CN101622248B - 用作axl抑制剂的n3-杂芳基取代的三唑和n5-杂芳基取代的三唑 - Google Patents
用作axl抑制剂的n3-杂芳基取代的三唑和n5-杂芳基取代的三唑 Download PDFInfo
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- CN101622248B CN101622248B CN2007800489092A CN200780048909A CN101622248B CN 101622248 B CN101622248 B CN 101622248B CN 2007800489092 A CN2007800489092 A CN 2007800489092A CN 200780048909 A CN200780048909 A CN 200780048909A CN 101622248 B CN101622248 B CN 101622248B
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- Prior art keywords
- optionally substituted
- triazole
- diamines
- pyrimidine
- thiotolene
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- Expired - Fee Related
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- 0 *N(*)C(N1)NNC1N(*)* Chemical compound *N(*)C(N1)NNC1N(*)* 0.000 description 1
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- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
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- A—HUMAN NECESSITIES
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- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
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- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- 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
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- 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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- 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
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- 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
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- 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
- C07D405/02—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 two hetero rings
- C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
- C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
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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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- 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
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- 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
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Ophthalmology & Optometry (AREA)
- Reproductive Health (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Endocrinology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Gynecology & Obstetrics (AREA)
- Vascular Medicine (AREA)
- Dermatology (AREA)
- Immunology (AREA)
- Oncology (AREA)
- Pregnancy & Childbirth (AREA)
- Pain & Pain Management (AREA)
- Diabetes (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US88287506P | 2006-12-29 | 2006-12-29 | |
| US60/882,875 | 2006-12-29 | ||
| US97544307P | 2007-09-26 | 2007-09-26 | |
| US60/975,443 | 2007-09-26 | ||
| PCT/US2007/089153 WO2008083354A1 (en) | 2006-12-29 | 2007-12-28 | N3-heteroaryl substituted triazoles and n5-heteroaryl substituted triazoles useful as axl inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN101622248A CN101622248A (zh) | 2010-01-06 |
| CN101622248B true CN101622248B (zh) | 2013-04-17 |
Family
ID=39203174
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2007800489092A Expired - Fee Related CN101622248B (zh) | 2006-12-29 | 2007-12-28 | 用作axl抑制剂的n3-杂芳基取代的三唑和n5-杂芳基取代的三唑 |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US9650391B2 (OSRAM) |
| EP (2) | EP2074115B1 (OSRAM) |
| JP (2) | JP5567837B2 (OSRAM) |
| CN (1) | CN101622248B (OSRAM) |
| AU (1) | AU2007342005A1 (OSRAM) |
| CA (1) | CA2710046C (OSRAM) |
| ES (2) | ES2607065T3 (OSRAM) |
| WO (1) | WO2008083354A1 (OSRAM) |
Families Citing this family (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007030680A2 (en) * | 2005-09-07 | 2007-03-15 | Rigel Pharmaceuticals, Inc. | Triazole derivatives useful as axl inhibitors |
| EP2114954B1 (en) * | 2006-12-29 | 2013-02-13 | Rigel Pharmaceuticals, Inc. | Bicyclic aryl and bicyclic heteroaryl substituted triazoles useful as axl inhibitors |
| ME01832B (me) * | 2006-12-29 | 2014-12-20 | Rigel Pharmaceuticals Inc | Policiklični heteroaril supstituisani triazoli koji su korisni kao axl inhibitori |
| US8012965B2 (en) | 2006-12-29 | 2011-09-06 | Rigel Pharmaceuticals, Inc. | Bridged bicyclic aryl and bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors |
| US9650391B2 (en) * | 2006-12-29 | 2017-05-16 | Rigel Pharmaceuticals Inc. | N3-heteroaryl substituted triazoles and N5-heteroaryl substituted triazoles useful as Axl inhibitors |
| ES2656496T3 (es) | 2006-12-29 | 2018-02-27 | Rigel Pharmaceuticals, Inc. | Triazoles sustituidos útiles como inhibidores de AXL |
| EP2205592B1 (en) * | 2007-10-26 | 2013-05-08 | Rigel Pharmaceuticals, Inc. | Polycyclic aryl substituted triazoles and polycyclic heteroaryl substituted triazoles useful as axl inhibitors |
| MX2010008926A (es) | 2008-02-15 | 2011-02-23 | Rigel Pharmaceuticals Inc | Compuestos de pirimidin-2-amina y su uso como inhibidores de jak cinasas. |
| SI2328888T1 (sl) | 2008-07-09 | 2013-03-29 | Rigel Pharmaceuticals, Inc. | Premoščeni biciklični heteroaril substituirani triazoli, uporabni kot inhibitorji Axl |
| JP5592884B2 (ja) | 2008-07-09 | 2014-09-17 | ライジェル ファーマシューティカルズ, インコーポレイテッド | Axl阻害剤として有用な多環式ヘテロアリール置換トリアゾール |
| WO2010083465A1 (en) * | 2009-01-16 | 2010-07-22 | Rigel Pharmaceuticals, Inc. | Axl inhibitors for use in combination therapy for preventing, treating or managing metastatic cancer |
| NZ627586A (en) | 2012-01-31 | 2016-08-26 | Daiichi Sankyo Co Ltd | Pyridone derivatives |
| CA2879542A1 (en) | 2012-07-25 | 2014-01-30 | Salk Institute For Biological Studies | Regulating the interaction between tam ligands and lipid membranes with exposed phosphatidylserine |
| GB201213556D0 (en) | 2012-07-31 | 2012-09-12 | Luminectric Ltd | Cases for portable electronic devices |
| CA2929188C (en) | 2013-11-20 | 2022-08-09 | Signalchem Lifesciences Corp. | Quinazoline derivatives as tam family kinase inhibitors |
| US10233176B2 (en) | 2013-11-27 | 2019-03-19 | Signalchem Lifesciences Corporation | Aminopyridine derivatives as TAM family kinase inhibitors |
| TWI723572B (zh) | 2014-07-07 | 2021-04-01 | 日商第一三共股份有限公司 | 具有四氫吡喃基甲基之吡啶酮衍生物及其用途 |
| US9840503B2 (en) | 2015-05-11 | 2017-12-12 | Incyte Corporation | Heterocyclic compounds and uses thereof |
| GB201509338D0 (en) | 2015-05-29 | 2015-07-15 | Bergenbio As | Combination therapy |
| WO2017027717A1 (en) | 2015-08-12 | 2017-02-16 | Incyte Corporation | Bicyclic fused pyrimidine compounds as tam inhibitors |
| WO2017035366A1 (en) | 2015-08-26 | 2017-03-02 | Incyte Corporation | Pyrrolopyrimidine derivatives as tam inhibitors |
| US20190099413A1 (en) | 2016-02-26 | 2019-04-04 | Ono Pharmaceutical Co., Ltd. | Drug for cancer therapy characterized in that axl inhibitor and immune checkpoint inhibitor are administered in combination |
| EP3436461B1 (en) | 2016-03-28 | 2023-11-01 | Incyte Corporation | Pyrrolotriazine compounds as tam inhibitors |
| EP3673907A4 (en) | 2017-08-23 | 2020-08-19 | ONO Pharmaceutical Co., Ltd. | CANCER TREATMENT PHARMACEUTICAL INCLUDING AX1 INHIBITOR AS AN EFFECTIVE INGREDIENT |
| MY208007A (en) | 2017-09-27 | 2025-04-04 | Incyte Corp | Salts of pyrrolotriazine derivatives useful as tam inhibitors |
| JP7223998B2 (ja) | 2017-10-13 | 2023-02-17 | 小野薬品工業株式会社 | Axl阻害剤を有効成分として含む固形がん治療剤 |
| AR117600A1 (es) | 2018-06-29 | 2021-08-18 | Incyte Corp | Formulaciones de un inhibidor de axl / mer |
| KR20210142154A (ko) | 2019-03-21 | 2021-11-24 | 옹쎄오 | 암 치료를 위한 키나제 억제제와 조합된 dbait 분자 |
| GB201912059D0 (en) | 2019-08-22 | 2019-10-09 | Bergenbio As | Combaination therapy of a patient subgroup |
| CN114761006A (zh) | 2019-11-08 | 2022-07-15 | Inserm(法国国家健康医学研究院) | 对激酶抑制剂产生耐药性的癌症的治疗方法 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| EP4114401A1 (en) | 2020-03-06 | 2023-01-11 | Incyte Corporation | Combination therapy comprising axl/mer and pd-1/pd-l1 inhibitors |
| GB202004189D0 (en) | 2020-03-23 | 2020-05-06 | Bergenbio As | Combination therapy |
| EP4132652A1 (en) | 2020-04-08 | 2023-02-15 | BerGenBio ASA | Axl inhibitors for antiviral therapy |
| GB202006072D0 (en) | 2020-04-24 | 2020-06-10 | Bergenbio Asa | Method of selecting patients for treatment with cmbination therapy |
| GB202104037D0 (en) | 2021-03-23 | 2021-05-05 | Bergenbio Asa | Combination therapy |
| GB202209285D0 (en) | 2022-06-24 | 2022-08-10 | Bergenbio Asa | Dosage regimen for AXL inhibitor |
| AR129722A1 (es) | 2022-06-28 | 2024-09-18 | Arcus Biosciences Inc | Compuestos inhibidores de axl |
| WO2024051667A1 (zh) * | 2022-09-05 | 2024-03-14 | 南京正大天晴制药有限公司 | 具有axl抑制活性的取代三唑化合物 |
| WO2024218236A1 (en) * | 2023-04-18 | 2024-10-24 | Centre National De La Recherche Scientifique | 3,5-diaminotriazole derivatives and uses thereof for treating ocular diseases |
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|---|---|---|---|---|
| WO2004046120A2 (en) * | 2002-11-15 | 2004-06-03 | Vertex Pharmaceuticals Incorporated | Diaminotriazoles useful as inhibitors of protein kinases |
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| WO2007030680A2 (en) | 2005-09-07 | 2007-03-15 | Rigel Pharmaceuticals, Inc. | Triazole derivatives useful as axl inhibitors |
| WO2008045978A1 (en) | 2006-10-10 | 2008-04-17 | Rigel Pharmaceuticals, Inc. | Pinane-substituted pyrimidinediamine derivatives useful as axl inhibitors |
| US8012965B2 (en) | 2006-12-29 | 2011-09-06 | Rigel Pharmaceuticals, Inc. | Bridged bicyclic aryl and bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors |
| ES2656496T3 (es) | 2006-12-29 | 2018-02-27 | Rigel Pharmaceuticals, Inc. | Triazoles sustituidos útiles como inhibidores de AXL |
| ME01832B (me) * | 2006-12-29 | 2014-12-20 | Rigel Pharmaceuticals Inc | Policiklični heteroaril supstituisani triazoli koji su korisni kao axl inhibitori |
| US9650391B2 (en) | 2006-12-29 | 2017-05-16 | Rigel Pharmaceuticals Inc. | N3-heteroaryl substituted triazoles and N5-heteroaryl substituted triazoles useful as Axl inhibitors |
| EP2114954B1 (en) | 2006-12-29 | 2013-02-13 | Rigel Pharmaceuticals, Inc. | Bicyclic aryl and bicyclic heteroaryl substituted triazoles useful as axl inhibitors |
| MX2009010127A (es) * | 2007-03-22 | 2009-11-05 | Vertex Pharma | Compuestos utiles como inhibidores de janus cinasas. |
| JP2010529990A (ja) | 2007-06-15 | 2010-09-02 | アイアールエム・リミテッド・ライアビリティ・カンパニー | タンパク質キナーゼ阻害剤およびそれを使用するための方法 |
| EP2205592B1 (en) | 2007-10-26 | 2013-05-08 | Rigel Pharmaceuticals, Inc. | Polycyclic aryl substituted triazoles and polycyclic heteroaryl substituted triazoles useful as axl inhibitors |
| MX2010008926A (es) | 2008-02-15 | 2011-02-23 | Rigel Pharmaceuticals Inc | Compuestos de pirimidin-2-amina y su uso como inhibidores de jak cinasas. |
| JP5592884B2 (ja) | 2008-07-09 | 2014-09-17 | ライジェル ファーマシューティカルズ, インコーポレイテッド | Axl阻害剤として有用な多環式ヘテロアリール置換トリアゾール |
| SI2328888T1 (sl) | 2008-07-09 | 2013-03-29 | Rigel Pharmaceuticals, Inc. | Premoščeni biciklični heteroaril substituirani triazoli, uporabni kot inhibitorji Axl |
| WO2010083465A1 (en) | 2009-01-16 | 2010-07-22 | Rigel Pharmaceuticals, Inc. | Axl inhibitors for use in combination therapy for preventing, treating or managing metastatic cancer |
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2007
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- 2007-12-28 WO PCT/US2007/089153 patent/WO2008083354A1/en not_active Ceased
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| Publication number | Priority date | Publication date | Assignee | Title |
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| WO2004046120A2 (en) * | 2002-11-15 | 2004-06-03 | Vertex Pharmaceuticals Incorporated | Diaminotriazoles useful as inhibitors of protein kinases |
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| CA2710046C (en) | 2016-02-09 |
| HK1174631A1 (en) | 2013-06-14 |
| JP2010514809A (ja) | 2010-05-06 |
| WO2008083354A1 (en) | 2008-07-10 |
| CA2710046A1 (en) | 2008-07-10 |
| JP5890445B2 (ja) | 2016-03-22 |
| EP2484679A3 (en) | 2012-10-10 |
| ES2607065T3 (es) | 2017-03-29 |
| EP2074115B1 (en) | 2018-03-07 |
| EP2074115A1 (en) | 2009-07-01 |
| US8796259B2 (en) | 2014-08-05 |
| US20080182862A1 (en) | 2008-07-31 |
| ES2672172T3 (es) | 2018-06-12 |
| AU2007342005A1 (en) | 2008-07-10 |
| CN101622248A (zh) | 2010-01-06 |
| JP5567837B2 (ja) | 2014-08-06 |
| EP2484679A2 (en) | 2012-08-08 |
| US20130090330A1 (en) | 2013-04-11 |
| EP2484679B1 (en) | 2016-09-28 |
| JP2014111641A (ja) | 2014-06-19 |
| US9650391B2 (en) | 2017-05-16 |
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