JP2017528498A - Kras g12c変異体タンパク質のインヒビター - Google Patents
Kras g12c変異体タンパク質のインヒビター Download PDFInfo
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- JP2017528498A JP2017528498A JP2017516106A JP2017516106A JP2017528498A JP 2017528498 A JP2017528498 A JP 2017528498A JP 2017516106 A JP2017516106 A JP 2017516106A JP 2017516106 A JP2017516106 A JP 2017516106A JP 2017528498 A JP2017528498 A JP 2017528498A
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- 0 C*(C)(C(C=C)=O)N Chemical compound C*(C)(C(C=C)=O)N 0.000 description 11
- AGAHETWGCFCMDK-UHFFFAOYSA-N COc(cc1)cc(N)c1N Chemical compound COc(cc1)cc(N)c1N AGAHETWGCFCMDK-UHFFFAOYSA-N 0.000 description 2
- MENVGNBSPBEPKD-FARCUNLSSA-N CC(/C(/C#N)=C/c1cnc[s]1)=O Chemical compound CC(/C(/C#N)=C/c1cnc[s]1)=O MENVGNBSPBEPKD-FARCUNLSSA-N 0.000 description 1
- IBAZRLSJAGDVRZ-UXBLZVDNSA-N CCC(C)C(/C(/C#N)=C/C(C)(C)CO)=O Chemical compound CCC(C)C(/C(/C#N)=C/C(C)(C)CO)=O IBAZRLSJAGDVRZ-UXBLZVDNSA-N 0.000 description 1
- HDZKUBSFRTUPMM-UHFFFAOYSA-N CCC(C=C)=N Chemical compound CCC(C=C)=N HDZKUBSFRTUPMM-UHFFFAOYSA-N 0.000 description 1
- OSNOZELCAUYPKY-UHFFFAOYSA-N CCc(ccc(OC)c1)c1N Chemical compound CCc(ccc(OC)c1)c1N OSNOZELCAUYPKY-UHFFFAOYSA-N 0.000 description 1
- QPNUFMOSEVSCIZ-UHFFFAOYSA-N CNc(cc(cc1N)OC)c1N Chemical compound CNc(cc(cc1N)OC)c1N QPNUFMOSEVSCIZ-UHFFFAOYSA-N 0.000 description 1
- RPKCLSMBVQLWIN-UHFFFAOYSA-N CNc(cccc1)c1N Chemical compound CNc(cccc1)c1N RPKCLSMBVQLWIN-UHFFFAOYSA-N 0.000 description 1
- HHSOTJHMTWZCNK-UHFFFAOYSA-N COc(cc1N)cc(N)c1N Chemical compound COc(cc1N)cc(N)c1N HHSOTJHMTWZCNK-UHFFFAOYSA-N 0.000 description 1
- FLDIDKTWHOYFMG-UHFFFAOYSA-N COc1cc(N)cc(N)c1 Chemical compound COc1cc(N)cc(N)c1 FLDIDKTWHOYFMG-UHFFFAOYSA-N 0.000 description 1
- AQCRFDKOKZGTDE-UHFFFAOYSA-N COc1cnc(cccc2)c2c1 Chemical compound COc1cnc(cccc2)c2c1 AQCRFDKOKZGTDE-UHFFFAOYSA-N 0.000 description 1
- QXEYUZJKIGDWKA-UHFFFAOYSA-N CS(C)C(C=CC#N)=O Chemical compound CS(C)C(C=CC#N)=O QXEYUZJKIGDWKA-UHFFFAOYSA-N 0.000 description 1
- ZTWYBFHLUJUUDX-UHFFFAOYSA-N Nc(nc1)ccc1O Chemical compound Nc(nc1)ccc1O ZTWYBFHLUJUUDX-UHFFFAOYSA-N 0.000 description 1
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- C—CHEMISTRY; METALLURGY
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- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
- C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/10—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulphur atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
- C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
- C07D295/182—Radicals derived from carboxylic acids
- C07D295/185—Radicals derived from carboxylic acids from aliphatic carboxylic acids
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- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201462055188P | 2014-09-25 | 2014-09-25 | |
US62/055,188 | 2014-09-25 | ||
PCT/US2015/052349 WO2016049524A1 (en) | 2014-09-25 | 2015-09-25 | Inhibitors of kras g12c mutant proteins |
Publications (2)
Publication Number | Publication Date |
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JP2017528498A true JP2017528498A (ja) | 2017-09-28 |
JP2017528498A5 JP2017528498A5 (US07794700-20100914-C00152.png) | 2018-11-01 |
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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JP2017516106A Pending JP2017528498A (ja) | 2014-09-25 | 2015-09-25 | Kras g12c変異体タンパク質のインヒビター |
Country Status (6)
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2020085493A1 (ja) * | 2018-10-26 | 2020-04-30 | 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 |
JP2021020948A (ja) * | 2017-05-22 | 2021-02-18 | アムジエン・インコーポレーテツド | Kras g12c阻害剤及びその使用方法 |
US11697657B2 (en) | 2019-10-28 | 2023-07-11 | Merck Sharp & Dohme Llc | Small molecule inhibitors of KRAS G12C mutant |
Families Citing this family (98)
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US20150087628A1 (en) | 2012-04-10 | 2015-03-26 | The Regents Of The University Of California | Compositions and methods for treating cancer |
US9227978B2 (en) | 2013-03-15 | 2016-01-05 | Araxes Pharma Llc | Covalent inhibitors of Kras G12C |
US9745319B2 (en) | 2013-03-15 | 2017-08-29 | Araxes Pharma Llc | Irreversible covalent inhibitors of the GTPase K-Ras G12C |
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 |
WO2016049524A1 (en) | 2014-09-25 | 2016-03-31 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
BR112017021869A2 (pt) | 2015-04-10 | 2018-12-11 | Araxes Pharma Llc | compostos quinazolina substituídos e métodos de uso dos mesmos |
EP3283462B1 (en) | 2015-04-15 | 2020-12-02 | Araxes Pharma LLC | Fused-tricyclic inhibitors of kras and methods of use thereof |
US10144724B2 (en) | 2015-07-22 | 2018-12-04 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
US10882847B2 (en) | 2015-09-28 | 2021-01-05 | 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 |
WO2017058768A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
EP3356354A1 (en) | 2015-09-28 | 2018-08-08 | 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 |
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US10689356B2 (en) | 2015-09-28 | 2020-06-23 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
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JP7039489B2 (ja) | 2016-05-18 | 2022-03-22 | 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 |
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 |
TW201815766A (zh) * | 2016-09-22 | 2018-05-01 | 美商普雷辛肯公司 | 用於ido及tdo調節之化合物及方法以及其適應症 |
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WO2016049524A1 (en) | 2016-03-31 |
US20180141927A1 (en) | 2018-05-24 |
ES2826443T3 (es) | 2021-05-18 |
US20160108019A1 (en) | 2016-04-21 |
AR102094A1 (es) | 2017-02-01 |
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US9862701B2 (en) | 2018-01-09 |
EP3197870A1 (en) | 2017-08-02 |
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