ES2483242T3 - Moduladores de hidrolasa amida de ácido graso - Google Patents

Moduladores de hidrolasa amida de ácido graso Download PDF

Info

Publication number
ES2483242T3
ES2483242T3 ES11719136.1T ES11719136T ES2483242T3 ES 2483242 T3 ES2483242 T3 ES 2483242T3 ES 11719136 T ES11719136 T ES 11719136T ES 2483242 T3 ES2483242 T3 ES 2483242T3
Authority
ES
Spain
Prior art keywords
hydrolase
fatty acid
acid amide
minutes
dioxol
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.)
Active
Application number
ES11719136.1T
Other languages
English (en)
Inventor
John M. Keith
Jing Liu
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.)
Janssen Pharmaceutica NV
Original Assignee
Janssen Pharmaceutica NV
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 Janssen Pharmaceutica NV filed Critical Janssen Pharmaceutica NV
Application granted granted Critical
Publication of ES2483242T3 publication Critical patent/ES2483242T3/es
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12—Antidiarrhoeals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • 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

Abstract

Un compuesto que es 4-(2,2-difluoro-benzo[1,3]dioxol-5-ilmetil)-piperazina-1-ácido carboxílico (4-cloro-piridin-3-il)- amida o una sal farmacéuticamente aceptable del mismo.

Description

imagen1
imagen2
imagen3
imagen4
imagen5
imagen6
imagen7
imagen8
imagen9
imagen10
imagen11
imagen12
imagen13
imagen14
Tabla 3
Ejemplo 1 (mg/kg p.o.)
Compuesto Comparador HCl (mg/kg p.o.)
10
60 10 60
Mayor reactividad al tacto: ¼) en 180 min.
Sedación : (0/4) Paso anormal: (0/4) Hipotermia: (0/4) Mayor tono muscular abdominal: (1/4) a los 60 min. Mayor reactividad al tacto: (1/4) a los 60 min. (1/4) a los 180 min. Mayor reactividad al tacto: (3/3) en 15 min. Sedación : (3/3) de 15 a 120 min. Paso anormal (rodar): (3/3) a los 15 min. Hipotermia: Inducción ligera de 15 a 60 min y a los 180 min. Menor tono muscular: (1/3) a los 30 min. (3/3) de 60 a 120 min. Mayor reactividad al tacto: (0/3) a los 60 min. Y 180 min.
4-(2,2-difluoro-benzo[1,3]dioxol-5-ilmetil)-piperazina-1-ácido carboxílico (4-cloro-piridin-3-il)-amida hidrocloruro causó efectos excitantes transitorios en solamente una rata con un rango de dosis de 10-60 mg/kg en el Test de Irwin (Tabla 3). En 10 mg/kg 4-(2,2-difluoro-benzo[1,3]dioxol-5-ilmetil)-piperazina-1-ácido carboxílico (4cloro-piridin-3-il)-amida hidrocloruro aumentó la reactividad al tacto en 1 de 4 ratas a los 180 minutos. En 60 mg/kg 4-(2,2-difluoro-benzo[1,3]dioxol-5-ilmetil)-piperazina-1-ácido carboxílico (4-cloro-piridin-3-il)-amida hidrocloruro aumentó el tono muscular abdominal en 1 de 4 ratas a los 60 minutos y aumentó la reactividad al taco en 1 de 4 ratas a los 60 y 180 minutos. Aparte del aumento transitorio y ocasional en el tono muscular abdominal en 60 mg/kg, no se observaron otros signos hasta 24 horas después de la administración.
4-(2,2-difluoro-benzo[1,3]dioxol-5-ilmetil)-piperazina-1-ácido carboxílico (4-cloro-piridin-3-il)-amida hidrocloruro demostró diferenciación favorable de HCL del Compuesto Comparador en el Test de Irwin en ambas dosis. Mientras 4-(2,2-difluoro-benzo[1,3]dioxol-5-ilmetil)-piperazina-1-ácido carboxílico (4-cloro-piridin-3-il)-amida hidrocloruro causó una mayor actividad al tacto en solamente 1 de 4 ratas en 10 mg/kg, HCl del Compuesto Comparador aumentó la actividad al tacto las 3 ratas. En 60 mg/kg, HCL del Compuesto Comparador indujo sedación de 15 a 120 minutos y paso anormal (rodar) a los 15 minutos en las 3 ratas. Redujo el tono muscular en 1 rata a los 30 minutos y a partir de 60 a 120 minutos en las 3 ratas. También indujo hipotermia de 15 a 60 minutos y a los 180 minutos. Estos resultados sugieren la presencia de efectos sedantes/tranquilizantes (sedación, signos motores e hipotermia) para HCl del Compuesto Comparador en 60 mg/kg p.o que no se observaron con 4-(2,2difluoro-benzo[1,3]dioxol-5-ilmetil)-piperazina-1-ácido carboxílico (4-cloro-piridin-3-il)-amida hidrocloruro.
16

Claims (1)

  1. imagen1
ES11719136.1T 2010-05-03 2011-05-02 Moduladores de hidrolasa amida de ácido graso Active ES2483242T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US33052210P 2010-05-03 2010-05-03
US330522P 2010-05-03
PCT/US2011/034755 WO2011139951A1 (en) 2010-05-03 2011-05-02 Modulators of fatty acid amide hydrolase

Publications (1)

Publication Number Publication Date
ES2483242T3 true ES2483242T3 (es) 2014-08-06

Family

ID=44080143

Family Applications (1)

Application Number Title Priority Date Filing Date
ES11719136.1T Active ES2483242T3 (es) 2010-05-03 2011-05-02 Moduladores de hidrolasa amida de ácido graso

Country Status (26)

Country Link
US (2) US8940745B2 (es)
EP (1) EP2566861B1 (es)
JP (1) JP5841128B2 (es)
KR (1) KR101770619B1 (es)
CN (1) CN102869658B (es)
AU (1) AU2011248407B2 (es)
BR (1) BR112012028179A2 (es)
CA (1) CA2797100C (es)
CL (1) CL2012003071A1 (es)
DK (1) DK2566861T3 (es)
EA (1) EA022158B1 (es)
ES (1) ES2483242T3 (es)
HR (1) HRP20140724T1 (es)
IL (1) IL222631A (es)
ME (1) ME01912B (es)
MX (1) MX2012012759A (es)
NZ (1) NZ603175A (es)
PL (1) PL2566861T3 (es)
PT (1) PT2566861E (es)
RS (1) RS53376B (es)
SG (1) SG185411A1 (es)
SI (1) SI2566861T1 (es)
SM (1) SMT201400067B (es)
UA (1) UA108233C2 (es)
WO (1) WO2011139951A1 (es)
ZA (1) ZA201209042B (es)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20180296521A1 (en) * 2015-10-16 2018-10-18 Scythian Biosciences Inc. Methods and compositions for treating gastrointestinal inflammation
WO2017066744A1 (en) * 2015-10-16 2017-04-20 Scythian Biosciences Inc. Methods and compositions for treating traumatic brain injury
CN111743864B (zh) * 2020-08-05 2022-04-01 牡丹江医学院 一种体育外伤喷雾剂及其制备方法

Family Cites Families (54)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS4810160Y1 (es) 1969-10-14 1973-03-16
GB1292410A (en) 1970-05-13 1972-10-11 Yoshitomi Pharmaceutical Thienobenzothiazepine derivatives
JPS5515456A (en) 1978-07-19 1980-02-02 Morishita Seiyaku Kk 2-substituted-piperazinomethyl-1,4-benzodioxane
NZ223847A (en) 1987-04-01 1989-12-21 Janssen Pharmaceutica Nv Substituted piperazine derivatives and pharmaceutical compositions
JPH07502014A (ja) 1991-06-21 1995-03-02 ベーリンガー　マンハイム　イタリア　エス．ピー．エイ． 気道に対して抗喘息性、抗炎症性活性を有する２−アミノ−４−アリール−チアゾール
US5612380A (en) 1994-09-27 1997-03-18 The Scripps Research Institute Method for sleep induction
PL183865B1 (pl) * 1995-01-11 2002-07-31 Samjin Pharmaceutical Co Nowe pochodne piperazyny i środek farmaceutyczny
ZA9610738B (en) 1995-12-22 1997-06-24 Warner Lambert Co Subtype selective nmda receptor ligands and the use thereof
WO1997042230A1 (en) 1996-05-03 1997-11-13 Warner-Lambert Company Rapid purification by polymer supported quench
US5856537A (en) 1996-06-26 1999-01-05 The Scripps Research Institute Inhibitors of oleamide hydrolase
AU6179998A (en) 1997-02-24 1998-09-09 Zymogenetics Inc. Calcitonin mimetics
JPH11139969A (ja) 1997-08-07 1999-05-25 Tanabe Seiyaku Co Ltd 医薬組成物
AU1296799A (en) 1997-11-07 1999-05-31 Schering Corporation Imidazoylalkyl substituted with a five, six or seven membered heterocyclic ring containing one nitrogen atom
ATE319445T1 (de) 1997-11-24 2006-03-15 Scripps Research Inst HEMMER DER ßGAP JUNCTION COMMUNICATIONß
US6268367B1 (en) 1998-02-23 2001-07-31 Zymogenetics, Inc. Piperazine derivatives for treating bone deficit conditions
RU2230740C2 (ru) 1998-03-31 2004-06-20 Акадиа Фармасьютикалз, Инк. Производные азотсодержащих гетероциклических соединений и фармацевтическая композиция на их основе
US6528529B1 (en) 1998-03-31 2003-03-04 Acadia Pharmaceuticals Inc. Compounds with activity on muscarinic receptors
GB9823873D0 (en) 1998-10-30 1998-12-30 Pharmacia & Upjohn Spa 2-ureido-thiazole derivatives,process for their preparation,and their use as antitumour agents
US6100279A (en) 1998-11-05 2000-08-08 Schering Corporation Imidazoylalkyl substituted with a five, six or seven membered heterocyclic ring containing one nitrogen atom
US6387900B1 (en) 1999-08-12 2002-05-14 Pharmacia & Upjohn S.P.A. 3(5)-ureido-pyrazole derivatives process for their preparation and their use as antitumor agents
AU1413301A (en) 1999-11-17 2001-05-30 Sumitomo Pharmaceuticals Company, Limited Diabetic remedy containing dipiperazine derivative
US6462054B1 (en) 2000-03-27 2002-10-08 The Scripps Research Institute Inhibitors of fatty acid amide hydrolase
US6723730B2 (en) 2000-07-20 2004-04-20 Neurogen Corporation Capsaicin receptor ligands
US20020183316A1 (en) 2000-10-27 2002-12-05 Kevin Pan Amidoalkyl-piperidine and amidoalkyl-piperazine derivatives useful for the treatment of nervous system disorders
CA2445294A1 (en) 2001-04-27 2002-11-07 Bristol-Myers Squibb Company Bisarylimidazolyl fatty acid amide hydrolase inhibitors
SK288015B6 (sk) 2001-06-11 2012-11-05 Virochem Pharma Inc. Thiophene derivatives as antiviral agents for flavivirus infection
AU2002363236A1 (en) * 2001-10-30 2003-05-12 Millennium Pharmaceuticals, Inc. Compounds, pharmaceutical compositions and methods of use therefor
AU2002351200A1 (en) 2001-12-03 2003-06-17 Gpc Biotech, Inc. Compositions and methods for inhibiting prenyltransferases
US6727247B2 (en) 2001-12-10 2004-04-27 Hoffman-La Roche Inc. Substituted benzothiazole amide derivatives
AU2003210824A1 (en) 2002-02-08 2003-09-02 Bristol-Myers Squibb Company (oxime)carbamoyl fatty acid amide hydrolase inhibitors
US20040110802A1 (en) 2002-08-23 2004-06-10 Atli Thorarensen Antibacterial benzoic acid derivatives
MXPA05003762A (es) 2002-10-08 2005-07-22 Scripps Research Inst Inhibidores de hidrolasa de amida de acido graso.
FR2850377B1 (fr) 2003-01-23 2009-02-20 Sanofi Synthelabo Derives d'arylalkylcarbamates, leur preparation et leur application en therapeutique
DE10306250A1 (de) 2003-02-14 2004-09-09 Aventis Pharma Deutschland Gmbh Substituierte N-Arylheterozyklen, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
US7223788B2 (en) 2003-02-14 2007-05-29 Sanofi-Aventis Deutschland Gmbh Substituted N-aryl heterocycles, process for their preparation and their use as medicaments
BRPI0408332A (pt) 2003-03-14 2006-03-21 Ono Pharmaceutical Co derivados heterocìclicos contendo nitrogênio e medicamentos contendo os mesmos como ingrediente ativo
US20040191155A1 (en) 2003-03-25 2004-09-30 Mahler Barry Asher Thermal process for reducing the concentration of dinitrogen difluoride and dinitrogen tetrafluoride in nitrogen trifluoride
FR2854633B1 (fr) 2003-05-07 2005-06-24 Sanofi Synthelabo Derives de piperidinyl-et piperazinyl-alkylcarbamates, leur preparation et leur application en therapeutique
ES2307025T3 (es) 2003-06-10 2008-11-16 Janssen Pharmaceutica Nv Combinacion de opioides y un derivado de la piperazina para el tratamiento del dolor.
US7262020B2 (en) 2003-07-03 2007-08-28 The Regents Of The University Of California Methods for comparing relative flux rates of two or more biological molecules in vivo through a single protocol
FR2864080B1 (fr) 2003-12-23 2006-02-03 Sanofi Synthelabo Derives de 1-piperazine-et-1-homopiperazine-carboxylates, leur preparation et leur application en therapeutique
SE0401971D0 (sv) 2004-08-02 2004-08-02 Astrazeneca Ab Piperidne derivatives
ME02222B (me) 2004-12-30 2016-02-20 Janssen Pharmaceutica Nv Amid derivati piperidin-i piperazin-1-karboksilne kiseline te povezani spojevi kao modulatori amid hidrolaze masnih kiselina (faah) za liječenje tjeskobe, boli i drugih stanja
GB0503056D0 (en) 2005-02-14 2005-03-23 Smithkline Beecham Corp Chemical compounds
WO2007005510A1 (en) 2005-06-30 2007-01-11 Janssen Pharmaceutica N.V. N-heteroarylpiperazinyl ureas as modulators of fatty acid amide hydrolase
ITRM20060090A1 (it) 2006-02-22 2007-08-23 Sigma Tau Ind Farmaceuti Nuovi composti inibitori cpt a livello del snc come farmaci antidiabetici e o antiobesita
BRPI0712516A2 (pt) 2006-05-18 2016-08-23 Hoffmann La Roche compostos, composições farmacêuticas, antagonista receptor de a2b, método para uso terapêutico e/ou tratamento profilático e uso de antagonista receptor de a2b
WO2008024139A2 (en) 2006-08-18 2008-02-28 N.V. Organon Inhibitors of fatty acid amide hydrolase
CA2665804A1 (en) * 2006-08-23 2008-02-28 Astellas Pharma Inc. Urea compound or salt thereof
MX2009004233A (es) 2006-10-18 2009-08-12 Pfizer Prod Inc Compuestos de biaril eter urea.
MX2009012765A (es) 2007-05-25 2009-12-16 Janssen Pharmaceutica Nv Moduladores de urea con heteroarilo sustituido de acido graso amida hidrolasa.
MX2010003918A (es) 2007-10-10 2010-08-04 Takeda Pharmaceutical Compuesto de amida.
US8598356B2 (en) 2008-11-25 2013-12-03 Janssen Pharmaceutica Nv Heteroaryl-substituted urea modulators of fatty acid amide hydrolase
US8461159B2 (en) 2008-11-25 2013-06-11 Jannsen Pharmaceutica BV Heteroaryl-substituted urea modulators of fatty acid amide hydrolase

Also Published As

Publication number Publication date
SMT201400067B (it) 2014-07-07
IL222631A (en) 2016-04-21
CN102869658B (zh) 2015-09-02
ME01912B (me) 2014-12-20
KR20130096639A (ko) 2013-08-30
US20150099761A1 (en) 2015-04-09
ZA201209042B (en) 2014-05-28
NZ603175A (en) 2014-05-30
MX2012012759A (es) 2012-12-17
AU2011248407A1 (en) 2012-11-22
SI2566861T1 (sl) 2014-07-31
EA201291155A1 (ru) 2013-08-30
SG185411A1 (en) 2012-12-28
HRP20140724T1 (hr) 2014-08-29
RS53376B (en) 2014-10-31
CA2797100C (en) 2019-01-15
PL2566861T3 (pl) 2014-09-30
CA2797100A1 (en) 2011-11-10
BR112012028179A2 (pt) 2016-08-02
CL2012003071A1 (es) 2013-03-08
CN102869658A (zh) 2013-01-09
EP2566861A1 (en) 2013-03-13
UA108233C2 (uk) 2015-04-10
US9688664B2 (en) 2017-06-27
JP5841128B2 (ja) 2016-01-13
PT2566861E (pt) 2014-07-31
US20130053398A1 (en) 2013-02-28
DK2566861T3 (da) 2014-06-02
EP2566861B1 (en) 2014-05-14
EA022158B1 (ru) 2015-11-30
US8940745B2 (en) 2015-01-27
JP2013534905A (ja) 2013-09-09
IL222631A0 (en) 2012-12-31
KR101770619B1 (ko) 2017-08-23
AU2011248407B2 (en) 2015-07-09
WO2011139951A1 (en) 2011-11-10

Similar Documents

Publication Publication Date Title
EA201391758A1 (ru) Спрессованная сердцевина для фармацевтической композиции, содержащая органические кислоты
UY31639A1 (es) Derivados de amida espirocíclica de fórmula i, sales farmacéuticamente aceptables, composiciones farmacéuticas conteniéndolas, procesos de preparación y aplicaciones
MX2020000268A (es) Agonista de fxr.
MX2013004588A (es) Derivados de triazol y su uso para trastornos neurologicos.
MX2011007737A (es) Derivados de hidroximetil isoxazol como moduladores de acido gamma-aminobutirico a.
HRP20110697T1 (hr) Uporaba flibanserina za liječenje poremećaja seksualne želje u pre-menopauzi
RU2014149337A (ru) Аналоги этомидата с улучшенными фармакокинетическими и фармакодинамическими свойствами
WO2011008298A3 (en) Novel axomadol dosage forms
ES2483242T3 (es) Moduladores de hidrolasa amida de ácido graso
EA200970928A1 (ru) Антагонисты рецептора гонадотропин-рилизин-фактора и способы их применения
EA201390840A1 (ru) Полициклический lpaантагонист и его применение
GEP201606506B (en) Quinoline amide m1 receptor positive allosteric modulators
EA201071035A1 (ru) Фармацевтические композиции модифицированного высвобождения, содержащие микофенолат, и способ их получения
CO6640270A2 (es) Morfolinopirimidad y su uso en terapia
TN2013000293A1 (en) Derivatives of azaindazole or diazaindazole type as medicament
EA201171109A1 (ru) Новая композиция замедленного высвобождения соединений, выбранных из класса миорелаксантов центрального действия
EA201390766A1 (ru) БЕНЗОКСАЗЕПИНЫ КАК ИНГИБИТОРЫ PI3K/mTOR И СПОСОБЫ ИХ ИСПОЛЬЗОВАНИЯ И ПОЛУЧЕНИЯ
MX2011007772A (es) Derivados de isoxazol/o-piridina con enlazador etilo y etenilo.
EA201101147A1 (ru) Новый способ синтеза ивабрадина и его солей присоединения с фармацевтически приемлемой кислотой
RU2014129508A (ru) Новая комбинация
TN2013000257A1 (en) Immunosuppressant formulations
EA201171271A1 (ru) Фармацевтическая композиция в форме частиц с опиоидом и антагонистом опиоида
ES2676198T3 (es) Derivados amino-quinoxalina para el tratamiento de enfermedades neurodegenerativas
EA201291014A1 (ru) Трициклическое индазольное соединение, способ его получения и содержащая его фармацевтическая композиция
EA201391124A1 (ru) Новые бензодиоксолпиперазиновые соединения