PE1999A1 - Ciertos derivados de bencilamina amido y aminosustituidos utiles como ligandos especificos del neuropeptido y1 - Google Patents

Ciertos derivados de bencilamina amido y aminosustituidos utiles como ligandos especificos del neuropeptido y1

Info

Publication number
PE1999A1
PE1999A1 PE1997000652A PE00065297A PE1999A1 PE 1999 A1 PE1999 A1 PE 1999A1 PE 1997000652 A PE1997000652 A PE 1997000652A PE 00065297 A PE00065297 A PE 00065297A PE 1999 A1 PE1999 A1 PE 1999A1
Authority
PE
Peru
Prior art keywords
phenyl
alkyl
neuropeptide
compounds
cycllohexyl
Prior art date
Application number
PE1997000652A
Other languages
English (en)
Inventor
Robert Desimone
Alan Hutchison
John M Peterson
Charles A Blum
Original Assignee
Neurogen Corp
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 Neurogen Corp filed Critical Neurogen Corp
Publication of PE1999A1 publication Critical patent/PE1999A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • 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
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
    • C07D237/28—Cinnolines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/02—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/135—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/155—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Peptides Or Proteins (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Indole Compounds (AREA)
  • Steroid Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

SE REFIEREN A COMPUESTOS DE FORMULA (I) Y A SUS PROFARMACOS ACILADOS, EN DONDE: Ar ES FENILO, PIRIDILO, TIENILO, PIRIMIDILO OPCIONALMENTE SUSTITUIDOS; "A" Y "T" SON H, HALOGENO, OH, ALQUILO C1-C6 o ALCOXI C1-C6; "B" ES S, O, N(R5) o C(R5)(R6); UNO DE X1, X2 Y X3 ES -Q(D)-C(=E)-(CH2)o-G o -Q(D)-SO2-(CH2)o-G Y EL RESTO ES H; SI "Q" ES N, ENTONCES, "D" ES H, ALQUILO C1-C6 O PUEDE ESTAR UNIDO CON G PARA FORMAR UN ANILLO, o SI "Q" ES O, ENTONCES, "D" ESTA AUSENTE; "E" ES O o H2; "G" ES ALQUILO C1-C6, ARILO, HETEROARILO; R1 Y R2 SON H o ALQUILO C1-C6; R3 Y R4 SON H, ALQUILO C1-C6 o ALCOXI C1-C6; R5 ES H, ALQUILO C1-C6, FENILO o PIRIDILO; R6 ES H, AMINO, ALQUILO C1-C6, ENTRE OTROS; m ES 2-4; n ES 1-3; o ES 0 o 1; SON COMPUESTOS (I) PREFERIDOS: CIS-N-[3-[4-METIL-1-(4-FENIL-1-PIPERAZINIL)CICLOHEXIL]FENIL]-4-FLUOROBENZAMIDA; CIS-N-[3-[4-METIL-1-(4-FENIL-1-PIPERAZINIL)CICLOHEXIL]FENIL]-4-CINOLINOCARBOXAMIDA; 5-CLORO-CIS-N-[3-[4-METIL-1-(4-FENIL-1-PIPERAZINIL)CICLOHEXIL]FENIL]-1H-INDAZOL-3-CARBOXAMIDA. TAMBIEN SE REFIERE AL PROCEDIMIENTO DE PREPARACION DE LOS COMPUESTOS (I) MEDIANTE REACCIONES DE GRIGNARD. LOS COMPUESTOS (I) ACTUAN COMO ANTAGONISTAS DEL NEUROPEPTIDO "Y", SIENDO UTILES EN EL TRATAMIENTO DE TRASTORNOS DE LA ALIMENTACION COMO POR EJEMPLO OBESIDAD Y BULIMIA, Y ALGUNOS TRASTORNOS VASCULARES COMO HIPERTENSION, ENTRE OTROS
PE1997000652A 1996-07-23 1997-07-22 Ciertos derivados de bencilamina amido y aminosustituidos utiles como ligandos especificos del neuropeptido y1 PE1999A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US2229896P 1996-07-23 1996-07-23

Publications (1)

Publication Number Publication Date
PE1999A1 true PE1999A1 (es) 1999-02-02

Family

ID=21808875

Family Applications (1)

Application Number Title Priority Date Filing Date
PE1997000652A PE1999A1 (es) 1996-07-23 1997-07-22 Ciertos derivados de bencilamina amido y aminosustituidos utiles como ligandos especificos del neuropeptido y1

Country Status (20)

Country Link
US (2) US6133265A (es)
EP (1) EP0918761B1 (es)
JP (1) JP2000515527A (es)
AR (1) AR008071A1 (es)
AT (1) ATE239002T1 (es)
AU (1) AU3671897A (es)
CA (1) CA2260983A1 (es)
CO (1) CO4890841A1 (es)
DE (1) DE69721541T2 (es)
DK (1) DK0918761T3 (es)
ES (1) ES2197354T3 (es)
HR (1) HRP970412A2 (es)
ID (1) ID17453A (es)
MA (1) MA26435A1 (es)
PA (1) PA8434601A1 (es)
PE (1) PE1999A1 (es)
PT (1) PT918761E (es)
TN (1) TNSN97127A1 (es)
WO (1) WO1998003494A1 (es)
ZA (1) ZA976470B (es)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU3671897A (en) * 1996-07-23 1998-02-10 Neurogen Corporation Certain amido- and amino-substituted benzylamine derivatives; a new class of neuropeptite y1 specific ligands
SE9703414D0 (sv) * 1997-09-23 1997-09-23 Astra Ab New compounds
EP1033366A3 (en) * 1999-02-18 2000-12-27 Pfizer Products Inc. Amide derivatives useful as Neuropeptide Y (NPY) antagonists
EP1299362A4 (en) * 2000-07-05 2004-11-03 Synaptic Pharma Corp SELECTIVE RECEPTOR ANTAGONISTS OF MELANINE CONCENTRATING HORMON-1 (MCH1) AND THEIR USE
WO2002004433A2 (en) * 2000-07-06 2002-01-17 Neurogen Corporation Melanin concentrating hormone receptor ligands
EP1620091B1 (en) 2003-05-05 2010-03-31 Probiodrug AG Inhibitors of glutaminyl cyclase
US7514438B2 (en) 2003-08-13 2009-04-07 Amgen, Inc. Melanin concentrating hormone receptor antagonist
AU2004290499C1 (en) 2003-11-03 2011-02-24 Probiodrug Ag Combinations useful for the treatment of neuronal disorders
WO2005075436A2 (en) 2004-02-05 2005-08-18 Probiodrug Ag Novel inhibitors of glutaminyl cyclase
US8354427B2 (en) * 2004-06-24 2013-01-15 Vertex Pharmaceutical Incorporated Modulators of ATP-binding cassette transporters
CA2881078C (en) 2004-06-24 2018-10-02 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
WO2007075901A2 (en) * 2005-12-24 2007-07-05 Vertex Pharmaceuticals Incorporated Quinolin- 4 - one derivatives as modulators of abc transporters
LT1993360T (lt) 2005-12-28 2017-06-12 Vertex Pharmaceuticals Incorporated N-[2,4-bis(1,1-dimetiletil)-5-hidroksifenil]-1,4-dihidro-4-oksochinolin-3-karboksamido kieta forma
EP1834953A1 (en) 2006-03-14 2007-09-19 Ranbaxy Laboratories Limited Tetrahydropyrane derivatives as 5-lipoxygenase inhibitors
US8278345B2 (en) 2006-11-09 2012-10-02 Probiodrug Ag Inhibitors of glutaminyl cyclase
ATE554085T1 (de) 2006-11-30 2012-05-15 Probiodrug Ag Neue inhibitoren von glutaminylcyclase
JP5930573B2 (ja) 2007-03-01 2016-06-15 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤の新規使用
WO2008128985A1 (en) 2007-04-18 2008-10-30 Probiodrug Ag Thiourea derivatives as glutaminyl cyclase inhibitors
US20100074949A1 (en) 2008-08-13 2010-03-25 William Rowe Pharmaceutical composition and administration thereof
US12458635B2 (en) 2008-08-13 2025-11-04 Vertex Pharmaceuticals Incorporated Pharmaceutical composition and administrations thereof
SI3330255T1 (sl) 2009-03-20 2021-03-31 Vertex Pharmaceuticals Incorporated Postopek izdelave regulatorja transmembranske prevodnosti pri cistični fibrozi
PL2475428T3 (pl) 2009-09-11 2015-12-31 Probiodrug Ag Pochodne heterocykliczne jako inhibitory cyklazy glutaminowej
ES2586231T3 (es) 2010-03-03 2016-10-13 Probiodrug Ag Inhibidores de glutaminil ciclasa
MX2012010470A (es) 2010-03-10 2012-10-09 Probiodrug Ag Inhibidores heterociclicos d ciclasa de glutaminilo (qc, ec .3 2. 5).
US8541596B2 (en) 2010-04-21 2013-09-24 Probiodrug Ag Inhibitors
US8802700B2 (en) 2010-12-10 2014-08-12 Vertex Pharmaceuticals Incorporated Modulators of ATP-Binding Cassette transporters
EP2686313B1 (en) 2011-03-16 2016-02-03 Probiodrug AG Benzimidazole derivatives as inhibitors of glutaminyl cyclase
EP2819670B1 (en) 2012-02-27 2026-05-20 Vertex Pharmaceuticals Incorporated Pharmaceutical Composition and Their Administration
CA2963945C (en) 2014-10-07 2023-01-10 Vertex Pharmaceuticals Incorporated Co-crystals of modulators of cystic fibrosis transmembrane conductance regulator
PL3461819T3 (pl) 2017-09-29 2020-11-30 Probiodrug Ag Inhibitory cyklazy glutaminylowej
WO2020172609A1 (en) 2019-02-21 2020-08-27 Marquette University Heterocyclic ligands of par1 and methods of use
JP2022522534A (ja) 2019-04-02 2022-04-19 アリゴス セラピューティクス インコーポレイテッド Prmt5を標的にする化合物
US12698266B2 (en) 2019-12-19 2026-08-04 Casma Therapeutics, Inc. TRPML modulators

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4845221A (en) * 1988-04-15 1989-07-04 American Home Products Corporation Serotonergic substituted piperazinyl tetralins
IL94151A (en) * 1989-04-22 1995-08-31 Wyeth John & Brother Ltd History of piperazine, their preparation and pharmaceutical preparations containing them
US5900415A (en) * 1994-11-07 1999-05-04 Pfizer Inc. Certain substituted benzylamine derivatives; a new class of neuropeptide Y1 specific ligands
IL117997A0 (en) * 1995-06-07 1996-10-31 Pfizer Neuropeptide Y1 specific ligands
CA2261031A1 (en) * 1996-07-23 1998-01-29 Charles A. Blum Certain substituted benzylamine derivatives; a new class of neuropeptide y1 specific ligands
AU3671897A (en) * 1996-07-23 1998-02-10 Neurogen Corporation Certain amido- and amino-substituted benzylamine derivatives; a new class of neuropeptite y1 specific ligands
WO1998003493A1 (en) * 1996-07-23 1998-01-29 Neurogen Corporation Certain substituted benzylamine derivatives; a new class of neuropeptide-y1 specific ligands

Also Published As

Publication number Publication date
CA2260983A1 (en) 1998-01-29
EP0918761B1 (en) 2003-05-02
AR008071A1 (es) 1999-12-09
ID17453A (id) 1998-01-08
DE69721541T2 (de) 2004-03-18
JP2000515527A (ja) 2000-11-21
ATE239002T1 (de) 2003-05-15
HRP970412A2 (en) 1998-10-31
US6133265A (en) 2000-10-17
ZA976470B (en) 1998-08-04
AU3671897A (en) 1998-02-10
WO1998003494A1 (en) 1998-01-29
TNSN97127A1 (fr) 2005-03-15
DE69721541D1 (de) 2003-06-05
US6316617B1 (en) 2001-11-13
EP0918761A1 (en) 1999-06-02
DK0918761T3 (da) 2003-08-25
CO4890841A1 (es) 2000-02-28
ES2197354T3 (es) 2004-01-01
PA8434601A1 (es) 2000-05-24
PT918761E (pt) 2003-09-30
MA26435A1 (fr) 2004-12-20

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