WO2009124653A3 - Thienopyrimidine - Google Patents

Thienopyrimidine Download PDF

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Publication number
WO2009124653A3
WO2009124653A3 PCT/EP2009/002112 EP2009002112W WO2009124653A3 WO 2009124653 A3 WO2009124653 A3 WO 2009124653A3 EP 2009002112 W EP2009002112 W EP 2009002112W WO 2009124653 A3 WO2009124653 A3 WO 2009124653A3
Authority
WO
WIPO (PCT)
Prior art keywords
thienopyrimidines
tgf
tumors
things
novel
Prior art date
Application number
PCT/EP2009/002112
Other languages
English (en)
French (fr)
Other versions
WO2009124653A2 (de
Inventor
Guenter Hoelzemann
Hartmut Greiner
Christiane Amendt
Frank Zenke
Original Assignee
Merck Patent Gmbh
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
Priority to CA2720878A priority Critical patent/CA2720878A1/en
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Priority to EA201001576A priority patent/EA201001576A1/ru
Priority to JP2011503357A priority patent/JP2011518132A/ja
Priority to BRPI0911364A priority patent/BRPI0911364A2/pt
Priority to EP09731280A priority patent/EP2260044A2/de
Priority to US12/937,031 priority patent/US20110028472A1/en
Priority to MX2010011015A priority patent/MX2010011015A/es
Priority to AU2009235729A priority patent/AU2009235729A1/en
Priority to CN2009801122450A priority patent/CN102015724A/zh
Publication of WO2009124653A2 publication Critical patent/WO2009124653A2/de
Publication of WO2009124653A3 publication Critical patent/WO2009124653A3/de
Priority to IL208066A priority patent/IL208066A0/en
Priority to ZA2010/07979A priority patent/ZA201007979B/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Abstract

Neue Thienopyrimidine der Formel (I) worin R1, R2 und X die in Anspruch 1 angegebenen Bedeutungen haben, sind Inhibitoren der TGF-beta-Rezeptor-Kinase, und können u.a. zur Behandlung von Tumoren eingesetzt werden.
PCT/EP2009/002112 2008-04-09 2009-03-23 Thienopyrimidine WO2009124653A2 (de)

Priority Applications (11)

Application Number Priority Date Filing Date Title
US12/937,031 US20110028472A1 (en) 2008-04-09 2009-03-23 Thienopyrimidines
EA201001576A EA201001576A1 (ru) 2008-04-09 2009-03-23 Тиенопиримидины
JP2011503357A JP2011518132A (ja) 2008-04-09 2009-03-23 チエノピリミジン
BRPI0911364A BRPI0911364A2 (pt) 2008-04-09 2009-03-23 tienopirimidinas
EP09731280A EP2260044A2 (de) 2008-04-09 2009-03-23 Thienopyrimidine
CA2720878A CA2720878A1 (en) 2008-04-09 2009-03-23 Thienopyrimidines
MX2010011015A MX2010011015A (es) 2008-04-09 2009-03-23 Tienopirimidinas.
AU2009235729A AU2009235729A1 (en) 2008-04-09 2009-03-23 Thienopyrimidines
CN2009801122450A CN102015724A (zh) 2008-04-09 2009-03-23 噻吩并嘧啶类
IL208066A IL208066A0 (en) 2008-04-09 2010-09-07 Thienopyrimidines
ZA2010/07979A ZA201007979B (en) 2008-04-09 2010-11-08 Thienopyrimidines

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE102008017853.5 2008-04-09
DE102008017853A DE102008017853A1 (de) 2008-04-09 2008-04-09 Thienopyrimidine

Publications (2)

Publication Number Publication Date
WO2009124653A2 WO2009124653A2 (de) 2009-10-15
WO2009124653A3 true WO2009124653A3 (de) 2009-12-03

Family

ID=40765631

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2009/002112 WO2009124653A2 (de) 2008-04-09 2009-03-23 Thienopyrimidine

Country Status (15)

Country Link
US (1) US20110028472A1 (de)
EP (1) EP2260044A2 (de)
JP (1) JP2011518132A (de)
KR (1) KR20110010721A (de)
CN (1) CN102015724A (de)
AR (1) AR071586A1 (de)
AU (1) AU2009235729A1 (de)
BR (1) BRPI0911364A2 (de)
CA (1) CA2720878A1 (de)
DE (1) DE102008017853A1 (de)
EA (1) EA201001576A1 (de)
IL (1) IL208066A0 (de)
MX (1) MX2010011015A (de)
WO (1) WO2009124653A2 (de)
ZA (1) ZA201007979B (de)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2012530731A (ja) * 2009-06-22 2012-12-06 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング ＴＧＦ−β受容体キナーゼモジュレーターとしてのアルコキシ−チエノピリミジン
MX2012004990A (es) 2009-10-30 2012-06-12 Janssen Pharmaceutica Nv Deribados de imidazo [1,2-b] pirimideazina y su uso como inhibidores de la enzima fosfodiesterasa 10.
JP5675850B2 (ja) 2010-02-05 2015-02-25 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ ヘタリール−［１，８］ナフチリジン誘導体
CN103097381B (zh) 2010-02-22 2015-10-07 默克专利有限公司 作为激酶抑制剂的1,8-萘啶物质
AR080754A1 (es) 2010-03-09 2012-05-09 Janssen Pharmaceutica Nv Derivados de imidazo (1,2-a) pirazina y su uso como inhibidores de pde10
BR112013033375B1 (pt) 2011-06-27 2022-05-10 Janssen Pharmaceutica N.V Derivados de 1-aril-4-metil-[1,2,4]triazolo[4,3-a]quinoxa-lina, seu uso, composição farmacêutica que os compreende, processo de preparação dos mesmos, solução estéril e composto intermediário
FR2988722B1 (fr) 2012-04-03 2014-05-09 Sanofi Sa Nouveaux derives de thienopyrimidines, leurs procedes de preparation et leurs utilisations therapeutiques
CN104411312B (zh) 2012-06-26 2018-03-06 詹森药业有限公司 包括pde2抑制剂例如1‑芳基‑4‑甲基‑[1,2,4]***[4,3‑a]‑喹喔啉化合物和pde10抑制剂的用于在治疗神经病学障碍或代谢障碍中使用的组合
MX362197B (es) 2012-07-09 2019-01-08 Janssen Pharmaceutica Nv Derivados de imidazo[1,2-b]piridazina e imidazo[1,2-a]pirazina como inhibidores de la fosfodiesterasa 10; y el uso de los mismos en el tratamiento de trastornos neurológicos, psiquiátricos y metabólicos.

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006090094A1 (en) * 2005-02-28 2006-08-31 Vernalis R & D Ltd Pyrimidothiophene compounds for use as hsp90 inhibitors
DE102005013621A1 (de) * 2005-03-24 2006-09-28 Curacyte Discovery Gmbh Substituierte 2-Aryl(Hetaryl)-5-aminothieno[2,3-d]pyrimidin-6-carbonsäureamide, Verfahren zu ihrer Herstellung und Verwendung als Pharmazeutika
EP1724268A1 (de) * 2004-02-20 2006-11-22 Kirin Beer Kabushiki Kaisha Verbindungen mit tgf-beta-hemmender wirkung und pharmazeutische zusammensetzung, die diese enthält
WO2007084560A2 (en) * 2006-01-17 2007-07-26 Signal Pharmaceuticals, Llc INHIBITORS OF TNFα, PDE4 AND B-RAF, COMPOSITIONS THEREOF AND METHODS OF USE THEREWITH
WO2008020622A1 (fr) * 2006-08-17 2008-02-21 Kyorin Pharmaceutical Co., Ltd. NOUVEAU COMPOSÉ DE THIÉNO[2,3-d]PYRIMIDINE

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5747469A (en) 1991-03-06 1998-05-05 Board Of Regents, The University Of Texas System Methods and compositions comprising DNA damaging agents and p53
GB9904387D0 (en) 1999-02-25 1999-04-21 Pharmacia & Upjohn Spa Antitumour synergistic composition
WO2000061186A1 (en) 1999-04-08 2000-10-19 Arch Development Corporation Use of anti-vegf antibody to enhance radiation in cancer therapy

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1724268A1 (de) * 2004-02-20 2006-11-22 Kirin Beer Kabushiki Kaisha Verbindungen mit tgf-beta-hemmender wirkung und pharmazeutische zusammensetzung, die diese enthält
WO2006090094A1 (en) * 2005-02-28 2006-08-31 Vernalis R & D Ltd Pyrimidothiophene compounds for use as hsp90 inhibitors
DE102005013621A1 (de) * 2005-03-24 2006-09-28 Curacyte Discovery Gmbh Substituierte 2-Aryl(Hetaryl)-5-aminothieno[2,3-d]pyrimidin-6-carbonsäureamide, Verfahren zu ihrer Herstellung und Verwendung als Pharmazeutika
WO2007084560A2 (en) * 2006-01-17 2007-07-26 Signal Pharmaceuticals, Llc INHIBITORS OF TNFα, PDE4 AND B-RAF, COMPOSITIONS THEREOF AND METHODS OF USE THEREWITH
WO2008020622A1 (fr) * 2006-08-17 2008-02-21 Kyorin Pharmaceutical Co., Ltd. NOUVEAU COMPOSÉ DE THIÉNO[2,3-d]PYRIMIDINE

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
DATABASE CA [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; WADA, MEGUMI ET AL: "Preparation of thieno[2,3-d]pyrimidine compounds as IKK-.beta. and or TNF-.alpha. inhibitors", XP002533936, retrieved from STN Database accession no. 2008:221434 *
SOVAK M A ET AL: "The inhibitory effects of transforming growth factor beta1 on breast cancer cell proliferation are mediated through regulation of aberrant nuclear factor-kappaB/Rel expression.", CELL GROWTH & DIFFERENTIATION : THE MOLECULAR BIOLOGY JOURNAL OF THE AMERICAN ASSOCIATION FOR CANCER RESEARCH AUG 1999, vol. 10, no. 8, August 1999 (1999-08-01), pages 537 - 544, XP002533935, ISSN: 1044-9523 *

Also Published As

Publication number Publication date
BRPI0911364A2 (pt) 2015-12-29
IL208066A0 (en) 2010-12-30
AR071586A1 (es) 2010-06-30
JP2011518132A (ja) 2011-06-23
KR20110010721A (ko) 2011-02-07
CA2720878A1 (en) 2009-10-15
WO2009124653A2 (de) 2009-10-15
CN102015724A (zh) 2011-04-13
MX2010011015A (es) 2010-11-22
ZA201007979B (en) 2011-07-27
EP2260044A2 (de) 2010-12-15
AU2009235729A1 (en) 2009-10-15
US20110028472A1 (en) 2011-02-03
EA201001576A1 (ru) 2011-04-29
DE102008017853A1 (de) 2009-10-15

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