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

Aminotiazolonas como modulares de los receptores de estrogenos alfa

Info

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
Authority
AR
Argentina
Prior art keywords
alkyl
halo
substituted
groups
arthritis
Prior art date
Application number
ARP110100488A
Other languages
English (en)
Original Assignee
Janssen Pharmaceutica Nv
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 Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of AR080207A1 publication Critical patent/AR080207A1/es

Links

Classifications

    • 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
    • AHUMAN NECESSITIES
    • 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

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

Family Applications (1)

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)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
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
CN106267210A (zh) 2012-03-26 2017-01-04 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
JP6527822B2 (ja) 2013-09-25 2019-06-05 日本ケミファ株式会社 骨・軟部に発生する巨細胞性腫瘍、軟骨肉腫または骨肉腫の予防、治療または転移の予防のための薬剤、動脈塞栓術用局所注入剤、および、人工骨
EP3233087B1 (en) 2014-12-16 2019-10-02 Axovant Sciences GmbH Geminal substituted quinuclidine amide compounds as agonists of alpha-7 nicotinic 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
WO2017027600A1 (en) 2015-08-12 2017-02-16 Forum Pharmaceuticals, Inc. GEMINAL SUBSTITUTED AMINOBENZISOXAZOLE COMPOUNDS AS AGONISTS OF α7-NICOTINIC ACETYLCHOLINE RECEPTORS
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

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
EP0946595A2 (en) 1996-12-17 1999-10-06 Quadrant Holdings Cambridge Limited Melanocortins
BRPI0513367A (pt) 2004-07-14 2008-05-06 Janssen Pharmaceutica Nv arilidenos para o tratamento de doenças mediadas pelo receptor alfa relacionado a estrogênio
EP2081928B1 (en) * 2006-11-10 2014-02-26 Bristol-Myers Squibb Company Pyrrolo-pyridine kinase inhibitors
WO2008109731A2 (en) 2007-03-07 2008-09-12 Jassen Pharmaceutica N.V. Substituted phenoxy n-alkylated thiazoledinedione as estrogen related receptor-alpha modulators
PT2276732E (pt) * 2008-04-16 2015-09-28 Karobio Ab Novos ligandos do recetor de estrogénio

Also Published As

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

Similar Documents

Publication Publication Date Title
AR080207A1 (es) Aminotiazolonas como modulares de los receptores de estrogenos alfa
NI200900163A (es) Tiazolidinedionas fenoxi sustituidos como estrógenos relacionados a los moduladores del receptor alfa.
AR065656A1 (es) Tiazolidindionas n-alquiladas fenoxi sustituidas como moduladoras del receptor alfa relacionado con estrogeno
AR065657A1 (es) DERIVADOS DE 4-OXO-TIAZOL, COMPOSICIoN FARMACÉUTICA, MÉTODO DE PREPARACIoN DE LA MISMA Y SU USO EN LA FABRICACIoN DE UN MEDICAMENTO PARA EL TRATAMIENTO DE ENFERMEDADES MODULADAS POR EL RECEPTOR ALFA RELACIONADOS CON ESTRoGENOS.
AR080206A1 (es) Aminotiazolonas como moduladores del receptor alfa relacionados con estrogeno
AR065876A1 (es) Compuestos activos para 11 beta -hsd1
RU2016143333A (ru) Амидные производные и их фармацевтически приемлемые соли, способ их получения и медицинское применение
AR071788A1 (es) Derivados de 3-aminocarbazol, composiciones farmaceuticas que los contienen, metodo de preparacion y uso de los mismos para tratar y/o prevenir trastornos asociados con la produccion de prostaglandina e2(pge2), tales como aterosclerosis, artritis, artrosis y tumores, entre otros.
JP2010520308A5 (es)
AR078497A1 (es) Isoxazoles como antagonistas de los receptores de acido lisofosfatidico
AR078153A1 (es) Compuestos y composiciones como moduladores de la actividad de tlr
CO6531444A2 (es) Métodos sintéticos para compuestos espiro-oxoindol
AR089644A1 (es) Compuestos tipo anilina utiles como intermediarios para preparar insecticidas
UY33278A (es) Pirimidinas sustituidas como antagonistas del receptor de la protaglandina d2
AR093042A1 (es) Derivados de etinilo
AR087470A1 (es) Derivados imidazolicos bifenilenicos y composiciones farmaceuticas que los contienen
ECSP11011118A (es) ESPIRO AZEPAN OXAZOLIDINONAS COMO BLOQUEADORES DEL CANAL DE POTASIO Kv1.3
RU2017121460A (ru) Производные пиридинкарбоксамида, способ их получения и их фармацевтическое применение
PE20181319A1 (es) Compuestos de isoindol
AR099047A1 (es) Derivados etinilo
MY162998A (en) Ethynyl derivatives
AR104863A1 (es) Derivados imidazol
AR071486A1 (es) 2-( fenil sustituido ) -6- hidroxi o alcoxi -5- substituido -4- pirimidin carboxilatos y su uso como herbicidas
PE20150733A1 (es) Derivados de etinilo como moduladores de la actividad del receptor mglur5
AR105327A1 (es) Derivados de imidazol

Legal Events

Date Code Title Description
FB Suspension of granting procedure