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

    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • 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
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • 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
    • C07D409/14—Heterocyclic 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)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (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)
  • Transplantation (AREA)
  • Hematology (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 (29)

Country Link
US (2) US7595330B2 (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)
HK (1) HK1117504A1 (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)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007139795A1 (en) * 2006-05-23 2007-12-06 Vertex Pharmaceuticals Incorporated Thiophene-carboxamides useful as inhibitors of protein kinases
US20090326029A1 (en) * 2006-06-02 2009-12-31 Kevin Wayne Kuntz Non-cyclic substituted benzimidazole thiophene benzyl ether compounds
US7615643B2 (en) 2006-06-02 2009-11-10 Smithkline Beecham Corporation Benzimidazole thiophene compounds
JP2009539770A (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 Ｐｌｋに対する活性を有するベンゾイミダゾール置換チオフェン誘導体
EP2123627B1 (en) * 2007-01-19 2013-11-20 Ube Industries, Ltd. Process for producing aromatic amine having aralkyloxy or heteroaralkyloxy group
WO2009002916A2 (en) * 2007-06-26 2008-12-31 Smithkline Beecham Corporation Processes for preparing benzimidazole thiophenes
WO2009003911A1 (en) * 2007-06-29 2009-01-08 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
JP2012512223A (ja) * 2008-12-18 2012-05-31 エフ．ホフマン−ラ ロシュ アーゲー チアゾリル−ベンズイミダゾール類
WO2011049625A1 (en) 2009-10-20 2011-04-28 Mansour Samadpour Method for aflatoxin screening of products
EP3444242A3 (en) 2009-11-05 2019-03-20 Rhizen Pharmaceuticals S.A. Novel benzopyran kinase modulators
PL2705029T3 (pl) 2011-05-04 2019-04-30 Rhizen Pharmaceuticals S A Nowe związki jako modulatory kinaz białkowych
RS56494B1 (sr) 2012-07-04 2018-01-31 Rhizen Pharmaceuticals S A Selektivni inhibitori pi3k delta
KR20210122164A (ko) * 2020-03-27 2021-10-08 (주) 업테라 Plk1의 선택적 분해를 유도하는 벤즈이미다졸 티오펜 유도체 화합물
KR102574152B1 (ko) * 2020-03-27 2023-09-05 (주) 업테라 Plk1의 선택적 분해를 유도하는 벤즈이미다졸 티오펜 유도체 화합물

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
AU760020B2 (en) 1998-08-31 2003-05-08 Merck & Co., Inc. Novel angiogenesis inhibitors
CA2493908A1 (en) 2002-08-08 2004-02-19 Smithkline Beecham Corporation Thiophene compounds
AU2003903440A0 (en) * 2003-07-04 2003-07-17 James Hardie International Finance B.V. Rainscreen apparatus and method
EP1685128A1 (en) 2003-10-16 2006-08-02 Smithkline Beecham Corporation Process for preparing benzimidazole thiophenes
JP4721428B2 (ja) 2003-10-20 2011-07-13 日本精工株式会社 ステアリング装置
GB0402809D0 (en) 2004-02-09 2004-03-10 Glaxo Group Ltd Chemical compounds
ATE459620T1 (de) * 2005-09-06 2010-03-15 Glaxosmithkline Llc Benzimidazolthiophenverbindungen als plk- modulatoren
ES2338590T3 (es) * 2005-09-06 2010-05-10 Glaxosmithkline Llc Procedimiento regioselectivo de preparacion de benzoimidazoltiofenos.
WO2007087283A2 (en) 2006-01-23 2007-08-02 Vertex Pharmaceuticals Incorporated Thiophene-carboxamides useful as inhibitors of protein kinases
JP2009539770A (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 Ｐｌｋに対する活性を有するベンゾイミダゾール置換チオフェン誘導体
US20090326029A1 (en) * 2006-06-02 2009-12-31 Kevin Wayne Kuntz Non-cyclic substituted benzimidazole thiophene benzyl ether compounds

Also Published As

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

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