AR085099A1 - Derivados de (1,2,4)triazolo[4,3-a]quinoxalina como inhibidores de fosfodiesterasas - Google Patents

Derivados de (1,2,4)triazolo[4,3-a]quinoxalina como inhibidores de fosfodiesterasas

Info

Publication number
AR085099A1
AR085099A1 ARP120100303A ARP120100303A AR085099A1 AR 085099 A1 AR085099 A1 AR 085099A1 AR P120100303 A ARP120100303 A AR P120100303A AR P120100303 A ARP120100303 A AR P120100303A AR 085099 A1 AR085099 A1 AR 085099A1
Authority
AR
Argentina
Prior art keywords
triazolo
quinoxaline
halo
methyl
optionally substituted
Prior art date
Application number
ARP120100303A
Other languages
English (en)
Inventor
Hans Lankau
Barbara Joachim-Langen
Christian Grunwald
Norbert Hfgen
Hans Stange
Rita Dost
Ute Egerland
Original Assignee
Biocrea Gmbh
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 Biocrea Gmbh filed Critical Biocrea Gmbh
Publication of AR085099A1 publication Critical patent/AR085099A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32Alcohol-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34Tobacco-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Addiction (AREA)
  • Diabetes (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Reproductive Health (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Gynecology & Obstetrics (AREA)
  • Psychology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Anesthesiology (AREA)
  • Vascular Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Cardiology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Hospice & Palliative Care (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)

Abstract

La presente se refiere a derivados de (1,2,4)triazolo[4,3-a]quinoxalina que son inhibidores de fosfodiesterasa 2 y/o 10, útiles en el tratamiento de enfermedades del sistema nervioso central.Reivindicación 1: Un compuesto de fórmula (1) o una de sus sales aceptables desde el punto de vista farmacéutico; en donde: R1 representa -fenilo, 2-piridilo, 3-piridilo o 4-piridilo, en cada caso sustituido con un sustituyente diferente de H en una posición orto de la ligadura a la estructura de la cadena principal y en forma opcional sustituido con sustituyentes adicionales diferentes de H; R2 representa hidrógeno, alquilo C1-4, en forma opcional sustituido con hasta 2 halo, por ej., átomos de flúor; R3, R4, R5 y R6 representan, en forma independiente unos de otros hidrógeno, halógeno, alquilo C1-4, en forma opcional sustituido con hasta 5, con preferencia hasta 3 halo, por ej., átomos de flúor, y/o -O(halo)alquilo C1-2, cicloalquilo C3-8, en forma opcional sustituido con halo, -haloalquilo C1-2 y/o O(halo)alquilo C1-2, CN, OH, -O-alquilo C1-4, en forma opcional sustituido con hasta 5, con preferencia hasta 3 halo, por ej., átomos de flúor, y/o -O(halo)alquilo C1-2, cicloalquilo C3-8 en forma opcional sustituido con halo, -haloalquilo C1-2 y/o -O(halo)alquilo C1-2, -O(CH2)n-R10, en donde n puede ser 1 ó 2; R10 representa: un grupo cíclico que puede ser no sustituido o sustituido con preferencia hasta 4 veces por halógeno, alquilo C1-4, en forma opcional sustituido con hasta 5, con preferencia hasta 3 átomos de halógeno, u O-alquilo C1-4, en forma opcional sustituido con hasta 5, con preferencia hasta 3 átomos de halógeno, pero no los siguientes compuestos: 1-(2-hidroxifenil)-4-metil-(1,2,4)triazolo[4,3-a]quinoxalina, 1-(2-clorofenil)-4-metil-(1,2,4)triazolo[4,3-a]quinoxalina, 1-(2-nitrofenil)-4-metil-(1,2,4)triazolo[4,3-a]quinoxalina, 1-(2-metoxifenil)-4-metil-(1,2,4)triazolo[4,3-a]quinoxalina, 1-(5-amino-2-clorofenil)-4-metil-(1,2,4)triazolo[4,3-a]quinoxalina, 1-(5-amino-2-metoxifenil)-4-metil(1,2,4)triazolo[4,3-a]quinoxalina, 1-(5-amino-2-metilfenil)-4-metil-(1,2,4)triazolo[4, 3-a]quinoxalina, o 1-(2-hidroxi-3-metoxifenil)-4-metil-(1,2,4)triazolo[4,3-a]quinoxalina.
ARP120100303A 2011-01-31 2012-01-31 Derivados de (1,2,4)triazolo[4,3-a]quinoxalina como inhibidores de fosfodiesterasas AR085099A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201161437848P 2011-01-31 2011-01-31

Publications (1)

Publication Number Publication Date
AR085099A1 true AR085099A1 (es) 2013-09-11

Family

ID=45833359

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP120100303A AR085099A1 (es) 2011-01-31 2012-01-31 Derivados de (1,2,4)triazolo[4,3-a]quinoxalina como inhibidores de fosfodiesterasas

Country Status (24)

Country Link
US (1) US9540379B2 (es)
EP (1) EP2670754B1 (es)
JP (1) JP6027547B2 (es)
KR (1) KR20140019342A (es)
CN (1) CN103459395A (es)
AR (1) AR085099A1 (es)
AU (1) AU2012213471B2 (es)
BR (1) BR112013019354A2 (es)
CA (1) CA2824929A1 (es)
CL (1) CL2013002003A1 (es)
CO (1) CO6811848A2 (es)
EA (1) EA023792B1 (es)
EC (1) ECSP13012824A (es)
GE (1) GEP20156333B (es)
IL (1) IL226826A (es)
MA (1) MA34844B1 (es)
MX (1) MX2013008667A (es)
PE (1) PE20141023A1 (es)
SG (1) SG192210A1 (es)
TN (1) TN2013000325A1 (es)
TW (1) TWI535718B (es)
UA (1) UA111963C2 (es)
UY (1) UY33888A (es)
WO (1) WO2012104293A1 (es)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA027418B1 (ru) * 2011-06-27 2017-07-31 Янссен Фармацевтика Нв ПРОИЗВОДНЫЕ 1-АРИЛ-4-МЕТИЛ[1,2,4]ТРИАЗОЛО[4,3-a]ХИНОКСАЛИНА, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ, СПОСОБЫ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ ИХ, ПРОМЕЖУТОЧНЫЕ СОЕДИНЕНИЯ
WO2013034755A1 (en) * 2011-09-09 2013-03-14 H. Lundbeck A/S Triazolopyrazine derivatives and their use for treating neurological and psychiatric disorders
WO2013034758A1 (en) * 2011-09-09 2013-03-14 H. Lundbeck A/S Substituted triazolopyrazines and uses thereof
US9056863B2 (en) * 2011-09-09 2015-06-16 H. Lundbeck A/S Substituted 2,3,5,9,9B-pentaazacyclopenta[a]naphthalenes and uses thereof
RU2657540C2 (ru) 2012-06-26 2018-06-14 Янссен Фармацевтика Нв Комбинации, содержащие ингибиторы pde 2, такие как 1-арил-4-метил-[1,2,4]триазоло[4,3-а]хиноксалиновые соединения, и ингибиторы pde 10, для применения в лечении неврологических или метаболических расстройств
US20140045856A1 (en) 2012-07-31 2014-02-13 Boehringer Ingelheim International Gmbh 4-Methyl-2,3,5,9,9b-pentaaza-cyclopenta[a]naphthalenes
WO2014139983A1 (en) 2013-03-13 2014-09-18 H. Lundbeck A/S [1,2,4]triazolo[4,3-a]quinoxalines as dual pde2/pde10 inhibitors
WO2015106032A1 (en) 2014-01-08 2015-07-16 Intra-Cellular Therapies, Inc. Products and pharmaceutical compositions
PL3597649T3 (pl) 2014-04-23 2022-04-04 Dart Neuroscience Llc Kompozycje zawierające podstawione związki [1,2,4]triazolo[1,5-a]pirymidyn-7-ylowe jako inhibitory pde2
EP3215508A1 (en) 2014-11-05 2017-09-13 Dart NeuroScience (Cayman) Ltd. Substituted 5-methyl-[1, 2, 4]triazolo [1,5-a) pyrimidin-2-amine compounds as pde2 inhibitors
MX2017007377A (es) 2014-12-06 2017-11-06 Intra-Cellular Therapies Inc Compuestos organicos.
WO2016090380A1 (en) 2014-12-06 2016-06-09 Intra-Cellular Therapies, Inc. Organic compounds
EP3156405A1 (en) 2015-10-13 2017-04-19 Boehringer Ingelheim International GmbH Spirocyclic ether derivatives of pyrazolo[1,5-a]pyrimidine-3-carboxamide
EP3440071A1 (en) 2016-03-21 2019-02-13 Perlara PBC Fused heterocyclic organic compounds and uses thereof
CN106212487B (zh) * 2016-07-28 2018-11-13 浙江工业大学 一种含甲氧基苯并吡嗪结构的1,2,4-三唑衍生物作为杀菌剂的应用
CA3083176A1 (en) 2017-11-23 2019-05-31 Oslo University Hospital Hf Treatment of tachycardia

Family Cites Families (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5153196A (en) 1991-06-05 1992-10-06 Eli Lilly And Company Excitatory amino acid receptor antagonists and methods for the use thereof
US6235740B1 (en) * 1997-08-25 2001-05-22 Bristol-Myers Squibb Co. Imidazoquinoxaline protein tyrosine kinase inhibitors
DE10108752A1 (de) 2001-02-23 2002-09-05 Bayer Ag Neue Substituierte Imidazotriazinone
JP2006521343A (ja) * 2003-03-27 2006-09-21 ファイザー・プロダクツ・インク 置換4−アミノ[1,2,4]トリアゾロ[4,3−a]キノキサリン
WO2004096220A1 (en) * 2003-04-30 2004-11-11 Merck Frosst Canada Ltd. 8-(3-biaryl)phenylquinoline phosphodiesterase-4-inhibitors
WO2005041957A1 (en) 2003-10-29 2005-05-12 Pfizer Products Inc. Oxindole derivatives and their use as phosphodiesterase type 2 inhibitors
WO2005061497A1 (en) 2003-12-16 2005-07-07 Pfizer Products Inc. Pyrido[2,3-d]pyrimidine-2,4-diamines as pde 2 inhibitors
EP1548011A1 (en) 2003-12-23 2005-06-29 Neuro3D Benzo[1,4]diazepin-2-one derivatives as phosphodiesterase PDE2 inhibitors, preparation and therapeutic use thereof
FR2870539B1 (fr) 2004-05-19 2006-08-04 Greenpharma Sa Sa Nouvelles methodes et medicaments
BRPI0514586A (pt) 2004-09-02 2008-06-17 Altana Pharma Ag triazolftalazinas
AU2006204451C1 (en) 2005-01-05 2012-05-24 Takeda Gmbh Triazolophthalazines as PDE2-inhibitors
KR20070095986A (ko) 2005-01-05 2007-10-01 니코메드 게엠베하 Pde2 억제제로서의 트리아졸로프탈라진
BRPI0502411A (pt) 2005-03-31 2006-11-28 Univ Minas Gerais processo de desenvolvimento de substáncias como inibidores potentes e seletivos de isoformas de fosfodiesterases dos tipos 1 a 5 (pde1,pde2,pde3, pde4, pde5) na base de diocleìna, fluranol ou análogos e suas composições farmacêuticas para o estudo e tratamento de doenças cardiovasculares e produtos associados
CA2636043A1 (en) 2006-01-23 2007-08-02 Amira Pharmaceuticals, Inc. Tricyclic inhibitors of 5-lipoxygenase
WO2007121319A2 (en) 2006-04-14 2007-10-25 University Of California Compostions and methods for determining and predicting treatment responses for depression and anxiety
TW200815436A (en) 2006-05-30 2008-04-01 Elbion Ag 4-amino-pyrido[3,2-e]pyrazines, their use as inhibitors of phosphodiesterase 10, and processes for preparing them
TW200817400A (en) 2006-05-30 2008-04-16 Elbion Ag Pyrido [3,2-e] pyrazines, their use as inhibitors of phosphodiesterase 10, and processes for preparing them
US20080090834A1 (en) 2006-07-06 2008-04-17 Pfizer Inc Selective azole pde10a inhibitor compounds
DE102006048693A1 (de) 2006-10-14 2008-04-17 Bayer Healthcare Ag Inhibition der PDE2A
KR101563103B1 (ko) 2006-12-13 2015-10-23 아스카 세이야쿠 가부시키가이샤 퀴녹살린 유도체
CN101918408A (zh) 2007-11-30 2010-12-15 惠氏有限责任公司 作为磷酸二酯酶10的抑制剂的芳基和杂芳基稠合的咪唑并[1,5-a]吡嗪
WO2009086303A2 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
TWI501965B (zh) 2008-06-20 2015-10-01 Lundbeck & Co As H 作為pde10a酵素抑制劑之新穎苯基咪唑衍生物
KR20110095857A (ko) 2008-09-10 2011-08-25 칼립시스, 인코포레이티드 질환의 치료를 위한 히스타민 수용체의 헤테로시클릭 억제제
WO2010054253A1 (en) 2008-11-07 2010-05-14 Biotie Therapies Gmbh Triazine derivatives as inhibitors of phosphodiesterases
WO2010104933A1 (en) 2009-03-11 2010-09-16 Merck Sharp & Dohme Corp. Inhibitors of akt activity
TW201111383A (en) * 2009-05-29 2011-04-01 Wyeth Llc Substituted imidazo[1,5-a]quinoxalines as inhibitors of phosphodiesterase 10
EP2266985A1 (en) 2009-06-26 2010-12-29 Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts Tricyclic Pyrimidine Derivatives as Wnt antagonists
WO2012096929A2 (en) 2011-01-11 2012-07-19 Sunovion Pharmaceuticals Inc. Heteroaryl compounds and methods of use thereof
EA027418B1 (ru) 2011-06-27 2017-07-31 Янссен Фармацевтика Нв ПРОИЗВОДНЫЕ 1-АРИЛ-4-МЕТИЛ[1,2,4]ТРИАЗОЛО[4,3-a]ХИНОКСАЛИНА, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ, СПОСОБЫ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ ИХ, ПРОМЕЖУТОЧНЫЕ СОЕДИНЕНИЯ
US9056863B2 (en) 2011-09-09 2015-06-16 H. Lundbeck A/S Substituted 2,3,5,9,9B-pentaazacyclopenta[a]naphthalenes and uses thereof
WO2013034758A1 (en) 2011-09-09 2013-03-14 H. Lundbeck A/S Substituted triazolopyrazines and uses thereof
RU2657540C2 (ru) 2012-06-26 2018-06-14 Янссен Фармацевтика Нв Комбинации, содержащие ингибиторы pde 2, такие как 1-арил-4-метил-[1,2,4]триазоло[4,3-а]хиноксалиновые соединения, и ингибиторы pde 10, для применения в лечении неврологических или метаболических расстройств
US20140045856A1 (en) 2012-07-31 2014-02-13 Boehringer Ingelheim International Gmbh 4-Methyl-2,3,5,9,9b-pentaaza-cyclopenta[a]naphthalenes

Also Published As

Publication number Publication date
CN103459395A (zh) 2013-12-18
EA023792B1 (ru) 2016-07-29
US20120302564A1 (en) 2012-11-29
TN2013000325A1 (en) 2015-01-20
ECSP13012824A (es) 2013-10-31
GEP20156333B (en) 2015-07-27
CA2824929A1 (en) 2012-08-09
EP2670754B1 (en) 2017-05-24
WO2012104293A1 (en) 2012-08-09
NZ611630A (en) 2015-03-27
KR20140019342A (ko) 2014-02-14
IL226826A (en) 2016-10-31
UY33888A (es) 2012-08-31
SG192210A1 (en) 2013-09-30
PE20141023A1 (es) 2014-09-04
AU2012213471B2 (en) 2016-07-14
BR112013019354A2 (pt) 2019-09-24
CO6811848A2 (es) 2013-12-16
CL2013002003A1 (es) 2013-12-06
TW201245198A (en) 2012-11-16
US9540379B2 (en) 2017-01-10
EA201300871A1 (ru) 2014-01-30
EP2670754A1 (en) 2013-12-11
MX2013008667A (es) 2013-10-01
AU2012213471A1 (en) 2013-07-04
JP6027547B2 (ja) 2016-11-16
TWI535718B (zh) 2016-06-01
MA34844B1 (fr) 2014-01-02
JP2014503576A (ja) 2014-02-13
UA111963C2 (uk) 2016-07-11

Similar Documents

Publication Publication Date Title
AR085099A1 (es) Derivados de (1,2,4)triazolo[4,3-a]quinoxalina como inhibidores de fosfodiesterasas
AR119698A2 (es) Compuesto amida n-urea sustituida derivado de aminoácido
PE20191613A1 (es) Compuestos de pirazolo[1,5-a]piridina sustituidos como inhibidores de la quinasa ret
AR082799A1 (es) Derivados de quinolina y quinoxalina como inhibidores de quinasa
PE20151860A1 (es) Derivados de 6-(5-hidroxi-1h-pirazol-1-il)nicotinamida y su uso como inhidores de la phd
CY1120826T1 (el) Τριυποκατεστημενα παραγωγα βενζοτριαζολης ως αναστολεις διϋδροοροτικης οξυγενασης
PE20160540A1 (es) Inhibidores de bromodominios
AR076435A1 (es) Compuestos de indazoles sustituidos, composiciones farmaceuticas que los contienen y procesos de obtencion de los mismos
PE20161388A1 (es) Inhibidores de la jak1 para el tratamiento de sindromes mielodisplasicos
AR081978A1 (es) Derivados fusionados de pirimidina para la inhibicion de la actividad quinasa de tirosina
CO6280485A2 (es) Inhibidores de 11-beta hidroxiesteroide deshidrogenasa tipo i de triazolopiridina
PE20150666A1 (es) Inhibidores de serina/treonina cinasa
CO6140024A2 (es) Uso de compuestos inhibidores de quinaxolina de pi3k-alfa para el tratamiento del cancer
CR11757A (es) Compuestos de triazina como inhibidores mtor y quinasa pi3
AR097431A1 (es) Compuestos de carboxamida de furo y tienopiridina útiles como inhibidores de quinasas pim
AR067886A1 (es) Derivados de acido azabifenilaminobenzoico
PE20160932A1 (es) Compuesto de (6s,9as)-n-bencil-6-[(4-hidroxifenil)metil]-4,7-dioxo-8-({6-[3-(piperazin-1-il)azetidin-1-il]piridin-2-il}metil)-2-(prop-2-en-1-il)-octahidro-1h-pirazino[2,1-c][1,2,4]triazina-1-carboxamida
EA201490949A1 (ru) Ингибиторы киназ
EA201100580A1 (ru) Имидазопиридазинкарбонитрилы, используемые в качестве ингибиторов киназы
AR053554A1 (es) Derivados de pirimidina para el tratamiento de trastornos hiperproliferativos
AR083903A1 (es) Derivados de benzooxazol y benzotiazol sulfonamidas, utiles para tratar trastornos del ritmo cardiaco y cancer, composiciones farmaceuticas que los contienen y metodo para prepararlos
CO7131360A2 (es) Novedosas n-piridinil amidas cíclicas sustituidas como inhibidores de quinasa
AR054425A1 (es) Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico.
CU20170026A7 (es) Compuestos derivados de 2-(benzamido/picolinamido/nicotinamido/isonicotinamido)-(2-metil-6-morfolino-(fenil/ (3,4´-bipiridin))-2-il)oxi)etil dihidrógeno fosfato como inhibidores de quinasa raf
IN2014DN07283A (es)

Legal Events

Date Code Title Description
FB Suspension of granting procedure