JP2018513853A5 - - Google Patents
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- JP2018513853A5 JP2018513853A5 JP2017552484A JP2017552484A JP2018513853A5 JP 2018513853 A5 JP2018513853 A5 JP 2018513853A5 JP 2017552484 A JP2017552484 A JP 2017552484A JP 2017552484 A JP2017552484 A JP 2017552484A JP 2018513853 A5 JP2018513853 A5 JP 2018513853A5
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- JP
- Japan
- Prior art keywords
- alkyl
- compound according
- compound
- cycloalkyl
- heteroaryl
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims description 216
- 125000000217 alkyl group Chemical group 0.000 claims description 69
- -1 aminylalkylaminyl Chemical group 0.000 claims description 65
- 125000000623 heterocyclic group Chemical group 0.000 claims description 65
- 125000001072 heteroaryl group Chemical group 0.000 claims description 64
- 125000005843 halogen group Chemical group 0.000 claims description 58
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 56
- 125000004181 carboxyalkyl group Chemical group 0.000 claims description 52
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 51
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 50
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims description 46
- 125000003118 aryl group Chemical group 0.000 claims description 46
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims description 46
- 125000001188 haloalkyl group Chemical group 0.000 claims description 37
- 125000004966 cyanoalkyl group Chemical group 0.000 claims description 36
- 125000002837 carbocyclic group Chemical group 0.000 claims description 34
- 125000003545 alkoxy group Chemical group 0.000 claims description 33
- 102100029974 GTPase HRas Human genes 0.000 claims description 23
- 102100030708 GTPase KRas Human genes 0.000 claims description 23
- 101000584633 Homo sapiens GTPase HRas Proteins 0.000 claims description 23
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 23
- 125000004438 haloalkoxy group Chemical group 0.000 claims description 22
- 102100039788 GTPase NRas Human genes 0.000 claims description 19
- 101000744505 Homo sapiens GTPase NRas Proteins 0.000 claims description 19
- 101000584612 Homo sapiens GTPase KRas Proteins 0.000 claims description 18
- 239000008194 pharmaceutical composition Substances 0.000 claims description 18
- 125000000304 alkynyl group Chemical group 0.000 claims description 17
- 230000035772 mutation Effects 0.000 claims description 15
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 14
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 14
- 206010028980 Neoplasm Diseases 0.000 claims description 13
- 125000002947 alkylene group Chemical group 0.000 claims description 12
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims description 12
- 235000018102 proteins Nutrition 0.000 claims description 12
- 102000004169 proteins and genes Human genes 0.000 claims description 12
- 108090000623 proteins and genes Proteins 0.000 claims description 12
- 125000001424 substituent group Chemical group 0.000 claims description 12
- 201000011510 cancer Diseases 0.000 claims description 11
- 125000003386 piperidinyl group Chemical group 0.000 claims description 11
- 125000001153 fluoro group Chemical group F* 0.000 claims description 10
- 229910052757 nitrogen Inorganic materials 0.000 claims description 10
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims description 10
- 125000000151 cysteine group Chemical group N[C@@H](CS)C(=O)* 0.000 claims description 9
- 239000000651 prodrug Substances 0.000 claims description 9
- 229940002612 prodrug Drugs 0.000 claims description 9
- 150000003839 salts Chemical class 0.000 claims description 9
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 8
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 8
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 8
- 102200006538 rs121913530 Human genes 0.000 claims description 8
- 125000002393 azetidinyl group Chemical group 0.000 claims description 7
- 125000004103 aminoalkyl group Chemical group 0.000 claims description 6
- 125000005114 heteroarylalkoxy group Chemical group 0.000 claims description 6
- 125000002757 morpholinyl group Chemical group 0.000 claims description 6
- 102200124918 rs121913250 Human genes 0.000 claims description 6
- 125000003282 alkyl amino group Chemical group 0.000 claims description 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 4
- 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
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 4
- 208000035475 disorder Diseases 0.000 claims description 4
- 201000005787 hematologic cancer Diseases 0.000 claims description 4
- 125000002883 imidazolyl group Chemical group 0.000 claims description 4
- 230000002401 inhibitory effect Effects 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
- 230000001404 mediated effect Effects 0.000 claims description 4
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 4
- 125000001624 naphthyl group Chemical group 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
- 125000004076 pyridyl group Chemical group 0.000 claims description 4
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 4
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 4
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims description 4
- MDFFNEOEWAXZRQ-UHFFFAOYSA-N aminyl Chemical group [NH2] MDFFNEOEWAXZRQ-UHFFFAOYSA-N 0.000 claims description 3
- 230000005764 inhibitory process Effects 0.000 claims description 3
- 230000035755 proliferation Effects 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
- 206010027476 Metastases Diseases 0.000 claims description 2
- 229910019142 PO4 Inorganic materials 0.000 claims description 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-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
- 125000002619 bicyclic group Chemical group 0.000 claims description 2
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims description 2
- ZADPBFCGQRWHPN-UHFFFAOYSA-N boronic acid Chemical compound OBO ZADPBFCGQRWHPN-UHFFFAOYSA-N 0.000 claims description 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 2
- 230000003833 cell viability Effects 0.000 claims description 2
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims description 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 2
- 125000006222 dimethylaminomethyl group Chemical group [H]C([H])([H])N(C([H])([H])[H])C([H])([H])* 0.000 claims description 2
- 125000005879 dioxolanyl group Chemical group 0.000 claims description 2
- 230000000694 effects Effects 0.000 claims description 2
- 125000005241 heteroarylamino group Chemical group 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
- 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
- 125000002950 monocyclic group Chemical group 0.000 claims description 2
- 125000002911 monocyclic heterocycle group Chemical group 0.000 claims description 2
- 125000002971 oxazolyl group Chemical group 0.000 claims description 2
- 125000003566 oxetanyl group Chemical group 0.000 claims description 2
- 125000004043 oxo group Chemical group O=* 0.000 claims description 2
- 229910052760 oxygen Inorganic materials 0.000 claims description 2
- 239000001301 oxygen Substances 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
- 125000004193 piperazinyl group Chemical group 0.000 claims description 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims description 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 2
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims description 2
- 125000003107 substituted aryl group Chemical group 0.000 claims description 2
- 125000004632 tetrahydrothiopyranyl group Chemical group S1C(CCCC1)* 0.000 claims description 2
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims description 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 2
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 23
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 22
- 125000006728 (C1-C6) alkynyl group Chemical group 0.000 claims 15
- 239000000203 mixture Substances 0.000 claims 15
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 12
- 125000006727 (C1-C6) alkenyl group Chemical group 0.000 claims 4
- 102000008300 Mutant Proteins Human genes 0.000 claims 3
- 108010021466 Mutant Proteins Proteins 0.000 claims 3
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 2
- 125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 claims 1
- 125000000278 alkyl amino alkyl group Chemical group 0.000 claims 1
- XTKDAFGWCDAMPY-UHFFFAOYSA-N azaperone Chemical compound C1=CC(F)=CC=C1C(=O)CCCN1CCN(C=2N=CC=CC=2)CC1 XTKDAFGWCDAMPY-UHFFFAOYSA-N 0.000 claims 1
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 1
- 125000003003 spiro group Chemical group 0.000 claims 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 1
- 0 C*(*=C1)c2c1c(NC)c(C)cc2 Chemical compound C*(*=C1)c2c1c(NC)c(C)cc2 0.000 description 13
- 238000000034 method Methods 0.000 description 13
- 125000003342 alkenyl group Chemical group 0.000 description 4
- 125000004448 alkyl carbonyl group Chemical group 0.000 description 2
- 102200006614 rs104894229 Human genes 0.000 description 2
- 101710117545 C protein Proteins 0.000 description 1
- BDYKZMNDOYRQTR-UHFFFAOYSA-N CC(C)(C)c(c(O)ccc1)c1F Chemical compound CC(C)(C)c(c(O)ccc1)c1F BDYKZMNDOYRQTR-UHFFFAOYSA-N 0.000 description 1
- OOYBRAROSDTXQV-UHFFFAOYSA-N Cc(c(F)ccc1)c1OCP(O)(O)=O Chemical compound Cc(c(F)ccc1)c1OCP(O)(O)=O OOYBRAROSDTXQV-UHFFFAOYSA-N 0.000 description 1
- HFMDUDRMJQUVMN-UHFFFAOYSA-N Cc(c([nH]nc1)c1cc1)c1F Chemical compound Cc(c([nH]nc1)c1cc1)c1F HFMDUDRMJQUVMN-UHFFFAOYSA-N 0.000 description 1
- RIOSCUNPEBJRRM-UHFFFAOYSA-N Cc1cc(O)cc2c1cccc2 Chemical compound Cc1cc(O)cc2c1cccc2 RIOSCUNPEBJRRM-UHFFFAOYSA-N 0.000 description 1
- JCLJFOALEJVDAC-UHFFFAOYSA-N Cc1ccc2[nH]ncc2c1C Chemical compound Cc1ccc2[nH]ncc2c1C JCLJFOALEJVDAC-UHFFFAOYSA-N 0.000 description 1
- LFMWZTSOMGDDJU-UHFFFAOYSA-N Ic(cc1)ccc1I Chemical compound Ic(cc1)ccc1I LFMWZTSOMGDDJU-UHFFFAOYSA-N 0.000 description 1
- 125000005196 alkyl carbonyloxy group Chemical group 0.000 description 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 239000012039 electrophile Substances 0.000 description 1
- 238000002372 labelling Methods 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2021034710A JP2021098721A (ja) | 2015-04-10 | 2021-03-04 | 置換キナゾリン化合物およびその使用方法 |
Applications Claiming Priority (11)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562145705P | 2015-04-10 | 2015-04-10 | |
| US201562145818P | 2015-04-10 | 2015-04-10 | |
| US62/145,818 | 2015-04-10 | ||
| US62/145,705 | 2015-04-10 | ||
| US201562255891P | 2015-11-16 | 2015-11-16 | |
| US62/255,891 | 2015-11-16 | ||
| US201562265316P | 2015-12-09 | 2015-12-09 | |
| US201562265320P | 2015-12-09 | 2015-12-09 | |
| US62/265,316 | 2015-12-09 | ||
| US62/265,320 | 2015-12-09 | ||
| PCT/US2016/026573 WO2016164675A1 (en) | 2015-04-10 | 2016-04-08 | Substituted quinazoline compounds and methods of use thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021034710A Division JP2021098721A (ja) | 2015-04-10 | 2021-03-04 | 置換キナゾリン化合物およびその使用方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2018513853A JP2018513853A (ja) | 2018-05-31 |
| JP2018513853A5 true JP2018513853A5 (enExample) | 2019-04-18 |
Family
ID=55754477
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017552484A Withdrawn JP2018513853A (ja) | 2015-04-10 | 2016-04-08 | 置換キナゾリン化合物およびその使用方法 |
| JP2021034710A Pending JP2021098721A (ja) | 2015-04-10 | 2021-03-04 | 置換キナゾリン化合物およびその使用方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021034710A Pending JP2021098721A (ja) | 2015-04-10 | 2021-03-04 | 置換キナゾリン化合物およびその使用方法 |
Country Status (15)
| Country | Link |
|---|---|
| US (3) | US10246424B2 (enExample) |
| EP (1) | EP3280708B1 (enExample) |
| JP (2) | JP2018513853A (enExample) |
| KR (1) | KR20180005178A (enExample) |
| CN (1) | CN107849022A (enExample) |
| AU (1) | AU2016245864C1 (enExample) |
| BR (1) | BR112017021869A2 (enExample) |
| EA (1) | EA201792214A1 (enExample) |
| ES (1) | ES2898765T3 (enExample) |
| HK (1) | HK1248231A1 (enExample) |
| JO (1) | JO3707B1 (enExample) |
| MX (1) | MX382355B (enExample) |
| TW (1) | TW201702232A (enExample) |
| UY (1) | UY36612A (enExample) |
| WO (1) | WO2016164675A1 (enExample) |
Families Citing this family (220)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UY35464A (es) | 2013-03-15 | 2014-10-31 | Araxes Pharma Llc | Inhibidores covalentes de kras g12c. |
| WO2014143659A1 (en) | 2013-03-15 | 2014-09-18 | Araxes Pharma Llc | Irreversible covalent inhibitors of the gtpase k-ras 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 |
| WO2016049568A1 (en) | 2014-09-25 | 2016-03-31 | Araxes Pharma Llc | Methods and compositions for inhibition of ras |
| ES2826443T3 (es) | 2014-09-25 | 2021-05-18 | Araxes Pharma Llc | Inhibidores de proteínas mutantes KRAS G12C |
| AU2016245864C1 (en) * | 2015-04-10 | 2021-09-09 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
| MX2017013275A (es) | 2015-04-15 | 2018-01-26 | Araxes Pharma Llc | Inhibidores triciclicos fusionados de kras y metodos de uso de los mismos. |
| US10144724B2 (en) | 2015-07-22 | 2018-12-04 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
| EP3356339A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| US10647703B2 (en) | 2015-09-28 | 2020-05-12 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| WO2017058807A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| US10858343B2 (en) | 2015-09-28 | 2020-12-08 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| WO2017058915A1 (en) | 2015-09-28 | 2017-04-06 | 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 |
| WO2017058792A1 (en) | 2015-09-28 | 2017-04-06 | 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 |
| CA3005089A1 (en) * | 2015-11-16 | 2017-05-26 | Araxes Pharma Llc | 2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use thereof |
| WO2017100546A1 (en) | 2015-12-09 | 2017-06-15 | Araxes Pharma Llc | Methods for preparation of quinazoline derivatives |
| AU2016378723B2 (en) | 2015-12-22 | 2021-09-30 | SHY Therapeutics LLC | Compounds for the treatment of cancer and inflammatory disease |
| US10822312B2 (en) | 2016-03-30 | 2020-11-03 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use |
| 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 |
| EP3519402A1 (en) | 2016-09-29 | 2019-08-07 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| WO2018068017A1 (en) | 2016-10-07 | 2018-04-12 | Araxes Pharma Llc | Heterocyclic compounds as inhibitors of ras and methods of use thereof |
| EP4001269A1 (en) * | 2016-12-22 | 2022-05-25 | Amgen Inc. | Benzoisothiazole, isothiazolo[3,4-b]pyridine, quinazoline, phthalazine, pyrido[2,3-d]pyridazine and pyrido[2,3-d]pyrimidine derivatives as kras g12c inhibitors for treating lung, pancreatic or colorectal cancer |
| WO2018140512A1 (en) * | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | Fused bicyclic benzoheteroaromatic compounds and methods of use thereof |
| EP3573964A1 (en) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | Benzothiophene and benzothiazole compounds and methods of use thereof |
| WO2018140514A1 (en) | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | 1-(6-(3-hydroxynaphthalen-1-yl)quinazolin-2-yl)azetidin-1-yl)prop-2-en-1-one derivatives and similar compounds as kras g12c inhibitors for the treatment of 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 |
| US11279689B2 (en) | 2017-01-26 | 2022-03-22 | Araxes Pharma Llc | 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1 yl)prop-2-en-1-one derivatives and similar compounds as KRAS G12C modulators for treating cancer |
| JOP20190186A1 (ar) | 2017-02-02 | 2019-08-01 | Astellas Pharma Inc | مركب كينازولين |
| JOP20190272A1 (ar) | 2017-05-22 | 2019-11-21 | Amgen Inc | مثبطات kras g12c وطرق لاستخدامها |
| CN110831933A (zh) * | 2017-05-25 | 2020-02-21 | 亚瑞克西斯制药公司 | 喹唑啉衍生物作为突变kras、hras或nras的调节剂 |
| CA3063440A1 (en) * | 2017-05-25 | 2018-11-29 | Araxes Pharma Llc | Covalent inhibitors of kras |
| JP2020521741A (ja) * | 2017-05-25 | 2020-07-27 | アラクセス ファーマ エルエルシー | がんの処置のための化合物およびその使用の方法 |
| AU2018288841B2 (en) | 2017-06-21 | 2022-09-29 | SHY Therapeutics LLC | Compounds that interact with the Ras superfamily for the treatment of cancers, inflammatory diseases, Rasopathies, and fibrotic disease |
| ES2985118T3 (es) | 2017-09-08 | 2024-11-04 | Amgen Inc | Inhibidores de KRAS G12C y métodos de uso de los mismos |
| US10647715B2 (en) | 2017-11-15 | 2020-05-12 | Mirati Therapeutics, Inc. | KRas G12C inhibitors |
| MX2020005063A (es) | 2017-11-15 | 2021-01-08 | Mirati Therapeutics Inc | Inhibidores de kras g12c. |
| EP3741756B1 (en) | 2018-01-19 | 2023-11-01 | Medshine Discovery Inc. | Pyridone-pyrimidine derivative acting as krasg12c mutein inhibitor |
| TW201942115A (zh) * | 2018-02-01 | 2019-11-01 | 美商輝瑞股份有限公司 | 作為抗癌藥之經取代的喹唑啉和吡啶並嘧啶衍生物 |
| MX2020010836A (es) | 2018-05-04 | 2021-01-08 | Amgen Inc | Inhibidores de kras g12c y métodos para su uso. |
| US11045484B2 (en) | 2018-05-04 | 2021-06-29 | 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 |
| ES2986917T3 (es) | 2018-05-10 | 2024-11-13 | Amgen Inc | Inhibidores de KRAS G12C para el tratamiento del cáncer |
| MA52765A (fr) | 2018-06-01 | 2021-04-14 | Amgen Inc | Inhibiteurs de kras g12c et leurs procédés d'utilisation |
| EP3802537A1 (en) * | 2018-06-11 | 2021-04-14 | Amgen Inc. | Kras g12c inhibitors for treating cancer |
| WO2020050890A2 (en) | 2018-06-12 | 2020-03-12 | Amgen Inc. | Kras g12c inhibitors and methods of using the same |
| RS64641B1 (sr) | 2018-06-27 | 2023-10-31 | Bristol Myers Squibb Co | Supstituisana jedinjenja naftiridinona korisna kao aktivatori t ćelija |
| FI3814347T3 (fi) | 2018-06-27 | 2023-06-12 | Bristol Myers Squibb Co | Naftyridinoniyhdisteitä, jotka ovat käyttökelpoisia t-solun aktivoijina |
| JP2021176820A (ja) * | 2018-07-31 | 2021-11-11 | アステラス製薬株式会社 | キナゾリン化合物を有効成分とする医薬組成物 |
| JP2021176819A (ja) * | 2018-07-31 | 2021-11-11 | アステラス製薬株式会社 | キナゾリン化合物を有効成分とする医薬組成物 |
| CN112584833A (zh) * | 2018-08-01 | 2021-03-30 | 亚瑞克西斯制药公司 | 杂环螺化合物及其用于治疗癌症的使用方法 |
| HUE070338T2 (hu) | 2018-09-10 | 2025-05-28 | Mirati Therapeutics Inc | Kombinációs terápiák |
| AU2019340366B2 (en) | 2018-09-10 | 2025-01-02 | Mirati Therapeutics, Inc. | Combination therapies |
| 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 |
| CA3111980A1 (en) | 2018-09-10 | 2020-03-19 | Mirati Therapeutics, Inc. | Combination therapies |
| WO2020061103A1 (en) | 2018-09-18 | 2020-03-26 | Nikang Therapeutics, Inc. | Fused tricyclic ring derivatives as src homology-2 phosphatase inhibitors |
| TW202033518A (zh) | 2018-10-15 | 2020-09-16 | 美商美國禮來大藥廠 | Kras g12c 抑制劑 |
| BR112021007726A2 (pt) * | 2018-10-24 | 2021-07-27 | Araxes Pharma Llc | derivados de 2-(2-acriloil-2,6-diazaspiro[3.4] octan-6-il)-6-(1h-indazol-4-il)-benzonitrilo e compostos relacionados como inibidores de proteína kras mutante g12c para inibir metástase tumoral |
| 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 |
| CN113226321B (zh) * | 2018-10-26 | 2024-12-17 | 阿利安制药有限责任公司 | 吡唑基化合物及其使用方法 |
| RS66280B1 (sr) | 2018-11-09 | 2025-01-31 | Hoffmann La Roche | Jedinjenja sa kondenzovanim prstenovima |
| 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 |
| WO2020106640A1 (en) | 2018-11-19 | 2020-05-28 | 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 |
| US20220112192A1 (en) * | 2018-11-29 | 2022-04-14 | Araxes Pharma Llc | Compounds and methods of use thereof for treatment of cancer |
| CN113164418A (zh) | 2018-12-05 | 2021-07-23 | 米拉蒂治疗股份有限公司 | 组合疗法 |
| EP3898609A1 (en) | 2018-12-19 | 2021-10-27 | Shy Therapeutics LLC | Compounds that interact with the ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease |
| JP7592601B2 (ja) | 2019-01-10 | 2024-12-02 | ミラティ セラピューティクス， インコーポレイテッド | Ｋｒａｓ ｇ１２ｃ阻害剤 |
| WO2020147525A1 (zh) * | 2019-01-16 | 2020-07-23 | 上海璎黎药业有限公司 | 吗啉基喹唑啉化合物的制备方法及其中间体 |
| WO2020156285A1 (zh) * | 2019-01-29 | 2020-08-06 | 博瑞生物医药（苏州）股份有限公司 | 一种苯并吡啶酮杂环化合物及其用途 |
| CN111499634B (zh) * | 2019-01-31 | 2023-05-12 | 贝达药业股份有限公司 | 一种喹唑啉化合物及其在医药上的应用 |
| WO2020165732A1 (en) | 2019-02-12 | 2020-08-20 | Novartis Ag | Pharmaceutical combination comprising tno155 and a krasg12c inhibitor |
| EP3927701B1 (en) * | 2019-02-18 | 2024-11-06 | PI Industries Ltd. | A process for preparing anthranilic diamides and intermediates thereof |
| WO2020177629A1 (zh) * | 2019-03-01 | 2020-09-10 | 劲方医药科技(上海)有限公司 | 螺环取代的嘧啶并环类化合物，其制法与医药上的用途 |
| JOP20210241A1 (ar) | 2019-03-05 | 2023-01-30 | Astrazeneca Ab | مركبات مدمجة ثلاثية الحلقة مفيدة كعوامل مضادة للسرطان |
| CN113891749A (zh) * | 2019-03-28 | 2022-01-04 | 埃皮齐梅股份有限公司 | 喹啉衍生物及其用于治疗癌症的用途 |
| WO2020216190A1 (zh) * | 2019-04-22 | 2020-10-29 | 贝达药业股份有限公司 | 一种喹唑啉化合物及其在医药上的应用 |
| EP3738593A1 (en) | 2019-05-14 | 2020-11-18 | Amgen, Inc | Dosing of kras inhibitor for treatment of cancers |
| BR112021023359A2 (pt) * | 2019-05-20 | 2022-02-01 | 1200 Pharma Llc | Inibidores de g12c de kras e usos dos mesmos |
| KR20220011670A (ko) | 2019-05-21 | 2022-01-28 | 암젠 인크 | 고체 상태 형태 |
| EP3972972A1 (en) | 2019-05-21 | 2022-03-30 | Amgen Inc. | Solid state forms |
| EP3972963A1 (en) | 2019-05-21 | 2022-03-30 | Bayer Aktiengesellschaft | Identification and use of kras inhibitors |
| CN118745177A (zh) * | 2019-05-29 | 2024-10-08 | 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 |
| CN112110918B (zh) * | 2019-06-21 | 2023-08-22 | 劲方医药科技(上海)有限公司 | 螺环取代的嘧啶并环类化合物，其制法与医药上的用途 |
| TW202115089A (zh) * | 2019-07-01 | 2021-04-16 | 大陸商江蘇恆瑞醫藥股份有限公司 | 喹唑啉酮類衍生物、其製備方法及其在醫藥上的應用 |
| US20220363681A1 (en) * | 2019-08-16 | 2022-11-17 | Genfleet Therapeutics (Shanghai) Inc. | Oxo six-membered cyclopyrimidine compound, preparation method and medical use thereof |
| AR119821A1 (es) | 2019-08-28 | 2022-01-12 | Bristol Myers Squibb Co | Compuestos de piridopirimidinonilo sustituidos útiles como activadores de células t |
| EP4021444A4 (en) | 2019-08-29 | 2023-01-04 | Mirati Therapeutics, Inc. | KRAS G12D INHIBITORS |
| EP4031542B1 (en) * | 2019-09-18 | 2025-10-15 | Merck Sharp & Dohme LLC | Small molecule inhibitors of kras g12c mutant |
| US12122787B2 (en) | 2019-09-20 | 2024-10-22 | Shanghai Jemincare Pharmaceuticals Co., Ltd | Fused pyridone compound, and preparation method therefor and use thereof |
| CN118619971A (zh) * | 2019-09-20 | 2024-09-10 | 上海济煜医药科技有限公司 | 稠合吡啶酮类化合物及其制备方法和应用 |
| CA3152025A1 (en) | 2019-09-24 | 2021-04-01 | David BRIERE | Combination therapies |
| CN112552295A (zh) * | 2019-09-25 | 2021-03-26 | 北京加科思新药研发有限公司 | Kras突变蛋白抑制剂 |
| CN112574224A (zh) * | 2019-09-30 | 2021-03-30 | 上海迪诺医药科技有限公司 | Kras g12c抑制剂及其应用 |
| KR20220106980A (ko) | 2019-10-28 | 2022-08-01 | 머크 샤프 앤드 돔 코포레이션 | Kras g12c 돌연변이체의 소분자 억제제 |
| WO2021091982A1 (en) | 2019-11-04 | 2021-05-14 | Revolution Medicines, Inc. | Ras inhibitors |
| PH12022550988A1 (en) | 2019-11-04 | 2023-10-09 | Revolution Medicines Inc | Ras inhibitors |
| CN114901366A (zh) | 2019-11-04 | 2022-08-12 | 锐新医药公司 | Ras抑制剂 |
| WO2021088458A1 (en) * | 2019-11-04 | 2021-05-14 | Jacobio Pharmaceuticals Co., Ltd. | Kras mutant protein inhibitor |
| WO2021093758A1 (zh) * | 2019-11-15 | 2021-05-20 | 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 |
| WO2021106230A1 (ja) | 2019-11-29 | 2021-06-03 | 大鵬薬品工業株式会社 | 新規なフェノール化合物又はその塩 |
| WO2021106231A1 (en) * | 2019-11-29 | 2021-06-03 | Taiho Pharmaceutical Co., Ltd. | A compound having inhibitory activity against kras g12d mutation |
| WO2021109737A1 (zh) * | 2019-12-02 | 2021-06-10 | 上海璎黎药业有限公司 | 一种含氧杂环化合物、其制备方法及应用 |
| CN113024544B (zh) * | 2019-12-09 | 2024-07-02 | 武汉誉祥医药科技有限公司 | 一种含氰基并杂环化合物及其用途 |
| CN114828964B (zh) * | 2019-12-11 | 2023-11-24 | 伊莱利利公司 | Kras g12c抑制剂 |
| WO2021120890A1 (en) | 2019-12-20 | 2021-06-24 | Novartis Ag | Pyrazolyl derivatives useful as anti-cancer agents |
| WO2021127429A1 (en) | 2019-12-20 | 2021-06-24 | Mirati Therapeutics, Inc. | Sos1 inhibitors |
| EP4081516B1 (en) | 2019-12-23 | 2025-07-30 | Bristol-Myers Squibb Company | Substituted quinazolinyl compounds useful as t cell activators |
| AR120823A1 (es) | 2019-12-23 | 2022-03-23 | Bristol Myers Squibb Co | Compuestos bicíclicos sustituidos útiles como activadores de células t |
| KR20220120624A (ko) | 2019-12-23 | 2022-08-30 | 브리스톨-마이어스 스큅 컴퍼니 | T 세포 활성화제로서 유용한 치환된 피페라진 유도체 |
| WO2021129820A1 (zh) * | 2019-12-27 | 2021-07-01 | 微境生物医药科技(上海)有限公司 | 含螺环的喹唑啉化合物 |
| WO2021138391A1 (en) | 2019-12-30 | 2021-07-08 | Tyra Biosciences, Inc. | Indazole compounds |
| 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 |
| TW202140450A (zh) * | 2020-02-24 | 2021-11-01 | 大陸商泰勵生物科技（上海）有限公司 | 用於癌症治療的ｋｒａｓ抑制劑 |
| WO2021190467A1 (zh) | 2020-03-25 | 2021-09-30 | 微境生物医药科技(上海)有限公司 | 含螺环的喹唑啉化合物 |
| 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 |
| AU2021293228A1 (en) | 2020-06-18 | 2023-02-09 | Revolution Medicines, Inc. | Methods for delaying, preventing, and treating acquired resistance to RAS inhibitors |
| WO2021259331A1 (zh) * | 2020-06-24 | 2021-12-30 | 南京明德新药研发有限公司 | 八元含n杂环类化合物 |
| CA3191279A1 (en) | 2020-08-28 | 2022-03-03 | Yi Liu | Heterocyclic compounds and uses thereof |
| CN116209438A (zh) | 2020-09-03 | 2023-06-02 | 锐新医药公司 | 使用sos1抑制剂治疗具有shp2突变的恶性疾病 |
| 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 |
| AU2021340716A1 (en) | 2020-09-11 | 2023-03-30 | Mirati Therapeutics, Inc. | Crystalline forms of a KRas G12C inhibitor |
| JP2023541916A (ja) | 2020-09-15 | 2023-10-04 | レボリューション メディシンズ インコーポレイテッド | がんの治療における、ｒａｓ阻害剤としてのインドール誘導体 |
| MX2023003338A (es) | 2020-09-23 | 2023-06-14 | Erasca Inc | Piridonas y pirimidonas tricíclicas. |
| WO2022068921A1 (zh) * | 2020-09-30 | 2022-04-07 | 上海医药集团股份有限公司 | 一种喹唑啉类化合物及其应用 |
| AU2021370660A1 (en) * | 2020-10-27 | 2023-06-08 | Amgen Inc. | Heterocyclic spiro compounds and methods of use |
| EP4240489A4 (en) * | 2020-11-03 | 2024-09-25 | Mirati Therapeutics, Inc. | KRAS-G12D INHIBITORS |
| CN120887884A (zh) * | 2020-11-06 | 2025-11-04 | 泰励生物科技（上海）有限公司 | 用于癌症治疗的KRas抑制剂 |
| TWI880049B (zh) | 2020-12-04 | 2025-04-11 | 美商美國禮來大藥廠 | Kras g12c抑制劑 |
| CN112574127B (zh) * | 2020-12-09 | 2022-11-01 | 深圳湾实验室 | 喹唑啉类化合物及其制备方法、药物组合物及其应用 |
| MX2023007084A (es) | 2020-12-15 | 2023-08-30 | Mirati Therapeutics Inc | Inhibidores de pan-kras de azaquinazolina. |
| EP4262803A4 (en) | 2020-12-16 | 2025-03-12 | Mirati Therapeutics, Inc. | Tetrahydropyridopyrimidine pan-kras inhibitors |
| WO2022127847A1 (zh) * | 2020-12-17 | 2022-06-23 | 广东东阳光药业有限公司 | 嘧啶酮衍生物及其在药物中的应用 |
| WO2022133345A1 (en) | 2020-12-18 | 2022-06-23 | Erasca, Inc. | Tricyclic pyridones and pyrimidones |
| WO2022140246A1 (en) | 2020-12-21 | 2022-06-30 | Hangzhou Jijing Pharmaceutical Technology Limited | Methods and compounds for targeted autophagy |
| CA3202355A1 (en) | 2020-12-22 | 2022-06-30 | Jiping Fu | 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 |
| WO2022152313A1 (zh) * | 2021-01-18 | 2022-07-21 | 成都百裕制药股份有限公司 | 嘧啶衍生物及其在医药上的应用 |
| WO2022184178A1 (en) * | 2021-03-05 | 2022-09-09 | Jacobio Pharmaceuticals Co., Ltd. | Kras g12d inhibitors |
| CN115304603B (zh) * | 2021-05-07 | 2024-04-09 | 药雅科技(上海)有限公司 | 喹唑啉类抑制剂的制备及其应用 |
| CN115073450A (zh) * | 2021-03-15 | 2022-09-20 | 药雅科技(上海)有限公司 | Krasg12c突变蛋白抑制剂的制备及其应用 |
| CN115490689B (zh) * | 2021-06-17 | 2024-04-09 | 药雅科技(上海)有限公司 | 不可逆krasg12c抑制剂的制备及其应用 |
| TWI814234B (zh) * | 2021-03-15 | 2023-09-01 | 大陸商藥雅科技（上海）有限公司 | 突變蛋白抑制劑的製備及其應用 |
| CN115141215B (zh) * | 2021-03-30 | 2023-09-15 | 上海德琪医药科技有限公司 | Kras g12d蛋白抑制剂和其用途 |
| CN118852330A (zh) | 2021-05-05 | 2024-10-29 | 锐新医药公司 | 用于治疗癌症的ras抑制剂 |
| AU2022270116A1 (en) | 2021-05-05 | 2023-12-21 | Revolution Medicines, Inc. | Ras inhibitors |
| US20240293558A1 (en) | 2021-06-16 | 2024-09-05 | 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 |
| WO2023284730A1 (en) | 2021-07-14 | 2023-01-19 | Nikang Therapeutics, Inc. | Alkylidene derivatives as kras inhibitors |
| EP4373822A2 (en) | 2021-07-23 | 2024-05-29 | Theras Inc. | Compositions and methods for inhibition of ras |
| WO2023031781A1 (en) | 2021-09-01 | 2023-03-09 | Novartis Ag | Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers |
| EP4389751A1 (en) * | 2021-09-03 | 2024-06-26 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| US20250145589A1 (en) | 2021-09-22 | 2025-05-08 | Sichuan Huiyu Pharmaceutical Co., Ltd. | Pyridine derivative and use thereof |
| AR127308A1 (es) | 2021-10-08 | 2024-01-10 | Revolution Medicines Inc | Inhibidores ras |
| CA3234517A1 (en) | 2021-10-22 | 2023-04-27 | Xin Li | Nitrogen-containing tetracyclic compound, preparation method therefor, and medical use thereof |
| 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 |
| CN118434740A (zh) * | 2021-12-31 | 2024-08-02 | 上海医药集团股份有限公司 | 一种喹唑啉类化合物及其应用 |
| EP4472980A2 (en) * | 2022-02-03 | 2024-12-11 | Mirati Therapeutics, Inc. | Quinazoline pan-kras inhibitors |
| 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 |
| CN119136805A (zh) | 2022-03-04 | 2024-12-13 | 伊莱利利公司 | 包括kras g12c抑制剂和shp2抑制剂的治疗方法 |
| 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 |
| JP2025509886A (ja) | 2022-03-28 | 2025-04-11 | ニカング セラピューティクス， インコーポレイテッド | サイクリン依存性キナーゼ２阻害剤としてのスルホンアミド誘導体 |
| CA3247183A1 (en) | 2022-04-08 | 2023-10-12 | Eli Lilly And Company | TREATMENT METHOD INCLUDING KRAS G12C INHIBITORS AND AURORA A INHIBITORS |
| WO2023199180A1 (en) | 2022-04-11 | 2023-10-19 | Novartis Ag | Therapeutic uses of a krasg12c inhibitor |
| CA3256645A1 (en) | 2022-05-06 | 2025-04-23 | Chugai Seiyaku Kabushiki Kaisha | CYCLIC COMPOUND HAVING A SELECTIVE KRAS INHIBITORY EFFECT ON HRAS AND NRAS |
| EP4536363A1 (en) | 2022-06-08 | 2025-04-16 | Nikang Therapeutics, Inc. | Sulfamide derivatives as cyclin-dependent kinase 2 inhibitors |
| CN120504682A (zh) | 2022-06-10 | 2025-08-19 | 锐新医药公司 | 大环ras抑制剂 |
| WO2023246914A1 (zh) * | 2022-06-24 | 2023-12-28 | 南京明德新药研发有限公司 | 杂环取代的嘧啶并吡喃类化合物及其应用 |
| JP2025525938A (ja) * | 2022-08-05 | 2025-08-07 | セラス， インコーポレイテッド | Ｋｒａｓの阻害のための組成物及び方法 |
| WO2024030647A1 (en) * | 2022-08-05 | 2024-02-08 | Theras, Inc. | Compositions and methods for inhibition of ras |
| CN119731180A (zh) | 2022-08-05 | 2025-03-28 | 金橘生物科技公司 | 杂环化合物及其用途 |
| JP2025528836A (ja) | 2022-08-17 | 2025-09-02 | ツリーライン バイオサイエンシズ インコーポレイテッド | ピリドピリミジンＫＲａｓ阻害剤 |
| GB202212641D0 (en) | 2022-08-31 | 2022-10-12 | Jazz Pharmaceuticals Ireland Ltd | Novel compounds |
| CN117659050A (zh) * | 2022-09-08 | 2024-03-08 | 深圳福沃药业有限公司 | 用于治疗癌症的kras突变抑制剂的喹唑啉杂环类衍生物 |
| IL320639A (en) | 2022-11-09 | 2025-07-01 | Revolution Medicines Inc | Compounds, complexes and methods for their preparation and use |
| 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 |
| KR20250109197A (ko) | 2022-11-21 | 2025-07-16 | 트리라인 바이오사이언시스, 인크. | 스피로환식 디하이드로피라노피리미딘 KRas 억제제 |
| WO2024109233A1 (zh) * | 2022-11-22 | 2024-05-30 | 四川汇宇制药股份有限公司 | 一种嘧啶并芳环化合物及其制备方法和用途 |
| EP4655298A1 (en) * | 2023-01-24 | 2025-12-03 | Theras Inc. | Compositions and methods for inhibition of ras |
| TW202504611A (zh) | 2023-03-30 | 2025-02-01 | 美商銳新醫藥公司 | 用於誘導ｒａｓ ｇｔｐ水解之組合物及其用途 |
| AU2024253668A1 (en) | 2023-04-07 | 2025-11-13 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| CR20250420A (es) | 2023-04-07 | 2025-11-20 | Revolution Medicines Inc | Inhibidores macrocíclicos de ras |
| WO2024216016A1 (en) | 2023-04-14 | 2024-10-17 | Revolution Medicines, Inc. | Crystalline forms of a ras inhibitor |
| WO2024216048A1 (en) | 2023-04-14 | 2024-10-17 | Revolution Medicines, Inc. | Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof |
| WO2024229406A1 (en) | 2023-05-04 | 2024-11-07 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| AU2024276994A1 (en) | 2023-05-24 | 2025-10-23 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| CN121219016A (zh) | 2023-06-02 | 2025-12-26 | 第一三共株式会社 | 抗-her3抗体-药物缀合物和rasg12c抑制剂的组合 |
| TW202502779A (zh) | 2023-06-30 | 2025-01-16 | 美商金橘生物科技公司 | 取代的雜芳族胺及其用途 |
| 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 |
| WO2025034702A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Rmc-6291 for use in the treatment of ras protein-related disease or disorder |
| TW202528315A (zh) | 2023-09-21 | 2025-07-16 | 美商樹線生物科學公司 | 螺環二氫哌喃并吡啶ＫＲａｓ抑制劑 |
| WO2025072462A1 (en) | 2023-09-27 | 2025-04-03 | Nikang Therapeutics, Inc. | Sulfonamide derivatives as cyclin-dependent kinase 2 inhibitors |
| TW202530228A (zh) | 2023-10-12 | 2025-08-01 | 美商銳新醫藥公司 | Ｒａｓ抑制劑 |
| TW202535891A (zh) | 2023-10-20 | 2025-09-16 | 美商默沙東有限責任公司 | Ｋｒａｓ蛋白之小分子抑制劑 |
| 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 |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025245127A1 (en) | 2024-05-21 | 2025-11-27 | Treeline Biosciences, Inc. | Spirocyclic dihydropyranopyrimidine kras inhibitors |
| WO2025254394A1 (ko) * | 2024-06-05 | 2025-12-11 | 연세대학교 산학협력단 | Slc1a5 변이체 미토콘드리아 글루타민 수송체의 억제제를 포함하는 항암용 조성물 |
| US20250375445A1 (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 |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| 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 |
Family Cites Families (213)
| 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 |
| US5033252A (en) | 1987-12-23 | 1991-07-23 | Entravision, Inc. | Method of packaging and sterilizing a pharmaceutical product |
| US5052558A (en) | 1987-12-23 | 1991-10-01 | Entravision, Inc. | Packaged 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 |
| ATE141502T1 (de) | 1991-01-15 | 1996-09-15 | Alcon Lab Inc | Verwendung von karrageenan in topischen ophthalmologischen zusammensetzungen |
| 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 |
| US6017696A (en) | 1993-11-01 | 2000-01-25 | Nanogen, Inc. | Methods for electronic stringency control for molecular biological analysis and diagnostics |
| US6051380A (en) | 1993-11-01 | 2000-04-18 | Nanogen, Inc. | Methods and procedures 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 |
| AU694187B2 (en) | 1994-02-07 | 1998-07-16 | Beckman Coulter, Inc. | Ligase/polymerase-mediated genetic bit analysis TM 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 |
| US5861510A (en) | 1995-04-20 | 1999-01-19 | Pfizer Inc | Arylsulfonyl hydroxamic acid derivatives as MMP and TNF inhibitors |
| FR2734816B1 (fr) | 1995-05-31 | 1997-07-04 | Adir | Nouveaux aryl (alkyl) propylamides, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| DE69638269D1 (de) | 1995-06-14 | 2010-11-18 | Univ California | Hochaffine humane antikörper gegen tumorantigene |
| PT780386E (pt) | 1995-12-20 | 2003-02-28 | Hoffmann La Roche | Inibidores de metaloprotease de matriz |
| 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 |
| CN1225639A (zh) | 1996-07-18 | 1999-08-11 | 美国辉瑞有限公司 | 基于次膦酸酯的基质金属蛋白酶抑制剂 |
| SK21499A3 (en) | 1996-08-23 | 2000-05-16 | Pfizer | Arylsulfonylamino hydroxamic acid derivatives |
| US5777324A (en) | 1996-09-19 | 1998-07-07 | Sequenom, Inc. | Method and apparatus for maldi analysis |
| EP0950059B1 (en) | 1997-01-06 | 2004-08-04 | Pfizer Inc. | Cyclic sulfone derivatives |
| SK283963B6 (sk) | 1997-02-03 | 2004-06-08 | Pfizer Products Inc. | Deriváty arylsulfonylaminohydroxamovej kyseliny, farmaceutický prostriedok, spôsob inhibície matričných metaloproteináz alebo produkcie faktora nekrózy nádorov |
| GB9702194D0 (en) | 1997-02-04 | 1997-03-26 | Lilly Co Eli | Sulphonide derivatives |
| WO1998034915A1 (en) | 1997-02-07 | 1998-08-13 | Pfizer Inc. | N-hydroxy-beta-sulfonyl-propionamide derivatives and their use as inhibitors of matrix metalloproteinases |
| JP3710489B2 (ja) | 1997-02-11 | 2005-10-26 | ファイザー・インク | アリールスルホニルヒドロキサム酸誘導体 |
| EP0968201A2 (en) | 1997-02-17 | 2000-01-05 | Fujisawa Pharmaceutical Co., Ltd. | New aminopiperazine derivatives |
| US6002008A (en) * | 1997-04-03 | 1999-12-14 | American Cyanamid Company | Substituted 3-cyano quinolines |
| UA73073C2 (uk) | 1997-04-03 | 2005-06-15 | Уайт Холдінгз Корпорейшн | Заміщені 3-ціанохіноліни, спосіб їх одержання та фармацевтична композиція |
| US5919626A (en) | 1997-06-06 | 1999-07-06 | Orchid Bio Computer, Inc. | Attachment of unmodified nucleic acids to silanized solid phase surfaces |
| IL133389A0 (en) | 1997-06-17 | 2001-04-30 | Schering Corp | Novel n-substituted urea inhibitors of farnesyl-protein transferase |
| UA61963C2 (en) | 1997-08-08 | 2003-12-15 | Pfizer Prod Inc | Aryloxysulfonylaminohydroxamic 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 |
| BR9813835A (pt) | 1997-12-22 | 2000-10-10 | Du Pont Pharm Co | Composto, composição farmacêutica e método de tratamento ou prevenção de uma desordem tromboembólica |
| 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 |
| WO1999067641A2 (en) | 1998-06-24 | 1999-12-29 | 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 |
| GB9912961D0 (en) | 1999-06-03 | 1999-08-04 | Pfizer Ltd | Metalloprotease inhibitors |
| 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 |
| ES2447419T3 (es) | 1999-09-13 | 2014-03-12 | Nugen Technologies, Inc. | Composiciones para la amplificación isotérmica lineal de secuencias de polinucleótidos |
| HK1048775B (en) * | 2000-03-13 | 2006-01-20 | Wyeth Holdings Corporation | Use of cyanoquinolines for treating or inhibiting colonic polyps |
| IL151124A0 (en) | 2000-03-21 | 2003-04-10 | Procter & Gamble | Heterocyclic side chain containing metalloprotease inhibitors |
| US6689779B2 (en) | 2000-06-05 | 2004-02-10 | Dong A Pharm. Co., Ltd. | 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 |
| WO2002016351A1 (en) | 2000-08-18 | 2002-02-28 | Cor Therapeutics, Inc. | Quinazoline derivatives as kinase inhibitors |
| 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 |
| EP1390034A4 (en) | 2001-04-03 | 2005-07-13 | Merck & Co Inc | N-SUBSTITUTED NONARYL HETEROCYCLO AMIDYL-NMDA / NR2B ANTAGONISTS |
| JP4310109B2 (ja) | 2001-04-26 | 2009-08-05 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | ピラゾリル基を置換基として有する含窒素縮合環化合物およびその医薬組成物 |
| 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 |
| MXPA05003632A (es) | 2002-10-11 | 2005-06-03 | Astrazeneca Ab | Derivados de piperidina 1, 4-disustituidos y su uso como inhibidores de 11-beta-hidroesteroide deshidrogenasa humana de tipo 1 (11betahsd1). |
| 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. |
| NZ542680A (en) | 2003-03-12 | 2008-08-29 | Kudos Pharm Ltd | Phthalazinone derivatives |
| US20050119266A1 (en) | 2003-10-01 | 2005-06-02 | Yan Shi | Pyrrolidine and piperidine derivatives as factor Xa inhibitors |
| SE0302811D0 (sv) | 2003-10-23 | 2003-10-23 | Astrazeneca Ab | Novel compounds |
| 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 |
| WO2005070891A2 (en) | 2004-01-23 | 2005-08-04 | Amgen Inc | Compounds and methods of use |
| 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 |
| US20060167044A1 (en) | 2004-12-20 | 2006-07-27 | Arnaiz Damian O | Piperidine derivatives and their use as anti-inflammatory agents |
| 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 |
| US20090264415A2 (en) | 2004-12-30 | 2009-10-22 | Steven De Jonghe | Pyrido(3,2-d)pyrimidines and pharmaceutical compositions useful for medical treatment |
| 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 |
| JP2008543888A (ja) | 2005-06-24 | 2008-12-04 | ギリアード サイエンシーズ， インコーポレイテッド | ピリド（３，２−ｄ）ピリミジン、およびＣ型肝炎を治療するのに有用な医薬組成物 |
| CN101304976A (zh) | 2005-10-11 | 2008-11-12 | 因特蒙公司 | 病毒复制抑制剂 |
| JP2009519349A (ja) | 2005-12-15 | 2009-05-14 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｃｂ２受容体を変調する化合物 |
| PE20070978A1 (es) | 2006-02-14 | 2007-11-15 | Novartis Ag | COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks) |
| AU2007233709A1 (en) | 2006-03-31 | 2007-10-11 | Novartis Ag | Organic compounds |
| EP2059515A2 (en) | 2006-04-12 | 2009-05-20 | Pfizer Limited | Pyrrolidine derivatives as modulators of chemokine ccr5 receptors |
| US20090306048A1 (en) | 2006-06-16 | 2009-12-10 | John Paul Kilburn | Pharmaceutical use of substituted piperidine carboxamides |
| RU2009101911A (ru) | 2006-06-22 | 2010-07-27 | Биовитрум Аб (Пабл) (Se) | Производные пиридина и пиразина в качестве ингибиторов mnk-киназы |
| 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 |
| KR20090066287A (ko) | 2006-09-15 | 2009-06-23 | 쉐링 코포레이션 | 통증, 당뇨병, 및 지질 대사 장애의 치료방법 |
| CN101679261A (zh) | 2007-03-09 | 2010-03-24 | 阿斯利康(瑞典)有限公司 | 哌嗪和哌啶mGluR5增效剂 |
| NZ579833A (en) | 2007-04-16 | 2012-11-30 | Abbott Lab | 7-substituted indole mcl-1 inhibitors |
| AU2009229157B2 (en) | 2008-03-28 | 2015-01-29 | 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 |
| WO2010027746A2 (en) | 2008-08-25 | 2010-03-11 | Irm Llc | Hedgehog pathway modulators |
| 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 |
| MY153880A (en) | 2009-04-20 | 2015-04-15 | Hoffmann La Roche | Proline derivatives as cathepsin inhibitors |
| RU2011147181A (ru) | 2009-04-22 | 2013-05-27 | Янссен Фармацевтика Нв | Азетидинилдиамиды в качестве ингибиторов моноациглицерин-липазы |
| SE533816C2 (sv) | 2009-05-06 | 2011-01-25 | Tetra Laval Holdings & Finance | Förfarande för framställning av kartongflaskor |
| WO2010141817A1 (en) | 2009-06-05 | 2010-12-09 | Janssen Pharmaceutica Nv | Heteroaryl-substituted spirocyclic diamine urea modulators of fatty acid amide hydrolase |
| 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 |
| CA2766873C (en) | 2009-06-29 | 2018-08-21 | Agios Pharmaceuticals, Inc. | Therapeutic compositions and related methods of use |
| 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 |
| PH12012500491A1 (en) | 2009-09-09 | 2018-03-21 | Celgene Avilomics Res Inc | P13 kinase inhibitors and uses thereof |
| BR112012018386A8 (pt) | 2009-12-22 | 2017-12-19 | Vertex Pharma | "inibidores isoindolinona de fosfatidilinositol 3-quinase" |
| BR112012015721A2 (pt) | 2009-12-30 | 2017-09-26 | Avila Therapeutics Inc | modificação covalente de proteínas dirigida por ligante |
| PH12012501532A1 (en) | 2010-01-29 | 2012-10-22 | Otsuka Pharma Co Ltd | Di-substituted pyridine derivatives as anticancers |
| JP2013520998A (ja) | 2010-03-03 | 2013-06-10 | オーエスアイ・ファーマシューティカルズ，エルエルシー | インスリン様増殖因子−１受容体キナーゼ阻害剤に対する抗癌反応の予測に役立つ生物学的マーカー |
| CN102803227B (zh) | 2010-03-16 | 2016-01-20 | 默克专利有限公司 | 吗啉基喹唑啉 |
| AU2011246067A1 (en) | 2010-04-28 | 2012-09-27 | Daiichi Sankyo Company, Limited | [5,6] heterocyclic compound |
| 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 |
| US20110319290A1 (en) | 2010-06-08 | 2011-12-29 | Nugen Technologies, Inc. | Methods and Compositions for Multiplex Sequencing |
| US8658131B2 (en) | 2010-06-21 | 2014-02-25 | Washington University | Compounds comprising 4-benzoylpiperidine as a sigma-1-selective ligand |
| DK2597955T3 (en) | 2010-07-30 | 2016-03-14 | Onco Therapy Science Inc | QUINOLINE DERIVATIVES AND MILK INHIBITORS CONTAINING THESE |
| AU2011296068B2 (en) | 2010-09-03 | 2015-07-09 | Janssen Pharmaceutica Nv | Di-azetidinyl diamide as monoacylglycerol lipase inhibitors |
| EP2621923B1 (en) | 2010-09-29 | 2017-03-29 | Intervet International B.V. | 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 |
| JP2014504269A (ja) * | 2010-11-05 | 2014-02-20 | グラクソスミスクライン、インテレクチュアル、プロパティー、ナンバー２、リミテッド | 化学化合物 |
| WO2012174489A2 (en) | 2011-06-15 | 2012-12-20 | The Ohio State University | Small molecule composite surfaces as inhibitors of protein-protein interactions |
| BR112013033417A2 (pt) | 2011-06-29 | 2016-08-16 | Otsuka Pharma Co Ltd | compostos terapêuticos e métodos relacionados de uso |
| 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 |
| WO2013106641A1 (en) | 2012-01-13 | 2013-07-18 | Bristol-Myers Squibb Company | Thiazolyl- or thiadiazolyl-substituted pyridyl compounds useful as kinase inhibitors |
| 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 |
| MX2014013475A (es) | 2012-05-09 | 2015-05-15 | Gradalis Inc | Rna de horquilla corta bifuncional (bi-shrna) especifico para mutaciones kras de un solo nucleotido. |
| JO3300B1 (ar) | 2012-06-06 | 2018-09-16 | Novartis Ag | مركبات وتركيبات لتعديل نشاط egfr |
| PL2872491T3 (pl) | 2012-07-11 | 2021-12-13 | Blueprint Medicines Corporation | Inhibitory receptora czynnika wzrostu fibroblastów |
| TW201414737A (zh) | 2012-07-13 | 2014-04-16 | 必治妥美雅史谷比公司 | 作爲激酶抑制劑之咪唑并三□甲腈 |
| WO2014030743A1 (ja) | 2012-08-24 | 2014-02-27 | 武田薬品工業株式会社 | 複素環化合物 |
| MX386085B (es) | 2012-11-01 | 2025-03-18 | Infinity Pharmaceuticals Inc | Tratamiento de canceres utilizando moduladores de las isoformas de pi3 cinasa |
| BR112015022417A2 (pt) | 2013-03-14 | 2017-07-18 | Convergene Llc | métodos e composições para inibição de proteínas contendo bromodomínio |
| TW201524952A (zh) | 2013-03-15 | 2015-07-01 | Araxes Pharma Llc | Ｋｒａｓ ｇ１２ｃ之共價抑制劑 |
| WO2014143659A1 (en) * | 2013-03-15 | 2014-09-18 | Araxes Pharma Llc | Irreversible covalent inhibitors of the gtpase k-ras g12c |
| UY35464A (es) * | 2013-03-15 | 2014-10-31 | Araxes Pharma Llc | Inhibidores covalentes de kras g12c. |
| GB2538216A (en) | 2013-06-13 | 2016-11-16 | Biodesy Inc | Method of screening candidate biochemical entities targeting a target biochemical entity |
| CN108440515B (zh) | 2013-07-03 | 2022-05-03 | 卡尔约药物治疗公司 | 取代的苯并呋喃基和苯并噁唑基化合物及其用途 |
| SG10201900025UA (en) | 2013-07-31 | 2019-02-27 | Merck Patent Gmbh | Pyridines, pyrimidines, and pyrazines, as btk inhibitors and uses thereof |
| 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 |
| KR20160076519A (ko) * | 2013-10-10 | 2016-06-30 | 아락세스 파마 엘엘씨 | Kras g12c 억제제 |
| US9376559B2 (en) | 2013-11-22 | 2016-06-28 | Exxonmobil Chemical Patents Inc. | Reverse staged impact copolymers |
| WO2015108992A1 (en) | 2014-01-15 | 2015-07-23 | Blueprint Medicines Corporation | Heterobicyclic compounds and their use as fgfr4 receptor inhibitors |
| EP3102579B1 (en) | 2014-02-03 | 2019-04-10 | Cadila Healthcare Limited | Heterocyclic compounds |
| MX377384B (es) | 2014-03-20 | 2025-03-10 | Capella Therapeutics Inc | Derivados de bencimidazol como inhibidores de tirosina cinasa erbb para el tratamiento del cáncer. |
| EP3124482B1 (en) | 2014-03-24 | 2019-09-11 | Guangdong Zhongsheng Pharmaceutical Co., Ltd | Quinoline derivatives as smo inhibitors |
| EP3148981A4 (en) | 2014-05-30 | 2017-11-08 | The Trustees of Columbia University in the City of New York | Multivalent ras binding compounds |
| WO2015200795A1 (en) | 2014-06-27 | 2015-12-30 | Celgene Corporation | Compositions and methods for inducing conformational changes in cereblon other e3 ubiquitin ligases |
| JO3556B1 (ar) | 2014-09-18 | 2020-07-05 | Araxes Pharma Llc | علاجات مدمجة لمعالجة السرطان |
| 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 |
| ES2826443T3 (es) | 2014-09-25 | 2021-05-18 | Araxes Pharma Llc | Inhibidores de proteínas mutantes KRAS G12C |
| HK1245677A1 (zh) | 2015-01-23 | 2018-08-31 | Aclaris Therapeutics, Inc. | 用於治疗炎症和癌症的杂环itk抑制剂 |
| AU2016245864C1 (en) | 2015-04-10 | 2021-09-09 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
| MX2017013275A (es) | 2015-04-15 | 2018-01-26 | Araxes Pharma Llc | Inhibidores triciclicos fusionados de kras y metodos de uso de los mismos. |
| US10144724B2 (en) | 2015-07-22 | 2018-12-04 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
| EP3325447A1 (en) | 2015-07-22 | 2018-05-30 | Araxes Pharma LLC | Substituted quinazoline compounds and their use as inhibitors of g12c mutant kras, hras and/or nras proteins |
| EP3356339A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| WO2017058792A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| US10647703B2 (en) | 2015-09-28 | 2020-05-12 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| US10858343B2 (en) | 2015-09-28 | 2020-12-08 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| WO2017058807A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| WO2017058915A1 (en) | 2015-09-28 | 2017-04-06 | 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 |
| WO2017070256A2 (en) | 2015-10-19 | 2017-04-27 | Araxes Pharma Llc | Method for screening inhibitors of ras |
| FI3365334T3 (fi) | 2015-10-21 | 2024-09-19 | Otsuka Pharma Co Ltd | Bentsolaktaamiyhdisteitä proteiinikinaasin estäjinä |
| CA3005089A1 (en) | 2015-11-16 | 2017-05-26 | Araxes Pharma Llc | 2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use thereof |
| WO2017100546A1 (en) | 2015-12-09 | 2017-06-15 | Araxes Pharma Llc | Methods for preparation of quinazoline derivatives |
| US10822312B2 (en) | 2016-03-30 | 2020-11-03 | 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 |
| EP3519402A1 (en) | 2016-09-29 | 2019-08-07 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| WO2018068017A1 (en) | 2016-10-07 | 2018-04-12 | Araxes Pharma Llc | Heterocyclic compounds as inhibitors of ras and methods of use thereof |
| JP7236996B2 (ja) | 2016-11-03 | 2023-03-10 | コーバス・ファーマシューティカルズ・インコーポレイテッド | インターロイキン－２誘導性ｔ細胞キナーゼを調節する化合物及び方法 |
| 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 |
| EP3573964A1 (en) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | Benzothiophene and benzothiazole compounds and methods of use thereof |
| WO2018140512A1 (en) | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | Fused bicyclic benzoheteroaromatic compounds and methods of use thereof |
| WO2018140514A1 (en) | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | 1-(6-(3-hydroxynaphthalen-1-yl)quinazolin-2-yl)azetidin-1-yl)prop-2-en-1-one derivatives and similar compounds as kras g12c inhibitors for the treatment of cancer |
| US11279689B2 (en) | 2017-01-26 | 2022-03-22 | Araxes Pharma Llc | 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1 yl)prop-2-en-1-one derivatives and similar compounds as KRAS G12C modulators for treating cancer |
| JOP20190186A1 (ar) | 2017-02-02 | 2019-08-01 | Astellas Pharma Inc | مركب كينازولين |
| JP2020521741A (ja) | 2017-05-25 | 2020-07-27 | アラクセス ファーマ エルエルシー | がんの処置のための化合物およびその使用の方法 |
| CA3063440A1 (en) * | 2017-05-25 | 2018-11-29 | Araxes Pharma Llc | Covalent inhibitors of kras |
| CN110831933A (zh) | 2017-05-25 | 2020-02-21 | 亚瑞克西斯制药公司 | 喹唑啉衍生物作为突变kras、hras或nras的调节剂 |
| MX2020010836A (es) | 2018-05-04 | 2021-01-08 | Amgen Inc | Inhibidores de kras g12c y métodos para su uso. |
| CN112584833A (zh) | 2018-08-01 | 2021-03-30 | 亚瑞克西斯制药公司 | 杂环螺化合物及其用于治疗癌症的使用方法 |
| BR112021007726A2 (pt) | 2018-10-24 | 2021-07-27 | Araxes Pharma Llc | derivados de 2-(2-acriloil-2,6-diazaspiro[3.4] octan-6-il)-6-(1h-indazol-4-il)-benzonitrilo e compostos relacionados como inibidores de proteína kras mutante g12c para inibir metástase tumoral |
| JP2020203966A (ja) | 2019-06-14 | 2020-12-24 | 大塚化学株式会社 | 摩擦材組成物、摩擦材、及び摩擦部材 |
| JP2024163372A (ja) | 2023-05-11 | 2024-11-22 | 株式会社大一商会 | 遊技機 |
-
2016
- 2016-04-08 AU AU2016245864A patent/AU2016245864C1/en active Active
- 2016-04-08 JP JP2017552484A patent/JP2018513853A/ja not_active Withdrawn
- 2016-04-08 BR BR112017021869A patent/BR112017021869A2/pt not_active Application Discontinuation
- 2016-04-08 HK HK18107777.4A patent/HK1248231A1/zh unknown
- 2016-04-08 CN CN201680033135.5A patent/CN107849022A/zh active Pending
- 2016-04-08 KR KR1020177032417A patent/KR20180005178A/ko not_active Ceased
- 2016-04-08 EA EA201792214A patent/EA201792214A1/ru unknown
- 2016-04-08 MX MX2017012979A patent/MX382355B/es unknown
- 2016-04-08 WO PCT/US2016/026573 patent/WO2016164675A1/en not_active Ceased
- 2016-04-08 EP EP16716802.0A patent/EP3280708B1/en active Active
- 2016-04-08 ES ES16716802T patent/ES2898765T3/es active Active
- 2016-04-08 US US15/093,951 patent/US10246424B2/en active Active
- 2016-04-08 TW TW105111140A patent/TW201702232A/zh unknown
- 2016-04-10 JO JOP/2016/0068A patent/JO3707B1/ar active
- 2016-04-11 UY UY0001036612A patent/UY36612A/es not_active Application Discontinuation
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2019
- 2019-02-21 US US16/281,905 patent/US10829458B2/en not_active Ceased
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2021
- 2021-03-04 JP JP2021034710A patent/JP2021098721A/ja active Pending
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2022
- 2022-11-10 US US17/985,017 patent/USRE50490E1/en active Active
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