AR080207A1 - Aminotiazolonas como modulares de los receptores de estrogenos alfa - Google Patents

Aminotiazolonas como modulares de los receptores de estrogenos alfa

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Publication number
AR080207A1
AR080207A1 ARP110100488A ARP110100488A AR080207A1 AR 080207 A1 AR080207 A1 AR 080207A1 AR P110100488 A ARP110100488 A AR P110100488A AR P110100488 A ARP110100488 A AR P110100488A AR 080207 A1 AR080207 A1 AR 080207A1
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AR
Argentina
Prior art keywords
alkyl
halo
substituted
groups
arthritis
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Application number
ARP110100488A
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English (en)
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Janssen Pharmaceutica Nv
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Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of AR080207A1 publication Critical patent/AR080207A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/06Heterocyclic 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
    • 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
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic rings
    • 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
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • 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
    • 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
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • 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
    • 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
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P35/04Antineoplastic agents specific for metastasis
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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

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

Abstract

Composiciones, intermedios y derivados de éstos y para tratar una condicion que incluye, pero sin limitarse a, espondilitis anquilosante, arterioescrelosis, artritis (tales como, artritis reumatoide, artritis infecciosa, artritis infantil, artritis psoriática, artritis reactiva), enfermedades relacionadas con los huesos (que incluyen aquellas relacionadas con la formacion de los huesos), cáncer de mamas (que incluyen aquellos insensibles a! tratamiento antiestrogenos), trastornos cardiovasculares, enfermedades relacionadas con cartílagos (tales como lesion/pérdida de cartílago, degeneracion de cartílago y aquellas relacionadas con la formacion del cartílago), condrodisplasia, condrosarcoma, lesion cronica en la espalda, bronquitis cronica, enfermedad inflamatoria cronica de las vías respiratorias, enfermedad pulmonar obstructiva cronica, diabetes, trastornos de homeostasis de energía, gota, seudogota, trastornos lipídicos, síndrome metabolico, mieloma multiple, obesidad, osteoartritis, osteogenesis imperfecta, metástasis osea osteolítica, osteomalacia, osteoporosis, enfermedad de Paget, enfermedad periodontal, polimialgia reumática, síndrome de Reiter, lesion por esfuerzo repetitivo, hiperglicemia, nivel elevado de glucosa en sangre y resistencia a la insulina. Reivindicacion 1: Un compuesto de formula (1) en donde X es CH o N; R1 es alquilo C1-4, halo o alquilo -C(O)-C1-4; en donde el alquilo C1-4 podría estar sustituido con halo; R2 es halo, ciano, H, alquilo C1-4, alquenilo C1-4, alcoxi C1-4, -C(O)N(R5)(R6), o hidroxilo; en donde el alquilo C1-4 podría estar sustituido con halo; R3 es H, halo, -CN o alquilo C1-4; y R4 es heteroarilo o alquilo, cicloalquilo o heterociclilo C1-4; en donde el alquilo C1-4 podría estar sustituido con uno o cinco grupos, los grupos se seleccionan independientemente de halo, -OR5, cicloalquilo, -N(R5)(R6), -C(O)OR5, -C(O)N(R5)(R6), -SO2N(R5)(R6), alquilo O-C1-4-OR5, heterociclilo opcionalmente sustituido con halo, oxo o alquilo C1-4 y heteroarilo opcionalmente sustituido con alquilo C1-4; en donde el cicloalquilo podría estar sustituido con uno a tres grupos, los grupos se seleccionan independientemente de halo, -C(O)OR5 y alquilo C1-4; en donde el heterociclilo podría estar sustituido independientemente con uno a tres grupos, los grupos seleccionados independientemente de halo, alquilo C1-4, y -OR5, en donde el alquilo C1-4 podría estar sustituido con -OR5; en donde R5 y R6 son independientemente H o alquilo C1-4; o un isomero optico, enantiomero, diastereomero, isomero cis-trans, racemato o una sal farmacéuticamente aceptable de éstos.
ARP110100488A 2010-02-17 2011-02-17 Aminotiazolonas como modulares de los receptores de estrogenos alfa AR080207A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US30518110P 2010-02-17 2010-02-17

Publications (1)

Publication Number Publication Date
AR080207A1 true AR080207A1 (es) 2012-03-21

Family

ID=43927926

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Application Number Title Priority Date Filing Date
ARP110100488A AR080207A1 (es) 2010-02-17 2011-02-17 Aminotiazolonas como modulares de los receptores de estrogenos alfa

Country Status (13)

Country Link
US (1) US8445690B2 (es)
EP (1) EP2536717B1 (es)
JP (1) JP2013519730A (es)
KR (1) KR20130001242A (es)
CN (1) CN102834392A (es)
AR (1) AR080207A1 (es)
AU (1) AU2011218190A1 (es)
CA (1) CA2789757A1 (es)
MX (1) MX2012009529A (es)
RU (1) RU2012139463A (es)
TW (1) TW201144303A (es)
UY (1) UY33231A (es)
WO (1) WO2011103134A1 (es)

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Publication number Priority date Publication date Assignee Title
WO2013051632A1 (ja) * 2011-10-04 2013-04-11 武田薬品工業株式会社 含窒素縮合複素環化合物
CN104302322A (zh) 2012-03-26 2015-01-21 日本化学药品株式会社 骨·软组织中产生的巨细胞性肿瘤或软骨肉瘤的预防或治疗剂
CN104119285B (zh) * 2013-04-28 2016-06-29 中国科学院广州生物医药与健康研究院 用作雌激素相关受体调节剂的化合物及其应用
EP3050573B1 (en) 2013-09-25 2019-12-11 Nippon Chemiphar Co., Ltd. Zaltoprofen for preventing metastasis of giant cell tumor that occurs in bone or soft parts, metastasis of chondrosarcoma, or metastasis of osteosarcoma
US10183938B2 (en) 2014-12-16 2019-01-22 Axovant Sciences Gmbh Geminal substituted quinuclidine amide compounds as agonists of α-7 nicotonic acetylcholine receptors
CN104610157A (zh) * 2015-02-13 2015-05-13 佛山市赛维斯医药科技有限公司 一类环丙基酰肼和卤代苯类结构的gpr119激动剂及其用途
JP2018516973A (ja) 2015-06-10 2018-06-28 フォーラム・ファーマシューティカルズ・インコーポレイテッドForum Pharmaceuticals Inc. α7−ニコチン性アセチルコリン受容体のアゴニストとしてのアミノベンゾイソオキサゾール化合物
EP3334740A4 (en) 2015-08-12 2019-02-06 Axovant Sciences GmbH GEMINAL SUBSTITUTED AMINOBENZISOXAZOLE COMPOUNDS AS AGONISTS OF ALPHA 7-NICOTINIC ACETYLCHOLINE RECEPTORS
WO2020087031A1 (en) 2018-10-26 2020-04-30 The Research Foundation For The State University Of New York Combination serotonin specific reuptake inhibitor and serotonin 1a receptor partial agonist for reducing l-dopa-induced dyskinesia

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US5217983A (en) * 1992-03-27 1993-06-08 Du Pont Merck Pharmaceutical Company (N-benzyl) acetaldehyde bicyclic heterocycles useful as topical antiinflammatories
AU2381397A (en) * 1996-04-19 1997-11-12 Novo Nordisk A/S Modulators of molecules with phosphotyrosine recognition units
AU5348098A (en) 1996-12-17 1998-07-15 Quadrant Holdings Cambridge Limited Melanocortins
KR20070041560A (ko) 2004-07-14 2007-04-18 얀센 파마슈티카 엔.브이. 에스트로겐 관련 수용체-알파 매개 질병 치료를 위한아릴리덴
US8148361B2 (en) * 2006-11-10 2012-04-03 Bristol-Myers Squibb Company Kinase inhibitors
EP2132188B1 (en) * 2007-03-07 2011-12-14 Janssen Pharmaceutica N.V. Substituted phenoxy n-alkylated thiazoledinedione as estrogen related receptor-alpha modulators
RU2492164C2 (ru) * 2008-04-16 2013-09-10 Каро Био Аб Новые лиганды эстрогеновых рецепторов

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Publication number Publication date
CA2789757A1 (en) 2011-08-25
TW201144303A (en) 2011-12-16
UY33231A (es) 2011-08-31
KR20130001242A (ko) 2013-01-03
JP2013519730A (ja) 2013-05-30
WO2011103134A1 (en) 2011-08-25
US20110200587A1 (en) 2011-08-18
AU2011218190A1 (en) 2012-09-06
RU2012139463A (ru) 2014-03-27
CN102834392A (zh) 2012-12-19
EP2536717B1 (en) 2014-06-04
MX2012009529A (es) 2013-01-14
EP2536717A1 (en) 2012-12-26
US8445690B2 (en) 2013-05-21

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