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 (enExample) | 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 (enExample) |
| EP (1) | EP3071204B1 (enExample) |
| JP (1) | JP6527513B2 (enExample) |
| CN (1) | CN105916506B (enExample) |
| AU (1) | AU2014353006B2 (enExample) |
| CA (1) | CA2929188C (enExample) |
| WO (1) | WO2015077375A1 (enExample) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112018006873A2 (pt) | 2015-10-05 | 2018-11-06 | The Trustees Of Columbia University In The City Of New York | ativadores do fluxo autofágico e fosfolipase d e depuração de agregados de proteína incluindo tau e tratamento de proteinopatias |
| KR20200110687A (ko) | 2018-01-17 | 2020-09-24 | 버텍스 파마슈티칼스 인코포레이티드 | 유전체 편집 효율을 증가시키기 위한 퀴녹살리논 화합물, 조성물, 방법 및 키트 |
| ES2980444T3 (es) | 2018-01-17 | 2024-10-01 | Vertex Pharma | Inhibidores de ADN-PK |
| JP7466448B2 (ja) | 2018-01-17 | 2024-04-12 | 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 | Ｄｎａ－ｐｋ阻害剤 |
| 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 |
|---|---|---|---|---|
| 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 |
| DE69925141T2 (de) | 1998-10-08 | 2006-04-27 | Astrazeneca Ab | Chinazolin derivate |
| UA73993C2 (uk) | 2000-06-06 | 2005-10-17 | Астразенека Аб | Хіназолінові похідні для лікування пухлин та фармацевтична композиція |
| ATE423104T1 (de) * | 2001-11-03 | 2009-03-15 | Astrazeneca Ab | Quinazolin derivate als antitumor-mittel |
| GB0126433D0 (en) * | 2001-11-03 | 2002-01-02 | Astrazeneca Ab | Compounds |
| 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 |
| ES2333702T3 (es) | 2001-12-24 | 2010-02-26 | Astrazeneca Ab | Derivados de quinazolina sustituidos que actuan como unhibidores de cinasas aurora. |
| ATE489384T1 (de) | 2002-05-06 | 2010-12-15 | Vertex Pharma | Thiadiazole oder oxadiazole und ihre verwendung als jak proteinkinaseinhibitoren |
| WO2004094401A1 (en) | 2003-04-21 | 2004-11-04 | Eli Lilly And Company | Substituted benzopyrans as selective estrogen receptor-beta agonists |
| EP1802608A1 (en) | 2004-10-12 | 2007-07-04 | AstraZeneca AB | Quinazoline derivatives for use against cancer |
| 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 |
| US7884119B2 (en) | 2005-09-07 | 2011-02-08 | 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 |
| CA2710043C (en) | 2006-12-29 | 2016-02-09 | Rigel Pharmaceuticals, Inc. | Bicyclic aryl and bicyclic heteroaryl substituted triazoles useful as axl inhibitors |
| WO2008083367A2 (en) | 2006-12-29 | 2008-07-10 | Rigel Pharmaceuticals, Inc. | Polycyclic heteroaryl substituted triazoles useful as axl inhibitors |
| CA2710230C (en) | 2006-12-29 | 2016-02-23 | 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 |
| JP5567837B2 (ja) | 2006-12-29 | 2014-08-06 | 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インヒビターとして有用なＮ３−ヘテロアリール置換トリアゾールおよびＮ５−ヘテロアリール置換トリアゾール |
| KR101444489B1 (ko) * | 2007-02-01 | 2014-09-24 | 리스버로직스 코퍼레이션 | 심혈관 질환을 예방 및 치료하기 위한 화합물 |
| WO2008128072A2 (en) | 2007-04-13 | 2008-10-23 | 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 |
| JP2011500778A (ja) | 2007-10-25 | 2011-01-06 | アストラゼネカ・アクチエボラーグ | ピリジン及びピラジン誘導体−０８３ |
| WO2009054864A1 (en) | 2007-10-26 | 2009-04-30 | Rigel Pharmaceuticals, Inc. | Polycyclic aryl substituted triazoles and polycyclic heteroaryl substituted triazoles useful as axl inhibitors |
| DK3012251T3 (en) | 2008-01-18 | 2017-10-09 | Natco Pharma Ltd | PROCEDURE FOR PREPARATION 6,7-DIALCOXY-QUINAZOLINE DERIVATIVES |
| PT2947072T (pt) | 2008-03-17 | 2016-12-06 | Ambit Biosciences Corp | 1-(3-(6,7-dimetoxiquinazolin-4-iloxi)fenil)-3-(5-(1,1,1-trifluoro-2-metilpropan-2-il)isoxazol-3-il)ureia como modulador da cinase raf no tratamento de doenças oncológicas |
| WO2009127417A1 (en) | 2008-04-16 | 2009-10-22 | MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. | Quinoline derivatives as axl kinase inhibitors |
| WO2010005879A1 (en) | 2008-07-09 | 2010-01-14 | Rigel Pharmaceuticals, Inc. | Bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors |
| 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 |
| CN102281875B (zh) | 2009-01-16 | 2017-09-22 | 里格尔药品股份有限公司 | 预防、治疗或应对转移癌的使用axl抑制剂的组合疗法 |
| WO2010090764A1 (en) | 2009-02-09 | 2010-08-12 | Supergen, Inc. | Pyrrolopyrimidinyl axl kinase inhibitors |
| CA2762347A1 (en) | 2009-05-29 | 2010-12-02 | 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 |
| JP5836963B2 (ja) | 2009-11-03 | 2015-12-24 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニーＧｌａｘｏＳｍｉｔｈＫｌｉｎｅ ＬＬＣ | キナゾリン化合物 |
| 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 |
| WO2011138751A2 (en) | 2010-05-04 | 2011-11-10 | 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 |
| JP6118794B2 (ja) | 2011-04-01 | 2017-04-19 | ザ ユニバーシティ オブ ユタ リサーチ ファウンデイション | Ａｘｌキナーゼの阻害剤としての置換ｎ−フェニルピリミジン−２−アミン類似体 |
| EP3045453A1 (en) * | 2011-11-14 | 2016-07-20 | Cephalon, Inc. | Uracil derivatives as axl and c-met kinase inhibitors |
| DK2810937T3 (en) | 2012-01-31 | 2017-03-13 | Daiichi Sankyo Co Ltd | PYRIDONE DERIVATIVES |
| 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 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 JP JP2016533631A patent/JP6527513B2/ja active Active
- 2014-11-19 CN CN201480073218.8A patent/CN105916506B/zh active Active
- 2014-11-19 CA CA2929188A patent/CA2929188C/en active Active
- 2014-11-19 AU AU2014353006A patent/AU2014353006B2/en active Active
- 2014-11-19 EP EP14864125.1A patent/EP3071204B1/en active Active