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 | |
| US62/145,705 | 2015-04-10 | ||
| US62/145,818 | 2015-04-10 | ||
| US201562255891P | 2015-11-16 | 2015-11-16 | |
| US62/255,891 | 2015-11-16 | ||
| US201562265320P | 2015-12-09 | 2015-12-09 | |
| US201562265316P | 2015-12-09 | 2015-12-09 | |
| US62/265,320 | 2015-12-09 | ||
| US62/265,316 | 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 (223)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014143659A1 (en) | 2013-03-15 | 2014-09-18 | 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 |
| 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 |
| 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 |
| ES2898765T3 (es) | 2015-04-10 | 2022-03-08 | Araxes Pharma Llc | Compuestos de quinazolina sustituidos y métodos de uso de los mismos |
| ES2856880T3 (es) | 2015-04-15 | 2021-09-28 | Araxes Pharma Llc | Inhibidores tricíclicos condensados de KRAS y métodos de uso de los mismos |
| US10144724B2 (en) * | 2015-07-22 | 2018-12-04 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
| US10689356B2 (en) | 2015-09-28 | 2020-06-23 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| US10975071B2 (en) | 2015-09-28 | 2021-04-13 | 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 |
| EP3356347A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| EP3356353A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| US10730867B2 (en) | 2015-09-28 | 2020-08-04 | 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 |
| US10414757B2 (en) | 2015-11-16 | 2019-09-17 | Araxes Pharma Llc | 2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use thereof |
| US9988357B2 (en) | 2015-12-09 | 2018-06-05 | Araxes Pharma Llc | Methods for preparation of quinazoline derivatives |
| EP3394056B1 (en) | 2015-12-22 | 2021-04-14 | Shy Therapeutics LLC | Compounds for the treatment of cancer and inflammatory disease |
| WO2017172979A1 (en) | 2016-03-30 | 2017-10-05 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use |
| SG11201810171SA (en) | 2016-05-18 | 2018-12-28 | Mirati Therapeutics Inc | Kras g12c inhibitors |
| 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 |
| US10377743B2 (en) | 2016-10-07 | 2019-08-13 | Araxes Pharma Llc | Inhibitors of RAS and methods of use thereof |
| NZ754994A (en) * | 2016-12-22 | 2022-12-23 | Amgen Inc | Benzisothiazole, 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 |
| WO2018140600A1 (en) * | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | Fused hetero-hetero bicyclic compounds and methods of use thereof |
| EP3573971A1 (en) | 2017-01-26 | 2019-12-04 | 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 |
| EP3573954A1 (en) * | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | Fused bicyclic benzoheteroaromatic compounds and methods of use thereof |
| 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 |
| 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 |
| 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 |
| KR20200010306A (ko) | 2017-05-25 | 2020-01-30 | 아락세스 파마 엘엘씨 | Kras의 공유적 억제제 |
| WO2018218069A1 (en) * | 2017-05-25 | 2018-11-29 | Araxes Pharma Llc | Quinazoline derivatives as modulators of mutant kras, hras or nras |
| CA3066939A1 (en) | 2017-06-21 | 2018-12-27 | SHY Therapeutics LLC | Compounds that interact with the ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease |
| ES2928576T3 (es) | 2017-09-08 | 2022-11-21 | 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 |
| PT3710439T (pt) * | 2017-11-15 | 2023-05-15 | Array Biopharma Inc | Inibidores de kras g12c |
| ES2969284T3 (es) * | 2018-01-19 | 2024-05-17 | Medshine Discovery Inc | Derivado de piridona-pirimidina que actúa como inhibidor de la muteína krasg12c |
| 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 |
| MA52501A (fr) | 2018-05-04 | 2021-03-10 | Amgen Inc | Inhibiteurs de kras g12c et leurs procédés d'utilisation |
| CA3099118A1 (en) | 2018-05-04 | 2019-11-07 | 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 |
| EP3790886B1 (en) * | 2018-05-10 | 2024-06-26 | Amgen Inc. | Kras g12c inhibitors for the treatment of cancer |
| EP3802535B1 (en) | 2018-06-01 | 2022-12-14 | Amgen, Inc | Kras g12c inhibitors and methods of using the same |
| CA3099799A1 (en) * | 2018-06-11 | 2019-12-19 | Amgen Inc. | Kras g12c inhibitors for treating cancer |
| MA51848A (fr) | 2018-06-12 | 2021-04-21 | Amgen Inc | Inhibiteurs de kras g12c et leurs procédés d'utilisation |
| HRP20231253T1 (hr) | 2018-06-27 | 2024-02-02 | Bristol-Myers Squibb Company | Supstituirani spojevi naftiridina korisni kao aktivatori t stanica |
| ES2950007T3 (es) | 2018-06-27 | 2023-10-04 | Bristol Myers Squibb Co | Compuestos de naftiridinona útiles como activadores de células T |
| 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 |
| 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 |
| CA3107168A1 (en) * | 2018-08-01 | 2020-02-06 | Araxes Pharma Llc | Heterocyclic spiro compounds and methods of use thereof for the treatment of cancer |
| 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 |
| IL281344B2 (en) | 2018-09-10 | 2025-09-01 | Mirati Therapeutics Inc | Combination of adagrasib and cetuximab for cancer treatment |
| EP3849537B1 (en) | 2018-09-10 | 2024-10-23 | Mirati Therapeutics, Inc. | Combination therapies |
| CN112996795B (zh) | 2018-09-18 | 2024-11-12 | 尼坎治疗公司 | 作为src同源-2磷酸酶抑制剂的稠合的三环衍生物 |
| AR116604A1 (es) | 2018-10-15 | 2021-05-26 | Lilly Co Eli | Inhibidores de kras g12c |
| KR20210083286A (ko) * | 2018-10-24 | 2021-07-06 | 아락세스 파마 엘엘씨 | 종양 전이를 억제하기 위한 g12c 돌연변이 kras 단백질의 억제제로서 2-(2-아크릴로일-2,6-디아자스피로[3.4]옥탄-6-일)-6-(1h-인다졸-4-일)-벤조니트릴 유도체 및 관련 화합물 |
| JP7186874B2 (ja) * | 2018-10-26 | 2022-12-09 | アーリーン ファーマシューティカルズ エルエルシー | ピラゾリル化合物およびその使用方法 |
| JP7451419B2 (ja) | 2018-10-26 | 2024-03-18 | 大鵬薬品工業株式会社 | 新規なインダゾール化合物又はその塩 |
| 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 |
| 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 |
| US11053226B2 (en) | 2018-11-19 | 2021-07-06 | Amgen Inc. | KRAS G12C inhibitors and methods of using the same |
| MX2021005924A (es) * | 2018-11-29 | 2021-06-30 | Araxes Pharma Llc | Compuestos y metodos de uso de los mismos para el tratamiento del cancer. |
| CA3112129A1 (en) | 2018-12-05 | 2020-06-11 | Mirati Therapeutics, Inc. | Combination therapies |
| US12391705B2 (en) | 2018-12-19 | 2025-08-19 | Shy Therapeutics, Llc | Compounds that interact with the Ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease |
| EP3908283A4 (en) * | 2019-01-10 | 2022-10-12 | Mirati Therapeutics, Inc. | KRAS G12C INHIBITORS |
| KR102405055B1 (ko) * | 2019-01-16 | 2022-06-07 | 상하이 잉리 파마슈티컬 컴퍼니 리미티드 | 모르폴리노퀴나졸린 화합물의 제조방법 및 이의 중간체 |
| US20220064141A1 (en) * | 2019-01-29 | 2022-03-03 | Brightgene Bio-Medical Technology Co., Ltd. | Benzopyridone heterocyclic compound and use thereof |
| 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 |
| CA3129876A1 (en) * | 2019-02-18 | 2020-08-27 | 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 |
| CR20210504A (es) | 2019-03-05 | 2022-02-08 | Astrazeneca Ab | Compuestos tricíclicos condensados útiles como agentes anticancerígenos |
| JP2022527279A (ja) * | 2019-03-28 | 2022-06-01 | エピザイム,インコーポレイティド | キノリン誘導体及び癌の治療のためのその使用 |
| CA3137608A1 (en) * | 2019-04-22 | 2020-10-29 | Betta Pharmaceuticals Co., Ltd | Quinazoline compound and pharmaceutical application thereof |
| EP3738593A1 (en) | 2019-05-14 | 2020-11-18 | Amgen, Inc | Dosing of kras inhibitor for treatment of cancers |
| US20220227738A1 (en) * | 2019-05-20 | 2022-07-21 | California Institute Of Technology | Kras g12c inhibitors and uses thereof |
| WO2020234103A1 (en) | 2019-05-21 | 2020-11-26 | Bayer Aktiengesellschaft | Identification and use of kras inhibitors |
| WO2020236948A1 (en) | 2019-05-21 | 2020-11-26 | Amgen Inc. | Solid state forms |
| EP3972973A1 (en) | 2019-05-21 | 2022-03-30 | Amgen Inc. | Solid state forms |
| KR20220027879A (ko) * | 2019-05-29 | 2022-03-08 | 상하이 한서 바이오메디컬 컴퍼니 리미티드 | 질소 함유 헤테로사이클릭 유도체의 조절제, 이의 제조방법 및 용도 |
| 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 |
| CN114040914B (zh) * | 2019-07-01 | 2024-10-22 | 江苏恒瑞医药股份有限公司 | 喹唑啉酮类衍生物、其制备方法及其在医药上的应用 |
| CN114222743A (zh) * | 2019-08-16 | 2022-03-22 | 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 |
| AR119821A1 (es) | 2019-08-28 | 2022-01-12 | Bristol Myers Squibb Co | Compuestos de piridopirimidinonilo sustituidos útiles como activadores de células t |
| AU2020337938B2 (en) | 2019-08-29 | 2025-09-25 | Array Biopharma Inc. | KRas G12D inhibitors |
| WO2021055728A1 (en) * | 2019-09-18 | 2021-03-25 | Merck Sharp & Dohme Corp. | Small molecule inhibitors of kras g12c mutant |
| CN116947885B (zh) * | 2019-09-20 | 2026-01-23 | 上海济煜医药科技股份有限公司 | 稠合吡啶酮类化合物及其制备方法和应用 |
| US12122787B2 (en) | 2019-09-20 | 2024-10-22 | Shanghai Jemincare Pharmaceuticals Co., Ltd | Fused pyridone compound, and preparation method therefor and use thereof |
| MX2022003537A (es) | 2019-09-24 | 2022-07-11 | Mirati Therapeutics Inc | Terapias de combinacion. |
| WO2021057832A1 (en) * | 2019-09-25 | 2021-04-01 | Jacobio Pharmaceuticals Co., Ltd. | Kras mutant protein inhibitor |
| 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 |
| CR20220230A (es) | 2019-10-28 | 2022-06-15 | Merck Sharp & Dohme | Inhibidores de pequeñas moléculas de mutante g12c de kras |
| WO2021088458A1 (en) * | 2019-11-04 | 2021-05-14 | Jacobio Pharmaceuticals Co., Ltd. | Kras mutant protein inhibitor |
| EP4054719B1 (en) | 2019-11-04 | 2026-02-11 | Revolution Medicines, Inc. | Ras inhibitors |
| JP7823816B2 (ja) | 2019-11-04 | 2026-03-04 | レヴォリューション・メディスンズ,インコーポレイテッド | Ras阻害剤 |
| KR20220109407A (ko) | 2019-11-04 | 2022-08-04 | 레볼루션 메디슨즈, 인크. | Ras 억제제 |
| 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 |
| WO2021108683A1 (en) | 2019-11-27 | 2021-06-03 | 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 |
| US20220315598A1 (en) * | 2019-12-02 | 2022-10-06 | Shanghai Yingli Pharmaceutical Co., Ltd | Oxygen-containing Heterocyclic Compound, Preparation Method Therefor and Use Thereof |
| 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 |
| UA128806C2 (uk) * | 2019-12-11 | 2024-10-23 | Елі Ліллі Енд Компані | Інгібітори kras g12c |
| WO2021120890A1 (en) | 2019-12-20 | 2021-06-24 | Novartis Ag | Pyrazolyl derivatives useful as anti-cancer agents |
| EP4076418A4 (en) | 2019-12-20 | 2024-01-24 | Mirati Therapeutics, Inc. | Sos1 inhibitors |
| CN115175907B (zh) | 2019-12-23 | 2024-08-02 | 百时美施贵宝公司 | 可用作t细胞激活剂的经取代的哌嗪衍生物 |
| AR120823A1 (es) | 2019-12-23 | 2022-03-23 | Bristol Myers Squibb Co | Compuestos bicíclicos sustituidos útiles como activadores de células t |
| ES3038401T3 (en) | 2019-12-23 | 2025-10-13 | Bristol Myers Squibb Co | Substituted quinazolinyl compounds useful as t cell activators |
| US12479843B2 (en) | 2019-12-27 | 2025-11-25 | Soochow University | Spiro ring-containing quinazoline compounds |
| US12441707B2 (en) | 2019-12-30 | 2025-10-14 | 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 |
| CN113637005B (zh) * | 2020-02-24 | 2024-05-24 | 泰励生物科技(上海)有限公司 | 用于癌症治疗的kras抑制剂 |
| JP7773987B2 (ja) * | 2020-03-25 | 2025-11-20 | ウィゲン・バイオメディシン・テクノロジー・(シャンハイ)・カンパニー・リミテッド | スピロ環含有キナゾリン化合物 |
| 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 |
| CA3183032A1 (en) | 2020-06-18 | 2021-12-23 | Mallika Singh | 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 |
| EP4203952A4 (en) | 2020-08-28 | 2024-12-11 | Kumquat Biosciences Inc. | HETEROCYCLIC COMPOUNDS AND USES THEREOF |
| MX2023002248A (es) | 2020-09-03 | 2023-05-16 | Revolution Medicines Inc | Uso de inhibidores de sos1 para tratar neoplasias malignas con mutaciones de shp2. |
| US20250268901A1 (en) | 2020-09-11 | 2025-08-28 | Medshine Discovery Inc. | Crystal form of azetidine-substituted compound |
| AU2021340716A1 (en) | 2020-09-11 | 2023-03-30 | Mirati Therapeutics, Inc. | Crystalline forms of a KRas G12C inhibitor |
| CR20230165A (es) | 2020-09-15 | 2023-06-02 | Revolution Medicines Inc | Derivados indólicos como inhibidores de ras en el tratamiento del cáncer |
| US12162893B2 (en) | 2020-09-23 | 2024-12-10 | Erasca, Inc. | Tricyclic pyridones and pyrimidones |
| US20230365563A1 (en) * | 2020-09-30 | 2023-11-16 | Shanghai Pharmaceuticals Holding Co., Ltd. | Quinazoline compound and application thereof |
| US20230406860A1 (en) * | 2020-10-27 | 2023-12-21 | Amgen Inc. | Heterocyclic spiro compounds and methods of use |
| US20240034733A1 (en) * | 2020-11-03 | 2024-02-01 | 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 |
| AU2021401232A1 (en) | 2020-12-15 | 2023-06-22 | Mirati Therapeutics, Inc. | Azaquinazoline pan-kras inhibitors |
| US11999753B2 (en) | 2020-12-16 | 2024-06-04 | 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| CN117659051A (zh) * | 2021-03-30 | 2024-03-08 | 上海德琪医药科技有限公司 | Kras g12d蛋白抑制剂和其用途 |
| CR20230558A (es) | 2021-05-05 | 2024-01-24 | Revolution Medicines Inc | Inhibidores de ras para el tratamiento del cáncer |
| IL308193A (en) | 2021-05-05 | 2024-01-01 | Revolution Medicines Inc | RAS inhibitors |
| 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 |
| WO2023284730A1 (en) | 2021-07-14 | 2023-01-19 | Nikang Therapeutics, Inc. | Alkylidene derivatives as kras inhibitors |
| IL310291A (en) | 2021-07-23 | 2024-03-01 | Theras Inc | Compositions and methods for inhibition of ras |
| TW202327569A (zh) | 2021-09-01 | 2023-07-16 | 瑞士商諾華公司 | 包含tead抑制劑的藥物組合及其用於癌症治療之用途 |
| EP4389751A1 (en) * | 2021-09-03 | 2024-06-26 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| CN117957219A (zh) | 2021-09-22 | 2024-04-30 | 四川汇宇制药股份有限公司 | 一种吡啶类衍生物及其用途 |
| AR127308A1 (es) | 2021-10-08 | 2024-01-10 | Revolution Medicines Inc | Inhibidores ras |
| AU2022371727A1 (en) | 2021-10-22 | 2024-05-02 | Jiangsu Hengrui Pharmaceuticals Co., Ltd. | Nitrogen-containing tetracyclic compound, preparation method therefor, and medical use thereof |
| JP2025500878A (ja) | 2021-12-17 | 2025-01-15 | ジェンザイム・コーポレーション | Shp2阻害剤としてのピラゾロピラジン化合物 |
| 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 |
| CN118696046A (zh) | 2022-02-10 | 2024-09-24 | 拜耳公司 | 作为kras抑制剂的稠合嘧啶 |
| EP4227307A1 (en) | 2022-02-11 | 2023-08-16 | Genzyme Corporation | Pyrazolopyrazine compounds as shp2 inhibitors |
| US20250177389A1 (en) | 2022-03-04 | 2025-06-05 | Eli Lilly And Company | Method of treatment including kras g12c inhibitors and shp2 inhibitors |
| CN119136806A (zh) | 2022-03-08 | 2024-12-13 | 锐新医药公司 | 用于治疗免疫难治性肺癌的方法 |
| IL315603A (en) | 2022-03-28 | 2024-11-01 | Nikang Therapeutics Inc | Sulfonamido derivatives as cycle-dependent KINASE 2 inhibitors |
| EP4504209A1 (en) | 2022-04-08 | 2025-02-12 | Eli Lilly and Company | Method of treatment including kras g12c inhibitors and aurora a inhibitors |
| WO2023199180A1 (en) | 2022-04-11 | 2023-10-19 | Novartis Ag | Therapeutic uses of a krasg12c inhibitor |
| AU2023264918A1 (en) | 2022-05-06 | 2025-01-09 | Chugai Seiyaku Kabushiki Kaisha | Cyclic compound having 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 |
| WO2023240263A1 (en) | 2022-06-10 | 2023-12-14 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| CN119855822A (zh) | 2022-06-24 | 2025-04-18 | 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 |
| WO2024031088A1 (en) | 2022-08-05 | 2024-02-08 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| US20260035376A1 (en) * | 2022-08-05 | 2026-02-05 | Theras, Inc. | Compositions and methods for inhibition of ras |
| WO2024040131A1 (en) | 2022-08-17 | 2024-02-22 | Treeline Biosciences, Inc. | Pyridopyrimidine kras inhibitors |
| GB202212641D0 (en) | 2022-08-31 | 2022-10-12 | Jazz Pharmaceuticals Ireland Ltd | Novel compounds |
| WO2024051763A1 (zh) * | 2022-09-08 | 2024-03-14 | 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 |
| AU2023377064A1 (en) | 2022-11-09 | 2025-05-22 | Revolution Medicines, Inc. | Compounds, complexes, and methods for their preparation and of their use |
| TW202434563A (zh) | 2022-11-11 | 2024-09-01 | 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的含有2,5-取代的嘧啶衍生物之雙功能化合物 |
| PE20252384A1 (es) | 2022-11-21 | 2025-10-10 | Treeline Biosciences Inc | Inhibidores espirociclicos de kras basados en dihidropiranopirimidina |
| 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 |
| AU2024241633A1 (en) | 2023-03-30 | 2025-11-06 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| PE20260039A1 (es) | 2023-04-07 | 2026-01-09 | Revolution Medicines Inc | Inhibidores macrociclicos de ras |
| WO2024211663A1 (en) | 2023-04-07 | 2024-10-10 | Revolution Medicines, Inc. | Condensed macrocyclic compounds as ras inhibitors |
| CN121100123A (zh) | 2023-04-14 | 2025-12-09 | 锐新医药公司 | Ras抑制剂的结晶形式 |
| TW202448897A (zh) | 2023-04-14 | 2024-12-16 | 美商銳新醫藥公司 | Ras抑制劑之結晶形式、含有其之組合物及其使用方法 |
| WO2024229406A1 (en) | 2023-05-04 | 2024-11-07 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| TW202500126A (zh) | 2023-05-24 | 2025-01-01 | 美商金橘生物科技公司 | 雜環化合物及其用途 |
| KR20260020406A (ko) | 2023-06-02 | 2026-02-11 | 다이이찌 산쿄 가부시키가이샤 | 항 her3 항체-약물 콘주게이트와 rasg12c 저해제의 조합 |
| WO2025007000A1 (en) | 2023-06-30 | 2025-01-02 | Kumquat Biosciences Inc. | Substituted condensed tricyclic amine compounds and uses thereof as ras inhibitors |
| 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 |
| WO2025064848A1 (en) | 2023-09-21 | 2025-03-27 | Treeline Biosciences, Inc. | Spirocyclic dihydropyranopyridine kras inhibitors |
| 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 |
| WO2025117616A1 (en) | 2023-11-27 | 2025-06-05 | 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 |
| 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 |
| TW202545999A (zh) | 2024-02-06 | 2025-12-01 | 美商金橘生物科技公司 | 雜環綴合物及其用途 |
| 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 |
| 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 |
| 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 |
| WO2026015801A1 (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 |
| WO2026015796A1 (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 |
| WO2026035947A1 (en) | 2024-08-07 | 2026-02-12 | Tesseract Medicines Us, Llc | Kras-targeting covalent-induced drug conjugates comprising a topoisomerase payload |
| WO2026035945A1 (en) | 2024-08-07 | 2026-02-12 | Tesseract Medicines Us, Llc | Covalent-induced drug conjugates targeting kras and comprising a topoisomerase payload |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
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 |
| EP0094498A3 (en) | 1982-05-06 | 1985-04-03 | American Cyanamid Company | Antiatherosclerotic 1-piperazine derivatives |
| US4439606A (en) | 1982-05-06 | 1984-03-27 | American Cyanamid Company | Antiatherosclerotic 1-piperazinecarbonyl compounds |
| 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 |
| 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 |
| EP0754240B1 (en) | 1994-02-07 | 2003-08-20 | Beckman Coulter, Inc. | Ligase/polymerase-mediated genetic bit analysis 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 |
| CA2200468A1 (en) | 1994-10-27 | 1996-05-09 | Wayne J. Thompson | Muscarine antagonists |
| US5863949A (en) | 1995-03-08 | 1999-01-26 | Pfizer Inc | Arylsulfonylamino hydroxamic acid derivatives |
| DK0821671T3 (da) | 1995-04-20 | 2001-04-23 | Pfizer | Arylsulfonylhydroxamsyrederivater som MMP- og TNF-inhibitorer |
| FR2734816B1 (fr) | 1995-05-31 | 1997-07-04 | Adir | Nouveaux aryl (alkyl) propylamides, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| ATE483733T1 (de) | 1995-06-14 | 2010-10-15 | Univ California | Hochaffine humane antikörper gegen tumorantigene |
| ES2183905T3 (es) | 1995-12-20 | 2003-04-01 | Hoffmann La Roche | Inhibidores de metaloproteasa 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 |
| HUP9903014A3 (en) | 1996-07-18 | 2000-08-28 | Pfizer | Phosphinate derivatives having matrix metalloprotease inhibitor effect and medicaments containing the same |
| US6153609A (en) | 1996-08-23 | 2000-11-28 | Pfizer Inc | Arylsulfonylamino hydroxamic acid derivatives |
| US5777324A (en) | 1996-09-19 | 1998-07-07 | Sequenom, Inc. | Method and apparatus for maldi analysis |
| AU5131998A (en) | 1997-01-06 | 1998-08-03 | Pfizer Inc. | Cyclic sulfone derivatives |
| ES2202796T3 (es) | 1997-02-03 | 2004-04-01 | Pfizer Products Inc. | Derivados de acidos arilsulfonilaminohidroxamicos. |
| 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 |
| BR9807678A (pt) | 1997-02-11 | 2000-02-15 | Pfizer | Derivados de ácidos arilsulfonil-hidroxâmicos |
| WO1998035951A2 (en) | 1997-02-17 | 1998-08-20 | Fujisawa Pharmaceutical Co., Ltd. | New 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 |
| ID23668A (id) | 1997-08-08 | 2000-05-11 | Pfizer Prod Inc | Turunan asam ariloksiarilsulfonilamino hidroksamat |
| GB9725782D0 (en) | 1997-12-05 | 1998-02-04 | Pfizer Ltd | Therapeutic agents |
| US6903118B1 (en) | 1997-12-17 | 2005-06-07 | Klinge Pharma Gmbh | Piperazinyl-substituted pyridylalkane, alkene and alkine carboxamides |
| DE19756236A1 (de) | 1997-12-17 | 1999-07-01 | Klinge Co Chem Pharm Fab | Neue piperazinylsubstituierte Pyridylalkan-, alken- und -alkincarbonsäureamide |
| WO1999032454A1 (en) | 1997-12-22 | 1999-07-01 | 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 |
| PA8469401A1 (es) | 1998-04-10 | 2000-05-24 | Pfizer Prod Inc | Derivados biciclicos del acido hidroxamico |
| PA8469501A1 (es) | 1998-04-10 | 2000-09-29 | Pfizer Prod Inc | Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico |
| DE69940430D1 (de) | 1998-06-24 | 2009-04-02 | Illumina Inc | Dekodierung von matrixartig-angeordneten Sensoren durch Mikropartikel |
| ES2213985T3 (es) | 1998-11-05 | 2004-09-01 | Pfizer Products Inc. | Derivados de hidroxiamida de acido 5-oxo-pirrolidin-2-carboxilico. |
| 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 |
| US6251639B1 (en) | 1999-09-13 | 2001-06-26 | Nugen Technologies, Inc. | Methods and compositions for linear isothermal amplification of polynucleotide sequences, using a RNA-DNA composite primer |
| NZ521117A (en) * | 2000-03-13 | 2005-02-25 | Wyeth Corp | Method of treating or inhibiting colonic polyps |
| JP2003528079A (ja) | 2000-03-21 | 2003-09-24 | ザ プロクター アンド ギャンブル カンパニー | 複素環式側鎖含有メタロプロテアーゼ阻害剤 |
| JP2003535860A (ja) | 2000-06-05 | 2003-12-02 | ドン・ア・ファーム・カンパニー・リミテッド | 新規なオキサゾリジノン誘導体及びその製造方法 |
| TWI227231B (en) | 2000-07-12 | 2005-02-01 | Novartis Ag | 4-benzoyl-piperidine derivatives for treating conditions mediated by CCR-3 |
| EP2277877A1 (en) | 2000-08-18 | 2011-01-26 | Millennium Pharmaceuticals, 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 |
| CA2443108A1 (en) | 2001-04-03 | 2002-10-17 | Merck & Co. Inc. | N-substituted nonaryl-heterocyclo amidyl nmda/nr2b antagonists |
| DE60227794D1 (de) | 2001-04-26 | 2008-09-04 | Eisai R&D Man Co Ltd | Stickstoffhaltige verbindung mit kondensiertem ring und pyrazolylgruppe als substituent und medizinische zusammensetzung davon |
| JP2005502623A (ja) | 2001-07-02 | 2005-01-27 | ノボ ノルディスク アクティーゼルスカブ | 置換ピペラジンおよびジアゼパン |
| EP1348434A1 (en) | 2002-03-27 | 2003-10-01 | Fujisawa Deutschland GmbH | Use of pyridyl amides as inhibitors of angiogenesis |
| BR0315166A (pt) | 2002-10-11 | 2005-08-16 | Astrazeneca Ab | Uso de um composto ou de um sal farmaceuticamente aceitável do mesmo, composto ou um sal farmaceuticamente aceitável do mesmo, composição farmacêutica, e, método para produzir um efeito inibidor de 11betahsd1 em um animal de sangue quente, tal como o homem, que necessita de tratamento |
| 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 |
| EP1597256A1 (en) | 2003-02-21 | 2005-11-23 | Pfizer Inc. | N-heterocyclyl-substituted amino-thiazole derivatives as protein kinase inhibitors |
| BRPI0408284B8 (pt) | 2003-03-12 | 2021-05-25 | Kudos Pharm Ltd | compostos derivados de ftalazinona, seu uso e composição farmacêutica compreendendo os mesmos |
| 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 |
| WO2005095327A1 (ja) | 2004-03-31 | 2005-10-13 | Ajinomoto Co., Inc. | 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 |
| US7579368B2 (en) | 2005-03-16 | 2009-08-25 | Hoffman-La Roche Inc. | Cis-imidazolines |
| 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 |
| KR20080066949A (ko) | 2005-10-11 | 2008-07-17 | 인터뮨, 인크. | 바이러스 복제 억제제 |
| CA2632030A1 (en) | 2005-12-15 | 2007-06-21 | 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) |
| US8097617B2 (en) | 2006-03-31 | 2012-01-17 | Novartis Ag | Organic compounds |
| WO2007116313A2 (en) | 2006-04-12 | 2007-10-18 | Pfizer Limited | Pyrrolidine derivatives as modulators of chemokine ccr5 receptors |
| WO2007144394A2 (en) | 2006-06-16 | 2007-12-21 | High Point Pharmaceuticals, Llc. | Pharmaceutical use of substituted piperidine carboxamides |
| EP2044051B1 (en) | 2006-06-22 | 2010-01-27 | BIOVITRUM AB (publ) | Pyridine and pyrazine derivatives as mnk kinase inhibitors |
| FR2903101B1 (fr) | 2006-06-30 | 2008-09-26 | Servier Lab | Nouveaux derives naphtaleniques, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| US9259426B2 (en) | 2006-07-20 | 2016-02-16 | Gilead Sciences, Inc. | 4,6-di- 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 |
| US20080070892A1 (en) | 2006-09-15 | 2008-03-20 | Harris Joel M | Treating pain, diabetes, and disorders of lipid metabolism |
| 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 |
| CA2682356C (en) | 2007-04-16 | 2016-06-14 | Abbott Laboratories | 7-substituted indole mcl-1 inhibitors |
| EP3045542B1 (en) | 2008-03-28 | 2016-11-16 | Pacific Biosciences of California, Inc. | Methods for nucleic acid sequencing |
| EP2133334A1 (en) | 2008-06-09 | 2009-12-16 | DAC S.r.l. | Heterocyclic derivatives as HDAC inhibitors |
| KR101354763B1 (ko) | 2008-08-25 | 2014-01-22 | 아이알엠 엘엘씨 | 헷지호그 경로 조절제 |
| 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 |
| ES2436550T3 (es) | 2009-04-20 | 2014-01-02 | F. Hoffmann-La Roche Ag | Nuevos derivados de prolina como inhibidores de catepsina |
| CA2759547A1 (en) | 2009-04-22 | 2010-10-28 | Janssen Pharmaceutica Nv | Azetidinyl diamides as monoacylglycerol lipase inhibitors |
| SE533816C2 (sv) | 2009-05-06 | 2011-01-25 | Tetra Laval Holdings & Finance | Förfarande för framställning av kartongflaskor |
| US20120083476A1 (en) | 2009-06-05 | 2012-04-05 | 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 |
| EP2448581B1 (en) | 2009-06-29 | 2016-12-07 | 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 |
| WO2011031896A2 (en) | 2009-09-09 | 2011-03-17 | Avila Therapeutics, Inc. | Pi3 kinase inhibitors and uses thereof |
| NZ600954A (en) | 2009-12-22 | 2013-11-29 | Isoindolinone inhibitors of phosphatidylinositol 3-kinase | |
| US20110269244A1 (en) | 2009-12-30 | 2011-11-03 | Petter Russell C | Ligand-directed covalent modification of protein |
| AR080057A1 (es) | 2010-01-29 | 2012-03-07 | Otsuka Pharma Co Ltd | Piridinas disustituidas como anticancerigenos |
| AU2011223655A1 (en) | 2010-03-03 | 2012-06-28 | OSI Pharmaceuticals, LLC | Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors |
| SG183855A1 (en) | 2010-03-16 | 2012-10-30 | Merck Patent Gmbh | Morpholinylquinazolines |
| 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 |
| CN103119439A (zh) | 2010-06-08 | 2013-05-22 | 纽亘技术公司 | 用于多重测序的方法和组合物 |
| US8658131B2 (en) | 2010-06-21 | 2014-02-25 | Washington University | Compounds comprising 4-benzoylpiperidine as a sigma-1-selective ligand |
| SG187633A1 (en) | 2010-07-30 | 2013-03-28 | 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 |
| 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 |
| KR20130142137A (ko) | 2010-10-22 | 2013-12-27 | 얀센 파마슈티카 엔.브이. | 모노아실글리세롤 리파아제 억제제로서의 피페리딘-4-일-아제티딘 다이아미드 |
| EP2635279A4 (en) | 2010-11-05 | 2014-10-29 | Glaxosmithkline Ip No 2 Ltd | CHEMICAL COMPOUNDS |
| US9260484B2 (en) | 2011-06-15 | 2016-02-16 | Ohio State Innovation Foundation | Small molecule composite surfaces as inhibitors of protein-protein interactions |
| SG195200A1 (en) | 2011-06-29 | 2013-12-30 | Otsuka Pharma 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 |
| US9242976B2 (en) | 2012-01-13 | 2016-01-26 | Bristol-Myers Squibb Company | Thiazolyl- or thiadiazolyl-substituted pyridyl compounds useful as kinase inhibitors |
| US9932317B2 (en) | 2012-03-19 | 2018-04-03 | Imperial Innovations Limited | 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 |
| CN104379563B (zh) | 2012-04-10 | 2018-12-21 | 加利福尼亚大学董事会 | 用于治疗癌症的组合物和方法 |
| AR091004A1 (es) | 2012-05-09 | 2014-12-30 | Gradalis Inc | Arn en horquilla corta bifuncional (bi-arnhc) especifico de mutaciones de nucleotidos individuales en k-ras |
| JO3300B1 (ar) | 2012-06-06 | 2018-09-16 | Novartis Ag | مركبات وتركيبات لتعديل نشاط egfr |
| DK2872491T3 (da) | 2012-07-11 | 2021-08-09 | Blueprint Medicines Corp | Inhibitorer af fibroblastvækstfaktorreceptoren |
| 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 |
| CA2882879A1 (en) | 2012-08-24 | 2014-02-27 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
| IL291945B2 (en) | 2012-11-01 | 2025-11-01 | Infinity Pharmaceuticals Inc | Treatment of cancers using pi3 kinase isoform modulators |
| CN105407894A (zh) | 2013-03-14 | 2016-03-16 | 康威基内有限公司 | 用于抑制含布罗莫结构域的蛋白质的方法和组合物 |
| US9227978B2 (en) | 2013-03-15 | 2016-01-05 | Araxes Pharma Llc | Covalent inhibitors of Kras G12C |
| WO2014143659A1 (en) * | 2013-03-15 | 2014-09-18 | Araxes Pharma Llc | Irreversible covalent inhibitors of the gtpase k-ras g12c |
| EP2970121B1 (en) | 2013-03-15 | 2017-12-13 | 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 |
| 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 |
| PT3049417T (pt) | 2013-07-31 | 2019-01-24 | Merck Patent Gmbh | Piridinas, pirimidinas e pirazinas, como inibidores de btk e utilizações das mesmas |
| 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 |
| EP3636639A1 (en) * | 2013-10-10 | 2020-04-15 | Araxes Pharma LLC | Inhibitors of kras g12c |
| JO3805B1 (ar) | 2013-10-10 | 2021-01-31 | Araxes Pharma Llc | مثبطات كراس جي12سي |
| 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 |
| BR112016016844A2 (pt) | 2014-02-03 | 2017-08-08 | Cadila Healthcare Ltd | Compostos heterocíclicos |
| EP3119762B9 (en) | 2014-03-20 | 2021-10-20 | Capella Therapeutics, Inc. | Benzimidazole derivatives as erbb tyrosine kinase inhibitors for the treatment of cancer |
| JP6377245B2 (ja) | 2014-03-24 | 2018-08-22 | グアンドン ジョンシェン ファーマシューティカル カンパニー リミテッド | Smo阻害剤としてのキノリン誘導体 |
| 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 |
| 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 |
| EP3247353A4 (en) | 2015-01-23 | 2018-07-04 | Confluence Life Sciences, Inc. | Heterocyclic itk inhibitors for treating inflammation and cancer |
| ES2898765T3 (es) * | 2015-04-10 | 2022-03-08 | Araxes Pharma Llc | Compuestos de quinazolina sustituidos y métodos de uso de los mismos |
| ES2856880T3 (es) | 2015-04-15 | 2021-09-28 | Araxes Pharma Llc | Inhibidores tricíclicos condensados de KRAS y métodos de uso de los mismos |
| US10144724B2 (en) | 2015-07-22 | 2018-12-04 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
| CA2993013A1 (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 |
| US10647703B2 (en) | 2015-09-28 | 2020-05-12 | 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 |
| US10975071B2 (en) | 2015-09-28 | 2021-04-13 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| US10730867B2 (en) | 2015-09-28 | 2020-08-04 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| US10689356B2 (en) | 2015-09-28 | 2020-06-23 | 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 |
| EP3356353A1 (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 |
| ES2989326T3 (es) | 2015-10-21 | 2024-11-26 | Otsuka Pharma Co Ltd | Compuestos de benzolactama como inhibidores de la proteína cinasa |
| US10414757B2 (en) | 2015-11-16 | 2019-09-17 | Araxes Pharma Llc | 2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use thereof |
| 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 |
| US10377743B2 (en) | 2016-10-07 | 2019-08-13 | Araxes Pharma Llc | Inhibitors of RAS and methods of use thereof |
| PT3534899T (pt) | 2016-11-03 | 2022-07-07 | Corvus Pharmaceuticals Inc | Compostos e métodos de modulação da cinase de células t induzível por interleucina-2 |
| US11136308B2 (en) | 2017-01-26 | 2021-10-05 | Araxes Pharma Llc | Substituted quinazoline and quinazolinone compounds and methods of use thereof |
| WO2018140600A1 (en) | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | Fused hetero-hetero bicyclic compounds 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 |
| EP3573971A1 (en) | 2017-01-26 | 2019-12-04 | 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 |
| WO2018140599A1 (en) | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | Benzothiophene and benzothiazole compounds and methods of use thereof |
| JOP20190186A1 (ar) | 2017-02-02 | 2019-08-01 | Astellas Pharma Inc | مركب كينازولين |
| WO2018218069A1 (en) | 2017-05-25 | 2018-11-29 | Araxes Pharma Llc | Quinazoline derivatives as modulators of mutant kras, hras or nras |
| KR20200010306A (ko) * | 2017-05-25 | 2020-01-30 | 아락세스 파마 엘엘씨 | Kras의 공유적 억제제 |
| 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 |
| MA52501A (fr) | 2018-05-04 | 2021-03-10 | Amgen Inc | Inhibiteurs de kras g12c et leurs procédés d'utilisation |
| CA3107168A1 (en) | 2018-08-01 | 2020-02-06 | Araxes Pharma Llc | Heterocyclic spiro compounds and methods of use thereof for the treatment of cancer |
| KR20210083286A (ko) | 2018-10-24 | 2021-07-06 | 아락세스 파마 엘엘씨 | 종양 전이를 억제하기 위한 g12c 돌연변이 kras 단백질의 억제제로서 2-(2-아크릴로일-2,6-디아자스피로[3.4]옥탄-6-일)-6-(1h-인다졸-4-일)-벤조니트릴 유도체 및 관련 화합물 |
| 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 |
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2016
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- 2016-04-08 TW TW105111140A patent/TW201702232A/zh unknown
- 2016-04-08 KR KR1020177032417A patent/KR20180005178A/ko not_active Ceased
- 2016-04-08 US US15/093,951 patent/US10246424B2/en active Active
- 2016-04-10 JO JOP/2016/0068A patent/JO3707B1/ar active
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