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)
Spanish (es)
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)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Reproductive Health (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Gynecology & Obstetrics (AREA)
  • Emergency Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Analytical Chemistry (AREA)
  • Cell Biology (AREA)
  • Pathology (AREA)
  • General Physics & Mathematics (AREA)
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 (enExample)
EP (1) EP2531029B1 (enExample)
JP (2) JP5964756B2 (enExample)
AU (1) AU2011212813B2 (enExample)
BR (1) BR112012019551A2 (enExample)
CA (1) CA2788907A1 (enExample)
MX (1) MX338831B (enExample)
WO (1) WO2011097496A1 (enExample)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK2187965T3 (da) 2007-08-17 2020-01-20 Purdue Research Foundation Psma-bindingsligand-linker-konjugater og fremgangsmåder til anvendelse
JP5964756B2 (ja) 2010-02-04 2016-08-03 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
US9951324B2 (en) 2010-02-25 2018-04-24 Purdue Research Foundation PSMA binding ligand-linker conjugates and methods for using
PL2568806T3 (pl) 2010-05-12 2017-03-31 Radius Health, Inc. Schematy lecznicze
AU2011312490B2 (en) 2010-09-28 2015-06-25 Radius Pharmaceuticals, Inc. Selective androgen receptor modulators
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
KR102318999B1 (ko) 2012-11-15 2021-10-29 엔도사이트, 인코포레이티드 Psma 발현 세포에 의해 야기되는 질병을 치료하기 위한 컨쥬게이트
AU2014336638C1 (en) 2013-10-18 2020-09-17 Novartis Ag Labeled inhibitors of prostate specific membrane antigen (PSMA), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer
WO2015073678A1 (en) 2013-11-14 2015-05-21 Endocyte, Inc. Compounds for positron emission tomography
US9682960B2 (en) 2013-12-19 2017-06-20 Endorecherche, Inc. Non-steroidal antiandrogens and selective androgen receptor modulators with a pyridyl moiety
ES2939940T3 (es) 2014-03-28 2023-04-28 Univ Duke Tratamiento del cáncer de mama utilizando moduladores selectivos de los receptores de estrógenos
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
WO2017223115A1 (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
MX2020010813A (es) 2018-04-17 2021-01-08 Endocyte Inc Metodos de tratamiento de cancer.
SG11202013177WA (en) 2018-07-04 2021-01-28 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
US12441745B2 (en) 2019-02-12 2025-10-14 Radius Pharmaceuticals, Inc. Processes and compounds
EP3972627A4 (en) 2019-05-20 2023-06-21 Endocyte, Inc. Methods for preparing psma conjugates
WO2022106629A1 (en) 2020-11-19 2022-05-27 Novartis Ag Synthesis of prostate specific membrane antigen (psma) ligands
US20250034089A1 (en) * 2021-11-19 2025-01-30 Nain Biotech (Hangzhou) Co., Ltd. Tetrahydrocarbazole compound, and pharmaceutical composition and use thereof

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
BR9710988A (pt) 1996-06-27 2002-01-15 Ligand Pharm Inc Método e compostos moduladores receptores de androgênio
US20090264534A1 (en) 1996-11-27 2009-10-22 Dalton James T Selective androgen receptor modulators
US6569896B2 (en) 2000-08-24 2003-05-27 The University Of Tennessee Research Corporation Selective androgen receptor modulators and methods of use thereof
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
HUP0303172A3 (en) 2000-06-28 2006-05-29 Bristol Myers Squibb Co Selective androgen receptor modulators and methods for their identification, desing and use
WO2003011824A1 (en) 2001-07-31 2003-02-13 Bristol-Myers Squibb Company Bicyclic modulators of androgen receptor function
US8853266B2 (en) 2001-12-06 2014-10-07 University Of Tennessee Research Foundation Selective androgen receptor modulators for treating diabetes
ATE345125T1 (de) 2002-02-15 2006-12-15 Endorech Inc Biphenylderivate und ihre verwendung als antiandrogene
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
ES2393333T3 (es) 2002-07-12 2012-12-20 Astellas Pharma Inc. Derivado de N-fenil-(2R,5S)dimetilpiperazina
NZ538713A (en) 2002-08-12 2007-01-26 Takeda Chemical Industries Ltd Fused benzene derivative and use
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
EP1567487A4 (en) 2002-11-15 2005-11-16 Bristol Myers Squibb Co OPEN-CHAINED, PROLYL-FROSTED MODULATORS OF ANDROGEN RECEPTOR FUNCTION
JP2006523196A (ja) 2003-03-11 2006-10-12 ニューロサーチ、アクティーゼルスカブ 新規ｋｃｎｑチャネルを調節する化合物及びその医薬用途
WO2004110978A2 (en) 2003-06-10 2004-12-23 Smithkline Beecham Corporation 1-aminonaphthalenes as modulators of androgen, glucocorticoid, mineralocorticoid and progesterone receptors
WO2005000795A2 (en) 2003-06-10 2005-01-06 Smithkline Beecham Corporation Aniline derivatived androgen-, glucocorticoid-, mineralcorticoid- and progesterone- receptor modulators
FI20030958A0 (fi) 2003-06-27 2003-06-27 Orion Corp Uusia yhdisteitä
WO2005000309A2 (en) 2003-06-27 2005-01-06 Ionix Pharmaceuticals Limited Chemical compounds
EP1663228A4 (en) 2003-09-10 2010-10-06 Merck Sharp & Dohme 17-heterocyclic 4-azasteroid derivatives as androgen receptor modules
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
CA2545048A1 (en) 2003-11-20 2005-06-02 Warner-Lambert Company Llc Androgen receptor modulators
US20070196395A1 (en) 2003-12-12 2007-08-23 Mackerell Alexander Immunomodulatory compounds that target and inhibit the py'binding site of tyrosene kinase p56 lck sh2 domain
CN1930181A (zh) 2004-01-07 2007-03-14 恩多研究公司 螺旋12定向的甾族药品
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
ES2523017T3 (es) 2004-03-03 2014-11-20 Glaxosmithkline Llc Derivados de anilina como moduladores selectivos de los receptores de andrógenos
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
CA2562132A1 (en) 2004-04-08 2005-10-27 Merck & Co., Inc. 17 beta-acetamide-4-azasteroids as androgen receptor modulators
TW200602317A (en) 2004-04-23 2006-01-16 Akzo Nobel Nv Novel androgens
ATE525354T1 (de) * 2004-05-03 2011-10-15 Janssen Pharmaceutica Nv Benzofuranderivate als selektive androgenrezeptormodulatoren (sarms)
WO2005111028A1 (en) 2004-05-03 2005-11-24 Janssen Pharmaceutica N.V. Novel indole derivatives as selective androgen receptor modulators (sarms)
MXPA06013115A (es) 2004-05-11 2007-02-28 Pfizer Prod Inc Derivados de benzonitrilo para tratar la fragilidad musculoesqueletica.
EP1756101A2 (en) 2004-05-17 2007-02-28 Acadia Pharmaceuticals Inc. Androgen receptor modulators and method of treating disease using the same
CA2568742A1 (en) 2004-05-29 2005-12-08 7Tm Pharma A/S Substituted thiazoleacetic as crth2 ligands
DK2289872T3 (en) 2004-06-07 2017-10-09 Univ Tennessee Res Found Medical use of a selective androgen receptor modulator
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
CA2582356A1 (en) 2004-09-30 2006-04-13 Janssen Pharmaceutica N.V. Novel benzimidazole derivatives useful as selective androgen receptor modulators (sarms)
US8143425B2 (en) 2004-10-12 2012-03-27 Bristol-Myers Squibb Company Heterocyclic aromatic compounds useful as growth hormone secretagogues
JP2008515998A (ja) 2004-10-13 2008-05-15 スミスクライン ビーチャム コーポレーション 化合物
AU2005310238A1 (en) 2004-10-29 2006-06-08 Merck Sharp & Dohme Corp. N-(pyridin-3-yl)-2-phenylbutanamides as androgen receptor modulators
CN101103003A (zh) 2004-11-16 2008-01-09 詹森药业有限公司 用作选择性雄激素受体调节剂(sarms)的新的杂环衍生物
EP1817025A2 (en) * 2004-11-23 2007-08-15 PTC Therapeutics, Inc. Tetrahydrocarbazoles as active agents for inhibiting vegf production by translational control
NZ555974A (en) 2005-01-10 2010-11-26 Acadia Pharm Inc Aminophenyl derivatives as selective androgen receptor modulators
JP2008536868A (ja) 2005-04-15 2008-09-11 スミスクライン・ビーチャム・コーポレイション シアノアリールアミン
DE602006003432D1 (de) 2005-05-13 2008-12-11 Lilly Co Eli Latoren des androgenrezeptors
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
AU2006262283B2 (en) 2005-06-24 2011-10-13 Eli Lilly And Company Tetrahydrocarbazole derivatives useful as androgen receptor modulators (SARM)
US20090227571A1 (en) 2005-07-01 2009-09-10 Ligand Pharmaceuticals Incorporated Androgen Receptor Modulator Compounds and Methods
WO2007015567A1 (ja) 2005-08-01 2007-02-08 Takeda Pharmaceutical Company Limited 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
SI1984343T1 (sl) 2006-01-24 2013-05-31 Janssen Pharmaceutica N.V. 2-substituirani benzimidazoli kot selektivni modulatorji androgenskih receptorjev (sarms)
CA2642598C (en) 2006-03-03 2014-05-27 Orion Corporation Selective androgen receptor modulators
ES2780193T3 (es) 2006-07-12 2020-08-24 Univ Tennessee Res Found Compuesto para tratar el cáncer de mama y afecciones dependientes de la progestina
WO2008011072A2 (en) 2006-07-19 2008-01-24 Osurf (Ohio State University Research Foundation) Selective androgen receptor modulators, analogs and derivatives thereof and uses thereof
AU2007287070C1 (en) 2006-08-24 2013-02-14 University Of Tennessee Research Foundation Substituted acylanilides and methods of use thereof
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
WO2008128100A1 (en) 2007-04-13 2008-10-23 The Regents Of The University Of California Small-molecule inhibitors of the androgen receptor
MY159910A (en) 2007-08-07 2017-02-15 Takeda Pharmaceuticals Co Pyrrolidin-2-one derivatives as androgen receptor modulator
WO2009065600A2 (en) 2007-11-21 2009-05-28 Technische Universität Dresden Means for treating myosin-related diseases
CN101945853B (zh) 2007-12-21 2014-08-20 配体药物公司 选择性雄激素受体调节剂(sarm)及其应用
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
BRPI0907844B8 (pt) 2008-02-22 2021-05-25 Radius Health Inc compostos e método para modular um receptor de andrógeno, processos de preparação e composição farmacêutica dos mesmos e seus usos
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
EA019713B1 (ru) 2008-05-16 2014-05-30 Эли Лилли Энд Компани ТЕТРАГИДРОЦИКЛОПЕНТА[b]ИНДОЛЬНЫЕ МОДУЛЯТОРЫ РЕЦЕПТОРОВ АНДРОГЕНОВ
WO2010118287A1 (en) 2009-04-10 2010-10-14 Radius Health, Inc. Selective androgen receptor modulators
JP5964756B2 (ja) 2010-02-04 2016-08-03 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
US8642632B2 (en) 2010-07-02 2014-02-04 Radius Health, Inc. Selective androgen receptor modulators
AU2011312490B2 (en) 2010-09-28 2015-06-25 Radius Pharmaceuticals, Inc. Selective androgen receptor modulators

Also Published As

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

Similar Documents

Publication Publication Date Title
WO2010118287A8 (en) Selective androgen receptor modulators
WO2009105214A3 (en) Selective androgen receptor modulators
BR112013007685A2 (pt) aplicações relacionadas com moduladores de receptor anfrógeno seletivos
BR112012019551A2 (pt) moduladores seletivos do receptor de androgênio.
TN2014000030A1 (en) Tetrahydropyrido-pyridine and tetrahydropyrido-pyrimidine compounds and use thereof as c5a receptor modulators
MX2013012588A (es) Inhibidores de cinasa.
PH12014502462A1 (en) Complement pathway modulators and uses thereof
EA201190021A1 (ru) Модуляторы toll-подобных рецепторов
EP4527461A3 (en) A compound, compositions thereof and this compound for use in methods of treating cns disorders
MX351305B (es) Antagonistas del receptor de mineralocorticoides.
MX2012003389A (es) Moduladores de gpr40 de pirrolidina.
EA200970500A1 (ru) СОЕДИНЕНИЯ ТЕТРАГИДРОЦИКЛОПЕНТА[b]ИНДОЛА В КАЧЕСТВЕ МОДУЛЯТОРОВ РЕЦЕПТОРА АНДРОГЕНОВ
WO2009025785A3 (en) Cb2 receptor ligands for the treatment of pain
MY164354A (en) Asymmetric ureas and medical uses thereof
PH12013502204A1 (en) 3-spirocyclic piperidine derivatives as ghrelin receptor agonists
TN2013000413A1 (en) Glycoside derivatives and their uses for the treatment of diabetes
IN2012DN02139A (enExample)
MX2011011776A (es) Nuevos profarmacos de triptolite.
MX2011006132A (es) Imidazol carboxamidas fusionadas como moduladores de trpv3.
ATE412647T1 (de) Substituierte n-arylpyrrolidine als selektive modulatoren des androgenrezeptors
MX2011008195A (es) Derivados de indol como agentes anticancer.
WO2013040227A3 (en) Therapeutic compounds
HK1209105A1 (en) Vegfr3 inhibitors
UA98772C2 (ru) Производные циклопропиламина как модуляторы н3-гистаминового рецептора
MX2011006821A (es) Derivados de imidazol fusionados como antagonistas de trpv3.

Legal Events

Date Code Title Description
FG Grant or registration