IL168190A - 2-(6- METHYL-PYRIDIN-2-YL)-3-(6-AMIDO-QUINOLIN-4-YL)-5,6-DIHYDRO- 4H-PYRROLO[1,2-b]PYRAZOLE, PHARMACEUTICAL FORMULATIONS COMPRISING IT AND USE THEREOF IN THE PREPARATION OF MEDICAMENTS FOR TREATING CANCER - Google Patents
2-(6- METHYL-PYRIDIN-2-YL)-3-(6-AMIDO-QUINOLIN-4-YL)-5,6-DIHYDRO- 4H-PYRROLO[1,2-b]PYRAZOLE, PHARMACEUTICAL FORMULATIONS COMPRISING IT AND USE THEREOF IN THE PREPARATION OF MEDICAMENTS FOR TREATING CANCERInfo
- Publication number
- IL168190A IL168190A IL168190A IL16819005A IL168190A IL 168190 A IL168190 A IL 168190A IL 168190 A IL168190 A IL 168190A IL 16819005 A IL16819005 A IL 16819005A IL 168190 A IL168190 A IL 168190A
- Authority
- IL
- Israel
- Prior art keywords
- tgf
- pyridin
- preparation
- pyrrolo
- dihydro
- Prior art date
Links
Classifications
-
- 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
-
- 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
- A61K31/415—1,2-Diazoles
- A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
-
- 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
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- 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
- 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
- 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
- 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
- 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
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Neurology (AREA)
- Epidemiology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Virology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Tropical Medicine & Parasitology (AREA)
- Urology & Nephrology (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Pulmonology (AREA)
- Dermatology (AREA)
- Pain & Pain Management (AREA)
- Oncology (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychiatry (AREA)
- Cardiology (AREA)
- Vascular Medicine (AREA)
- Ophthalmology & Optometry (AREA)
- AIDS & HIV (AREA)
- Hospice & Palliative Care (AREA)
- Molecular Biology (AREA)
- Communicable Diseases (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US42889302P | 2002-11-22 | 2002-11-22 | |
| PCT/US2003/032747 WO2004048382A1 (en) | 2002-11-22 | 2003-11-10 | Quinolinyl-pyrrolopyrazoles |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| IL168190A true IL168190A (en) | 2011-01-31 |
Family
ID=32393478
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL168190A IL168190A (en) | 2002-11-22 | 2005-04-21 | 2-(6- METHYL-PYRIDIN-2-YL)-3-(6-AMIDO-QUINOLIN-4-YL)-5,6-DIHYDRO- 4H-PYRROLO[1,2-b]PYRAZOLE, PHARMACEUTICAL FORMULATIONS COMPRISING IT AND USE THEREOF IN THE PREPARATION OF MEDICAMENTS FOR TREATING CANCER |
Country Status (28)
| Country | Link |
|---|---|
| US (2) | US7265225B2 (https=) |
| EP (1) | EP1565471B1 (https=) |
| JP (1) | JP4542906B2 (https=) |
| KR (1) | KR101057282B1 (https=) |
| CN (1) | CN100345852C (https=) |
| AT (1) | ATE341550T1 (https=) |
| AU (1) | AU2003291643B2 (https=) |
| BR (1) | BR0315337A (https=) |
| CA (1) | CA2501322C (https=) |
| CO (1) | CO5570677A2 (https=) |
| CR (1) | CR7830A (https=) |
| CY (1) | CY1106283T1 (https=) |
| DE (1) | DE60308893T2 (https=) |
| DK (1) | DK1565471T3 (https=) |
| EA (1) | EA008387B1 (https=) |
| EC (1) | ECSP055807A (https=) |
| EG (1) | EG25822A (https=) |
| ES (1) | ES2273046T3 (https=) |
| HR (1) | HRP20050436B1 (https=) |
| IL (1) | IL168190A (https=) |
| MX (1) | MXPA05005432A (https=) |
| NO (1) | NO331403B1 (https=) |
| NZ (1) | NZ538942A (https=) |
| PL (1) | PL227840B1 (https=) |
| PT (1) | PT1565471E (https=) |
| UA (1) | UA80571C2 (https=) |
| WO (1) | WO2004048382A1 (https=) |
| ZA (1) | ZA200503121B (https=) |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR039241A1 (es) | 2002-04-04 | 2005-02-16 | Biogen Inc | Heteroarilos trisustituidos y metodos para su produccion y uso de los mismos |
| AU2003290734A1 (en) * | 2002-11-27 | 2004-06-23 | Eli Lilly And Company | Novel compounds as pharmaceutical agents |
| EP1910370B1 (en) * | 2005-07-22 | 2015-04-22 | Eli Lilly And Company | A pyridin quinolin substituted pyrrolo [1,2-b] pyrazole monohydrate as tgf-beta inhibitor |
| WO2007039151A1 (en) * | 2005-09-28 | 2007-04-12 | Universität Zürich | Blockers of transforming growth factor beta and its receptors for the treatment of infectious diseases |
| DK2083863T3 (da) | 2006-10-03 | 2015-06-22 | Genzyme Corp | Antistoffer mod tgf-beta til anvendelse til behandling af spædbørn med risiko for udvikling af bronkopulmonal dysplasi |
| CN101528752A (zh) * | 2006-10-16 | 2009-09-09 | 辉瑞产品公司 | 治疗性吡唑基噻吩并吡啶 |
| KR20130124291A (ko) | 2010-07-02 | 2013-11-13 | 길리애드 사이언시즈, 인코포레이티드 | Ｈｉｖ 항바이러스 화합물로서의 2-퀴놀리닐-아세트산 유도체 |
| AP2013006706A0 (en) | 2010-07-02 | 2013-02-28 | Gilead Sciences Inc | Napht-2-ylacetic acid derivatives to treat AIDS |
| US8871744B2 (en) | 2010-07-21 | 2014-10-28 | B & G Partyers, LLC | Compounds and methods for selectively targeting tumor-associated mucins |
| BR112013027096A2 (pt) | 2011-04-21 | 2016-12-27 | Gilead Sciences Inc | compostos de benzotiazol e seu uso farmacêutico |
| US20140308275A1 (en) | 2011-07-27 | 2014-10-16 | Inserm (Institut National De La Sante Et De La Recherche Medicale | Methods for diagnosing and treating myhre syndrome |
| WO2013062544A1 (en) | 2011-10-26 | 2013-05-02 | Seattle Children's Research Institute | Cysteamine in the treatment of fibrotic disease |
| WO2013078286A1 (en) | 2011-11-22 | 2013-05-30 | Cornell University | Methods for stimulating hematopoietic recovery by inhibiting tgf beta signaling |
| WO2013103724A1 (en) | 2012-01-04 | 2013-07-11 | Gilead Sciences, Inc. | 2- (tert - butoxy) -2- (7 -methylquinolin- 6 - yl) acetic acid derivatives for treating aids |
| US9284323B2 (en) | 2012-01-04 | 2016-03-15 | Gilead Sciences, Inc. | Naphthalene acetic acid derivatives against HIV infection |
| ES2571479T3 (es) | 2012-04-20 | 2016-05-25 | Gilead Sciences Inc | Derivados del ácido benzotiazol-6-il acético y su uso para tratar una infección por VIH |
| PL3685855T3 (pl) | 2012-10-05 | 2024-04-08 | Kadmon Corporation, Llc | Ludzkie przeciwciała anty-vegfr-2/kdr |
| WO2014072517A1 (en) | 2012-11-12 | 2014-05-15 | Institució Catalana De Recerca I Estudis Avançats | Methods and kits for the prognosis of colorectal cancer |
| JO3336B1 (ar) | 2014-10-07 | 2019-03-13 | Lilly Co Eli | مركبات أمينو بيريديلوكسي بيرازول |
| TWI704151B (zh) | 2014-12-22 | 2020-09-11 | 美商美國禮來大藥廠 | Ｅｒｋ抑制劑 |
| HK1247861A1 (zh) | 2015-01-30 | 2018-10-05 | President And Fellows Of Harvard College | 用於癌症治疗的肿瘤周围和肿瘤内部材料 |
| ES2918924T3 (es) | 2015-04-01 | 2022-07-21 | Rigel Pharmaceuticals Inc | Inhibidores de TGF-beta |
| KR102738306B1 (ko) | 2015-12-15 | 2024-12-03 | 브리스톨-마이어스 스큅 컴퍼니 | Cxcr4 수용체 길항제 |
| CN109548403A (zh) * | 2016-07-07 | 2019-03-29 | 苏州科睿思制药有限公司 | Galunisertib的晶型及其制备方法和用途 |
| CN110582497B (zh) * | 2017-03-17 | 2022-03-11 | 杭州领业医药科技有限公司 | Galunisertib的晶型及其制备方法和药物组合物 |
| US10995083B2 (en) | 2017-03-21 | 2021-05-04 | Hangzhou Solipharma Co., Ltd. | Cocrystal of 2-(6-methyl-pyridine-2-yl)-3-yl-[6-amide-quinoline-4-yl]-5,6-dihydro-4H-pyrrole[1,2-b]pyrazole, preparation method therefor, and pharmaceutical composition |
| WO2019042383A1 (zh) * | 2017-08-31 | 2019-03-07 | 苏州科睿思制药有限公司 | Galunisertib的晶型及其制备方法和用途 |
| WO2019105082A1 (zh) * | 2017-11-30 | 2019-06-06 | 苏州科睿思制药有限公司 | Galunisertib的晶型及其制备方法和用途 |
| WO2019137027A1 (zh) * | 2018-01-12 | 2019-07-18 | 苏州科睿思制药有限公司 | Galunisertib的晶型及其制备方法和用途 |
| US12049475B2 (en) | 2018-07-23 | 2024-07-30 | Brise Pharmaceuticals Co., Ltd. | Bisphosphonate drug conjugates |
| CA3117838A1 (en) | 2018-12-27 | 2020-07-02 | Nexys Therapeutics, Inc. | (pyridin-2-yl)amine derivatives as tgf-beta r1 (alk5) inhibitors for the treatment of cancer |
| JP2022527972A (ja) | 2019-04-02 | 2022-06-07 | アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル | 前悪性病変を有する患者において癌を予測及び予防する方法 |
| WO2020248908A1 (zh) * | 2019-06-10 | 2020-12-17 | 中国科学院广州生物医药与健康研究院 | 一种双功能免疫调节剂及其在药学上可接受的盐、药物组合物 |
| AU2021205893A1 (en) | 2020-01-08 | 2022-06-23 | Synthis Therapeutics, Inc. | ALK5 inhibitor conjugates and uses thereof |
| US11801304B2 (en) | 2020-02-19 | 2023-10-31 | Nammi Therapeutics, Inc. | Formulated and/or co-formulated liposome compositions containing TFGB antagonist prodrugs useful in the treatment of cancer and methods thereof |
| CN121712526A (zh) | 2023-06-13 | 2026-03-20 | 辛瑟斯治疗股份有限公司 | 抗cd5抗体及其用途 |
| GB202309553D0 (en) | 2023-06-24 | 2023-08-09 | Ucl Business Ltd | Compostions and uses thereof |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5356897A (en) * | 1991-09-09 | 1994-10-18 | Fujisawa Pharmaceutical Co., Ltd. | 3-(heteroaryl)-pyrazololi[1,5-a]pyrimidines |
| DK1206474T3 (da) * | 1999-08-27 | 2004-10-04 | Abbott Lab | Sulfonylphenylpyrazolforbindelser anvendelige som cox-2-inhibitorer |
| EP1397364B1 (en) * | 2001-05-24 | 2007-07-25 | Eli Lilly And Company | Novel pyrrole derivatives as pharmaceutical agents |
| CA2506799A1 (en) | 2002-11-21 | 2004-06-10 | Eli Lilly And Company | Mixed lineage kinase modulators |
-
2003
- 2003-10-11 UA UAA200504767A patent/UA80571C2/uk unknown
- 2003-11-10 CN CNB2003801038400A patent/CN100345852C/zh not_active Expired - Fee Related
- 2003-11-10 AT AT03768531T patent/ATE341550T1/de active
- 2003-11-10 DK DK03768531T patent/DK1565471T3/da active
- 2003-11-10 WO PCT/US2003/032747 patent/WO2004048382A1/en not_active Ceased
- 2003-11-10 NZ NZ538942A patent/NZ538942A/en not_active IP Right Cessation
- 2003-11-10 EP EP03768531A patent/EP1565471B1/en not_active Expired - Lifetime
- 2003-11-10 BR BR0315337-1A patent/BR0315337A/pt not_active Application Discontinuation
- 2003-11-10 MX MXPA05005432A patent/MXPA05005432A/es active IP Right Grant
- 2003-11-10 JP JP2004555329A patent/JP4542906B2/ja not_active Expired - Fee Related
- 2003-11-10 AU AU2003291643A patent/AU2003291643B2/en not_active Ceased
- 2003-11-10 EA EA200500859A patent/EA008387B1/ru not_active IP Right Cessation
- 2003-11-10 KR KR1020057009199A patent/KR101057282B1/ko not_active Expired - Fee Related
- 2003-11-10 PT PT03768531T patent/PT1565471E/pt unknown
- 2003-11-10 HR HRP20050436AA patent/HRP20050436B1/hr not_active IP Right Cessation
- 2003-11-10 ES ES03768531T patent/ES2273046T3/es not_active Expired - Lifetime
- 2003-11-10 CA CA2501322A patent/CA2501322C/en not_active Expired - Fee Related
- 2003-11-10 DE DE60308893T patent/DE60308893T2/de not_active Expired - Lifetime
- 2003-11-10 PL PL376797A patent/PL227840B1/pl unknown
- 2003-11-10 US US10/531,237 patent/US7265225B2/en not_active Expired - Fee Related
-
2005
- 2005-04-18 ZA ZA200503121A patent/ZA200503121B/en unknown
- 2005-04-21 IL IL168190A patent/IL168190A/en active IP Right Grant
- 2005-05-06 CR CR7830A patent/CR7830A/es unknown
- 2005-05-18 CO CO05048136A patent/CO5570677A2/es active IP Right Grant
- 2005-05-18 EG EGNA2005000237 patent/EG25822A/xx active
- 2005-05-19 EC EC2005005807A patent/ECSP055807A/es unknown
- 2005-06-21 NO NO20053045A patent/NO331403B1/no not_active IP Right Cessation
-
2006
- 2006-12-08 CY CY20061101769T patent/CY1106283T1/el unknown
-
2007
- 2007-07-25 US US11/782,659 patent/US7834029B2/en not_active Expired - Fee Related
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| KB | Patent renewed |