CO5570677A2 - Quinolinilpirrolopirazoles - Google Patents
QuinolinilpirrolopirazolesInfo
- Publication number
- CO5570677A2 CO5570677A2 CO05048136A CO05048136A CO5570677A2 CO 5570677 A2 CO5570677 A2 CO 5570677A2 CO 05048136 A CO05048136 A CO 05048136A CO 05048136 A CO05048136 A CO 05048136A CO 5570677 A2 CO5570677 A2 CO 5570677A2
- Authority
- CO
- Colombia
- Prior art keywords
- pharmaceutically acceptable
- compound according
- prodrug
- ester
- acceptable salt
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 abstract 4
- 150000003839 salts Chemical class 0.000 abstract 4
- 150000002148 esters Chemical class 0.000 abstract 2
- 239000000651 prodrug Substances 0.000 abstract 2
- 229940002612 prodrug Drugs 0.000 abstract 2
- -1 6-methylpyridin-2-yl Chemical group 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 239000003085 diluting agent Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
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)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Neurology (AREA)
- Virology (AREA)
- Physical Education & Sports Medicine (AREA)
- Pulmonology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Tropical Medicine & Parasitology (AREA)
- Urology & Nephrology (AREA)
- Rheumatology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Oncology (AREA)
- Molecular Biology (AREA)
- Hospice & Palliative Care (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Vascular Medicine (AREA)
- Communicable Diseases (AREA)
- Ophthalmology & Optometry (AREA)
- Dermatology (AREA)
- AIDS & HIV (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US42889302P | 2002-11-22 | 2002-11-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO5570677A2 true CO5570677A2 (es) | 2005-10-31 |
Family
ID=32393478
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CO05048136A CO5570677A2 (es) | 2002-11-22 | 2005-05-18 | Quinolinilpirrolopirazoles |
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 |
| WO2004050659A1 (en) * | 2002-11-27 | 2004-06-17 | Eli Lilly And Company | Novel compounds as pharmaceutical agents |
| PT1910370E (pt) * | 2005-07-22 | 2015-06-30 | Lilly Co Eli | Um pirrolo[1,2-b]pirazole mono-hidratado substituído com piridina e quinolina como inibidor do tgf-beta |
| 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 |
| MX2009003518A (es) | 2006-10-03 | 2009-08-25 | Genzyme Corp | Uso de antagonistas de tgf-beta para tratar a los infantes en riesgo de desarrollar displasia brocopulmonar. |
| ES2559521T3 (es) * | 2006-10-16 | 2016-02-12 | Thesan Pharmaceuticals, Inc. | Pirazolil tienopiridinas terapéuticas |
| MX2012015097A (es) | 2010-07-02 | 2013-05-28 | Gilead Sciences Inc | Derivados de acido naft-2-ilacetico para tratar sida. |
| EP2588455B1 (en) | 2010-07-02 | 2018-04-04 | Gilead Sciences, Inc. | 2-quinolinyl-acetic acid derivatives as hiv antiviral compounds |
| US8871744B2 (en) | 2010-07-21 | 2014-10-28 | B & G Partyers, LLC | Compounds and methods for selectively targeting tumor-associated mucins |
| UA111841C2 (uk) | 2011-04-21 | 2016-06-24 | Гіліад Сайєнсіз, Інк. | Сполуки бензотіазолу та їх фармацевтичне застосування |
| 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 |
| AU2011379972B2 (en) | 2011-10-26 | 2016-05-12 | 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 |
| US9284323B2 (en) | 2012-01-04 | 2016-03-15 | Gilead Sciences, Inc. | Naphthalene acetic acid derivatives against HIV infection |
| US9376392B2 (en) | 2012-01-04 | 2016-06-28 | Gilead Sciences, Inc. | 2-(tert-butoxy)-2-(7-methylquinolin-6-yl) acetic acid derivatives for treating AIDS |
| UY34750A (es) | 2012-04-20 | 2013-11-29 | Gilead Sciences Inc | ?compuestos para el tratamiento del hiv, composiciones,métodos de preparación, intermediarios y métodos terapéuticos?. |
| EA039595B1 (ru) | 2012-10-05 | 2022-02-15 | Кадмон Корпорейшн, Ллк | Нуклеиновые кислоты, кодирующие человеческие анти-vegfr-2/kdr-антитела |
| ES2791627T3 (es) | 2012-11-12 | 2020-11-05 | Inst Catalana Recerca Estudis Avancats | Métodos y kits para el pronóstico del cáncer colorrectal |
| TWI582083B (zh) | 2014-10-07 | 2017-05-11 | 美國禮來大藥廠 | 胺基吡啶基氧基吡唑化合物 |
| TWI704151B (zh) | 2014-12-22 | 2020-09-11 | 美商美國禮來大藥廠 | Ｅｒｋ抑制劑 |
| US11786457B2 (en) | 2015-01-30 | 2023-10-17 | President And Fellows Of Harvard College | Peritumoral and intratumoral materials for cancer therapy |
| ES2918924T3 (es) | 2015-04-01 | 2022-07-21 | Rigel Pharmaceuticals Inc | Inhibidores de TGF-beta |
| JP6856648B2 (ja) | 2015-12-15 | 2021-04-07 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | Ｃｘｃｒ４受容体アンタゴニスト |
| US10604528B2 (en) | 2016-07-07 | 2020-03-31 | Crystal Pharmaceutical (Suzhou) Co., Ltd. | Galunisertib crystalline form, preparation method thereof and use thereof |
| 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 |
| WO2018170724A1 (zh) | 2017-03-21 | 2018-09-27 | 杭州领业医药科技有限公司 | 2-(6-甲基-吡啶-2-基)-3-基-[6-酰胺基-喹啉-4-基]-5,6-二氢-4H-吡咯并[1,2-b]吡唑的共晶，其制备方法和药物组合物 |
| 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 |
| WO2020019108A1 (en) | 2018-07-23 | 2020-01-30 | Guangzhou Othrotx Co., Ltd. | Bisphosphonate drug conjugates |
| AU2019417418B2 (en) | 2018-12-27 | 2025-02-27 | Nexys Therapeutics, Inc. | (pyridin-2-yl)amine derivatives as ΤGFβR1 (Alk5) inhibitors for the treatment of cancer |
| EP3947737A2 (en) | 2019-04-02 | 2022-02-09 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods of predicting and preventing cancer in patients having premalignant lesions |
| 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 |
| JP2023509760A (ja) | 2020-01-08 | 2023-03-09 | シンシス セラピューティクス，インコーポレイテッド | Ａｌｋ５阻害剤複合体およびその使用 |
| WO2021167703A1 (en) | 2020-02-19 | 2021-08-26 | Nammi Therapeutics, Inc. | Formulated and/or co-formulated liposome compositions containing tgfb 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 |
| JP2003508401A (ja) * | 1999-08-27 | 2003-03-04 | アボット・ラボラトリーズ | Ｃｏｘ−２阻害薬として有用なスルホニルフェニルピラゾール化合物 |
| SK287857B6 (sk) * | 2001-05-24 | 2012-01-04 | Eli Lilly And Company | Novel pyrrole derivatives as pharmaceutical agents |
| AU2003298611A1 (en) | 2002-11-21 | 2004-06-18 | Eli Lilly And Company | Mixed lineage kinase modulators |
-
2003
- 2003-10-11 UA UAA200504767A patent/UA80571C2/uk unknown
- 2003-11-10 EA EA200500859A patent/EA008387B1/ru not_active IP Right Cessation
- 2003-11-10 DK DK03768531T patent/DK1565471T3/da active
- 2003-11-10 NZ NZ538942A patent/NZ538942A/en not_active IP Right Cessation
- 2003-11-10 BR BR0315337-1A patent/BR0315337A/pt not_active Application Discontinuation
- 2003-11-10 JP JP2004555329A patent/JP4542906B2/ja not_active Expired - Fee Related
- 2003-11-10 ES ES03768531T patent/ES2273046T3/es not_active Expired - Lifetime
- 2003-11-10 KR KR1020057009199A patent/KR101057282B1/ko not_active Expired - Fee Related
- 2003-11-10 MX MXPA05005432A patent/MXPA05005432A/es active IP Right Grant
- 2003-11-10 AU AU2003291643A patent/AU2003291643B2/en not_active Ceased
- 2003-11-10 AT AT03768531T patent/ATE341550T1/de active
- 2003-11-10 PL PL376797A patent/PL227840B1/pl unknown
- 2003-11-10 HR HRP20050436AA patent/HRP20050436B1/hr not_active IP Right Cessation
- 2003-11-10 PT PT03768531T patent/PT1565471E/pt unknown
- 2003-11-10 CA CA2501322A patent/CA2501322C/en not_active Expired - Fee Related
- 2003-11-10 WO PCT/US2003/032747 patent/WO2004048382A1/en not_active Ceased
- 2003-11-10 US US10/531,237 patent/US7265225B2/en not_active Expired - Fee Related
- 2003-11-10 CN CNB2003801038400A patent/CN100345852C/zh not_active Expired - Fee Related
- 2003-11-10 EP EP03768531A patent/EP1565471B1/en not_active Expired - Lifetime
- 2003-11-10 DE DE60308893T patent/DE60308893T2/de not_active Expired - Lifetime
-
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 EG EGNA2005000237 patent/EG25822A/xx active
- 2005-05-18 CO CO05048136A patent/CO5570677A2/es active IP Right Grant
- 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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| MY144229A (en) | Pyridazine derivatives and their use as therapeutic agents |
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