CO2017012994A2 - Compuestos tricíclicos y su uso como inhibidores de la fosfodiesterasa - Google Patents

Compuestos tricíclicos y su uso como inhibidores de la fosfodiesterasa

Info

Publication number
CO2017012994A2
CO2017012994A2 CONC2017/0012994A CO2017012994A CO2017012994A2 CO 2017012994 A2 CO2017012994 A2 CO 2017012994A2 CO 2017012994 A CO2017012994 A CO 2017012994A CO 2017012994 A2 CO2017012994 A2 CO 2017012994A2
Authority
CO
Colombia
Prior art keywords
compounds
phosphodiesterase inhibitors
tricyclic compounds
formula
methods
Prior art date
Application number
CONC2017/0012994A
Other languages
English (en)
Inventor
Thomas Allen Chappie
Patrick Robert Verhoest
Christopher John Helal
Erik Alphie Lachapelle
Nandini Chaturbhai Patel
Simone Sciabola
Ramalakshmi Yegna Chandrasekaran
Travis T Wager
Original Assignee
Pfizer
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 Pfizer filed Critical Pfizer
Publication of CO2017012994A2 publication Critical patent/CO2017012994A2/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14Ortho-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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • 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
    • A61P25/14Drugs 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
    • A61P25/22Anxiolytics
    • 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
    • A61P27/00Drugs for disorders of the senses
    • 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
    • A61P27/14Decongestants or antiallergics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/22Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed systems contains four or more hetero rings
    • 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
    • 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
    • C07D487/12Heterocyclic 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 three hetero rings
    • C07D487/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/14Ortho-condensed systems
    • C07D491/147Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/22Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D513/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

La presente invención se refiere a compuestos de la Fórmula I: Fórmula I o una sal farmacéuticamente aceptable del mismo, en donde los sustituyentes A, R1, R2, R3a, R3b, R4a, R4b y n son como se define en el presente documento. Las invenciones también se refieren a composiciones farmacéuticas que comprenden los compuestos, métodos de tratamiento que usan los compuestos y métodos de preparación de los compuestos.
CONC2017/0012994A 2015-06-17 2017-12-19 Compuestos tricíclicos y su uso como inhibidores de la fosfodiesterasa CO2017012994A2 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201562180815P 2015-06-17 2015-06-17
PCT/IB2016/053398 WO2016203347A1 (en) 2015-06-17 2016-06-09 Tricyclic compounds and their use as phosphodiesterase inhibitors

Publications (1)

Publication Number Publication Date
CO2017012994A2 true CO2017012994A2 (es) 2018-03-09

Family

ID=56418558

Family Applications (1)

Application Number Title Priority Date Filing Date
CONC2017/0012994A CO2017012994A2 (es) 2015-06-17 2017-12-19 Compuestos tricíclicos y su uso como inhibidores de la fosfodiesterasa

Country Status (29)

Country Link
US (3) US11472805B2 (es)
EP (2) EP3310784B1 (es)
JP (1) JP6827959B2 (es)
KR (2) KR102426986B1 (es)
CN (1) CN107787322B (es)
AU (2) AU2016280137B2 (es)
BR (1) BR112017026191B1 (es)
CA (1) CA2989456C (es)
CO (1) CO2017012994A2 (es)
CR (1) CR20170572A (es)
CU (1) CU20170153A7 (es)
DK (2) DK3766885T3 (es)
DO (1) DOP2017000297A (es)
EA (1) EA039714B1 (es)
EC (1) ECSP18003372A (es)
ES (2) ES2924371T3 (es)
HK (2) HK1245790A1 (es)
HU (2) HUE051898T2 (es)
IL (1) IL255444B (es)
MX (1) MX2017016149A (es)
PE (1) PE20180478A1 (es)
PH (1) PH12017502260A1 (es)
PL (2) PL3310784T3 (es)
PT (2) PT3766885T (es)
SG (1) SG10201912333PA (es)
TN (1) TN2017000485A1 (es)
TW (1) TWI623538B (es)
UA (1) UA125334C2 (es)
WO (1) WO2016203347A1 (es)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016203347A1 (en) * 2015-06-17 2016-12-22 Pfizer Inc. Tricyclic compounds and their use as phosphodiesterase inhibitors
CN109438448B (zh) * 2018-11-07 2021-08-27 成都大学 一种吲哚并七元环化合物及其制备方法和用途
CA3127357A1 (en) * 2019-01-23 2020-07-30 Path Therapeutics, Inc. Methods of treating epilepsy via phosphodiesterase 4 (pde4) inhibition
US11542276B2 (en) * 2019-11-25 2023-01-03 Alkermes, Inc. Substituted macrocyclic compounds and related methods of treatment
US20240009195A1 (en) * 2020-07-26 2024-01-11 Intra-Cellular Therapies, Inc. Novel uses
WO2023076547A1 (en) * 2021-10-29 2023-05-04 Sensorium Therapeutics, Inc. Deuterated forms of alkaloid compounds and therapeutic uses thereof
US11999694B2 (en) 2021-10-29 2024-06-04 Sensorium Therapeutics, Inc. Delivery of therapeutic alkaloid compounds
WO2024118524A1 (en) * 2022-11-28 2024-06-06 Cerevel Therapeutics, Llc Azaindole compounds and their use as phosphodiesterase inhibitors

Family Cites Families (94)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1965980C3 (de) * 1968-02-13 1979-03-01 Sumitomo Chemical Co., Ltd., Osaka (Japan) 2-(2r3-Dioxopiperazino)-benzophenone und Verfahren zu ihrer Herstellung
DE2005845A1 (de) 1969-02-12 1970-09-03 Sumitomo Chemical Company, Ltd., Osaka (Japan) Verfahren zur Herstellung von Benzodiazepinen und ihren Salzen
CH561702A5 (es) 1969-03-11 1975-05-15 Hoffmann La Roche
AT299964B (de) * 1969-04-14 1972-07-10 Sumitomo Chemical Co Verfahren zur Herstellung neuer [2-(Dioxo-piperazino)-benzoyl]-pyridinderivate bzw. von Salzen hievon
DE2144272A1 (en) * 1971-09-03 1972-03-23 Sumitomo Chemical Co Ltd , Osaka (Japan) Nitro-benzodiazepines - prepn from 2-(2,3-diketopiperazino) nitrobenzophenones
US4022778A (en) * 1971-11-05 1977-05-10 American Home Products Corporation 10-Aryl-1,2,3,4-tetrahydropyrazino(1,2-α)indole and derivatives thereof
JPS5033259B2 (es) * 1972-03-31 1975-10-29
DE3065190D1 (en) 1979-11-05 1983-11-10 Beecham Group Plc Enzyme derivatives, and their preparation
ATE239797T1 (de) 1993-01-25 2003-05-15 Takeda Chemical Industries Ltd Antikörper gegen beta-amyloid oder derivative davon und seine verwendung
US5612359A (en) 1994-08-26 1997-03-18 Bristol-Myers Squibb Company Substituted biphenyl isoxazole sulfonamides
TW536540B (en) 1997-01-30 2003-06-11 Bristol Myers Squibb Co Endothelin antagonists: N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]-2-yl]methyl]-N,3,3-trimethylbutanamide and N-(4,5-dimethyl-3-isoxazolyl)-2'-[(3,3-dimethyl-2-oxo-1-pyrrolidinyl)methyl]-4'-(2-oxazolyl)[1,1'-biphe
DE19709877A1 (de) 1997-03-11 1998-09-17 Bayer Ag 1,5-Dihydro-pyrazolo[3,4-d]-pyrimidinon-derivate
JP3816111B2 (ja) 1997-04-09 2006-08-30 インテレクト・ニューロサイエンシズ・インコーポレーテッド β−アミロイド末端に特異的な組換え抗体、それをコードするDNA及びその使用法
US8173127B2 (en) 1997-04-09 2012-05-08 Intellect Neurosciences, Inc. Specific antibodies to amyloid beta peptide, pharmaceutical compositions and methods of use thereof
GB9722520D0 (en) 1997-10-24 1997-12-24 Pfizer Ltd Compounds
TWI239847B (en) 1997-12-02 2005-09-21 Elan Pharm Inc N-terminal fragment of Abeta peptide and an adjuvant for preventing and treating amyloidogenic disease
US6905686B1 (en) 1997-12-02 2005-06-14 Neuralab Limited Active immunization for treatment of alzheimer's disease
ES2318899T3 (es) 1998-07-06 2009-05-01 Bristol-Myers Squibb Company Bifenil sulfonamidas como antagonistas duales de los receptores de angiotensina y endotelina.
IT1313593B1 (it) 1999-08-03 2002-09-09 Novuspharma Spa Derivati di 1,2-diidro-1-oxo-pirazino 1,2-a indolo.
MY125533A (en) 1999-12-06 2006-08-30 Bristol Myers Squibb Co Heterocyclic dihydropyrimidine compounds
BRPI0108676B8 (pt) 2000-02-24 2021-05-25 Lilly Co Eli anticorpos humanizados que sequestram peptídeo amilóide beta e seus usos no tratamento de condições caracterizadas por formação de placas amiloides, bem como composição farmacêutica que compreende os referidos anticorpos
AU2001283955B2 (en) 2000-07-31 2006-05-18 F. Hoffmann-La Roche Ag Piperazine derivatives
DE10045112A1 (de) 2000-09-11 2002-03-21 Merck Patent Gmbh Verwendung von Indolderivaten zur Behandlung von Erkrankungen des zentralen Nervensystems
EP1335738A4 (en) 2000-11-03 2004-09-08 Proteotech Inc METHODS OF ISOLATING AMYLOID INHIBITOR COMPOUNDS AND USE OF COMPOUNDS USED FROM UNCARIA TOMENTOSA AND PARENT PLANTS
CN1633297A (zh) 2001-02-28 2005-06-29 麦克公司 作为黑皮质素-4受体激动剂的酰化哌啶衍生物
EP1406631A4 (en) 2001-06-13 2005-03-23 Univ Michigan DOPAMINE RECEPTOR LIGANDS AND CORRESPONDING THERAPEUTIC METHODS
EP1285922A1 (en) * 2001-08-13 2003-02-26 Warner-Lambert Company 1-Alkyl or 1-cycloalkyltriazolo[4,3-a]quinazolin-5-ones as phosphodiesterase inhibitors
EP1432444A4 (en) 2001-08-17 2005-11-02 Lilly Co Eli ANTI-BETA ANTIBODIES
US20030195205A1 (en) 2001-11-02 2003-10-16 Pfizer Inc. PDE9 inhibitors for treating cardiovascular disorders
FR2832711B1 (fr) 2001-11-26 2004-01-30 Warner Lambert Co Derives de triazolo [4,3-a] pyrido [2,3-d] pyrimidin-5-ones, compositions les contenant, procede de preparation et utilisation
EP1478437B1 (en) 2002-02-27 2005-08-31 Pfizer Products Inc. Acc inhibitors
DE10238723A1 (de) 2002-08-23 2004-03-11 Bayer Ag Phenyl-substituierte Pyrazolyprimidine
DE10238724A1 (de) 2002-08-23 2004-03-04 Bayer Ag Alkyl-substituierte Pyrazolpyrimidine
EP1633786A4 (en) 2002-10-09 2007-07-25 Rinat Neuroscience Corp METHOD FOR TREATING ALZHEIMER DISEASE WITH ANTIBODIES TO AMYLOID BETA PEPTIDE AND COMPOSITIONS THEREOF
FR2853329B1 (fr) 2003-04-02 2006-07-14 Onera (Off Nat Aerospatiale) Procede pour former sur un metal un revetement protecteur contenant de l'aluminium et du zirconium
US20040220186A1 (en) 2003-04-30 2004-11-04 Pfizer Inc. PDE9 inhibitors for treating type 2 diabetes,metabolic syndrome, and cardiovascular disease
BRPI0410630A (pt) 2003-06-19 2006-06-13 Pfizer Prod Inc antagonista de nk1
WO2005025616A1 (ja) 2003-09-09 2005-03-24 Takeda Pharmaceutical Company Limited 抗体の用途
GB0327319D0 (en) 2003-11-24 2003-12-24 Pfizer Ltd Novel pharmaceuticals
BRPI0507374A (pt) 2004-02-02 2007-07-10 Pfizer Prod Inc moduladores do receptor de histamina-3
RU2266906C1 (ru) 2004-04-29 2005-12-27 Общество с ограниченной ответственностью "Исследовательский Институт Химического Разнообразия" (ООО "Исследовательский Институт Химического Разнообразия") Анелированные карбамоилазагетероциклы, способы их получения (варианты), фармацевтическая композиция, фокусированная библиотека
ITMI20040874A1 (it) * 2004-04-30 2004-07-30 Ist Naz Stud Cura Dei Tumori Derivati indolici ed azaindolici con azione antitumorale
US7456164B2 (en) 2004-05-07 2008-11-25 Pfizer, Inc 3- or 4-monosubtituted phenol and thiophenol derivatives useful as H3 ligands
KR100869616B1 (ko) 2004-05-12 2008-11-21 화이자 프로덕츠 인코포레이티드 프롤린 유도체 및 그의 다이펩티딜 펩티다제-iv저해제로서의 용도
EP1595881A1 (en) 2004-05-12 2005-11-16 Pfizer Limited Tetrahydronaphthyridine derivates useful as histamine H3 receptor ligands
JP4069159B2 (ja) 2004-05-25 2008-04-02 ファイザー・プロダクツ・インク テトラアザベンゾ[e]アズレン誘導体及びそれらのアナログ
EP2298807A3 (en) 2004-07-30 2011-05-18 Rinat Neuroscience Corp. Antibodies directed against amyloid-beta peptide and methods using same
GB0423356D0 (en) 2004-10-21 2004-11-24 Merck Sharp & Dohme Therapeutic agents
WO2006069081A2 (en) 2004-12-22 2006-06-29 Washington University In St. Louis USE OF ANTI-Aβ ANTIBODY TO TREAT TRAUMATIC BRAIN INJURY
US20090238761A1 (en) 2005-01-03 2009-09-24 Universita Degli Studi Di Siena Novel Aryl Piperazine Derivatives With Medical Utility
PA8660701A1 (es) 2005-02-04 2006-09-22 Pfizer Prod Inc Agonistas de pyy y sus usos
UY29504A1 (es) 2005-04-29 2006-10-31 Rinat Neuroscience Corp Anticuerpos dirigidos contra el péptido amiloide beta y métodos que utilizan los mismos.
NZ564187A (en) 2005-05-12 2010-03-26 Pfizer Anhydrous crystalline forms of N-[1-(2-ethoxyethyl)-5-(N-ethyl-N-methylamino)-7-(4-methylpyridin-2-yl-amino)-1H-pyrazolo[4,3-d]pyrimidine-3-carbonyl]methanesulfonamide
CA2608672A1 (en) 2005-05-24 2006-11-30 Pharmacia & Upjohn Company Llc Pyridine [3,4-b] pyrazinones as pde-5 inhibitors
WO2006126081A2 (en) 2005-05-24 2006-11-30 Pharmacia & Upjohn Company Llc Pyridino [2 , 3-b] pyrazinones as pde-5 inhibitors
WO2006126083A1 (en) 2005-05-24 2006-11-30 Pharmacia & Upjohn Company Llc Pyridine [3 , 4-b] pyrazinone compounds as pde-5 inhibitors
US7812040B2 (en) 2005-06-22 2010-10-12 Pfizer Inc. Histamine-3 receptor antagonists
US8158673B2 (en) 2005-10-27 2012-04-17 Pfizer Inc. Histamine-3 receptor antagonists
EP1779849A1 (en) 2005-10-28 2007-05-02 Nikem Research S.R.L. V-ATPase inhibitors for the treatment of septic shock
EP1779848A1 (en) 2005-10-28 2007-05-02 Nikem Research S.R.L. V-ATPase inhibitors for the treatment of inflammatory and autoimmune diseases
CA2624625A1 (en) 2005-11-04 2007-05-10 Pfizer Limited Tetrahydronaphthyridine derivative
WO2007063385A2 (en) 2005-12-01 2007-06-07 Pfizer Products Inc. Spirocyclic amine histamine-3 receptor antagonists
WO2007069053A1 (en) 2005-12-14 2007-06-21 Pfizer Products Inc. Benzimidazole antagonists of the h-3 receptor
WO2007088462A1 (en) 2006-02-01 2007-08-09 Pfizer Products Inc. Spirochromane antagonists of the h-3 receptor
WO2007088450A2 (en) 2006-02-01 2007-08-09 Pfizer Products Inc. Chromane antagonist of the h-3 receptor
WO2007099423A1 (en) 2006-03-02 2007-09-07 Pfizer Products Inc. 1-pyrrolidine indane derivatives as histamine-3 receptor antagonists
US20090163482A1 (en) 2006-03-13 2009-06-25 Mchardy Stanton Furst Tetralines antagonists of the h-3 receptor
DK2463283T3 (da) 2006-04-20 2014-08-18 Pfizer Prod Inc Kondenserede heterocykliske phenylamidoforbindelser til forebyggelse og behandling af glucokinase-medierede sygdomme
AU2007242555B2 (en) 2006-04-21 2010-12-16 Pfizer Products Inc. Pyridine[3,4-b]pyrazinones
WO2007138431A2 (en) 2006-05-30 2007-12-06 Pfizer Products Inc. Azabicyclic ether histamine-3 antagonists
EP2097420B1 (en) 2006-11-29 2012-04-04 Pfizer Products Inc. Spiroketone inhibitors of acetyl-coa carboxylase
PT2124933E (pt) 2007-01-22 2013-01-07 Pfizer Prod Inc Sal tosilato de um composto terapêutico e composições farmacêuticas do mesmo
US20090036425A1 (en) 2007-08-02 2009-02-05 Pfizer Inc Substituted bicyclolactam compounds
EA018462B1 (ru) * 2008-01-25 2013-08-30 ХАЙ ПОЙНТ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи ТРИЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ КАК МОДУЛЯТОРЫ СИНТЕЗА TNF-α И КАК ИНГИБИТОРЫ PDE4
US20100137320A1 (en) 2008-02-29 2010-06-03 Schering Corporation Gamma secretase modulators
US8318762B2 (en) 2008-05-28 2012-11-27 Pfizer Inc. Pyrazolospiroketone acetyl-CoA carboxylase inhibitors
CA2724603A1 (en) 2008-05-28 2009-12-03 Pfizer Inc. Pyrazolospiroketone acetyl-coa carboxylase inhibitors
CA2729581A1 (en) 2008-07-29 2010-02-04 Pfizer Inc. Fluorinated heteroaryls
BRPI0918841B8 (pt) 2008-08-28 2021-05-25 Pfizer derivados de dioxa-biciclo[3.2.1]octano-2,3,4-triol, seus cristais, composições farmacêuticas e usos
WO2010086820A1 (en) 2009-02-02 2010-08-05 Pfizer Inc. 4-amino-5-oxo-7, 8-dihydropyrimido [5,4-f] [1,4] oxazepin-6 (5h) -yl) phenyl derivatives, pharmaceutical compositions and uses thereof
US20110319379A1 (en) 2009-03-11 2011-12-29 Corbett Jeffrey W Substituted Indazole Amides And Their Use As Glucokinase Activators
NZ595024A (en) 2009-03-11 2013-01-25 Pfizer Benzofuranyl derivatives used as glucokinase inhibitors
EP2408780A2 (en) 2009-03-20 2012-01-25 Pfizer Inc. 3-oxa-7-azabicycloý3.3.1¨nonanes
JP2012526097A (ja) 2009-05-08 2012-10-25 ファイザー・インク Gpr119調節因子
WO2010128414A1 (en) 2009-05-08 2010-11-11 Pfizer Inc. Gpr 119 modulators
EA020106B1 (ru) 2009-06-05 2014-08-29 Пфайзер Инк. Производные l-(пиперидин-4-ил)пиразола в качестве модуляторов gpr119
WO2011005611A1 (en) 2009-07-09 2011-01-13 Merck Sharp & Dohme Corp. Neuromedin u receptor agonists and uses thereof
AU2013239816B2 (en) * 2012-03-29 2017-08-24 G1 Therapeutics, Inc. Lactam kinase inhibitors
CN104302620A (zh) * 2012-04-26 2015-01-21 弗朗西斯·泽维尔·塔瓦雷斯 内酰胺的合成
MX2015010714A (es) * 2013-02-19 2016-06-14 Pfizer Compuestos de azabencimidazol.
ME03557B (me) 2013-03-15 2020-07-20 G1 Therapeutics Inc Privremena zaštiтa normalnih ćelija током hemoterapije
CN106413623B (zh) 2014-03-21 2020-07-03 阿莱恩技术有限公司 具有弹性体的分段的正畸矫正器
WO2016203347A1 (en) * 2015-06-17 2016-12-22 Pfizer Inc. Tricyclic compounds and their use as phosphodiesterase inhibitors
AU2017223132B2 (en) * 2016-02-23 2019-12-05 Pfizer Inc. 6,7-Dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-2-carboxamide compounds

Also Published As

Publication number Publication date
US20190263816A1 (en) 2019-08-29
KR20200058599A (ko) 2020-05-27
BR112017026191A2 (pt) 2018-08-14
PE20180478A1 (es) 2018-03-07
CR20170572A (es) 2018-03-20
DOP2017000297A (es) 2018-03-15
HK1254661A1 (zh) 2019-07-26
US20230146535A1 (en) 2023-05-11
KR102426986B1 (ko) 2022-07-28
SG10201912333PA (en) 2020-02-27
JP2018521986A (ja) 2018-08-09
PH12017502260A1 (en) 2018-06-11
WO2016203347A1 (en) 2016-12-22
AU2016280137A1 (en) 2017-11-30
HK1245790A1 (zh) 2018-08-31
IL255444B (en) 2021-02-28
ECSP18003372A (es) 2018-07-31
AU2016280137B2 (en) 2021-02-04
PT3766885T (pt) 2022-08-09
EA039714B1 (ru) 2022-03-03
PT3310784T (pt) 2020-11-30
KR20180004817A (ko) 2018-01-12
EP3766885B1 (en) 2022-05-25
CN107787322A (zh) 2018-03-09
ES2924371T3 (es) 2022-10-06
HUE059372T2 (hu) 2022-11-28
IL255444A0 (en) 2017-12-31
TWI623538B (zh) 2018-05-11
EP3310784B1 (en) 2020-10-07
DK3310784T3 (da) 2020-11-09
BR112017026191B1 (pt) 2023-10-10
TW201712013A (zh) 2017-04-01
US11472805B2 (en) 2022-10-18
CU20170153A7 (es) 2018-01-10
CA2989456A1 (en) 2016-12-22
TN2017000485A1 (en) 2019-04-12
PL3766885T3 (pl) 2022-09-19
HUE051898T2 (hu) 2021-03-29
JP6827959B2 (ja) 2021-02-10
AU2021200232A1 (en) 2021-03-18
EP3766885A1 (en) 2021-01-20
DK3766885T3 (da) 2022-08-01
UA125334C2 (uk) 2022-02-23
CN107787322B (zh) 2023-07-07
EP3310784A1 (en) 2018-04-25
PL3310784T3 (pl) 2021-03-08
CA2989456C (en) 2022-01-04
EA201792425A1 (ru) 2018-05-31
US20230002386A1 (en) 2023-01-05
ES2832893T3 (es) 2021-06-11
MX2017016149A (es) 2018-04-18

Similar Documents

Publication Publication Date Title
CO2017012994A2 (es) Compuestos tricíclicos y su uso como inhibidores de la fosfodiesterasa
SV2017005472A (es) Compuestos de triazolopirimidina y usos de los mismos
ECSP20033467A (es) Compuestos macrocíclicos para tratar enfermedades
CO2017012267A2 (es) Compuestos de naftiridina como inhibidores de la quinasa jak
CO2018006475A2 (es) Compuestos que inhiben eif4a y métodos relacionados a los mismos
SV2017005487A (es) Derivados de 4h-pirrol[3,2-c]piridin-4-ona
UY36308A (es) Inhibidores de histona acetiltransferasas espirocíclicas (hat) y métodos para su uso
CR20150628A (es) Derivados de la pirazolopirrolidina y su uso en el tratamiento de enfermedades
UY36342A (es) Nuevos derivados de aminoalquilbenzotiazepinas y usos de los mismos
CU20160192A7 (es) Derivados de indano e indolina útiles como activadores de la guanilato ciclasa soluble
DOP2017000034A (es) Compuestos de imidazopiridazina
CU20160140A7 (es) CROMENE Y 1,1 A,2,7B- tetrahidrociclopropa[C]CROMENE PIRIDOPIRAZINEDIONES COMO MODULADORES DE GAMMA-SECRETASA
MX2020003732A (es) Derivado de anillo fusionado como inhibidor del receptor a2a.
CR20160527A (es) Derivados de carboxamida
DOP2016000297A (es) Composiciones farmacéuticas útiles para tratar enfermedades infecciosas
UY36228A (es) Derivados de heteroarilo como inhibidores de aldosterona sintasa (cyp11b2) y composiciones farmacéuticas que los contienen
DOP2019000100A (es) Derivados de naftiridinona y su uso en el tratamiento de la arritmia
CO2019001644A2 (es) Derivado de triazolopirazinona útil como un inhibidor de pde1 humana
ECSP18056196A (es) Derivados de indano
UY36096A (es) Inhibir el canal de iones del potencial del receptor transitorio a1