JP2020505395A5 - - Google Patents
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- JP2020505395A5 JP2020505395A5 JP2019540035A JP2019540035A JP2020505395A5 JP 2020505395 A5 JP2020505395 A5 JP 2020505395A5 JP 2019540035 A JP2019540035 A JP 2019540035A JP 2019540035 A JP2019540035 A JP 2019540035A JP 2020505395 A5 JP2020505395 A5 JP 2020505395A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- prodrug
- pharmaceutically acceptable
- acceptable salt
- stereoisomer
- 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.)
- Pending
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- 150000001875 compounds Chemical class 0.000 claims description 67
- 239000000651 prodrug Substances 0.000 claims description 34
- 229940002612 prodrug Drugs 0.000 claims description 34
- 150000003839 salts Chemical class 0.000 claims description 34
- 238000000034 method Methods 0.000 claims description 21
- 102200124918 rs121913250 Human genes 0.000 claims description 20
- 125000000217 alkyl group Chemical group 0.000 claims description 18
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 18
- 239000008194 pharmaceutical composition Substances 0.000 claims description 17
- 125000005843 halogen group Chemical group 0.000 claims description 16
- 125000001072 heteroaryl group Chemical group 0.000 claims description 16
- 102100029974 GTPase HRas Human genes 0.000 claims description 14
- 102100030708 GTPase KRas Human genes 0.000 claims description 14
- 101000584633 Homo sapiens GTPase HRas Proteins 0.000 claims description 14
- 101000584612 Homo sapiens GTPase KRas Proteins 0.000 claims description 14
- 206010028980 Neoplasm Diseases 0.000 claims description 14
- 125000003118 aryl group Chemical group 0.000 claims description 14
- 125000004181 carboxyalkyl group Chemical group 0.000 claims description 14
- 125000004966 cyanoalkyl group Chemical group 0.000 claims description 14
- 125000000623 heterocyclic group Chemical group 0.000 claims description 14
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 14
- 201000011510 cancer Diseases 0.000 claims description 11
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims description 10
- 125000002837 carbocyclic group Chemical group 0.000 claims description 10
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 10
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims description 10
- -1 heterocyclylene Chemical group 0.000 claims description 10
- 230000035772 mutation Effects 0.000 claims description 10
- 125000004438 haloalkoxy group Chemical group 0.000 claims description 8
- 102200006538 rs121913530 Human genes 0.000 claims description 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 7
- 230000001404 mediated effect Effects 0.000 claims description 6
- 102200006614 rs104894229 Human genes 0.000 claims description 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 5
- 208000035475 disorder Diseases 0.000 claims description 5
- 206010009944 Colon cancer Diseases 0.000 claims description 4
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 4
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 4
- 102000008300 Mutant Proteins Human genes 0.000 claims description 4
- 108010021466 Mutant Proteins Proteins 0.000 claims description 4
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 4
- 125000002947 alkylene group Chemical group 0.000 claims description 4
- 201000005787 hematologic cancer Diseases 0.000 claims description 4
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims description 4
- 125000004404 heteroalkyl group Chemical group 0.000 claims description 4
- 201000005202 lung cancer Diseases 0.000 claims description 4
- 208000020816 lung neoplasm Diseases 0.000 claims description 4
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 4
- 201000002528 pancreatic cancer Diseases 0.000 claims description 4
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 4
- 208000015768 polyposis Diseases 0.000 claims description 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 4
- 235000018102 proteins Nutrition 0.000 claims description 4
- 102000004169 proteins and genes Human genes 0.000 claims description 4
- 108090000623 proteins and genes Proteins 0.000 claims description 4
- 125000001424 substituent group Chemical group 0.000 claims description 4
- 206010027476 Metastases Diseases 0.000 claims description 3
- 230000002401 inhibitory effect Effects 0.000 claims description 3
- 230000009401 metastasis Effects 0.000 claims description 3
- 229910052757 nitrogen Inorganic materials 0.000 claims description 3
- HYZJCKYKOHLVJF-UHFFFAOYSA-N 1H-benzimidazole Chemical compound C1=CC=C2NC=NC2=C1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 claims description 2
- 229910019142 PO4 Inorganic materials 0.000 claims description 2
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 2
- 125000004103 aminoalkyl group Chemical group 0.000 claims description 2
- MDFFNEOEWAXZRQ-UHFFFAOYSA-N aminyl Chemical group [NH2] MDFFNEOEWAXZRQ-UHFFFAOYSA-N 0.000 claims description 2
- QRUDEWIWKLJBPS-UHFFFAOYSA-N benzotriazole Chemical compound C1=CC=C2N[N][N]C2=C1 QRUDEWIWKLJBPS-UHFFFAOYSA-N 0.000 claims description 2
- 239000012964 benzotriazole Substances 0.000 claims description 2
- ZADPBFCGQRWHPN-UHFFFAOYSA-N boronic acid Chemical compound OBO ZADPBFCGQRWHPN-UHFFFAOYSA-N 0.000 claims description 2
- 125000000151 cysteine group Chemical group N[C@@H](CS)C(=O)* 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 230000000694 effects Effects 0.000 claims description 2
- 125000001153 fluoro group Chemical group F* 0.000 claims description 2
- 125000004474 heteroalkylene group Chemical group 0.000 claims description 2
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims description 2
- 125000001041 indolyl group Chemical group 0.000 claims description 2
- 238000002347 injection Methods 0.000 claims description 2
- 239000007924 injection Substances 0.000 claims description 2
- 125000005647 linker group Chemical group 0.000 claims description 2
- 125000001624 naphthyl group Chemical group 0.000 claims description 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims description 2
- 239000010452 phosphate Substances 0.000 claims description 2
- 230000035755 proliferation Effects 0.000 claims description 2
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims description 2
- 230000000155 isotopic effect Effects 0.000 claims 14
- 239000000203 mixture Substances 0.000 claims 6
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 1
- 229910017464 nitrogen compound Inorganic materials 0.000 claims 1
- 150000002830 nitrogen compounds Chemical class 0.000 claims 1
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- 125000001188 haloalkyl group Chemical group 0.000 description 7
- 125000003545 alkoxy group Chemical group 0.000 description 6
- 125000000304 alkynyl group Chemical group 0.000 description 5
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| JP2000507975A (ja) | 1997-02-07 | 2000-06-27 | ファイザー・インク | Ｎ−ヒドロキシ−β−スルホニルプロピオンアミド誘導体類及びそれらのマトリックスメタロプロテイナーゼ阻害薬としての使用 |
| IL131123A0 (en) | 1997-02-11 | 2001-01-28 | Pfizer | Arylsulfonyl hydroxamic acid derivatives |
| GB9725782D0 (en) | 1997-12-05 | 1998-02-04 | Pfizer Ltd | Therapeutic agents |
| GB9801690D0 (en) | 1998-01-27 | 1998-03-25 | Pfizer Ltd | Therapeutic agents |
| PA8469501A1 (es) | 1998-04-10 | 2000-09-29 | Pfizer Prod Inc | Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico |
| PA8469401A1 (es) | 1998-04-10 | 2000-05-24 | Pfizer Prod Inc | Derivados biciclicos del acido hidroxamico |
| JP2004250329A (ja) * | 2002-12-26 | 2004-09-09 | Dainippon Pharmaceut Co Ltd | イサチン誘導体 |
| GB0405628D0 (en) * | 2004-03-12 | 2004-04-21 | Glaxo Group Ltd | Novel compounds |
| KR101256018B1 (ko) * | 2009-08-20 | 2013-04-18 | 한국과학기술연구원 | 단백질 키나아제 저해활성을 갖는 1,3,6-치환된 인돌 화합물 |
| CA2916298C (en) * | 2013-06-26 | 2021-10-12 | Abbvie Inc. | Primary carboxamides as btk inhibitors |
| RU2718876C2 (ru) * | 2013-08-23 | 2020-04-15 | Ньюфарма, Инк. | Некоторые химические соединения, композиции и способы |
| CN106488910B (zh) * | 2013-10-10 | 2020-07-31 | 亚瑞克西斯制药公司 | Kras g12c的抑制剂 |
| TWI659021B (zh) * | 2013-10-10 | 2019-05-11 | 亞瑞克西斯製藥公司 | Ｋｒａｓ ｇ１２ｃ之抑制劑 |
| CA2981677A1 (en) * | 2015-04-03 | 2016-10-06 | Nantbioscience, Inc. | Compositions and methods of targeting mutant k-ras |
| CN105348271A (zh) * | 2015-12-23 | 2016-02-24 | 常州润诺生物科技有限公司 | 喹唑啉类衍生物药用用途及其制备方法 |
| CN105399734A (zh) * | 2015-12-23 | 2016-03-16 | 吉林省长源药业有限公司 | 新型egfr抑制剂及其制备方法 |
| CN105924840A (zh) * | 2016-06-01 | 2016-09-07 | 扬州兰都塑料科技有限公司 | 一种阻燃电力电缆 |
| CN106084164A (zh) * | 2016-06-12 | 2016-11-09 | 四川大学 | 一种结构抗菌型聚氨酯用扩链剂的制备方法 |
-
2018
- 2018-01-25 US US16/480,849 patent/US20200385364A1/en not_active Abandoned
- 2018-01-25 CN CN201880008592.8A patent/CN110382483A/zh active Pending
- 2018-01-25 JP JP2019540035A patent/JP2020505395A/ja active Pending
- 2018-01-25 EP EP18704371.6A patent/EP3573966A1/en not_active Withdrawn
- 2018-01-25 WO PCT/US2018/015227 patent/WO2018140598A1/en not_active Ceased
-
2022
- 2022-06-13 US US17/839,232 patent/US20230147053A1/en active Pending
-
2023
- 2023-01-23 JP JP2023008128A patent/JP2023041763A/ja active Pending
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