CN101309918B - 作为IKK-β抑制剂用于治疗癌症和炎性疾病的[4-(苯并[B]噻吩-2-基)嘧啶-2-基]-胺衍生物 - Google Patents

作为IKK-β抑制剂用于治疗癌症和炎性疾病的[4-(苯并[B]噻吩-2-基)嘧啶-2-基]-胺衍生物 Download PDF

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Publication number
CN101309918B
CN101309918B CN2006800428126A CN200680042812A CN101309918B CN 101309918 B CN101309918 B CN 101309918B CN 2006800428126 A CN2006800428126 A CN 2006800428126A CN 200680042812 A CN200680042812 A CN 200680042812A CN 101309918 B CN101309918 B CN 101309918B
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China
Prior art keywords
benzo
thiophene
pyrimidin
carboxylic acid
sup
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Chinese (zh)
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CN101309918A (zh
Inventor
K·R·达恩克
H-S·林
C·希恩
Q·M·王
张波
M·E·里凯特
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Eli Lilly and Co
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Eli Lilly and Co
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN2006800428126A 2005-11-18 2006-11-15 作为IKK-β抑制剂用于治疗癌症和炎性疾病的[4-(苯并[B]噻吩-2-基)嘧啶-2-基]-胺衍生物 Expired - Fee Related CN101309918B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US73809705P 2005-11-18 2005-11-18
US60/738,097 2005-11-18
PCT/US2006/060911 WO2007092095A2 (en) 2005-11-18 2006-11-15 [4-(benzo [b] thi0phen-2-yl) pyrimidin-2yl] -amine derivatives as ikk-beta inhibitors for the treatment of cancer and inflammatory diseases.

Publications (2)

Publication Number Publication Date
CN101309918A CN101309918A (zh) 2008-11-19
CN101309918B true CN101309918B (zh) 2010-12-29

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CN2006800428126A Expired - Fee Related CN101309918B (zh) 2005-11-18 2006-11-15 作为IKK-β抑制剂用于治疗癌症和炎性疾病的[4-(苯并[B]噻吩-2-基)嘧啶-2-基]-胺衍生物

Country Status (27)

Country Link
US (1) US7547691B2 (enExample)
EP (1) EP1989200B1 (enExample)
JP (1) JP2009516697A (enExample)
KR (1) KR100990771B1 (enExample)
CN (1) CN101309918B (enExample)
AR (1) AR057911A1 (enExample)
AT (1) ATE437873T1 (enExample)
AU (1) AU2006337626B2 (enExample)
BR (1) BRPI0618245A2 (enExample)
CA (1) CA2629336A1 (enExample)
CR (1) CR9947A (enExample)
DE (1) DE602006008187D1 (enExample)
DK (1) DK1989200T3 (enExample)
EA (1) EA014426B1 (enExample)
EC (1) ECSP088456A (enExample)
ES (1) ES2329085T3 (enExample)
IL (1) IL190489A0 (enExample)
MA (1) MA30053B1 (enExample)
NO (1) NO20082594L (enExample)
PE (1) PE20070833A1 (enExample)
PL (1) PL1989200T3 (enExample)
PT (1) PT1989200E (enExample)
SI (1) SI1989200T1 (enExample)
TN (1) TNSN08227A1 (enExample)
TW (1) TW200800201A (enExample)
WO (1) WO2007092095A2 (enExample)
ZA (1) ZA200803940B (enExample)

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KR101054325B1 (ko) 2006-03-31 2011-08-04 얀센 파마슈티카 엔.브이. 히스타민 ｈ４ 수용체 조절제로서의 벤조이미다졸―２―일 피리미딘 및 피라진
CN101790527A (zh) * 2006-07-20 2010-07-28 凯利普西斯公司 Rho激酶的苯并噻吩抑制剂
WO2008076705A1 (en) * 2006-12-21 2008-06-26 Eli Lilly And Company Imidazolidinonyl aminopyrimidine compounds for the treatment of cancer
JP5166441B2 (ja) * 2006-12-21 2013-03-21 イーライ リリー アンド カンパニー 癌治療用イミダゾリジノニルアミノピリミジン化合物
JP5248600B2 (ja) 2007-05-16 2013-07-31 イーライ リリー アンド カンパニー トリアゾリルアミノピリミジン化合物
AU2008254318B2 (en) 2007-05-16 2012-04-05 Eli Lilly And Company Triazolyl aminopyrimidine compounds
EP2310012B1 (en) 2008-06-30 2015-03-04 Janssen Pharmaceutica N.V. Process for the preparation of substituted pyrimidine derivatives
US9371311B2 (en) 2008-06-30 2016-06-21 Janssen Pharmaceutica Nv Benzoimidazol-2-yl pyrimidine derivatives
KR101123178B1 (ko) * 2009-04-09 2012-06-13 (주)에스메디 2-아릴벤조싸이오펜 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 퇴행성 뇌질환의 진단 또는 치료용 약학적 조성물
KR20120059558A (ko) 2009-08-19 2012-06-08 암비트 바이오사이언시즈 코포레이션 바이아릴 화합물 및 이의 사용 방법
KR20130069641A (ko) 2010-04-27 2013-06-26 허치슨 메디파르마 리미티드 피리미디닐 인돌 화합물
EP2694707B1 (en) 2011-04-07 2018-08-15 Cornell University Monomers capable of dimerizing in an aqueous solution, and methods of using same
US9245773B2 (en) 2011-09-02 2016-01-26 Taiwan Semiconductor Manufacturing Company, Ltd. Semiconductor device packaging methods and structures thereof
CN103159742B (zh) * 2011-12-16 2015-08-12 北京韩美药品有限公司 5-氯嘧啶类化合物及其作为egfr酪氨酸激酶抑制剂的应用
AU2013216935C1 (en) 2012-02-08 2017-12-14 John Emmerson Campbell Heteroaryl compounds and methods of use thereof
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of 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
CN105085434B (zh) * 2014-05-09 2018-02-09 上海特化医药科技有限公司 硫乙拉嗪或其中间体的制备方法
WO2017076888A1 (en) 2015-11-03 2017-05-11 Janssen Pharmaceutica Nv 2-[3-(1-methyl-piperidin-4-yl)-propylamino]-pyrimidine-5-carboxylic acids and amides and methods of making the same
ES2996835T3 (en) 2016-07-29 2025-02-13 Sumitomo Pharma America Inc Compounds and compositions and uses thereof
MA45795A (fr) 2016-07-29 2019-06-05 Sunovion Pharmaceuticals Inc Composés et compositions, et utilisations associées
WO2018140512A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
US11136308B2 (en) 2017-01-26 2021-10-05 Araxes Pharma Llc Substituted quinazoline and quinazolinone compounds and methods of use thereof
WO2018140599A1 (en) * 2017-01-26 2018-08-02 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
US11279689B2 (en) 2017-01-26 2022-03-22 Araxes Pharma Llc 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1 yl)prop-2-en-1-one derivatives and similar compounds as KRAS G12C modulators for treating cancer
KR20200010306A (ko) 2017-05-25 2020-01-30 아락세스 파마 엘엘씨 Kras의 공유적 억제제
US11639346B2 (en) 2017-05-25 2023-05-02 Araxes Pharma Llc Quinazoline derivatives as modulators of mutant KRAS, HRAS or NRAS
AU2018312559B2 (en) 2017-08-02 2022-06-02 Pgi Drug Discovery Llc Isochroman compounds and uses thereof
US12134620B2 (en) 2018-08-01 2024-11-05 Araxes Pharma Llc Heterocyclic spiro compounds and methods of use thereof for the treatment of cancer
WO2020186165A1 (en) 2019-03-14 2020-09-17 Sunovion Pharmaceuticals Inc. Salts of a isochromanyl compound and crystalline forms, processes for preparing, therapeutic uses, and pharmaceutical compositions thereof

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Also Published As

Publication number Publication date
AU2006337626B2 (en) 2012-03-22
PL1989200T3 (pl) 2009-12-31
US7547691B2 (en) 2009-06-16
EP1989200A2 (en) 2008-11-12
ECSP088456A (es) 2008-06-30
ATE437873T1 (de) 2009-08-15
US20080306082A1 (en) 2008-12-11
ES2329085T3 (es) 2009-11-20
DE602006008187D1 (de) 2009-09-10
CR9947A (es) 2008-11-28
NO20082594L (no) 2008-06-10
TNSN08227A1 (en) 2009-10-30
AU2006337626A8 (en) 2008-06-19
JP2009516697A (ja) 2009-04-23
MA30053B1 (fr) 2008-12-01
CN101309918A (zh) 2008-11-19
TW200800201A (en) 2008-01-01
PE20070833A1 (es) 2007-08-27
AR057911A1 (es) 2007-12-26
WO2007092095A2 (en) 2007-08-16
DK1989200T3 (da) 2009-11-09
PT1989200E (pt) 2009-10-12
BRPI0618245A2 (pt) 2011-08-23
KR20080059451A (ko) 2008-06-27
AU2006337626A1 (en) 2007-08-16
CA2629336A1 (en) 2007-08-16
IL190489A0 (en) 2008-11-03
EA200801362A1 (ru) 2009-02-27
SI1989200T1 (sl) 2009-12-31
WO2007092095A3 (en) 2007-11-08
ZA200803940B (en) 2009-09-30
EP1989200B1 (en) 2009-07-29
EA014426B1 (ru) 2010-12-30
KR100990771B1 (ko) 2010-10-29

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Granted publication date: 20101229

Termination date: 20131115