CA1249823A - Acylanilides having antiandrogenic properties - Google Patents

Acylanilides having antiandrogenic properties

Info

Publication number
CA1249823A
CA1249823A CA000432811A CA432811A CA1249823A CA 1249823 A CA1249823 A CA 1249823A CA 000432811 A CA000432811 A CA 000432811A CA 432811 A CA432811 A CA 432811A CA 1249823 A CA1249823 A CA 1249823A
Authority
CA
Canada
Prior art keywords
hydroxy
trifluoromethyl
aniline
acylanilide
cyano
Prior art date
Legal status (The legal status 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 status listed.)
Expired
Application number
CA000432811A
Other languages
English (en)
French (fr)
Inventor
Howard Tucker
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
AstraZeneca UK Ltd
Original Assignee
Imperial Chemical Industries Ltd
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=10531878&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CA1249823(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Imperial Chemical Industries Ltd filed Critical Imperial Chemical Industries Ltd
Application granted granted Critical
Publication of CA1249823A publication Critical patent/CA1249823A/en
Expired legal-status Critical Current

Links

Classifications

    • 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
    • C07D285/125—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C321/00—Thiols, sulfides, hydropolysulfides or polysulfides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/40—Unsaturated compounds
    • C07C59/58—Unsaturated compounds containing ether groups, groups, groups, or groups
    • C07C59/64—Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings
    • C07C59/66—Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings the non-carboxylic part of the ether containing six-membered aromatic rings
    • C07C59/68—Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings the non-carboxylic part of the ether containing six-membered aromatic rings the oxygen atom of the ether group being bound to a non-condensed six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/70—Sulfur atoms
    • 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
    • C07D233/84—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/38—One sulfur atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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
    • C07D277/36—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D303/00—Compounds containing three-membered rings having one oxygen atom as the only ring hetero atom
    • C07D303/02—Compounds containing oxirane rings
    • C07D303/48—Compounds containing oxirane rings with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/62—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes 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 hetero ring

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (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)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Dermatology (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Polysaccharides And Polysaccharide Derivatives (AREA)
  • Addition Polymer Or Copolymer, Post-Treatments, Or Chemical Modifications (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Cosmetics (AREA)
CA000432811A 1982-07-23 1983-07-20 Acylanilides having antiandrogenic properties Expired CA1249823A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB8221421 1982-07-23
GB8221421 1982-07-23

Publications (1)

Publication Number Publication Date
CA1249823A true CA1249823A (en) 1989-02-07

Family

ID=10531878

Family Applications (1)

Application Number Title Priority Date Filing Date
CA000432811A Expired CA1249823A (en) 1982-07-23 1983-07-20 Acylanilides having antiandrogenic properties

Country Status (23)

Country Link
US (1) US4636505A (cg-RX-API-DMAC7.html)
EP (1) EP0100172B1 (cg-RX-API-DMAC7.html)
JP (2) JPS5933250A (cg-RX-API-DMAC7.html)
AT (1) ATE28864T1 (cg-RX-API-DMAC7.html)
AU (1) AU556328B2 (cg-RX-API-DMAC7.html)
CA (1) CA1249823A (cg-RX-API-DMAC7.html)
CS (1) CS399991A3 (cg-RX-API-DMAC7.html)
DE (1) DE3372965D1 (cg-RX-API-DMAC7.html)
DK (1) DK322783D0 (cg-RX-API-DMAC7.html)
ES (4) ES524392A0 (cg-RX-API-DMAC7.html)
FI (1) FI83770C (cg-RX-API-DMAC7.html)
GR (1) GR79232B (cg-RX-API-DMAC7.html)
HK (1) HK92690A (cg-RX-API-DMAC7.html)
HU (1) HU191296B (cg-RX-API-DMAC7.html)
IE (1) IE55941B1 (cg-RX-API-DMAC7.html)
IL (1) IL69217A (cg-RX-API-DMAC7.html)
LU (1) LU88769I2 (cg-RX-API-DMAC7.html)
MX (1) MX9203451A (cg-RX-API-DMAC7.html)
NL (1) NL950029I2 (cg-RX-API-DMAC7.html)
NO (2) NO164974C (cg-RX-API-DMAC7.html)
NZ (1) NZ204995A (cg-RX-API-DMAC7.html)
PT (1) PT77087B (cg-RX-API-DMAC7.html)
ZA (1) ZA835182B (cg-RX-API-DMAC7.html)

Families Citing this family (311)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS54115075A (en) * 1978-02-28 1979-09-07 Cho Lsi Gijutsu Kenkyu Kumiai Plasma etching method
FR2540495B1 (fr) * 1983-02-07 1986-02-14 Roussel Uclaf Nouveaux derives de o-mercaptopropanamide et de ses homologues, leur procede de preparation, leur application comme medicaments, les compositions les renfermant et les nouveaux intermediaires obtenus
GB8617652D0 (en) * 1986-07-18 1986-08-28 Ici Plc Acylanilide derivatives
GB8617653D0 (en) * 1986-07-18 1986-08-28 Ici Plc Amide derivatives
US4921941A (en) * 1987-07-01 1990-05-01 Schering Corporation Orally active antiandrogens
US4970303A (en) * 1988-02-03 1990-11-13 Xoma Corporation Linking agents and methods
US4895715A (en) * 1988-04-14 1990-01-23 Schering Corporation Method of treating gynecomastia
US5204337A (en) * 1988-10-31 1993-04-20 Endorecherche Inc. Estrogen nucleus derivatives for use in inhibition of sex steroid activity
US5364847A (en) * 1989-03-10 1994-11-15 Endorecherche Inhibitors of sex steroid biosynthesis and methods for their production and use
ZA924811B (en) * 1991-06-28 1993-12-29 Endorecherche Inc Controlled release systems and low dose androgens
GB9214120D0 (en) * 1991-07-25 1992-08-12 Ici Plc Therapeutic amides
GB9305295D0 (en) * 1993-03-15 1993-05-05 Zeneca Ltd Therapeutic compounds
GB9310095D0 (en) * 1993-05-17 1993-06-30 Zeneca Ltd Therapeutic compounds
EP0748220A4 (en) * 1994-01-21 1997-09-10 Sepracor Inc METHOD AND COMPOSITIONS FOR TREATING ANDROGEN-DEPENDENT DISEASES USING OPTICALLY PURE R - (-) CASODEX
DE4420777A1 (de) 1994-06-15 1995-12-21 Bayer Ag Verfahren zur Herstellung von 4-Fluorthiophenol
DE69529665T2 (de) * 1994-06-27 2004-02-19 Neutron Therapies Inc., San Diego Bor enthaltende hormonanaloga und verfahren fuer ihre verwendung zur bildlichen darstellung oder zum abtoeten von zellen, die hormonrezeptoren besitzen
US6995284B2 (en) 2000-08-24 2006-02-07 The University Of Tennessee Research Foundation Synthesis of selective androgen receptor modulators
US20090264534A1 (en) * 1996-11-27 2009-10-22 Dalton James T Selective androgen receptor modulators
US7205437B2 (en) * 1996-11-27 2007-04-17 University Of Tennessee Research Foundation Selective androgen receptor modulators
US20050038110A1 (en) * 2000-08-24 2005-02-17 Steiner Mitchell S. Selective androgen receptor modulators and methods of use thereof
US7518013B2 (en) 2000-08-24 2009-04-14 University Of Tennessee Research Foundation Selective androgen receptor modulators
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
AU7604798A (en) * 1997-05-30 1998-12-30 University Of Tennessee Research Corporation, The Non-steroidal agonist compounds and their use in male hormone therapy
AU7723198A (en) * 1997-06-04 1998-12-21 University Of Tennessee Research Corporation, The Non-steroidal radiolabeled agonist/antagonist compounds and their use in prostate cancer imaging
DE19746512A1 (de) 1997-10-22 1999-04-29 Bayer Ag Verfahren zur Herstellung von Arylmercaptanen durch Hydrierung von Diaryldisulfiden
GB9804648D0 (en) 1998-03-06 1998-04-29 Zeneca Ltd Chemical compounds
GB9805520D0 (en) 1998-03-17 1998-05-13 Zeneca Ltd Chemical compounds
US20040176470A1 (en) * 1998-05-07 2004-09-09 Steiner Mitchell S. Method for treatment and chemoprevention of prostate cancer
GB9811427D0 (en) 1998-05-29 1998-07-22 Zeneca Ltd Chemical compounds
CA2341711A1 (en) * 1998-08-28 2000-03-09 Smithkline Beecham Corporation Process for making 2-amino-5-cyanophenol
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
HU223950B1 (hu) 1999-06-10 2005-03-29 Richter Gedeon Vegyészeti Gyár Rt. Eljárás a racém, valamint az R-(-)- és S-(+)-N-[4-ciano-3-(trifluor-metil)-fenil]-3-[(4-fluor-fenil)-szulfonil]-2-hidroxi-2-metil-propánsavamid előállítására
US6566372B1 (en) * 1999-08-27 2003-05-20 Ligand Pharmaceuticals Incorporated Bicyclic androgen and progesterone receptor modulator compounds and methods
HUP0202725A3 (en) 1999-09-04 2005-04-28 Astrazeneca Ab Substituted n-phenyl 2-hydroxy-2-methyl-3,3,3-trifluoropropanamide derivatives which elevate pyruvate dehydrogenase activity, process for their preparation and pharmaceutical compositions containing them
JP2003508514A (ja) 1999-09-04 2003-03-04 アストラゼネカ アクチボラグ 化学的化合物
ES2307528T3 (es) 1999-09-04 2008-12-01 Astrazeneca Ab Amidas como inhibidores para la piruvato deshidrogenasa.
US6713454B1 (en) * 1999-09-13 2004-03-30 Nobex Corporation Prodrugs of etoposide and etoposide analogs
JP5112583B2 (ja) 1999-10-19 2013-01-09 バイオコン・リミテッド カソデックス、その誘導体およびその中間体の鏡像体を非対照的に合成する方法
CA2389100A1 (en) * 1999-10-27 2001-05-17 Nobex Corporation Resolution of intermediates in the synthesis of substantially pure bicalutamide
GB9930839D0 (en) * 1999-12-30 2000-02-16 Pharmacia & Upjohn Spa Process for treating gynecomastia
GB0012293D0 (en) * 2000-05-23 2000-07-12 Astrazeneca Ab Pharmaceutical combination
GB0012291D0 (en) * 2000-05-23 2000-07-12 Astrazeneca Ab Pharmaceutical combination
MY128449A (en) 2000-05-24 2007-02-28 Sugen Inc Prodrugs of 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives
US6828458B2 (en) 2000-05-25 2004-12-07 Biophysica, Inc. Topical antiandrogen for hair loss and other hyperandrogenic conditions
GB0016426D0 (en) * 2000-07-05 2000-08-23 Astrazeneca Ab Pharmaceutical combination
US20030232792A1 (en) * 2000-08-24 2003-12-18 Dalton James T. Selective androgen receptor modulators and methods of use thereof
US8008348B2 (en) 2001-12-06 2011-08-30 University Of Tennessee Research Foundation Treating muscle wasting with selective androgen receptor modulators
US7855229B2 (en) 2000-08-24 2010-12-21 University Of Tennessee Research Foundation Treating wasting disorders with selective androgen receptor modulators
US7645898B2 (en) 2000-08-24 2010-01-12 University Of Tennessee Research Foundation Selective androgen receptor modulators and method of use thereof
US8445534B2 (en) 2000-08-24 2013-05-21 University Of Tennessee Research Foundation Treating androgen decline in aging male (ADAM)-associated conditions with SARMs
US6838484B2 (en) 2000-08-24 2005-01-04 University Of Tennessee Research Foundation Formulations comprising selective androgen receptor modulators
US7026500B2 (en) * 2000-08-24 2006-04-11 University Of Tennessee Research Foundation Halogenated selective androgen receptor modulators and methods of use thereof
US20040260108A1 (en) * 2001-06-25 2004-12-23 Dalton James T. Metabolites of selective androgen receptor modulators and methods of use thereof
US7622503B2 (en) 2000-08-24 2009-11-24 University Of Tennessee Research Foundation Selective androgen receptor modulators and methods of use thereof
US20070173546A1 (en) * 2000-08-24 2007-07-26 Dalton James T Selective androgen receptor modulators and method of use thereof
ATE344233T1 (de) 2000-08-24 2006-11-15 Univ Tennessee Res Corp Selektive modulatoren des andro genrezeptors und methoden zu deren verwendung
US7919647B2 (en) 2000-08-24 2011-04-05 University Of Tennessee Research Foundation Selective androgen receptor modulators and methods of use thereof
IL154425A0 (en) 2000-08-24 2003-09-17 Univ Tennessee Res H Corp Selective androgen receptor modulators and methods of use thereof
US6998500B2 (en) 2000-08-24 2006-02-14 University Of Tennessee Research Foundation Selective androgen receptor modulators and methods of use thereof
KR20030048408A (ko) * 2000-09-21 2003-06-19 브리스톨-마이어즈 스퀴브 컴페니 Ｎ-(치환 페닐)-3-알킬-, 아릴- 및헤테로아릴설포닐-2-히드록시-2-알킬- 및할로알킬프로판아미드 화합물의 제조방법
CZ309178B6 (cs) 2001-02-19 2022-04-20 Novartis Pharma Ag 40-O-(2-hydroxyethyl)rapamycin pro použití při léčení
DE60206889T2 (de) * 2001-02-27 2006-07-27 Astrazeneca Ab Pharmazeutische formulierung enthaltend bicalutamid
US6479692B1 (en) 2001-05-02 2002-11-12 Nobex Corporation Methods of synthesizing acylanilides including bicalutamide and derivatives thereof
US20040167134A1 (en) 2001-05-16 2004-08-26 Christian Bruns Combination comprising n-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2pyrimidine-amine and a chemotherapeutic agent
US7102026B2 (en) * 2001-06-13 2006-09-05 Teva Gyógyszergyár Zártkörüen Müködö Részvénytársaság Process for preparing and isolating rac-bicalutamide and its intermediates
AU2002312431A1 (en) * 2001-06-13 2002-12-23 Biogal Gyogyszergyar Rt. Novel process for preparing rac-bicalutamide and its intermediates
US20060287282A1 (en) * 2001-06-25 2006-12-21 Steiner Mitchell S Compositions comprising a SARM ad GnRH agonist or a GnRH antagonist, and methods of use thereof
AU2002322493A1 (en) * 2001-07-10 2003-01-29 Ams Research Corporation Surgical kit for treating prostate tissue
US20060004042A1 (en) * 2001-08-23 2006-01-05 Dalton James T Formulations comprising selective androgen receptor modulators
SE0103424D0 (sv) * 2001-10-15 2001-10-15 Astrazeneca Ab Pharmaceutical formulation
AT410545B (de) * 2001-11-07 2003-05-26 Dsm Fine Chem Austria Gmbh Verfahren zur herstellung von chiralen alpha-hydroxycarbonsäuren
GB0128510D0 (en) * 2001-11-28 2002-01-23 Novartis Ag Organic compounds
US20070161608A1 (en) * 2001-12-06 2007-07-12 Dalton James T Selective androgen receptor modulators for treating muscle wasting
DK1463497T3 (da) * 2001-12-06 2012-01-30 Gtx Inc Behandling af muskelsvind med selektive androgenreceptormodulatorer
US8853266B2 (en) 2001-12-06 2014-10-07 University Of Tennessee Research Foundation Selective androgen receptor modulators for treating diabetes
EP1462442B1 (en) * 2001-12-13 2009-08-26 Sumitomo Chemical Company, Limited Crystals of bicalutamide and process for their production
JP4677516B2 (ja) * 2002-02-07 2011-04-27 ユニバーシティ オブ テネシー リサーチ ファウンデーション Ｓａｒｍを用いた前立腺肥大症治療
IL163666A0 (en) 2002-02-22 2005-12-18 New River Pharmaceuticals Inc Active agent delivery systems and methods for protecting and administering active agents
JP5113979B2 (ja) * 2002-02-28 2013-01-09 ユニバーシティ オブ テネシー リサーチ ファウンデーション 複数置換の選択的アンドロゲンレセプタ修飾因子及びその使用方法
US7803970B2 (en) 2002-02-28 2010-09-28 University Of Tennessee Research Foundation Multi-substitued selective androgen receptor modulators and methods of use thereof
CN1639110A (zh) * 2002-02-28 2005-07-13 田纳西大学研究基金会 卤代乙酰胺和叠氮化物取代的化合物及其使用方法
AU2003217304A1 (en) 2002-02-28 2003-09-16 The University Of Tennessee Research Corporation Radiolabeled selective androgen receptor modulators and their use in prostate cancer imaging and therapy
US7772433B2 (en) 2002-02-28 2010-08-10 University Of Tennessee Research Foundation SARMS and method of use thereof
GB0206215D0 (en) 2002-03-15 2002-05-01 Novartis Ag Organic compounds
SI1505959T1 (sl) 2002-05-16 2009-04-30 Novartis Ag Uporaba vezavnih sredstev EDG receptorjev pri raku
US7022870B2 (en) 2002-06-17 2006-04-04 University Of Tennessee Research Foundation N-bridged selective androgen receptor modulators and methods of use thereof
US7741371B2 (en) 2002-06-17 2010-06-22 University Of Tennessee Research Foundation Selective androgen receptor modulators and methods of use thereof
JP4449746B2 (ja) 2002-07-12 2010-04-14 アステラス製薬株式会社 Ｎ−フェニル−（２ｒ，５ｓ）ジメチルピペラジン誘導体
US20040063782A1 (en) * 2002-09-27 2004-04-01 Westheim Raymond J.H. Bicalutamide forms
US6818766B2 (en) 2002-10-02 2004-11-16 Synthon Bv Process for making bicalutamide and intermediates thereof
JP2006506369A (ja) * 2002-10-15 2006-02-23 ユニバーシティ・オブ・テネシー・リサーチ・ファウンデーション メチレン架橋選択的アンドロゲン受容体調節剤及びその使用方法
US20040197928A1 (en) * 2002-10-15 2004-10-07 Dalton James T. Method for detecting selective androgen receptor modulators
CN1726193A (zh) * 2002-10-15 2006-01-25 田纳西大学研究基金会 杂环选择性雄激素受体调节剂及其使用方法
US20040224979A1 (en) * 2002-10-15 2004-11-11 Dalton James T. Treating obesity with selective androgen receptor modulators
CA2501874A1 (en) * 2002-10-16 2004-04-29 Gtx, Inc. Treating androgen decline in aging male (adam)-associated conditions with sarms
US20060276539A1 (en) * 2002-10-16 2006-12-07 Dalton James T Treating Androgen Decline in Aging Male (ADAM)- associated conditions with SARMS
US20040087810A1 (en) * 2002-10-23 2004-05-06 Dalton James T. Irreversible selective androgen receptor modulators and methods of use thereof
PL201540B1 (pl) * 2002-10-30 2009-04-30 Inst Farmaceutyczny Sposób wytwarzania wysokiej czystości N-(4-cyjano-3-trifluorometylofenylo)-3-(4-fluorofenylosulfonylo)-2-hydroksy-2-metylopropanamidu
PL201541B1 (pl) * 2002-10-30 2009-04-30 Inst Farmaceutyczny Sposób wytwarzania N-(4-cyjano-3-trifluorometylofenylo)-2,3-epoksy-2-metylopropanamidu
US8309603B2 (en) 2004-06-07 2012-11-13 University Of Tennessee Research Foundation SARMs and method of use thereof
CA2513242C (en) * 2003-01-13 2013-07-09 Gtx Inc. Large-scale synthesis of selective androgen receptor modulators
US7332525B2 (en) * 2003-01-17 2008-02-19 Castle Erik P Method of treatment of prostate cancer and composition for treatment thereof
US20050020675A1 (en) * 2003-02-21 2005-01-27 Parthasaradhi Reddy Bandi Bicalutamide polymorphs
US20040167103A1 (en) * 2003-02-24 2004-08-26 Dalton James T. Haloacetamide and azide substituted compounds and methods of use thereof
WO2005011658A2 (en) 2003-02-27 2005-02-10 Wisconsin Alumni Research Foundation Chroman-derivated anti-androgens for treatment of androgen-mediated disorders
US20050008691A1 (en) * 2003-05-14 2005-01-13 Arturo Siles Ortega Bicalutamide compositions
CA2529232A1 (en) * 2003-06-25 2005-02-03 Teva Gyogyszergyar Reszvenytarsasag Process for purifying and isolating rac-bicalutamide
HRP20060036B1 (hr) * 2003-06-27 2014-04-25 Orion Corporation Derivati propionamida koji se koriste kao modulatori androgenih receptora
FI20030958A0 (fi) * 2003-06-27 2003-06-27 Orion Corp Uusia yhdisteitä
CN100462353C (zh) * 2003-06-27 2009-02-18 奥赖恩公司 用作雄激素受体调节剂的丙酰胺衍生物
EP1651612B9 (en) 2003-07-22 2012-09-05 Astex Therapeutics Limited 3,4-disubstituted 1h-pyrazole compounds and their use as cyclin dependent kinases (cdk) and glycogen synthase kinase-3 (gsk-3) modulators
JP2005060302A (ja) * 2003-08-12 2005-03-10 Sumitomo Chemical Co Ltd Ｎ−メタクリロイル−４−シアノ−３−トリフルオロメチルアニリンの製造方法および安定化方法
BRPI0413820A (pt) * 2003-08-22 2006-10-24 Ligand Pharm Inc derivados de 6-cicloamino-2-quinolinona como compostos moduladores de receptor de androgênio
MXPA06002462A (es) * 2003-10-14 2006-06-20 Gtx Inc Tratamiento de desordenes relacionados con huesos con moduladores del receptor de angrogeno selectivo.
TW200523235A (en) * 2003-10-15 2005-07-16 Gtx Inc Anti-cancer compounds and methods of use thereof
US7829552B2 (en) 2003-11-19 2010-11-09 Metabasis Therapeutics, Inc. Phosphorus-containing thyromimetics
EA200501761A1 (ru) 2003-12-16 2006-04-28 Джи Ти Икс, ИНК. Пролекарственные формы селективных модуляторов андрогеновых рецепторов и способы их применения
WO2005060951A2 (en) * 2003-12-19 2005-07-07 Bionaut Pharmaceuticals, Inc. Anti-neoplastic agents, combination therapies and related methods
KR100783255B1 (ko) 2004-02-13 2007-12-06 워너-램버트 캄파니 엘엘씨 안드로젠 수용체 조절제
US8519158B2 (en) * 2004-03-12 2013-08-27 Ligand Pharmaceuticals Incorporated Androgen receptor modulator compounds and methods
PE20110102A1 (es) 2004-04-07 2011-02-07 Novartis Ag Derivados de n-(2-oxo-2-pirrolidinil-1-il)etil-2-amino-acetamida como inhibidores de proteinas de apoptosis (iap)
JP2007532621A (ja) 2004-04-13 2007-11-15 ワーナー−ランバート カンパニー リミテッド ライアビリティー カンパニー アンドロゲンモジュレータ
JP2007533726A (ja) 2004-04-22 2007-11-22 ワーナー−ランバート カンパニー リミテッド ライアビリティー カンパニー アンドロゲンモジュレーター
US20110237664A1 (en) * 2004-06-07 2011-09-29 Dalton James T Selective androgen receptor modulators for treating diabetes
PL1753417T3 (pl) * 2004-06-07 2012-09-28 Univ Tennessee Res Found Selektywny modulator receptora androgenowego i jego zastosowania medyczne
US9889110B2 (en) 2004-06-07 2018-02-13 University Of Tennessee Research Foundation Selective androgen receptor modulator for treating hormone-related conditions
US9884038B2 (en) 2004-06-07 2018-02-06 University Of Tennessee Research Foundation Selective androgen receptor modulator and methods of use thereof
ITMI20041222A1 (it) 2004-06-17 2004-09-17 Cosma S P A Procedimento perfezionato per la sintesi di bicalutamide
GB0512324D0 (en) 2005-06-16 2005-07-27 Novartis Ag Organic compounds
BRPI0513020A (pt) 2004-07-08 2008-04-22 Warner Lambert Co moduladores de andrÈgenio, seus usos, composição farmacêutica, formulação farmacêutica tópica e artigo de fabricação
WO2006006736A1 (ja) * 2004-07-14 2006-01-19 Sumitomo Chemical Company, Limited ビカルタミドの晶析方法
US20060258628A1 (en) * 2004-07-20 2006-11-16 Steiner Mitchell S Compositions comprising 5-alpha reductase inhibitors, and SARMs and methods of use thereof
US20080027010A1 (en) * 2004-09-02 2008-01-31 Bionaut Pharmaceuticals, Inc. Treatment of refractory cancers using Na+/K+-ATPase inhibitors
WO2006028969A1 (en) * 2004-09-02 2006-03-16 Bionaut Pharmaceuticals, Inc. Pancreatic cancer treatment using na+/k+ atpase inhibitors
US20070105790A1 (en) * 2004-09-02 2007-05-10 Bionaut Pharmaceuticals, Inc. Pancreatic cancer treatment using Na+/K+ ATPase inhibitors
US20060135468A1 (en) * 2004-09-02 2006-06-22 Bionaut Pharmaceuticals, Inc. Treatment of refractory cancers using NA+/K+ ATPase inhibitors
WO2006029018A2 (en) * 2004-09-02 2006-03-16 Bionaut Pharmaceuticals, Inc. Combinatorial chemotherapy treatment using na+/k+-atpase inhibitors
EP1812010A2 (en) * 2004-10-18 2007-08-01 BTG International Limited Use of na+/ k+-atpase inhibitors and antagonists thereof
US20060159767A1 (en) * 2004-12-22 2006-07-20 Elan Pharma International Limited Nanoparticulate bicalutamide formulations
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
RU2436575C2 (ru) * 2005-01-21 2011-12-20 Астекс Терапьютикс Лимитед Соединения для использования в фармацевтике
ES2552338T3 (es) 2005-01-21 2015-11-27 Astex Therapeutics Limited Compuestos farmacéuticos
AR054425A1 (es) 2005-01-21 2007-06-27 Astex Therapeutics Ltd Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico.
US20080177109A1 (en) * 2005-03-29 2008-07-24 Usv Limited Novel Process for Preparation of Bicalutamide
TW200724139A (en) 2005-05-05 2007-07-01 Warner Lambert Co Androgen modulators
US7709517B2 (en) * 2005-05-13 2010-05-04 The Regents Of The University Of California Diarylhydantoin compounds
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
US7709516B2 (en) 2005-06-17 2010-05-04 Endorecherche, Inc. Helix 12 directed non-steroidal antiandrogens
EP1891067B1 (en) * 2005-06-17 2016-01-13 Ligand Pharmaceuticals Incorporated Androgen receptor modulator compounds and methods
CA2513356A1 (en) * 2005-07-26 2007-01-26 Apotex Pharmachem Inc. Process for production of bicalutamide
BRPI0616755A2 (pt) 2005-09-27 2011-06-28 Novartis Ag compostos de carboxiamina e métodos de uso dos mesmos
US7741317B2 (en) 2005-10-21 2010-06-22 Bristol-Myers Squibb Company LXR modulators
CA2629245C (en) 2005-11-21 2016-07-12 Novartis Ag Neuroendocrine tumor treatment
US7888376B2 (en) 2005-11-23 2011-02-15 Bristol-Myers Squibb Company Heterocyclic CETP inhibitors
AU2006329551A1 (en) * 2005-12-27 2007-07-05 Dabur Pharma Limited An improved process for preparation of Bicalutamide
JP5373405B2 (ja) * 2006-03-03 2013-12-18 オリオン コーポレーション 選択的アンドロゲン受容体モジュレーター
GB0605120D0 (en) 2006-03-14 2006-04-26 Novartis Ag Organic Compounds
CN102755318B (zh) 2006-03-29 2014-09-10 加利福尼亚大学董事会 二芳基硫代乙内酰脲化合物
BRPI0709749A2 (pt) 2006-04-05 2011-07-26 Novartis Ag combinaÇÕes de agentes terapÊuticos para tratamento de cÂncer
EP2004163B1 (en) 2006-04-05 2014-09-17 Novartis Pharma AG Combination of everolimus and vinorelbine
JP2009536180A (ja) 2006-05-09 2009-10-08 ノバルティス アクチエンゲゼルシャフト 鉄キレート剤と抗新生物剤を含む組合せ剤およびそれらの使用
US7550505B2 (en) * 2006-07-24 2009-06-23 University Of Delaware Pan-antagonists for the androgen receptor and androgen receptor mutants associated with anti-androgen withdrawal
US9844528B2 (en) 2006-08-24 2017-12-19 University Of Tennessee Research Foundation SARMs and method of use thereof
US10010521B2 (en) 2006-08-24 2018-07-03 University Of Tennessee Research Foundation SARMs and method of use thereof
EP3056483A1 (en) 2006-08-24 2016-08-17 University of Tennessee Research Foundation Substituted acylanilides and methods of use thereof
US9730908B2 (en) 2006-08-24 2017-08-15 University Of Tennessee Research Foundation SARMs and method of use thereof
MX2009003185A (es) 2006-09-29 2009-04-03 Novartis Ag Pirazolopirimidinas como inhibidores de lipido cinasa pi3k.
WO2008044033A1 (en) * 2006-10-11 2008-04-17 Astrazeneca Ab Amide derivatives
US8883790B2 (en) 2006-10-12 2014-11-11 Astex Therapeutics Limited Pharmaceutical combinations
US8916552B2 (en) 2006-10-12 2014-12-23 Astex Therapeutics Limited Pharmaceutical combinations
ATE547394T1 (de) 2006-12-01 2012-03-15 Bristol Myers Squibb Co N-((3-benzyl)-2,2-(bis-phenyl)-propan-1- aminderivate als cetp-hemmer für die behandlung von atherosklerose und herz-kreislauf- erkrankungen
JP5369336B2 (ja) 2007-01-02 2013-12-18 アクアビーム エルエルシー 前立腺の疾患を治療するための侵襲性が最小である方法及びデバイス
US12290277B2 (en) 2007-01-02 2025-05-06 Aquabeam, Llc Tissue resection with pressure sensing
US9232959B2 (en) 2007-01-02 2016-01-12 Aquabeam, Llc Multi fluid tissue resection methods and devices
CA2677651A1 (en) 2007-02-15 2008-08-21 Novartis Ag Combinations of therapeutic agents for treating cancer
US20080245375A1 (en) * 2007-04-05 2008-10-09 Medtronic Vascular, Inc. Benign Prostatic Hyperplasia Treatments
US9284345B2 (en) 2007-04-12 2016-03-15 Endorecherche, Inc. 17alpha-substituted steroids as systemic antiandrogens and selective androgen receptor modulators
EP2167090A4 (en) 2007-06-06 2010-08-25 Univ Maryland HDAC INHIBITORS AND HORMONE TREATMENT MEDICAMENTS
US7968603B2 (en) 2007-09-11 2011-06-28 University Of Tennessee Research Foundation Solid forms of selective androgen receptor modulators
US20090076158A1 (en) * 2007-09-13 2009-03-19 Protia, Llc Deuterium-enriched bicalutamide
PE20121470A1 (es) 2007-10-26 2012-11-18 Univ California Compuestos de diarilhidantoina como antagonistas del receptor de androgeno
EP3622910B1 (en) 2008-03-06 2024-07-10 AquaBeam LLC Tissue ablation and cautery with optical energy carried in fluid stream
BRPI0908603A2 (pt) 2008-03-24 2020-08-18 Novartis Ag inibidores de metaloprotease de matriz com base em arilsulfonamida.
EP2260020B1 (en) 2008-03-26 2014-07-23 Novartis AG Hydroxamate-based inhibitors of deacetylases b
WO2010083617A1 (en) 2009-01-21 2010-07-29 Oncalis Ag Pyrazolopyrimidines as protein kinase inhibitors
PL2391366T3 (pl) 2009-01-29 2013-04-30 Novartis Ag Podstawione benzimidazole do leczenia gwiaździaków
US20120046364A1 (en) 2009-02-10 2012-02-23 Metabasis Therapeutics, Inc. Novel Sulfonic Acid-Containing Thyromimetics, and Methods for Their Use
WO2014127242A2 (en) 2013-02-14 2014-08-21 Procept Biorobotics Corporation Aquablation aquabeam eye surgery methods and apparatus
US9848904B2 (en) 2009-03-06 2017-12-26 Procept Biorobotics Corporation Tissue resection and treatment with shedding pulses
WO2010116342A2 (en) * 2009-04-10 2010-10-14 Consiglio Nazionale Delle Ricerche Non-steroidal compounds for androgen receptor modulation
ITBO20090235A1 (it) * 2009-04-10 2010-10-11 Consiglio Nazionale Ricerche Composti per il trattamento del tumore alla prostata e procedimenti per la loro sintesi
AU2010264698C1 (en) 2009-06-26 2013-05-16 Novartis Ag 1, 3-disubstituted imidazolidin-2-one derivatives as inhibitors of CYP 17
US8450374B2 (en) * 2009-06-29 2013-05-28 University Of Delaware Pan-antagonists for the androgen receptor and androgen receptor mutants associated with anti-androgen withdrawal
US8389526B2 (en) 2009-08-07 2013-03-05 Novartis Ag 3-heteroarylmethyl-imidazo[1,2-b]pyridazin-6-yl derivatives
EP2464649A1 (en) 2009-08-12 2012-06-20 Novartis AG Heterocyclic hydrazone compounds and their uses to treat cancer and inflammation
BR112012008061A2 (pt) 2009-08-20 2016-03-01 Novartis Ag compostos de oxima heterocíclica
CA2771936A1 (en) 2009-08-26 2011-03-03 Novartis Ag Tetra-substituted heteroaryl compounds and their use as mdm2 and/or mdm4 modulators
EA201200471A1 (ru) 2009-09-10 2012-10-30 Новартис Аг Простые эфирные производные бициклических гетероарилов
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
JP5466767B2 (ja) 2009-11-04 2014-04-09 ノバルティス アーゲー Ｍｅｋ阻害剤として有用なヘテロ環式スルホンアミド誘導体
CN102712648A (zh) 2009-11-25 2012-10-03 诺瓦提斯公司 双环杂芳基的与苯稠合的6元含氧杂环衍生物
WO2011064663A1 (en) 2009-11-25 2011-06-03 Festuccia, Claudio Combination treatment employing belinostat and bicalutamide
ES2484171T3 (es) 2009-12-08 2014-08-11 Novartis Ag Derivados de sulfonamidas heterocíclicas
US8440693B2 (en) 2009-12-22 2013-05-14 Novartis Ag Substituted isoquinolinones and quinazolinones
CU24130B1 (es) 2009-12-22 2015-09-29 Novartis Ag Isoquinolinonas y quinazolinonas sustituidas
CN101759597B (zh) * 2009-12-31 2013-09-04 上海康鹏化学有限公司 2-三氟甲基-4-氨基苯腈的制备方法
EP2523556A4 (en) * 2010-01-11 2013-08-28 Gtx Inc METHOD FOR TREATING MIBROMED DYNAMIC FUNCTION
WO2016004071A1 (en) 2014-06-30 2016-01-07 Procept Biorobotics Corporation Fluid jet tissue resection and cold coagulation (aquablation) methods and apparatus
JP2013528635A (ja) 2010-06-17 2013-07-11 ノバルティス アーゲー ビフェニル置換１，３−ジヒドロ−ベンゾイミダゾール−２−イリデンアミン誘導体
EP2582681A1 (en) 2010-06-17 2013-04-24 Novartis AG Piperidinyl substituted 1,3-dihydro-benzoimidazol-2-ylideneamine derivatives
UA112517C2 (uk) 2010-07-06 2016-09-26 Новартіс Аг Тетрагідропіридопіримідинові похідні
FI20105806A0 (fi) 2010-07-15 2010-07-15 Medeia Therapeutics Ltd Uudet aryyliamidijohdannaiset, joilla on antiandrogeenisia ominaisuuksia
EP2627648A1 (en) 2010-09-16 2013-08-21 Novartis AG 17aHYDROXYLASE/C17,20-LYASE INHIBITORS
US8895772B2 (en) 2010-09-29 2014-11-25 Shilpa Medicare Limited Process for preparing bicalutamide
EP2672958A1 (en) 2011-02-08 2013-12-18 Halozyme, Inc. Composition and lipid formulation of a hyaluronan-degrading enzyme and the use thereof for treatment of benign prostatic hyperplasia
EP2673277A1 (en) 2011-02-10 2013-12-18 Novartis AG [1, 2, 4]triazolo [4, 3 -b]pyridazine compounds as inhibitors of the c-met tyrosine kinase
JP2014507465A (ja) 2011-03-08 2014-03-27 ノバルティス アーゲー フルオロフェニル二環式ヘテロアリール化合物
MX360611B (es) 2011-04-21 2018-11-09 Orion Corp Carboxamidas que modulan el receptor de andrógeno.
MX359399B (es) 2011-04-28 2018-09-27 Novartis Ag Inhibidores de 17alfa-hidroxilasa/c17-20-liasa.
JP2014513727A (ja) 2011-05-16 2014-06-05 ジェンザイム・コーポレーション Ｃｘｃｒ４拮抗薬の使用
KR20140034898A (ko) 2011-06-09 2014-03-20 노파르티스 아게 헤테로시클릭 술폰아미드 유도체
US8859535B2 (en) 2011-06-20 2014-10-14 Novartis Ag Hydroxy substituted isoquinolinone derivatives
WO2012175487A1 (en) 2011-06-20 2012-12-27 Novartis Ag Cyclohexyl isoquinolinone compounds
PH12013502524A1 (en) 2011-06-27 2014-01-27 Novartis Ag Solid forms and salts of tetrahydro-pyrido-pyrimidine derivatives
WO2013038362A1 (en) 2011-09-15 2013-03-21 Novartis Ag 6 - substituted 3 - (quinolin- 6 - ylthio) - [1,2,4] triazolo [4, 3 -a] pyradines as tyrosine kinase
WO2013080141A1 (en) 2011-11-29 2013-06-06 Novartis Ag Pyrazolopyrrolidine compounds
US20140329786A1 (en) 2011-11-30 2014-11-06 Astrazeneca Ab Combination treatment of cancer
SI2794600T1 (en) 2011-12-22 2018-03-30 Novartis Ag 2,3-Dihydro-benzo (1,4) oxazine derivatives and related compounds as phosphoinositide-3 kinase inhibitors (PI3K) for the treatment, e.g. rheumatoid arthritis
US20150148377A1 (en) 2011-12-22 2015-05-28 Novartis Ag Quinoline Derivatives
KR20140107573A (ko) 2011-12-23 2014-09-04 노파르티스 아게 Bcl2와 결합 파트너의 상호작용을 억제하기 위한 화합물
US20140350014A1 (en) 2011-12-23 2014-11-27 Novartis Ag Compounds for inhibiting the interaction of bcl2 with binding partners
EA201491264A1 (ru) 2011-12-23 2014-11-28 Новартис Аг Соединения для ингибирования взаимодействия bcl-2 с партнерами по связыванию
WO2013096055A1 (en) 2011-12-23 2013-06-27 Novartis Ag Compounds for inhibiting the interaction of bcl2 with binding partners
AU2012355624A1 (en) 2011-12-23 2014-07-17 Novartis Ag Compounds for inhibiting the interaction of BCL2 with binding partners
WO2013104829A1 (en) 2012-01-13 2013-07-18 Medeia Therapeutics Ltd Novel arylamide derivatives having antiandrogenic properties
KR102058886B1 (ko) 2012-01-13 2019-12-24 아란다 파르마 리미티드 항안드로겐 특성을 갖는 신규한 헤테로아릴아미드 유도체
AR089703A1 (es) 2012-01-13 2014-09-10 Medeia Therapeutics Ltd Derivados de arilamida que tienen propiedades antiandrogenicas
UY34591A (es) 2012-01-26 2013-09-02 Novartis Ag Compuestos de imidazopirrolidinona
JP6080872B2 (ja) 2012-02-29 2017-02-15 プロセプト バイオロボティクス コーポレイション 自動化された画像誘導組織切除および治療
JP2015512425A (ja) 2012-04-03 2015-04-27 ノバルティス アーゲー チロシンキナーゼ阻害剤との組合せ製品及びそれらの使用
WO2013152170A1 (en) 2012-04-04 2013-10-10 Catylix, Inc. Selective androgen receptor modulators
AU2013204533B2 (en) 2012-04-17 2017-02-02 Astrazeneca Ab Crystalline forms
US20130310387A1 (en) 2012-05-16 2013-11-21 Novartis Ag Monocyclic Heteroaryl Cycloalkyldiamine Derivatives
EP2855483B1 (en) 2012-05-24 2017-10-25 Novartis AG Pyrrolopyrrolidinone compounds
US10314807B2 (en) 2012-07-13 2019-06-11 Gtx, Inc. Method of treating HER2-positive breast cancers with selective androgen receptor modulators (SARMS)
HUE052574T2 (hu) 2012-07-13 2021-05-28 Oncternal Therapeutics Inc Eljárás mellrákok kezelésére szelektív ösztrogén receptor modulátorral (SARM)
US9622992B2 (en) 2012-07-13 2017-04-18 Gtx, Inc. Method of treating androgen receptor (AR)-positive breast cancers with selective androgen receptor modulator (SARMs)
US9969683B2 (en) 2012-07-13 2018-05-15 Gtx, Inc. Method of treating estrogen receptor (ER)-positive breast cancers with selective androgen receptor modulator (SARMS)
US10258596B2 (en) 2012-07-13 2019-04-16 Gtx, Inc. Method of treating HER2-positive breast cancers with selective androgen receptor modulators (SARMS)
US9744149B2 (en) 2012-07-13 2017-08-29 Gtx, Inc. Method of treating androgen receptor (AR)-positive breast cancers with selective androgen receptor modulator (SARMs)
US10987334B2 (en) 2012-07-13 2021-04-27 University Of Tennessee Research Foundation Method of treating ER mutant expressing breast cancers with selective androgen receptor modulators (SARMs)
JP6236083B2 (ja) 2012-08-13 2017-11-22 ノバルティス ティーアゲズントハイト アーゲー 脾臓チロシンキナーゼ（ｓｙｋ）の阻害剤としての二環式ヘテロアリールシクロアルキルジアミン誘導体
DK2903968T3 (en) 2012-10-02 2017-01-30 Gilead Sciences Inc INHIBITORS OF HISTON DEMETHYLASES
TW201422625A (zh) 2012-11-26 2014-06-16 Novartis Ag 二氫－吡啶并－□衍生物之固體形式
RU2510392C1 (ru) * 2012-12-21 2014-03-27 Федеральное государственное бюджетное учреждение науки Институт химии растворов им. Г.А. Крестова Российской академии наук (ИХР РАН) Сокристаллическая форма бикалутамида
WO2014115077A1 (en) 2013-01-22 2014-07-31 Novartis Ag Substituted purinone compounds
WO2014115080A1 (en) 2013-01-22 2014-07-31 Novartis Ag Pyrazolo[3,4-d]pyrimidinone compounds as inhibitors of the p53/mdm2 interaction
WO2014128612A1 (en) 2013-02-20 2014-08-28 Novartis Ag Quinazolin-4-one derivatives
EP3170811A1 (en) 2013-02-27 2017-05-24 Gilead Sciences, Inc. Ethyl pyridine-4-carboxylate compound as inhibitor of histone demethylases
WO2014155268A2 (en) 2013-03-25 2014-10-02 Novartis Ag Fgf-r tyrosine kinase activity inhibitors - use in diseases associated with lack of or reduced snf5 activity
US20150018376A1 (en) 2013-05-17 2015-01-15 Novartis Ag Pyrimidin-4-yl)oxy)-1h-indole-1-carboxamide derivatives and use thereof
UY35675A (es) 2013-07-24 2015-02-27 Novartis Ag Derivados sustituidos de quinazolin-4-ona
WO2015022664A1 (en) 2013-08-14 2015-02-19 Novartis Ag Compounds and compositions as inhibitors of mek
WO2015022663A1 (en) 2013-08-14 2015-02-19 Novartis Ag Compounds and compositions as inhibitors of mek
US9227969B2 (en) 2013-08-14 2016-01-05 Novartis Ag Compounds and compositions as inhibitors of MEK
EP3041422A4 (en) 2013-09-06 2017-04-12 Procept Biorobotics Corporation Automated image-guided tissue resection and treatment
KR20160058889A (ko) 2013-09-22 2016-05-25 칼리토르 사이언시즈, 엘엘씨 치환된 아미노피리미딘 화합물 및 이용 방법
TW201605450A (zh) 2013-12-03 2016-02-16 諾華公司 Ｍｄｍ２抑制劑與ＢＲＡＦ抑制劑之組合及其用途
US9682960B2 (en) 2013-12-19 2017-06-20 Endorecherche, Inc. Non-steroidal antiandrogens and selective androgen receptor modulators with a pyridyl moiety
CN103772238B (zh) * 2014-01-24 2017-03-22 苏州伊莱特新药研发有限公司 一类新的含酯基芳香丙酰胺化合物及其制备方法和用途
EP3122728A4 (en) 2014-03-28 2017-10-25 Calitor Sciences, LLC Substituted heteroaryl compounds and methods of use
AR099890A1 (es) 2014-03-31 2016-08-24 Epitherapeutics Aps Inhibidores de histona demetilasas
WO2015196144A2 (en) 2014-06-20 2015-12-23 England Pamela M Androgen receptor antagonists
WO2016011658A1 (en) 2014-07-25 2016-01-28 Novartis Ag Combination therapy
CN104151197B (zh) * 2014-07-25 2017-02-22 苏州伊莱特新药研发有限公司 芳香丙酰胺类化合物及其制备方法和应用
WO2016016822A1 (en) 2014-07-31 2016-02-04 Novartis Ag Combination therapy
CN107074807A (zh) 2014-08-27 2017-08-18 吉利德科学公司 用于抑制组蛋白脱甲基酶的组合物和方法
CN107072591B (zh) 2014-09-05 2021-10-26 普罗赛普特生物机器人公司 与靶器官图像的治疗映射结合的医师控制的组织切除
WO2016079521A1 (en) 2014-11-20 2016-05-26 University College Cardiff Consultants Limited Androgen receptor modulators and their use as anti-cancer agents
WO2016079522A1 (en) 2014-11-20 2016-05-26 University College Cardiff Consultants Limited Androgen receptor modulators and their use as anti-cancer agents
US9834507B2 (en) 2015-04-21 2017-12-05 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) ligands and methods of use thereof
RU2724103C2 (ru) 2015-04-21 2020-06-22 Джи Ти Икс, ИНК. Селективные лиганды-разрушители андрогенных рецептов (sard) и способы их применения
US10865184B2 (en) 2015-04-21 2020-12-15 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) ligands and methods of use thereof
US10093613B2 (en) 2015-04-21 2018-10-09 Gtx, Inc. Selective androgen receptor degrader (SARD) ligands and methods of use thereof
US10035763B2 (en) 2015-04-21 2018-07-31 Gtx, Inc. Selective androgen receptor degrader (SARD) ligands and methods of use thereof
US10806720B2 (en) 2015-04-21 2020-10-20 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) ligands and methods of use thereof
US10441570B2 (en) 2015-04-21 2019-10-15 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) Ligands and methods of use thereof
CN107709290B (zh) 2015-04-21 2023-02-28 Gtx公司 选择性雄激素受体降解剂(sard)配体和其使用方法
US10017471B2 (en) 2015-04-21 2018-07-10 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) ligands and methods of use thereof
US10654809B2 (en) 2016-06-10 2020-05-19 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) ligands and methods of use thereof
EP3347097B1 (en) 2015-09-11 2021-02-24 Sunshine Lake Pharma Co., Ltd. Substituted aminopyrimidine derivatives as modulators of the kinases jak, flt3 and aurora
US11230523B2 (en) 2016-06-10 2022-01-25 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) ligands and methods of use thereof
CN106748884B (zh) * 2016-12-13 2021-08-20 山西振东制药股份有限公司 一种比卡鲁胺中间体的制备方法
WO2019099311A1 (en) 2017-11-19 2019-05-23 Sunshine Lake Pharma Co., Ltd. Substituted heteroaryl compounds and methods of use
EP3730483B1 (en) 2017-12-21 2023-08-30 Hefei Institutes of Physical Science, Chinese Academy of Sciences Class of pyrimidine derivative kinase inhibitors
EP3740468B1 (en) 2018-01-20 2025-12-31 Sunshine Lake Pharma Co., Ltd. Substituted Aminopyrimidine Compounds and Methods of Use
WO2019222272A1 (en) 2018-05-14 2019-11-21 Nuvation Bio Inc. Anti-cancer nuclear hormone receptor-targeting compounds
WO2020051344A1 (en) 2018-09-05 2020-03-12 University Of Tennessee Research Foundation Selective androgen receptor degrader (sard) ligands and methods of use thereof
US20210386826A1 (en) 2018-11-05 2021-12-16 Pfizer Inc. Combination for Treating Cancer
CN109438297B (zh) * 2018-12-03 2021-05-14 昆明积大制药股份有限公司 雄激素受体拮抗剂、其制备方法及其应用
MX2021012690A (es) 2019-04-19 2022-01-31 Ligand Pharm Inc Formas cristalinas y metodos para producir formas cristalinas de un compuesto.
BR112021022008A2 (pt) 2019-05-14 2022-05-17 Nuvation Bio Inc Compostos de direcionamento a receptor de hormônio nuclear anticâncer
US12404332B2 (en) 2020-03-13 2025-09-02 Research Development Foundation Methods for diagnosing and treating cancers
MX2023001823A (es) 2020-08-13 2023-03-13 Pfizer Terapia de combinacion.
JP2024510666A (ja) 2021-03-24 2024-03-08 ファイザー・インク Ｄｄｒ遺伝子変異転移性去勢感受性前立腺がんを処置するためのタラゾパリブおよび抗アンドロゲンの組合せ
TWI883565B (zh) 2022-10-02 2025-05-11 美商輝瑞大藥廠 用於治療轉移性去勢抵抗性前列腺癌之他拉唑帕尼及恩雜魯胺之組合
TW202425976A (zh) 2022-12-17 2024-07-01 美商輝瑞大藥廠 用於治療轉移性去勢抵抗性前列腺癌之他拉唑帕尼及恩雜魯胺之組合
WO2025045058A1 (zh) * 2023-08-28 2025-03-06 中国药科大学 作为雄激素受体拮抗剂的化合物
WO2025067483A1 (zh) * 2023-09-28 2025-04-03 中国药科大学 酰胺类化合物

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3133119A (en) * 1961-11-09 1964-05-12 Givaudan Corp Substituted acetanilides and propionanilides
US3995060A (en) * 1972-06-20 1976-11-30 Schering Corporation Antiandrogenic agents and method for the treatment of androgen dependent disease states
CH493198A (de) * 1968-05-06 1970-07-15 Ciba Geigy Schädlingsbekämpfungsmittel
FR2142803A1 (en) * 1971-06-25 1973-02-02 Scherico Ltd 3,4-disubstd anilides - having antiandrogenic activity
US3875229A (en) * 1972-11-24 1975-04-01 Schering Corp Substituted carboxanilides
US4144270A (en) * 1973-04-19 1979-03-13 Schering Corporation Substituted anilides as anti-androgens
US4329364A (en) * 1974-09-11 1982-05-11 Schering Corporation Antiandrogenic agents and methods for the treatment of androgen dependent disease states
US4039684A (en) * 1976-03-25 1977-08-02 Schering Corporation Method for treatment of canine seborrhea
JPS6044294B2 (ja) * 1976-04-15 1985-10-02 帝国臓器製薬株式会社 アニリド誘導体
US4139638A (en) * 1976-09-23 1979-02-13 Schering Corporation Methods for the treatment of hirsutism
DE2862100D1 (en) * 1977-10-12 1983-01-05 Ici Plc Acylanilides, process for their manufacture and pharmaceutical and veterinary compositions containing them
US4191775A (en) * 1977-12-15 1980-03-04 Imperial Chemical Industries Limited Amide derivatives
NZ197008A (en) * 1980-05-22 1984-10-19 Ici Ltd Acylanilide derivatives and pharmaceutical compositions

Also Published As

Publication number Publication date
AU556328B2 (en) 1986-10-30
NO1996014I1 (no) 1996-12-10
PT77087A (en) 1983-08-01
IE55941B1 (en) 1991-02-27
IL69217A0 (en) 1983-11-30
FI832644A0 (fi) 1983-07-20
MX9203451A (es) 1992-08-01
ES8601106A1 (es) 1985-11-01
ATE28864T1 (de) 1987-08-15
US4636505A (en) 1987-01-13
LU88769I2 (fr) 1996-11-05
DK322783D0 (da) 1983-07-13
ES524392A0 (es) 1985-11-01
ES8700231A1 (es) 1986-09-16
FI83770B (fi) 1991-05-15
NO164974B (no) 1990-08-27
PT77087B (en) 1986-01-27
JPH0432061B2 (cg-RX-API-DMAC7.html) 1992-05-28
EP0100172B1 (en) 1987-08-12
IE831732L (en) 1984-01-23
JPS5933250A (ja) 1984-02-23
CS399991A3 (en) 1992-06-17
NL950029I2 (nl) 1997-03-03
FI832644A7 (fi) 1984-01-24
AU1693783A (en) 1984-01-26
NO164974C (no) 1990-12-05
EP0100172A1 (en) 1984-02-08
GR79232B (cg-RX-API-DMAC7.html) 1984-10-22
NO832599L (no) 1984-01-24
ES539614A0 (es) 1986-06-01
ES8607936A1 (es) 1986-06-01
NZ204995A (en) 1985-08-30
ES8607915A1 (es) 1986-06-01
ES539615A0 (es) 1986-06-01
DE3372965D1 (en) 1987-09-17
FI83770C (fi) 1991-08-26
IL69217A (en) 1987-03-31
HK92690A (en) 1990-11-16
NL950029I1 (cg-RX-API-DMAC7.html) 1996-02-01
ZA835182B (en) 1984-05-30
HU191296B (en) 1987-02-27
ES544189A0 (es) 1986-09-16
JPH02131462A (ja) 1990-05-21

Similar Documents

Publication Publication Date Title
CA1249823A (en) Acylanilides having antiandrogenic properties
US4386080A (en) Anti-androgenic amide derivative
EP0253503A2 (en) Substituted anilides having antiandrogenic properties
CA2285037C (fr) Nouveaux derives du 2-(iminomethyl)amino-phenyle, leur preparation, leur application a titre de medicaments et les compositions pharmaceutiques les contenant
AU2003212578A1 (en) Compounds that modulate ppar activity and methods for their preparation
HUP0203532A2 (hu) HPPAR-alfa aktivátor szubsztituált oxazol- és tiazolszármazékok, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk
NO179246B (no) Aromatiske amino-alkoholderivater og mellomprodukter til fremstilling derav
IL97565A (en) Processes for the preparation of 2-chloro-5-) chloromethyl or aminomethyl (thiazole and aminomethylthiazole salts
DE60319080T2 (de) Phenyloxyalkansäure-derivate als hppar aktivatore
WO1991009857A1 (fr) Derives heterocycliques, leur procede de preparation et leur application therapeutique
FR2804681A1 (fr) Compose antidiabetique et procede pour sa production
CA2086277A1 (en) Thiazolidine compounds, their preparation and their therapeutic uses
US4845119A (en) Alkene, alkyne or cycloalkylene derivatives
CA2657625A1 (en) Therapeutic compounds
EP0079191A1 (en) Amide derivatives
US4980363A (en) Novel amide derivatives, processes for production thereof, and agricultural-horticultural fungicide containing them
FR2621038A1 (fr) Derives d'alcadienes, leurs preparations, les medicaments les contenant et produits intermediaires
JPH03178954A (ja) ベンズアニリド
IE904522A1 (en) Pharmacologically Active Amide Carboxylate Derivatives
FR2576900A1 (fr) Derives de cyclohepto-imidazole 2-substitue, agents anti-ulcereux et procede pour leur preparation
EP0073704B1 (fr) Nouveaux nitriles hétérocycliques, leur préparation et leur utilisation pour la préparation de médicaments
EP0409692B1 (fr) Dérivés d'imino-2 hétérocyclylalkyl-3 benzothiazoline, leur préparation et les médicaments les contenant
EP0528968B1 (fr) Derives d'(alkylthio-3 propyl)-3 benzothiazoline, leur preparation et les medicaments les contenant
JPS60105669A (ja) 新規な２−メルカプトチアゾ−ル誘導体、その製造方法及び薬剤としての使用
US5192782A (en) Alkoxy-substituted dihydrobenzopyran-2-carboxylic acids and derivatives thereof

Legal Events

Date Code Title Description
MKEX Expiry