BRPI0611095B8 - compostos inibidores de pde1, composição farmacêutica compreendendo-os, usos dos mesmos como inibidores de pde1 para o tratamento de doenças relacionadas, tal como doença de parkinson e deficiência cognitiva, e métodos para produção dos ditos compostos - Google Patents

compostos inibidores de pde1, composição farmacêutica compreendendo-os, usos dos mesmos como inibidores de pde1 para o tratamento de doenças relacionadas, tal como doença de parkinson e deficiência cognitiva, e métodos para produção dos ditos compostos

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Publication number
BRPI0611095B8
BRPI0611095B8 BRPI0611095A BRPI0611095A BRPI0611095B8 BR PI0611095 B8 BRPI0611095 B8 BR PI0611095B8 BR PI0611095 A BRPI0611095 A BR PI0611095A BR PI0611095 A BRPI0611095 A BR PI0611095A BR PI0611095 B8 BRPI0611095 B8 BR PI0611095B8
Authority
BR
Brazil
Prior art keywords
compounds
pde1
parkinson
disease
producing
Prior art date
Application number
BRPI0611095A
Other languages
English (en)
Inventor
Wu Haiyan
Li Peng
Original Assignee
Intracellular Therapies Inc
Takeda Pharmaceuticals Co
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 Intracellular Therapies Inc, Takeda Pharmaceuticals Co filed Critical Intracellular Therapies Inc
Publication of BRPI0611095A2 publication Critical patent/BRPI0611095A2/pt
Publication of BRPI0611095B1 publication Critical patent/BRPI0611095B1/pt
Publication of BRPI0611095B8 publication Critical patent/BRPI0611095B8/pt

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    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • A61P25/14—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
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    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/26—Psychostimulants, e.g. nicotine, cocaine
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    • 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
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    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P25/36—Opioid-abuse
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • 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
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic 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
    • C07D487/14—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
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  • Heart & Thoracic Surgery (AREA)
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  • Pain & Pain Management (AREA)
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  • Endocrinology (AREA)
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  • Anesthesiology (AREA)
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  • Gynecology & Obstetrics (AREA)
  • Otolaryngology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

compostos orgânicos. a invenção fornece novos compostos 7,8-diidros-imidazo[1,2-<244>]pirazol[4,3-e]pirimidin-4-ona e compostos 7,8,9-triidro-[1h ou 2h]-pirimido[1,2-a]pirazol [4,3-e]pirimidin-4 (5h)-ona, substituídos na posição 1 ou 2 com alquila c2-g, cicloalquila c~ 3-9~, heteroarilalquila, ou arilalquila substituída, na forma livre, de sal ou pró-fármaco, processos para sua produção, seu uso como compostos farmacêuticos, particularmente como inibidores de pde1, e composições farmacêuticas compreendendo os mesmos.
BRPI0611095A 2005-06-06 2006-06-06 compostos inibidores de pde1, composição farmacêutica compreendendo-os, usos dos mesmos como inibidores de pde1 para o tratamento de doenças relacionadas, tal como doença de parkinson e deficiência cognitiva, e métodos para produção dos ditos compostos BRPI0611095B8 (pt)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US68771505P 2005-06-06 2005-06-06
US60/687,715 2005-06-06
US60/687.715 2005-06-06
PCT/US2006/022066 WO2006133261A2 (en) 2005-06-06 2006-06-06 Organic compounds

Publications (3)

Publication Number Publication Date
BRPI0611095A2 BRPI0611095A2 (pt) 2010-12-07
BRPI0611095B1 BRPI0611095B1 (pt) 2021-02-02
BRPI0611095B8 true BRPI0611095B8 (pt) 2021-05-25

Family

ID=37499079

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0611095A BRPI0611095B8 (pt) 2005-06-06 2006-06-06 compostos inibidores de pde1, composição farmacêutica compreendendo-os, usos dos mesmos como inibidores de pde1 para o tratamento de doenças relacionadas, tal como doença de parkinson e deficiência cognitiva, e métodos para produção dos ditos compostos

Country Status (10)

Country Link
US (3) US8273750B2 (pt)
EP (1) EP1888534B1 (pt)
JP (3) JP5084725B2 (pt)
KR (2) KR20140022114A (pt)
CN (2) CN103467471A (pt)
AU (1) AU2006255028B2 (pt)
BR (1) BRPI0611095B8 (pt)
CA (1) CA2611312C (pt)
ES (1) ES2645371T3 (pt)
WO (1) WO2006133261A2 (pt)

Families Citing this family (62)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003020702A2 (en) 2001-08-31 2003-03-13 The Rockefeller University Phosphodiesterase activity and regulation of phosphodiesterase 1-b-mediated signaling in brain
WO2006133261A2 (en) 2005-06-06 2006-12-14 Intra-Cellular Therapies, Inc. Organic compounds
US20080194592A1 (en) * 2005-08-23 2008-08-14 Intra-Cellular Therapies, Inc. Organic Compounds
JP5453086B2 (ja) 2006-06-06 2014-03-26 イントラ−セルラー・セラピーズ・インコーポレイテッド 有機化合物
US9198924B2 (en) * 2006-11-13 2015-12-01 Intra-Cellular Therapies, Inc. Organic compounds
EP2089034A4 (en) * 2006-12-05 2010-07-28 Intra Cellular Therapies Inc NEW USES
WO2009073210A1 (en) * 2007-12-06 2009-06-11 Intra-Cellular Therapies, Inc Organic compounds
AU2012204137B2 (en) * 2007-12-06 2015-06-18 Intra-Cellular Therapies, Inc. Organic compounds
CN104370920A (zh) * 2007-12-06 2015-02-25 武田药品工业株式会社 有机化合物
US20120070443A1 (en) * 2008-12-02 2012-03-22 University Of Utah Research Foundation Pde1 as a target therapeutic in heart disease
EA201170772A1 (ru) 2008-12-06 2012-03-30 Интра-Селлулар Терапиз, Инк. Органические соединения
EA201170771A1 (ru) 2008-12-06 2012-01-30 Интра-Селлулар Терапиз, Инк. Органические соединения
WO2010065148A1 (en) * 2008-12-06 2010-06-10 Intra-Cellular Therapies, Inc. Organic compounds
MX2011005935A (es) 2008-12-06 2011-12-16 Intra Cellular Therapies Inc Compuestos organicos.
JP5778582B2 (ja) * 2008-12-06 2015-09-16 イントラ−セルラー・セラピーズ・インコーポレイテッドＩｎｔｒａ−Ｃｅｌｌｕｌａｒ Ｔｈｅｒａｐｉｅｓ， Ｉｎｃ． 有機化合物
BRPI0922700A2 (pt) 2008-12-06 2015-08-11 Intracellular Therapies Inc Compostos orgânicos
EP2400970A4 (en) * 2009-02-25 2012-07-18 Intra Cellular Therapies Inc PDE-1-HEMMER FOR EYE DRESSING
US9468637B2 (en) 2009-05-13 2016-10-18 Intra-Cellular Therapies, Inc. Organic compounds
JP6166534B2 (ja) 2009-08-05 2017-07-19 イントラ−セルラー・セラピーズ・インコーポレイテッドＩｎｔｒａ−Ｃｅｌｌｕｌａｒ Ｔｈｅｒａｐｉｅｓ， Ｉｎｃ． 新規調節タンパク質および阻害剤
JP2013507360A (ja) * 2009-10-08 2013-03-04 イントラ−セルラー・セラピーズ・インコーポレイテッド ホスホジエステラーゼ１−標的トレーサーおよび方法
TW201206937A (en) 2010-05-31 2012-02-16 Intra Cellular Therapies Inc Organic compounds
US9371327B2 (en) 2010-05-31 2016-06-21 Intra-Cellular Therapies, Inc. PDE1 inhibitor compounds
US9434730B2 (en) 2010-05-31 2016-09-06 Intra-Cellular Therapies, Inc. PDE1 inhibitor compounds
US9763948B2 (en) * 2010-05-31 2017-09-19 Intra-Cellular Therapies, Inc. PDE1 inhibitory compounds and methods
WO2012171016A1 (en) * 2011-06-10 2012-12-13 Intra-Cellular Therapies, Inc. Organic compounds
JP2015514135A (ja) * 2012-04-14 2015-05-18 イントラ−セルラー・セラピーズ・インコーポレイテッドＩｎｔｒａ−Ｃｅｌｌｕｌａｒ Ｔｈｅｒａｐｉｅｓ， Ｉｎｃ． 新規組成物および方法
AR091507A1 (es) * 2012-06-21 2015-02-11 Intra Cellular Therapies Inc SALES DE (6aR,9aS)-5,6a,7,8,9,9a-HEXAHIDRO-5-METIL-3-(FENILAMINO)-2-((4-(6-FLUOROPIRIDIN-2-IL)FENIL)METIL)-CICLOPENT[4,5]IMIDAZO[1,2-a]PIRAZOLO[4,3-e]PIRIMIDIN-4(2H)-ONA
CN103012287B (zh) * 2012-12-24 2015-06-17 济南圣泉唐和唐生物科技有限公司 6-氯-3-甲基脲嘧啶的制备方法
WO2014127331A1 (en) 2013-02-17 2014-08-21 Intra-Cellular Therapies, Inc. Novel uses
US9545406B2 (en) 2013-03-15 2017-01-17 Intra-Cellular Therapies, Inc. Method of treating a CNS injury with a PDE1 inhibitor
US9598426B2 (en) 2013-03-15 2017-03-21 Intra-Cellular Therapies, Inc. Organic compounds
KR20160040522A (ko) * 2013-06-21 2016-04-14 인트라-셀룰라 써래피스, 인코퍼레이티드. 유리 염기 결정
EP3091983B1 (en) 2014-01-08 2019-10-02 Intra-Cellular Therapies, Inc. Pharmaceutical compositions comprising a pde-1 inhibitor and a pde-2 inhibitor
US9884872B2 (en) 2014-06-20 2018-02-06 Intra-Cellular Therapies, Inc. Organic compounds
US9938284B2 (en) 2014-08-07 2018-04-10 Intra-Cellular Therapies, Inc. Organic compounds
US10285992B2 (en) 2014-08-07 2019-05-14 Intra-Cellular Therapies, Inc. Combinations of PDE1 inhibitors and NEP inhibitors and associated methods
US9546175B2 (en) 2014-08-07 2017-01-17 Intra-Cellular Therapies, Inc. Organic compounds
WO2016022836A1 (en) * 2014-08-07 2016-02-11 Intra-Cellular Therapies, Inc. Organic compounds
DK3177627T3 (da) * 2014-08-07 2019-10-21 Intra Cellular Therapies Inc Imidazo[1,2-a]-pyrazolo[4,3-e]-pyrimidin-4-on-derivater med pde1-hæmmende aktivitet
IL292225B2 (en) * 2014-09-17 2024-12-01 Intra Cellular Therapies Inc Derivatives of 5,7,7-trimethyl-[2H]-imidazo-[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H)-one and pharmaceutical compositions comprising them.
US10300064B2 (en) 2014-12-06 2019-05-28 Intra-Cellular Therapies, Inc. Organic compounds
AU2015357498B2 (en) 2014-12-06 2019-09-12 Intra-Cellular Therapies, Inc. Organic compounds
WO2016191935A1 (en) * 2015-05-29 2016-12-08 Merck Sharp & Dohme Corp. 6-alkyl dihydropyrazolopyrimidinone compounds as pde2 inhibitors
WO2016192083A1 (en) * 2015-06-04 2016-12-08 Merck Sharp & Dohme Corp. Dihydropyrazolopyrimidinone compounds as pde2 inhibitors
US10682354B2 (en) 2016-03-28 2020-06-16 Intra-Cellular Therapies, Inc. Compositions and methods
JP6996074B2 (ja) * 2016-06-28 2022-01-17 住友ゴム工業株式会社 ゴム組成物およびタイヤ
EP3970719A1 (en) 2016-09-12 2022-03-23 Intra-Cellular Therapies, Inc. Pde1 inhibitor for use in a method of treatment or prophylaxis of inflammation and/or an inflammatory disease or disorder
KR102590848B1 (ko) 2016-12-28 2023-10-19 다트 뉴로사이언스, 엘엘씨 Pde2 억제제로서 치환된 피라졸로피리미디논 화합물
CN109422749B (zh) * 2017-08-21 2023-01-24 重庆医药工业研究院有限责任公司 一种抑制单羧酸转运蛋白的嘧啶二酮衍生物
ES2902365T3 (es) 2017-11-27 2022-03-28 Dart Neuroscience Llc Compuestos de furanopirimidina sustituidos como inhibidores de PDE1
JP7401442B2 (ja) 2018-01-31 2023-12-19 イントラ－セルラー・セラピーズ・インコーポレイテッド 新規使用
KR20210013214A (ko) 2018-05-25 2021-02-03 인트라-셀룰라 써래피스, 인코퍼레이티드. 유기 화합물
US20210338679A1 (en) 2018-09-25 2021-11-04 Intra-Cellular Therapies, Inc. Novel uses
WO2020146384A1 (en) * 2019-01-07 2020-07-16 Intra-Cellular Therapies, Inc. Organic compounds
US11628171B2 (en) 2019-03-13 2023-04-18 Children's Medical Center Corporation Method for treating brain or nerve injury
WO2020210614A1 (en) 2019-04-12 2020-10-15 Intra-Cellular Therapies, Inc. Organic compounds
CN114340636A (zh) 2019-09-03 2022-04-12 细胞内治疗公司 治疗方法
EP4025202A4 (en) * 2019-09-03 2023-08-02 Intra-Cellular Therapies, Inc. NOVEL CONNECTIONS
EP4065573A4 (en) * 2019-11-27 2023-12-27 Intra-Cellular Therapies, Inc. PROCEDURE FOR TREATMENT
US12435093B2 (en) 2020-05-06 2025-10-07 Intra-Cellular Therapies, Inc. Free base crystals
US12364695B2 (en) 2020-06-02 2025-07-22 Intra-Cellular Therapies, Inc. Methods of treating inflammatory disease
EP4188353A4 (en) * 2020-07-26 2024-07-03 Intra-Cellular Therapies, Inc. Novel uses

Family Cites Families (73)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS6032638B2 (ja) 1976-09-01 1985-07-29 武田薬品工業株式会社 ３−アミノピラゾロ〔３，４−ｄ〕ピリミジン誘導体
JPS58500966A (ja) 1981-04-22 1983-06-09 ビイク　グルデン　ロンベルク　ヒエ−ミツシエ　フアブリ−ク　ゲゼルシヤフト　ミツト　ベシユレンクテル　ハフツング 新規ピラゾロ〔３，４−ｄ〕ピリミジン、その製法及びこれを含有する医薬品
US4469868A (en) 1982-05-24 1984-09-04 Warner-Lambert Company Alkylimidazo[1,2-c]pyrazolo[3,4-e]pyrimidines
US4666908A (en) 1985-04-05 1987-05-19 Warner-Lambert Company 5-Substituted pyrazolo[4,3-d]pyrimidine-7-ones and methods of use
KR920004437B1 (ko) 1989-09-12 1992-06-05 삼성전자 주식회사 금전등록기의 거래선 관리방법
ZA914727B (en) * 1990-06-21 1992-03-25 Schering Corp Polycyclic guanine derivatives
US5202328A (en) 1991-03-06 1993-04-13 Merck & Co., Inc. Substituted fused pyrimidinones
US5294612A (en) 1992-03-30 1994-03-15 Sterling Winthrop Inc. 6-heterocyclyl pyrazolo [3,4-d]pyrimidin-4-ones and compositions and method of use thereof
NZ262797A (en) * 1993-02-26 1997-08-22 Schering Corp Polycyclic guanine derivatives, purine and pyrimidine precursors; medicaments
GB9304919D0 (en) 1993-03-10 1993-04-28 Celltech Ltd Chemical compounds
GB9315017D0 (en) 1993-07-20 1993-09-01 Glaxo Lab Sa Chemical compounds
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
US5824683A (en) * 1995-11-28 1998-10-20 Schering Corporation 2'- 4'-halo- 1,1'-biphenyl!-4-yl!methyl!-5'-methyl-spiro cyclopentane-1,7' (8'H)- 3H! imidazo 2,1-b!purin!-4' (5'H)-ones
GB9526245D0 (en) 1995-12-21 1996-02-21 Celltech Therapeutics Ltd Chemical compounds
GB9622363D0 (en) 1996-10-28 1997-01-08 Celltech Therapeutics Ltd Chemical compounds
AU5330698A (en) 1996-12-23 1998-07-17 Celltech Therapeutics Limited Fused polycyclic 2-aminopyrimidine derivatives, their preparation and their use as protein tyrosine kinase inhibitors
SE9701398D0 (sv) 1997-04-15 1997-04-15 Astra Pharma Prod Novel compounds
IT1291372B1 (it) 1997-05-21 1999-01-07 Schering Plough S P A Uso di analoghi eterociclici di 1,2,4-triazolo (1,5-c) pirimidine per la preparazione di medicamenti utili per il trattamento delle malattie
JP3391466B2 (ja) 1997-06-13 2003-03-31 アースロケア コーポレイション 閉塞した体内管腔の再疎通のための電気外科のカテーテルシステム及びカテーテル
US6013621A (en) 1997-10-17 2000-01-11 The Rockfeller University Method of treating psychosis and/or hyperactivity
GB9722520D0 (en) 1997-10-24 1997-12-24 Pfizer Ltd Compounds
AU3053999A (en) 1998-03-31 1999-10-25 Kyowa Hakko Kogyo Co. Ltd. Nitrogenous heterocyclic compounds
US6133273A (en) 1998-05-08 2000-10-17 American Home Products Corporation Pyrazolopyrimidine-2,4-dione sulfonamides
GB9907658D0 (en) 1999-04-06 1999-05-26 Zeneca Ltd Chemical compounds
JP2003503354A (ja) 1999-06-30 2003-01-28 メルク エンド カムパニー インコーポレーテッド Ｓｒｃキナーゼ阻害剤化合物
AU5636900A (en) 1999-06-30 2001-01-31 Merck & Co., Inc. Src kinase inhibitor compounds
DE19931206A1 (de) * 1999-07-07 2001-01-11 Stief Christian Arzneimittel zur Erhöhung des cAMP-Spiegels und deren Verwendung
BR0013899A (pt) 1999-09-10 2003-07-08 Merck & Co Inc Composto, composição farmacêutica, processos de tratamento ou prevenção de câncer, de uma doença em que a angiogênese esteja implicada, da vascularização retinal, da retinopatia diabética, da degeneração macular relacionada a idade, de doenças inflamatórias, de uma doença ou condições dependentes da tirosina quinase, de patologias associadas com ossos, e, processos para produzir uma composição farmacêutica, e de reduzir ou prevenir dano tecidual em seguida a um evento isquêmico cerebral
KR20020047198A (ko) 1999-09-30 2002-06-21 해피 페너 ; 해리 에이치. 페너 2세 특정 알킬렌 디아민-치환된피라졸로[1,5-ａ]-1,5-피리미딘 및피라졸로[1,5-ａ]-1,3,5-트리아진
TWI265925B (en) 1999-10-11 2006-11-11 Pfizer Pyrazolo[4,3-d]pyrimidin-7-ones useful in inhibiting type 5 cyclic guanosine 3',5'-monophosphate phosphodiesterases(cGMP PDE5), process and intermediates for their preparation, their uses and composition comprising them
EP1222190A1 (en) 1999-10-11 2002-07-17 Pfizer Limited 5-(2-substituted-5-heterocyclylsulphonylpyrid-3-yl)-dihydropyrazolo[4,3-d]pyrimidin-7-ones as phosphodiesterase inhibitors
IL139073A0 (en) 1999-10-21 2001-11-25 Pfizer Treatment of neuropathy
MY125533A (en) 1999-12-06 2006-08-30 Bristol Myers Squibb Co Heterocyclic dihydropyrimidine compounds
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
CA2407031A1 (en) 2000-04-19 2001-10-25 Lilly Icos Llc Use of cyclic gmp-specific phosphodiesterase inhibitors for treatment of parkinson's disease
US6693099B2 (en) 2000-10-17 2004-02-17 The Procter & Gamble Company Substituted piperazine compounds optionally containing a quinolyl moiety for treating multidrug resistance
ATE298238T1 (de) 2001-03-16 2005-07-15 Pfizer Pyrazolo(4,3-d)pyrimidinon-verbindungen als cgmp pde-inhibitoren
WO2002088079A2 (en) 2001-05-01 2002-11-07 Bristol-Myers Squibb Company Dual inhibitors of pde 7 and pde 4
SE0102315D0 (sv) 2001-06-28 2001-06-28 Astrazeneca Ab Compounds
MXPA04001891A (es) 2001-08-28 2004-06-15 Schering Corp Inhibidores policiclicos de guanina fosfodiesterasa v.
WO2003020702A2 (en) 2001-08-31 2003-03-13 The Rockefeller University Phosphodiesterase activity and regulation of phosphodiesterase 1-b-mediated signaling in brain
WO2003042216A1 (en) 2001-11-09 2003-05-22 Schering Corporation Polycyclic guanine derivative phosphodiesterase v inhibitors
WO2003070174A2 (en) 2002-02-15 2003-08-28 Sympore Gmbh Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof
US20050153372A1 (en) 2002-02-21 2005-07-14 Paul Greengard Compositions and method for regulation of calcium-dependent signaling in brain
GB0230045D0 (en) 2002-12-23 2003-01-29 Glaxo Group Ltd Compounds
WO2004087906A1 (en) 2003-03-31 2004-10-14 Pfizer Products Inc. Crystal structure of 3',5'-cyclic nucleotide phosphodiesterase 1b (pde1b) and uses thereof
EA200501548A1 (ru) 2003-04-01 2006-02-24 Апплайд Резеч Системз Арс Холдинг Н.В. Ингибиторы фосфодиэстераз при бесплодии
BRPI0414087A (pt) 2003-09-05 2006-10-31 Neurogen Corp composto, métodos para tratar um distúrbio, para demostrar a presença de receptores de crf em amostras de célula ou tecido, e para inibir a ligação de crf a um receptor de crf1, composição farmacêutica, e, embalagem
WO2006133261A2 (en) * 2005-06-06 2006-12-14 Intra-Cellular Therapies, Inc. Organic compounds
US20080194592A1 (en) 2005-08-23 2008-08-14 Intra-Cellular Therapies, Inc. Organic Compounds
JP5453086B2 (ja) 2006-06-06 2014-03-26 イントラ−セルラー・セラピーズ・インコーポレイテッド 有機化合物
US20070286890A1 (en) 2006-06-07 2007-12-13 John Garnett Walt Eyelash applicator and method
US9198924B2 (en) 2006-11-13 2015-12-01 Intra-Cellular Therapies, Inc. Organic compounds
EP2089034A4 (en) 2006-12-05 2010-07-28 Intra Cellular Therapies Inc NEW USES
CN104370920A (zh) 2007-12-06 2015-02-25 武田药品工业株式会社 有机化合物
WO2009073210A1 (en) 2007-12-06 2009-06-11 Intra-Cellular Therapies, Inc Organic compounds
JPWO2009107578A1 (ja) 2008-02-25 2011-06-30 佐藤　謙治 音響装置
EA201170772A1 (ru) 2008-12-06 2012-03-30 Интра-Селлулар Терапиз, Инк. Органические соединения
EA201170771A1 (ru) 2008-12-06 2012-01-30 Интра-Селлулар Терапиз, Инк. Органические соединения
BRPI0922700A2 (pt) 2008-12-06 2015-08-11 Intracellular Therapies Inc Compostos orgânicos
MX2011005935A (es) 2008-12-06 2011-12-16 Intra Cellular Therapies Inc Compuestos organicos.
WO2010065148A1 (en) 2008-12-06 2010-06-10 Intra-Cellular Therapies, Inc. Organic compounds
JP5778582B2 (ja) 2008-12-06 2015-09-16 イントラ−セルラー・セラピーズ・インコーポレイテッドＩｎｔｒａ−Ｃｅｌｌｕｌａｒ Ｔｈｅｒａｐｉｅｓ， Ｉｎｃ． 有機化合物
EP2400970A4 (en) 2009-02-25 2012-07-18 Intra Cellular Therapies Inc PDE-1-HEMMER FOR EYE DRESSING
US9468637B2 (en) 2009-05-13 2016-10-18 Intra-Cellular Therapies, Inc. Organic compounds
JP2013507360A (ja) 2009-10-08 2013-03-04 イントラ−セルラー・セラピーズ・インコーポレイテッド ホスホジエステラーゼ１−標的トレーサーおよび方法
TW201206937A (en) 2010-05-31 2012-02-16 Intra Cellular Therapies Inc Organic compounds
US9371327B2 (en) 2010-05-31 2016-06-21 Intra-Cellular Therapies, Inc. PDE1 inhibitor compounds
US9763948B2 (en) 2010-05-31 2017-09-19 Intra-Cellular Therapies, Inc. PDE1 inhibitory compounds and methods
US9434730B2 (en) 2010-05-31 2016-09-06 Intra-Cellular Therapies, Inc. PDE1 inhibitor compounds
WO2012171016A1 (en) 2011-06-10 2012-12-13 Intra-Cellular Therapies, Inc. Organic compounds
AR091507A1 (es) 2012-06-21 2015-02-11 Intra Cellular Therapies Inc SALES DE (6aR,9aS)-5,6a,7,8,9,9a-HEXAHIDRO-5-METIL-3-(FENILAMINO)-2-((4-(6-FLUOROPIRIDIN-2-IL)FENIL)METIL)-CICLOPENT[4,5]IMIDAZO[1,2-a]PIRAZOLO[4,3-e]PIRIMIDIN-4(2H)-ONA
US9598426B2 (en) 2013-03-15 2017-03-21 Intra-Cellular Therapies, Inc. Organic compounds

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WO2006133261A3 (en) 2007-06-21
CA2611312C (en) 2013-12-03
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JP2012180369A (ja) 2012-09-20
EP1888534A2 (en) 2008-02-20
CN101248050B (zh) 2013-07-17
JP2015007121A (ja) 2015-01-15
US20080188492A1 (en) 2008-08-07
US9624230B2 (en) 2017-04-18
KR101478368B1 (ko) 2014-12-31
JP5084725B2 (ja) 2012-11-28
US8273750B2 (en) 2012-09-25
CN101248050A (zh) 2008-08-20
BRPI0611095A2 (pt) 2010-12-07
JP5649614B2 (ja) 2015-01-07
US9000001B2 (en) 2015-04-07
WO2006133261A2 (en) 2006-12-14
AU2006255028B2 (en) 2012-04-19
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US20150197528A1 (en) 2015-07-16
US20130018063A1 (en) 2013-01-17
EP1888534A4 (en) 2010-06-16
CN103467471A (zh) 2013-12-25
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