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)
  • Compounds Of Unknown Constitution (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (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
DE60112742T2 (de) * 2000-05-19 2006-02-02 Applied Research Systems Ars Holding N.V. Verwendung von pyrazolderivaten zur behandlung von unfruchtbarkeit
AU2003265395A1 (en) * 2002-08-14 2004-03-03 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
WO2006113505A2 (en) 2005-04-15 2006-10-26 Clarus Therapeutics, Inc. Pharmaceutical delivery systems for hydrophobic drugs and compositions comprising same
WO2007002563A1 (en) 2005-06-27 2007-01-04 Exelixis, Inc. Imidazole based lxr modulators
KR20090023562A (ko) 2006-06-23 2009-03-05 제이-오일 밀스, 인코포레이티드 테스토스테론 증가제
UY30892A1 (es) * 2007-02-07 2008-09-02 Smithkline Beckman Corp Inhibidores de la actividad akt
CA2750565C (en) * 2009-01-30 2015-10-20 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
WO2012003405A1 (en) 2010-06-30 2012-01-05 Ironwood Pharmaceuticals, Inc. Sgc stimulators
NZ609955A (en) 2010-11-09 2015-05-29 Ironwood Pharmaceuticals Inc Sgc stimulators
CN104066731B (zh) 2011-12-27 2016-06-15 铁木医药有限公司 可用作sgc刺激剂的2-苄基、3-(嘧啶-2-基)取代的吡唑类
US11564933B2 (en) 2019-04-12 2023-01-31 Tolmar, Inc. Methods of treating testosterone deficiency
US20250171429A1 (en) * 2022-02-23 2025-05-29 Biohaven Therapeutics Ltd. Pyrazolyl compounds as kv7 channel activators

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
CA2150703C (en) * 1992-12-17 2002-01-08 Pfizer Limited Substituted pyrazoles
CN1174504A (zh) * 1993-11-09 1998-02-25 麦克公司 促进生长激素释放的哌啶、吡咯烷和六氢－1h－吖庚因
US5869688A (en) * 1994-07-20 1999-02-09 Monsanto Company Preparation of substituted 3-aryl-5-haloalkyl-pyrazoles having herbicidal activity
JP2002502380A (ja) * 1997-05-22 2002-01-22 ジー．ディー．サール アンド カンパニー ｐ３８キナーゼ阻害剤としてのピラゾール誘導体
US6080763A (en) * 1997-11-03 2000-06-27 Boehringer Ingelheim Pharmaceuticals, Inc. Aromatic heterocyclic compounds and their use as anti-inflammatory agents
CZ20013912A3 (cs) * 1999-05-04 2002-05-15 Strakan Limited Androgen glykosid, sloučenina, testosteron-ß-D-glukosid, 5 alfa-Dihydrotestosteron- 17ß-D-glukosid, farmaceutický prostředek a pouľití sloučeniny
NZ523656A (en) * 2000-08-31 2004-11-26 Pfizer Prod Inc Pyrazole derivatives and their use as protein kinase inhibitors

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

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Legal Events

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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