CN1575191A - 用pde9抑制剂治疗胰岛素耐受性综合征和ⅱ型糖尿病 - Google Patents

用pde9抑制剂治疗胰岛素耐受性综合征和ⅱ型糖尿病 Download PDF

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Publication number
CN1575191A
CN1575191A CNA028211529A CN02821152A CN1575191A CN 1575191 A CN1575191 A CN 1575191A CN A028211529 A CNA028211529 A CN A028211529A CN 02821152 A CN02821152 A CN 02821152A CN 1575191 A CN1575191 A CN 1575191A
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alkyl
phenyl
group
halogen
heteroaryl
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Chinese (zh)
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戴维·A·弗赖伯格
厄尔·M·吉布斯
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Pfizer Products Inc
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Pfizer Products Inc
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • 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
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
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    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CNA028211529A 2001-11-02 2002-09-12 用pde9抑制剂治疗胰岛素耐受性综合征和ⅱ型糖尿病 Pending CN1575191A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US33698101P 2001-11-02 2001-11-02
US60/336,981 2001-11-02

Publications (1)

Publication Number Publication Date
CN1575191A true CN1575191A (zh) 2005-02-02

Family

ID=23318571

Family Applications (1)

Application Number Title Priority Date Filing Date
CNA028211529A Pending CN1575191A (zh) 2001-11-02 2002-09-12 用pde9抑制剂治疗胰岛素耐受性综合征和ⅱ型糖尿病

Country Status (13)

Country Link
US (2) US6967204B2 (https=)
EP (1) EP1444009A1 (https=)
JP (1) JP2005508978A (https=)
KR (1) KR20040053210A (https=)
CN (1) CN1575191A (https=)
BR (1) BR0213817A (https=)
CA (1) CA2465632A1 (https=)
HU (1) HUP0401998A2 (https=)
IL (1) IL161155A0 (https=)
MX (1) MXPA04004170A (https=)
PL (1) PL370599A1 (https=)
WO (1) WO2003037432A1 (https=)
ZA (1) ZA200402173B (https=)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103313988A (zh) * 2010-09-20 2013-09-18 英维沃医药有限公司 咪唑并三嗪酮化合物
CN104093720A (zh) * 2012-01-26 2014-10-08 H.隆德贝克有限公司 具有咪唑并三嗪酮骨架的pde9抑制剂
CN111183140A (zh) * 2017-05-26 2020-05-19 伊马拉公司 制备和使用pde9抑制剂的方法
US11608342B2 (en) 2015-07-07 2023-03-21 H. Lundbeck A/S PDE9 inhibitors with imidazo triazinone backbone and imidazo pyrazinone backbone for treatment of peripheral diseases

Families Citing this family (79)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL160307A0 (en) 2001-08-31 2004-07-25 Univ Rockefeller Phosphodiesterase activity and regulation of phosphodiesterase 1-b-mediated signaling in brain
JP2005508978A (ja) * 2001-11-02 2005-04-07 ファイザー・プロダクツ・インク Ｐｄｅ９阻害薬によるインスリン抵抗性症候群及び２型糖尿病の治療
US20030195205A1 (en) * 2001-11-02 2003-10-16 Pfizer Inc. PDE9 inhibitors for treating cardiovascular disorders
CA2468156A1 (en) 2001-12-06 2003-06-19 Merck & Co., Inc. Azolopyrimidinone compounds and their use
ES2280596T3 (es) * 2001-12-29 2007-09-16 Novo Nordisk A/S Uso combinado de un compuesto de glp-1 y un inhibidor de una aldosa reductasa.
IS1935B (is) * 2002-03-19 2004-06-16 Actavis Group Hf. Fósínópríl lyfjasamsetning
ATE478872T1 (de) * 2002-03-28 2010-09-15 Ustav Ex Botan Av Cr V V I I O Pyrazoloä4,3-düpyrimidine, verfahren zu ihrer herstellung und therapeutische anwendung
DE10238724A1 (de) * 2002-08-23 2004-03-04 Bayer Ag Alkyl-substituierte Pyrazolpyrimidine
DE10238723A1 (de) * 2002-08-23 2004-03-11 Bayer Ag Phenyl-substituierte Pyrazolyprimidine
DE10238722A1 (de) 2002-08-23 2004-03-11 Bayer Ag Selektive Phosphodiesterase 9A-Inhibitoren als Arzneimittel zur Verbesserung kognitiver Prozesse
US20040220186A1 (en) * 2003-04-30 2004-11-04 Pfizer Inc. PDE9 inhibitors for treating type 2 diabetes,metabolic syndrome, and cardiovascular disease
DE10320785A1 (de) * 2003-05-09 2004-11-25 Bayer Healthcare Ag 6-Arylmethyl-substituierte Pyrazolopyrimidine
DE102004004142A1 (de) * 2003-05-09 2004-11-25 Bayer Healthcare Ag 6-Cyclylmethyl- und 6-Alkylmethyl-substituierte Pyrazolopyrimidine
US8044060B2 (en) 2003-05-09 2011-10-25 Boehringer Ingelheim International Gmbh 6-cyclylmethyl- and 6-alkylmethyl pyrazolo[3,4-D]pyrimidines, methods for their preparation and methods for their use to treat impairments of perception, concentration learning and/or memory
WO2004099211A1 (de) * 2003-05-09 2004-11-18 Bayer Healthcare Ag 6-cyclylmethyl- und 6-alkylmethyl-substituierte pyrazolopyrimidine
WO2005041972A1 (en) * 2003-10-31 2005-05-12 Pfizer Products Inc. Phosphodiesterase 9 inhibition as treatment for obesity-related conditions
EP1734963A4 (en) 2004-04-02 2008-06-18 Merck & Co Inc METHOD FOR TREATING PEOPLE WITH METABOLIC AND ANTHROPOMETRIC DISORDER
WO2005105780A2 (en) * 2004-04-28 2005-11-10 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of rock and other protein kinases
AU2005245240B2 (en) * 2004-05-20 2010-04-29 Scimar Ltd. Use of drug combinations for treating insulin resistance
CA2612176C (en) 2005-06-14 2015-02-17 Aska Pharmaceutical Co., Ltd. Dihydrothieno[2,3-d]pyramidine-6-carboxylic acid derivatives as pde9 inhibitors
US20080194592A1 (en) * 2005-08-23 2008-08-14 Intra-Cellular Therapies, Inc. Organic Compounds
AU2007282678B2 (en) * 2006-08-08 2012-09-27 Aska Pharmaceutical Co., Ltd. Quinazoline derivative
WO2008028914A1 (en) 2006-09-07 2008-03-13 Nycomed Gmbh Combination treatment for diabetes mellitus
AU2007299920A1 (en) * 2006-09-19 2008-03-27 Braincells, Inc. PPAR Mediated Modulation of Neurogenesis
US8299080B2 (en) 2006-12-13 2012-10-30 Aska Pharmaceutical Co., Ltd. Substituted imidazo[1,5-A] quinoxalines as a PDE9 inhibitor
WO2008072778A1 (ja) 2006-12-13 2008-06-19 Aska Pharmaceutical Co., Ltd. 尿路系疾患の処置剤
ITMI20070140A1 (it) * 2007-01-30 2008-07-31 Campagnolo Srl Dispositivo di interazione uomo-bicicletta
US20100144864A1 (en) * 2007-04-05 2010-06-10 Ironwood Pharmaceuticals, Inc. Soluble guanylate cyclase (sgc) modulators for treatment of lipid related disorders
RS52166B (sr) * 2007-05-11 2012-08-31 Pfizer Inc. Amino-heterociklična jedinjenja
KR101560844B1 (ko) 2007-06-04 2015-10-15 벤-구리온 유니버시티 오브 더 네게브 리서치 앤드 디벨럽먼트 어쏘러티 트라이-아릴계 화합물 및 이를 포함하는 조성물
JP5498392B2 (ja) * 2007-11-30 2014-05-21 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング １，５−ジヒドロ−ピラゾロ［３，４−ｄ］ピリミジン−４−オン誘導体及びｃｎｓ障害の治療のためのｐｄｅ９ａモジュレーターとしてのそれらの使用
CN101998957B (zh) 2008-02-29 2013-06-05 康塞特医药品有限公司 取代的黄嘌呤衍生物
UA105362C2 (en) 2008-04-02 2014-05-12 Бьорингер Ингельхайм Интернациональ Гмбх 1-heterocyclyl-1, 5-dihydro-pyrazolo [3, 4-d] pyrimidin-4-one derivatives and their use as pde9a modulators
KR20110063447A (ko) 2008-09-08 2011-06-10 베링거 인겔하임 인터내셔날 게엠베하 피라졸로피리미딘 및 ｃｎｓ 장애의 치료를 위한 이들의 용도
EP2348857B1 (en) 2008-10-22 2016-02-24 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
US8329914B2 (en) 2008-10-31 2012-12-11 Merck Sharp & Dohme Corp Cyclic benzimidazole derivatives useful as anti-diabetic agents
TWI404721B (zh) 2009-01-26 2013-08-11 Pfizer 胺基－雜環化合物
US20110053961A1 (en) 2009-02-27 2011-03-03 Concert Pharmaceuticals, Inc. Substituted xanthine derivatives
PT2414363E (pt) 2009-03-31 2014-02-26 Boehringer Ingelheim Int Derivados de 1-heterociclil-1,5-di-hidro-pirazolo[3,4- d]pirimidin-4-ona e sua utilização como moduladores de pde9a
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
AR078793A1 (es) 2009-10-27 2011-12-07 Orion Corp Derivados de carboxamidas no esteroidales y acil hidrazona moduladores de receptores androgenicos de tejido selectivo (sarm), composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento del cancer de prostata entre otros
JP2013520502A (ja) 2010-02-25 2013-06-06 メルク・シャープ・エンド・ドーム・コーポレイション 有用な抗糖尿病薬である新規な環状ベンズイミダゾール誘導体
EP2603511B1 (en) 2010-08-12 2017-03-15 Boehringer Ingelheim International GmbH 6-cycloalkyl-1, 5-dihydro-pyrazolo [3, 4-d] pyrimidin-4-one derivatives and their use as pde9a inhibitors
RS54834B1 (sr) 2010-09-07 2016-10-31 Astellas Pharma Inc Jedinjenja pirazolokvinolina
US8809345B2 (en) 2011-02-15 2014-08-19 Boehringer Ingelheim International Gmbh 6-cycloalkyl-pyrazolopyrimidinones for the treatment of CNS disorders
SG192941A1 (en) 2011-02-25 2013-09-30 Merck Sharp & Dohme Novel cyclic azabenzimidazole derivatives useful as anti-diabetic agents
WO2013013052A1 (en) 2011-07-19 2013-01-24 Concert Pharmaceuticals, Inc. Substituted xanthine derivatives
BR112015007731B1 (pt) 2011-10-10 2022-05-31 H. Lundbeck A/S Composto, composição farmacêutica que o compreende e uso do mesmo
HK1206726A1 (en) 2012-03-19 2016-01-15 Ironwood Pharmaceuticals, Inc. Imidazotriazinone compounds
US20130315891A1 (en) 2012-05-25 2013-11-28 Matthew Charles Formulations of human tissue kallikrein-1 for parenteral delivery and related methods
US20130323222A1 (en) 2012-06-04 2013-12-05 Matthew Charles Human tissue kallikrein 1 glycosylation isoforms
RU2015106909A (ru) 2012-08-02 2016-09-27 Мерк Шарп И Доум Корп. Антидиабетические трициклические соединения
WO2014024125A1 (en) 2012-08-08 2014-02-13 Celon Pharma S.A. Pyrazolo[4,3-d]pyrimidin-7(6h)-one derivatives as pde9 inhibitors
CN102786525B (zh) 2012-08-08 2014-12-17 中山大学 N-取代吡唑并[3,4-d]嘧啶酮类化合物、其制备方法及其应用
KR20150118158A (ko) 2013-02-22 2015-10-21 머크 샤프 앤드 돔 코포레이션 항당뇨병 비시클릭 화합물
WO2014139388A1 (en) 2013-03-14 2014-09-18 Merck Sharp & Dohme Corp. Novel indole derivatives useful as anti-diabetic agents
JP2015067538A (ja) * 2013-09-26 2015-04-13 株式会社アイエイアイ 血糖値降下剤
WO2015051496A1 (en) 2013-10-08 2015-04-16 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
MX2016005995A (es) 2013-11-05 2016-08-17 Ben-Gurion Univ Of The Negev Res And Dev Authority Compuestos para el tratamiento de diabetes y complicaciones de la enfermedad derivadas de la misma.
CA2981791A1 (en) 2014-04-18 2015-10-22 Concert Pharmaceuticals, Inc. Methods of treating hyperglycemia
US20180072741A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyrimidine compounds and uses thereof
WO2018049214A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyridine derivatives as hpk1 modulators and uses thereof for the treatment of cancer
CN115819417A (zh) 2016-09-09 2023-03-21 因赛特公司 作为hpk1调节剂的吡唑并吡啶衍生物及其用于治疗癌症的用途
US11072602B2 (en) 2016-12-06 2021-07-27 Merck Sharp & Dohme Corp. Antidiabetic heterocyclic compounds
EP3558298B1 (en) 2016-12-20 2026-03-11 Merck Sharp & Dohme LLC Antidiabetic spirochroman compounds
WO2018152220A1 (en) 2017-02-15 2018-08-23 Incyte Corporation Pyrazolopyridine compounds and uses thereof
AU2018230478B2 (en) 2017-03-09 2025-01-23 Diamedica Inc. Dosage forms of tissue kallikrein 1
AU2018281131B2 (en) 2017-06-08 2022-01-20 Merck Sharp & Dohme Corp. Pyrazolopyrimidine PDE9 inhibitors
US10722495B2 (en) 2017-09-08 2020-07-28 Incyte Corporation Cyanoindazole compounds and uses thereof
US10752635B2 (en) 2018-02-20 2020-08-25 Incyte Corporation Indazole compounds and uses thereof
EP3755703B1 (en) 2018-02-20 2022-05-04 Incyte Corporation N-(phenyl)-2-(phenyl)pyrimidine-4-carboxamide derivatives and related compounds as hpk1 inhibitors for treating cancer
US10745388B2 (en) 2018-02-20 2020-08-18 Incyte Corporation Indazole compounds and uses thereof
US11299473B2 (en) 2018-04-13 2022-04-12 Incyte Corporation Benzimidazole and indole compounds and uses thereof
CA3100988A1 (en) 2018-05-25 2019-11-28 Imara Inc. Monohydrate and crystalline forms of 6-[(3s,4s)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-3-tetrahydropyran-4-yl-7h-imidazo[1,5-a]pyrazin-8-one
US10899755B2 (en) 2018-08-08 2021-01-26 Incyte Corporation Benzothiazole compounds and uses thereof
CA3110680A1 (en) 2018-08-31 2020-03-05 Imara Inc. Pde9 inhibitors for treating sickle cell disease
WO2020068729A1 (en) 2018-09-25 2020-04-02 Incyte Corporation Pyrazolo[4,3-d]pyrimidine compounds as alk2 abd/or fgfr modulators
BR112022002059A2 (pt) 2019-08-06 2022-06-07 Incyte Corp Formas sólidas de um inibidor de hpk1
US20240025904A1 (en) * 2020-10-27 2024-01-25 Cardurion Pharmaceuticals, Inc. Pde9 inhibitors for treating cardiac failure

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4666908A (en) * 1985-04-05 1987-05-19 Warner-Lambert Company 5-Substituted pyrazolo[4,3-d]pyrimidine-7-ones and methods of use
DE19541264A1 (de) 1995-11-06 1997-05-07 Bayer Ag Purin-6-on-derivate
WO1997024334A1 (en) * 1995-12-28 1997-07-10 Fujisawa Pharmaceutical Co., Ltd. Benzimidazole derivatives
GB9722520D0 (en) * 1997-10-24 1997-12-24 Pfizer Ltd Compounds
US6444816B1 (en) * 1997-10-27 2002-09-03 Dr. Reddy's Research Foundation Fused 7-oxo-pyrimidinyl compounds, preparation, composition and use thereof
US5922595A (en) * 1997-12-09 1999-07-13 Incyte Pharmaceuticals, Inc. Cyclic GMP phosphodiesterase
US6225456B1 (en) 1998-05-07 2001-05-01 University Technololy Corporation Ras suppressor SUR-5
JP2003526608A (ja) 1998-10-15 2003-09-09 バイオイメージ エイ／エス 再分布及び／又は標的化での干渉によって得られる特異的治療の介入
AU2001276607A1 (en) * 2000-08-11 2002-02-25 Pfizer Inc. Treatment of the insulin resistance syndrome with selective CGMP PDE5 inhibitors
MXPA03006936A (es) * 2001-02-02 2003-11-18 Pfizer Tratamiento de diabetes mellitus.
AUPR576801A0 (en) 2001-06-19 2001-07-12 University Of Tasmania Methods and pharmaceuticals for treating muscle insulin resistance and related conditions
JP2005508978A (ja) * 2001-11-02 2005-04-07 ファイザー・プロダクツ・インク Ｐｄｅ９阻害薬によるインスリン抵抗性症候群及び２型糖尿病の治療
US20040220186A1 (en) * 2003-04-30 2004-11-04 Pfizer Inc. PDE9 inhibitors for treating type 2 diabetes,metabolic syndrome, and cardiovascular disease

Cited By (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103313988A (zh) * 2010-09-20 2013-09-18 英维沃医药有限公司 咪唑并三嗪酮化合物
CN103313988B (zh) * 2010-09-20 2016-06-08 论坛医药有限公司 咪唑并三嗪酮化合物
CN104093720A (zh) * 2012-01-26 2014-10-08 H.隆德贝克有限公司 具有咪唑并三嗪酮骨架的pde9抑制剂
CN104093720B (zh) * 2012-01-26 2017-04-12 H.隆德贝克有限公司 具有咪唑并三嗪酮骨架的pde9抑制剂
CN107082783A (zh) * 2012-01-26 2017-08-22 H.隆德贝克有限公司 具有咪唑并三嗪酮骨架的pde9抑制剂
CN107082783B (zh) * 2012-01-26 2019-03-22 H.隆德贝克有限公司 具有咪唑并三嗪酮骨架的pde9抑制剂
US11608342B2 (en) 2015-07-07 2023-03-21 H. Lundbeck A/S PDE9 inhibitors with imidazo triazinone backbone and imidazo pyrazinone backbone for treatment of peripheral diseases
CN111183140A (zh) * 2017-05-26 2020-05-19 伊马拉公司 制备和使用pde9抑制剂的方法
CN111183140B (zh) * 2017-05-26 2022-12-02 伊马拉公司 制备和使用pde9抑制剂的方法
CN115746003A (zh) * 2017-05-26 2023-03-07 伊马拉公司 制备和使用pde9抑制剂的方法
US11999741B2 (en) 2017-05-26 2024-06-04 Cardurion Pharmaceuticals, Inc. Process for the synthesis of 6-((3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl)-3-(tetrahydropyran-4-yl-7H-imidazo[1,5-a]pyrazin-8-one

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