JP2016537396A5 - - Google Patents
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- Publication number
- JP2016537396A5 JP2016537396A5 JP2016533631A JP2016533631A JP2016537396A5 JP 2016537396 A5 JP2016537396 A5 JP 2016537396A5 JP 2016533631 A JP2016533631 A JP 2016533631A JP 2016533631 A JP2016533631 A JP 2016533631A JP 2016537396 A5 JP2016537396 A5 JP 2016537396A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- hydrogen
- cycloalkyl
- cycloalkylalkyl
- haloalkyl
- 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
- 125000000217 alkyl group Chemical group 0.000 claims description 38
- 150000001875 compounds Chemical class 0.000 claims description 37
- 229910052739 hydrogen Inorganic materials 0.000 claims description 36
- 239000001257 hydrogen Substances 0.000 claims description 36
- -1 cyano, amino Chemical group 0.000 claims description 33
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims description 33
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 32
- 125000000623 heterocyclic group Chemical group 0.000 claims description 30
- 125000001188 haloalkyl group Chemical group 0.000 claims description 29
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 25
- 150000002431 hydrogen Chemical class 0.000 claims description 25
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 23
- 125000001072 heteroaryl group Chemical group 0.000 claims description 22
- 125000003342 alkenyl group Chemical group 0.000 claims description 16
- 125000003545 alkoxy group Chemical group 0.000 claims description 16
- 125000000304 alkynyl group Chemical group 0.000 claims description 16
- 125000003118 aryl group Chemical group 0.000 claims description 15
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims description 15
- 125000005843 halogen group Chemical group 0.000 claims description 14
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 13
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims description 12
- 125000005842 heteroatom Chemical group 0.000 claims description 9
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 9
- 125000000278 alkyl amino alkyl group Chemical group 0.000 claims description 8
- 125000002947 alkylene group Chemical group 0.000 claims description 8
- 125000004475 heteroaralkyl group Chemical group 0.000 claims description 8
- 239000008194 pharmaceutical composition Substances 0.000 claims description 8
- 201000010099 disease Diseases 0.000 claims description 7
- 229910052757 nitrogen Inorganic materials 0.000 claims description 7
- 229910052760 oxygen Inorganic materials 0.000 claims description 7
- 229910052717 sulfur Inorganic materials 0.000 claims description 7
- 230000000694 effects Effects 0.000 claims description 6
- 208000011580 syndromic disease Diseases 0.000 claims description 6
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims description 5
- 125000001424 substituent group Chemical group 0.000 claims description 5
- 102000001253 Protein Kinase Human genes 0.000 claims description 4
- 239000000651 prodrug Substances 0.000 claims description 4
- 229940002612 prodrug Drugs 0.000 claims description 4
- 108060006633 protein kinase Proteins 0.000 claims description 4
- 150000003839 salts Chemical class 0.000 claims description 4
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims description 3
- 230000001105 regulatory effect Effects 0.000 claims description 3
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims description 2
- 125000004432 carbon atom Chemical group C* 0.000 claims description 2
- 229920006395 saturated elastomer Polymers 0.000 claims description 2
- 108091000080 Phosphotransferase Proteins 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 102000020233 phosphotransferase Human genes 0.000 claims 2
- 238000000034 method Methods 0.000 description 4
- 239000000203 mixture Substances 0.000 description 2
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361906779P | 2013-11-20 | 2013-11-20 | |
| US61/906,779 | 2013-11-20 | ||
| PCT/US2014/066467 WO2015077375A1 (en) | 2013-11-20 | 2014-11-19 | Quinazoline derivatives as tam family kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016537396A JP2016537396A (ja) | 2016-12-01 |
| JP2016537396A5 true JP2016537396A5 (https=) | 2017-12-28 |
| JP6527513B2 JP6527513B2 (ja) | 2019-06-05 |
Family
ID=53180111
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016533631A Active JP6527513B2 (ja) | 2013-11-20 | 2014-11-19 | Ｔａｍファミリーキナーゼ阻害剤としてのキナゾリン誘導体 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US9771333B2 (https=) |
| EP (1) | EP3071204B1 (https=) |
| JP (1) | JP6527513B2 (https=) |
| CN (1) | CN105916506B (https=) |
| AU (1) | AU2014353006B2 (https=) |
| CA (1) | CA2929188C (https=) |
| WO (1) | WO2015077375A1 (https=) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20180086187A (ko) | 2015-10-05 | 2018-07-30 | 더 트러스티이스 오브 콜롬비아 유니버시티 인 더 시티 오브 뉴욕 | 자가포식 유동의 활성체 및 포스포리파제 d 및 타우를 포함하는 단백질 응집물의 클리어런스 및 단백질질환의 치료 |
| CA3088788A1 (en) | 2018-01-17 | 2019-07-25 | Vertex Pharmaceuticals Incorporated | Dna-pk inhibitors |
| JP7483612B2 (ja) | 2018-01-17 | 2024-05-15 | バーテックス ファーマシューティカルズ インコーポレイテッド | ゲノム編集効率を増加するためのキノキサリノン化合物、組成物、方法、およびキット |
| MA51619A (fr) | 2018-01-17 | 2021-04-14 | Vertex Pharma | Inhibiteurs de la protéine kinase dépendante de l'adn |
| CN111269125A (zh) * | 2018-12-05 | 2020-06-12 | 上海复星星泰医药科技有限公司 | 一种艾乐替尼中间体及其制备方法 |
| CN114380770B (zh) * | 2021-12-24 | 2022-12-09 | 山东艾孚特科技有限公司 | 利用固体超强酸催化的甲基巯基噻二唑的合成工艺 |
Family Cites Families (50)
| Publication number | Priority date | Publication date | Assignee | Title |
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| US3971783A (en) * | 1973-03-07 | 1976-07-27 | Pfizer Inc. | 4-Aminoquinazoline derivatives as cardiac stimulants |
| US5721237A (en) * | 1991-05-10 | 1998-02-24 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Protein tyrosine kinase aryl and heteroaryl quinazoline compounds having selective inhibition of HER-2 autophosphorylation properties |
| US5710158A (en) | 1991-05-10 | 1998-01-20 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Aryl and heteroaryl quinazoline compounds which inhibit EGF and/or PDGF receptor tyrosine kinase |
| KR100860295B1 (ko) | 1998-10-08 | 2008-09-25 | 아스트라제네카 아베 | 퀴나졸린 유도체 |
| UA73993C2 (uk) | 2000-06-06 | 2005-10-17 | Астразенека Аб | Хіназолінові похідні для лікування пухлин та фармацевтична композиція |
| GB0126433D0 (en) * | 2001-11-03 | 2002-01-02 | Astrazeneca Ab | Compounds |
| JP2005515176A (ja) | 2001-11-03 | 2005-05-26 | アストラゼネカ アクチボラグ | 抗腫瘍剤としてのキナゾリン誘導体 |
| GB0128108D0 (en) | 2001-11-23 | 2002-01-16 | Astrazeneca Ab | Therapeutic use |
| AU2002361846A1 (en) | 2001-12-21 | 2003-07-15 | Bayer Pharmaceuticals Corporation | Quinazoline and quinoline derivative compounds as inhibitors of prolylpeptidase, inducers of apoptosis and cancer treatment agents |
| DE60234125D1 (de) | 2001-12-24 | 2009-12-03 | Astrazeneca Ab | E inhibitoren |
| EP1501829B1 (en) | 2002-05-06 | 2010-11-24 | Vertex Pharmaceuticals Incorporated | Thiadiazoles or oxadiazoles and their use as inhibitors of jak protein kinase |
| ATE457308T1 (de) | 2003-04-21 | 2010-02-15 | Lilly Co Eli | Substituierte benzopyrane als selektive antagonisten am östrogenrezeptor-beta |
| JP2008515961A (ja) | 2004-10-12 | 2008-05-15 | アストラゼネカ アクチボラグ | 癌に対する使用のためのキナゾリン誘導体 |
| GB0427917D0 (en) | 2004-12-21 | 2005-01-26 | Astrazeneca Ab | Chemical compounds |
| WO2006129064A1 (en) | 2005-05-28 | 2006-12-07 | Astrazeneca Ab | Quinazolines and their use as aurora kinase inhibitors |
| WO2007030680A2 (en) | 2005-09-07 | 2007-03-15 | Rigel Pharmaceuticals, Inc. | Triazole derivatives useful as axl inhibitors |
| GB0601215D0 (en) | 2006-01-21 | 2006-03-01 | Astrazeneca Ab | Chemical compounds |
| NZ546477A (en) | 2006-04-07 | 2009-04-30 | Auckland Uniservices Ltd | 4-Alkylamino-2-(heterocyclic)quinazolines and their use in cancer therapy |
| WO2008045978A1 (en) | 2006-10-10 | 2008-04-17 | Rigel Pharmaceuticals, Inc. | Pinane-substituted pyrimidinediamine derivatives useful as axl inhibitors |
| WO2008080134A2 (en) | 2006-12-22 | 2008-07-03 | Rigel Pharmaceuticals, Inc. | 4-amin0-2- (hetero) arylamino-5- (hetero) arylthiazoles useful as axl inhibitors |
| EP2078010B1 (en) | 2006-12-29 | 2014-01-29 | Rigel Pharmaceuticals, Inc. | Polycyclic heteroaryl substituted triazoles useful as axl inhibitors |
| WO2008083353A1 (en) | 2006-12-29 | 2008-07-10 | Rigel Pharmaceuticals, Inc. | Bicyclic aryl and bicyclic heteroaryl substituted triazoles useful as axl inhibitors |
| EP2114955B1 (en) | 2006-12-29 | 2013-02-13 | Rigel Pharmaceuticals, Inc. | Bridged bicyclic aryl and bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors |
| EP2079736B1 (en) | 2006-12-29 | 2017-10-18 | Rigel Pharmaceuticals, Inc. | Substituted triazoles useful as axl inhibitors |
| ES2672172T3 (es) | 2006-12-29 | 2018-06-12 | Rigel Pharmaceuticals, Inc. | Triazoles N3-heteroarilsustituidos y triazoles N5-heteroarilsustituidos útiles como inhibidores de Axl |
| WO2008092231A1 (en) * | 2007-02-01 | 2008-08-07 | Resverlogix Corp. | Compounds for the prevention and treatment of cardiovascular diseases |
| EP2139869A2 (en) | 2007-04-13 | 2010-01-06 | SuperGen, Inc. | Axl kinase inhibitors useful for the treatment of cancer or hyperproliferative disorders |
| GB0713259D0 (en) | 2007-07-09 | 2007-08-15 | Astrazeneca Ab | Pyrazine derivatives 954 |
| WO2009024825A1 (en) | 2007-08-21 | 2009-02-26 | Astrazeneca Ab | 2-pyrazinylbenzimidazole derivatives as receptor tyrosine kinase inhibitors |
| GB0719803D0 (en) | 2007-10-10 | 2007-11-21 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
| ATE523508T1 (de) | 2007-10-25 | 2011-09-15 | Astrazeneca Ab | Für die behandlung von zellproliferativen erkrankungen geeignete pyridin- und pyrazinderivate |
| WO2009054864A1 (en) | 2007-10-26 | 2009-04-30 | Rigel Pharmaceuticals, Inc. | Polycyclic aryl substituted triazoles and polycyclic heteroaryl substituted triazoles useful as axl inhibitors |
| MX2010007852A (es) | 2008-01-18 | 2010-11-30 | Natco Pharma Ltd | Derivados de 6,7-dialcoxi-quinazolina utiles para el tratamiento de trastornos relacionados con cancer. |
| SI2947072T1 (sl) * | 2008-03-17 | 2017-03-31 | Ambit Biosciences Corporation | 1-(3-(6,7-dimetoksikinazolin-4-iloksi)fenil)-3-(5-1,1,1-trifluoro-2- metilpropan-2-il)izoksazol-3-il)urea kot modulator raf kinaze pri zdravljenju rakavih bolezni |
| EP2262772B8 (en) | 2008-04-16 | 2013-03-13 | Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. | Quinoline derivatives as axl kinase inhibitors |
| CA2730231C (en) | 2008-07-09 | 2016-10-18 | Rigel Pharmaceuticals, Inc. | Polycyclic heteroaryl substituted triazoles useful as axl inhibitors |
| US8431594B2 (en) | 2008-07-09 | 2013-04-30 | Rigel Pharmaceuticals, Inc. | Bridged bicyclic heteroaryl substituted triazoles useful as AXL inhibitors |
| SG172997A1 (en) | 2009-01-16 | 2011-08-29 | Rigel Pharmaceuticals Inc | Axl inhibitors for use in combination therapy for preventing, treating or managing metastatic cancer |
| US20100204221A1 (en) | 2009-02-09 | 2010-08-12 | Hariprasad Vankayalapati | Pyrrolopyrimidinyl axl kinase inhibitors |
| NZ596546A (en) | 2009-05-29 | 2012-12-21 | Syngenta Participations Ag | Substituted quinazolines as fungicides |
| EP2311809A1 (en) | 2009-10-16 | 2011-04-20 | Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. | Quinolinyloxyphenylsulfonamides |
| AU2010315361B2 (en) | 2009-11-03 | 2014-06-12 | Glaxosmithkline Llc | Quinazoline compounds |
| CN101747329A (zh) | 2009-12-31 | 2010-06-23 | 四川大学 | 一类4-芳硫基喹唑啉衍生物及制备方法和医药用途 |
| EP2566858A2 (en) | 2010-05-04 | 2013-03-13 | Pfizer Inc. | Heterocyclic derivatives as alk inhibitors |
| EP2423208A1 (en) | 2010-08-28 | 2012-02-29 | Lead Discovery Center GmbH | Pharmaceutically active compounds as Axl inhibitors |
| CN102382065B (zh) | 2010-08-30 | 2014-05-28 | 山东轩竹医药科技有限公司 | 苯胺取代的喹唑啉衍生物 |
| BR112013025387B1 (pt) | 2011-04-01 | 2021-07-27 | University Of Utah Research Foundation | Compostos análogos substituídos da n-fenilpirimidin-2-amina como inibidores da quinase axl, uso dos ditos compostos para o tratamento de um distúrbio de proliferação celular descontrolada, bem como kit compreendendo ditos compostos |
| EP2780338B1 (en) * | 2011-11-14 | 2016-11-09 | Ignyta, Inc. | Uracil derivatives as axl and c-met kinase inhibitors |
| RS55728B1 (sr) | 2012-01-31 | 2017-07-31 | Daiichi Sankyo Co Ltd | Derivat piridona |
| WO2013162061A1 (ja) | 2012-04-26 | 2013-10-31 | 第一三共株式会社 | 二環性ピリミジン化合物 |
-
2014
- 2014-11-19 JP JP2016533631A patent/JP6527513B2/ja active Active
- 2014-11-19 CN CN201480073218.8A patent/CN105916506B/zh active Active
- 2014-11-19 AU AU2014353006A patent/AU2014353006B2/en active Active
- 2014-11-19 EP EP14864125.1A patent/EP3071204B1/en active Active
- 2014-11-19 US US15/038,038 patent/US9771333B2/en active Active
- 2014-11-19 WO PCT/US2014/066467 patent/WO2015077375A1/en not_active Ceased
- 2014-11-19 CA CA2929188A patent/CA2929188C/en active Active
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