JP5242391B2 - Ｔｇｆ−ベータ阻害剤としてのピリジンキノリン置換ピロロ［１，２−ｂ］ピラゾール一水和物 - Google Patents
Ｔｇｆ−ベータ阻害剤としてのピリジンキノリン置換ピロロ［１，２−ｂ］ピラゾール一水和物 Download PDFInfo
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- JP5242391B2 JP5242391B2 JP2008522796A JP2008522796A JP5242391B2 JP 5242391 B2 JP5242391 B2 JP 5242391B2 JP 2008522796 A JP2008522796 A JP 2008522796A JP 2008522796 A JP2008522796 A JP 2008522796A JP 5242391 B2 JP5242391 B2 JP 5242391B2
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- methyl
- pyridin
- quinolin
- ppm
- pyrrolo
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- 125000004549 quinolin-4-yl group Chemical group N1=CC=C(C2=CC=CC=C12)* 0.000 description 1
- 238000011084 recovery Methods 0.000 description 1
- 238000001953 recrystallisation Methods 0.000 description 1
- 238000012552 review Methods 0.000 description 1
- 230000019491 signal transduction Effects 0.000 description 1
- 239000000741 silica gel Substances 0.000 description 1
- 229910002027 silica gel Inorganic materials 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 201000003120 testicular cancer Diseases 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- UGNWTBMOAKPKBL-UHFFFAOYSA-N tetrachloro-1,4-benzoquinone Chemical compound ClC1=C(Cl)C(=O)C(Cl)=C(Cl)C1=O UGNWTBMOAKPKBL-UHFFFAOYSA-N 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 230000023750 transforming growth factor beta production Effects 0.000 description 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 description 1
- 238000001622 two pulse phase modulation pulse sequence Methods 0.000 description 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US70164105P | 2005-07-22 | 2005-07-22 | |
| US60/701,641 | 2005-07-22 | ||
| PCT/US2006/025377 WO2007018818A1 (en) | 2005-07-22 | 2006-06-29 | A pyridin quinolin substituted pyrrolo [1,2-b] pyrazole monohydrate as tgf-beta inhibitor |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2009502780A JP2009502780A (ja) | 2009-01-29 |
| JP2009502780A5 JP2009502780A5 (https=) | 2009-08-20 |
| JP5242391B2 true JP5242391B2 (ja) | 2013-07-24 |
Family
ID=37450942
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008522796A Expired - Fee Related JP5242391B2 (ja) | 2005-07-22 | 2006-06-29 | Ｔｇｆ−ベータ阻害剤としてのピリジンキノリン置換ピロロ［１，２−ｂ］ピラゾール一水和物 |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US7872020B2 (https=) |
| EP (1) | EP1910370B1 (https=) |
| JP (1) | JP5242391B2 (https=) |
| BR (1) | BRPI0613639A2 (https=) |
| CA (1) | CA2616196C (https=) |
| DK (1) | DK1910370T3 (https=) |
| ES (1) | ES2542425T3 (https=) |
| HR (1) | HRP20150474T1 (https=) |
| HU (1) | HUE025209T2 (https=) |
| IL (1) | IL188181A (https=) |
| MX (1) | MX2008001020A (https=) |
| PL (1) | PL1910370T3 (https=) |
| PT (1) | PT1910370E (https=) |
| RS (1) | RS53999B1 (https=) |
| SI (1) | SI1910370T1 (https=) |
| WO (1) | WO2007018818A1 (https=) |
Families Citing this family (43)
| Publication number | Priority date | Publication date | Assignee | Title |
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| AR081810A1 (es) | 2010-04-07 | 2012-10-24 | Bayer Cropscience Ag | Piridinilpirazoles biciclicos |
| AU2012281281B2 (en) * | 2011-07-13 | 2017-06-01 | Tiumbio Co., Ltd | 2-pyridyl substituted imidazoles as ALK5 and/or ALK4 inhibitors |
| ES2791627T3 (es) | 2012-11-12 | 2020-11-05 | Inst Catalana Recerca Estudis Avancats | Métodos y kits para el pronóstico del cáncer colorrectal |
| PL2970890T3 (pl) | 2013-03-14 | 2020-11-16 | The Brigham And Women's Hospital, Inc. | Kompozycje i sposoby ekspansji i hodowli nabłonkowych komórek macierzystych |
| EP3189134A1 (en) | 2014-09-03 | 2017-07-12 | The Brigham and Women's Hospital, Inc. | Compositions, systems, and methods for generating inner ear hair cells for treatment of hearing loss |
| 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 |
| US10669528B2 (en) | 2015-06-25 | 2020-06-02 | Children's Medical Center Corporation | Methods and compositions relating to hematopoietic stem cell expansion, enrichment, and maintenance |
| 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 |
| US11021687B2 (en) | 2016-01-08 | 2021-06-01 | The Brigham And Women's Hospital, Inc. | Production of differentiated enteroendocrine cells and insulin producing cells |
| US11260130B2 (en) | 2016-03-02 | 2022-03-01 | Frequency Therapeutics, Inc. | Solubilized compositions for controlled proliferation of stem cells / generating inner ear hair cells using a GSK3 inhibitor: IV |
| US10213511B2 (en) | 2016-03-02 | 2019-02-26 | Frequency Therapeutics, Inc. | Thermoreversible compositions for administration of therapeutic agents |
| US10201540B2 (en) | 2016-03-02 | 2019-02-12 | Frequency Therapeutics, Inc. | Solubilized compositions for controlled proliferation of stem cells / generating inner ear hair cells using GSK3 inhibitors: I |
| EP4049665B1 (en) | 2016-03-15 | 2025-03-12 | The Children's Medical Center Corporation | Methods and compositions relating to hematopoietic stem cell expansion |
| US10604528B2 (en) | 2016-07-07 | 2020-03-31 | Crystal Pharmaceutical (Suzhou) Co., Ltd. | Galunisertib crystalline form, preparation method thereof and use thereof |
| 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 |
| EP3562827A1 (en) | 2016-12-30 | 2019-11-06 | Frequency Therapeutics, Inc. | 1h-pyrrole-2,5-dione compounds and methods of using them to induce self-renewal of stem/progenitor supporting cells |
| 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 |
| CN112135613A (zh) | 2018-03-20 | 2020-12-25 | 西奈山伊坎医学院 | 激酶抑制剂化合物和组合物及使用方法 |
| US20210254006A1 (en) | 2018-06-06 | 2021-08-19 | Ideaya Biosciences, Inc. | Methods of culturing and/or expanding stem cells and/or lineage committed progenitor cells using lactam compounds |
| JP2021533788A (ja) | 2018-08-17 | 2021-12-09 | フリークエンシー セラピューティクス インコーポレイテッド | Ｊａｇ−１を上方制御することにより有毛細胞を生成するための組成物及び方法 |
| US11617745B2 (en) | 2018-08-17 | 2023-04-04 | Frequency Therapeutics, Inc. | Compositions and methods for generating hair cells by downregulating FOXO |
| WO2020142485A1 (en) | 2018-12-31 | 2020-07-09 | Icahn School Of Medicine At Mount Sinai | Kinase inhibitor compounds and compositions and methods of use |
| CN115282280A (zh) * | 2022-08-12 | 2022-11-04 | 中国科学技术大学 | TGF-β1信号抑制剂的新用途 |
| TW202508595A (zh) | 2023-05-04 | 2025-03-01 | 美商銳新醫藥公司 | 用於ｒａｓ相關疾病或病症之組合療法 |
| GB202309553D0 (en) | 2023-06-24 | 2023-08-09 | Ucl Business Ltd | Compostions and uses thereof |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| TW202547461A (zh) | 2024-05-17 | 2025-12-16 | 美商銳新醫藥公司 | Ｒａｓ抑制劑 |
| WO2025255438A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
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| 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 |
| UA80571C2 (en) * | 2002-11-22 | 2007-10-10 | Lilly Co Eli | Quinolinyl-pyrrolopyrazoles |
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- 2006-06-29 BR BRPI0613639-7A patent/BRPI0613639A2/pt not_active Application Discontinuation
- 2006-06-29 SI SI200631924T patent/SI1910370T1/sl unknown
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- 2006-06-29 MX MX2008001020A patent/MX2008001020A/es active IP Right Grant
- 2006-06-29 HR HRP20150474TT patent/HRP20150474T1/hr unknown
- 2006-06-29 ES ES06774280.9T patent/ES2542425T3/es active Active
- 2006-06-29 JP JP2008522796A patent/JP5242391B2/ja not_active Expired - Fee Related
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- 2006-06-29 RS RS20150319A patent/RS53999B1/sr unknown
- 2006-06-29 DK DK06774280.9T patent/DK1910370T3/en active
- 2006-06-29 PL PL06774280T patent/PL1910370T3/pl unknown
- 2006-06-29 HU HUE06774280A patent/HUE025209T2/en unknown
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2007
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Also Published As
| Publication number | Publication date |
|---|---|
| US20100120854A1 (en) | 2010-05-13 |
| HUE025209T2 (en) | 2016-03-29 |
| EP1910370B1 (en) | 2015-04-22 |
| JP2009502780A (ja) | 2009-01-29 |
| BRPI0613639A2 (pt) | 2012-02-22 |
| IL188181A0 (en) | 2008-03-20 |
| WO2007018818A1 (en) | 2007-02-15 |
| PT1910370E (pt) | 2015-06-30 |
| CA2616196A1 (en) | 2007-02-15 |
| EP1910370A1 (en) | 2008-04-16 |
| HRP20150474T1 (xx) | 2015-06-05 |
| CA2616196C (en) | 2012-08-21 |
| SI1910370T1 (sl) | 2015-06-30 |
| RS53999B1 (sr) | 2015-10-30 |
| PL1910370T3 (pl) | 2015-09-30 |
| US7872020B2 (en) | 2011-01-18 |
| MX2008001020A (es) | 2008-03-25 |
| DK1910370T3 (en) | 2015-06-08 |
| ES2542425T3 (es) | 2015-08-05 |
| IL188181A (en) | 2014-05-28 |
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