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)
  • Animal Behavior & Ethology (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)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Steroid Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Quinoline 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 (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE239002T1 (de) * 1996-07-23 2003-05-15 Neurogen Corp Einige amido-und amino-substituierte benzylaminderivate: eine neue klasse von neuropeptid y1 spezifischen liganden
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
WO2002006245A1 (en) * 2000-07-05 2002-01-24 Synaptic Pharmarceutical Corporation Selective melanin concentrating hormone-1 (mch1) receptor antagonists and uses thereof
EP1366030A2 (en) 2000-07-06 2003-12-03 Neurogen Corporation Melanin concentrating hormone receptor ligands
US20100074949A1 (en) 2008-08-13 2010-03-25 William Rowe Pharmaceutical composition and administration thereof
JP4806628B2 (ja) 2003-05-05 2011-11-02 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
JP2007502287A (ja) 2003-08-13 2007-02-08 アムジェン インコーポレイテッド メラニン凝集ホルモン受容体アンタゴニスト
NZ546887A (en) 2003-11-03 2009-04-30 Probiodrug Ag Combinations useful for the treatment of neuronal disorders
CN1918131B (zh) 2004-02-05 2011-05-04 前体生物药物股份公司 谷氨酰胺酰基环化酶抑制剂
US8354427B2 (en) * 2004-06-24 2013-01-15 Vertex Pharmaceutical Incorporated Modulators of ATP-binding cassette transporters
CN101891680B (zh) 2004-06-24 2014-10-29 沃泰克斯药物股份有限公司 Atp-结合弹夹转运蛋白的调控剂
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
US7674811B2 (en) 2006-03-14 2010-03-09 Ranbaxy Laboratories Limited 5-lipoxygenase inhibitors
WO2008055945A1 (en) 2006-11-09 2008-05-15 Probiodrug Ag 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases
DK2091948T3 (da) 2006-11-30 2012-07-23 Probiodrug Ag Nye inhibitorer af glutaminylcyclase
KR20090115951A (ko) 2007-03-01 2009-11-10 프로비오드룩 아게 글루타미닐 사이클라제 저해제의 신규 용도
EP2865670B1 (en) 2007-04-18 2017-01-11 Probiodrug AG Thiourea derivatives as glutaminyl cyclase inhibitors
SI3330255T1 (sl) 2009-03-20 2021-03-31 Vertex Pharmaceuticals Incorporated Postopek izdelave regulatorja transmembranske prevodnosti pri cistični fibrozi
CA2772488C (en) 2009-09-11 2018-04-17 Probiodrug Ag Heterocyclic derivatives as inhibitors of glutaminyl cyclase
ES2586231T3 (es) 2010-03-03 2016-10-13 Probiodrug Ag Inhibidores de glutaminil ciclasa
DK2545047T3 (da) 2010-03-10 2014-07-28 Probiodrug Ag Heterocycliske inhibitorer af glutaminylcyclase (QC, EC 2.3.2.5)
EP2560953B1 (en) 2010-04-21 2016-01-06 Probiodrug AG Inhibitors of glutaminyl cyclase
US8802700B2 (en) 2010-12-10 2014-08-12 Vertex Pharmaceuticals Incorporated Modulators of ATP-Binding Cassette transporters
DK2686313T3 (en) 2011-03-16 2016-05-02 Probiodrug Ag Benzimidazole derivatives as inhibitors of glutaminyl cyclase
MX2014010253A (es) 2012-02-27 2014-11-12 Vertex Pharma Composicion farmaceutica y administraciones de la misma.
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
US11130743B2 (en) 2019-02-21 2021-09-28 Marquette University Heterocyclic ligands of PAR1 and methods of use
CN114072407A (zh) 2019-04-02 2022-02-18 阿里戈斯治疗公司 靶向prmt5的化合物

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
HUT54666A (en) * 1989-04-22 1991-03-28 Wyeth John & Brother Ltd Process for producing peperazine derivatives and pharmaceutical compositions 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
ES2186907T3 (es) * 1996-07-23 2003-05-16 Neurogen Corp Ciertos derivados de bencilamina sustituidos; una nueva clase de ligandos especificos del neuropeptido y1.
JP2000515151A (ja) * 1996-07-23 2000-11-14 ニューロジェン・コーポレーション 特定の置換ベンジルアミン誘導体；新規クラスの神経ペプチド―ｙ１特異的リガンド
ATE239002T1 (de) * 1996-07-23 2003-05-15 Neurogen Corp Einige amido-und amino-substituierte benzylaminderivate: eine neue klasse von neuropeptid y1 spezifischen liganden

Also Published As

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

Similar Documents

Publication Publication Date Title
PE1999A1 (es) Ciertos derivados de bencilamina amido y aminosustituidos utiles como ligandos especificos del neuropeptido y1
DE69725007D1 (de) Delta 1,6 bicyclo (4,4,0) basierte farbstoffe zur kontrastverstaerkung in der optischen bilderzeugung
DE69005248D1 (de) 2-Aminopyrimidin-3-oxid-Derivate enthaltende Zusammensetzungen zur Verwendung zum Vermindern des Haarausfalles und zum Induzieren und Stimulieren des Haarwuchses und neue von 2-Aminopyrimidin-3-oxid abgeleitete Verbindungen.
NO2014022I1 (no) Rosuvastatin (som sink) og ezetimib
PE108898A1 (es) Derivados 6,5-heterobiciclicos sustituidos
PE115999A1 (es) Secretagogos de la hormona del crecimiento
DE60236600D1 (de) Substituierte 1h-dihydropyrazole, ihre herstellung und verwendung
DE69020466D1 (de) Collagen-Zubereitungen und Verfahren zur Herstellung davon.
AR006720A1 (es) Un compuesto derivado de azahexano heterociclico, su uso para la preparacion de una composicion farmaceutica, procedimiento para prepararlo y una composicion farmaceutica que lo comprende
ES2059327T3 (es) Derivados de tetrahidronaftaleno y de indano, obtencion de los mismos y utilizacion en preparados farmaceuticos.
AR004219A1 (es) Nuevos derivados de quinazolina, procedimientos para su preparacion, composiciones que los contienen y su uso en la preparacion de medicamentos,particularmente en el tratamiento de trastornos inflamatorios
DE60335552D1 (de) Neue zusammensetzung und verfahren zur behandlung von immunerkrankungen
ATE215062T1 (de) Verfahren zur herstellung von cyclohexen- carboxylatderivate
PE20040762A1 (es) Ureas substituidas y carbamatos utiles para el tratamiento de la enfermedad de alzheimer
DE69433984D1 (de) Arylpiperazinderivate von indol als liganden der rezeptoren 5 ht1-like, 5 ht1b und 5 ht1d
ATE220925T1 (de) Trizyklische funktional farbstoffe zur verbesserung von kontrast und optische bilderzeugung
PE20030539A1 (es) Derivados de piperazina antagonistas de los receptores de somatostatina sst1
NO992676L (no) 1,4-diazabicyklo[2,2,2]okt-2-ylmetylderivater, deres fremstilling og terapeutiske anvendelse
DE69723880D1 (de) Delta 1,2 bicyclo 4,4,0] basierte farbstoffe zur kontrastverstärkung in der optischen bilderzeugung
DE69611502D1 (de) (Oxo-1-Alkyl)amino-2-desoxy-2-glucopyranosid von Dihydroxy-2,3-propyl, Verfahren zur Herstellung und ihre Verwendungen
ATE114468T1 (de) Ethyl-(+)-apovincaminat zur behandlung der demyelinisierung klinischer erscheinungen autoimmunen ursprungs.
NZ221314A (en) 1,4-dihydropyridine derivatives and pharmaceutical composition
DE69911689D1 (de) Verfahren zur Herstellung von S-Aryl-L-cystein und Derivate
PE52496A1 (es) Nueva sulfonamida y procedimiento de obtencion
ATE203533T1 (de) INDOLDERIVATE ALS PRODRUGS VON ß5-HT1-LIKEß REZEPTOR AGONISTEN

Legal Events

Date Code Title Description
FD Application declared void or lapsed