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AR079554A1 - Indazoles aminotiazolona sustituidos moduladores de receptores alfa relacionados con estrogenos, composiciones farmaceuticas que los contienen y uso de los mismos para tratar artritis, diabetes, dislipemias y otras enfermedades. - Google Patents

Indazoles aminotiazolona sustituidos moduladores de receptores alfa relacionados con estrogenos, composiciones farmaceuticas que los contienen y uso de los mismos para tratar artritis, diabetes, dislipemias y otras enfermedades.

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Publication number
AR079554A1
AR079554A1 ARP100104776A ARP100104776A AR079554A1 AR 079554 A1 AR079554 A1 AR 079554A1 AR P100104776 A ARP100104776 A AR P100104776A AR P100104776 A ARP100104776 A AR P100104776A AR 079554 A1 AR079554 A1 AR 079554A1
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AR
Argentina
Prior art keywords
alkyl
halo
substituted
heterocyclyl
hydroxyl
Prior art date
Application number
ARP100104776A
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English (en)
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Janssen Pharmaceutica Nv
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Filing date
Publication date
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of AR079554A1 publication Critical patent/AR079554A1/es

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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • 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
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A61P19/04—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
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • 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
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
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    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P35/04—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
    • 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
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D471/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
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    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
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    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08—Bridged systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Neurology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Reproductive Health (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Reivindicacion 1: Un compuesto de la formula (1), en donde X es -CH- o N; R1 es alquilo C1-3, halo, cicloalquilo y -C(O)-alquilo C1-4 en donde el alquilo C1-3 puede ser sustituido por halo; R2 es -H, halo, ciano, alquilo C1-3, alquenilo C2-3, alcoxi C1-4, hidroxilo, cicloalquilo, -C(O)O-alquilo C1-4, -C(O)NH2, -OS(O2)-alquilo C1-4, -O-alquil C1-4-O-alquilo C1-4, heterociclilo, heteroarilo, o -S(O2)-alquilo C1-4, en donde el alquilo C1-3 puede ser sustituido con halo o hidroxilo; R3 es -H, halo, ciano, o alquilo C1-3; y el anillo HET es un heterociclilo de 4 a 9 miembros unido al resto de la molécula a través de un átomo de nitrogeno del anillo y, opcionalmente, contiene 1 - 2 heteroátomos en adicion al átomo de nitrogeno del anillo, en donde los 1 - 2 heteroátomos adicionales opcionales se seleccionan, independientemente, del grupo consistente de N, O y S, en donde el heterociclilo de 4 a 9 miembros puede ser sustituido con alquilo C1-4, alquenilo C2-4, alquinilo C2-4, halo, oxo, ciano, hidroxilo, -OR5, -O-alquil C1-4-C(O)OR5, cicloalquilo, heteroarilo, heterociclilo, -C(O)OR5, -C(O)N(R5)(R6), -C(O)N(R5)(OR6), -C(O)R5, -C(O)-alquil C1-4-N(R5)(R6), -C(O)-alquil C1-4-O-alquilo C1-4, -C(O)N(R5)-S(O)2(R6), -C(O)N(R5)-OR6, -C(O)N(R5)S(O)2N(R5)(R6), -C(O)N(R5)-alquil C1-4-C(O)OR6, -N(R5)(R6), -N(R5)-alquil C1-4-OR6, -N(R5)C(O)R6, -N(R5)C(O)OR6, - N(R5)S(O)2R6, -N(R5)C(O)-NH(R6), -N(R5)-alquil C1-4-C(O)-NH(R6), -SR5, -S(O)2R5, o -S(O)2-N(R5)(R6), en donde el alquilo C1-4 puede ser sustituido con -OH, -O-alquilo C1-4, -C(O)OR5, -C(O)N(R5)(R6), -N(R5)(R6), -N(R5)C(O)OR6, heterociclilo, heteroarilo, cicloalquilo, o halo, en donde el heteroarilo puede ser sustituido con alquilo C1-4, halo, ciano, -CF3, alcoxi o hidroxilo, en donde el heterociclilo puede ser sustituido con alquilo C1-4, oxo, halo, amino, alcoxi, o hidroxilo, en donde el alquenilo C2-4 y el alquinilo C2-4 pueden ser independientemente sustituidos con oxo, heterociclilo, hidroxilo, o halo, en donde R5 y R6 son cada uno independientemente H, alquilo C1-4, cicloalquilo, o heterociclilo, en donde el alquilo C1-4 puede ser sustituido con halo o hidroxilo; o alternativamente R5 y R6 están unidos para formar un anillo de 5 a 7 miembros; o un isomero optico, enantiomero, diastereomero, isomero cis-trans, racemato, o sal farmacéuticamente aceptable de éste.
ARP100104776A 2009-12-18 2010-12-20 Indazoles aminotiazolona sustituidos moduladores de receptores alfa relacionados con estrogenos, composiciones farmaceuticas que los contienen y uso de los mismos para tratar artritis, diabetes, dislipemias y otras enfermedades. AR079554A1 (es)

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US (2) US8263781B2 (es)
EP (1) EP2513096A1 (es)
JP (1) JP2013514385A (es)
CN (1) CN102770429A (es)
AR (1) AR079554A1 (es)
AU (1) AU2010330894A1 (es)
CA (1) CA2784753A1 (es)
TW (1) TW201130829A (es)
UY (1) UY33118A (es)
WO (1) WO2011075565A1 (es)

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WO2014026327A1 (en) 2012-08-15 2014-02-20 Merck Sharp & Dohme Corp. 4-heteroaryl substituted benzoic acid compounds as rorgammat inhibitors and uses thereof
WO2014026329A1 (en) * 2012-08-15 2014-02-20 Merck Sharp & Dohme Corp. N-alkylated indole and indazole compounds as rorgammat inhibitors and uses thereof
WO2014026330A1 (en) 2012-08-15 2014-02-20 Merck Sharp & Dohme Corp. 3-AMINOCYCLOALKYL COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF
JP6023630B2 (ja) * 2013-04-03 2016-11-09 株式会社ヤクルト本社 チアゾロン誘導体
WO2016130818A1 (en) 2015-02-11 2016-08-18 Merck Sharp & Dohme Corp. SUBSTITUTED PYRAZOLE COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF
CA3002846A1 (en) 2015-10-27 2017-05-04 Merck Sharp & Dohme Corp. Substituted bicyclic pyrazole compounds as rorgammat inhibitors and uses thereof
KR20180070697A (ko) 2015-10-27 2018-06-26 머크 샤프 앤드 돔 코포레이션 Ror감마t 저해제로서의 치환된 인다졸 화합물 및 이의 용도
AU2016344118A1 (en) 2015-10-27 2018-05-10 Merck Sharp & Dohme Corp. Heteroaryl substituted benzoic acids as rorgammat inhibitors and uses thereof
EP3870292A4 (en) 2018-10-26 2022-11-09 The Research Foundation for The State University of New York COMBINATION OF SEROTONIN-SPECIFIC RESUPPUT INHIBITOR AND SEROTONIN 1A RECEPTOR PARTIAL AGONIST TO REDUCE L-DOPA-INDUCED DYSKINESIA
CN110172068A (zh) * 2019-06-05 2019-08-27 河南龙湖生物技术有限公司 具有抗肿瘤活性的苯并噻唑类化合物及其制备方法和应用
CN112538038B (zh) * 2019-09-20 2022-05-20 暨南大学 2-吲哚酮类ERRα反向激动剂及其药物组合物和应用

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JP2013514385A (ja) 2013-04-25
WO2011075565A1 (en) 2011-06-23
US20110150864A1 (en) 2011-06-23
US20120302544A1 (en) 2012-11-29
CA2784753A1 (en) 2011-06-23
EP2513096A1 (en) 2012-10-24
UY33118A (es) 2011-06-30
CN102770429A (zh) 2012-11-07
AU2010330894A1 (en) 2012-07-05
TW201130829A (en) 2011-09-16
US8399681B2 (en) 2013-03-19
US8263781B2 (en) 2012-09-11

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