MA29613B1 - Antiandrogenes non-steroidiens a affinite pour le helix 12 - Google Patents

Antiandrogenes non-steroidiens a affinite pour le helix 12

Info

Publication number
MA29613B1
MA29613B1 MA30549A MA30549A MA29613B1 MA 29613 B1 MA29613 B1 MA 29613B1 MA 30549 A MA30549 A MA 30549A MA 30549 A MA30549 A MA 30549A MA 29613 B1 MA29613 B1 MA 29613B1
Authority
MA
Morocco
Prior art keywords
steroidian
antiandrogenes
helix
affinity
compounds
Prior art date
Application number
MA30549A
Other languages
English (en)
Inventor
Fernand Labrie
Rock Breton
Shankar Mohan Singh
Rene Maltais
Original Assignee
Endorech 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 Endorech Inc filed Critical Endorech Inc
Publication of MA29613B1 publication Critical patent/MA29613B1/fr

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms
    • C07D207/36—Oxygen or sulfur atoms
    • C07D207/40—2,5-Pyrrolidine-diones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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 ring carbon atoms
    • C07D233/30—Oxygen or sulfur atoms
    • C07D233/42—Sulfur atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4166—1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • 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
    • 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
    • A61P19/08—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
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/28—Antiandrogens
    • 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
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms
    • C07D211/40—Oxygen atoms
    • C07D211/44—Oxygen atoms attached in position 4
    • C07D211/48—Oxygen atoms attached in position 4 having an acyclic carbon atom attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms
    • C07D233/72—Two oxygen atoms, e.g. hydantoin
    • C07D233/74—Two oxygen atoms, e.g. hydantoin with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to other ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms
    • C07D233/86—Oxygen and sulfur atoms, e.g. thiohydantoin
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Neurology (AREA)
  • Reproductive Health (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Pregnancy & Childbirth (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Cosmetics (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyrrole Compounds (AREA)

Abstract

L'invention porte sur des composés de structure suivante et sur leurs sels, utilisés pour traiter ou réduire la probabilité d'acquérir des maladies dépendantes des androgènes telles que: le cancer de la prostate, l'hyperplasie bénigne de la prostate, le syndrome des ovaires polykystiques, l'acné, l'hirsutisme, la séborrhée, l'alopécie androgène et la calvitie masculine. Lesdits composés peuvent être associés à des diluants ou excipients pharmacocompatibles, ou autrement produits en tant que formes posologiques. On peut également prévoir leur combinaison avec d'autres principes pharmaceutiques actifs.
MA30549A 2005-06-17 2008-01-07 Antiandrogenes non-steroidiens a affinite pour le helix 12 MA29613B1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US69139105P 2005-06-17 2005-06-17
US11/452,545 US7709516B2 (en) 2005-06-17 2006-06-14 Helix 12 directed non-steroidal antiandrogens

Publications (1)

Publication Number Publication Date
MA29613B1 true MA29613B1 (fr) 2008-07-01

Family

ID=37531932

Family Applications (1)

Application Number Title Priority Date Filing Date
MA30549A MA29613B1 (fr) 2005-06-17 2008-01-07 Antiandrogenes non-steroidiens a affinite pour le helix 12

Country Status (24)

Country Link
US (2) US7709516B2 (fr)
EP (1) EP1899305B1 (fr)
JP (2) JP5069229B2 (fr)
KR (1) KR101036670B1 (fr)
CN (1) CN101243052B (fr)
AP (1) AP2621A (fr)
AU (1) AU2006257678B2 (fr)
BR (1) BRPI0611828B8 (fr)
CA (1) CA2612398C (fr)
EA (1) EA016382B1 (fr)
GE (1) GEP20125397B (fr)
HR (1) HRP20070567B1 (fr)
IL (1) IL188152A (fr)
MA (1) MA29613B1 (fr)
MX (1) MX2007016145A (fr)
MY (1) MY148146A (fr)
NO (1) NO342354B1 (fr)
NZ (1) NZ564466A (fr)
PH (1) PH12011501683B1 (fr)
RS (1) RS20070489A (fr)
SG (1) SG162763A1 (fr)
TN (1) TNSN07473A1 (fr)
TW (1) TWI394571B (fr)
WO (1) WO2006133567A1 (fr)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2495383A1 (fr) * 2002-08-12 2004-02-26 Takeda Pharmaceutical Company Limited Derive de benzene a cycles accoles et son utilisation
CA2551737C (fr) 2004-01-07 2009-11-10 Endorecherche, Inc. Produits pharmaceutiques steroidiens diriges sur l'helice 12
CN102357248A (zh) 2004-10-20 2012-02-22 恩多研究公司 单独的性甾体前体或与选择性雌激素受体调节剂联合用于防治绝经后女性的阴道疾病和病症
US7709516B2 (en) 2005-06-17 2010-05-04 Endorecherche, Inc. Helix 12 directed non-steroidal antiandrogens
US9284345B2 (en) * 2007-04-12 2016-03-15 Endorecherche, Inc. 17alpha-substituted steroids as systemic antiandrogens and selective androgen receptor modulators
US8268806B2 (en) 2007-08-10 2012-09-18 Endorecherche, Inc. Pharmaceutical compositions
US8067448B2 (en) 2008-02-22 2011-11-29 Radius Health, Inc. Selective androgen receptor modulators
US8268872B2 (en) * 2008-02-22 2012-09-18 Radius Health, Inc. Selective androgen receptor modulators
WO2011029392A1 (fr) 2009-09-10 2011-03-17 Youzhi Tong Antagonistes du récepteur des androgènes et leurs utilisations
TW201111378A (en) 2009-09-11 2011-04-01 Bayer Schering Pharma Ag Substituted (heteroarylmethyl) thiohydantoins
AR078793A1 (es) 2009-10-27 2011-12-07 Orion Corp Derivados de carboxamidas no esteroidales y acil hidrazona moduladores de receptores androgenicos de tejido selectivo (sarm), composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento del cancer de prostata entre otros
JP5897783B2 (ja) * 2009-12-24 2016-03-30 株式会社ロッテ 抗アンドロゲン剤及び皮脂分泌抑制剤
CA2788907A1 (fr) 2010-02-04 2011-08-11 Radius Health, Inc. Modulateurs selectifs du recepteur des androgenes
WO2011143469A1 (fr) 2010-05-12 2011-11-17 Radius Health,Inc Schémas thérapeutiques
US8642632B2 (en) 2010-07-02 2014-02-04 Radius Health, Inc. Selective androgen receptor modulators
EP2590969B1 (fr) 2010-07-06 2014-10-15 AstraZeneca AB Agents thérapeutiques 976
WO2012050868A1 (fr) * 2010-09-28 2012-04-19 Georgia Tech Research Corporation Inhibiteurs d'histone désacétylase (hdac) ciblant les tumeurs de la prostate et procédés pour les préparer et les utiliser
ES2550319T3 (es) 2010-09-28 2015-11-06 Radius Health, Inc Moduladores selectivos del receptor de andrógenos
CA2829322C (fr) 2011-03-10 2017-01-10 Suzhou Kintor Pharmaceuticals, Inc. Antagonistes de recepteur d'androgene thioimidazolidinone substitues et leurs utilisations
MX360611B (es) 2011-04-21 2018-11-09 Orion Corp Carboxamidas que modulan el receptor de andrógeno.
EP2565186A1 (fr) 2011-09-02 2013-03-06 Hybrigenics S.A. Inhibiteurs sélectifs et réversibles de la protéase 7 spécifique de l'ubiquitine
US9682960B2 (en) * 2013-12-19 2017-06-20 Endorecherche, Inc. Non-steroidal antiandrogens and selective androgen receptor modulators with a pyridyl moiety
ITUB20151256A1 (it) 2015-05-28 2016-11-28 Olon Spa Processo industriale per la preparazione di enzalutamide
EP4066827A1 (fr) 2016-06-22 2022-10-05 Ellipses Pharma Ltd Méthodes de traitement du cancer du sein ar+
US11292782B2 (en) 2018-11-30 2022-04-05 Nuvation Bio Inc. Diarylhydantoin compounds and methods of use thereof
US11034669B2 (en) 2018-11-30 2021-06-15 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
CN115181043B (zh) * 2022-07-27 2024-05-07 爱斯特（成都）生物制药股份有限公司 一种连续流制备4-异硫氰基-2-(三氟甲基)苯甲腈的方法

Family Cites Families (76)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3085005A (en) 1958-01-16 1963-04-09 Fansteel Metallurgical Corp Alloys
US3277094A (en) * 1965-05-10 1966-10-04 Ciba Geigy Corp Piperazine derivatives
US3797494A (en) 1969-04-01 1974-03-19 Alza Corp Bandage for the administration of drug by controlled metering through microporous materials
US3742951A (en) 1971-08-09 1973-07-03 Alza Corp Bandage for controlled release of vasodilators
US4191775A (en) 1977-12-15 1980-03-04 Imperial Chemical Industries Limited Amide derivatives
JPS5629581A (en) * 1979-08-20 1981-03-24 Otsuka Pharmaceut Co Ltd 4-phenylpiperazinyl alkoxy anilide derivative
JPS56115769A (en) * 1980-02-18 1981-09-11 Tanabe Seiyaku Co Ltd Piperazine derivative and its preparation
DE3101502A1 (de) * 1981-01-19 1982-08-26 Basf Ag, 6700 Ludwigshafen Phenylpiperazinderivate von hetarylphenolen und hetarylanilinen, ihre hersttellung und diese enthaltendetherapeutische mittel
JPS57176910A (en) * 1981-04-24 1982-10-30 Tanabe Seiyaku Co Ltd Medicinal composition
JPS58159413A (ja) * 1982-03-17 1983-09-21 Mitsubishi Chem Ind Ltd 中枢神経抑制剤
ATE28864T1 (de) 1982-07-23 1987-08-15 Ici Plc Amide-derivate.
DE3333240A1 (de) 1983-09-12 1985-03-28 Schering AG, 1000 Berlin und 4709 Bergkamen Mittel zur transdermalen applikation von arzneimittelwirkstoffen
US4568343A (en) 1984-10-09 1986-02-04 Alza Corporation Skin permeation enhancer compositions
EP0254341B1 (fr) 1986-07-23 1990-01-03 Akzo N.V. Dérivés de 18-phényl estranes
WO1988003136A1 (fr) * 1986-10-27 1988-05-05 Yoshitomi Pharmaceutical Industries, Ltd. Composes de piperazine et leur utilisation medicinale
US4816258A (en) 1987-02-26 1989-03-28 Alza Corporation Transdermal contraceptive formulations
JP2549396B2 (ja) * 1987-10-19 1996-10-30 吉富製薬株式会社 フェニルピペラジン化合物
US5064654A (en) 1989-01-11 1991-11-12 Ciba-Geigy Corporation Mixed solvent mutually enhanced transdermal therapeutic system
DE69009785T2 (de) * 1989-02-10 1994-11-03 Otsuka Pharma Co Ltd Carbostyrilderivate.
US5071644A (en) 1990-08-07 1991-12-10 Mediventures, Inc. Topical drug delivery with thermo-irreversible gels
US5411981A (en) 1991-01-09 1995-05-02 Roussel Uclaf Phenylimidazolidines having antiandrogenic activity
FR2671348B1 (fr) 1991-01-09 1993-03-26 Roussel Uclaf Nouvelles phenylimidazolidines, leur procede de preparation, leur application comme medicaments et les compositions pharmaceutiques les renfermant.
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.
JPH05255291A (ja) * 1992-03-11 1993-10-05 Ajinomoto Co Inc ピペラジン誘導体
FR2694290B1 (fr) 1992-07-08 1994-09-02 Roussel Uclaf Nouvelles phénylimidazolidines éventuellement substituées, leur procédé de préparation, leur application comme médicaments et les compositions pharmaceutiques les renfermant.
JPH06345714A (ja) * 1993-06-11 1994-12-20 Taiho Yakuhin Kogyo Kk ウレア誘導体及びその塩
JPH07138258A (ja) * 1993-11-16 1995-05-30 Taiho Yakuhin Kogyo Kk チアゾリジンジオン誘導体又はその塩
TW521073B (en) 1994-01-05 2003-02-21 Hoechst Marion Roussel Inc New optionally substituted phenylimidazolidines, their preparation process, their use as anti-androgenic agent and the pharmaceutical compositions containing them
DE69531998T2 (de) 1994-12-22 2004-07-22 Ligand Pharmaceuticals, Inc., San Diego Steroidrezeptor-modulator verbindungen und methoden
US5656651A (en) 1995-06-16 1997-08-12 Biophysica Inc. Androgenic directed compositions
JPH09136877A (ja) * 1995-06-16 1997-05-27 Takeda Chem Ind Ltd 複素環化合物、その製造法及び用途
AT828U1 (de) * 1995-06-16 1996-06-25 Kaestle Ag Ski
FR2741342B1 (fr) 1995-11-22 1998-02-06 Roussel Uclaf Nouvelles phenylimidazolidines fluorees ou hydroxylees, procede, intermediaires de preparation, application comme medicaments, nouvelle utilisation et compositions pharmaceutiques
FR2742749B1 (fr) 1995-12-22 1998-02-06 Roussel Uclaf Nouvelles phenylimidazolidines comportant notamment un radical nitrooxy ou carbonyloxy, procede et intermediaires de preparation, application comme medicaments, nouvelles utilisations et compositions pharmaceutiques
US6071957A (en) 1996-11-27 2000-06-06 The University Of Tennessee Research Corporation Irreversible non-steroidal antagonist compound and its use in the treatment of prostate cancer
US7759520B2 (en) 1996-11-27 2010-07-20 University Of Tennessee Research Foundation Synthesis of selective androgen receptor modulators
WO1998053826A1 (fr) 1997-05-30 1998-12-03 The University Of Tennessee Research Corporation Composes agonistes non steroidiens et leur utilisation dans le cadre de therapies a base d'hormones males
EP1094798A2 (fr) 1998-03-11 2001-05-02 Endorecherche Inc. INHIBITEURS DE LA 17beta-HYDROXYSTEROIDE DESHYDROGENASE DU TYPE 5 ET DU TYPE 3 ET METHODES D'UTILISATION ASSOCIEES
CN1305470A (zh) * 1998-04-10 2001-07-25 日本烟草产业株式会社 脒化合物
US6184249B1 (en) 1998-12-18 2001-02-06 Biophysica, Inc. Androgen receptor suppressors in the therapy and diagnosis of prostate cancer, alopecia and other hyper-androgenic syndromes
US6472415B1 (en) * 1998-12-18 2002-10-29 Biophysica, Inc. Androgen receptor suppressors in the therapy and diagnosis of prostate cancer, alopecia and other hyper-androgenic syndromes
AU6941200A (en) 1999-08-27 2001-03-26 Ligand Pharmaceuticals Incorporated 8-substituted-6-trifluoromethyl-9-pyrido(3,2-g)quinoline compounds as androgen receptor modulators
US6566372B1 (en) 1999-08-27 2003-05-20 Ligand Pharmaceuticals Incorporated Bicyclic androgen and progesterone receptor modulator compounds and methods
JP2001072660A (ja) * 1999-09-08 2001-03-21 Welfide Corp ＴＮＦ−α産生抑制剤および／またはＩＬ−１０産生促進剤
US20040077605A1 (en) 2001-06-20 2004-04-22 Salvati Mark E. Fused heterocyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function
AU2001288213B2 (en) 2000-06-28 2005-04-14 Bristol-Myers Squibb Company Selective androgen receptor modulators and methods for their identification, design and use
US7001911B2 (en) 2000-06-28 2006-02-21 Bristol-Myers Squibb Company Fused cyclic modulators of nuclear hormone receptor function
HUP0301657A3 (en) * 2000-07-07 2010-01-28 Eisai R & D Man Co Fungal cell wall synthesis gene
JP2002088073A (ja) 2000-09-08 2002-03-27 Yamanouchi Pharmaceut Co Ltd 抗アンドロゲン剤
GEP20074144B (en) 2000-09-19 2007-07-10 Bristol Myers Squibb Co Fused heterocyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function
IL158454A0 (en) * 2001-05-11 2004-05-12 Pharmacia Corp Aromatic sulfone hydroxamates and their use as protease inhibitors
NZ530810A (en) 2001-09-06 2006-05-26 Schering Corp 17beta-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases
US6861432B2 (en) * 2001-11-23 2005-03-01 Schering Aktiengesellschaft Piperazine derivatives that destabilize androgen receptors
DE60309667D1 (de) 2002-02-15 2006-12-28 Endorech Inc Biphenylderivate und ihre verwendung als antiandrogene
US7803970B2 (en) 2002-02-28 2010-09-28 University Of Tennessee Research Foundation Multi-substitued selective androgen receptor modulators and methods of use thereof
US6875438B2 (en) * 2002-04-27 2005-04-05 Aventis Pharma Deutschland Gmbh Preparations for topical administration of substances having antiandrogenic activity
TW200407324A (en) 2002-05-17 2004-05-16 Bristol Myers Squibb Co Bicyclic modulators of androgen receptor function
FR2850652B1 (fr) * 2003-01-31 2008-05-30 Aventis Pharma Sa Nouveaux derives d'uree cyclique, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de kinases
WO2004078114A2 (fr) * 2003-02-28 2004-09-16 Encysive Pharmaceuticals Inc. Pyridine, pyrimidine, quinoline, quinazoline et naphtalene, antagonistes du recepteur de l'urotensine ii
BRPI0409227C1 (pt) 2003-04-07 2021-05-25 Axys Pharm Inc composto, composição farmacêutica, uso de um composto e processo para a preparação de um composto de fórmula (i)
DE10322108B4 (de) 2003-05-09 2008-12-11 Bayer Schering Pharma Aktiengesellschaft Antiandrogene Pyrrolidine mit tumorhemmender Wirksamkeit
WO2004103971A1 (fr) 2003-05-21 2004-12-02 Aska Pharmaceutical Co., Ltd. Derive de sulfamate d'aminophenyle cyclique
US7271188B2 (en) 2003-06-12 2007-09-18 Chugai Seikayu Kabushiki Kaisha Imidazolidine derivatives
CN1835937B (zh) 2003-06-13 2012-07-18 詹森药业有限公司 作为选择性雄激素受体调节剂(sarms)的噻唑啉衍生物
SE525459C2 (sv) 2003-06-30 2005-02-22 Delaval Holding Ab Mjölkningsanordning och förfarande för hantering av en mjölkningsanordning
WO2005034856A2 (fr) * 2003-09-05 2005-04-21 The Regents Of The University Of Colorado Conjugues cibles medicament-formaldehyde et procedes de fabrication associes
US20050124625A1 (en) 2003-10-21 2005-06-09 Salvati Mark E. Piperazine derivatives and their use as modulators of nuclear hormone receptor function
KR100851802B1 (ko) * 2003-10-31 2008-08-13 오쓰까 세이야꾸 가부시키가이샤 결핵의 치료를 위한2,3-디히드로-6-니트로이미다조[2,1-ｂ]옥사졸 화합물
US7256208B2 (en) 2003-11-13 2007-08-14 Bristol-Myers Squibb Company Monocyclic N-Aryl hydantoin modulators of androgen receptor function
CA2551737C (fr) 2004-01-07 2009-11-10 Endorecherche, Inc. Produits pharmaceutiques steroidiens diriges sur l'helice 12
WO2005111042A1 (fr) 2004-05-03 2005-11-24 Janssen Pharmaceutica N.V. Nouveaux dérivés d'indole agissant comme modulateurs de récepteurs androgènes sélectifs (sarm)
ZA200610270B (en) 2004-05-17 2008-06-25 Acadia Pharm Inc Androgen receptor modulators and method of treating disease using the same
DK2289872T3 (en) 2004-06-07 2017-10-09 Univ Tennessee Res Found Medical use of a selective androgen receptor modulator
CA2579514A1 (fr) 2004-09-10 2006-03-23 Janssen Pharmaceutica N.V. Derives d'imidazolidine-2-one en tant que modulateurs selectifs du recepteur androgenique
WO2006038594A1 (fr) * 2004-10-04 2006-04-13 Ono Pharmaceutical Co., Ltd. Inhibiteur de canal de calcium de type n
US7709516B2 (en) 2005-06-17 2010-05-04 Endorecherche, Inc. Helix 12 directed non-steroidal antiandrogens

Also Published As

Publication number Publication date
IL188152A0 (en) 2008-03-20
TNSN07473A1 (en) 2009-03-17
KR101036670B1 (ko) 2011-05-25
JP2008543792A (ja) 2008-12-04
EP1899305A4 (fr) 2010-05-12
EA200800067A1 (ru) 2008-04-28
GEP20125397B (en) 2012-02-27
CA2612398A1 (fr) 2006-12-21
BRPI0611828B1 (pt) 2020-11-17
BRPI0611828A2 (pt) 2010-09-28
EP1899305B1 (fr) 2018-12-12
US8168627B2 (en) 2012-05-01
NO342354B1 (no) 2018-05-14
JP2012176988A (ja) 2012-09-13
NZ564466A (en) 2011-01-28
US7709516B2 (en) 2010-05-04
AU2006257678A1 (en) 2006-12-21
TWI394571B (zh) 2013-05-01
WO2006133567A1 (fr) 2006-12-21
AU2006257678B2 (en) 2010-06-03
IL188152A (en) 2016-12-29
US20060287327A1 (en) 2006-12-21
CN101243052A (zh) 2008-08-13
HRP20070567B1 (hr) 2019-11-01
AP2007004276A0 (en) 2007-12-31
HRP20070567A2 (en) 2008-05-31
RS20070489A (en) 2009-01-22
PH12011501683A1 (en) 2015-03-16
EA016382B1 (ru) 2012-04-30
PH12011501683B1 (en) 2015-03-16
TW200727901A (en) 2007-08-01
US20100227855A1 (en) 2010-09-09
NO20080143L (no) 2008-03-07
BRPI0611828B8 (pt) 2021-05-25
AP2621A (en) 2013-03-19
MY148146A (en) 2013-03-15
CN101243052B (zh) 2012-05-30
JP5069229B2 (ja) 2012-11-07
EP1899305A1 (fr) 2008-03-19
CA2612398C (fr) 2011-08-09
KR20080033277A (ko) 2008-04-16
SG162763A1 (en) 2010-07-29
MX2007016145A (es) 2008-03-10

Similar Documents

Publication Publication Date Title
MA29613B1 (fr) Antiandrogenes non-steroidiens a affinite pour le helix 12
MY157898A (en) Helix 12 directed steroidal pharmaceutical products
BR0213452A (pt) Derivados de piperazina com atividade antagonista receptora de ccr1
BR0317572A (pt) Benzoxazinas e seus derivados como inibidores de pi3ks
TNSN01130A1 (fr) Formulations a liberation prolongee pour des secretagogues d'hormone de croissance
MA30784B1 (fr) Derives phenyliques et utilisation de ceux-ci en tant qu'immunomodulateurs.
ATE355278T1 (de) Isochinolinon derivate als parp inhibitoren
MA29378B1 (fr) Composition pharmaceutique comprenant une diphenyluree substituee par un omega-carboxyaryle pour le traitement du cancer
ATE447970T1 (de) Mittel zur behandlung von harnwegserkrankungen, umfassend mittel zur kontrolle des lpa-rezeptors
BRPI0508125A (pt) formulação de alcalóide, método para melhorar a eficácia de um alcalóide, uso do produto da reação de um ou mais alcalóides com um mais derivados de fosfato de um ou mais agentes de transferência de elétrons, junto com excipientes e composição farmacêutica
PE20011167A1 (es) Composiciones farmaceuticas que comprenden un antagonista del alfa-adrenoreceptor y un antagonista muscarinico para el tratamiento de hiperplasia prostatica benigna
MA29775B1 (fr) Derives de pyrazolone
WO2006104870A3 (fr) Methodes de traitement d'hyperplasie prostatique benigne ou de symptomes des voies urinaires inferieures faisant appel a des inhibiteurs de pde 5
WO2004064736A3 (fr) Traitement de l'hyperplasie benigne de la prostate au moyen d'agents energolytiques
BRPI0520503A2 (pt) composições antiinflamatórias e métodos de uso
Zomorodi et al. Diazepam–omeprazole inhibition interaction: an in vitro investigation using human liver microsomes
BR0115865A (pt) Derivados de piperazina 1,4-di-substituìda utilizáveis como bloqueadores de receptores adrenérgicos alfa1 uro-seletivos
WO2006031719A3 (fr) Composes de 1,4-bis-n-oxyde-5,8-dihydroxyanthracenedione et leur utilisation
ATE198274T1 (de) 17 beta-aryl-4-aza-steroidderivate
PT1206444E (pt) Compostos que inibem a actividade da triptase
BR0213357A (pt) Compostos orgânicos
BR0211121A (pt) Composto, métodos para o tratamento ou prevenção de doenças e para fabricar um composto, intermediário, e, uso de um composto ou sal
DK1345907T3 (da) 7-Heterocyclyl-quinolin- og thieno-2,3-B-pyridin-derivater anvendelige som antagonister af gonadotropin-frigörende hormon
UA97786C2 (ru) Нестероидные антиандрогены, направленные на 12-спираль рецептора антиандрогенов
WO2007029078A3 (fr) Derives de succinimide et de glutarimide comme antagonistes de recepteurs adrenergiques