JP5005127B2 - アンドロゲングリコシド及びそのアンドロゲン作用活性 - Google Patents

アンドロゲングリコシド及びそのアンドロゲン作用活性 Download PDF

Info

Publication number
JP5005127B2
JP5005127B2 JP2000615641A JP2000615641A JP5005127B2 JP 5005127 B2 JP5005127 B2 JP 5005127B2 JP 2000615641 A JP2000615641 A JP 2000615641A JP 2000615641 A JP2000615641 A JP 2000615641A JP 5005127 B2 JP5005127 B2 JP 5005127B2
Authority
JP
Japan
Prior art keywords
compound
hydrogen
testosterone
medicament
manufacture
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 - Fee Related
Application number
JP2000615641A
Other languages
English (en)
Japanese (ja)
Other versions
JP2002543217A (ja
JP2002543217A5 (enExample
Inventor
マイケル・フランシス・ホリック
ジョン・アンソニー・ケニス
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.)
Strakan International Ltd Great Britain
Original Assignee
Strakan International Ltd Great Britain
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 Strakan International Ltd Great Britain filed Critical Strakan International Ltd Great Britain
Publication of JP2002543217A publication Critical patent/JP2002543217A/ja
Publication of JP2002543217A5 publication Critical patent/JP2002543217A5/ja
Application granted granted Critical
Publication of JP5005127B2 publication Critical patent/JP5005127B2/ja
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Images

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J17/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0036—Nitrogen-containing hetero ring
    • C07J71/0057—Nitrogen and oxygen
    • C07J71/0063—Nitrogen and oxygen at position 2(3)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/16—Masculine contraceptives
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J17/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J17/005—Glycosides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0036—Nitrogen-containing hetero ring
    • C07J71/0042—Nitrogen only
    • C07J71/0047—Nitrogen only at position 2(3)

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Reproductive Health (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Virology (AREA)
  • AIDS & HIV (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Gynecology & Obstetrics (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Oncology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Coloring Foods And Improving Nutritive Qualities (AREA)
JP2000615641A 1999-05-04 2000-05-04 アンドロゲングリコシド及びそのアンドロゲン作用活性 Expired - Fee Related JP5005127B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US13250099P 1999-05-04 1999-05-04
US60/132,500 1999-05-04
US19529400P 2000-04-07 2000-04-07
US60/195,294 2000-04-07
PCT/GB2000/001700 WO2000066612A1 (en) 1999-05-04 2000-05-04 Androgen glycosides and androgenic activity thereof

Publications (3)

Publication Number Publication Date
JP2002543217A JP2002543217A (ja) 2002-12-17
JP2002543217A5 JP2002543217A5 (enExample) 2005-12-22
JP5005127B2 true JP5005127B2 (ja) 2012-08-22

Family

ID=26830416

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2000615641A Expired - Fee Related JP5005127B2 (ja) 1999-05-04 2000-05-04 アンドロゲングリコシド及びそのアンドロゲン作用活性

Country Status (20)

Country Link
US (2) US6630453B1 (enExample)
EP (1) EP1175433B1 (enExample)
JP (1) JP5005127B2 (enExample)
KR (1) KR20020013533A (enExample)
CN (1) CN1250563C (enExample)
AT (1) ATE301129T1 (enExample)
AU (1) AU777770C (enExample)
BR (1) BR0010708A (enExample)
CA (1) CA2372720C (enExample)
CZ (1) CZ20013912A3 (enExample)
DE (1) DE60021720T2 (enExample)
DK (1) DK1175433T3 (enExample)
ES (1) ES2246234T3 (enExample)
HU (1) HUP0200871A3 (enExample)
IL (2) IL146284A0 (enExample)
MX (1) MXPA01011227A (enExample)
NO (1) NO321296B1 (enExample)
NZ (1) NZ515134A (enExample)
PT (1) PT1175433E (enExample)
WO (1) WO2000066612A1 (enExample)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE60021720T2 (de) 1999-05-04 2006-06-01 Strakan International Ltd. Androgen glykoside und die androgenische aktivität davon
EP1441724B8 (en) * 2001-09-27 2007-10-17 Laboratoires Serono SA Methods of increasing endogenous testosterone levels
US7217696B2 (en) * 2002-02-28 2007-05-15 A & D Bioscience, Inc. Glycuronamides, glycosides and orthoester glycosides of fluoxetine, analogs and uses thereof
US20050107310A1 (en) * 2002-03-19 2005-05-19 Holick Michael F. Carboxylic acid glycuronides, glycosamides and glycosides of quinolones, penicillins, analogs, and uses thereof
WO2003086475A1 (en) * 2002-04-12 2003-10-23 A & D Bioscience, Inc. Conjugates comprising cancer cell specific ligands, a sugar and diagnostic agents, and uses thereof
EP1549323A2 (en) * 2002-05-07 2005-07-06 A & D Bioscience, Inc. Conjugates comprising central nervous system active drug
US20050215487A1 (en) * 2002-06-27 2005-09-29 Holick Michael F Conjugates comprising an nsaid and a sugar and uses thereof
US20070225354A1 (en) * 2006-03-21 2007-09-27 Eric Marchewitz Use of dihydrolipoamide for enhancing physical performance
US10966916B2 (en) 2014-11-10 2021-04-06 The Procter And Gamble Company Personal care compositions
EP3217948B1 (en) 2014-11-10 2020-09-16 The Procter and Gamble Company Personal care compositions with two benefit phases
EP3217949B1 (en) 2014-11-10 2020-06-17 The Procter and Gamble Company Personal care compositions with two benefit phases
CN105388245A (zh) * 2015-12-25 2016-03-09 浙江省水产技术推广总站 适用于水产品中46种药物的筛查方法
CN111212625B (zh) 2017-10-20 2023-05-23 宝洁公司 气溶胶泡沫洁肤剂
WO2019079405A1 (en) 2017-10-20 2019-04-25 The Procter & Gamble Company AEROSOL FOAMING CLEANSER FOR THE SKIN
CN113015904B (zh) 2018-11-29 2024-06-18 宝洁公司 用于筛选个人护理产品的方法

Family Cites Families (173)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3126375A (en) 1964-03-24 Chioacyl
US3124571A (en) 1964-03-10 Process for hydrgxyiation of
GB584062A (en) 1943-12-28 1947-01-06 Chem Ind Basel Manufacture of saccharide derivatives
US2447325A (en) 1946-06-24 1948-08-17 Research Corp Production of 3,11-oxygenated steroids
US3053865A (en) 1958-03-19 1962-09-11 Merck & Co Inc Novel 16-alkyl and 16-alkylene steroids and processes
US3007923A (en) 1959-01-22 1961-11-07 Lab Francais Chimiotherapie Process for the fluorination of 9beta, 11beta-epoxy and 5alpha, 6alpha-epoxy steroids
GB916778A (en) 1959-10-15 1963-01-30 Vismara Francesco Spa Oral compositions containing 3-substituted 17-ª--methyl testosterones
US3021347A (en) 1959-10-13 1962-02-13 American Cyanamid Co Process for hydrolyzing 16, 17 steroid acetonides
US3104246A (en) 1961-08-18 1963-09-17 Roussel Uclaf Process of preparation of beta-methasone
US3185682A (en) 1961-10-04 1965-05-25 Merck & Co Inc Steroid glucuronides and processes for preparing the same
GB1047542A (en) 1963-02-18 1966-11-09 Merck & Co Inc 21-galacturonides of steroids
US3427300A (en) 1965-11-12 1969-02-11 Merck & Co Inc Anti-inflammatory steroid 2'-acetamido-2'-deoxy-glucoside compounds
GB1175219A (en) 1967-06-22 1969-12-23 Ici Ltd 3-Aminoalkoxycarbonylmethylene Steroid Derivatives
US3721712A (en) 1968-08-19 1973-03-20 Richardson Merrell Inc Aminoalkoxy-or aminomethyl-triarylalkenones
US3862193A (en) 1970-12-02 1975-01-21 Ortho Pharma Corp O-(nitroaryl) oximes of 3-keto steroids
GB1338547A (en) 1971-04-20 1973-11-28 Syntex Corp 17beta-tetrahydropyran-4-yloxy- steroids
US3917831A (en) 1972-03-20 1975-11-04 Richardson Merrell Inc 3-Keto-7 {60 ,{62 -loweralkyl-{66 {0 5-steroids
US3733318A (en) 1972-03-23 1973-05-15 Syntex Corp 21-orthoesters of cortical steroids and methods of preparing same
SE378109B (enExample) 1972-05-19 1975-08-18 Bofors Ab
NL7305171A (enExample) 1973-04-13 1974-10-15
NL7317358A (nl) 1973-12-19 1975-06-23 Akzo Nv Nieuwe 11(beta)-alkylsteroiden van de oestraanreeks.
NL189235C (nl) 1974-02-28 1993-02-16 Akzo Nv Werkwijze voor de bereiding van een oraal toe te dienen farmaceutisch preparaat met androgene werking.
DE2410443A1 (de) 1974-03-01 1975-09-11 Schering Ag 11beta-fluor-androstene
DE2519645C2 (de) 1975-05-02 1982-08-26 Robert Bosch Gmbh, 7000 Stuttgart Verpackungsanlage
NL7613248A (nl) 1976-11-26 1978-05-30 Akzo Nv Werkwijze voor het bereiden van nieuwe steroid- esters.
NL7701384A (nl) 1977-02-10 1978-08-14 Akzo Nv Werkwijze voor het bereiden van nieuwe steroiden van de oestraanreeks.
GB1560274A (en) 1977-02-28 1980-02-06 Ici Ltd Phenylbut 1-ene derivatives having antiostrogenicactivity
DE2860900D1 (en) 1977-08-22 1981-11-05 Ici Plc Triphenylalkene derivatives, process for their preparation and pharmaceutical compositions containing them
DE2817157A1 (de) 1978-04-17 1979-10-25 Schering Ag Verwendung von antioestrogenen und antigonadotrop wirkenden antiandrogenen zur prophylaxe und therapie der prostatahyperplasie
US4201029A (en) 1978-08-14 1980-05-06 Automated Packaging Systems, Inc. Method and apparatus for packaging
EP0011372B1 (en) 1978-11-07 1983-02-09 Imperial Chemical Industries Plc 1-acyloxyphenyl-1,2-diphenylalkene derivatives, processes for their manufacture and a pharmaceutical composition containing these derivatives
JPS624527Y2 (enExample) 1979-04-13 1987-02-02
US4410515A (en) 1981-04-01 1983-10-18 Massachusetts General Hospital Vitamin D glycosides and a method of use
US4418068A (en) 1981-04-03 1983-11-29 Eli Lilly And Company Antiestrogenic and antiandrugenic benzothiophenes
US4656187A (en) 1981-08-03 1987-04-07 Eli Lilly And Company Treatment of mammary cancer
JPS5831088U (ja) 1981-08-25 1983-03-01 株式会社マキ製作所 複数条型選果機の計測用照明装置
GB2126576B (en) 1982-06-25 1985-06-19 Farmos Group Limited Alkane and alkene derivatives
US5491173A (en) 1982-06-25 1996-02-13 Orion-Yhtyma Oy Tri-phenyl alkene derivatives and their preparation and use
WO1984004041A1 (en) 1983-04-14 1984-10-25 Univ California Colon-specific drug delivery system
CA1229604A (en) 1984-02-14 1987-11-24 Lorne J. Brandes Aminoalkyl ethers of phenols as antiproliferative anticancer agents
US4521410A (en) 1984-05-03 1985-06-04 The General Hospital Corporation Vitamin D glycosyl orthoesters
US4729999A (en) 1984-10-12 1988-03-08 Bcm Technologies Antiestrogen therapy for symptoms of estrogen deficiency
GB8604528D0 (en) 1986-02-24 1986-04-03 Ici Plc Therapeutic agents
GB8615916D0 (en) 1986-06-30 1986-08-06 Amersham Int Plc Bone-seeking complexes of technetium-99m
US5024833A (en) 1988-03-10 1991-06-18 Industrial Farmaceutica Serono Spa Combined interferon/antiestrogen therapy for treatment of breast cancer
DE3733478A1 (de) 1987-10-01 1989-04-13 Schering Ag Antigestagen- und antioestrogenwirksame verbindungen zur geburtseinleitung und zum schwangerschaftsabbruch sowie zur behandlung gynaekologischer stoerungen und hormonabhaengiger tumore
US5540925A (en) 1988-04-06 1996-07-30 Alfacell Corporation Compositions comprising ONCONASE (TM) and STELAZINE (TM) or TAMOXIFEN (TM)
IL91362A0 (en) 1989-08-20 1990-03-19 Yissum Res Dev Co Bisphosphonates,process for preparing them and pharmaceutical compositions containing them
US5196409A (en) 1989-08-20 1993-03-23 Yissum, Research Development Company Of The Hebrew University Of Jerusalem Bisphosphonates, pharmaceutical compositions, and process for the treatment of irregularities in calcium metabolism
US5134001A (en) 1990-08-07 1992-07-28 Mobil Oil Corporation Liminated multilayer film composite and heat sealed bag made therefrom
ES2072015T3 (es) 1990-08-21 1995-07-01 Upjohn Co Derivados del acido bisfosfonico como agente anti-artritico.
US5189212A (en) 1990-09-07 1993-02-23 University Of Georgia Research Foundation, Inc. Triarylethylene carboxylic acids with estrogenic activity
WO1992004365A1 (en) 1990-09-10 1992-03-19 Schering Corporation Mometasone furoate monohydrate, process for making same and pharmaceutical compositions
US5219548A (en) 1990-10-01 1993-06-15 Board Of Regents, The University Of Texas System High affinity halogenated-tamoxifen derivatives and uses thereof
US6096874A (en) 1990-10-01 2000-08-01 Board Of Regents, The University Of Texas System High affinity tamoxifen derivatives
JPH06504522A (ja) 1990-10-01 1994-05-26 ボード　オブ　リージェンツ，　ザ　ユニバーシティ　オブ　テキサス　システム 高親和性タモキシフェン誘導体とその使用
JPH06503329A (ja) 1990-12-07 1994-04-14 ジ・アップジョン・カンパニー 抗炎症剤として有用なホスホン酸誘導体
US5183815A (en) 1991-01-22 1993-02-02 Merck & Co., Inc. Bone acting agents
US5118667A (en) 1991-05-03 1992-06-02 Celtrix Pharmaceuticals, Inc. Bone growth factors and inhibitors of bone resorption for promoting bone formation
US5103036A (en) 1991-05-13 1992-04-07 E. R. Squibb & Sons, Inc. Process for preparing 3-alkenylidene-1,1-bisphosphonates
US5157027A (en) 1991-05-13 1992-10-20 E. R. Squibb & Sons, Inc. Bisphosphonate squalene synthetase inhibitors and method
DE69210607T2 (de) 1991-06-26 1996-09-26 Schering Corp., Kenilworth, N.J. Inhalator für Medikamente in Pulverform
ZA924811B (en) 1991-06-28 1993-12-29 Endorecherche Inc Controlled release systems and low dose androgens
HU222501B1 (hu) 1991-06-28 2003-07-28 Endorecherche Inc. MPA-t vagy MGA-t tartalmazó nyújtott hatóanyag-felszabadulású gyógyászati készítmény és eljárás előállítására
US5260065A (en) 1991-09-17 1993-11-09 Micro Vesicular Systems, Inc. Blended lipid vesicles
US5196435A (en) 1991-11-21 1993-03-23 Eli Lilly And Company Melatonin derivatives and combinations with antiestrogen compounds for treating mammalian breast carcinoma
US5338837A (en) 1991-12-13 1994-08-16 The Trustees Of Princeton University Glycosylated steroid derivatives for transport across biological membranes and process for making same
JP3141053B2 (ja) 1991-12-26 2001-03-05 アベンティス ファーマ株式会社 ビスホスホン酸誘導体
IT1259534B (it) 1992-04-09 1996-03-20 Cavanna Spa Procedimento e dispositivo per il controllo del movimento di articoli, particolarmente per macchine confezionatrici
JPH05286992A (ja) 1992-04-13 1993-11-02 Mect Corp 新規シアリルステロイド
US5317015A (en) 1992-05-01 1994-05-31 Rhone-Poulenc Rorer Pharmaceuticals Inc. Azacyclic bisphosphonates as anticholesterolemic agents
WO1993022334A1 (en) 1992-05-04 1993-11-11 Sri International Pharmaceutical compositions and methods for colonic delivery of corticosteroids
JPH07507317A (ja) 1992-05-29 1995-08-10 プロクター、エンド、ギャンブル、ファーマスーティカルズ、インコーポレーテッド 異常なカルシウムおよびホスフェート代謝を治療するためのチオ置換窒素含有複素環式ホスホネート化合物
US5753634A (en) 1992-05-29 1998-05-19 The Procter & Gamble Company Quaternary nitrogen containing phosphonate compounds, pharmaceutical compostions, and methods for treating abnormal calcium and phosphate metabolism
US5763611A (en) 1992-05-29 1998-06-09 The Procter & Gamble Company Thio-substituted cyclic phosphonate compounds, pharmaceutical compositions, and methods for treating abnormal calcium and phosphate metabolism
TW366342B (en) 1992-07-28 1999-08-11 Lilly Co Eli The use of 2-phenyl-3-aroylbenzothiophenes in inhibiting bone loss
US5446203A (en) 1992-08-25 1995-08-29 New York University Synthesis of haloenones and aryl or alkyl substituted enones or alkenes
US5409911A (en) 1992-09-11 1995-04-25 Merck & Co., Inc. Prostaglandin analog for treating osteoporosis
JPH08502287A (ja) 1992-10-09 1996-03-12 ジ・アップジョン・カンパニー 抗炎症剤としてのピリミジンビスホスホン酸エステルおよび（アルコキシメチルホスフィニル）アルキルホスホン酸
DE4236237A1 (de) 1992-10-27 1994-04-28 Behringwerke Ag Prodrugs, ihre Herstellung und Verwendung als Arzneimittel
DK0676951T3 (da) 1992-12-29 2002-06-03 Michael F Holick Anvendelse af vitamin-D-glycosider til behandling eller forebyggelse af osteoporose
SK87295A3 (en) 1993-01-08 1996-04-03 Astra Ab Novel colon or ileum-specific steroid derivatives
ES2261836T3 (es) 1993-01-19 2006-11-16 Endorecherche Inc. Usos terapeuticos de dehidroepiandrosterona para tratamiento de libido disminuida y osteoporosis.
US5844001A (en) 1993-02-26 1998-12-01 Research Development Foundation Combination platinum chemotherapeutic/antiestrogen therapy for human cancers
US5403829A (en) 1993-03-24 1995-04-04 Leiras Oy Use of bisphosphonates in endo-osteal bone surgery
DE4312034A1 (de) 1993-04-13 1994-10-20 Hesch Rolf Dieter Prof Dr Med Neuartige Androgene und Anabolika
US5486511A (en) 1993-05-25 1996-01-23 Merrell Dow Pharmaceuticals Inc. 4-amino-17β-(cyclopropyloxy)androst-4-en-3-one, 4-amino-17β-(cyclopropylamino)androst-4-en-3-one and related compounds as C17-20 lyase and 5α-reductase
TW369521B (en) 1993-09-17 1999-09-11 Smithkline Beecham Corp Androstenone derivative
CA2172983A1 (en) 1993-09-29 1995-04-06 Kei Sugai 21-substituted steroid compound
US5461065A (en) 1993-10-15 1995-10-24 Eli Lilly And Company Methods for inhibiting endometriosis
US5418252A (en) 1993-10-15 1995-05-23 Eli Lilly And Company Method for inhibiting cartilage degradation
US5441964A (en) 1993-10-15 1995-08-15 Eli Lilly And Company Methods for inhibiting bone loss using substituted benzothiophene
UA32427C2 (uk) 1993-10-15 2000-12-15 Елі Ліллі Енд Компані Застосування бензотіофенів або їх фармацевтично прийнятних солей або сольватів для інгібування ангіогенезу і/або ангіогенних захворювань
DE4335876A1 (de) 1993-10-17 1995-04-20 Schering Ag Kombination von Progesteronantagonisten und Antiöstrogenen mit partialer agonistischer Wirkung für die Hormonsubstitutions-Therapie für peri- und postmenopausale Frauen
AU696167B2 (en) 1993-10-29 1998-09-03 Trustees Of Boston University Physiologically stable compositions of butyric acid, and butyric acid salts and derivatives as anti-neoplastic agents
US5451590A (en) 1993-12-21 1995-09-19 Eli Lilly & Co. Methods of inhibiting sexual precocity
US5462950A (en) 1993-12-21 1995-10-31 Eli Lilly And Company Methods of treating menstrual symptoms and compositions therefore
US5672610A (en) 1993-12-21 1997-09-30 Eli Lilly And Company Methods of increasing macrophage function
US5708009A (en) 1993-12-21 1998-01-13 Eli Lilly And Company Methods of inhibiting myeloperoxidase activity
US5552415A (en) 1993-12-21 1996-09-03 Eli Lilly And Company Method of inhibiting Alzheimer's Disease
US5446053A (en) 1993-12-21 1995-08-29 Eli Lilly And Company Methods of inhibiting dysfunctional uterine bleeding
US5441965A (en) 1993-12-21 1995-08-15 Eli Lilly And Company Methods of inhibiting thrombin
US5441966A (en) 1993-12-21 1995-08-15 Eli Lilly And Company Methods of inhibiting Turner's syndrome
US5574047A (en) 1993-12-21 1996-11-12 Eli Lilly And Company Methods of inhibiting imperfect tissue repair
US5439923A (en) 1993-12-21 1995-08-08 Eli Lilly And Company Method of inhibiting seborrhea and acne
US5447941A (en) 1993-12-21 1995-09-05 Eli Lilly And Company Methods of inhibiting pulmonary hypertensive diseases with raloxifene and related benzothiophenes
CZ321394A3 (en) 1993-12-21 1995-08-16 Lilly Co Eli Pharmaceutical preparation for inhibiting woman hirsutism and alopecia
US5439931A (en) 1993-12-21 1995-08-08 Eli Lilly And Company Method for increasing libido in post-menopausal women
US6417198B1 (en) 1993-12-21 2002-07-09 Eli Lilly And Company Methods of inhibiting CNS problems in post-menopausal women
US5492927A (en) 1993-12-21 1996-02-20 Eli Lilly And Company Non-peptide tachykinin receptor antagonists to treat allergy
US5461064A (en) 1993-12-21 1995-10-24 Eli Lilly And Company Methods of inhibiting atrophy of the skin and vagina
US5578613A (en) 1993-12-21 1996-11-26 Eli Lilly And Company Methods for inhibiting weight gain or inducing weight loss
US5476862A (en) 1993-12-21 1995-12-19 Eli Lilly And Company Methods of increasing thrombomodulin expression
US5451589A (en) 1993-12-21 1995-09-19 Eli Lilly And Company Methods of inhibiting ovarian dysgenesis, delayed puberty, or sexual infantilism
US5534526A (en) 1993-12-21 1996-07-09 Eli Lilly And Company Methods for inhibiting vasomotor symptoms and attending psychological disturbances surrounding post-menopausal syndrome
US5521198A (en) 1993-12-21 1996-05-28 Eli Lilly And Company Methods of inhibiting autoimmune diseases
US5593987A (en) 1993-12-21 1997-01-14 Eli Lilly And Company Methods of inhibiting breast disorders
US5591753A (en) 1994-01-28 1997-01-07 Eli Lilly And Company Combination treatment for osteoporosis
US5811120A (en) 1994-03-02 1998-09-22 Eli Lilly And Company Solid orally administerable raloxifene hydrochloride pharmaceutical formulation
US5972383A (en) 1994-03-02 1999-10-26 Eli Lilly And Company Solid orally administerable raloxifene hydrochloride pharmaceutical formulation
US5478847A (en) 1994-03-02 1995-12-26 Eli Lilly And Company Methods of use for inhibiting bone loss and lowering serum cholesterol
DE4407742C1 (de) 1994-03-08 1995-06-22 Hexal Pharma Gmbh Transdermales System in Form eines Pflasters mit einem Tamoxifen-Derivat
CA2145614A1 (en) 1994-03-31 1995-10-01 Jeffrey A. Dodge Intermediates and processes for preparing benzothiophene compounds
US5650425A (en) 1994-04-04 1997-07-22 Pharmos Corporation Permanently ionic derivatives of steroid hormones and their antagonists
JPH09511927A (ja) 1994-04-18 1997-12-02 ザ、プロクター、エンド、ギャンブル、カンパニー 歯槽骨へのビスホスホネート類のイオン導入デリバリー
US5681835A (en) 1994-04-25 1997-10-28 Glaxo Wellcome Inc. Non-steroidal ligands for the estrogen receptor
US5604248A (en) 1994-05-05 1997-02-18 Eli Lilly And Company Method for minimizing the uterotrophic effect of tamoxifen and tamoxifen analogs
US6723739B1 (en) 1994-05-20 2004-04-20 Eli Lilly And Company Glucopyranoside benzothiophenes
US5470883A (en) 1994-05-23 1995-11-28 Stromberg; Brent V. Method of treating peripheral vasoconstriction with tamoxifen citrate
US5466810A (en) 1994-06-10 1995-11-14 Eli Lilly And Company 2-amino-3-aroyl-benzo[β]thiophenes and methods for preparing and using same to produce 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-aminoethoxy)-benzoyl]benzo[β]thiophenes
US5441986A (en) 1994-07-19 1995-08-15 Pfizer Inc. Estrogen agonists as remedies for prostate and cardiovascular diseases
US5612317A (en) 1994-08-04 1997-03-18 Holick; Michael F. Method for delivering estrogen
US5502074A (en) 1994-08-22 1996-03-26 Eli Lilly And Company Benzothiophenes for bone healing and fracture repair
US5550123A (en) 1994-08-22 1996-08-27 Eli Lilly And Company Methods for inhibiting bone prosthesis degeneration
US5496828A (en) 1994-08-22 1996-03-05 Eli Lilly And Company Methods of inhibiting ulcerative mucositis
US5512296A (en) 1994-08-22 1996-04-30 Eli Lilly And Company Methods for inhibiting neuronal damage
US5434166A (en) 1994-08-22 1995-07-18 Eli Lilly And Company Methods of inhibiting demyelinating and desmyelinating diseases
US5494920A (en) 1994-08-22 1996-02-27 Eli Lilly And Company Methods of inhibiting viral replication
US5629425A (en) 1994-09-19 1997-05-13 Eli Lilly And Company Haloalkyl hemisolvates of 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-piperidinoethoxy)-benzoyl]benzo[b]thiophene
CO4410191A1 (es) 1994-09-19 1997-01-09 Lilly Co Eli SINTESIS DE 3-[4-(2-AMINOETOXI)BENZOIL]-2-ARIL-6- HIDROXIBENZO [b] TIOFENOS
US5658931A (en) 1994-09-20 1997-08-19 Eli Lilly And Company Method for inhibiting mammalian breast carcinoma with tamoxifen, and analogs thereof, and certain naphthyl compounds
US7501441B1 (en) 1994-09-20 2009-03-10 Eli Lilly And Company Naphthyl compounds, intermediates, processes, compositions, and methods
US5843964A (en) 1994-09-22 1998-12-01 Eli Lilly And Company Methods of inhibiting endometrial mitoses
US5545641A (en) 1994-10-20 1996-08-13 Eli Lilly And Company Methods of inhibiting physiological conditions associated with an excess of bradykinin
US5521214A (en) 1995-01-25 1996-05-28 Eli Lilly And Company Methods of inhibiting environmental estrogens
US5484808A (en) 1995-02-09 1996-01-16 Eli Lilly And Company Methods of inhibiting cell-cell adhesion
US5821254A (en) 1995-02-17 1998-10-13 The United States Of America As Represented By The Department Of Health And Human Services Uses of 9-cis-retinoic acids and derivatives thereof alone or in combination with antineoplastic agents in the prevention or treatment of cancer
US5510357A (en) 1995-02-28 1996-04-23 Eli Lilly And Company Benzothiophene compounds as anti-estrogenic agents
US5563054A (en) 1995-03-31 1996-10-08 Eli Lilly And Company Process for preparation of benzo[B]thiophene glucuronides
US5614639A (en) 1995-03-31 1997-03-25 Eli Lilly And Company Process for preparing 2-substituted benzo[b]thiophene compounds and intermediates thereof
WO1996038466A1 (en) 1995-05-29 1996-12-05 Pfizer Inc. Steroidal glycosides
US5622975A (en) 1995-06-01 1997-04-22 Eli Lilly And Company Methods for inhibiting vascular smooth muscle cell migration
US5843974A (en) 1995-06-06 1998-12-01 Eli Lilly And Company Methods of inhibiting melanoma using Benzothiophenes as cytotoxic agents per se
US5616571A (en) 1995-06-06 1997-04-01 Merck & Co., Inc. Bisphosphonates prevent bone loss associated with immunosuppressive therapy
US5569772A (en) 1995-06-07 1996-10-29 Eli Lilly And Company Process for the synthesis of benzo[b]thiophenes
US5659087A (en) 1995-06-07 1997-08-19 Eli Lilly And Company Diarylvinyl sulfoxides
US5514826A (en) 1995-06-07 1996-05-07 Eli Lilly And Company Vinyl sulfenic acid derivatives
DE19526146A1 (de) 1995-07-07 1997-01-09 Schering Ag Triphenylethylene, Verfahren zu deren Herstellung, diese Triphenylethylene enthaltene pharmazeutische Präparate sowie deren Verwendung zur Herstellung von Arzneimitteln
US5739307A (en) 1995-08-28 1998-04-14 Washington University Polynucleotide encoding neurturin neurotrophic factor
US5902582A (en) 1995-09-05 1999-05-11 Chiron Corporation Use of TFPI inhibitor for treatment of cancer
US5726168A (en) 1995-10-12 1998-03-10 Eli Lilly And Company Lipophilic benzothiophenes
US5731342A (en) 1996-02-22 1998-03-24 Eli Lilly And Company Benzothiophenes, formulations containing same, and methods
ES2257756T3 (es) 1996-03-12 2006-08-01 Sanofi-Aventis Deutschland Gmbh Nuevos profarmacos para la terapia de tumores y enfermedades inflamatorias.
DE19619045C1 (de) 1996-05-02 1997-11-13 Jenapharm Gmbh Verwendung von Kombinationspräparaten zur Behandlung hypogonadaler Männer sowie Männern mit Hypophysenerkrankungen
US5843984A (en) 1996-05-09 1998-12-01 Eli Lilly And Company Sulfated benzothiophene derivatives, methods of use and formulations containing same
US5753633A (en) 1997-04-11 1998-05-19 Colgate-Palmolive Company Method of inhibiting bone resorption
DE19720312A1 (de) 1997-05-15 1998-11-19 Hoechst Ag Zubereitung mit erhöhter in vivo Verträglichkeit
JPH1175863A (ja) 1997-07-10 1999-03-23 Kyowa Hakko Kogyo Co Ltd ２５−ヒドロキシビタミンＤ３−１α−水酸化酵素および該酵素をコードするＤＮＡ
US6090843A (en) 1997-08-11 2000-07-18 Eli Lilly And Company Benzothiophenes compounds which have useful pharmaceutical activity
US5952319A (en) * 1997-11-26 1999-09-14 Research Triangle Institute Androgenic steroid compounds and a method of making and using the same
DE60021720T2 (de) 1999-05-04 2006-06-01 Strakan International Ltd. Androgen glykoside und die androgenische aktivität davon
WO2001027127A1 (en) 1999-10-08 2001-04-19 Strakan Group Plc Tamoxifen and tamoxifen analogue glycosides and uses thereof
AU7673900A (en) 1999-10-08 2001-04-23 Strakan Limited Glycosides and orthoester glycosides of raloxifene and analogues and the use thereof

Also Published As

Publication number Publication date
CA2372720C (en) 2007-09-11
AU777770C (en) 2005-11-10
EP1175433B1 (en) 2005-08-03
KR20020013533A (ko) 2002-02-20
HUP0200871A2 (en) 2002-08-28
US6916791B2 (en) 2005-07-12
PT1175433E (pt) 2005-11-30
NO20015338D0 (no) 2001-11-01
IL146284A (en) 2006-07-05
CN1360590A (zh) 2002-07-24
NZ515134A (en) 2004-01-30
AU4589300A (en) 2000-11-17
NO20015338L (no) 2001-11-19
BR0010708A (pt) 2002-02-19
ATE301129T1 (de) 2005-08-15
MXPA01011227A (es) 2002-07-02
US20030216328A1 (en) 2003-11-20
CN1250563C (zh) 2006-04-12
DK1175433T3 (da) 2005-09-19
CA2372720A1 (en) 2000-11-09
US6630453B1 (en) 2003-10-07
JP2002543217A (ja) 2002-12-17
EP1175433A1 (en) 2002-01-30
DE60021720D1 (de) 2005-09-08
HUP0200871A3 (en) 2004-04-28
AU777770B2 (en) 2004-10-28
ES2246234T3 (es) 2006-02-16
WO2000066612A1 (en) 2000-11-09
NO321296B1 (no) 2006-04-18
IL146284A0 (en) 2002-07-25
DE60021720T2 (de) 2006-06-01
CZ20013912A3 (cs) 2002-05-15

Similar Documents

Publication Publication Date Title
JP5005127B2 (ja) アンドロゲングリコシド及びそのアンドロゲン作用活性
US7196074B2 (en) Methods of making, using and pharmaceutical formulations comprising 7α, 11β-dimethyl-17β-hydroxyestra-4, 14-dien-3-one and 17 esters thereof
JP2000256390A (ja) 性ステロイド活性を抑制するために用いるエストロゲン核誘導体の医薬組成物
EP0210665B1 (en) Steroids useful as anti-cancer, anti-obesity, anti-hyperglycemic, anti-autoimmune and anti-hyper-cholesterolemic agents
US20090023695A1 (en) METHOD OF MAKING AND USING 7alpha,11beta-DIMETHYL-17beta-HYDROXYESTR-4-EN-3-ONE 17-UNDECANOATE
US20100331292A1 (en) Substituted 16,17-annellated steriod compounds for use in womens healthcare
KR100940054B1 (ko) 호르몬 효과를 갖는 17알파-히드록시-14베타-스테로이드
EP1379253B1 (en) Methods of making and pharmaceutical formulations comprising 7alpha,11beta-dimethyl-17beta-hydroxyestra-4, 14-dien-3-one and 17 esters thereof
EP2440567B1 (en) Substituted 16,17-annellated steroid compounds for use in women's healthcare
CA2412864C (en) Methods of making, using and pharmaceutical formulations comprising 7.alpha.,11.beta.-dimethyl-17.beta.-hydroxyestra-4,14-dien-3-one and 17 esters thereof
AU2002339536A1 (en) 17alpha-hydroxy-14beta-steroids with hormonal effect
AU2002258664A1 (en) Methods of making, using and pharmaceutical formulations comprising 7alpha, 11beta-dimethyl-17beta-hydroxyestra-4, 14-dien-3-one and 17-esters thereof
HK1063637B (en) 17alpha-hydroxy-14beta-steroids with hormonal effect

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20050329

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20050513

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20070502

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20100921

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20101216

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20101224

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20110322

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20110510

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20110810

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20110817

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20110912

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20110920

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20111011

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20120424

A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20120523

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20150601

Year of fee payment: 3

R150 Certificate of patent or registration of utility model

Free format text: JAPANESE INTERMEDIATE CODE: R150

LAPS Cancellation because of no payment of annual fees