TW201524952A - Ｋｒａｓ ｇ１２ｃ之共價抑制劑 - Google Patents

Ｋｒａｓ ｇ１２ｃ之共價抑制劑 Download PDF

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TW201524952A
TW201524952A TW103109459A TW103109459A TW201524952A TW 201524952 A TW201524952 A TW 201524952A TW 103109459 A TW103109459 A TW 103109459A TW 103109459 A TW103109459 A TW 103109459A TW 201524952 A TW201524952 A TW 201524952A
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TW103109459A
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Chinese (zh)
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ping-da Ren
Yi Liu
Lian-Sheng Li
Jun Feng
Tao Wu
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Araxes Pharma Llc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/56—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/56—Nitrogen atoms
    • C07D211/58—Nitrogen atoms attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
    • 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/64—One oxygen atom attached in position 2 or 6
    • 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
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/38—Nitrogen atoms
    • C07D231/40—Acylated on said nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/04—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having less than three double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/14—Thiadiazoles; Hydrogenated thiadiazoles condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/15—Six-membered rings
    • C07D285/16—Thiadiazines; Hydrogenated thiadiazines
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D401/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
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    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
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    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D419/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms containing two hetero rings
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • C07D487/10—Spiro-condensed systems
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/58—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving labelled substances

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  • Chemical & Material Sciences (AREA)
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  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Urology & Nephrology (AREA)
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  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Microbiology (AREA)
  • Physics & Mathematics (AREA)
  • Analytical Chemistry (AREA)
  • Biochemistry (AREA)
  • Cell Biology (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biotechnology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Food Science & Technology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
TW103109459A 2013-03-15 2014-03-14 Ｋｒａｓ ｇ１２ｃ之共價抑制劑 TW201524952A (zh)

Applications Claiming Priority (3)

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US201361852123P 2013-03-15 2013-03-15
US201361889480P 2013-10-10 2013-10-10
JOP20140098 2014-03-13

Publications (1)

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TW201524952A true TW201524952A (zh) 2015-07-01

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EP (2) EP2970121B1 (OSRAM)
JP (2) JP6473133B2 (OSRAM)
CN (1) CN105189456B (OSRAM)
AU (2) AU2014239542A1 (OSRAM)
CA (1) CA2904393A1 (OSRAM)
MX (1) MX364438B (OSRAM)
TW (1) TW201524952A (OSRAM)
WO (1) WO2014152588A1 (OSRAM)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI862525B (zh) * 2018-11-16 2024-11-21 美商安進公司 Kras g12c抑制劑化合物的關鍵中間體之改善合成

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* Cited by examiner, † Cited by third party
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JP6433974B2 (ja) 2013-03-14 2018-12-05 トレロ ファーマシューティカルズ， インコーポレイテッド Ｊａｋ２およびａｌｋ２阻害剤およびその使用方法
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.
TWI659021B (zh) 2013-10-10 2019-05-11 亞瑞克西斯製藥公司 Ｋｒａｓ ｇ１２ｃ之抑制劑
KR102509043B1 (ko) 2014-06-06 2023-03-09 리써치 트라이앵글 인스티튜트 아펠린 수용체(apj) 효능제 및 이의 용도
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
US9862701B2 (en) 2014-09-25 2018-01-09 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2016049568A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Methods and compositions for inhibition of ras
AU2016240033B2 (en) 2015-03-30 2020-04-16 Mission Therapeutics Limited 1-cyano-pyrrolidine compounds as USP30 inhibitors
EA201792214A1 (ru) * 2015-04-10 2018-01-31 Араксис Фарма Ллк Соединения замещенного хиназолина
JP6789239B2 (ja) * 2015-04-15 2020-11-25 アラクセス ファーマ エルエルシー Ｋｒａｓの縮合三環系インヒビターおよびその使用の方法
CA2983927A1 (en) 2015-05-06 2016-11-10 The Regents Of The University Of California K-ras modulators
US10463649B2 (en) 2015-06-08 2019-11-05 Texas Tech University System Inhibitors of Mc1-1 as drugs to overcome resistance to BRAF inhibitors and MEK inhibitors
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
WO2017058728A1 (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
EP3356347A1 (en) 2015-09-28 2018-08-08 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
US10689356B2 (en) 2015-09-28 2020-06-23 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
US10882847B2 (en) 2015-09-28 2021-01-05 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
EP3364977A4 (en) 2015-10-19 2019-09-04 Araxes Pharma LLC PROCESS 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
PE20190258A1 (es) 2015-12-09 2019-02-25 Res Triangle Inst Antagonistas del receptor de la apelina (apj) mejorados y usos de los mismos
US9988357B2 (en) 2015-12-09 2018-06-05 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
AU2017266911B2 (en) * 2016-05-18 2021-09-02 Array Biopharma, 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
US11260049B2 (en) 2016-09-20 2022-03-01 Glaxosmithkline Intellectual Property (No. 2) Limited TRPV4 antagonists
TW201825458A (zh) 2016-09-20 2018-07-16 英商葛蘭素史克智慧財產（第二）有限公司 Ｔｒｐｖ４拮抗劑
WO2018055527A1 (en) 2016-09-20 2018-03-29 Glaxosmithkline Intellectual Property (No.2) Limited Trpv4 antagonists
JP2019529484A (ja) 2016-09-29 2019-10-17 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阻害剤
CN110312711A (zh) 2016-10-07 2019-10-08 亚瑞克西斯制药公司 作为ras抑制剂的杂环化合物及其使用方法
WO2018098352A2 (en) 2016-11-22 2018-05-31 Jun Oishi Targeting kras induced immune checkpoint expression
AU2017378487B2 (en) * 2016-12-15 2022-03-31 The Regents Of The University Of California Compositions and methods for treating cancer
EP3878850A1 (en) 2016-12-22 2021-09-15 Boehringer Ingelheim International GmbH Novel benzylamino substituted quinazolines and derivatives as sos1 inhibitors
SI3558955T1 (sl) * 2016-12-22 2021-12-31 Amgen Inc., Derivati benzizotiazola, izotiazola(3,4-b)piridina, kinazolina, ftalazina, pirido(2,3-d)piridazina in pirido(2,3-D)pirimidina, kot zaviralci KRAS G12C za zdravljenje pljučnega raka, raka trebušne slinavke ali kolorektalnega raka
WO2018143403A1 (ja) 2017-02-03 2018-08-09 国立大学法人東北大学 複素環化合物
JP6594570B2 (ja) 2017-03-20 2019-10-23 フォーマ セラピューティクス，インコーポレイテッド ピルビン酸キナーゼ（ｐｋｒ）活性化剤としてのピロロピロール組成物
SG11201909570PA (en) * 2017-04-20 2019-11-28 Univ California K-ras modulators
JOP20190272A1 (ar) 2017-05-22 2019-11-21 Amgen Inc مثبطات kras g12c وطرق لاستخدامها
US10745385B2 (en) 2017-05-25 2020-08-18 Araxes Pharma Llc Covalent inhibitors of KRAS
TW201906832A (zh) 2017-05-25 2019-02-16 美商亞瑞克西斯製藥公司 用於癌症治療之化合物及其使用方法
EP3679040B1 (en) 2017-09-08 2022-08-03 Amgen Inc. Inhibitors of kras g12c and methods of using the same
WO2019084026A1 (en) 2017-10-24 2019-05-02 Genentech, Inc. (4-HYDROXYPYRROLIDIN-2-YL) -HETEROCYCLIC COMPOUNDS AND METHODS OF USE
US10647715B2 (en) 2017-11-15 2020-05-12 Mirati Therapeutics, Inc. KRas G12C inhibitors
EP3710439B1 (en) 2017-11-15 2023-02-15 Mirati Therapeutics, Inc. Kras g12c inhibitors
DK3728254T3 (da) 2017-12-21 2023-06-06 Boehringer Ingelheim Int Benzylamin-substituerede pyridopyrimidinoner og derivater som sos1-inhibitorer
RS63124B1 (sr) 2018-03-08 2022-05-31 Incyte Corp Aminopirazin diol jedinjenja kao pi3k-y inhibitori
AU2019247498A1 (en) 2018-04-05 2020-11-26 Sumitomo Pharma Oncology, Inc. AXL kinase inhibitors and use of the same
TW202012396A (zh) * 2018-04-18 2020-04-01 美商德洛斯股份有限公司 具乙烯磺醯胺部分之k-ras調節劑
MA52496A (fr) 2018-05-04 2021-03-10 Amgen Inc Inhibiteurs de kras g12c et leurs procédés d'utilisation
JP7266043B2 (ja) 2018-05-04 2023-04-27 アムジエン・インコーポレーテツド ＫＲａｓ Ｇ１２Ｃ阻害剤及びそれを使用する方法
US11932633B2 (en) 2018-05-07 2024-03-19 Mirati Therapeutics, Inc. KRas G12C inhibitors
TW202012415A (zh) 2018-05-08 2020-04-01 瑞典商阿斯特捷利康公司 化學化合物
MA52564A (fr) 2018-05-10 2021-03-17 Amgen Inc Inhibiteurs de kras g12c pour le traitement du cancer
MA52765A (fr) 2018-06-01 2021-04-14 Amgen Inc Inhibiteurs de kras g12c et leurs procédés d'utilisation
MA51848A (fr) 2018-06-12 2021-04-21 Amgen Inc Inhibiteurs de kras g12c et leurs procédés d'utilisation
US11046658B2 (en) 2018-07-02 2021-06-29 Incyte Corporation Aminopyrazine derivatives as PI3K-γ inhibitors
AU2019310590A1 (en) 2018-07-26 2021-01-14 Sumitomo Pharma Oncology, Inc. Methods for treating diseases associated with abnormal acvr1 expression and acvr1 inhibitors for use in the same
US12336995B2 (en) 2018-09-10 2025-06-24 Mirati Therapeutics, Inc. Combination therapies
HRP20250059T1 (hr) 2018-09-10 2025-03-28 Mirati Therapeutics, Inc. Kombinirane terapije
WO2020055760A1 (en) 2018-09-10 2020-03-19 Mirati Therapeutics, Inc. Combination therapies
WO2020061378A1 (en) 2018-09-19 2020-03-26 Forma Therapeutics, Inc. Treating sickle cell disease with a pyruvate kinase r activating compound
WO2020061255A1 (en) 2018-09-19 2020-03-26 Forma Therapeutics, Inc. Activating pyruvate kinase r
EP3628664A1 (en) 2018-09-25 2020-04-01 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Irreversible inhibitors of kras g12c mutant
EP3870585A1 (en) * 2018-10-24 2021-09-01 Araxes Pharma LLC 2-(2-acryloyl-2,6-diazaspiro[3.4]octan-6-yl)-6-(1h-indazol-4-yl)-benzonitrile derivatives and related compounds as inhibitors of g12c mutant kras protein for inhibiting tumor metastasis
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
EP3883565A1 (en) * 2018-11-19 2021-09-29 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
JP2022509724A (ja) 2018-12-05 2022-01-24 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
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
CN109646680B (zh) * 2019-01-31 2020-02-11 四川大学华西医院 一种治疗kras突变型肠癌的联合用药物
EP3924053A1 (en) 2019-02-12 2021-12-22 Novartis AG Pharmaceutical combination comprising tno155 and a krasg12c inhibitor
JP7426398B2 (ja) 2019-02-26 2024-02-01 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 Ｒａｓ阻害剤としての新規イソインドリノン置換インドールおよび誘導体
SG11202109451TA (en) 2019-03-05 2021-09-29 Astrazeneca Ab Fused tricyclic compounds useful as anticancer agents
CN111662232B (zh) * 2019-03-06 2022-08-02 中国科学院上海药物研究所 具有2h-吲唑结构的小分子化合物及其合成和应用
WO2020205867A1 (en) 2019-04-02 2020-10-08 Aligos Therapeutics, Inc. Compounds targeting prmt5
EP3738593A1 (en) 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
EP3972963A1 (en) 2019-05-21 2022-03-30 Bayer Aktiengesellschaft Identification and use of kras inhibitors
JP7092935B2 (ja) 2019-05-21 2022-06-28 アムジエン・インコーポレーテツド 固体形態
WO2020239123A1 (zh) * 2019-05-31 2020-12-03 上海翰森生物医药科技有限公司 芳香杂环类衍生物调节剂、其制备方法和应用
US12421236B2 (en) 2019-06-25 2025-09-23 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Seven-membered heterocyclic derivative acting as KRAS G12C mutant protein inhibitor
JP7622043B2 (ja) 2019-08-29 2025-01-27 ミラティ セラピューティクス， インコーポレイテッド Ｋｒａｓ ｇ１２ｄ阻害剤
AU2020350763A1 (en) 2019-09-19 2022-04-07 Novo Nordisk Health Care Ag Pyruvate kinase R (PKR) activating compositions
AU2020356455A1 (en) 2019-09-24 2022-04-14 Mirati Therapeutics, Inc. Combination therapies
CN112225734B (zh) * 2019-10-25 2021-12-07 南京瑞捷医药科技有限公司 Kras g12c抑制剂及其用途
PE20221253A1 (es) 2019-10-28 2022-08-16 Merck Sharp & Dohme Inhibidores de pequenas moleculas de mutante g12c de kras
CN115551500A (zh) 2019-10-31 2022-12-30 大鹏药品工业株式会社 4-氨基丁-2-烯酰胺衍生物及其盐
US11739074B2 (en) 2019-11-04 2023-08-29 Revolution Medicines, Inc. Ras inhibitors
CR20220241A (es) 2019-11-04 2022-08-03 Revolution Medicines Inc Inhibidores de ras
BR112022008535A2 (pt) 2019-11-04 2022-08-09 Revolution Medicines Inc Composto, composição farmacêutica, métodos para tratar câncer e um distúrbio relativo à proteína ras
CN110698378B (zh) * 2019-11-19 2021-03-19 上海皓元生物医药科技有限公司 2-(羟基-(甲基环丙基)苯基氨基)-1-哌嗪基乙酮衍生物的制备方法
MX2022006052A (es) * 2019-11-22 2022-08-15 Univ California Inhibidores de la caspasa 6 y usos de los mismos.
CN114980976A (zh) 2019-11-27 2022-08-30 锐新医药公司 共价ras抑制剂及其用途
US12479834B2 (en) 2019-11-29 2025-11-25 Taiho Pharmaceutical Co., Ltd. Phenol compound or salt thereof
CN115135315B (zh) 2019-12-20 2024-11-26 米拉蒂治疗股份有限公司 Sos1抑制剂
WO2021120890A1 (en) 2019-12-20 2021-06-24 Novartis Ag Pyrazolyl derivatives useful as anti-cancer agents
CN113045565A (zh) * 2019-12-27 2021-06-29 微境生物医药科技(上海)有限公司 新型K-Ras G12C抑制剂
US20230181536A1 (en) * 2020-04-24 2023-06-15 Taiho Pharmaceutical Co., Ltd. Anticancer combination therapy with n-(1-acryloyl-azetidin-3-yl)-2-((1h-indazol-3-yl)amino)methyl)-1h-imidazole-5-carboxamide inhibitor of kras-g12c
WO2021215544A1 (en) * 2020-04-24 2021-10-28 Taiho Pharmaceutical Co., Ltd. Kras g12d protein inhibitors
CN115135636B (zh) * 2020-04-29 2024-08-23 北京泰德制药股份有限公司 喹喔啉酮衍生物作为kras g12c突变蛋白的不可逆抑制剂
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
EP4168002A1 (en) 2020-06-18 2023-04-26 Revolution Medicines, Inc. Methods for delaying, preventing, and treating acquired resistance to ras inhibitors
IL301062A (en) 2020-09-03 2023-05-01 Revolution Medicines Inc Use of sos1 inhibitors to treat malignancies with shp2 mutations
JP2023540809A (ja) 2020-09-11 2023-09-26 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阻害剤の結晶形態
US11690915B2 (en) 2020-09-15 2023-07-04 Revolution Medicines, Inc. Ras inhibitors
MX2023003338A (es) 2020-09-23 2023-06-14 Erasca Inc Piridonas y pirimidonas tricíclicas.
CN114249703B (zh) * 2020-09-25 2023-10-13 四川科瑞德制药股份有限公司 适合工业放大的医药中间体的制备方法
KR20230142465A (ko) 2020-12-15 2023-10-11 미라티 테라퓨틱스, 인크. 아자퀴나졸린 범-KRas 저해제
WO2022133038A1 (en) 2020-12-16 2022-06-23 Mirati Therapeutics, Inc. Tetrahydropyridopyrimidine pan-kras inhibitors
US20230107642A1 (en) 2020-12-18 2023-04-06 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
CA3203111A1 (en) 2020-12-22 2022-06-30 Kailiang Wang Sos1 inhibitors and uses thereof
US12128035B2 (en) 2021-03-19 2024-10-29 Novo Nordisk Health Care Ag Activating pyruvate kinase R
IL308193A (en) 2021-05-05 2024-01-01 Revolution Medicines Inc RAS inhibitors
EP4334325A1 (en) 2021-05-05 2024-03-13 Revolution Medicines, Inc. Ras inhibitors for the treatment of cancer
US20240293558A1 (en) 2021-06-16 2024-09-05 Erasca, Inc. Kras inhibitor conjugates
US20240317721A1 (en) 2021-06-23 2024-09-26 Novartis Ag Pyrazolyl derivatives as inhibitors of the kras mutant protein
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
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
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
JP2024539228A (ja) 2021-10-22 2024-10-28 江▲蘇▼恒瑞医▲薬▼股▲フン▼有限公司 含窒素四環式化合物、その調製方法及びその医薬的使用
CN113956233B (zh) * 2021-10-22 2023-06-06 南方医科大学 一种酰胺类化合物或其药学上可接受的盐及其制备方法和应用
CN114380682A (zh) * 2021-10-27 2022-04-22 上海毕得医药科技股份有限公司 一种2,3-二氟-4-甲氧基苯乙酸合成方法
US20250282782A1 (en) 2021-12-17 2025-09-11 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
EP4476221A1 (en) 2022-02-10 2024-12-18 Bayer Aktiengesellschaft Fused pyrimidines as kras inhibitors
EP4227307A1 (en) 2022-02-11 2023-08-16 Genzyme Corporation Pyrazolopyrazine compounds as 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
WO2023199180A1 (en) 2022-04-11 2023-10-19 Novartis Ag Therapeutic uses of a krasg12c inhibitor
EP4536364A1 (en) 2022-06-10 2025-04-16 Revolution Medicines, Inc. Macrocyclic ras inhibitors
WO2024102421A2 (en) 2022-11-09 2024-05-16 Revolution Medicines, Inc. Compounds, complexes, and methods for their preparation and of their use
WO2024182447A1 (en) * 2023-02-28 2024-09-06 Vividion Therapeutics, Inc. Compounds and methods for modulating ras-pi3k
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
AR132338A1 (es) 2023-04-07 2025-06-18 Revolution Medicines Inc Inhibidores de ras
AU2024243852A1 (en) 2023-04-07 2025-11-06 Revolution Medicines, Inc. Macrocyclic ras inhibitors
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
CN121100123A (zh) 2023-04-14 2025-12-09 锐新医药公司 Ras抑制剂的结晶形式
WO2024229406A1 (en) 2023-05-04 2024-11-07 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
GB2631397A (en) 2023-06-28 2025-01-08 Sevenless Therapeutics Ltd New treatments for pain
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
GB2633813A (en) 2023-09-21 2025-03-26 Sevenless Therapeutics Ltd New treatments for pain
US20250154171A1 (en) 2023-10-12 2025-05-15 Revolution Medicines, Inc. Ras inhibitors
WO2025083426A1 (en) 2023-10-20 2025-04-24 Sevenless Therapeutics Limited New treatments for pain
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
WO2025137507A1 (en) 2023-12-22 2025-06-26 Regor Pharmaceuticals, Inc. Sos1 inhibitors and uses thereof
WO2025146548A1 (en) 2024-01-04 2025-07-10 Sevenless Therapeutics Limited Sos1 inhibitors useful to treat pain and cancer
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
CN119039303A (zh) * 2024-09-20 2024-11-29 上海信诺维生物医药有限公司 一种螺环化合物

Family Cites Families (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
GB8827305D0 (en) 1988-11-23 1988-12-29 British Bio Technology Compounds
US5323907A (en) 1992-06-23 1994-06-28 Multi-Comp, Inc. Child resistant package assembly for dispensing pharmaceutical medications
US5455258A (en) 1993-01-06 1995-10-03 Ciba-Geigy Corporation Arylsulfonamido-substituted hydroxamic acids
IL111730A (en) * 1993-11-29 1998-12-06 Fujisawa Pharmaceutical Co Piperazine derivatives processes for the preparation thereof and pharmaceutical compositions containing the same
US5863949A (en) 1995-03-08 1999-01-26 Pfizer Inc Arylsulfonylamino hydroxamic acid derivatives
MX9708026A (es) 1995-04-20 1997-11-29 Pfizer Derivados del acido arislfulfonil hidroxamico, composiciones que los contienen y uso de los mismos.
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
IL127567A0 (en) 1996-07-18 1999-10-28 Pfizer Phosphinate based inhibitors of matrix metalloproteases
JP2000501423A (ja) 1996-08-23 2000-02-08 ファイザー インク． アリールスルホニルアミノヒドロキサム酸誘導体
PT950059E (pt) 1997-01-06 2004-10-29 Pfizer Derivados de sulfona ciclicos
ES2202796T3 (es) 1997-02-03 2004-04-01 Pfizer Products Inc. Derivados de acidos arilsulfonilaminohidroxamicos.
EP0966438A1 (en) 1997-02-07 1999-12-29 Pfizer Inc. N-hydroxy-beta-sulfonyl-propionamide derivatives and their use as inhibitors of matrix metalloproteinases
CA2280151C (en) 1997-02-11 2005-12-13 Pfizer Inc. Arylsulfonyl hydroxamic acid derivatives
US6291464B1 (en) * 1997-02-17 2001-09-18 Fujisawa Pharmaceutical Co., Ltd. Aminopiperazine derivatives
CN1267291A (zh) * 1997-06-17 2000-09-20 先灵公司 新的n－取代的脲的法呢基蛋白转移酶抑制剂
GB9725782D0 (en) 1997-12-05 1998-02-04 Pfizer Ltd Therapeutic agents
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
TWI227231B (en) * 2000-07-12 2005-02-01 Novartis Ag 4-benzoyl-piperidine derivatives for treating conditions mediated by CCR-3
US7429599B2 (en) * 2000-12-06 2008-09-30 Signal Pharmaceuticals, Llc Methods for treating or preventing an inflammatory or metabolic condition or inhibiting JNK
CA2443108A1 (en) * 2001-04-03 2002-10-17 Merck & Co. Inc. N-substituted nonaryl-heterocyclo amidyl nmda/nr2b antagonists
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).
KR101146806B1 (ko) * 2003-03-12 2012-05-22 메이브릿지 리미티드 프탈라지논 유도체
US20050119266A1 (en) * 2003-10-01 2005-06-02 Yan Shi Pyrrolidine and piperidine derivatives as factor Xa inhibitors
JP4923380B2 (ja) * 2003-12-22 2012-04-25 Ｊｎｃ株式会社 低屈折率異方性化合物、組成物およびそれらの重合体または重合体組成物
US7579368B2 (en) * 2005-03-16 2009-08-25 Hoffman-La Roche Inc. Cis-imidazolines
BRPI0617271A2 (pt) * 2005-10-11 2011-07-19 Intermune Inc inibidores de replicação viral
EP2133334A1 (en) * 2008-06-09 2009-12-16 DAC S.r.l. Heterocyclic derivatives as HDAC inhibitors
TW201105665A (en) * 2009-04-22 2011-02-16 Janssen Pharmaceutica Nv Azetidinyl diamides as monoacylglycerol lipase inhibitors
CN102625708A (zh) * 2009-09-09 2012-08-01 阿维拉制药公司 Pi3激酶抑制剂及其用途
US8658131B2 (en) * 2010-06-21 2014-02-25 Washington University Compounds comprising 4-benzoylpiperidine as a sigma-1-selective ligand
CA2815350A1 (en) * 2010-10-22 2012-04-26 Janssen Pharmaceutica Nv Piperidin-4-yl-azetidine diamides as monoacylglycerol lipase inhibitors
WO2013008217A1 (en) * 2011-07-13 2013-01-17 Novartis Ag 4 - piperidinyl compounds for use as tankyrase inhibitors
WO2013106641A1 (en) * 2012-01-13 2013-07-18 Bristol-Myers Squibb Company Thiazolyl- or thiadiazolyl-substituted pyridyl compounds useful as kinase inhibitors
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

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI862525B (zh) * 2018-11-16 2024-11-21 美商安進公司 Kras g12c抑制劑化合物的關鍵中間體之改善合成

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