BRPI0907844B8 - compostos e método para modular um receptor de andrógeno, processos de preparação e composição farmacêutica dos mesmos e seus usos - Google Patents

compostos e método para modular um receptor de andrógeno, processos de preparação e composição farmacêutica dos mesmos e seus usos

Info

Publication number
BRPI0907844B8
BRPI0907844B8 BRPI0907844A BRPI0907844A BRPI0907844B8 BR PI0907844 B8 BRPI0907844 B8 BR PI0907844B8 BR PI0907844 A BRPI0907844 A BR PI0907844A BR PI0907844 A BRPI0907844 A BR PI0907844A BR PI0907844 B8 BRPI0907844 B8 BR PI0907844B8
Authority
BR
Brazil
Prior art keywords
compounds
androgen receptor
modulating
formulas
pharmaceutical composition
Prior art date
Application number
BRPI0907844A
Other languages
English (en)
Inventor
P Miller Chris
Original Assignee
Radius Health Inc
Radius Pharmaceuticals 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, Radius Pharmaceuticals Inc filed Critical Radius Health Inc
Publication of BRPI0907844A2 publication Critical patent/BRPI0907844A2/pt
Publication of BRPI0907844B1 publication Critical patent/BRPI0907844B1/pt
Publication of BRPI0907844B8 publication Critical patent/BRPI0907844B8/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/10—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • 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
    • A61P19/08—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
    • A61P25/20—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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • 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
    • 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
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • 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
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D263/32—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/12—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

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

Abstract

moduladores seletivos do receptor de andrógeno. a presente invenção refere-se a compostos de formulas (i), la, ib, ic, id, le e ou seus sais, composições farmacêuticas que compreendem um composto de fórmulas i, la, ib, ic, id, le e um excipiente farmaceuticamente aceitável,métodos para modular o receptor de andrógeno, métodos para tratar doenças beneficamente tratadas por um modulador de andrógeno (por exemplo, sarcopenia, câncer da próstata, anticoncepção, distúrbios ou doenças relacionadas com a diabetes tipo 2, anemia, depressão e doença renal) e processos para preparar os compostos de fórmulas (i), la, ib, ic, id,le e intermediários úteis na preparação dos mesmos.
BRPI0907844A 2008-02-22 2009-02-19 compostos e método para modular um receptor de andrógeno, processos de preparação e composição farmacêutica dos mesmos e seus usos BRPI0907844B8 (pt)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US6669708P 2008-02-22 2008-02-22
US61/066,697 2008-02-22
US13235308P 2008-06-18 2008-06-18
US61/132,353 2008-06-18
US20572709P 2009-01-21 2009-01-21
US61/205,727 2009-01-21
PCT/US2009/001035 WO2009105214A2 (en) 2008-02-22 2009-02-19 Selective androgen receptor modulators

Publications (3)

Publication Number Publication Date
BRPI0907844A2 BRPI0907844A2 (pt) 2018-01-30
BRPI0907844B1 BRPI0907844B1 (pt) 2020-08-18
BRPI0907844B8 true BRPI0907844B8 (pt) 2021-05-25

Family

ID=40887412

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0907844A BRPI0907844B8 (pt) 2008-02-22 2009-02-19 compostos e método para modular um receptor de andrógeno, processos de preparação e composição farmacêutica dos mesmos e seus usos

Country Status (9)

Country Link
US (2) US8067448B2 (pt)
EP (1) EP2260028B1 (pt)
JP (1) JP5308458B2 (pt)
AU (1) AU2009215843B2 (pt)
BR (1) BRPI0907844B8 (pt)
CA (1) CA2716320C (pt)
ES (1) ES2488990T3 (pt)
MX (1) MX2010009162A (pt)
WO (1) WO2009105214A2 (pt)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
PL2568806T3 (pl) 2010-05-12 2017-03-31 Radius Health, Inc. Schematy lecznicze
US20130231385A1 (en) * 2010-05-28 2013-09-05 The Board Of Regents Of The University Of Texas Systems Oligo-benzamide compounds and their use
US8642632B2 (en) * 2010-07-02 2014-02-04 Radius Health, Inc. Selective androgen receptor modulators
FI20105806A0 (fi) * 2010-07-15 2010-07-15 Medeia Therapeutics Ltd Uudet aryyliamidijohdannaiset, joilla on antiandrogeenisia ominaisuuksia
AU2011312490B2 (en) 2010-09-28 2015-06-25 Radius Pharmaceuticals, Inc. Selective androgen receptor modulators
WO2013042782A1 (ja) 2011-09-22 2013-03-28 武田薬品工業株式会社 縮合複素環化合物
AR088082A1 (es) 2011-10-13 2014-05-07 Lilly Co Eli Moduladores selectivos del receptor androgeno
MY176727A (en) * 2012-12-03 2020-08-20 Pfizer Selective androgen receptor modulators
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
ES2864079T3 (es) * 2014-05-30 2021-10-13 Pfizer Derivados de carbonitrilo como moduladores selectivos del receptor de andrógenos
WO2017223115A1 (en) * 2016-06-22 2017-12-28 Radius Health, Inc. Ar+ breast cancer treatment methods
DE112017003415T5 (de) 2016-07-07 2019-03-28 Mark, S. Stern Dornfortsatz-laminaklemmvorrichtung
EP3565542B1 (en) 2017-01-05 2024-04-10 Radius Pharmaceuticals, Inc. Polymorphic forms of rad1901-2hcl
WO2019055687A1 (en) 2017-09-13 2019-03-21 Ohio State Innovation Foundation METHODS AND COMPOSITIONS FOR THE TREATMENT OF CANCER CACHEXIA
SG11202013177WA (en) 2018-07-04 2021-01-28 Radius Pharmaceuticals Inc Polymorphic forms of rad 1901-2hcl
US12441745B2 (en) 2019-02-12 2025-10-14 Radius Pharmaceuticals, Inc. Processes and compounds
US11555378B2 (en) * 2020-04-14 2023-01-17 Exxonmobil Upstream Research Company Self-destructible frac ball enclosed within a destructible ball retainer
HRP20251564T1 (hr) 2022-05-19 2026-01-30 Astrazeneca Ab Amidni heteroaromatski spojevi korisni u liječenju bolesti jetre
CN115232039B (zh) * 2022-09-21 2023-01-13 启农生物科技(北京)有限公司 一种3-甲基-2-氯-4-甲基磺酰基苯甲酸甲酯的制备方法

Family Cites Families (83)

* 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
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.
US5411981A (en) 1991-01-09 1995-05-02 Roussel Uclaf Phenylimidazolidines having antiandrogenic activity
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
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
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
GB0324551D0 (en) 2003-10-21 2003-11-26 Karobio Ab Novel compounds
US20050124625A1 (en) 2003-10-21 2005-06-09 Salvati Mark E. Piperazine derivatives and their use as modulators of nuclear hormone receptor function
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
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
US7820702B2 (en) 2004-02-04 2010-10-26 Bristol-Myers Squibb Company Sulfonylpyrrolidine modulators of androgen receptor function and method
ES2523017T3 (es) 2004-03-03 2014-11-20 Glaxosmithkline Llc Derivados de anilina como moduladores selectivos de los receptores de andrógenos
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
US7696241B2 (en) 2004-03-04 2010-04-13 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
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
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
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
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
US8642632B2 (en) 2010-07-02 2014-02-04 Radius Health, Inc. Selective androgen receptor modulators

Also Published As

Publication number Publication date
US20110224267A1 (en) 2011-09-15
EP2260028B1 (en) 2014-05-07
EP2260028A2 (en) 2010-12-15
US8455525B2 (en) 2013-06-04
MX2010009162A (es) 2010-12-21
WO2009105214A2 (en) 2009-08-27
AU2009215843B2 (en) 2011-09-08
ES2488990T3 (es) 2014-09-01
US8067448B2 (en) 2011-11-29
AU2009215843A1 (en) 2009-08-27
US20090253758A1 (en) 2009-10-08
BRPI0907844B1 (pt) 2020-08-18
JP5308458B2 (ja) 2013-10-09
CA2716320C (en) 2014-01-28
BRPI0907844A2 (pt) 2018-01-30
WO2009105214A3 (en) 2009-10-15
CA2716320A1 (en) 2009-08-27
JP2011513219A (ja) 2011-04-28

Similar Documents

Publication Publication Date Title
BR112012019551A2 (pt) moduladores seletivos do receptor de androgênio.
BR112013007685A2 (pt) aplicações relacionadas com moduladores de receptor anfrógeno seletivos
BRPI0908353B8 (pt) composto ou um sal farmaceuticamente aceitavel do mesmo e composição farmaceutica
WO2009105214A3 (en) Selective androgen receptor modulators
BRPI0508820B8 (pt) compostos moduladores de receptor de opióide e composição que os compreende
BR112015000578A2 (pt) moduladores da via do complemento e usos dos mesmos
BR112015014592A2 (pt) composto, composição farmacêutica, e, método para o tratamento de um humano
BR112015022096A8 (pt) compostos moduladores de canal de sódio, composição que os compreende e uso dos mesmos
WO2010118287A8 (en) Selective androgen receptor modulators
BRPI0818533B8 (pt) composto, composição farmacêutica, uso de um composto, e, processo para a preparação de um composto
BRPI0719092B8 (pt) compostos do tipo tetra-hidrociclopen-ta[b]indol, seus usos, e composição farmacêutica
EA025086B9 (ru) Производные индоламида и родственные соединения для использования при лечении нейродегенеративных заболеваний
BRPI0511072B8 (pt) compostos derivados de alquinila como moduladores dos receptores de glutamato metabotróbico, seus usos e suas composições farmacêuticas
BR112014031375A2 (pt) moduladores da série de reação complementar e usos dos mesmos
BR112014029868A2 (pt) compostos, e, composição farmacêutica
BR112015014585A2 (pt) composto, composição farmacêutica, e, método de tratamento de um ser humano
BRPI0805826A2 (pt) compostos espiro-substituìdos como inibidores de angiogênese, método de produção de um composto, composição farmacêutica e métodos de tratamento
BRPI0507481A (pt) composto, composição farmacêutica, uso do composto, e, métodos para tratar distúrbios mediados por mglur 5 e para inibir ativação de receptores de mglur 5
BR112014009717A2 (pt) "derivados de 2-(fenil ou pirid-3-il)aminopirimidina, seus usos, e composição farmacêutica"
EA201071244A1 (ru) Новые терапевтические подходы в лечении болезни альцгеймера и обусловленных ею расстройств посредством модуляции ангиогенеза
NO20082124L (no) Bifenyloksyeddiksyrederivater for behandling av respiratorisk sykdom
BR112012009376B8 (pt) composição farmacêutica sólida compreendendo um inibidor de sglt-2 e sua forma de dosagem farmacêutica
BRPI0517263A (pt) novos derivados de sulfonamida como moduladores do receptor de glicocorticóide para o tratamento de doenças inflamatórias
BRPI0612287A8 (pt) composição para uso farmacêutico no tratamento de doenças através da medicina nuclear e métodos de uso e para modulação de atividade de receptor nuclear
BRPI0606930A2 (pt) composto ou um sal farmaceuticamente aceitável do mesmo, processo para preparar um composto ou um sal farmaceuticamente aceitável do mesmo, composição farmacêutica, uso de um composto ou de um sal farmaceuticamente aceitável do mesmo, e, métodos para a produção de um efeito de inibição de b-raf em um animal de sangue quente, para a produção de um efeito anti-cáncer em um animal de sangue quente e para o tratamento de doenças de um animal em um animal de sangue quente

Legal Events

Date Code Title Description
B25G Requested change of headquarter approved

Owner name: RADIUS HEALTH, INC (US)

B25A Requested transfer of rights approved

Owner name: RADIUS PHARMACEUTICALS, INC. (US)

B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]

Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS.

B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B06U Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 10 (DEZ) ANOS CONTADOS A PARTIR DE 18/08/2020, OBSERVADAS AS CONDICOES LEGAIS.

B16C Correction of notification of the grant [chapter 16.3 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 19/02/2009 OBSERVADAS AS CONDICOES LEGAIS. PATENTE CONCEDIDA CONFORME ADI 5.529/DF

B25G Requested change of headquarter approved

Owner name: RADIUS PHARMACEUTICALS, INC. (US)

B25A Requested transfer of rights approved

Owner name: ELLIPSES PHARMA LTD (GB)