JP2019529484A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2019529484A5 JP2019529484A5 JP2019516992A JP2019516992A JP2019529484A5 JP 2019529484 A5 JP2019529484 A5 JP 2019529484A5 JP 2019516992 A JP2019516992 A JP 2019516992A JP 2019516992 A JP2019516992 A JP 2019516992A JP 2019529484 A5 JP2019529484 A5 JP 2019529484A5
- Authority
- JP
- Japan
- Prior art keywords
- compound according
- alkyl
- compound
- cancer
- halo
- 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
Links
- 150000001875 compounds Chemical class 0.000 claims description 113
- 238000000034 method Methods 0.000 claims description 27
- 125000005843 halogen group Chemical group 0.000 claims description 26
- 125000000217 alkyl group Chemical group 0.000 claims description 25
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 25
- 239000008194 pharmaceutical composition Substances 0.000 claims description 24
- -1 C 1 -C 6 alkyl Chemical group 0.000 claims description 22
- 230000035772 mutation Effects 0.000 claims description 21
- 206010028980 Neoplasm Diseases 0.000 claims description 20
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 20
- 201000011510 cancer Diseases 0.000 claims description 18
- 102200006538 rs121913530 Human genes 0.000 claims description 16
- 125000001424 substituent group Chemical group 0.000 claims description 16
- 102100030708 GTPase KRas Human genes 0.000 claims description 15
- 101000584612 Homo sapiens GTPase KRas Proteins 0.000 claims description 15
- 125000002837 carbocyclic group Chemical group 0.000 claims description 14
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 14
- 102100029974 GTPase HRas Human genes 0.000 claims description 13
- 101000584633 Homo sapiens GTPase HRas Proteins 0.000 claims description 13
- 125000004181 carboxyalkyl group Chemical group 0.000 claims description 12
- 125000004966 cyanoalkyl group Chemical group 0.000 claims description 12
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 12
- 125000001153 fluoro group Chemical group F* 0.000 claims description 12
- 125000001072 heteroaryl group Chemical group 0.000 claims description 12
- 102200124918 rs121913250 Human genes 0.000 claims description 11
- 125000003118 aryl group Chemical group 0.000 claims description 10
- 125000000623 heterocyclic group Chemical group 0.000 claims description 10
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 10
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 10
- 102100039788 GTPase NRas Human genes 0.000 claims description 8
- 101000744505 Homo sapiens GTPase NRas Proteins 0.000 claims description 8
- 125000005097 aminocarbonylalkyl group Chemical group 0.000 claims description 8
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 8
- 102000008300 Mutant Proteins Human genes 0.000 claims description 7
- 108010021466 Mutant Proteins Proteins 0.000 claims description 7
- 125000006728 (C1-C6) alkynyl group Chemical group 0.000 claims description 6
- 206010009944 Colon cancer Diseases 0.000 claims description 6
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 6
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 6
- 125000000304 alkynyl group Chemical group 0.000 claims description 6
- 208000029742 colonic neoplasm Diseases 0.000 claims description 6
- 201000005787 hematologic cancer Diseases 0.000 claims description 6
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims description 6
- 201000005202 lung cancer Diseases 0.000 claims description 6
- 208000020816 lung neoplasm Diseases 0.000 claims description 6
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 6
- 230000001404 mediated effect Effects 0.000 claims description 6
- 201000002528 pancreatic cancer Diseases 0.000 claims description 6
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 6
- 208000015768 polyposis Diseases 0.000 claims description 6
- 125000002924 primary amino group Chemical group [H]N([H])* 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
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 4
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 4
- 230000002401 inhibitory effect Effects 0.000 claims description 4
- 239000000651 prodrug Substances 0.000 claims description 4
- 229940002612 prodrug Drugs 0.000 claims description 4
- 150000003839 salts Chemical class 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 3
- 230000005764 inhibitory process Effects 0.000 claims description 3
- 125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims description 2
- 206010027476 Metastases Diseases 0.000 claims description 2
- 229910019142 PO4 Inorganic materials 0.000 claims description 2
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims description 2
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 2
- 125000002947 alkylene group Chemical group 0.000 claims description 2
- MDFFNEOEWAXZRQ-UHFFFAOYSA-N aminyl Chemical group [NH2] MDFFNEOEWAXZRQ-UHFFFAOYSA-N 0.000 claims description 2
- ZADPBFCGQRWHPN-UHFFFAOYSA-N boronic acid Chemical group OBO ZADPBFCGQRWHPN-UHFFFAOYSA-N 0.000 claims description 2
- 125000005620 boronic acid group Chemical group 0.000 claims description 2
- 230000003833 cell viability Effects 0.000 claims description 2
- 125000000596 cyclohexenyl group Chemical group C1(=CCCCC1)* 0.000 claims description 2
- 125000002433 cyclopentenyl group Chemical group C1(=CCCC1)* 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
- 150000002148 esters Chemical class 0.000 claims description 2
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims description 2
- 238000002347 injection Methods 0.000 claims description 2
- 239000007924 injection Substances 0.000 claims description 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 2
- 230000009401 metastasis Effects 0.000 claims description 2
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims description 2
- 125000004043 oxo group Chemical group O=* 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
- 230000001105 regulatory effect Effects 0.000 claims description 2
- 229940124597 therapeutic agent Drugs 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 7
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 description 2
- 125000001188 haloalkyl group Chemical group 0.000 description 2
- 125000004183 alkoxy alkyl group Chemical group 0.000 description 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 description 1
- 125000004103 aminoalkyl group Chemical group 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 235000018102 proteins Nutrition 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662401345P | 2016-09-29 | 2016-09-29 | |
| US62/401,345 | 2016-09-29 | ||
| PCT/US2017/054363 WO2018064510A1 (en) | 2016-09-29 | 2017-09-29 | Inhibitors of kras g12c mutant proteins |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2019529484A JP2019529484A (ja) | 2019-10-17 |
| JP2019529484A5 true JP2019529484A5 (https=) | 2020-11-12 |
Family
ID=60043402
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019516992A Pending JP2019529484A (ja) | 2016-09-29 | 2017-09-29 | Ｋｒａｓ ｇ１２ｃ変異体タンパク質の阻害剤 |
Country Status (5)
| Country | Link |
|---|---|
| US (2) | US10280172B2 (https=) |
| EP (1) | EP3519402A1 (https=) |
| JP (1) | JP2019529484A (https=) |
| CN (1) | CN110036010A (https=) |
| WO (1) | WO2018064510A1 (https=) |
Families Citing this family (172)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9227978B2 (en) | 2013-03-15 | 2016-01-05 | Araxes Pharma Llc | Covalent inhibitors of Kras G12C |
| JO3805B1 (ar) | 2013-10-10 | 2021-01-31 | Araxes Pharma Llc | مثبطات كراس جي12سي |
| JO3556B1 (ar) | 2014-09-18 | 2020-07-05 | Araxes Pharma Llc | علاجات مدمجة لمعالجة السرطان |
| ES2898765T3 (es) | 2015-04-10 | 2022-03-08 | Araxes Pharma Llc | Compuestos de quinazolina sustituidos y métodos de uso de los mismos |
| US10428064B2 (en) | 2015-04-15 | 2019-10-01 | Araxes Pharma Llc | Fused-tricyclic inhibitors of KRAS and methods of use thereof |
| US10144724B2 (en) | 2015-07-22 | 2018-12-04 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
| EP3356351A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| EP3356349A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| WO2017058728A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| EP3356359B1 (en) | 2015-09-28 | 2021-10-20 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| WO2017058902A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| EP3356347A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| WO2017058805A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| KR20180081596A (ko) | 2015-11-16 | 2018-07-16 | 아락세스 파마 엘엘씨 | 치환된 헤테로사이클릭 그룹을 포함하는 2-치환된 퀴나졸린 화합물 및 이의 사용 방법 |
| WO2017172979A1 (en) | 2016-03-30 | 2017-10-05 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use |
| CN109311889B (zh) | 2016-04-15 | 2021-11-16 | 缆图药品公司 | 激活素受体样激酶抑制剂 |
| KR102444509B1 (ko) | 2016-05-18 | 2022-09-19 | 미라티 테라퓨틱스, 인크. | Kras g12c 억제제 |
| US10646488B2 (en) | 2016-07-13 | 2020-05-12 | Araxes Pharma Llc | Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof |
| WO2018064510A1 (en) | 2016-09-29 | 2018-04-05 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| EP3523289A1 (en) | 2016-10-07 | 2019-08-14 | Araxes Pharma LLC | Heterocyclic compounds as inhibitors of ras and methods of use thereof |
| CN110366550A (zh) | 2016-12-22 | 2019-10-22 | 美国安进公司 | 作为用于治疗肺癌、胰腺癌或结直肠癌的KRAS G12C抑制剂的苯并异噻唑、异噻唑并[3,4-b]吡啶、喹唑啉、酞嗪、吡啶并[2,3-d]哒嗪和吡啶并[2,3-d]嘧啶衍生物 |
| EP3573954A1 (en) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | Fused bicyclic benzoheteroaromatic compounds and methods of use thereof |
| US11136308B2 (en) | 2017-01-26 | 2021-10-05 | Araxes Pharma Llc | Substituted quinazoline and quinazolinone compounds and methods of use thereof |
| WO2018140513A1 (en) | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer |
| JP7327802B2 (ja) | 2017-01-26 | 2023-08-16 | アラクセス ファーマ エルエルシー | 縮合ヘテロ－ヘテロ二環式化合物およびその使用方法 |
| WO2018140599A1 (en) | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | Benzothiophene and benzothiazole compounds and methods of use thereof |
| AU2018273356B2 (en) | 2017-05-22 | 2021-09-16 | Amgen Inc. | KRAS G12C inhibitors and methods of using the same |
| CN110869357A (zh) | 2017-05-25 | 2020-03-06 | 亚瑞克西斯制药公司 | 化合物及其用于治疗癌症的使用方法 |
| WO2018218069A1 (en) | 2017-05-25 | 2018-11-29 | Araxes Pharma Llc | Quinazoline derivatives as modulators of mutant kras, hras or nras |
| US10745385B2 (en) | 2017-05-25 | 2020-08-18 | Araxes Pharma Llc | Covalent inhibitors of KRAS |
| AU2018329920B2 (en) | 2017-09-08 | 2022-12-01 | Amgen Inc. | Inhibitors of KRAS G12C and methods of using the same |
| LT3710439T (lt) | 2017-11-15 | 2023-05-10 | Mirati Therapeutics, Inc. | Kras g12c inhibitoriai |
| US10647715B2 (en) | 2017-11-15 | 2020-05-12 | Mirati Therapeutics, Inc. | KRas G12C inhibitors |
| EP3842433B1 (en) | 2018-01-19 | 2023-11-01 | Medshine Discovery Inc. | Pyridone-pyrimidine derivative acting as krasg12c mutein inhibitor |
| EP3765459A1 (en) | 2018-03-13 | 2021-01-20 | Shire Human Genetic Therapies, Inc. | Substituted imidazopyridines as inhibitors of plasma kallikrein and uses thereof |
| CA3098574A1 (en) | 2018-05-04 | 2019-11-07 | Amgen Inc. | Kras g12c inhibitors and methods of using the same |
| EP3788053B1 (en) | 2018-05-04 | 2024-07-10 | Amgen Inc. | Kras g12c inhibitors and methods of using the same |
| WO2019217307A1 (en) | 2018-05-07 | 2019-11-14 | Mirati Therapeutics, Inc. | Kras g12c inhibitors |
| TW202012415A (zh) | 2018-05-08 | 2020-04-01 | 瑞典商阿斯特捷利康公司 | 化學化合物 |
| MA52564A (fr) | 2018-05-10 | 2021-03-17 | Amgen Inc | Inhibiteurs de kras g12c pour le traitement du cancer |
| US11096939B2 (en) | 2018-06-01 | 2021-08-24 | Amgen Inc. | KRAS G12C inhibitors and methods of using the same |
| MX2020012204A (es) | 2018-06-11 | 2021-03-31 | Amgen Inc | Inhibidores de kras g12c para tratar el cáncer. |
| US11285156B2 (en) | 2018-06-12 | 2022-03-29 | Amgen Inc. | Substituted piperazines as KRAS G12C inhibitors |
| MX2021000887A (es) | 2018-08-01 | 2021-03-31 | Araxes Pharma Llc | Compuestos espiroheterociclicos y metodos de uso de los mismos para el tratamiento de cancer. |
| AU2019320945C1 (en) | 2018-08-16 | 2021-09-30 | F. Hoffmann-La Roche Ag | Fused ring compounds |
| ES2961253T3 (es) * | 2018-08-31 | 2024-03-11 | Mirati Therapeutics Inc | Inhibidores de KRas G12C |
| EP3849535A4 (en) | 2018-09-10 | 2022-06-29 | Mirati Therapeutics, Inc. | Combination therapies |
| EP3849537B1 (en) | 2018-09-10 | 2024-10-23 | Mirati Therapeutics, Inc. | Combination therapies |
| EA202190749A1 (ru) | 2018-09-10 | 2021-07-09 | Мирати Терапьютикс, Инк. | Способы комбинированной терапии |
| JP2022500385A (ja) | 2018-09-10 | 2022-01-04 | ミラティ セラピューティクス， インコーポレイテッド | 組み合わせ療法 |
| CR20210175A (es) | 2018-09-18 | 2021-06-01 | Nikang Therapeutics Inc | Derivados de anillo tricíclico condensado como inhibidores de la fosfatasa de homología a src 2 (shp2) |
| WO2020085504A1 (ja) | 2018-10-26 | 2020-04-30 | 大鵬薬品工業株式会社 | 光照射ザンドマイヤー反応を用いたクロロアゾールカルボキシレート誘導体の製造方法 |
| JP7516029B2 (ja) * | 2018-11-16 | 2024-07-16 | アムジエン・インコーポレーテツド | Ｋｒａｓ ｇ１２ｃ阻害剤化合物の重要な中間体の改良合成法 |
| AU2019384118B2 (en) | 2018-11-19 | 2025-06-12 | Amgen Inc. | KRAS G12C inhibitors and methods of using the same |
| JP7377679B2 (ja) | 2018-11-19 | 2023-11-10 | アムジエン・インコーポレーテツド | がん治療のためのｋｒａｓｇ１２ｃ阻害剤及び１種以上の薬学的に活性な追加の薬剤を含む併用療法 |
| MX2021002804A (es) | 2018-12-05 | 2021-07-15 | Mirati Therapeutics Inc | Terapias de combinacion. |
| EP3908283A4 (en) * | 2019-01-10 | 2022-10-12 | Mirati Therapeutics, Inc. | KRAS G12C INHIBITORS |
| WO2020159942A1 (en) * | 2019-01-29 | 2020-08-06 | Tosk, Inc. | Pyrazolopyrimidine modulators of ras gtpase |
| US20220152026A1 (en) | 2019-02-12 | 2022-05-19 | Novartis Ag | Pharmaceutical combination comprising tno155 and a krasg12c inhibitor |
| WO2020173935A1 (en) | 2019-02-26 | 2020-09-03 | Boehringer Ingelheim International Gmbh | New isoindolinone substituted indoles and derivatives as ras inhibitors |
| KR102934231B1 (ko) | 2019-03-05 | 2026-03-06 | 아스트라제네카 아베 | 항암제로 유용한 융합 삼환식 화합물 |
| WO2020214537A1 (en) | 2019-04-15 | 2020-10-22 | Tosk, Inc. | Modulators of ras gtpase |
| EP3738593A1 (en) | 2019-05-14 | 2020-11-18 | Amgen, Inc | Dosing of kras inhibitor for treatment of cancers |
| WO2020234103A1 (en) | 2019-05-21 | 2020-11-26 | Bayer Aktiengesellschaft | Identification and use of kras inhibitors |
| WO2020236947A1 (en) | 2019-05-21 | 2020-11-26 | Amgen Inc. | Solid state forms |
| WO2020239077A1 (zh) * | 2019-05-29 | 2020-12-03 | 上海翰森生物医药科技有限公司 | 含氮杂环类衍生物调节剂、其制备方法和应用 |
| CN112047948B (zh) * | 2019-06-06 | 2022-08-16 | 山东轩竹医药科技有限公司 | Kras突变体抑制剂 |
| US12421236B2 (en) | 2019-06-25 | 2025-09-23 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Seven-membered heterocyclic derivative acting as KRAS G12C mutant protein inhibitor |
| CN110452180A (zh) * | 2019-06-25 | 2019-11-15 | 南京普锐达医药科技有限公司 | 一种合成2-氯-5-氨基-6-嘧啶甲酸乙酯的方法 |
| WO2021031952A1 (zh) * | 2019-08-16 | 2021-02-25 | 劲方医药科技(上海)有限公司 | 氧代六元环并嘧啶类化合物，其制法与医药上的用途 |
| MX2022002465A (es) | 2019-08-29 | 2022-05-19 | Mirati Therapeutics Inc | Inhibidores de kras g12d. |
| DK4031547T3 (da) | 2019-09-18 | 2024-09-09 | Takeda Pharmaceuticals Co | Plasmakallikreininhibitorer og anvendelser deraf |
| EP4031245A1 (en) | 2019-09-18 | 2022-07-27 | Takeda Pharmaceutical Company Limited | Heteroaryl plasma kallikrein inhibitors |
| US12122787B2 (en) | 2019-09-20 | 2024-10-22 | Shanghai Jemincare Pharmaceuticals Co., Ltd | Fused pyridone compound, and preparation method therefor and use thereof |
| WO2021061749A1 (en) | 2019-09-24 | 2021-04-01 | Mirati Therapeutics, Inc. | Combination therapies |
| WO2021058018A1 (en) * | 2019-09-29 | 2021-04-01 | Beigene, Ltd. | Inhibitors of kras g12c |
| WO2021063346A1 (zh) * | 2019-09-30 | 2021-04-08 | 上海迪诺医药科技有限公司 | Kras g12c抑制剂及其应用 |
| CN112694475B (zh) * | 2019-10-23 | 2025-09-23 | 苏州泽璟生物制药股份有限公司 | 环烷基类和杂环烷基类抑制剂及其制备方法和应用 |
| UA129778C2 (uk) | 2019-10-28 | 2025-07-30 | Мерк Шарп Енд Доум Елелсі | Низькомолекулярні інгібітори g12c-мутантного kras |
| AU2020377925A1 (en) | 2019-11-04 | 2022-05-05 | Revolution Medicines, Inc. | Ras inhibitors |
| TW202132316A (zh) | 2019-11-04 | 2021-09-01 | 美商銳新醫藥公司 | Ｒａｓ抑制劑 |
| IL322454A (en) | 2019-11-04 | 2025-09-01 | Revolution Medicines Inc | ras inhibitors |
| CN114630832A (zh) * | 2019-11-15 | 2022-06-14 | 四川海思科制药有限公司 | 一种嘧啶并环衍生物及其在医药上的应用 |
| EP4065231A1 (en) | 2019-11-27 | 2022-10-05 | Revolution Medicines, Inc. | Covalent ras inhibitors and uses thereof |
| EP4067343A4 (en) | 2019-11-29 | 2024-01-03 | Taiho Pharmaceutical Co., Ltd. | NEW PHENOLIC COMPOUND OR SALT THEREOF |
| WO2021106231A1 (en) * | 2019-11-29 | 2021-06-03 | Taiho Pharmaceutical Co., Ltd. | A compound having inhibitory activity against kras g12d mutation |
| IL293962B2 (en) * | 2019-12-19 | 2025-10-01 | Jacobio Pharmaceuticals Co Ltd | Mutant KRAS protein inhibitors |
| PH12022551513A1 (en) | 2019-12-20 | 2023-04-24 | Mirati Therapeutics Inc | Sos1 inhibitors |
| CN113045565A (zh) * | 2019-12-27 | 2021-06-29 | 微境生物医药科技(上海)有限公司 | 新型K-Ras G12C抑制剂 |
| GB202001344D0 (en) | 2020-01-31 | 2020-03-18 | Redx Pharma Plc | Ras Inhibitors |
| WO2023205701A1 (en) | 2022-04-20 | 2023-10-26 | Kumquat Biosciences Inc. | Macrocyclic heterocycles and uses thereof |
| US20210292330A1 (en) * | 2020-02-28 | 2021-09-23 | Erasca, Inc. | Pyrrolidine-fused heterocycles |
| CA3177261A1 (en) * | 2020-04-29 | 2021-11-04 | Shanghai Ringene Biopharma Co., Ltd. | Benzothiazolyl biaryl compound, and preparation method and use |
| TW202210633A (zh) | 2020-06-05 | 2022-03-16 | 法商昂席歐公司 | 用於治療癌症之dbait分子與kras抑制劑的組合 |
| IL299131A (en) | 2020-06-18 | 2023-02-01 | Revolution Medicines Inc | Methods for delaying, preventing and treating acquired resistance to RAS inhibitors |
| WO2022015375A1 (en) * | 2020-07-16 | 2022-01-20 | Mirati Therapeutics, Inc. | Kras g12d inhibitors |
| EP4204412A4 (en) * | 2020-08-26 | 2024-10-09 | InventisBio Co., Ltd. | HETEROARYL COMPOUNDS, PRODUCTION PROCESSES AND USES THEREOF |
| CN116018343A (zh) * | 2020-09-01 | 2023-04-25 | 勤浩医药（苏州）有限公司 | 一种吡啶并嘧啶化合物的晶型 |
| US20250195521A1 (en) | 2020-09-03 | 2025-06-19 | Revolution Medicines, Inc. | Use of sos1 inhibitors to treat malignancies with shp2 mutations |
| WO2022052895A1 (zh) * | 2020-09-11 | 2022-03-17 | 南京明德新药研发有限公司 | 氮杂环丁烷取代化合物的晶型 |
| EP4210833A4 (en) | 2020-09-11 | 2024-09-11 | Mirati Therapeutics, Inc. | CRYSTALLINE FORMS OF A KRAS G12C INHIBITOR |
| CA3194067A1 (en) | 2020-09-15 | 2022-03-24 | Revolution Medicines, Inc. | Ras inhibitors |
| JP2023544450A (ja) | 2020-09-23 | 2023-10-23 | エラスカ・インコーポレイテッド | 三環式ピリドン及びピリミドン |
| US12180220B2 (en) | 2020-10-14 | 2024-12-31 | Tosk, Inc. | Heteroaryl modulators of RAS GTPase |
| JP2023553492A (ja) | 2020-12-15 | 2023-12-21 | ミラティ セラピューティクス， インコーポレイテッド | アザキナゾリン汎ＫＲａｓ阻害剤 |
| EP4262803A4 (en) | 2020-12-16 | 2025-03-12 | Mirati Therapeutics, Inc. | Tetrahydropyridopyrimidine pan-kras inhibitors |
| WO2022133345A1 (en) | 2020-12-18 | 2022-06-23 | Erasca, Inc. | Tricyclic pyridones and pyrimidones |
| US20240100172A1 (en) | 2020-12-21 | 2024-03-28 | Hangzhou Jijing Pharmaceutical Technology Limited | Methods and compounds for targeted autophagy |
| WO2022140472A1 (en) | 2020-12-22 | 2022-06-30 | Nikang Therapeutics, Inc. | Compounds for degrading cyclin-dependent kinase 2 via ubiquitin proteosome pathway |
| US20240166660A1 (en) * | 2021-01-15 | 2024-05-23 | Beigene Switzerland Gmbh | Kras g12c inhibitors |
| JP2024509280A (ja) * | 2021-03-10 | 2024-02-29 | ベータ・ファーマ・インコーポレイテッド | Ｋｒａｓ阻害物質としてのピリドピリミジン誘導体 |
| KR20240017811A (ko) | 2021-05-05 | 2024-02-08 | 레볼루션 메디슨즈, 인크. | 암의 치료를 위한 ras 억제제 |
| TW202309052A (zh) | 2021-05-05 | 2023-03-01 | 美商銳新醫藥公司 | Ｒａｓ抑制劑 |
| WO2022246092A1 (en) * | 2021-05-21 | 2022-11-24 | Blossomhill Therapeutics, Inc. | Macrocyclic compounds for treating disease |
| WO2022266206A1 (en) | 2021-06-16 | 2022-12-22 | Erasca, Inc. | Kras inhibitor conjugates |
| TW202317100A (zh) | 2021-06-23 | 2023-05-01 | 瑞士商諾華公司 | 包含ｋｒａｓ ｇ１２ｃ抑制劑的藥物組合及其用於治療癌症之用途 |
| TW202317589A (zh) | 2021-07-14 | 2023-05-01 | 美商尼坎醫療公司 | 作為ｋｒａｓ抑制劑的伸烷基衍生物 |
| CN117858878A (zh) * | 2021-08-18 | 2024-04-09 | 北京加科思新药研发有限公司 | N-环丙基吡啶并[4,3-d]嘧啶-4-胺衍生物及其用途 |
| CN116323625A (zh) * | 2021-08-25 | 2023-06-23 | 浙江海正药业股份有限公司 | 杂环类衍生物、其制备方法及其医药上的用途 |
| KR20240055778A (ko) | 2021-09-01 | 2024-04-29 | 노파르티스 아게 | Tead 억제제를 포함하는 제약 조합물 및 암의 치료를 위한 이의 용도 |
| EP4389751A1 (en) | 2021-09-03 | 2024-06-26 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| AR127308A1 (es) | 2021-10-08 | 2024-01-10 | Revolution Medicines Inc | Inhibidores ras |
| CN119212994A (zh) | 2021-12-17 | 2024-12-27 | 建新公司 | 作为shp2抑制剂的吡唑并吡嗪化合物 |
| WO2023152255A1 (en) | 2022-02-10 | 2023-08-17 | Bayer Aktiengesellschaft | Fused pyrimidines as kras inhibitors |
| EP4227307A1 (en) | 2022-02-11 | 2023-08-16 | Genzyme Corporation | Pyrazolopyrazine compounds as shp2 inhibitors |
| JP2025510572A (ja) | 2022-03-08 | 2025-04-15 | レボリューション メディシンズ インコーポレイテッド | 免疫不応性肺癌を治療するための方法 |
| CN119053595A (zh) | 2022-03-28 | 2024-11-29 | 尼坎治疗公司 | 作为细胞周期蛋白依赖性激酶2抑制剂的磺酰氨基衍生物 |
| WO2023199180A1 (en) | 2022-04-11 | 2023-10-19 | Novartis Ag | Therapeutic uses of a krasg12c inhibitor |
| WO2023219941A1 (en) * | 2022-05-09 | 2023-11-16 | Beta Pharma, Inc. | 8- and 6-substituted pyridopyrimidine derivatives as kras inhibitors |
| CN119790053A (zh) | 2022-06-08 | 2025-04-08 | 霖康疗法公司 | 作为细胞周期蛋白依赖性激酶2抑制剂的磺酰胺衍生物 |
| WO2023240263A1 (en) | 2022-06-10 | 2023-12-14 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| GB202212641D0 (en) | 2022-08-31 | 2022-10-12 | Jazz Pharmaceuticals Ireland Ltd | Novel compounds |
| CN120659773A (zh) | 2022-11-09 | 2025-09-16 | 锐新医药公司 | 化合物、复合物以及其制备方法和用途 |
| AU2023375457A1 (en) | 2022-11-11 | 2025-05-01 | Nikang Therapeutics, Inc. | Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 via ubiquitin proteasome pathway |
| WO2024123102A1 (ko) * | 2022-12-07 | 2024-06-13 | 에스케이바이오팜 주식회사 | Kras g12d 저해제로서 신규한 3환 화합물 및 이의 용도 |
| AU2024241633A1 (en) | 2023-03-30 | 2025-11-06 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| CR20250420A (es) | 2023-04-07 | 2025-11-20 | Revolution Medicines Inc | Inhibidores macrocíclicos de ras |
| AR132338A1 (es) | 2023-04-07 | 2025-06-18 | Revolution Medicines Inc | Inhibidores de ras |
| CN121464140A (zh) | 2023-04-14 | 2026-02-03 | 锐新医药公司 | Ras抑制剂的结晶形式、含有其的组合物及其使用方法 |
| CN121100123A (zh) | 2023-04-14 | 2025-12-09 | 锐新医药公司 | Ras抑制剂的结晶形式 |
| 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 |
| PE20252789A1 (es) | 2023-05-24 | 2025-12-22 | Kumquat Biosciences Inc | Compuestos heterociclicos y usos de estos |
| EP4721766A1 (en) | 2023-06-02 | 2026-04-08 | Daiichi Sankyo Company, Limited | Combination of (anti-her3 antibody)-drug conjugate and rasg12c inhibitor |
| CN121263417A (zh) | 2023-06-30 | 2026-01-02 | 金橘生物科技公司 | 取代的稠合三环胺化合物及其作为ras抑制剂的用途 |
| WO2025016899A1 (en) | 2023-07-19 | 2025-01-23 | Bayer Aktiengesellschaft | Spirocyclic compounds for the treatment of cancer |
| WO2025026903A1 (en) | 2023-07-31 | 2025-02-06 | Bayer Aktiengesellschaft | Imidazo pyrimidine compounds for the treatment of cancer |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025072462A1 (en) | 2023-09-27 | 2025-04-03 | Nikang Therapeutics, Inc. | Sulfonamide derivatives as cyclin-dependent kinase 2 inhibitors |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| AU2024361909A1 (en) | 2023-10-20 | 2026-03-26 | Merck Sharp & Dohme Llc | Small molecule inhibitors of kras proteins |
| TW202527955A (zh) | 2023-11-27 | 2025-07-16 | 美商尼坎醫療公司 | 用於經由泛素蛋白酶體途徑降解週期蛋白依賴性激酶２和週期蛋白依賴性激酶４的含有２，５－取代的嘧啶衍生物的雙功能化合物 |
| WO2025117981A1 (en) | 2023-12-02 | 2025-06-05 | Nikang Therapeutics, Inc. | Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 via ubiquitin proteasome pathway |
| WO2025171055A1 (en) | 2024-02-06 | 2025-08-14 | Kumquat Biosciences Inc. | Heterocyclic conjugates and uses thereof |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025212828A1 (en) | 2024-04-03 | 2025-10-09 | Nikang Therapeutics, Inc. | Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 and cyclin-dependent kinase 4 via ubiquitin proteasome pathway |
| WO2025230971A1 (en) | 2024-04-30 | 2025-11-06 | Kumquat Biosciences Inc. | Macrocyclic heterocycles as anticancer agents |
| WO2025240536A1 (en) | 2024-05-15 | 2025-11-20 | Nikang Therapeutics, Inc. | Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 and/or cyclin-dependent kinase 4 via ubiquitin proteasome pathway |
| TW202547461A (zh) | 2024-05-17 | 2025-12-16 | 美商銳新醫藥公司 | Ｒａｓ抑制劑 |
| WO2025253326A1 (ko) * | 2024-06-05 | 2025-12-11 | 에스케이바이오팜 주식회사 | Kras 저해제로서 신규한 3환 화합물 및 이의 용도 |
| 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 |
| WO2026015790A1 (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 |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026035945A1 (en) | 2024-08-07 | 2026-02-12 | Tesseract Medicines Us, Llc | Covalent-induced drug conjugates targeting kras and comprising a topoisomerase payload |
| WO2026035947A1 (en) | 2024-08-07 | 2026-02-12 | Tesseract Medicines Us, Llc | Kras-targeting covalent-induced drug conjugates comprising a topoisomerase payload |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026064520A1 (en) | 2024-09-19 | 2026-03-26 | Tesseract Medicines Us, Llc | Covalent-induced drug conjugates targeting kras and comprising a tubulin inhibitor payload |
| WO2026064527A1 (en) | 2024-09-19 | 2026-03-26 | Tesseract Medicines Us, Llc | Kras-targeting covalent-induced drug conjugates comprising a tubulin inhibitor payload |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
Family Cites Families (202)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB939516A (en) | 1961-05-29 | 1963-10-16 | British Drug Houses Ltd | Sulphonyl ureas |
| US3702849A (en) | 1967-10-26 | 1972-11-14 | Pfizer | 4-(isoquinolin-1-yl) piperazine-1-carboxylic acid esters |
| US3752660A (en) | 1971-03-15 | 1973-08-14 | Allied Chem | Chlorophenoxyacetyloxazolidone herbicides and preparation thereof |
| US4439606A (en) | 1982-05-06 | 1984-03-27 | American Cyanamid Company | Antiatherosclerotic 1-piperazinecarbonyl compounds |
| EP0094498A3 (en) | 1982-05-06 | 1985-04-03 | American Cyanamid Company | Antiatherosclerotic 1-piperazine derivatives |
| US4656181A (en) | 1982-11-24 | 1987-04-07 | Cermol S.A. | Esters of 1,4-dihydropyridines, processes for the preparation of the new esters, and medicaments containing the same |
| JPS59163372A (ja) | 1983-03-09 | 1984-09-14 | Showa Denko Kk | ピラゾ−ル誘導体とその製造法及び除草剤 |
| JPS60193955A (ja) | 1984-03-13 | 1985-10-02 | Mitsui Toatsu Chem Inc | 環式不飽和アミド置換エ−テル化合物及びその製造方法 |
| JPS6143190A (ja) | 1984-08-06 | 1986-03-01 | Mitsui Petrochem Ind Ltd | ピリドピリミジン誘導体およびその製法 |
| US4911920A (en) | 1986-07-30 | 1990-03-27 | Alcon Laboratories, Inc. | Sustained release, comfort formulation for glaucoma therapy |
| FR2588189B1 (fr) | 1985-10-03 | 1988-12-02 | Merck Sharp & Dohme | Composition pharmaceutique de type a transition de phase liquide-gel |
| US5052558A (en) | 1987-12-23 | 1991-10-01 | Entravision, Inc. | Packaged pharmaceutical product |
| US5033252A (en) | 1987-12-23 | 1991-07-23 | Entravision, Inc. | Method of packaging and sterilizing a pharmaceutical product |
| US5010175A (en) | 1988-05-02 | 1991-04-23 | The Regents Of The University Of California | General method for producing and selecting peptides with specific properties |
| GB8827305D0 (en) | 1988-11-23 | 1988-12-29 | British Bio Technology | Compounds |
| US5925525A (en) | 1989-06-07 | 1999-07-20 | Affymetrix, Inc. | Method of identifying nucleotide differences |
| IE66205B1 (en) | 1990-06-14 | 1995-12-13 | Paul A Bartlett | Polypeptide analogs |
| US5650489A (en) | 1990-07-02 | 1997-07-22 | The Arizona Board Of Regents | Random bio-oligomer library, a method of synthesis thereof, and a method of use thereof |
| JP2594486B2 (ja) | 1991-01-15 | 1997-03-26 | アルコン ラボラトリーズ インコーポレイテッド | 局所的眼薬組成物 |
| US5212162A (en) | 1991-03-27 | 1993-05-18 | Alcon Laboratories, Inc. | Use of combinations gelling polysaccharides and finely divided drug carrier substrates in topical ophthalmic compositions |
| US6051380A (en) | 1993-11-01 | 2000-04-18 | Nanogen, Inc. | Methods and procedures for molecular biological analysis and diagnostics |
| US6017696A (en) | 1993-11-01 | 2000-01-25 | Nanogen, Inc. | Methods for electronic stringency control for molecular biological analysis and diagnostics |
| US5573905A (en) | 1992-03-30 | 1996-11-12 | The Scripps Research Institute | Encoded combinatorial chemical libraries |
| US5323907A (en) | 1992-06-23 | 1994-06-28 | Multi-Comp, Inc. | Child resistant package assembly for dispensing pharmaceutical medications |
| US5288514A (en) | 1992-09-14 | 1994-02-22 | The Regents Of The University Of California | Solid phase and combinatorial synthesis of benzodiazepine compounds on a solid support |
| US5455258A (en) | 1993-01-06 | 1995-10-03 | Ciba-Geigy Corporation | Arylsulfonamido-substituted hydroxamic acids |
| US5605798A (en) | 1993-01-07 | 1997-02-25 | Sequenom, Inc. | DNA diagnostic based on mass spectrometry |
| US5858659A (en) | 1995-11-29 | 1999-01-12 | Affymetrix, Inc. | Polymorphism detection |
| US6045996A (en) | 1993-10-26 | 2000-04-04 | Affymetrix, Inc. | Hybridization assays on oligonucleotide arrays |
| US6068818A (en) | 1993-11-01 | 2000-05-30 | Nanogen, Inc. | Multicomponent devices for molecular biological analysis and diagnostics |
| US5538848A (en) | 1994-11-16 | 1996-07-23 | Applied Biosystems Division, Perkin-Elmer Corp. | Method for detecting nucleic acid amplification using self-quenching fluorescence probe |
| IL111730A (en) | 1993-11-29 | 1998-12-06 | Fujisawa Pharmaceutical Co | Piperazine derivatives processes for the preparation thereof and pharmaceutical compositions containing the same |
| WO1995021271A1 (en) | 1994-02-07 | 1995-08-10 | Molecular Tool, Inc. | Ligase/polymerase-mediated genetic bit analysistm of single nucleotide polymorphisms and its use in genetic analysis |
| US5593853A (en) | 1994-02-09 | 1997-01-14 | Martek Corporation | Generation and screening of synthetic drug libraries |
| US5539083A (en) | 1994-02-23 | 1996-07-23 | Isis Pharmaceuticals, Inc. | Peptide nucleic acid combinatorial libraries and improved methods of synthesis |
| US6309853B1 (en) | 1994-08-17 | 2001-10-30 | The Rockfeller University | Modulators of body weight, corresponding nucleic acids and proteins, and diagnostic and therapeutic uses thereof |
| JP2002515008A (ja) | 1994-10-27 | 2002-05-21 | メルク エンド カンパニー インコーポレーテッド | ムスカリン・アンタゴニスト |
| US5863949A (en) | 1995-03-08 | 1999-01-26 | Pfizer Inc | Arylsulfonylamino hydroxamic acid derivatives |
| ES2153031T4 (es) | 1995-04-20 | 2001-05-16 | Pfizer | Derivados del acido arilsulfonil hidroxamico como inhibidores de mmp y tnf. |
| FR2734816B1 (fr) | 1995-05-31 | 1997-07-04 | Adir | Nouveaux aryl (alkyl) propylamides, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| US5977322A (en) | 1995-06-14 | 1999-11-02 | The Regents Of The University Of California | High affinity human antibodies to tumor antigens |
| ATE225343T1 (de) | 1995-12-20 | 2002-10-15 | Hoffmann La Roche | Matrix-metalloprotease inhibitoren |
| US6011029A (en) | 1996-02-26 | 2000-01-04 | Bristol-Myers Squibb Company | Inhibitors of farnesyl protein transferase |
| EP0818442A3 (en) | 1996-07-12 | 1998-12-30 | Pfizer Inc. | Cyclic sulphone derivatives as inhibitors of metalloproteinases and of the production of tumour necrosis factor |
| KR20000067904A (ko) | 1996-07-18 | 2000-11-25 | 디. 제이. 우드, 스피겔 알렌 제이 | 매트릭스 메탈로프로테아제의 포스피네이트계 억제제 |
| KR20000068248A (ko) | 1996-08-23 | 2000-11-25 | 디. 제이. 우드, 스피겔 알렌 제이 | 아릴설포닐아미노 하이드록삼산 유도체 |
| US5777324A (en) | 1996-09-19 | 1998-07-07 | Sequenom, Inc. | Method and apparatus for maldi analysis |
| JP3338064B2 (ja) | 1997-01-06 | 2002-10-28 | ファイザー・インク | 環状スルホン誘導体 |
| NZ336840A (en) | 1997-02-03 | 2001-01-26 | Pfizer Prod Inc | Arylsulfonylamino hydroxamic acid derivatives useful in the treatment of tumor necrosis factor and matrix metalloproteinase mediated diseases |
| GB9702194D0 (en) | 1997-02-04 | 1997-03-26 | Lilly Co Eli | Sulphonide derivatives |
| 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 |
| EP0960098A1 (en) | 1997-02-11 | 1999-12-01 | Pfizer Inc. | Arylsulfonyl hydroxamic acid derivatives |
| US6291464B1 (en) | 1997-02-17 | 2001-09-18 | Fujisawa Pharmaceutical Co., Ltd. | Aminopiperazine derivatives |
| UA73073C2 (uk) | 1997-04-03 | 2005-06-15 | Уайт Холдінгз Корпорейшн | Заміщені 3-ціанохіноліни, спосіб їх одержання та фармацевтична композиція |
| US6002008A (en) | 1997-04-03 | 1999-12-14 | American Cyanamid Company | Substituted 3-cyano quinolines |
| US5919626A (en) | 1997-06-06 | 1999-07-06 | Orchid Bio Computer, Inc. | Attachment of unmodified nucleic acids to silanized solid phase surfaces |
| ZA985205B (en) | 1997-06-17 | 1998-12-15 | Schering Corp | Novel n-substituted urea inhibitors of arnesyl-protein transferase |
| CA2299355C (en) | 1997-08-08 | 2005-09-27 | Pfizer Products Inc. | Aryloxyarylsulfonylamino hydroxamic acid derivatives |
| GB9725782D0 (en) | 1997-12-05 | 1998-02-04 | Pfizer Ltd | Therapeutic agents |
| DE19756236A1 (de) | 1997-12-17 | 1999-07-01 | Klinge Co Chem Pharm Fab | Neue piperazinylsubstituierte Pyridylalkan-, alken- und -alkincarbonsäureamide |
| US6903118B1 (en) | 1997-12-17 | 2005-06-07 | Klinge Pharma Gmbh | Piperazinyl-substituted pyridylalkane, alkene and alkine carboxamides |
| EP1042299A1 (en) | 1997-12-22 | 2000-10-11 | Du Pont Pharmaceuticals Company | Nitrogen containing heteroaromatics with ortho-substituted p1's as factor xa inhibitors |
| 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 |
| EP1090293B2 (en) | 1998-06-24 | 2019-01-23 | Illumina, Inc. | Decoding of array sensors with microspheres |
| EP1004578B1 (en) | 1998-11-05 | 2004-02-25 | Pfizer Products Inc. | 5-oxo-pyrrolidine-2-carboxylic acid hydroxamide derivatives |
| US6429027B1 (en) | 1998-12-28 | 2002-08-06 | Illumina, Inc. | Composite arrays utilizing microspheres |
| US6511993B1 (en) | 1999-06-03 | 2003-01-28 | Kevin Neil Dack | Metalloprotease inhibitors |
| EP1081137A1 (en) | 1999-08-12 | 2001-03-07 | Pfizer Products Inc. | Selective inhibitors of aggrecanase in osteoarthritis treatment |
| DK1218542T3 (da) | 1999-09-13 | 2004-08-02 | Nugen Technologies Inc | Fremgangsmåder og sammensætninger til lineær isotermisk amplifikation af polynukleotidsekvenser |
| NZ520656A (en) | 2000-03-21 | 2004-05-28 | Procter & Gamble | Heterocyclic side chain containing metalloprotease inhibitors |
| AU5889701A (en) | 2000-06-05 | 2001-12-17 | Dong A Pharm Co Ltd | Novel oxazolidinone derivatives and a process for the preparation thereof |
| TWI227231B (en) | 2000-07-12 | 2005-02-01 | Novartis Ag | 4-benzoyl-piperidine derivatives for treating conditions mediated by CCR-3 |
| PT1315715E (pt) | 2000-08-18 | 2008-10-30 | Millennium Pharm Inc | Derivados de quianazolina utilizados como inibidores de quinase |
| US6890747B2 (en) | 2000-10-23 | 2005-05-10 | Warner-Lambert Company | Phosphoinositide 3-kinases |
| US7429599B2 (en) | 2000-12-06 | 2008-09-30 | Signal Pharmaceuticals, Llc | Methods for treating or preventing an inflammatory or metabolic condition or inhibiting JNK |
| US20020169300A1 (en) | 2001-01-30 | 2002-11-14 | Waterman Marian L. | Method of detection and treatment of colon cancer by analysis of beta-catenin-sensitive isoforms of lymphoid enhancer factor-1 |
| CA2443108A1 (en) | 2001-04-03 | 2002-10-17 | Merck & Co. Inc. | N-substituted nonaryl-heterocyclo amidyl nmda/nr2b antagonists |
| US7074801B1 (en) | 2001-04-26 | 2006-07-11 | Eisai Co., Ltd. | Nitrogen-containing condensed cyclic compound having a pyrazolyl group as a substituent group and pharmaceutical composition thereof |
| ATE449090T1 (de) | 2001-07-02 | 2009-12-15 | High Point Pharmaceuticals Llc | Substituierte piperazin- und diazepanderivate zur verwendung als histamin h3 rezeptormodulatoren |
| EP1348434A1 (en) | 2002-03-27 | 2003-10-01 | Fujisawa Deutschland GmbH | Use of pyridyl amides as inhibitors of angiogenesis |
| WO2004033427A1 (en) | 2002-10-11 | 2004-04-22 | Astrazeneca Ab | 1,4-disubstituted piperidine derivatives and their use as 11-betahsd1 inhibitors |
| JP4608852B2 (ja) | 2002-10-15 | 2011-01-12 | チッソ株式会社 | 液晶性ビニルケトン誘導体およびその重合体 |
| MXPA05008878A (es) | 2003-02-21 | 2005-10-05 | Pfizer | Derivados de aminotiazol sustituidos con cicloalquilo que contiene n y composiciones farmaceuticas para inhibir la proliferacion celular, y metodos para su uso. |
| PL1633724T3 (pl) | 2003-03-12 | 2011-10-31 | Kudos Pharm Ltd | Pochodne ftalazynonu |
| US20050119266A1 (en) | 2003-10-01 | 2005-06-02 | Yan Shi | Pyrrolidine and piperidine derivatives as factor Xa inhibitors |
| JP4923380B2 (ja) | 2003-12-22 | 2012-04-25 | Ｊｎｃ株式会社 | 低屈折率異方性化合物、組成物およびそれらの重合体または重合体組成物 |
| GEP20084439B (en) | 2004-01-23 | 2008-07-25 | Amgen Inc | Nitrogen-containing heterocyclic derivatives and pharmaceutical use thereof |
| WO2005082892A2 (en) | 2004-02-17 | 2005-09-09 | Dr. Reddy's Laboratories Ltd. | Triazole compounds as antibacterial agents and pharmaceutical compositions containing them |
| JP4775259B2 (ja) | 2004-03-31 | 2011-09-21 | 味の素株式会社 | アニリン誘導体 |
| GT200500375A (es) | 2004-12-20 | 2006-11-28 | Derivados de piperidina y su uso como agentes antiinflamatorios | |
| US20090264415A2 (en) | 2004-12-30 | 2009-10-22 | Steven De Jonghe | Pyrido(3,2-d)pyrimidines and pharmaceutical compositions useful for medical treatment |
| GB0428475D0 (en) | 2004-12-30 | 2005-02-02 | 4 Aza Bioscience Nv | Pyrido(3,2-D)pyrimidine derivatives and pharmaceutical compositions useful as medicines for the treatment of autoimmune disorders |
| CA2599476A1 (en) | 2005-03-16 | 2006-09-21 | F. Hoffmann-La Roche Ag | Cis-2,4,5-triaryl-imidazolines and their use as anti-cancer medicaments |
| JP2007016011A (ja) | 2005-06-10 | 2007-01-25 | Nippon Soda Co Ltd | 抗酸化活性を有する新規な含窒素ヘテロ環化合物、及び該化合物を含有する抗酸化薬 |
| AU2006261607A1 (en) | 2005-06-24 | 2006-12-28 | Gilead Sciences, Inc. | Pyrido(3,2-d)pyrimidines and pharmaceutical compositions useful for treating hepatitis C. |
| WO2007047146A2 (en) | 2005-10-11 | 2007-04-26 | Intermune, Inc. | Inhibitors of viral replication |
| EP1966132A2 (en) | 2005-12-15 | 2008-09-10 | Boehringer Ingelheim International Gmbh | Compounds which modulate the cb2 receptor |
| PE20070978A1 (es) | 2006-02-14 | 2007-11-15 | Novartis Ag | COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks) |
| MX2008012617A (es) | 2006-03-31 | 2008-10-10 | Novartis Ag | Compuestos organicos. |
| EP2059515A2 (en) | 2006-04-12 | 2009-05-20 | Pfizer Limited | Pyrrolidine derivatives as modulators of chemokine ccr5 receptors |
| EP2038255A2 (en) | 2006-06-16 | 2009-03-25 | High Point Pharmaceuticals, LLC | Pharmaceutical use of substituted piperidine carboxamides |
| US20080039450A1 (en) | 2006-06-22 | 2008-02-14 | Jensen Annika J | Compounds |
| FR2903101B1 (fr) | 2006-06-30 | 2008-09-26 | Servier Lab | Nouveaux derives naphtaleniques, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| WO2008009078A2 (en) | 2006-07-20 | 2008-01-24 | Gilead Sciences, Inc. | 4,6-dl- and 2,4,6-trisubstituted quinazoline derivatives useful for treating viral infections |
| EP1903038A1 (de) | 2006-09-07 | 2008-03-26 | Bayer Schering Pharma Aktiengesellschaft | N-(1-Hetaryl-piperidin-4-yl)-(het)arylamide als EP2-Rezeptor Modulatoren |
| JP2010520876A (ja) | 2007-03-09 | 2010-06-17 | アストラゼネカ・アクチエボラーグ | ピペラジンおよびピペリジンｍＧｌｕＲ５増強剤 |
| EP2144606A2 (en) | 2007-04-05 | 2010-01-20 | Max-Delbrück-Centrum Für Molekulare Medizin | Remedy for the treatment of cardio-vascular diseases or disorders |
| MY162157A (en) | 2007-04-16 | 2017-05-31 | Abbott Lab | Substituted indole mcl-1 inhibitors |
| EP4230747A3 (en) | 2008-03-28 | 2023-11-15 | Pacific Biosciences Of California, Inc. | Compositions and methods for nucleic acid sequencing |
| EP2133334A1 (en) | 2008-06-09 | 2009-12-16 | DAC S.r.l. | Heterocyclic derivatives as HDAC inhibitors |
| JP5555236B2 (ja) | 2008-08-25 | 2014-07-23 | アイアールエム・リミテッド・ライアビリティ・カンパニー | ヘッジホッグ経路モジュレーター |
| WO2010087399A1 (ja) | 2009-01-30 | 2010-08-05 | 第一三共株式会社 | ウロテンシンｉｉ受容体拮抗薬 |
| CA2758210C (en) | 2009-04-20 | 2017-08-29 | F. Hoffmann-La Roche Ag | Proline derivatives as cathepsin inhibitors |
| JP2012524800A (ja) | 2009-04-22 | 2012-10-18 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | モノアシルグリセロールリパーゼ阻害剤としてのアゼチジニルジアミド |
| EP2270002A1 (en) | 2009-06-18 | 2011-01-05 | Vereniging voor Christelijk Hoger Onderwijs, Wetenschappelijk Onderzoek en Patiëntenzorg | Quinazoline derivatives as histamine H4-receptor inhibitors for use in the treatment of inflammatory disorders |
| ES2618630T3 (es) | 2009-06-29 | 2017-06-21 | Agios Pharmaceuticals, Inc. | Composiciones terapéuticas y métodos de uso relacionados |
| WO2011016559A1 (ja) | 2009-08-07 | 2011-02-10 | 武田薬品工業株式会社 | 複素環化合物およびその用途 |
| KR101256018B1 (ko) | 2009-08-20 | 2013-04-18 | 한국과학기술연구원 | 단백질 키나아제 저해활성을 갖는 1,3,6-치환된 인돌 화합물 |
| JP2013504325A (ja) | 2009-09-09 | 2013-02-07 | アビラ セラピューティクス， インコーポレイテッド | Ｐｉ３キナーゼインヒビターおよびその使用 |
| KR101758046B1 (ko) | 2009-12-22 | 2017-07-14 | 버텍스 파마슈티칼스 인코포레이티드 | 포스파티딜이노시톨 3-키나제의 이소인돌리논 억제제 |
| JP2013516422A (ja) | 2009-12-30 | 2013-05-13 | アビラ セラピューティクス， インコーポレイテッド | タンパク質のリガンド−指向性共有的修飾 |
| HRP20141190T1 (hr) | 2010-01-29 | 2015-01-30 | Otsuka Pharmaceutical Co., Ltd. | Disupstituirani derivati piridina kao antikancerogena sredstva |
| CA2783665A1 (en) | 2010-03-03 | 2011-09-09 | OSI Pharmaceuticals, LLC | Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors |
| BR112012022868A2 (pt) | 2010-03-16 | 2018-06-05 | Merck Patent Gmbh | morfolinilquinazolinas |
| KR20130065632A (ko) | 2010-04-28 | 2013-06-19 | 다이이찌 산쿄 가부시키가이샤 | ［５，６］복소 고리 화합물 |
| TW201202230A (en) | 2010-05-24 | 2012-01-16 | Mitsubishi Tanabe Pharma Corp | Novel quinazoline compound |
| WO2011153553A2 (en) | 2010-06-04 | 2011-12-08 | The Regents Of The University Of California | Methods and compositions for kinase inhibition |
| EP2580378A4 (en) | 2010-06-08 | 2014-01-01 | Nugen Technologies Inc | MULTIPLEX SEQUENCING METHODS AND COMPOSITION |
| US8658131B2 (en) | 2010-06-21 | 2014-02-25 | Washington University | Compounds comprising 4-benzoylpiperidine as a sigma-1-selective ligand |
| CA2806332C (en) | 2010-07-30 | 2017-11-14 | Oncotherapy Science, Inc. | Quinoline derivatives and melk inhibitors containing the same |
| CN103068798A (zh) | 2010-09-03 | 2013-04-24 | 詹森药业有限公司 | 作为单酰甘油脂肪酶抑制剂的二-氮杂环丁烷二酰胺 |
| US8883791B2 (en) | 2010-09-29 | 2014-11-11 | Intervet Inc. | N-heteroaryl compounds with cyclic bridging unit for the treatment of parasitic diseases |
| JP2013540159A (ja) | 2010-10-22 | 2013-10-31 | ヤンセン ファーマシューティカ エヌ．ベー． | モノアシルグリセロールリパーゼ阻害剤としてのピペリジン−４−イル−アゼチジンジアミド |
| US20130225524A1 (en) | 2010-11-05 | 2013-08-29 | Deping Chai | Chemical Compounds |
| WO2012174489A2 (en) | 2011-06-15 | 2012-12-20 | The Ohio State University | Small molecule composite surfaces as inhibitors of protein-protein interactions |
| CA2840627A1 (en) | 2011-06-29 | 2013-01-03 | Otsuka Pharmaceutical Co., Ltd. | Quinazolines as therapeutic compounds and related methods of use |
| CN103087077B (zh) | 2011-11-03 | 2016-05-18 | 上海希迈医药科技有限公司 | 噻吩并嘧啶和呋喃并嘧啶类衍生物、其制备方法及其在医药上的应用 |
| JP2013107855A (ja) | 2011-11-22 | 2013-06-06 | Mitsubishi Tanabe Pharma Corp | 医薬組成物 |
| US9745631B2 (en) | 2011-12-20 | 2017-08-29 | Dana-Farber Cancer Institute, Inc. | Methods for diagnosing and treating oncogenic kras-associated cancer |
| WO2013096151A1 (en) | 2011-12-22 | 2013-06-27 | Glaxosmithkline Llc | Chemical compounds |
| ES2575604T3 (es) | 2012-01-13 | 2016-06-29 | Bristol-Myers Squibb Company | Compuestos de piridilo sustituidos con tiazolilo o tiadiazolilo útiles como inhibidores cinasa |
| AU2013237226A1 (en) | 2012-03-19 | 2014-10-09 | Emory University | Quinazoline compounds and their use in therapy |
| WO2013155077A1 (en) | 2012-04-09 | 2013-10-17 | Board Of Regents,The University Of Texas System | Response markers for src inhibitor therapies |
| EP2836482B1 (en) | 2012-04-10 | 2019-12-25 | The Regents of The University of California | Compositions and methods for treating cancer |
| ES3039913T3 (en) | 2012-05-09 | 2025-10-27 | Gradalis Inc | Bi-functional short-hairpin rna (bi-shrna) specific for single-nucleotide kras mutations |
| JO3300B1 (ar) | 2012-06-06 | 2018-09-16 | Novartis Ag | مركبات وتركيبات لتعديل نشاط egfr |
| SG11201500125QA (en) | 2012-07-11 | 2015-02-27 | Blueprint Medicines Corp | Inhibitors of the fibroblast growth factor receptor |
| JPWO2014030743A1 (ja) | 2012-08-24 | 2016-08-08 | 武田薬品工業株式会社 | 複素環化合物 |
| CN202931543U (zh) | 2012-10-19 | 2013-05-08 | 深圳Tcl新技术有限公司 | 扬声器 |
| AU2013337717B2 (en) | 2012-11-01 | 2018-10-25 | Infinity Pharmaceuticals, Inc. | Treatment of cancers using PI3 kinase isoform modulators |
| EA201591746A1 (ru) | 2013-03-14 | 2016-08-31 | КОНВЕРДЖЕН ЭлЭлСи | Способы и композиции для ингибирования бромодомен-содержащих белков |
| CA2904393A1 (en) | 2013-03-15 | 2014-09-25 | Araxes Pharma Llc | Covalent inhibitors of kras g12c |
| US9745319B2 (en) | 2013-03-15 | 2017-08-29 | Araxes Pharma Llc | Irreversible covalent inhibitors of the GTPase K-Ras G12C |
| US9227978B2 (en) | 2013-03-15 | 2016-01-05 | Araxes Pharma Llc | Covalent inhibitors of Kras G12C |
| JP6518656B2 (ja) | 2013-06-13 | 2019-05-22 | バイオデシー， インコーポレイテッド | 標的生体実体を標的にする生化学実体候補をスクリーニングする方法 |
| DK3016946T3 (da) | 2013-07-03 | 2023-01-09 | Karyopharm Therapeutics Inc | Substituerede benzofuranyl- og benzoxazolylforbindelser og anvendelser deraf |
| RS58361B1 (sr) | 2013-07-31 | 2019-03-29 | Merck Patent Gmbh | Piridini, pirimidini i pirazini, kao inhibitori btk i njihova upotreba |
| CN104418860B (zh) | 2013-08-20 | 2016-09-07 | 中国科学院广州生物医药与健康研究院 | 嘧啶并杂环类化合物及其药用组合物和应用 |
| JO3805B1 (ar) | 2013-10-10 | 2021-01-31 | Araxes Pharma Llc | مثبطات كراس جي12سي |
| EP3055290B1 (en) | 2013-10-10 | 2019-10-02 | Araxes Pharma LLC | Inhibitors of kras g12c |
| US9376559B2 (en) | 2013-11-22 | 2016-06-28 | Exxonmobil Chemical Patents Inc. | Reverse staged impact copolymers |
| US9695165B2 (en) | 2014-01-15 | 2017-07-04 | Blueprint Medicines Corporation | Inhibitors of the fibroblast growth factor receptor |
| WO2015132799A2 (en) * | 2014-02-03 | 2015-09-11 | Cadila Healthcare Limited | Novel heterocyclic compounds |
| CA2943220C (en) | 2014-03-20 | 2024-01-16 | Capella Therapeutics, Inc. | Benzimidazole derivatives as erbb tyrosine kinase inhibitors for the treatment of cancer |
| SG11201607973XA (en) | 2014-03-24 | 2016-11-29 | Guangdong Zhongsheng Pharmaceutical Co Ltd | Quinoline derivatives as smo inhibitors |
| MA40074A (fr) | 2014-05-30 | 2015-12-03 | Univ Columbia | Composés liant ras multivalents |
| EP3827836A1 (en) | 2014-06-27 | 2021-06-02 | Celgene Corporation | Compositions and methods for inducing conformational changes in cereblon and other e3 ubiquitin ligases |
| JO3556B1 (ar) | 2014-09-18 | 2020-07-05 | Araxes Pharma Llc | علاجات مدمجة لمعالجة السرطان |
| JP2017528498A (ja) | 2014-09-25 | 2017-09-28 | アラクセス ファーマ エルエルシー | Ｋｒａｓ ｇ１２ｃ変異体タンパク質のインヒビター |
| WO2016049568A1 (en) | 2014-09-25 | 2016-03-31 | Araxes Pharma Llc | Methods and compositions for inhibition of ras |
| WO2016049565A1 (en) | 2014-09-25 | 2016-03-31 | Araxes Pharma Llc | Compositions and methods for inhibition of ras |
| EP3247353A4 (en) * | 2015-01-23 | 2018-07-04 | Confluence Life Sciences, Inc. | Heterocyclic itk inhibitors for treating inflammation and cancer |
| US20160219959A1 (en) | 2015-01-23 | 2016-08-04 | Bella Lash Extensions, Llc | Tray for holding eyelash extensions and processes for applying eyelash extensions |
| ES2898765T3 (es) * | 2015-04-10 | 2022-03-08 | Araxes Pharma Llc | Compuestos de quinazolina sustituidos y métodos de uso de los mismos |
| US10428064B2 (en) | 2015-04-15 | 2019-10-01 | Araxes Pharma Llc | Fused-tricyclic inhibitors of KRAS and methods of use thereof |
| US10144724B2 (en) | 2015-07-22 | 2018-12-04 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
| WO2017015562A1 (en) | 2015-07-22 | 2017-01-26 | Araxes Pharma Llc | Substituted quinazoline compounds and their use as inhibitors of g12c mutant kras, hras and/or nras proteins |
| WO2017058805A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| EP3356347A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| WO2017058902A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| WO2017058728A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| EP3356351A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| EP3356359B1 (en) | 2015-09-28 | 2021-10-20 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| EP3356349A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| WO2017070256A2 (en) | 2015-10-19 | 2017-04-27 | Araxes Pharma Llc | Method for screening inhibitors of ras |
| HUE068392T2 (hu) | 2015-10-21 | 2024-12-28 | Otsuka Pharma Co Ltd | Benzolaktám vegyületek mint fehérje kináz gátlók |
| KR20180081596A (ko) | 2015-11-16 | 2018-07-16 | 아락세스 파마 엘엘씨 | 치환된 헤테로사이클릭 그룹을 포함하는 2-치환된 퀴나졸린 화합물 및 이의 사용 방법 |
| US9988357B2 (en) | 2015-12-09 | 2018-06-05 | Araxes Pharma Llc | Methods for preparation of quinazoline derivatives |
| WO2017172979A1 (en) | 2016-03-30 | 2017-10-05 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use |
| US10646488B2 (en) | 2016-07-13 | 2020-05-12 | Araxes Pharma Llc | Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof |
| WO2018064510A1 (en) | 2016-09-29 | 2018-04-05 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| EP3523289A1 (en) | 2016-10-07 | 2019-08-14 | Araxes Pharma LLC | Heterocyclic compounds as inhibitors of ras and methods of use thereof |
| EP3573954A1 (en) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | Fused bicyclic benzoheteroaromatic compounds and methods of use thereof |
| JP7327802B2 (ja) | 2017-01-26 | 2023-08-16 | アラクセス ファーマ エルエルシー | 縮合ヘテロ－ヘテロ二環式化合物およびその使用方法 |
| WO2018140599A1 (en) | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | Benzothiophene and benzothiazole compounds and methods of use thereof |
| US11136308B2 (en) | 2017-01-26 | 2021-10-05 | Araxes Pharma Llc | Substituted quinazoline and quinazolinone compounds and methods of use thereof |
| WO2018140513A1 (en) | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer |
| US10745385B2 (en) | 2017-05-25 | 2020-08-18 | Araxes Pharma Llc | Covalent inhibitors of KRAS |
| CN110869357A (zh) | 2017-05-25 | 2020-03-06 | 亚瑞克西斯制药公司 | 化合物及其用于治疗癌症的使用方法 |
| MX2021000887A (es) | 2018-08-01 | 2021-03-31 | Araxes Pharma Llc | Compuestos espiroheterociclicos y metodos de uso de los mismos para el tratamiento de cancer. |
-
2017
- 2017-09-29 WO PCT/US2017/054363 patent/WO2018064510A1/en not_active Ceased
- 2017-09-29 US US15/721,021 patent/US10280172B2/en active Active
- 2017-09-29 CN CN201780073660.4A patent/CN110036010A/zh active Pending
- 2017-09-29 JP JP2019516992A patent/JP2019529484A/ja active Pending
- 2017-09-29 EP EP17781353.2A patent/EP3519402A1/en not_active Withdrawn
-
2019
- 2019-04-03 US US16/374,356 patent/US10723738B2/en active Active