CN1374953A - 含氮的6－员芳香环化合物 - Google Patents

含氮的6－员芳香环化合物 Download PDF

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Publication number
CN1374953A
CN1374953A CN00812968A CN00812968A CN1374953A CN 1374953 A CN1374953 A CN 1374953A CN 00812968 A CN00812968 A CN 00812968A CN 00812968 A CN00812968 A CN 00812968A CN 1374953 A CN1374953 A CN 1374953A
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Prior art keywords
group
methoxy
chloro
compound
pyrimidine
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Pending
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CN00812968A
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Chinese (zh)
Inventor
山田幸一郎
松木健司
大森谦司
吉川公平
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Tanabe Pharma Corp
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Tanabe Seiyaku Co Ltd
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Application filed by Tanabe Seiyaku Co Ltd filed Critical Tanabe Seiyaku Co Ltd
Publication of CN1374953A publication Critical patent/CN1374953A/zh
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
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    • 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
    • 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
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
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    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/125—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/13—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
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    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
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    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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 two hetero rings
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    • C07D513/02—Heterocyclic 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 two hetero rings
    • C07D513/04—Ortho-condensed systems
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    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6509—Six-membered rings
    • C07F9/6512—Six-membered rings having the nitrogen atoms in positions 1 and 3
    • C—CHEMISTRY; METALLURGY
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    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
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    • C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom

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  • Animal Behavior & Ethology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Gynecology & Obstetrics (AREA)
  • Reproductive Health (AREA)
  • Pulmonology (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)
  • Compositions Of Macromolecular Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN00812968A 1999-09-16 2000-09-13 含氮的6－员芳香环化合物 Pending CN1374953A (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
JP261852/99 1999-09-16
JP26185299 1999-09-16
JP130371/00 2000-04-28
JP2000130371 2000-04-28

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CN2012100068594A Division CN102584799A (zh) 1999-09-16 2000-09-13 含氮的6-员芳香环化合物

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CN00812968A Pending CN1374953A (zh) 1999-09-16 2000-09-13 含氮的6－员芳香环化合物
CN2012100068594A Pending CN102584799A (zh) 1999-09-16 2000-09-13 含氮的6-员芳香环化合物

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EP (1) EP1219609B1 (enExample)
KR (1) KR100532546B1 (enExample)
CN (2) CN1374953A (enExample)
AR (1) AR025668A1 (enExample)
AT (1) ATE358670T1 (enExample)
AU (1) AU767558B2 (enExample)
BE (1) BE2013C051I2 (enExample)
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BR (1) BRPI0014526C1 (enExample)
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CY (2) CY1106534T1 (enExample)
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Cited By (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101798301A (zh) * 2010-04-13 2010-08-11 漆又毛 吡咯烷基嘧啶甲磺酰胺衍生物及制备方法
CN102372697A (zh) * 2010-08-19 2012-03-14 山东轩竹医药科技有限公司 取代的嘧啶类化合物
CN102887889A (zh) * 2011-07-21 2013-01-23 山东轩竹医药科技有限公司 杂环取代的嘧啶类化合物
CN103254179A (zh) * 2013-05-23 2013-08-21 苏州明锐医药科技有限公司 阿伐那非的制备方法
CN104003981A (zh) * 2014-05-28 2014-08-27 河北康泰药业有限公司 阿伐那非的合成方法
CN104356115A (zh) * 2014-11-21 2015-02-18 齐鲁天和惠世制药有限公司 一种4-[(3-氯-4-甲氧基苄基)氨基]-2-[2-(羟甲基)-1-吡咯烷基]嘧啶-5-羧酸乙酯的制备方法
CN104487434A (zh) * 2012-08-14 2015-04-01 山东轩竹医药科技有限公司 双环取代的嘧啶类化合物
CN104628708A (zh) * 2013-11-13 2015-05-20 北大方正集团有限公司 一种阿伐那非的晶型及其制备方法、用途和药物组合物
CN105102447A (zh) * 2013-03-29 2015-11-25 山东轩竹医药科技有限公司 双环取代的嘧啶类pde-5抑制剂的前药
CN109280049A (zh) * 2018-09-25 2019-01-29 重庆奥舍生物化工有限公司 一种医药化合物阿伐那非的合成方法
CN109776505A (zh) * 2019-03-14 2019-05-21 扬州市三药制药有限公司 一种阿伐那非的制备方法
CN110078713A (zh) * 2019-04-10 2019-08-02 北京精华耀邦医药科技有限公司 一种用于治疗男性勃起功能障碍的化合物

Families Citing this family (87)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6403597B1 (en) * 1997-10-28 2002-06-11 Vivus, Inc. Administration of phosphodiesterase inhibitors for the treatment of premature ejaculation
US20080027037A1 (en) * 2000-04-28 2008-01-31 Tanabe Seiyaku Co., Ltd. Cyclic compounds
US7273868B2 (en) * 2000-04-28 2007-09-25 Tanabe Seiyaku Co., Ltd. Pyrazine derivatives
MXPA02010693A (es) * 2000-04-28 2003-03-10 Tanabe Seiyaku Co Compuestos ciclicos.
KR100610131B1 (ko) * 2000-09-06 2006-08-09 다나베 세이야꾸 가부시키가이샤 경구 투여용 제제
US6710048B2 (en) * 2000-09-20 2004-03-23 Ortho-Mcneil Pharmaceutical, Inc. Pyrazine derivatives as modulators of tyrosine kinases
US6995162B2 (en) 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
US6878714B2 (en) * 2001-01-12 2005-04-12 Amgen Inc. Substituted alkylamine derivatives and methods of use
US20030134836A1 (en) 2001-01-12 2003-07-17 Amgen Inc. Substituted arylamine derivatives and methods of use
US20020147198A1 (en) * 2001-01-12 2002-10-10 Guoqing Chen Substituted arylamine derivatives and methods of use
ATE472319T1 (de) * 2001-02-15 2010-07-15 Mitsubishi Tanabe Pharma Corp Tabletten, die in der mundhöhle schnell zerfallen
AR036375A1 (es) * 2001-08-30 2004-09-01 Novartis Ag Compuestos pirrolo [2,3-d] pirimidina -2- carbonitrilo, un proceso para su preparacion, una composicion farmaceutica y el uso de dichos compuestos para la preparacion de medicamentos
EP1453516A2 (de) 2001-10-17 2004-09-08 Boehringer Ingelheim Pharma GmbH & Co.KG 5-substituierte 4-amino-2-phenylamino-pyrimdinderivate und ihre verwendung als beta-amyloid modulatoren
EP1438053B1 (de) * 2001-10-17 2008-09-10 Boehringer Ingelheim Pharma GmbH & Co.KG Pyrimidinderivate, arzneimittel enthaltend diese verbindungen, deren verwendung und verfahren zu ihrer herstellung
EP1321463B1 (en) * 2001-12-21 2007-08-08 Virochem Pharma Inc. Thiazole derivatives and their use for the treatment or prevention of Flavivirus infections
CA2473510A1 (en) * 2002-01-23 2003-07-31 Bayer Pharmaceuticals Corporation Pyrimidine derivatives as rho-kinase inhibitors
US7176310B1 (en) * 2002-04-09 2007-02-13 Ucb Sa Pyrimidinecarboxamide derivatives and their use as anti-inflammatory agents
US7166595B2 (en) 2002-05-09 2007-01-23 Cytokinetics, Inc. Compounds, methods and compositions
WO2003101994A1 (en) * 2002-05-29 2003-12-11 Abbott Laboratories Fused bicyclic aromatic compounds that are useful in treating sexual dysfunction
US7057042B2 (en) 2002-05-29 2006-06-06 Abbott Laboratories Fused bicyclic aromatic compounds that are useful in treating sexual dysfunction
AU2003250482A1 (en) * 2002-08-13 2004-02-25 Warner-Lambert Company Llc Phthalimide derivatives as matrix metalloproteinase inhibitors
EP1590338B1 (en) 2002-12-04 2009-08-26 Ore Pharmaceuticals Inc. Modulators of melanocortin receptor
MXPA06012505A (es) * 2004-04-30 2006-12-15 Warner Lambert Co Compuestos de morfolina sustituida para el tratamiento de trastornos del sistema nervioso central.
GB0409744D0 (en) * 2004-04-30 2004-06-09 Pfizer Ltd Novel compounds
GB0425758D0 (en) 2004-11-23 2004-12-22 Vectura Ltd Preparation of pharmaceutical compositions
BRPI0610498A2 (pt) 2005-04-19 2010-06-22 Nycomed Gmbh uso de roflumilast,composição farmacêutica, produto de combinação e kit para o tratamento de hipertensão pulmonar
WO2007025177A2 (en) 2005-08-26 2007-03-01 Braincells, Inc. Neurogenesis by muscarinic receptor modulation
EP2258359A3 (en) 2005-08-26 2011-04-06 Braincells, Inc. Neurogenesis by muscarinic receptor modulation with sabcomelin
CA2625153A1 (en) 2005-10-21 2007-04-26 Braincells, Inc. Modulation of neurogenesis by pde inhibition
US8247556B2 (en) 2005-10-21 2012-08-21 Amgen Inc. Method for preparing 6-substituted-7-aza-indoles
EP1942879A1 (en) 2005-10-31 2008-07-16 Braincells, Inc. Gaba receptor mediated modulation of neurogenesis
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
EP2021000A2 (en) 2006-05-09 2009-02-11 Braincells, Inc. Neurogenesis by modulating angiotensin
US20080051413A1 (en) * 2006-08-25 2008-02-28 Kaohsiung Medical University Nitrophenylpiperazine derivative of xanthine which relaxes tracheal airway and increases respiratory performance
JP2010502670A (ja) 2006-09-07 2010-01-28 ニコメッド ゲゼルシャフト ミット ベシュレンクテル ハフツング 真性糖尿病のための組合せ治療
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
TW200827346A (en) 2006-11-03 2008-07-01 Astrazeneca Ab Chemical compounds
TW200836719A (en) 2007-02-12 2008-09-16 Astrazeneca Ab Chemical compounds
TW200914457A (en) * 2007-05-31 2009-04-01 Kyowa Hakko Kogyo Kk Pyrimidodiazepinone derivative
PL2152663T3 (pl) 2007-06-04 2014-09-30 Ben Gurion Univ Of The Negev Research And Development Authority Związki triarylowe oraz kompozycje zawierające te związki
US8071557B2 (en) 2007-06-13 2011-12-06 Vivus, Inc. Treatment of pulmonary hypertension with carbonic anhydrase inhibitors
WO2009013286A1 (en) * 2007-07-24 2009-01-29 Novartis Ag Organic compounds
EP2202228B1 (en) * 2007-10-15 2014-12-10 Takeda Pharmaceutical Company Limited Amide compounds and use of the same
EP2082768A1 (en) 2008-01-24 2009-07-29 Vectura Delivery Devices Limited Inhaler
EP2082771A1 (en) 2008-01-24 2009-07-29 Vectura Delivery Devices Limited Inhaler
EP2082766A1 (en) 2008-01-24 2009-07-29 Vectura Delivery Devices Limited Blister Strip Coil Forming
EP2082767A1 (en) 2008-01-24 2009-07-29 Vectura Delivery Devices Limited Inhaler
EP2082772A1 (en) 2008-01-24 2009-07-29 Vectura Delivery Devices Limited Inhaler
WO2009117269A1 (en) * 2008-03-18 2009-09-24 Merck & Co., Inc. Substituted 4-hydroxypyrimidine-5-carboxamides
US20100216805A1 (en) 2009-02-25 2010-08-26 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
WO2010144647A1 (en) 2009-06-12 2010-12-16 Bristol-Myers Squibb Company Nicotinamide compounds useful as kinase modulators
US8354593B2 (en) * 2009-07-10 2013-01-15 Nanocomp Technologies, Inc. Hybrid conductors and method of making same
GB0921481D0 (en) 2009-12-08 2010-01-20 Vectura Ltd Process and product
EP2361911A1 (en) * 2010-02-18 2011-08-31 GenKyoTex SA Pyrazolo piperidine derivatives as NADPH oxidase inhibitors
EP2361912A1 (en) * 2010-02-18 2011-08-31 GenKyoTex SA Pyrazolo piperidine derivatives as NADPH oxidase inhibitors
WO2011126250A2 (ko) 2010-04-05 2011-10-13 에스케이케미칼 주식회사 Pde5 억제제를 함유하는 피부 주름 개선용 조성물
TW201210584A (en) 2010-08-18 2012-03-16 Alcon Res Ltd Bradykinin receptor agonists and uses thereof to treat ocular hypertension and glaucoma
US9402877B2 (en) 2011-11-04 2016-08-02 Xion Pharmaceuticals Corporation Methods and compositions for oral administration of melanocortin receptor agonist compounds
US20150119399A1 (en) 2012-01-10 2015-04-30 President And Fellows Of Harvard College Beta-cell replication promoting compounds and methods of their use
US9248122B2 (en) 2012-11-28 2016-02-02 Grünenthal GmbH Heteroquinoline-3-carboxamides as KCNQ2/3 modulators
JP2016508960A (ja) 2012-11-28 2016-03-24 グリュネンタール・ゲゼルシャフト・ミト・ベシュレンクテル・ハフツング Ｋｃｎｑ２／３モジュレーターとしての特定のカルボキサミド
JP2016508118A (ja) * 2012-11-28 2016-03-17 グリュネンタール・ゲゼルシャフト・ミト・ベシュレンクテル・ハフツング Ｋｃｎｑ２／３モジュレーターとしての置換アミノ−アリールカルボキサミド
CN104059025B (zh) * 2013-03-20 2017-07-04 广州朗圣药业有限公司 一种用于制备阿伐那非的中间体及其制备方法
WO2014174529A2 (en) * 2013-04-23 2014-10-30 Hetero Research Foundation Polymorphs of avanafil
WO2014187273A1 (zh) 2013-05-23 2014-11-27 苏州明锐医药科技有限公司 阿伐那非的制备方法
CN103265534B (zh) * 2013-05-23 2014-07-23 苏州明锐医药科技有限公司 阿伐那非的制备方法
CN103254180B (zh) * 2013-05-23 2014-07-23 苏州明锐医药科技有限公司 一种阿伐那非的制备方法
WO2015001567A1 (en) * 2013-07-01 2015-01-08 Msn Laboratories Private Limited Process for the preparation of (s)-4-[(3-chloro-4-methoxybenzyl)amino]-2-[2- (hydroxymethyl)-1-pyrrolidinyl]-n-(2-pyrimidinyl methyl-5-pyrimidine carboxamide
CN104557877B (zh) * 2013-10-28 2016-08-17 重庆安格龙翔医药科技有限公司 一种阿伐那非中间体及其制备方法和应用
AU2014347668A1 (en) 2013-11-05 2016-05-19 Ben-Gurion University Of The Negev Research And Development Authority Compounds for the treatment of diabetes and disease complications arising from same
CN104628707A (zh) * 2013-11-13 2015-05-20 北大方正集团有限公司 一种阿伐那非的无定型及其制备方法、用途和药物组合物
CN104650045B (zh) * 2013-11-19 2017-04-19 苏州旺山旺水生物医药有限公司 阿伐那非的制备方法
GB201321748D0 (en) * 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic agents
CN103833736A (zh) * 2014-03-04 2014-06-04 北京澳合药物研究院有限公司 一种阿伐那非的制备方法
WO2015177807A1 (en) * 2014-05-22 2015-11-26 Wanbury Ltd. A process for the preparation of avanafil and its novel intermediates
CN104151299B (zh) * 2014-08-22 2017-03-08 北京科莱博医药开发有限责任公司 化合物、晶型化合物及其制备方法
CN104530015B (zh) * 2014-12-10 2017-01-04 齐鲁天和惠世制药有限公司 一种阿伐那非的制备方法
WO2017168174A1 (en) 2016-04-02 2017-10-05 N4 Pharma Uk Limited New pharmaceutical forms of sildenafil
CN105924402A (zh) * 2016-05-06 2016-09-07 蚌埠中实化学技术有限公司 一种2-胺基甲基嘧啶盐酸盐的制备方法
KR20190026902A (ko) 2016-07-14 2019-03-13 화이자 인코포레이티드 바닌-1 효소의 억제제로서의 신규 피리미딘 카르복스아미드
CN106496201A (zh) * 2016-10-31 2017-03-15 昆药集团股份有限公司 一种阿伐那非原料药的制备方法
AU2017378409A1 (en) 2016-12-14 2019-07-04 Respira Therapeutics, Inc. Methods and compositions for treatment of pulmonary hypertension and other lung disorders
CN107879986A (zh) * 2017-12-20 2018-04-06 重庆英斯凯化工有限公司 一种阿伐那非杂质的合成方法
CN108658872B (zh) * 2018-05-03 2021-06-22 无锡富泽药业有限公司 一种阿伐那非中间体的制备方法
MX2021001503A (es) * 2018-08-06 2021-04-28 Nicox Sa Inhibidor de fosfodiesterasa tipo 5 con liberacion de oxido nitrico.
CN110117274A (zh) * 2019-05-08 2019-08-13 梯尔希（南京）药物研发有限公司 一种阿伐那非杂质的制备方法
CN117430591A (zh) * 2023-10-31 2024-01-23 康普药业股份有限公司 一种阿伐那非的合成方法

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1229413A (enExample) * 1967-06-14 1971-04-21
JPS5481299A (en) * 1977-12-09 1979-06-28 Daito Koeki Kk Preparation of 2,8-disubstituted-6-formyl-5,8-dihydro-5- oxopyrido 2,3-d pyrimidine derivative
AT392789B (de) * 1985-01-23 1991-06-10 Toyama Chemical Co Ltd Verfahren zur herstellung von 1-substituierten aryl-1,4-dihydro-4-oxonaphthyridinderivaten
US4959368A (en) * 1986-02-24 1990-09-25 Mitsui Petrochemical Industries Ltd. Therapeutic agent for neurological diseases
US5234746A (en) 1990-05-16 1993-08-10 Tomoegawa Paper Co., Ltd. Conductive substrate and printing media using the same
GB9012316D0 (en) 1990-06-01 1990-07-18 Wellcome Found Pharmacologically active cns compounds
JPH06509803A (ja) * 1991-08-14 1994-11-02 プロクター、エンド、ギャンブル、ファーマスーティカルズ、インコーポレーテッド 抗不整脈及び抗細動剤として有用な新規環状尿素類
US5252604A (en) 1992-07-10 1993-10-12 Hoffmann-La Roche Inc. Compositions of retinoic acids and tocopherol for prevention of dermatitis
GB9301192D0 (en) 1993-06-09 1993-06-09 Trott Francis W Flower shaped mechanised table
ATE163647T1 (de) * 1993-08-26 1998-03-15 Ono Pharmaceutical Co 4-aminopyrimidin derivate
US5491253A (en) * 1993-10-22 1996-02-13 Abbott Laboratories Process for the preparation of a substituted 2,5-diamino-3-hydroxyhexane
KR100189863B1 (ko) 1993-12-27 1999-06-01 나이또 하루오 안트라닐산 유도체
ES2224130T3 (es) 1994-08-09 2005-03-01 Eisai Co., Ltd. Compuesto de piridazina condensada.
KR100239800B1 (ko) 1996-11-28 2000-03-02 손경식 4,5-디아미노 피리미딘 유도체 및 이의 제조방법
JP2000072751A (ja) * 1998-08-26 2000-03-07 Tanabe Seiyaku Co Ltd イソキノリノン誘導体
IL132406A0 (en) 1998-10-21 2001-03-19 Pfizer Prod Inc Treatment of bph with cgmp elevators
GB9823101D0 (en) * 1998-10-23 1998-12-16 Pfizer Ltd Pharmaceutically active compounds

Cited By (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101798301A (zh) * 2010-04-13 2010-08-11 漆又毛 吡咯烷基嘧啶甲磺酰胺衍生物及制备方法
CN102372697A (zh) * 2010-08-19 2012-03-14 山东轩竹医药科技有限公司 取代的嘧啶类化合物
CN102887889A (zh) * 2011-07-21 2013-01-23 山东轩竹医药科技有限公司 杂环取代的嘧啶类化合物
CN102887889B (zh) * 2011-07-21 2014-12-10 山东轩竹医药科技有限公司 杂环取代的嘧啶类化合物
CN104487434A (zh) * 2012-08-14 2015-04-01 山东轩竹医药科技有限公司 双环取代的嘧啶类化合物
CN105102447A (zh) * 2013-03-29 2015-11-25 山东轩竹医药科技有限公司 双环取代的嘧啶类pde-5抑制剂的前药
CN103254179A (zh) * 2013-05-23 2013-08-21 苏州明锐医药科技有限公司 阿伐那非的制备方法
CN103254179B (zh) * 2013-05-23 2014-09-10 苏州明锐医药科技有限公司 阿伐那非的制备方法
CN104628708A (zh) * 2013-11-13 2015-05-20 北大方正集团有限公司 一种阿伐那非的晶型及其制备方法、用途和药物组合物
CN104003981A (zh) * 2014-05-28 2014-08-27 河北康泰药业有限公司 阿伐那非的合成方法
CN104356115A (zh) * 2014-11-21 2015-02-18 齐鲁天和惠世制药有限公司 一种4-[(3-氯-4-甲氧基苄基)氨基]-2-[2-(羟甲基)-1-吡咯烷基]嘧啶-5-羧酸乙酯的制备方法
CN104356115B (zh) * 2014-11-21 2016-08-24 齐鲁天和惠世制药有限公司 一种4-[(3-氯-4-甲氧基苄基)氨基]-2-[2-(羟甲基)-1-吡咯烷基]嘧啶-5-羧酸乙酯的制备方法
CN109280049A (zh) * 2018-09-25 2019-01-29 重庆奥舍生物化工有限公司 一种医药化合物阿伐那非的合成方法
CN109280049B (zh) * 2018-09-25 2021-02-02 重庆奥舍生物化工有限公司 一种医药化合物阿伐那非的合成方法
CN109776505A (zh) * 2019-03-14 2019-05-21 扬州市三药制药有限公司 一种阿伐那非的制备方法
CN109776505B (zh) * 2019-03-14 2021-07-27 扬州市三药制药有限公司 一种阿伐那非的制备方法
CN110078713A (zh) * 2019-04-10 2019-08-02 北京精华耀邦医药科技有限公司 一种用于治疗男性勃起功能障碍的化合物
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