28 | 2024-05-07 | 株式会社蒂奥姆生物 | 用于预防或治疗肿瘤的药物组合物及其用途 |
WO2023208986A1 (en) | 2022-04-27 | 2023-11-02 | Chiesi Farmaceutici S.P.A. | Imidazole derivatives as alk5 inhibitors |
WO2023247592A1 (en) | 2022-06-22 | 2023-12-28 | Chiesi Farmaceutici S.P.A. | 5-(4-fluorophenyl)-2,3-dihydro-1h-imidazo[1,2-a]imidazole derivatives as alk inhibitors for the treatment of fibrosis |
Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN86108538A (zh) * | 1985-12-12 | 1987-07-29 | 史密丝克莱恩贝克曼公司 | 5-脂肪氧合酶途径的抑制 |
WO2007018818A1 (en) * | 2005-07-22 | 2007-02-15 | Eli Lilly And Company | A pyridin quinolin substituted pyrrolo [1,2-b] pyrazole monohydrate as tgf-beta inhibitor |
CN102083811A (zh) * | 2008-06-12 | 2011-06-01 | Sk化学株式会社 | 作为alk5和/或alk4抑制剂的2-吡啶基取代的咪唑 |
Family Cites Families (15)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4175127A (en) * | 1978-09-27 | 1979-11-20 | Smithkline Corporation | Pyridyl substituted 2,3-dihydroimidazo[2,1-b]thiazoles |
US4719218A (en) * | 1985-12-12 | 1988-01-12 | Smithkline Beckman Corporation | Pyrrolo[1,2-a]imidazole and pyrrolo[1,2-a]pyridine derivatives and their use as 5-lipoxygenase pathway inhibitor |
ZW24186A1 (en) * | 1985-12-12 | 1987-07-08 | Smithkline Beckman Corp | Inhibition of the 5-lipoxygenase pathway |
CA2058952A1 (en) * | 1989-06-13 | 1990-12-14 | Nabil Hanna | Monokine activity interference |
JPH04273877A (ja) * | 1991-02-28 | 1992-09-30 | Sumitomo Pharmaceut Co Ltd | 新規なイミダゾール誘導体 |
EP1169317B1 (en) | 1999-04-09 | 2003-01-15 | SmithKline Beecham Corporation | Triarylimidazoles |
US6492408B1 (en) * | 1999-07-21 | 2002-12-10 | Boehringer Ingelheim Pharmaceuticals, Inc. | Small molecules useful in the treatment of inflammatory disease |
CO5271680A1 (es) | 2000-02-21 | 2003-04-30 | Smithkline Beecham Corp | Compuestos |
GB0007405D0 (en) | 2000-03-27 | 2000-05-17 | Smithkline Beecham Corp | Compounds |
GB0100762D0 (en) | 2001-01-11 | 2001-02-21 | Smithkline Beecham Plc | Novel use |
GB0108770D0 (en) * | 2001-04-06 | 2001-05-30 | Eisai London Res Lab Ltd | Inhibitors |
AR039241A1 (es) | 2002-04-04 | 2005-02-16 | Biogen Inc | Heteroarilos trisustituidos y metodos para su produccion y uso de los mismos |
WO2004024074A2 (en) * | 2002-09-13 | 2004-03-25 | Merck & Co., Inc. | Fused heterobicyclo substituted phenyl metabotropic glutamate-5 modulators |
US7405299B2 (en) * | 2002-11-27 | 2008-07-29 | Eli Lilly And Company | Compounds as pharmaceutical agents |
PA8595001A1 (es) * | 2003-03-04 | 2004-09-28 | Pfizer Prod Inc | Nuevos compuestos heteroaromaticos condensados que son inhibidores del factor de crecimiento transforante (tgf) |
-
2012
- 2012-07-13 WO PCT/KR2012/005617 patent/WO2013009140A2/en active Application Filing
- 2012-07-13 PT PT128118650T patent/PT2731949T/pt unknown
- 2012-07-13 KR KR1020147003555A patent/KR101938368B1/ko active IP Right Grant
- 2012-07-13 US US13/548,785 patent/US10155763B2/en active Active
- 2012-07-13 EP EP12811865.0A patent/EP2731949B1/en active Active
- 2012-07-13 CA CA2841252A patent/CA2841252C/en active Active
- 2012-07-13 PL PL12811865T patent/PL2731949T3/pl unknown
- 2012-07-13 TR TR2018/08033T patent/TR201808033T4/tr unknown
- 2012-07-13 ES ES12811865.0T patent/ES2671581T3/es active Active
- 2012-07-13 RU RU2014105169A patent/RU2612958C2/ru active
- 2012-07-13 CN CN201280034416.4A patent/CN103764655B/zh active Active
- 2012-07-13 AU AU2012281281A patent/AU2012281281B2/en active Active
- 2012-07-13 BR BR112014000774-8A patent/BR112014000774B1/pt active IP Right Grant
- 2012-07-13 JP JP2014520137A patent/JP6094975B2/ja active Active
- 2012-07-13 DK DK12811865.0T patent/DK2731949T3/en active
- 2012-07-13 MX MX2014000309A patent/MX369576B/es active IP Right Grant
-
2013
- 2013-06-07 NO NO13729240A patent/NO2861601T3/no unknown
Patent Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN86108538A (zh) * | 1985-12-12 | 1987-07-29 | 史密丝克莱恩贝克曼公司 | 5-脂肪氧合酶途径的抑制 |
WO2007018818A1 (en) * | 2005-07-22 | 2007-02-15 | Eli Lilly And Company | A pyridin quinolin substituted pyrrolo [1,2-b] pyrazole monohydrate as tgf-beta inhibitor |
CN102083811A (zh) * | 2008-06-12 | 2011-06-01 | Sk化学株式会社 | 作为alk5和/或alk4抑制剂的2-吡啶基取代的咪唑 |
Non-Patent Citations (5)
Title |
---|
CHENG HUA JIN: "Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)pyrazoles as transforming growth factor-b type 1 receptor kinase inhibitors", 《EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY》, vol. 46, 21 June 2011 (2011-06-21), pages 3917 - 3925, XP028278289, DOI: 10.1016/j.ejmech.2011.05.063 * |
DAE-KEE KIM,等: "Synthesis and biological evaluation of 4(5)-(6-methylpyridin-2-yl)imidazoles and -pyrazoles as transforming growth factor-b type 1 receptor kinase inhibitors", 《BIOORGANIC & MEDICINAL CHEMISTRY》, vol. 18, 28 April 2010 (2010-04-28), pages 4459 - 4467, XP027072365, DOI: 10.1016/j.bmc.2010.04.071 * |
JAMES F. CALLAHAN,等: "Identification of Novel Inhibitors of the Transforming Growth Factor β1 (TGF-β1) Type 1 Receptor (ALK5)", 《JOURNAL OF MEDICINAL CHEMISTRY》, vol. 45, no. 5, 30 January 2002 (2002-01-30), pages 999 - 1001, XP002293066, DOI: 10.1021/jm010493y * |
JI-XIA REN,等: "Pharmacophore modeling and virtual screening for the discovery of new transforming growth factor-b type I receptor (ALK5) inhibitors", 《EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY》, vol. 44, 16 July 2009 (2009-07-16), pages 4259 - 4265, XP009133644 * |
JUSWINDER SINGH,等: "Successful discovery of TβR1(ALK5) kinase inhibitors using HTS, target-hopping and virtual screening", 《CHEMISTRY TODAY》, vol. 23, no. 3, 30 June 2005 (2005-06-30), pages 35 - 37, XP055142561 * |
Cited By (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN107207531A (zh) * | 2014-11-21 | 2017-09-26 | 里格尔药品股份有限公司 | 作为TGF‑β抑制剂的稠合的咪唑衍生物 |
CN107663206A (zh) * | 2016-07-29 | 2018-02-06 | 上海璎黎药业有限公司 | 含氮芳香杂环化合物、其制备方法、药物组合物和应用 |
CN107663206B (zh) * | 2016-07-29 | 2021-06-18 | 上海璎黎药业有限公司 | 含氮芳香杂环化合物、其制备方法、药物组合物和应用 |
US11466003B2 (en) | 2016-07-29 | 2022-10-11 | Shanghai Yingli Pharmaceutical Co., Ltd | Nitrogenous heterocyclic aromatic compound, preparation method therefor, pharmaceutical composition thereof, and application thereof |
WO2018171611A1 (zh) * | 2017-03-22 | 2018-09-27 | 江苏恒瑞医药股份有限公司 | 6-吡唑-[1,2,4]三唑并[4,3-a]吡啶-3-酰胺类衍生物、其制备方法及其在医药上的应用 |
CN113272281A (zh) * | 2019-01-10 | 2021-08-17 | 大日本住友制药肿瘤公司 | 用于治疗骨髓增生异常综合征的alk5抑制剂 |
CN110563735A (zh) * | 2019-09-27 | 2019-12-13 | 江苏好收成韦恩农化股份有限公司 | 制备双氟磺草胺的方法 |
CN110563735B (zh) * | 2019-09-27 | 2022-03-29 | 江苏好收成韦恩农化股份有限公司 | 制备双氟磺草胺的方法 |
CN114787145A (zh) * | 2019-11-28 | 2022-07-22 | 奥里戈生物制药有限公司 | 作为转化生长因子-β受体I/ALK5抑制剂的苯甲酰胺衍生物 |
CN114787145B (zh) * | 2019-11-28 | 2024-03-26 | 阿戈麦布西班牙股份有限公司 | 作为转化生长因子-β受体I/ALK5抑制剂的苯甲酰胺衍生物 |
CN112759592A (zh) * | 2021-02-01 | 2021-05-07 | 无锡鸣鹭医药科技有限公司 | 一种6-碘[1,2,3]三唑并[1,5-a]吡啶的合成方法 |
Also Published As
Publication number | Publication date |
---|---|
ES2671581T3 (es) | 2018-06-07 |
CA2841252C (en) | 2019-02-26 |
EP2731949A2 (en) | 2014-05-21 |
BR112014000774A2 (pt) | 2016-08-23 |
BR112014000774A8 (pt) | 2017-10-10 |
CN103764655B (zh) | 2017-04-12 |
MX369576B (es) | 2019-11-13 |
KR101938368B1 (ko) | 2019-01-14 |
TR201808033T4 (tr) | 2018-06-21 |
RU2014105169A (ru) | 2015-08-20 |
RU2612958C2 (ru) | 2017-03-14 |
KR20140050048A (ko) | 2014-04-28 |
AU2012281281A1 (en) | 2014-03-06 |
EP2731949B1 (en) | 2018-04-04 |
CA2841252A1 (en) | 2013-01-17 |
AU2012281281B2 (en) | 2017-06-01 |
BR112014000774B1 (pt) | 2022-03-29 |
US10155763B2 (en) | 2018-12-18 |
DK2731949T3 (en) | 2018-06-14 |
WO2013009140A3 (en) | 2013-04-11 |
NO2861601T3 (zh) | 2018-07-07 |
JP6094975B2 (ja) | 2017-03-15 |
PL2731949T3 (pl) | 2018-10-31 |
JP2014520846A (ja) | 2014-08-25 |
MX2014000309A (es) | 2014-02-27 |
EP2731949A4 (en) | 2014-12-17 |
US20130018052A1 (en) | 2013-01-17 |
PT2731949T (pt) | 2018-06-15 |
WO2013009140A2 (en) | 2013-01-17 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
CN103764655A (zh) | 作为alk5和/或alk4抑制剂的经2-吡啶基取代的咪唑 | |
JP6993985B2 (ja) | イソキノリン-3イル-カルボキサミドならびにその調製および使用の方法 | |
AU2010336386B2 (en) | Aminopyrimidine kinase inhibitors | |
TWI534145B (zh) | 四氫吡啶并嘧啶衍生物 | |
JP2006517592A (ja) | ピラゾールおよびそれらを製造し使用する方法 | |
MX2012007403A (es) | Inhibidores de isoindolinona de fosfatidinositol 3-cinasa. | |
CA2847921A1 (en) | Pyrazoloquinolinone derivatives, preparation thereof and therapeutic use thereof | |
CN101501023A (zh) | 苯基取代的杂芳基衍生物及其作为抗肿瘤剂的用途 | |
BG107067A (bg) | Прозводни на 1н-имидазопиридин | |
AU2007264791A1 (en) | Derivatives of ureas of piperidine or pyrrolidine, their preparation and their therapeutical use | |
IL178757A (en) | Imidazoles are converted to 2-pyridyl as 5ALK and / or 4ALK inhibitors | |
NZ590862A (en) | Pyridino-pyridinone derivatives, preparation thereof, and therapeutic use thereof | |
EP2513108B1 (fr) | NOUVEAUX DERIVES D' (HETEROCYCLE-PIPERIDINE CONDENSEE)-(PIPERAZINYL)-1-ALCANONE OU D' (HETEROCYCLE-PYRROLIDINE CONDENSEE)-(PIPERAZINYL)-1-ALCANONE ET LEUR UTILISATION COMME INHIBITEURS DE p75 | |
KR20230122033A (ko) | Trpm3 매개 장애를 치료하기 위한 아릴 유도체 | |
JP2023523176A (ja) | コラーゲン1翻訳阻害剤及びその使用方法 | |
US20200055847A1 (en) | Modulators of hedgehog (hh) signalling pathway | |
AU2010338111B2 (en) | Novel (heterocycle/tetrahydropyridine)-(piperazinyl)-1-alcanone and (heterocycle/dihydropyrrolidine)-(piperazinyl)-1-alcanone derivatives, and use thereof as p75 inhibitors | |
WO2024115465A1 (en) | Pharmaceutical compounds as parp7 and/or parp1 inhibitors |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
C06 | Publication | ||
PB01 | Publication | ||
C10 | Entry into substantive examination | ||
SE01 | Entry into force of request for substantive examination | ||
CB03 | Change of inventor or designer information |
Inventor after: Li Zhouyong Inventor after: Shen Yinge Inventor after: Pu Yishan Inventor after: An Caicheng Inventor after: Jin Xunze Inventor after: Liu Jihu Inventor after: Liu Gengao Inventor after: Jin Zaishan Inventor after: Jin Ronghe Inventor after: Shen Dongche Inventor after: Li Fengyong Inventor after: Jiang Xianghuan Inventor after: Li Xuanzheng Inventor after: Zheng Huiche Inventor before: Li Zhouyong Inventor before: Shen Yinge Inventor before: Pu Yishan Inventor before: An Caicheng Inventor before: Liu Gengao Inventor before: Jin Zaishan Inventor before: Jin Ronghe Inventor before: Shen Dongche Inventor before: Li Fengyong Inventor before: Jiang Xianghuan Inventor before: Li Xuanzheng Inventor before: Zheng Huiche |
|
COR | Change of bibliographic data | ||
GR01 | Patent grant | ||
GR01 | Patent grant | ||
TR01 | Transfer of patent right | ||
TR01 | Transfer of patent right |
Effective date of registration: 20170605 Address after: Gyeonggi Do, South Korea Patentee after: Diaomu biological Co. Ltd. Address before: Gyeonggi Do, South Korea Patentee before: SK Chemicals Co., Ltd. |