CN101248050B - 有机化合物 - Google Patents

有机化合物 Download PDF

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Publication number
CN101248050B
CN101248050B CN2006800269736A CN200680026973A CN101248050B CN 101248050 B CN101248050 B CN 101248050B CN 2006800269736 A CN2006800269736 A CN 2006800269736A CN 200680026973 A CN200680026973 A CN 200680026973A CN 101248050 B CN101248050 B CN 101248050B
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China
Prior art keywords
compound
formula
methyl
pyrazolo
disease
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Chinese (zh)
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CN101248050A (zh
Inventor
P·李
H·吴
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Intra Cellular Therapies Inc
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Takeda Pharmaceutical Co Ltd
Intra Cellular Therapies Inc
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    • 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
    • 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
    • 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
    • A61P25/26—Psychostimulants, e.g. nicotine, cocaine
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • 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
    • 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
    • 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
    • A61P9/10—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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Addiction (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Psychology (AREA)
  • Reproductive Health (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Hospice & Palliative Care (AREA)
  • Anesthesiology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Otolaryngology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN2006800269736A 2005-06-06 2006-06-06 有机化合物 Active CN101248050B (zh)

Applications Claiming Priority (3)

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

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN2013102507232A Division CN103467471A (zh) 2005-06-06 2006-06-06 有机化合物

Publications (2)

Publication Number Publication Date
CN101248050A CN101248050A (zh) 2008-08-20
CN101248050B true CN101248050B (zh) 2013-07-17

Family

ID=37499079

Family Applications (2)

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CN2006800269736A Active CN101248050B (zh) 2005-06-06 2006-06-06 有机化合物
CN2013102507232A Pending CN103467471A (zh) 2005-06-06 2006-06-06 有机化合物

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN2013102507232A Pending CN103467471A (zh) 2005-06-06 2006-06-06 有机化合物

Country Status (10)

Country Link
US (3) US8273750B2 (enExample)
EP (1) EP1888534B1 (enExample)
JP (3) JP5084725B2 (enExample)
KR (2) KR20140022114A (enExample)
CN (2) CN101248050B (enExample)
AU (1) AU2006255028B2 (enExample)
BR (1) BRPI0611095B8 (enExample)
CA (1) CA2611312C (enExample)
ES (1) ES2645371T3 (enExample)
WO (1) WO2006133261A2 (enExample)

Families Citing this family (59)

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CA2459161A1 (en) 2001-08-31 2003-03-13 The Rockefeller University Phosphodiesterase activity and regulation of phosphodiesterase 1b-mediated signaling in brain
CN101248050B (zh) 2005-06-06 2013-07-17 武田药品工业株式会社 有机化合物
EP1919287A4 (en) * 2005-08-23 2010-04-28 Intra Cellular Therapies Inc ORGANIC COMPOUNDS FOR TREATING A REDUCED DOPAMINE RECEPTOR SIGNALING ACTIVITY
KR20090042227A (ko) 2006-06-06 2009-04-29 인트라-셀룰라 써래피스, 인코퍼레이티드. 유기 화합물
WO2008063505A1 (en) * 2006-11-13 2008-05-29 Intra-Cellular Therapies, Inc. Organic compounds
US9006258B2 (en) * 2006-12-05 2015-04-14 Intra-Cellular Therapies, Inc. Method of treating female sexual dysfunction with a PDE1 inhibitor
AU2008331833A1 (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
WO2009075784A1 (en) * 2007-12-06 2009-06-18 Intra-Cellular Therapies, Inc. Organic compounds
US20120070443A1 (en) * 2008-12-02 2012-03-22 University Of Utah Research Foundation Pde1 as a target therapeutic in heart disease
EP2358204B1 (en) * 2008-12-06 2015-08-05 Intra-Cellular Therapies, Inc. 4,5,7,8-tetrahydro-4-oxo-2H-imidazo[1,2-a]pyrrolo[3,4-e]pyrimidine compounds as PDE1 inhibitors.
EP2367429B1 (en) * 2008-12-06 2017-06-07 Intra-Cellular Therapies, Inc. Organic compounds
KR20110098731A (ko) 2008-12-06 2011-09-01 인트라-셀룰라 써래피스, 인코퍼레이티드. 유기 화합물
CN102223799A (zh) 2008-12-06 2011-10-19 细胞内治疗公司 有机化合物
CN102232077A (zh) 2008-12-06 2011-11-02 细胞内治疗公司 有机化合物
WO2010065147A1 (en) * 2008-12-06 2010-06-10 Intra-Cellular Therapies, Inc. Organic compounds
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
WO2011016861A2 (en) 2009-08-05 2011-02-10 Intra-Cellular Therapies, Inc. Novel regulatory proteins and inhibitors
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
WO2011153135A1 (en) 2010-05-31 2011-12-08 Intra-Cellular Therapies, Inc. Organic compounds
TW201206937A (en) 2010-05-31 2012-02-16 Intra Cellular Therapies Inc Organic compounds
JP5911854B2 (ja) * 2010-05-31 2016-04-27 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
JP5879336B2 (ja) 2010-05-31 2016-03-08 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
US10561656B2 (en) 2011-06-10 2020-02-18 Intra-Cellular Therapies, Inc. Organic compounds
MX2014012374A (es) * 2012-04-14 2015-04-17 Intra Cellular Therapies Inc Compuestos organicos.
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
US9801882B2 (en) 2013-02-17 2017-10-31 Intra-Cellular Therapies, Inc. Phosphodiesterase-1 inhibitors and their use in treatment of cardiovascular diseases
ES2836129T3 (es) * 2013-03-15 2021-06-24 Intra Cellular Therapies Inc Compuestos orgánicos
EP2968338B1 (en) 2013-03-15 2019-01-09 Intra-Cellular Therapies, Inc. Pde1 inhibitors for use in the treatment and/or prevention of cns injuries, and pns diseases, disorders or injuries
EP3010509B1 (en) * 2013-06-21 2021-07-28 Intra-Cellular Therapies, Inc. Free base crystals
JP6696904B2 (ja) * 2014-01-08 2020-05-20 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． 製剤および医薬組成物
US9884872B2 (en) 2014-06-20 2018-02-06 Intra-Cellular Therapies, Inc. Organic compounds
ES2745819T3 (es) * 2014-08-07 2020-03-03 Intra Cellular Therapies Inc Derivados de imidazo[1,2-a]-pirazolo[4,3-e]-pirimidin-4-ona con actividad inhibidora de la PDE1
US10005789B2 (en) 2014-08-07 2018-06-26 Intra-Cellular Therapies, Inc. Organic compounds
US9546175B2 (en) 2014-08-07 2017-01-17 Intra-Cellular Therapies, Inc. Organic compounds
WO2016022825A1 (en) * 2014-08-07 2016-02-11 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
EP3193878B1 (en) * 2014-09-17 2021-01-06 Intra-Cellular Therapies, Inc. 7,8-dihydro-[2h]-imidazo-[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5h)-one derivatives as phosphodiesterase 1 (pde1) inhibitors for treating diseases, disorders or injuries of the central nervous system (cns)
HK1243935A1 (zh) 2014-12-06 2018-07-27 Intra-Cellular Therapies, Inc. 有机化合物
HK1243936A1 (zh) 2014-12-06 2018-07-27 Intra-Cellular Therapies, Inc. 有机化合物
WO2016191935A1 (en) * 2015-05-29 2016-12-08 Merck Sharp & Dohme Corp. 6-alkyl dihydropyrazolopyrimidinone compounds as pde2 inhibitors
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JP2019510039A (ja) * 2016-03-28 2019-04-11 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
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
JP7134168B6 (ja) 2016-09-12 2024-02-02 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
AU2017388054B2 (en) 2016-12-28 2022-03-24 Dart Neuroscience, Llc Substituted pyrazolopyrimidinone compounds as PDE2 inhibitors
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
CA3120971A1 (en) 2017-11-27 2019-05-31 Dart Neuroscience, Llc Substituted furanopyrimidine compounds as pde1 inhibitors
EP3746081A4 (en) 2018-01-31 2021-10-27 Intra-Cellular Therapies, Inc. Novel uses
CN112189013A (zh) 2018-05-25 2021-01-05 细胞内治疗公司 有机化合物
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
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US20230355625A1 (en) * 2019-11-27 2023-11-09 Intra-Cellular Therapies, Inc. Methods of 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
JP2023535224A (ja) * 2020-07-26 2023-08-16 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

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