MX338831B - Moduladores selectivos de receptores de androgenos. - Google Patents

Moduladores selectivos de receptores de androgenos.

Info

Publication number
MX338831B
MX338831B MX2012008995A MX2012008995A MX338831B MX 338831 B MX338831 B MX 338831B MX 2012008995 A MX2012008995 A MX 2012008995A MX 2012008995 A MX2012008995 A MX 2012008995A MX 338831 B MX338831 B MX 338831B
Authority
MX
Mexico
Prior art keywords
androgen receptor
iia
iii
formula
receptor modulators
Prior art date
Application number
MX2012008995A
Other languages
English (en)
Other versions
MX2012008995A (es
Inventor
Chris P Miller
Original Assignee
Radius Health Inc
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 Radius Health Inc filed Critical Radius Health Inc
Publication of MX2012008995A publication Critical patent/MX2012008995A/es
Publication of MX338831B publication Critical patent/MX338831B/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/80—[b, c]- or [b, d]-condensed
    • C07D209/82—Carbazoles; Hydrogenated carbazoles
    • C07D209/88—Carbazoles; Hydrogenated carbazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring 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
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • 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
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • 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
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P17/08—Antiseborrheics
    • 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
    • A61P17/10—Anti-acne agents
    • 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
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • A61P19/08—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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/24—Antidepressants
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • 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
    • 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
    • A61P5/26—Androgens
    • 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
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • 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
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • 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
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/80—[b, c]- or [b, d]-condensed
    • C07D209/94—[b, c]- or [b, d]-condensed containing carbocyclic rings other than six-membered
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/74—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving hormones or other non-cytokine intercellular protein regulatory factors such as growth factors, including receptors to hormones and growth factors
    • G01N33/743—Steroid hormones
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/435—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
    • G01N2333/705—Assays involving receptors, cell surface antigens or cell surface determinants
    • G01N2333/72—Assays involving receptors, cell surface antigens or cell surface determinants for hormones
    • G01N2333/723—Steroid/thyroid hormone superfamily, e.g. GR, EcR, androgen receptor, oestrogen receptor
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value
    • G01N2500/04—Screening involving studying the effect of compounds C directly on molecule A (e.g. C are potential ligands for a receptor A, or potential substrates for an enzyme A)
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value
    • G01N2500/10—Screening for compounds of potential therapeutic value involving cells

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurosurgery (AREA)
  • Reproductive Health (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Gynecology & Obstetrics (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • General Physics & Mathematics (AREA)
  • Physics & Mathematics (AREA)
  • Microbiology (AREA)
  • Food Science & Technology (AREA)

Abstract

La presente invención se refiere a compuestos de las formulas (I), (Ia), (Ib), (Ic), (IIa) o (III) o sus sales, composiciones farmacéuticas que comprenden un compuesto de formula (I), (Ia), (Ib), (Ic), (IIa) o (III) y un excipiente farmacéuticamente aceptable, métodos para modular el receptor de andrógenos , métodos para tratar enfermedades tratadas beneficiosamente por un modulador del receptor de andrógenos (por ejemplo, sarcopenia, cáncer de próstata, anticoncepción, trastornos o enfermedades relacionadas a la diabetes tipo 2, anemia, depresión y enfermedad renal) y procesos para preparar compuestos de formulas (I), (Ia), (Ib), (Ic), (IIa) o (III) e intermedios útiles en la preparación de estos.
MX2012008995A 2010-02-04 2011-02-04 Moduladores selectivos de receptores de androgenos. MX338831B (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US30149210P 2010-02-04 2010-02-04
PCT/US2011/023768 WO2011097496A1 (en) 2010-02-04 2011-02-04 Selective androgen receptor modulators

Publications (2)

Publication Number Publication Date
MX2012008995A MX2012008995A (es) 2012-11-22
MX338831B true MX338831B (es) 2016-05-03

Family

ID=44355809

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2012008995A MX338831B (es) 2010-02-04 2011-02-04 Moduladores selectivos de receptores de androgenos.

Country Status (8)

Country Link
US (3) US8987319B2 (es)
EP (1) EP2531029B1 (es)
JP (2) JP5964756B2 (es)
AU (1) AU2011212813B2 (es)
BR (1) BR112012019551A2 (es)
CA (1) CA2788907A1 (es)
MX (1) MX338831B (es)
WO (1) WO2011097496A1 (es)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3388086B1 (en) 2007-08-17 2020-10-07 Purdue Research Foundation Psma binding ligand-linker conjugates and methods for using
AU2011212813B2 (en) 2010-02-04 2014-10-23 Radius Health, Inc. Selective androgen receptor modulators
US9951324B2 (en) 2010-02-25 2018-04-24 Purdue Research Foundation PSMA binding ligand-linker conjugates and methods for using
DK2568806T3 (en) 2010-05-12 2016-08-15 Radius Health Inc therapy Programs
JP5965909B2 (ja) 2010-09-28 2016-08-10 ラジウス ヘルス，インコーポレイテッド 選択的アンドロゲン受容体モジュレーター
CN103172643B (zh) * 2011-12-26 2016-03-02 中国医学科学院药物研究所 黄皮咔唑生物碱及其制备方法和其药物组合物与用途
EP3875082A1 (en) 2012-11-15 2021-09-08 Endocyte, Inc. Conjugates for treating diseases caused by psma expressing cells
EP4095130B1 (en) 2013-10-18 2024-01-31 Novartis AG Labeled inhibitors of prostate specific membrane antigen (psma), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer
US9682960B2 (en) 2013-12-19 2017-06-20 Endorecherche, Inc. Non-steroidal antiandrogens and selective androgen receptor modulators with a pyridyl moiety
EP3834824A1 (en) 2014-03-28 2021-06-16 Duke University Method of treating cancer using selective estrogen receptor modulators
US9421264B2 (en) 2014-03-28 2016-08-23 Duke University Method of treating cancer using selective estrogen receptor modulators
US10188759B2 (en) 2015-01-07 2019-01-29 Endocyte, Inc. Conjugates for imaging
JP6757037B2 (ja) * 2016-02-15 2020-09-16 学校法人近畿大学 ストレス評価方法
CA3027563A1 (en) 2016-06-22 2017-12-28 Radius Health, Inc. Ar+ breast cancer treatment methods
EP3565542B1 (en) 2017-01-05 2024-04-10 Radius Pharmaceuticals, Inc. Polymorphic forms of rad1901-2hcl
WO2020010216A1 (en) 2018-07-04 2020-01-09 Radius Pharmaceuticals, Inc. Polymorphic forms of rad 1901-2hcl
CN109239214B (zh) * 2018-09-19 2020-01-31 珠海润都制药股份有限公司 一种沙库比曲钠中沙库比曲异构体检验方法
WO2023088388A1 (zh) * 2021-11-19 2023-05-25 杭州拿因生物科技有限责任公司 四氢咔唑类化合物、其药物组合物及用途

Family Cites Families (95)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1547758A (en) 1975-07-29 1979-06-27 Shell Int Research Herbicidal composition
JPH01261381A (ja) 1988-04-12 1989-10-18 Nippon Soda Co Ltd オキサ（チア）ジアゾール誘導体、その製造方法及び殺ダニ剤
US5411981A (en) 1991-01-09 1995-05-02 Roussel Uclaf Phenylimidazolidines having antiandrogenic activity
FR2693461B1 (fr) 1992-07-08 1994-09-02 Roussel Uclaf Nouvelles phénylimidazolidines substituées, leur procédé de préparation, leur application comme médicaments et les compositions pharmaceutiques les renfermant.
GB9310635D0 (en) 1993-05-21 1993-07-07 Glaxo Group Ltd Chemical compounds
UA51652C2 (uk) 1995-06-08 2002-12-16 Новартіс Аг Спосіб гідрування імінів
PT918774E (pt) 1996-06-27 2002-05-31 Ligand Pharm Inc Compostos moduladores do receptor para androgenio e metodos
US20090264534A1 (en) 1996-11-27 2009-10-22 Dalton James T Selective androgen receptor modulators
FR2770842B1 (fr) 1997-11-13 1999-12-17 Oreal Nouveaux composes derives de n-aryl 2-hydroxy alkylamides
US6159959A (en) * 1999-05-06 2000-12-12 American Home Products Corporation Combined estrogen and antiestrogen therapy
KR20030016310A (ko) 2000-06-28 2003-02-26 브리스톨-마이어스스퀴브컴파니 선택적 안드로겐 수용체 조절제, 및 그의 확인, 고안 및사용 방법
JP2004518617A (ja) 2000-08-24 2004-06-24 ザ・ユニバーシティ・オブ・テネシー・リサーチ・コーポレーション 選択的アンドロゲン受容体モジュレーター及びその使用方法
EP1414795A4 (en) 2001-07-31 2006-03-01 Bristol Myers Squibb Co BICYCLIC MODULATORS OF THE FUNCTION OF THE ANDROGEN RECEPTOR
US8853266B2 (en) 2001-12-06 2014-10-07 University Of Tennessee Research Foundation Selective androgen receptor modulators for treating diabetes
WO2003068217A1 (en) 2002-02-15 2003-08-21 Endorecherche, Inc. Biphenil derivatives and their use as antiandrogenic agents
US7772433B2 (en) 2002-02-28 2010-08-10 University Of Tennessee Research Foundation SARMS and method of use thereof
TW200407324A (en) 2002-05-17 2004-05-16 Bristol Myers Squibb Co Bicyclic modulators of androgen receptor function
PT1557411E (pt) 2002-07-12 2012-11-22 Astellas Pharma Inc Derivado de n-fenil-(2r,5s)dimetilpiperazina
WO2004016576A1 (ja) 2002-08-12 2004-02-26 Takeda Pharmaceutical Company Limited 縮合ベンゼン誘導体および用途
WO2004041277A1 (en) 2002-11-01 2004-05-21 Merck & Co., Inc. Carbonylamino-benzimidazole derivatives as androgen receptor modulators
UA79504C2 (en) 2002-11-07 2007-06-25 Organon Nv Indols for treating diseases associated with androgen receptors
WO2004045518A2 (en) 2002-11-15 2004-06-03 Bristol-Myers Squibb Company Open chain prolyl urea-related modulators of androgen receptor function
WO2004080377A2 (en) 2003-03-11 2004-09-23 Neurosearch A/S Kcnq channel modulating compounds and their pharmaceutical use
JP2007500245A (ja) 2003-06-10 2007-01-11 スミスクライン ビーチャム コーポレーション 化合物
WO2004110978A2 (en) 2003-06-10 2004-12-23 Smithkline Beecham Corporation 1-aminonaphthalenes as modulators of androgen, glucocorticoid, mineralocorticoid and progesterone receptors
WO2005000309A2 (en) 2003-06-27 2005-01-06 Ionix Pharmaceuticals Limited Chemical compounds
FI20030958A0 (fi) 2003-06-27 2003-06-27 Orion Corp Uusia yhdisteitä
WO2005025572A1 (en) 2003-09-10 2005-03-24 Merck & Co., Inc. 17-heterocyclic-4-azasteroid derivatives as androgen receptor modulators
US20050124625A1 (en) 2003-10-21 2005-06-09 Salvati Mark E. Piperazine derivatives and their use as modulators of nuclear hormone receptor function
GB0324551D0 (en) 2003-10-21 2003-11-26 Karobio Ab Novel compounds
US7256208B2 (en) 2003-11-13 2007-08-14 Bristol-Myers Squibb Company Monocyclic N-Aryl hydantoin modulators of androgen receptor function
WO2005049574A1 (en) 2003-11-20 2005-06-02 Warner-Lambert Company Llc Androgen receptor modulators
AU2003297904A1 (en) 2003-12-12 2005-07-14 University Of Maryland, Baltimore Immunomodulatory compounds that target and inhibit the py+3 binding site of tyrosene kinase p56 lck sh2 domain
RU2397176C2 (ru) 2004-01-07 2010-08-20 Эндорешерш, Инк. Стероидные фармацевтические продукты, направленные на спираль 12
US7820702B2 (en) 2004-02-04 2010-10-26 Bristol-Myers Squibb Company Sulfonylpyrrolidine modulators of androgen receptor function and method
US20050182105A1 (en) 2004-02-04 2005-08-18 Nirschl Alexandra A. Method of using 3-cyano-4-arylpyridine derivatives as modulators of androgen receptor function
JP4805909B2 (ja) 2004-03-03 2011-11-02 スミスクライン ビーチャム コーポレーション 選択的アンドロゲン受容体モジュレーターとしてのアニリン誘導体
US7696241B2 (en) 2004-03-04 2010-04-13 Bristol-Myers Squibb Company Bicyclic compounds as modulators of androgen receptor function and method
US7625923B2 (en) 2004-03-04 2009-12-01 Bristol-Myers Squibb Company Bicyclic modulators of androgen receptor function
US7388027B2 (en) 2004-03-04 2008-06-17 Bristol-Myers Squibb Company Bicyclic compounds as modulators of androgen receptor function and method
GB0405033D0 (en) 2004-03-05 2004-04-07 Karobio Ab Novel pharmaceutical compositions
US8519158B2 (en) 2004-03-12 2013-08-27 Ligand Pharmaceuticals Incorporated Androgen receptor modulator compounds and methods
JP2007223901A (ja) 2004-03-24 2007-09-06 Takeda Chem Ind Ltd 複素環化合物およびその用途
US20080125399A1 (en) 2004-04-08 2008-05-29 Jiabing Wang 17 Beta-Acetamide-4-Azasteroids As Androgen Receptor Modulators
TW200602317A (en) 2004-04-23 2006-01-16 Akzo Nobel Nv Novel androgens
JP4917018B2 (ja) * 2004-05-03 2012-04-18 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 選択的アンドローゲン受容体モジュレーター（ｓａｒｍｓ）としての新規インドール化合物
CN1980917B (zh) 2004-05-03 2014-02-12 詹森药业有限公司 作为选择性雄激素受体调节剂（sarms）的新的吲哚衍生物
US20080045504A1 (en) 2004-05-11 2008-02-21 Pfizer Products Inc. Benzonitrile Derivatives to Treat Musculoskeletal Frailty
RU2006144863A (ru) 2004-05-17 2008-06-27 Акэдиа Фармасьютикалз Инк. (Us) Модуляторы андрогеновых рецепторов и способ лечения заболеваний с их помощью
JP2008503447A (ja) 2004-05-29 2008-02-07 ７ティーエム ファーマ エイ／エス Ｃｒｔｈ２リガンドとしての置換チアゾール酢酸
PL1753417T3 (pl) 2004-06-07 2012-09-28 Univ Tennessee Res Found Selektywny modulator receptora androgenowego i jego zastosowania medyczne
CA2579514A1 (en) 2004-09-10 2006-03-23 Janssen Pharmaceutica N.V. Novel imidazolidin-2-one derivatives as selective androgen receptor modulators (sarms)
US7338973B2 (en) 2004-09-20 2008-03-04 Janssen Pharmaceutica N.V. Tetracyclic heteroatom containing derivatives useful as sex steroid hormone receptor modulators
CN101065363B (zh) 2004-09-30 2012-05-02 詹森药业有限公司 可用作选择性雄激素受体调节剂（sarms）的新苯并咪唑衍生物
US8143425B2 (en) 2004-10-12 2012-03-27 Bristol-Myers Squibb Company Heterocyclic aromatic compounds useful as growth hormone secretagogues
US7834063B2 (en) 2004-10-13 2010-11-16 Glaxosmithkline Llc Benzonitryl and nitrobenzyl derivatives that modulate androgen receptors
WO2006060108A1 (en) 2004-10-29 2006-06-08 Merck & Co., Inc. N-(pyridin-3-yl)-2-phenylbutanamides as androgen receptor modulators
WO2006055184A2 (en) 2004-11-16 2006-05-26 Janssen Pharmaceutica N.V. Novel heterocycle derivatives useful as selective androgen receptor modulators (sarms)
MX2007006179A (es) 2004-11-23 2007-06-20 Ptc Therapeutics Inc Tetrahidrocarbazoles como agentes activos para inhibir la produccion del factor de crecimiento endotelial vascular por control de la traduccion.
KR20070112775A (ko) 2005-01-10 2007-11-27 아카디아 파마슈티칼스 인코포레이티드 선택적인 안드로겐 수용체 조절자로서의 아미노페닐 유도체
WO2006113552A2 (en) 2005-04-15 2006-10-26 Smithkline Beecham Corporation Cyanoarylamines
US7807691B2 (en) 2005-05-13 2010-10-05 Eli Lilly And Company Substituted N-arylpyrrolidines as selective androgen receptor modulators
JP2008546643A (ja) 2005-06-06 2008-12-25 スミスクライン ビーチャム コーポレーション ４−置換アリールアミン誘導体および医薬組成物におけるその使用
US7829589B2 (en) 2005-06-10 2010-11-09 Elixir Pharmaceuticals, Inc. Sulfonamide compounds and uses thereof
US7709516B2 (en) 2005-06-17 2010-05-04 Endorecherche, Inc. Helix 12 directed non-steroidal antiandrogens
BRPI0611705A2 (pt) 2005-06-24 2016-11-16 Lilly Co Eli composto ou um sal farmaceuticamente aceitável do mesmo, composição farmacêutica, e, uso de composto
WO2007005887A2 (en) 2005-07-01 2007-01-11 Ligand Pharmaceuticals Incorporated Androgen receptor modulator compounds, compositions and uses thereof
JP5070054B2 (ja) 2005-08-01 2012-11-07 武田薬品工業株式会社 環状アミン化合物
JP2008303145A (ja) 2005-09-22 2008-12-18 Takeda Chem Ind Ltd Ｇｒｋ阻害剤からなる強心薬
US7776859B2 (en) 2005-10-14 2010-08-17 Bristol-Myers Squibb Company Hexahydroimidazopyrazin-3-one compounds useful as modulators of androgen receptor function
TW200730505A (en) 2005-12-07 2007-08-16 Merck & Co Inc Polymorphs of an androgen receptor modulator
EP1984343B1 (en) 2006-01-24 2013-02-27 Janssen Pharmaceutica N.V. 2-substituted benzimidazoles as selective androgen receptor modulators (sarms)
NZ570533A (en) 2006-03-03 2011-02-25 Orion Corp Compounds useful as Selective androgen receptor modulators (SARM), in particular (2S)-3-(4-cyano-3-fluorophenoxy)-N-(4-cyano-3-methylphenyl)-2-hydroxy-2-methylpropionamide useful in hormonal therapy
MX2009000385A (es) 2006-07-12 2009-04-06 Univ Tennessee Res Foundation Acil-anilidas sustituidas y metodos de uso de las mismas.
KR20090035707A (ko) 2006-07-19 2009-04-10 더 오하이오 스테이트 유니버시티 리서치 파운데이션 선택적인 안드로겐 수용체 모듈레이터, 그 유사체와 유도체, 및 그의 용도
ES2581765T3 (es) 2006-08-24 2016-09-07 University Of Tennessee Research Foundation Acilanilidas sustituidas y métodos de uso de las mismas
WO2008042571A2 (en) 2006-09-29 2008-04-10 Smithkline Beecham Corporation Substituted indole compounds
WO2008044033A1 (en) 2006-10-11 2008-04-17 Astrazeneca Ab Amide derivatives
UA98777C2 (en) 2006-11-20 2012-06-25 Эли Лилли Энд Компани Tetrahydrocyclopenta[b]indole compounds as androgen receptor modulators
WO2008121602A1 (en) 2007-03-29 2008-10-09 Smithkline Beecham Corporation Chemical compounds
WO2008124000A2 (en) 2007-04-02 2008-10-16 Ligand Pharmaceuticals Incorporated Thiazole derivatives as androgen receptor modulator compounds
US9284345B2 (en) 2007-04-12 2016-03-15 Endorecherche, Inc. 17alpha-substituted steroids as systemic antiandrogens and selective androgen receptor modulators
US7696227B2 (en) 2007-04-13 2010-04-13 Regents Of The University Of California Small-molecule inhibitors of the androgen receptor
ES2406685T3 (es) 2007-08-07 2013-06-07 Takeda Pharmaceutical Company Limited Derivados de pirrolidin-2-ona como moduladores de los receptores de andrógenos
US20110105554A1 (en) * 2007-11-21 2011-05-05 Kinaris Biomedicals Gmbh Means for treating myosin-related diseases
MX2010006972A (es) 2007-12-21 2010-08-26 Ligand Pharm Inc Moduladores selectivos de receptores de andrógenos (sarm) y usos de los mismos.
CN101952286A (zh) 2007-12-21 2011-01-19 阿斯利康(瑞典)有限公司 用于治疗和雄激素受体有关的病症的双环衍生物
US8268872B2 (en) 2008-02-22 2012-09-18 Radius Health, Inc. Selective androgen receptor modulators
AU2009215843B2 (en) 2008-02-22 2011-09-08 Ellipses Pharma Ltd Selective androgen receptor modulators
WO2009133861A1 (ja) 2008-04-28 2009-11-05 武田薬品工業株式会社 環状アミン化合物
PT2297100E (pt) 2008-05-16 2013-01-24 Lilly Co Eli Moduladores dos receptores de andrógenos tetra-hidrociclopenta[b]indoles
WO2010118287A1 (en) 2009-04-10 2010-10-14 Radius Health, Inc. Selective androgen receptor modulators
AU2011212813B2 (en) 2010-02-04 2014-10-23 Radius Health, Inc. Selective androgen receptor modulators
US8642632B2 (en) 2010-07-02 2014-02-04 Radius Health, Inc. Selective androgen receptor modulators
JP5965909B2 (ja) 2010-09-28 2016-08-10 ラジウス ヘルス，インコーポレイテッド 選択的アンドロゲン受容体モジュレーター

Also Published As

Publication number Publication date
EP2531029B1 (en) 2016-10-19
US20150266821A1 (en) 2015-09-24
EP2531029A1 (en) 2012-12-12
JP2013518902A (ja) 2013-05-23
MX2012008995A (es) 2012-11-22
US20130041007A1 (en) 2013-02-14
US8987319B2 (en) 2015-03-24
BR112012019551A2 (pt) 2016-08-09
AU2011212813A1 (en) 2012-09-06
AU2011212813B2 (en) 2014-10-23
JP5964756B2 (ja) 2016-08-03
EP2531029A4 (en) 2013-05-29
JP2016138118A (ja) 2016-08-04
US20170121285A1 (en) 2017-05-04
CA2788907A1 (en) 2011-08-11
WO2011097496A1 (en) 2011-08-11

Similar Documents

Publication Publication Date Title
MX338831B (es) Moduladores selectivos de receptores de androgenos.
WO2010118287A8 (en) Selective androgen receptor modulators
WO2009105214A3 (en) Selective androgen receptor modulators
BR112013007685A2 (pt) aplicações relacionadas com moduladores de receptor anfrógeno seletivos
TN2014000030A1 (en) Tetrahydropyrido-pyridine and tetrahydropyrido-pyrimidine compounds and use thereof as c5a receptor modulators
MX2021004492A (es) Composiciones para el tratamiento de trastornos del snc.
EA201190021A1 (ru) Модуляторы toll-подобных рецепторов
WO2014002051A3 (en) Complement pathway modulators and uses thereof
MX2013008431A (es) Antagonista del receptor de mineralocorticoides.
WO2014002058A3 (en) Complement pathway modulators and uses thereof
MX347391B (es) Compuestos de indol o análogos de los mismos útiles para el tratamiento de degeneración macular relacionada con la edad (amd).
EA201390947A1 (ru) Соединения 2-амино-4-арилтиазола в качестве антагонистов trpa1
MX2013012588A (es) Inhibidores de cinasa.
WO2011127333A3 (en) Compounds for treating disease, for administering, and for pharmaceutical compositions
EA201500298A1 (ru) Алкоксипиразолы в качестве активаторов растворимой гуанилатциклазы
EA200970500A1 (ru) СОЕДИНЕНИЯ ТЕТРАГИДРОЦИКЛОПЕНТА[b]ИНДОЛА В КАЧЕСТВЕ МОДУЛЯТОРОВ РЕЦЕПТОРА АНДРОГЕНОВ
MX2013011927A (es) Derivados de glicosido y usos de los mismos para el tratamiento de diabetes.
IN2012DN02139A (es)
WO2009025785A3 (en) Cb2 receptor ligands for the treatment of pain
WO2013040227A3 (en) Therapeutic compounds
TN2013000346A1 (en) Asymmetric ureas and medical uses thereof
MX2011006132A (es) Imidazol carboxamidas fusionadas como moduladores de trpv3.
MY160392A (en) Triptolide prodrugs
UA98772C2 (ru) Производные циклопропиламина как модуляторы н3-гистаминового рецептора
EA201391524A1 (ru) Производные гликозида и их применение

Legal Events

Date Code Title Description
FG Grant or registration