AU2002330120B2 - Methods of increasing endogenous testosterone levels - Google Patents

Methods of increasing endogenous testosterone levels Download PDF

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Publication number
AU2002330120B2
AU2002330120B2 AU2002330120A AU2002330120A AU2002330120B2 AU 2002330120 B2 AU2002330120 B2 AU 2002330120B2 AU 2002330120 A AU2002330120 A AU 2002330120A AU 2002330120 A AU2002330120 A AU 2002330120A AU 2002330120 B2 AU2002330120 B2 AU 2002330120B2
Authority
AU
Australia
Prior art keywords
optionally substituted
tert
pyrazol
pyridin
tyrosinamide
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.)
Ceased
Application number
AU2002330120A
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English (en)
Other versions
AU2002330120A1 (en
Inventor
Stephen J. Arkinstall
William H. Brondyk
Sean Mckenna
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.)
Merck Serono SA
Original Assignee
Laboratoires Serono SA
Serono Laboratories UK 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
Application filed by Laboratoires Serono SA, Serono Laboratories UK Ltd filed Critical Laboratoires Serono SA
Publication of AU2002330120A1 publication Critical patent/AU2002330120A1/en
Application granted granted Critical
Publication of AU2002330120B2 publication Critical patent/AU2002330120B2/en
Assigned to LABORATOIRES SERONO SA reassignment LABORATOIRES SERONO SA Request for Assignment Assignors: APPLIED RESEARCH SYSTEMS ARS HOLDING N.V.
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K31/415—1,2-Diazoles
    • 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
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • 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
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/06—Anabolic 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Obesity (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Compounds Of Unknown Constitution (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU2002330120A 2001-09-27 2002-09-27 Methods of increasing endogenous testosterone levels Ceased AU2002330120B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US32547001P 2001-09-27 2001-09-27
US60/325,470 2001-09-27
PCT/US2002/030801 WO2003026649A1 (en) 2001-09-27 2002-09-27 Methods of increasing endogenous testosterone levels

Publications (2)

Publication Number Publication Date
AU2002330120A1 AU2002330120A1 (en) 2003-06-26
AU2002330120B2 true AU2002330120B2 (en) 2007-10-11

Family

ID=23268011

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2002330120A Ceased AU2002330120B2 (en) 2001-09-27 2002-09-27 Methods of increasing endogenous testosterone levels

Country Status (12)

Country Link
US (1) US20040198799A1 (enExample)
EP (1) EP1441724B8 (enExample)
JP (1) JP2005504093A (enExample)
AT (1) ATE372114T1 (enExample)
AU (1) AU2002330120B2 (enExample)
CA (1) CA2458661A1 (enExample)
DE (1) DE60222286T2 (enExample)
DK (1) DK1441724T3 (enExample)
ES (1) ES2289143T3 (enExample)
IL (1) IL161047A0 (enExample)
PT (1) PT1441724E (enExample)
WO (1) WO2003026649A1 (enExample)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT1282418E (pt) * 2000-05-19 2005-10-31 Applied Research Systems Utilizacao de derivados pirazolo para o tratamento da infertilidade
WO2004016592A1 (en) * 2002-08-14 2004-02-26 Ppd Discovery, Inc. Prenylation inhibitors and methods of their synthesis and use
US8492369B2 (en) 2010-04-12 2013-07-23 Clarus Therapeutics Inc Oral testosterone ester formulations and methods of treating testosterone deficiency comprising same
US8241664B2 (en) 2005-04-15 2012-08-14 Clarus Therapeutics, Inc Pharmaceutical delivery systems for hydrophobic drugs and compositions comprising same
KR101363278B1 (ko) 2005-06-27 2014-02-21 엑셀리시스 페이턴트 컴퍼니 엘엘씨 이미다졸계 ｌｘｒ 변조제
CN101472574B (zh) 2006-06-23 2011-06-15 J-制油株式会社 睾丸酮增强剂
UY30892A1 (es) * 2007-02-07 2008-09-02 Smithkline Beckman Corp Inhibidores de la actividad akt
NZ594064A (en) * 2009-01-30 2012-08-31 Glaxosmithkline Llc Crystalline n-{ (1s)-2-amino-1-[(3-fluorophenyl)methyl]ethyl} -5-chloro-4-(4-chloro-1-methyl-1h-pyrazol-5-yl)-2-thiophenecarboxamide hydrochloride
WO2011161615A1 (en) 2010-06-24 2011-12-29 Ranbaxy Laboratories Limited 5-lipoxygenase inhibitors
WO2011161645A1 (en) 2010-06-25 2011-12-29 Ranbaxy Laboratories Limited 5-lipoxygenase inhibitors
TWI532737B (zh) 2010-06-30 2016-05-11 艾諾屋製藥公司 可溶性鳥苷酸環化酶（ｓＧＣ）刺激物
JP5878546B2 (ja) 2010-11-09 2016-03-08 アイアンウッド ファーマシューティカルズ インコーポレイテッド ｓＧＣ刺激剤
CA2861804C (en) 2011-12-27 2021-10-26 Ironwood Pharmaceuticals, Inc. 2-benzyl,3(pyrimidin-2-yl)substituted pyrazoles useful as sgc stimulators
US11564933B2 (en) 2019-04-12 2023-01-31 Tolmar, Inc. Methods of treating testosterone deficiency
CN118695860A (zh) * 2022-02-23 2024-09-24 拜奥海芬治疗学有限公司 作为kv7通道激活剂的吡唑基化合物

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU6469401A (en) * 2000-05-19 2001-11-26 Serono Reproductive Biology In Pharmaceutically active compounds and methods of use

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2665898B1 (fr) * 1990-08-20 1994-03-11 Sanofi Derives d'amido-3 pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant.
DE4039733A1 (de) * 1990-12-13 1992-06-17 Basf Ag Substituierte 5-aminopyrazole
KR100190730B1 (ko) * 1992-12-17 1999-06-01 디. 제이. 우드, 스피겔 알렌 제이 부신피질 호르몬 유리인자(crf) 길항물질로서 치환된 피라졸
BR9408019A (pt) * 1993-11-09 1997-08-26 Merck & Co Inc Composto composição util para aumentar a produção endógena ou a liberaçao de hormonio do crescimento em ser humano ou um animal e para o tratamento da osteoporose processos para aumentar os niveis de hormônio do crescimento em um ser humano ou um animal e a eficácia de alimentação promover o crescimento aumentar a produçao de leite e melhorar a qualidade da carcaça de gado para tratar ou previnir uma condição selecionada para tratar osteoporose e para preparar um composto
US5869688A (en) * 1994-07-20 1999-02-09 Monsanto Company Preparation of substituted 3-aryl-5-haloalkyl-pyrazoles having herbicidal activity
US6087381A (en) * 1997-05-22 2000-07-11 G. D. Searle & Company Pyrazole derivatives as p38 kinase inhibitors
AU1367599A (en) * 1997-11-03 1999-05-24 Boehringer Ingelheim Pharmaceuticals, Inc. Aromatic heterocyclic compounds as anti-inflammatory agents
IL146284A0 (en) * 1999-05-04 2002-07-25 Strakan Ltd Androgen glycosides and pharmaceutical compositions containing the same
DZ3398A1 (fr) * 2000-08-31 2002-03-07 Pfizer Prod Inc Derives pyrazole et leur utilisation comme inhibiteurs des proteines kinases

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU6469401A (en) * 2000-05-19 2001-11-26 Serono Reproductive Biology In Pharmaceutically active compounds and methods of use

Also Published As

Publication number Publication date
EP1441724B1 (en) 2007-09-05
IL161047A0 (en) 2004-08-31
ES2289143T3 (es) 2008-02-01
US20040198799A1 (en) 2004-10-07
CA2458661A1 (en) 2003-04-03
EP1441724B8 (en) 2007-10-17
EP1441724A1 (en) 2004-08-04
JP2005504093A (ja) 2005-02-10
WO2003026649A1 (en) 2003-04-03
DE60222286D1 (de) 2007-10-18
PT1441724E (pt) 2007-10-15
ATE372114T1 (de) 2007-09-15
DK1441724T3 (da) 2007-12-03
DE60222286T2 (de) 2008-06-19

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Legal Events

Date Code Title Description
PC1 Assignment before grant (sect. 113)

Owner name: LABORATOIRES SERONO SA

Free format text: FORMER APPLICANT(S): APPLIED RESEARCH SYSTEMS ARS HOLDING N.V.

FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired