WO1995013069A1 - Piperidines, pyrrolidines and hexahydro-1h-azepines promote release of growth hormone - Google Patents

Piperidines, pyrrolidines and hexahydro-1h-azepines promote release of growth hormone Download PDF

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Publication number
WO1995013069A1
WO1995013069A1 PCT/US1994/012816 US9412816W WO9513069A1 WO 1995013069 A1 WO1995013069 A1 WO 1995013069A1 US 9412816 W US9412816 W US 9412816W WO 9513069 A1 WO9513069 A1 WO 9513069A1
Authority
WO
WIPO (PCT)
Prior art keywords
alkyl
hydrogen
aryl
cycloalkyl
phenyl
Prior art date
Application number
PCT/US1994/012816
Other languages
English (en)
French (fr)
Inventor
Gregori J. Morriello
Arthur A. Patchett
Lihu Yang
Meng H. Chen
Ravi Nargund
Original Assignee
Merck & Co., Inc.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from US08/323,998 external-priority patent/US5492920A/en
Priority claimed from US08/323,994 external-priority patent/US5494919A/en
Priority claimed from US08/323,988 external-priority patent/US5492916A/en
Priority to SK562-96A priority Critical patent/SK56296A3/sk
Priority to BR9408019A priority patent/BR9408019A/pt
Priority to JP7513932A priority patent/JPH10506091A/ja
Application filed by Merck & Co., Inc. filed Critical Merck & Co., Inc.
Priority to AU11729/95A priority patent/AU1172995A/en
Priority to EP95902467A priority patent/EP0739204A4/de
Priority to KR1019960702427A priority patent/KR960705808A/ko
Publication of WO1995013069A1 publication Critical patent/WO1995013069A1/en
Priority to BG100555A priority patent/BG100555A/bg
Priority to NO961865A priority patent/NO961865L/no
Priority to FI961951A priority patent/FI961951A/fi
Priority to LVP-96-151A priority patent/LV11525B/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/021—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)n-C(=0)-, n being 5 or 6; for n > 6, classification in C07K5/06 - C07K5/10, according to the moiety having normal peptide bonds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/582—Recycling of unreacted starting or intermediate materials

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Genetics & Genomics (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • General Health & Medical Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
PCT/US1994/012816 1993-11-09 1994-11-07 Piperidines, pyrrolidines and hexahydro-1h-azepines promote release of growth hormone WO1995013069A1 (en)

Priority Applications (10)

Application Number Priority Date Filing Date Title
KR1019960702427A KR960705808A (ko) 1993-11-09 1994-11-07 성장 호르몬의 방출을 촉진시키는 피페리딘, 피롤리딘 및 헥사하이드로-1H-아제핀(Piperidines, pyrrolidines and hexahydro-1H-azepines promote release of growth hormone)
EP95902467A EP0739204A4 (de) 1993-11-09 1994-11-07 Piperidine, pyrrolidine und hexahydro-1h-azepine unterstützen die freisetzung des wachstumshormon
AU11729/95A AU1172995A (en) 1993-11-09 1994-11-07 Piperidines, pyrrolidines and hexahydro-1h-azepines promote release of growth hormone
BR9408019A BR9408019A (pt) 1993-11-09 1994-11-07 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
JP7513932A JPH10506091A (ja) 1993-11-09 1994-11-07 成長ホルモン放出促進性のピペリジン、ピロリジンおよびヘキサヒドロ−１ｈ−アゼピン類
SK562-96A SK56296A3 (en) 1993-11-09 1994-11-07 Piperidinal, pyrrolidinal and hexahydro-1h-azepinal derivatives, manufacturing process thereof and pharmaceutical compositions containing them
BG100555A BG100555A (bg) 1993-11-09 1996-05-02 Пиперидини, пиролидини и хексахидро-1н-азепини, стимулиращи освобождаването на хормон на растежа
NO961865A NO961865L (no) 1993-11-09 1996-05-08 Piperidiner, pyrrolidiner og heksahydro-1H-azepiner fremmer frigjörelse av veksthormon
FI961951A FI961951A (fi) 1993-11-09 1996-05-08 Piperidiinit, pyrrolidiinit ja heksahydro-1H-atsepiinit edistävät kasvuhormonin vapautumista
LVP-96-151A LV11525B (en) 1993-11-09 1996-05-22 Piperidines, pyrrolidines and hexahydro-1h-azepines promote release of growth hormone

Applications Claiming Priority (12)

Application Number Priority Date Filing Date Title
US14944193A 1993-11-09 1993-11-09
US149,441 1993-11-09
US16514993A 1993-12-10 1993-12-10
US165,149 1993-12-10
US17344993A 1993-12-23 1993-12-23
US173,449 1993-12-23
US08/323,998 US5492920A (en) 1993-12-10 1994-10-17 Piperidine, pyrrolidine and hexahydro-1H-azepines promote release of growth hormone
US323,988 1994-10-17
US323,998 1994-10-17
US323,994 1994-10-17
US08/323,988 US5492916A (en) 1993-12-23 1994-10-17 Di- and tri-substituted piperidines, pyrrolidines and hexahydro-1H-azepines promote release of growth hormone
US08/323,994 US5494919A (en) 1993-11-09 1994-10-17 2-substituted piperidines, pyrrolidines and hexahydro-1H-azepines promote release of growth hormone

Publications (1)

Publication Number Publication Date
WO1995013069A1 true WO1995013069A1 (en) 1995-05-18

Family

ID=27558364

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1994/012816 WO1995013069A1 (en) 1993-11-09 1994-11-07 Piperidines, pyrrolidines and hexahydro-1h-azepines promote release of growth hormone

Country Status (16)

Country Link
EP (1) EP0739204A4 (de)
JP (1) JPH10506091A (de)
KR (1) KR960705808A (de)
CN (1) CN1174504A (de)
AU (1) AU1172995A (de)
BG (1) BG100555A (de)
BR (1) BR9408019A (de)
CA (1) CA2175218A1 (de)
CZ (1) CZ134296A3 (de)
FI (1) FI961951A (de)
HU (1) HUT74733A (de)
LV (1) LV11525B (de)
NO (1) NO961865L (de)
PL (1) PL322706A1 (de)
SK (1) SK56296A3 (de)
WO (1) WO1995013069A1 (de)

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WO1996015148A2 (en) * 1994-11-16 1996-05-23 Genentech, Inc. Low molecular weight peptidomimetic growth hormone secretagogues
US5559128A (en) * 1995-04-18 1996-09-24 Merck & Co., Inc. 3-substituted piperidines promote release of growth hormone
WO1996035713A1 (en) * 1995-05-08 1996-11-14 Pfizer, Inc. Dipeptides which promote release of growth hormone
US5622973A (en) * 1993-12-23 1997-04-22 Merck & Co., Inc. Treatment of osteoporosis with substituted piperidines, pyrrolidines and hexahydro-1H-azepines in combination with bisphosphonates
WO1997024323A1 (en) * 1995-12-28 1997-07-10 Chirotech Technology Process for the preparation of optically enriched 4-aryl-3-hydromethyl substituted piperidines to be used as intermediates in the synthesis of paroxetine
WO1997024369A1 (en) * 1995-12-28 1997-07-10 Pfizer Inc. Growth-hormone secretagogues
EP0785784A1 (de) * 1994-10-26 1997-07-30 Merck & Co., Inc. 4-heterocyclyl piperidine fördern die freisetzung von wachstumshormon
US5721250A (en) * 1993-12-23 1998-02-24 Merck & Co. Inc. Di-and tri-substituted piperidines, pyrrolidines and hexahydro-1H-azepines promote release of growth hormone
US5721251A (en) * 1993-12-10 1998-02-24 Merck & Co., Inc. Piperidine, pyrrolidine and hexahydro-1H-azepines promote release of growth hormone
US5731317A (en) * 1995-03-10 1998-03-24 Merck & Co., Inc. Bridged piperidines promote release of growth hormone
EP0831823A1 (de) * 1995-06-07 1998-04-01 Merck & Co., Inc. ALPHA 1a ADRENERGISCHE REZEPTOR-ANTAGONISTEN
WO1998058948A1 (en) * 1997-06-25 1998-12-30 Pfizer Products Inc. Tartrate salt of a substituted dipeptide as growth hormone secretagogue
WO1998058947A1 (en) * 1997-06-25 1998-12-30 Pfizer Inc. Dipeptide derivatives as growth hormone secretagogues
WO1999058501A1 (en) * 1998-05-11 1999-11-18 Novo Nordisk A/S Compounds with growth hormone releasing properties
US6011155A (en) * 1996-11-07 2000-01-04 Novartis Ag N-(substituted glycyl)-2-cyanopyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
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US6172081B1 (en) 1999-06-24 2001-01-09 Novartis Ag Tetrahydroisoquinoline 3-carboxamide derivatives
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US6323223B1 (en) 1997-08-18 2001-11-27 Syntex (U.S.A.) Llc Cyclic amine derivatives- CCR-3 receptor antagonists
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DE10105041A1 (de) * 2001-02-05 2002-08-14 Tell Pharm Ag Hergiswil Tripeptide und Tripeptid-Derivate für die Behandlung neurodegenerativer Krankheiten
EP2298760B1 (de) * 2004-06-29 2015-08-05 Helsinn Healthcare S.A. Kristallformen von (3R)-1-(2-Methylalanyl-D-tryptophyl)-3-(phenylmethyl)-3-piperidin-carbonsäure-1,2,2-trimethylhydrazid

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BR9408019A (pt) 1997-08-26
BG100555A (bg) 1996-10-31
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EP0739204A4 (de) 2000-03-15
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