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PE20070518A1 - Compuestos de tiofeno bencimidazol como agentes inhibidores de plk - Google Patents

Compuestos de tiofeno bencimidazol como agentes inhibidores de plk

Info

Publication number
PE20070518A1
PE20070518A1 PE2006001041A PE2006001041A PE20070518A1 PE 20070518 A1 PE20070518 A1 PE 20070518A1 PE 2006001041 A PE2006001041 A PE 2006001041A PE 2006001041 A PE2006001041 A PE 2006001041A PE 20070518 A1 PE20070518 A1 PE 20070518A1
Authority
PE
Peru
Prior art keywords
formula
benzimidazol
ethyl
thiophenocarboxamide
methyl
Prior art date
Application number
PE2006001041A
Other languages
English (en)
Inventor
Mui Cheung
Kyle Allen Emmitte
James M Salovich
Original Assignee
Smithkline Beecham Corp
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 Smithkline Beecham Corp filed Critical Smithkline Beecham Corp
Publication of PE20070518A1 publication Critical patent/PE20070518A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/04Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/14Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Dermatology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Transplantation (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

REFERIDA A UN COMPUESTO TIOFENO BENCIMIDAZOL SELECCIONADO DE: 5-{6-[(METILSULFONIL)METIL]-1H-BENZIMIDAZOL-1-IL}-3-({(1R)-1-[2-(TRIFLUOROMETIL)FENIL]ETIL}OXI)-2-TIOFENOCARBOXAMIDA (FORMULA A), 3-{[(1R)-1-(2-CLOROFENIL)ETIL]OXI}-5-{6-[(METILSULFONIL)METIL]-1H-BENZIMIDAZOL-1-IL}-2-TIOFENOCARBOXAMIDA (FORMULA B), 5-{6-[(4-METILPIPERAZIN-1-IL)METIL]-1H-BENZIMIDAZOL-1-IL}-3-{(1R)-1-[2-(TRIFLUOROMETIL)FENIL]ETOXI}TIOFENO-2-CARBOXAMIDA (FORMULA C), 3-{[(1R)-1-(2-CLOROFENIL)ETIL]OXI}-5-{6-[(4-METILPIPERAZIN-1-IL)METIL]-1H-BENZIMIDAZOL-1-IL}-TIOFENO-2-CARBOXAMIDA (FORMULA D), 5-[6-(4-PIPERIDINILOXI)-1H-BENZIMIDAZOL-1-IL]-3-({(1R)-1-[2-(TRIFLUOROMETIL)FENIL]ETIL}OXI)-2-TIOFENOCARBOXAMIDA (FORMULA E), 3-{[(1R)-1-(2-CLOROFENIL)ETIL]OXI}-5-[6-(4-PIPERIDINILOXI)-1H-BENZIMIDAZOL-1-IL]-2-TIOFENOCARBOXAMIDA (FORMULA F), 5-{6-[(1-METIL-4-PIPERIDINIL)OXI]-1H-BENZIMIDAZOL-1-IL}-3-({(1R)-1-[2-(TRIFLUOROMETIL)FENIL]ETIL}OXI)-2-TIOFENOCARBOXAMIDA (FORMULA G) Y 3-{[(1R)-1-(2-CLOROFENIL)ETIL]OXI}-5-{6-[1-METIL-4-PIPERIDINIL)OXI]-1H-BENZIMIDAZOL-1-IL}-2-TIOFENOCARBOXAMIDA (FORMULA H), DONDE EL ASTERISCO INDICA UN CARBONO QUIRAL. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA Y UN PROCEDIMIENTO DE PREPARACION. DICHOS COMPUESTOS SON INHIBIDORES DE LAS QUINASAS TIPO POLO (PLK), LAS CUALES SON QUINASAS DE SERINA/TREONINA, Y SON UTILES PARA EL TRATAMIENTO DE ENFERMEDADES PROLIFERATIVAS
PE2006001041A 2005-09-06 2006-08-28 Compuestos de tiofeno bencimidazol como agentes inhibidores de plk PE20070518A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US71433705P 2005-09-06 2005-09-06
US78624406P 2006-03-27 2006-03-27

Publications (1)

Publication Number Publication Date
PE20070518A1 true PE20070518A1 (es) 2007-06-12

Family

ID=37631488

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2006001041A PE20070518A1 (es) 2005-09-06 2006-08-28 Compuestos de tiofeno bencimidazol como agentes inhibidores de plk

Country Status (28)

Country Link
US (2) US7786127B2 (es)
EP (1) EP1937671B1 (es)
JP (1) JP5002597B2 (es)
KR (1) KR20080047585A (es)
AR (1) AR055616A1 (es)
AT (1) ATE452132T1 (es)
AU (1) AU2006287766B2 (es)
BR (1) BRPI0615668A2 (es)
CA (1) CA2621879A1 (es)
CR (1) CR9786A (es)
CY (1) CY1109916T1 (es)
DE (1) DE602006011192D1 (es)
DK (1) DK1937671T3 (es)
EA (1) EA014111B1 (es)
ES (1) ES2337929T3 (es)
HR (1) HRP20100122T1 (es)
IL (1) IL189897A0 (es)
JO (1) JO2578B1 (es)
MA (1) MA29816B1 (es)
MX (1) MX2008003173A (es)
NO (1) NO20081160L (es)
NZ (1) NZ566345A (es)
PE (1) PE20070518A1 (es)
PL (1) PL1937671T3 (es)
PT (1) PT1937671E (es)
SI (1) SI1937671T1 (es)
TW (1) TW200800967A (es)
WO (1) WO2007030361A2 (es)

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CN101495474A (zh) * 2006-05-23 2009-07-29 沃泰克斯药物股份有限公司 可用作蛋白激酶抑制剂的噻吩-甲酰胺类
JP2009539771A (ja) * 2006-06-02 2009-11-19 スミスクライン ビーチャム コーポレーション 置換ベンゾイミダゾールチオフェンベンジルエーテル化合物
EP2032563B1 (en) * 2006-06-02 2010-06-02 GlaxoSmithKline LLC Benzimidazol substituted thiophene derivatives with activity on plk
US7615643B2 (en) 2006-06-02 2009-11-10 Smithkline Beecham Corporation Benzimidazole thiophene compounds
EP2123627B1 (en) * 2007-01-19 2013-11-20 Ube Industries, Ltd. Process for producing aromatic amine having aralkyloxy or heteroaralkyloxy group
US8236954B2 (en) 2007-06-26 2012-08-07 Glaxosmithkline Llc Processes for preparing benzimidazole thiophenes
US8273890B2 (en) * 2007-06-29 2012-09-25 4Sc Ag Thiophene-imidazopyridines
EP2100894A1 (en) 2008-03-12 2009-09-16 4Sc Ag Pyridopyrimidines used as Plk1 (polo-like kinase) inhibitors
WO2009151914A1 (en) * 2008-05-27 2009-12-17 Smithkline Beecham Corporation Methods for treating neoplasms with a combination of a plk inhibitor and retinoid
WO2009154645A1 (en) * 2008-06-20 2009-12-23 Smithkline Beecham Corporation Methods for the treatment of central nervous system tumors
CA2745596A1 (en) 2008-12-18 2010-10-28 F. Hoffmann-La Roche Ag Thiazolyl-benzimidazoles
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BR112012010640A2 (pt) 2009-11-05 2016-11-22 Rhizen Pharmaceuticals S A novos moduladores de quinase
SG194718A1 (en) 2011-05-04 2013-12-30 Rhizen Pharmaceuticals Sa Novel compounds as modulators of protein kinases
KR101988079B1 (ko) 2012-07-04 2019-06-11 리젠 파마슈티컬스 소시에떼 아노님 선택적 pi3k 델타 억제제
KR102574152B1 (ko) * 2020-03-27 2023-09-05 (주) 업테라 Plk1의 선택적 분해를 유도하는 벤즈이미다졸 티오펜 유도체 화합물
US20230158158A1 (en) * 2020-03-27 2023-05-25 Uppthera Pyrazolo quinazoline derivative compounds inducing selective degradation of plk1
TW202508595A (zh) 2023-05-04 2025-03-01 美商銳新醫藥公司 用於ras相關疾病或病症之組合療法
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025080946A2 (en) 2023-10-12 2025-04-17 Revolution Medicines, Inc. Ras inhibitors

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US5990146A (en) 1997-08-20 1999-11-23 Warner-Lambert Company Benzimidazoles for inhibiting protein tyrosine kinase mediated cellular proliferation
US6162804A (en) * 1997-09-26 2000-12-19 Merck & Co., Inc. Tyrosine kinase inhibitors
CA2341409A1 (en) 1998-08-31 2000-03-09 Merck And Co., Inc. Novel angiogenesis inhibitors
MXPA05001544A (es) * 2002-08-08 2005-04-19 Smithkline Beecham Corp Compuestos de tiofeno.
AU2003903440A0 (en) * 2003-07-04 2003-07-17 James Hardie International Finance B.V. Rainscreen apparatus and method
WO2005037827A1 (en) * 2003-10-16 2005-04-28 Smithkline Beecham Corporation Process for preparing benzimidazole thiophenes
WO2005037627A1 (ja) 2003-10-20 2005-04-28 Nsk Ltd. ステアリング装置
GB0402809D0 (en) 2004-02-09 2004-03-10 Glaxo Group Ltd Chemical compounds
JP2009507022A (ja) * 2005-09-06 2009-02-19 スミスクライン ビーチャム コーポレーション ベンズイミダゾールチオフェン類の位置選択的調製方法
ATE459620T1 (de) * 2005-09-06 2010-03-15 Glaxosmithkline Llc Benzimidazolthiophenverbindungen als plk- modulatoren
WO2007087283A2 (en) 2006-01-23 2007-08-02 Vertex Pharmaceuticals Incorporated Thiophene-carboxamides useful as inhibitors of protein kinases
EP2032563B1 (en) * 2006-06-02 2010-06-02 GlaxoSmithKline LLC Benzimidazol substituted thiophene derivatives with activity on plk
JP2009539771A (ja) * 2006-06-02 2009-11-19 スミスクライン ビーチャム コーポレーション 置換ベンゾイミダゾールチオフェンベンジルエーテル化合物

Also Published As

Publication number Publication date
MA29816B1 (fr) 2008-09-01
WO2007030361A3 (en) 2007-05-31
EA014111B1 (ru) 2010-10-29
DE602006011192D1 (de) 2010-01-28
AR055616A1 (es) 2007-08-29
CR9786A (es) 2008-05-22
US20080214567A1 (en) 2008-09-04
CA2621879A1 (en) 2007-03-15
EP1937671B1 (en) 2009-12-16
HK1117504A1 (en) 2009-01-16
AU2006287766B2 (en) 2010-06-24
US7786127B2 (en) 2010-08-31
CY1109916T1 (el) 2014-09-10
SI1937671T1 (sl) 2010-04-30
ES2337929T3 (es) 2010-04-30
NO20081160L (no) 2008-05-29
EA200800546A1 (ru) 2008-08-29
DK1937671T3 (da) 2010-04-26
KR20080047585A (ko) 2008-05-29
BRPI0615668A2 (pt) 2011-05-24
NZ566345A (en) 2010-04-30
JP5002597B2 (ja) 2012-08-15
ATE452132T1 (de) 2010-01-15
US7595330B2 (en) 2009-09-29
PL1937671T3 (pl) 2010-05-31
HRP20100122T1 (hr) 2010-05-31
TW200800967A (en) 2008-01-01
JP2009508816A (ja) 2009-03-05
EP1937671A2 (en) 2008-07-02
PT1937671E (pt) 2010-03-12
AU2006287766A1 (en) 2007-03-15
US20070270437A1 (en) 2007-11-22
JO2578B1 (en) 2011-02-27
WO2007030361A2 (en) 2007-03-15
IL189897A0 (en) 2008-08-07
MX2008003173A (es) 2008-03-18

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