KR100990771B1 - 암 및 염증성 질환 치료를 위한 ｉｋｋ-베타 억제제로서의[4-벤조[ｂ]티오펜-2-일)피리미딘-2-일]-아민 유도체 - Google Patents

암 및 염증성 질환 치료를 위한 ｉｋｋ-베타 억제제로서의[4-벤조[ｂ]티오펜-2-일)피리미딘-2-일]-아민 유도체 Download PDF

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Publication number
KR100990771B1
KR100990771B1 KR1020087011830A KR20087011830A KR100990771B1 KR 100990771 B1 KR100990771 B1 KR 100990771B1 KR 1020087011830 A KR1020087011830 A KR 1020087011830A KR 20087011830 A KR20087011830 A KR 20087011830A KR 100990771 B1 KR100990771 B1 KR 100990771B1
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KR
South Korea
Prior art keywords
benzo
carboxylic acid
pyrimidin
thiophene
mmol
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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
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KR1020087011830A
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English (en)
Korean (ko)
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KR20080059451A (ko
Inventor
칼 로버트 단케
호-센 린
추안 쉬
큐 메이 왕
보 장
마이클 엔리코 리체트
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일라이 릴리 앤드 캄파니
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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)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (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)
KR1020087011830A 2005-11-18 2006-11-15 암 및 염증성 질환 치료를 위한 ｉｋｋ-베타 억제제로서의[4-벤조[ｂ]티오펜-2-일)피리미딘-2-일]-아민 유도체 Expired - Fee Related KR100990771B1 (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US73809705P 2005-11-18 2005-11-18
US60/738,097 2005-11-18

Publications (2)

Publication Number Publication Date
KR20080059451A KR20080059451A (ko) 2008-06-27
KR100990771B1 true KR100990771B1 (ko) 2010-10-29

Family

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Family Applications (1)

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KR1020087011830A Expired - Fee Related KR100990771B1 (ko) 2005-11-18 2006-11-15 암 및 염증성 질환 치료를 위한 ｉｋｋ-베타 억제제로서의[4-벤조[ｂ]티오펜-2-일)피리미딘-2-일]-아민 유도체

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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ATE478067T1 (de) 2006-03-31 2010-09-15 Janssen Pharmaceutica Nv Benzoimidazol-2-yl pyridine und pyrazine als modulatoren des histamin-h4-rezeptors
BRPI0713187A2 (pt) * 2006-07-20 2012-10-16 Mehmet Kahraman método de inibir rho-quinase, método de tratamento de doença mediada por rho-quinase, composto e composição farmacêutica
US8101628B2 (en) 2006-12-21 2012-01-24 Eli Lilly And Company Imidazolidinonyl aminopyrimidine compounds for the treatment of cancer
SI2125794T1 (sl) * 2006-12-21 2011-02-28 Lilly Co Eli Spojine imidazolidinonil aminopirimidina za zdravljenje raka
WO2008144222A2 (en) 2007-05-16 2008-11-27 Eli Lilly And Company Triazolyl aminopyrimidine compounds
EA016781B1 (ru) 2007-05-16 2012-07-30 Эли Лилли Энд Компани Триазолиламинопиримидиновые соединения
EP2924023A1 (en) 2008-06-30 2015-09-30 Janssen Pharmaceutica NV piperidine und piperazine derivativs
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
JP5634596B2 (ja) 2010-04-27 2014-12-03 ハチソン メディファーマ リミテッド ピリミジニルインドール化合物
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
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
US9796699B2 (en) 2015-11-03 2017-10-24 Janssen Pharmaceutica Nv Substituted 2-[3-(1-methyl-piperidin-4-yl)-propylamino]-pyrimidine-5-carboxylic acids and amides and methods of making the same
BR112019001407A2 (pt) 2016-07-29 2019-07-09 Sunovion Pharmaceuticals Inc. compostos e composições e usos dos mesmos
SG10202100724UA (en) 2016-07-29 2021-03-30 Sunovion Pharmaceuticals Inc Compounds and compositions and uses 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
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
WO2018218069A1 (en) 2017-05-25 2018-11-29 Araxes Pharma Llc Quinazoline derivatives as modulators of mutant kras, hras or nras
CN110869358A (zh) 2017-05-25 2020-03-06 亚瑞克西斯制药公司 Kras的共价抑制剂
MX2020000523A (es) 2017-08-02 2020-08-20 Sunovion Pharmaceuticals Inc Compuestos de isocromano y usos de los mismos.
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
JP7703449B2 (ja) 2019-03-14 2025-07-07 スミトモ・ファーマ・アメリカ・インコーポレイテッド イソクロマニル化合物の塩およびその結晶体、ならびにそれらの製造方法、治療用途および医薬組成物
US20260116871A1 (en) * 2024-10-24 2026-04-30 Fujian Haixi Pharmaceuticals Co., Ltd. Tyrosine Kinase Inhibitors and Uses Thereof

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WO2004089913A1 (en) 2003-04-11 2004-10-21 Novartis Ag Aminopyrimidine derivatives and their medical use

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WO1989011279A1 (en) * 1988-05-16 1989-11-30 Georgia State University Foundation, Inc. Nucleic acid interacting unfused heteropolycyclic compounds
AU2005316312B2 (en) 2004-12-17 2009-10-22 Amgen, Inc. Aminopyrimidine compounds and methods of use

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

Also Published As

Publication number Publication date
ATE437873T1 (de) 2009-08-15
ZA200803940B (en) 2009-09-30
AR057911A1 (es) 2007-12-26
US7547691B2 (en) 2009-06-16
ES2329085T3 (es) 2009-11-20
DE602006008187D1 (de) 2009-09-10
US20080306082A1 (en) 2008-12-11
ECSP088456A (es) 2008-06-30
PT1989200E (pt) 2009-10-12
WO2007092095A3 (en) 2007-11-08
KR20080059451A (ko) 2008-06-27
CR9947A (es) 2008-11-28
NO20082594L (no) 2008-06-10
SI1989200T1 (sl) 2009-12-31
EA014426B1 (ru) 2010-12-30
DK1989200T3 (da) 2009-11-09
JP2009516697A (ja) 2009-04-23
EP1989200B1 (en) 2009-07-29
IL190489A0 (en) 2008-11-03
WO2007092095A2 (en) 2007-08-16
PL1989200T3 (pl) 2009-12-31
AU2006337626A1 (en) 2007-08-16
CA2629336A1 (en) 2007-08-16
PE20070833A1 (es) 2007-08-27
AU2006337626B2 (en) 2012-03-22
MA30053B1 (fr) 2008-12-01
CN101309918A (zh) 2008-11-19
EA200801362A1 (ru) 2009-02-27
CN101309918B (zh) 2010-12-29
EP1989200A2 (en) 2008-11-12
AU2006337626A8 (en) 2008-06-19
TW200800201A (en) 2008-01-01
BRPI0618245A2 (pt) 2011-08-23
TNSN08227A1 (en) 2009-10-30

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