AR080206A1 - Aminotiazolonas como moduladores del receptor alfa relacionados con estrogeno - Google Patents
Aminotiazolonas como moduladores del receptor alfa relacionados con estrogenoInfo
- Publication number
- AR080206A1 AR080206A1 ARP110100487A ARP110100487A AR080206A1 AR 080206 A1 AR080206 A1 AR 080206A1 AR P110100487 A ARP110100487 A AR P110100487A AR P110100487 A ARP110100487 A AR P110100487A AR 080206 A1 AR080206 A1 AR 080206A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- halo
- substituted
- arthritis
- groups
- Prior art date
Links
Classifications
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- 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
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- 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
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
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- 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
- 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
- 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
-
- 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
- A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
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- 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
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- 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
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- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
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- 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]
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- 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
-
- 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
- A61P3/04—Anorexiants; Antiobesity agents
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- 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
- A61P3/06—Antihyperlipidemics
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/30—Oestrogens
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
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- 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
- C07D417/14—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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pain & Pain Management (AREA)
- Endocrinology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Oncology (AREA)
- Emergency Medicine (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Child & Adolescent Psychology (AREA)
- Reproductive Health (AREA)
- Immunology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Dermatology (AREA)
- Pulmonology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Los métodos para preparar esos compuestos, composiciones, productos intermedios y derivados de estos y para tratar una afeccion que incluye pero no se limita a, la espondilitis anquilosante, arterosclerosis, artritis (tales como artritis reumatoide, artritis infecciosa, artritis de la ninez, artritis psoriásica, artritis reactiva), enfermedades relacionadas con los huesos (que incluye aquellas relacionadas con la formacion de los huesos), cáncer de mama, (que incluye aquellos que no responden a la terapia anti-estrogeno), trastornos cardiovasculares, enfermedades relacionadas con los cartílagos (tales como lesion/pérdida del cartílago, degeneracion del cartílago, y aquellas relacionadas con la formacion del cartílago), condrodisplasia, condrosarcoma, lesiones cronicas de la espalda, bronquitis cronica, enfermedad inflamatoria cronica de las vías respiratorias, enfermedad pulmonar obstructiva cronica, diabetes, trastornos de la homeostasis energética, gota, seudogota, trastornos de lípidos, síndrome metabolico, mieloma multiple, obesidad, osteoartritis, osteogénesis imperfecta, metástasis osea osteolítica, osteomalacia, osteoporosis, enfermedad de Paget, enfermedad periodontal, polimialgia reumática, síndrome de Reiter, lesion por esfuerzo repetitivo, hiperglucemia, 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 -C(O)-alquilo C1-4, en donde el alquilo C1-4 puede ser sustituido con halo; R2 es halo, ciano, H, alquilo C1-4, alquenilo C1-4, alcoxi C1-4, -S(O2)-alquilo C1-4, -C(O)N(R5)(R6), o hidroxilo, en donde el alquilo C1-4 puede ser sustituido con halo o hidroxilo; R3 es H, halo, -CN, o alquilo C1-4; y R4 y R5 se seleccionan independientemente de alquenilo C1-4, -O-alquilo C1-4, alquilo C1-4, y heterociclilo; en donde el alquilo C1-4 puede ser sustituido con uno a cinco grupos, los grupos se seleccionan independientemente de halo, -OR6, ciano, -C(O)OR6, cicloalquilo, -N(R6)(R7), heterociclo opcionalmente sustituido con alquilo C1-4 o alquilo C1-4-OR6, arilo opcionalmente sustituido con hidroxilo, y heteroarilo opcionalmente sustituido con alquilo C1-4; en donde el heterociclilo puede ser sustituido con uno a cinco grupos, los grupos se seleccionan independientemente de halo, alquilo C1-6, -C(O)OR6, y -C(O)-N(R6)-OR7; en donde el alquilo C1-6 puede ser sustituido con -OR6, -C(O)NR6R7, y halo; en donde R6 y R7 son independientemente H o alquilo C1-4; o un isomero optico, enantiomero, diastereomero, isomero cis-trans, racemato o sal farmacéuticamente aceptable de este.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US30517710P | 2010-02-17 | 2010-02-17 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR080206A1 true AR080206A1 (es) | 2012-03-21 |
Family
ID=43920677
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110100487A AR080206A1 (es) | 2010-02-17 | 2011-02-17 | Aminotiazolonas como moduladores del receptor alfa relacionados con estrogeno |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US8426604B2 (es) |
| EP (1) | EP2536716B1 (es) |
| JP (1) | JP2013519729A (es) |
| KR (1) | KR20120133383A (es) |
| CN (1) | CN102869660A (es) |
| AR (1) | AR080206A1 (es) |
| AU (1) | AU2011218268A1 (es) |
| BR (1) | BR112012020604A2 (es) |
| CA (1) | CA2789753A1 (es) |
| MX (1) | MX2012009528A (es) |
| RU (1) | RU2012139459A (es) |
| TW (1) | TW201130831A (es) |
| UY (1) | UY33230A (es) |
| WO (1) | WO2011103130A1 (es) |
Families Citing this family (5)
| 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 |
| EP2832367B1 (en) | 2012-03-26 | 2020-07-15 | Nippon Chemiphar Co., Ltd. | Agent for preventing or treating giant cell tumor or chondrosarcoma arising in bone/soft tissue |
| KR20220000993A (ko) | 2013-09-25 | 2022-01-04 | 닛뽕 케미파 가부시키가이샤 | 골·연부에 발생하는 거세포성 종양, 연골육종 또는 골육종의 예방, 치료 또는 전이 예방을 위한 약제, 동맥색전술용 국소 주입제 및 인공골 |
| TW201811752A (zh) * | 2016-09-06 | 2018-04-01 | 比利時商健生藥品公司 | 用作升糖素受體拮抗劑之吲唑衍生物 |
| 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 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CZ378497A3 (cs) * | 1995-06-02 | 1998-04-15 | Synthelabo | Deriváty oxazolidinonu, způsob jejich přípravy a jejich terapeutické použití |
| CN1246868A (zh) | 1996-12-17 | 2000-03-08 | 扇形支撑剑桥有限公司 | 黑皮素 |
| EA200700262A1 (ru) | 2004-07-14 | 2007-08-31 | Янссен Фармацевтика Н.В. | Арилидены для лечения заболеваний, опосредуемых эстроген-родственным рецепторам альфа |
| US7977489B2 (en) * | 2004-10-22 | 2011-07-12 | Exelixis, Inc. | Benzylthiazolone inhibitors of estrogen-related receptors (ERR) |
| UA98484C2 (ru) * | 2007-03-07 | 2012-05-25 | Янссен Фармацевтика Н.В. | ЗАМЕЩЕННЫЕ ФЕНОКСИАМИНОТИАЗОЛОНЫ КАК МОДУЛЯТОРЫ α-РЕЦЕПТОРА ЭСТРОГЕНА |
-
2011
- 2011-02-16 KR KR1020127023756A patent/KR20120133383A/ko not_active Application Discontinuation
- 2011-02-16 AU AU2011218268A patent/AU2011218268A1/en not_active Abandoned
- 2011-02-16 BR BR112012020604A patent/BR112012020604A2/pt not_active IP Right Cessation
- 2011-02-16 CA CA2789753A patent/CA2789753A1/en not_active Abandoned
- 2011-02-16 CN CN2011800194232A patent/CN102869660A/zh active Pending
- 2011-02-16 TW TW100105005A patent/TW201130831A/zh unknown
- 2011-02-16 EP EP11705404.9A patent/EP2536716B1/en active Active
- 2011-02-16 RU RU2012139459/04A patent/RU2012139459A/ru not_active Application Discontinuation
- 2011-02-16 US US13/028,266 patent/US8426604B2/en active Active
- 2011-02-16 JP JP2012553980A patent/JP2013519729A/ja not_active Withdrawn
- 2011-02-16 WO PCT/US2011/024999 patent/WO2011103130A1/en active Application Filing
- 2011-02-16 MX MX2012009528A patent/MX2012009528A/es not_active Application Discontinuation
- 2011-02-17 AR ARP110100487A patent/AR080206A1/es unknown
- 2011-02-17 UY UY0001033230A patent/UY33230A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2013519729A (ja) | 2013-05-30 |
| AU2011218268A1 (en) | 2012-09-06 |
| MX2012009528A (es) | 2013-01-14 |
| CA2789753A1 (en) | 2011-08-25 |
| CN102869660A (zh) | 2013-01-09 |
| RU2012139459A (ru) | 2014-03-27 |
| UY33230A (es) | 2011-08-31 |
| WO2011103130A1 (en) | 2011-08-25 |
| EP2536716B1 (en) | 2014-05-21 |
| US8426604B2 (en) | 2013-04-23 |
| WO2011103130A8 (en) | 2012-09-13 |
| KR20120133383A (ko) | 2012-12-10 |
| US20110200586A1 (en) | 2011-08-18 |
| TW201130831A (en) | 2011-09-16 |
| EP2536716A1 (en) | 2012-12-26 |
| BR112012020604A2 (pt) | 2019-09-24 |
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