MXPA04004593A - Triazoles fenilo-sustituidos y su uso como inhibidores selectivos de cinasa de tipo activina-5. - Google Patents

Triazoles fenilo-sustituidos y su uso como inhibidores selectivos de cinasa de tipo activina-5.

Info

Publication number
MXPA04004593A
MXPA04004593A MXPA04004593A MXPA04004593A MXPA04004593A MX PA04004593 A MXPA04004593 A MX PA04004593A MX PA04004593 A MXPA04004593 A MX PA04004593A MX PA04004593 A MXPA04004593 A MX PA04004593A MX PA04004593 A MXPA04004593 A MX PA04004593A
Authority
MX
Mexico
Prior art keywords
6alkyl
phenyl
hydrogen
optionally substituted
independently selected
Prior art date
Application number
MXPA04004593A
Other languages
English (en)
Inventor
John David Harling
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 MXPA04004593A publication Critical patent/MXPA04004593A/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/14—Thiadiazoles; Hydrogenated thiadiazoles condensed with carbocyclic rings or ring systems
    • 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
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • C07D249/06—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/34—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings
    • C07D265/36—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings condensed with one six-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

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

Abstract

Se describen triazoles fenilo-sustituidos de la formula (I) (ver formula I)en donde R1 es naftilo o feniolo opcionalmente sustituido con uno o mas sustituyentes seleccionados de halogeno, -O-alquilo de C1-6, -S-alquilo de C1-6, alquilo de C1-6, halogenoalquilo de C1-6, -O-(CH2)n-Ph, -S--(CH2)n-Ph, ciano, fenilo y CO2R, en donde R es hidrogeno o alquilo de C1-6, y n es 0, 1, 2 o 3; o R1 es fenilo o piridilo fusionado con un anillo ciclico aromatico o no aromatico de 5-7 miembros den donde dicho anillo ciclico contienen opcionalmente hasta tres heteroatomos, independientemente seleccionados de N, O y S, y N puede ser opcionalmente sustituido por alquilo de C1-6, y en donde el anillo ciclico puede ser opcionalmente sustituido por =O; R2 y R3 se seleccionan independientemente de H, alquilo de C1-6, alcoxi de C1-6, fenilo, NH(CH2)n-Ph, NH-alquilo de C1-6, halogeno, alcoxi, CN, NO2, CONHR y SO2NHR; dos de X1, X2 y X3 son N y el otro es NR4 en donde R4 es hidrogeno, alquilo de C1-6,, a??cicloalquilo de C3-7, -(CH2)p-CN, -(CH2)p-Co2H, -(CH2)p-CONHR5R6, -(CH2)p-COR5, -(CH2)q-(OR7)2, -(CH2)p-OR5, (CH2)q-CH=CH-CN, -(CH2)q-CH=CH-CO2H, -(CH2)p-CHCH-CONHR5R6, -(CH2)p-NHCOR8 O -(CH2)p-NR9R10; R5 Y R6 son independientemente hidrogeno o alquilo de C1-6;R7 es alquilo de C1-6; R8 es alquilo de C1-7, o arilo opcionalmente sustituido, heteroarilo, arilo-alquilo de C1-6,o heteroarilo-alquilo de C1-6; R9 o R10 se seleccionan independientemente de hidrogeno, alquilo de C1-6, arilo y arilo alquilo de C1-6; p es 0-4; y q es 1-4 y sales y solventes de los mismos, asi como metodos para su preparacion, composiciones farmaceuticas que los contienen y su uso en medicina.
MXPA04004593A 2001-11-15 2002-11-14 Triazoles fenilo-sustituidos y su uso como inhibidores selectivos de cinasa de tipo activina-5. MXPA04004593A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB0127430.7A GB0127430D0 (en) 2001-11-15 2001-11-15 Compounds
PCT/EP2002/013482 WO2003042211A1 (en) 2001-11-15 2002-11-14 Phenyl substituted triazoles and their use as selective inhibors of akl5 kinase

Publications (1)

Publication Number Publication Date
MXPA04004593A true MXPA04004593A (es) 2004-08-13

Family

ID=9925832

Family Applications (1)

Application Number Title Priority Date Filing Date
MXPA04004593A MXPA04004593A (es) 2001-11-15 2002-11-14 Triazoles fenilo-sustituidos y su uso como inhibidores selectivos de cinasa de tipo activina-5.

Country Status (17)

Country Link
US (1) US20050014938A1 (es)
EP (1) EP1444232A1 (es)
JP (1) JP2005518352A (es)
KR (1) KR20050044476A (es)
CN (1) CN1608065A (es)
BR (1) BR0214160A (es)
CA (1) CA2467267A1 (es)
GB (1) GB0127430D0 (es)
HU (1) HUP0402227A2 (es)
IL (1) IL161852A0 (es)
IS (1) IS7252A (es)
MX (1) MXPA04004593A (es)
NO (1) NO20042244L (es)
PL (1) PL369605A1 (es)
RU (1) RU2004117862A (es)
WO (1) WO2003042211A1 (es)
ZA (1) ZA200403487B (es)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050165011A1 (en) * 2002-05-15 2005-07-28 Gellibert Francoise J. Benzoxazine and benzoxazinone substituted triazoles
GB0217787D0 (en) * 2002-07-31 2002-09-11 Glaxo Group Ltd C ompounds
GB0217780D0 (en) * 2002-07-31 2002-09-11 Glaxo Group Ltd Compounds
WO2004014900A1 (en) * 2002-08-09 2004-02-19 Eli Lilly And Company Benzimidazoles and benzothiazoles as inhibitors of map kinase
EP2261331A1 (en) 2003-09-11 2010-12-15 Hubit Genomix, Inc. Method and kit for detecting proliferative diseases causing sclerosis, preventive and/or remedy for proliferative diseases causing sclerosis and method and kit for identifying substance efficacious in preventing and/or treating proliferative diseases causing sclerosis
EP1720862A1 (en) * 2004-02-03 2006-11-15 Eli Lilly And Company Kinase inhibitors
JP2008508314A (ja) * 2004-07-28 2008-03-21 アイアールエム・リミテッド・ライアビリティ・カンパニー ステロイドホルモン核内受容体のモジュレーターとしての化合物および組成物
ATE517897T1 (de) * 2005-03-25 2011-08-15 Tibotec Pharm Ltd Heterobicyclische inhibitoren von hvc
AR056347A1 (es) 2005-05-12 2007-10-03 Tibotec Pharm Ltd Uso de compuestos de pteridina para fabricar medicamentos y composiciones farmaceuticas
DE102005061840A1 (de) * 2005-12-23 2007-06-28 Merck Patent Gmbh Triazolderivate
BRPI0713951B8 (pt) 2006-06-30 2021-05-25 Novartis Ag derivados de quinazolina, e composição farmacêutica
JP5616063B2 (ja) * 2006-10-04 2014-10-29 ヤンセン・アールアンドデイ・アイルランド Ｈｃｖ阻害剤として有用なカルボキシアミド４−［（４−ピリジル）アミノ］ピリミジン
EP1921072A1 (en) * 2006-11-10 2008-05-14 Laboratorios del Dr. Esteve S.A. 1,2,3-Triazole derivatives as cannabinoid-receptor modulators
US7678819B2 (en) * 2006-12-07 2010-03-16 The Trustees Of The University Of Pennsylvania Acetylene derivatives and their use for binding and imaging amyloid plaques
KR101076628B1 (ko) 2008-07-09 2011-10-27 포항공과대학교 산학협력단 불균일 구리 나노 촉매 및 그 제조방법
WO2010005127A2 (en) 2008-07-09 2010-01-14 Postech Academy-Industry Foundation Heterogeneous copper nanocatalyst and manufacturing methods thereof
US8586581B2 (en) * 2009-12-17 2013-11-19 Hoffmann-La Roche Inc Ethynyl compounds useful for treatment of CNS disorders
CN102443009B (zh) * 2010-09-30 2014-04-16 山东轩竹医药科技有限公司 并环激酶抑制剂
CN104520422B (zh) 2012-05-30 2019-08-23 康奈尔大学 由人羊水来源的细胞生成功能性的和持久的内皮细胞
CN105473134B (zh) 2013-06-05 2021-04-27 再生疗法有限公司 用于哺乳动物物种中诱导性组织再生的组合物和方法
US11078462B2 (en) 2014-02-18 2021-08-03 ReCyte Therapeutics, Inc. Perivascular stromal cells from primate pluripotent stem cells
US10240127B2 (en) 2014-07-03 2019-03-26 ReCyte Therapeutics, Inc. Exosomes from clonal progenitor cells
WO2022251359A1 (en) * 2021-05-26 2022-12-01 Theravance Biopharma R&D Ip, Llc Bicyclic inhibitors of alk5 and methods of use

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000010563A1 (en) * 1998-08-20 2000-03-02 Smithkline Beecham Corporation Novel substituted triazole compounds
DE60001229T2 (de) * 1999-04-09 2003-10-30 Smithkline Beecham Corp., Philadelphia Triarylimidazole
AR029803A1 (es) * 2000-02-21 2003-07-16 Smithkline Beecham Plc Imidazoles sustituidos con piridilo y composiciones farmaceuticas que las comprenden
GB0007405D0 (en) * 2000-03-27 2000-05-17 Smithkline Beecham Corp Compounds
JP2003530438A (ja) * 2000-04-12 2003-10-14 スミスクライン・ビーチャム・コーポレイション 化合物および方法
GB0027987D0 (en) * 2000-11-16 2001-01-03 Smithkline Beecham Plc Compounds

Also Published As

Publication number Publication date
WO2003042211A1 (en) 2003-05-22
CN1608065A (zh) 2005-04-20
US20050014938A1 (en) 2005-01-20
JP2005518352A (ja) 2005-06-23
RU2004117862A (ru) 2006-01-10
EP1444232A1 (en) 2004-08-11
PL369605A1 (en) 2005-05-02
KR20050044476A (ko) 2005-05-12
GB0127430D0 (en) 2002-01-09
BR0214160A (pt) 2004-09-28
CA2467267A1 (en) 2003-05-22
HUP0402227A2 (hu) 2005-02-28
IL161852A0 (en) 2005-11-20
NO20042244L (no) 2004-07-13
IS7252A (is) 2004-05-06
ZA200403487B (en) 2006-05-31

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