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

Info

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
Authority
CN
China
Prior art keywords
benzo
thiophene
pyrimidin
carboxylic acid
sup
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.)
Expired - Fee Related
Application number
CN2006800428126A
Other languages
English (en)
Chinese (zh)
Other versions
CN101309918A (zh
Inventor
K·R·达恩克
H-S·林
C·希恩
Q·M·王
张波
M·E·里凯特
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Eli Lilly and Co
Original Assignee
Eli Lilly and Co
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Eli Lilly and Co filed Critical Eli Lilly and Co
Publication of CN101309918A publication Critical patent/CN101309918A/zh
Application granted granted Critical
Publication of CN101309918B publication Critical patent/CN101309918B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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

Landscapes

  • 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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (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

Family

ID=38345605

Family Applications (1)

Application Number Title Priority Date Filing Date
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)

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RS51423B (sr) 2006-03-31 2011-02-28 Janssen Pharmaceutica N.V. Benzoimidazol-2-il pirimidini i pirazini kao modulatori histaminskog h4 receptora
WO2008011557A2 (en) * 2006-07-20 2008-01-24 Borchardt Allen J Heteroaryl inhibitors of rho kinase
MX2009006635A (es) 2006-12-21 2009-06-30 Lilly Co Eli Compuestos de imidazolidinonil aminopirimidina para el tratamiento de cancer.
AU2007334039B2 (en) 2006-12-21 2012-02-16 Eli Lilly And Company Imidazolidinonyl aminopyrimidine compounds for the treatment' of cancer
BRPI0811433A2 (pt) 2007-05-16 2016-03-22 Lilly Co Eli compostos do tipo triazolil aminopirimidina
US8114872B2 (en) 2007-05-16 2012-02-14 Eli Lilly And Company Triazolyl aminopyrimidine compounds
PT2310012E (pt) 2008-06-30 2015-04-02 Janssen Pharmaceutica Nv Processo para a preparação de derivados de pirimidina substituída
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
WO2011022473A1 (en) 2009-08-19 2011-02-24 Ambit Biosciences Corporation Biaryl compounds and methods of use thereof
MX2012012502A (es) 2010-04-27 2013-01-18 Hutchison Medipharma Ltd Compuestos pirimidinil indol.
US20140194383A1 (en) 2011-04-07 2014-07-10 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
JP6250561B2 (ja) 2012-02-08 2017-12-20 サノビオン ファーマシューティカルズ インクＳｕｎｏｖｉｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃ． ヘテロアリール化合物およびそれらの使用方法
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
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
CN110087687A (zh) 2016-07-29 2019-08-02 赛诺维信制药公司 化合物、组合物及其用途
CA3032302A1 (en) 2016-07-29 2018-02-01 Taleen G. Hanania Compounds and compositions and uses 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
EP3573964A1 (en) * 2017-01-26 2019-12-04 Araxes Pharma LLC Benzothiophene and benzothiazole compounds and methods of use thereof
US11274093B2 (en) 2017-01-26 2022-03-15 Araxes Pharma Llc Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
WO2018140514A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc 1-(6-(3-hydroxynaphthalen-1-yl)quinazolin-2-yl)azetidin-1-yl)prop-2-en-1-one derivatives and similar compounds as kras g12c inhibitors for the treatment of cancer
EP3630745A2 (en) 2017-05-25 2020-04-08 Araxes Pharma LLC Covalent inhibitors of kras
CN110831933A (zh) 2017-05-25 2020-02-21 亚瑞克西斯制药公司 喹唑啉衍生物作为突变kras、hras或nras的调节剂
CN111183138A (zh) 2017-08-02 2020-05-19 赛诺维信制药公司 异色满化合物以及用途
BR112021001709A2 (pt) 2018-08-01 2021-05-04 Araxes Pharma Llc compostos espiro heterocíclicos e métodos de uso dos mesmos para o tratamento de câncer
MX2021010880A (es) 2019-03-14 2022-01-18 Sunovion Pharmaceuticals Inc Sales de un compuesto de isocromanilo y formas cristalinas, procesos de preparacion, usos terapeuticos y composiciones farmaceuticas de las mismas.

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004089913A1 (en) * 2003-04-11 2004-10-21 Novartis Ag Aminopyrimidine derivatives and their medical use

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU3752589A (en) * 1988-05-16 1989-12-12 Georgia State University Research Foundation, Inc. Nucleic acid interacting unfused heteropolycyclic compounds
JP4932735B2 (ja) * 2004-12-17 2012-05-16 アムジエン・インコーポレーテツド アミノピリミジン化合物および使用方法

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004089913A1 (en) * 2003-04-11 2004-10-21 Novartis Ag Aminopyrimidine derivatives and their medical use

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
王勇等.IκB激酶的激活及其在NF-κB活化过程中的作用.《生物化学与生物物理进展》.2001,第28卷(第4期),455-458. *
王宁等.IκB激酶的结构和功能.《生命的化学》.2000,第20卷(第3期),97-99. *

Also Published As

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

Similar Documents

Publication Publication Date Title
CN101309918B (zh) 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
CN104080774B (zh) 吡嗪甲酰胺化合物
EP2044051B1 (en) Pyridine and pyrazine derivatives as mnk kinase inhibitors
TWI753892B (zh) 作為ｔａｍ抑制劑之吡咯并三嗪化合物
CN103626742B (zh) 激酶的联-芳基间-嘧啶抑制剂
CN103702990B (zh) 2-(2,4,5-取代苯胺)嘧啶衍生物作为egfr调谐子用于治疗癌症
CN104854101B (zh) Alk激酶抑制剂
CN105143206A (zh) 用于治疗癌症的嘧啶-2,4-二胺衍生物
KR20100016431A (ko) 약학적 화합물
US20090233928A1 (en) Imidazolo-5-yl-2-anilo-pyrimidines as agents for the inhibition of cell proliferation
CN101765597A (zh) 作为磷脂酰肌醇-3-激酶抑制剂的嘧啶衍生物
CN113637007A (zh) Rho激酶抑制剂
CN102421761A (zh) 二氨基杂环甲酰胺化合物
CN101484420A (zh) 作为5-ht6调节剂的吲哚
WO2018049781A1 (zh) 炔代杂环化合物、其制备方法及其在医药学上的应用
CN114105887B (zh) 一种氨基嘧啶衍生物及其制备方法和用途
CN107454899B (zh) Ripk2抑制剂及用其治疗癌症的方法
TW201934546A (zh) 嘧啶類化合物、其製備方法及其醫藥用途
CN101370792B (zh) 激酶的联-芳基间-嘧啶抑制剂
CN101273047A (zh) 作为蛋白激酶抑制剂的噻吩并[2,3-b]吡啶-5-甲腈
CN101258154B (zh) 作为组胺h3拮抗剂的吡唑并[3,4-d]氮杂䓬衍生物
CN101479277A (zh) 作为pi3k抑制剂的嘧啶衍生物
CN101668749A (zh) 新的嘧啶衍生物698
HK1203491B (en) Pyrazine carboxamide compound
CN1938295A (zh) 咪唑－5－基－苯胺基嘧啶类细胞增殖抑制剂

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C14 Grant of patent or utility model
GR01 Patent grant
C17 Cessation of patent right
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20101229

Termination date: 20131115