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1. 发明专利

JP2015057416A Ｎ１／Ｎ２−ラクタムアセチル−ＣｏＡカルボキシラーゼ阻害剤审中-公开
标题翻译： N1 / N2-LACTAM乙酰辅酶C羧酸酶抑制剂
公开(公告)号：JP2015057416A
公开(公告)日：2015-03-26
申请号：JP2014225021
申请日：2014-11-05
申请人：ファイザー・インク , Pfizer Inc
发明人： SCOTT WILLIAM BAGLEY , DOW ROBERT L , GRIFFITH DAVID ANDREW , AARON CHRISTOPHER SMITH
IPC分类号： C07D471/20 , A61K31/4709 , A61P3/10 , A61P5/50 , A61P43/00
CPC分类号： C07D471/20 , C07D519/00
摘要：【課題】脂肪酸合成を阻害し脂肪酸酸化を増加させることにより、肥満および肥満関連疾患(非アルコール性脂肪肝疾患および2型糖尿病等)を治療するための方法の提供。【解決手段】アセチル−CoAカルボキシラーゼ酵素(ACC1及び/又はACC2)阻害活性を有する、下記式で表される置換ピラゾロスピロケトンを上記疾患に対する治療薬として使用する。【選択図】なし
摘要翻译：要解决的问题：通过抑制脂肪酸合成和增加脂肪酸氧化来提供治疗肥胖和肥胖相关疾病（如非酒精性脂肪性肝病和2型糖尿病）的方法。解决方案：具有乙酰基 - 由下式表示的CoA羧化酶（ACC1和/或ACC2）抑制活性用于疾病的治疗剂。

2. 发明专利

JP2003012672A Method for producing growth hormone secretagogue and intermediate 审中-公开
标题翻译：生产生长激素分泌和中间体的方法
公开(公告)号：JP2003012672A
公开(公告)日：2003-01-15
申请号：JP2002174642
申请日：2002-06-14
申请人： Pfizer Prod Inc , ファイザー・プロダクツ・インク
发明人： CHIU CHARLES KWOK-FUNG , GRIFFITH DAVID ANDREW
IPC分类号： C07D247/00 , A61P5/06 , A61P43/00 , C07D487/04 , C07K5/062
CPC分类号： C07D487/04 , Y02P20/55
摘要： PROBLEM TO BE SOLVED: To provide a method for producing a specific hormone secretagogue and an intermediate capable of being used in the method.
SOLUTION: This method for producing a compound of formula VI, comprises reacting a compound of formula IV with a carbonyl equivalent and CF
3 CH
2 NH
2 in a reaction inert solvent to form a compound of formula VII, reacting the compound of formula VII with 2-picolyl-Z
1 in the presence of a base and a reaction inert solvent at about -78°C to about 25°C for about 1 hr to about 24 hr to form a compound of formula VIII, reacting the compound of formula VIII with a suitable acid in a reaction inert solvent at about -30°C to about 25°C for about 1 hr to about 10 hr to form a compound of formula IX, resolving the compound of formula IX with D-tartaric acid in a reaction inert solvent to form the D-tartrate salt of a compound of formula X, reacting the D-tartrate salt of a compound of formula X with a compound of formula XI, a peptide coupling reagent and a base in a reaction inert solvent to form a compound of formula XII and reacting the compound of formula XII under standard t- butyloxycarbonyl group removing conditions to form a compound of formula VI.
COPYRIGHT: (C)2003,JPO
摘要翻译：要解决的问题：提供一种特异性激素促分泌素的制备方法和能够用于该方法的中间体。解决方案：制备式Ⅵ化合物的方法包括在反应惰性溶剂中使式Ⅳ化合物与羰基当量和CF 3 CH 2 NH 2反应，形成式Ⅶ化合物，使式Ⅶ化合物与2-吡啶甲基 -Z 1在碱和反应惰性溶剂的存在下在约-78℃至约25℃下反应约1小时至约24小时以形成式VIII的化合物，使式 VIII与合适的酸在约-30℃至约25℃的反应惰性溶剂中反应约1小时至约10小时以形成式IX化合物，用D-酒石酸拆分式IX化合物在反应惰性溶剂中形成式X化合物的D-酒石酸盐，将式X化合物的D-酒石酸盐与式XI化合物，肽偶联剂和碱反应在反应惰性溶剂以形成式Ⅻ的化合物，并使式Ⅻ的化合物在标准下反应叔丁氧羰基除去条件以形成式VI化合物。

3. 发明专利

JP2007077144A AMINO-SUBSTITUTED PYRAZOLO[1,5-a]-1,5-PYRIMIDINES AND PYRAZOLO[1,5-a]-1,3,5-TRIAZINES 审中-公开
标题翻译：氨基取代的吡唑并[1,5-a] -1,5-二吡啶并[1,2-a] -1,3,5-三唑并[1,5-a]
公开(公告)号：JP2007077144A
公开(公告)日：2007-03-29
申请号：JP2006241067
申请日：2006-09-06
申请人： Neurogen Corp , Pfizer Inc , ニューロジェン・コーポレーション , ファイザー・インク
发明人： DARROW JAMES W , DE LOMBAERT STEPHANE , BLUM CHARLES , TRAN JENNIFER , GIANGIORDANO MARK , GRIFFITH DAVID ANDREW , CARPINO PHILIP ALBERT
IPC分类号： C07D487/04 , G01N33/50 , A61K31/155 , A61K31/427 , A61K31/519 , A61K31/53 , A61K31/64 , A61K31/7034 , A61K38/28 , A61K45/00 , A61P1/00 , A61P1/12 , A61P3/04 , A61P3/06 , A61P3/10 , A61P7/04 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/02 , A61P15/00 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C12N15/09 , G01N33/15 , G01N33/566
CPC分类号： C07D487/04 , G01N2333/5755 , G01N2333/70571
摘要： PROBLEM TO BE SOLVED: To obtain a new medicine useful as a localized probe of NPY1 and a standard substance in an NPY1 receptor binding assay. SOLUTION: The compound is represented by formula (I) (R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are each a substituted or nonsubstituted alkyl group or the like; X is N or the like). The compound is a selective modulator of NPY1 receptor. The compound is useful for treating many CNS disorders, metabolic disorders, peripheral disorders, eating disorder and hypertension. The method for treating the disorders is provided. The packaged medicine is obtained. COPYRIGHT: (C)2007,JPO&INPIT
摘要翻译：待解决的问题：获得可用作NPY1受体结合测定中NPY1和标准物质的局部探针的新药。解决方案：化合物由式（I）表示（R 1 SP 1，R 2 SP 2，R 3，SP 3，R 4， R SP＆lt; SP＆gt;和＆lt; SP＆gt; 6＆lt; SP＆gt;和R 6各自为取代或未取代的烷基等; X为N等）。该化合物是NPY1受体的选择性调节剂。该化合物可用于治疗许多CNS疾病，代谢紊乱，外周疾病，进食障碍和高血压。提供了治疗疾病的方法。获得包装的药物。版权所有（C）2007，JPO＆INPIT

4. 发明专利

JP2004043477A Dipeptide derivative as growth hormone secretion-accelerating agent 有权
公开(公告)号：JP2004043477A
公开(公告)日：2004-02-12
申请号：JP2003271598
申请日：2003-07-07
申请人： Pfizer Inc , ファイザー・インク
发明人： CARPINO PHILIP ALBERT , GRIFFITH DAVID ANDREW , LEFKER BRUCE ALLEN
IPC分类号： A61K31/138 , A61K31/40 , A61K31/4168 , A61K31/4174 , A61K31/437 , A61K31/4439 , A61K31/4453 , A61K31/4535 , A61K31/4725 , A61K31/4985 , A61K31/565 , A61K31/663 , A61K38/00 , A61K38/04 , A61K38/22 , A61K38/23 , A61K38/27 , A61K45/00 , A61P3/00 , A61P3/02 , A61P3/04 , A61P3/08 , A61P3/10 , A61P5/06 , A61P5/10 , A61P7/00 , A61P9/04 , A61P13/12 , A61P15/00 , A61P15/14 , A61P17/00 , A61P17/02 , A61P19/00 , A61P19/08 , A61P19/10 , A61P21/00 , A61P25/02 , A61P25/20 , A61P43/00 , C07D471/04 , C07D487/04 , C07D491/04 , C07D498/04 , C07D513/04 , C07K1/02 , C07K5/02 , C07K5/023 , C07K5/06 , C07K5/062
CPC分类号： C07D487/04 , A61K38/00 , C07D471/04 , C07D491/04 , C07D513/04 , C07K5/0202 , C07K5/0205 , C07K5/0207 , C07K5/021 , C07K5/06026
摘要： PROBLEM TO BE SOLVED: To provide a compound having a growth hormone secretion-accelerating activity and increasing the level of endogeneous growth hormone and its pharmaceutically permissible salts, and a medicinal composition containing the same. SOLUTION: This dipeptide derivative expressed by formula 1 increases the endogeneous production or release of the growth hormone of human or other animals, and useful for the treatment and prevention of osteoporosis and/or weakness. Also, the medicinal composition obtained by combining a bisphosphonic acid salt compound such as alendronate, etc., estrogen, premarin, calcitonin, etc., with the dipeptide is useful for the treatment. COPYRIGHT: (C)2004,JPO

5. 发明专利

JP2000159794A DIPEPTIDE DERIVATIVE 失效
公开(公告)号：JP2000159794A
公开(公告)日：2000-06-13
申请号：JP32935699
申请日：1999-11-19
申请人： PFIZER PROD INC
发明人： GRIFFITH DAVID ANDREW , BRONK BRIAN SCOTT
IPC分类号： A61K38/00 , A61K38/05 , A61P3/04 , A61P3/10 , A61P5/06 , A61P9/00 , A61P17/02 , A61P19/08 , A61P43/00 , C07K5/02 , C07K5/03 , C07K5/06 , C07K5/062
摘要： PROBLEM TO BE SOLVED: To obtain a new compound useful for treating congestive cardiac insufficiency as a growth hormone crinogenic substance. SOLUTION: This compound is shown by formula I [HET is a group of formula II or formula III (R1 is H, CN or the like; R2 is H, fluoro or the like; R2A is H, a 1-6C alkyl or the like; Z is C=O, C=S or the like; R3 is a 1-6C alkyl, a 1-6C alkyl to 3-7C cycloalkyl or the like; X4 together with R4, an N atom and a C atom form a 5- to 7-membered ring; R6 is a bond, a group of formula IV (X5 and X5a are each CF3 or the like; Z1 is O or the like; (a) and (b) are each 0-3) or the like; R7 and R8 are each H or a 1-6C alkyl], its salt or prodrug such as 2-amino-N- 1(R)-benzyloxymethyl-1-[8a(S)-(4-fluoro-benzyl)-6- methylsulfanyl-8-oxo-3,4,8,8a-tetrahydro-1H-pyrrolo[1,2-a]pyrazin-2-yl ]-2-oxo- ethyl}-2-methyl-propionamide hydrochloride. The compound is obtained, for example, by reacting an amino acid of formula V with a heterocyclic amine of HET.

6. 发明专利

JP2000159770A PRODUCTION PROCESS AND INTERMEDIATE FOR GROWTH HORMONE SECRETION-PROMOTING SUBSTANCE 失效
公开(公告)号：JP2000159770A
公开(公告)日：2000-06-13
申请号：JP32771999
申请日：1999-11-18
申请人： PFIZER PROD INC
发明人： CHIU CHARLES KWOK-FUNG , GRIFFITH DAVID ANDREW
IPC分类号： C07D247/00 , A61P5/06 , A61P43/00 , C07D487/04 , C07K5/062
摘要： PROBLEM TO BE SOLVED: To provide a novel compound that is useful as a synthetic intermediate for a specific growth hormone secretion-promoting substance. SOLUTION: This compound is represented by formula I (Pt is an amino group-protecting group, preferably t-butyloxycarbonyl). The compound of formula I is prepared by reaction of a compound of formula II (R3 is a 1-4C alkyl) with a carbonyl equivalent compound (for example, N,N'-carbonyldiimidazole or the like) and CF3CH2NH2 in a solvent inert to the reaction (for example, methylene chloride or the like). A useful compound of formula [II can be produced by using the compound of formula I as a synthetic intermediate.

7. 发明专利

JP2007302685A Bicyclic pyrazolyl and imidazolyl compound and use thereof 审中-公开
标题翻译：双酚PYRAZOLYL和咪唑啉化合物及其用途
公开(公告)号：JP2007302685A
公开(公告)日：2007-11-22
申请号：JP2007183117
申请日：2007-07-12
申请人： Pfizer Prod Inc , ファイザー・プロダクツ・インク
发明人： CARPINO PHILIP ALBERT , DOW ROBERT LEE , GRIFFITH DAVID ANDREW
IPC分类号： C07D498/04 , A61K31/55 , A61K31/551 , A61K31/553 , A61K31/554 , A61P1/00 , A61P3/04 , A61P3/10 , A61P25/10 , A61P25/16 , A61P25/24 , A61P25/28 , A61P25/34 , A61P25/36 , A61P29/00 , A61P43/00 , C07D471/04 , C07D487/04 , C07D487/12 , C07D487/14 , C07D491/02 , C07D498/02 , C07D513/04
CPC分类号： C07D487/14 , C07D471/04 , C07D487/04 , C07D513/04
摘要： PROBLEM TO BE SOLVED: To provide bicyclic pyrazolyl and imidazolyl compounds which are cannabinoid receptor ligands, particularly CB1 receptor antagonists. SOLUTION: Compounds represented by formula (I) have been shown to act as cannabinoid receptor ligands and are therefore useful in the treatment of diseases, particularly obesity linked to the mediation of the cannabinoid receptors in animals. COPYRIGHT: (C)2008,JPO&INPIT
摘要翻译：要解决的问题：提供作为大麻素受体配体的双环吡唑基和咪唑基化合物，特别是CB1受体拮抗剂。解决方案：已显示由式（I）表示的化合物作为大麻素受体配体，因此可用于治疗与动物中的大麻素受体的调解相关的疾病，特别是肥胖症。版权所有（C）2008，JPO＆INPIT

8. 发明专利

JP2004067685A Dipeptide derivative as growth hormone secretagogue agent 有权
标题翻译：代谢衍生物作为生长激素秘密代谢剂
公开(公告)号：JP2004067685A
公开(公告)日：2004-03-04
申请号：JP2003271592
申请日：2003-07-07
申请人： Pfizer Inc , ファイザー・インク
发明人： CARPINO PHILIP ALBERT , GRIFFITH DAVID ANDREW , LEFKER BRUCE ALLEN
IPC分类号： A61K31/138 , A61K31/40 , A61K31/4168 , A61K31/4174 , A61K31/437 , A61K31/4439 , A61K31/4453 , A61K31/4535 , A61K31/4725 , A61K31/4985 , A61K31/565 , A61K31/663 , A61K38/00 , A61K38/04 , A61K38/22 , A61K38/23 , A61K38/27 , A61K45/00 , A61P3/00 , A61P3/02 , A61P3/04 , A61P3/08 , A61P3/10 , A61P5/06 , A61P5/10 , A61P7/00 , A61P9/04 , A61P13/12 , A61P15/00 , A61P15/14 , A61P17/00 , A61P17/02 , A61P19/00 , A61P19/08 , A61P19/10 , A61P21/00 , A61P25/02 , A61P25/20 , A61P43/00 , C07D471/04 , C07D487/04 , C07D491/04 , C07D498/04 , C07D513/04 , C07K1/02 , C07K5/02 , C07K5/023 , C07K5/06 , C07K5/062
CPC分类号： C07D487/04 , A61K38/00 , C07D471/04 , C07D491/04 , C07D513/04 , C07K5/0202 , C07K5/0205 , C07K5/0207 , C07K5/021 , C07K5/06026
摘要： PROBLEM TO BE SOLVED: To provide a compound having a growth hormone secretagogue effect and capable of increasing a level of an endogenous growth hormone, to provide a pharmaceutically acceptable salt thereof, and to provide a pharmaceutical composition containing the same. SOLUTION: This compound comprises a dipeptide derivative having a specified structure, increases endogenous production or release of the growth hormone of a human or other animals, and is effective for treating and preventing osteoporosis and/or infirmity. The pharmaceutical composition which is given by combining the dipeptide derivative with a bisphosphonate salt compound, such as alendronate, and further with estrogen, premarin, calcitonin, etc., is effective for treating the diseases. COPYRIGHT: (C)2004,JPO
摘要翻译：待解决的问题：提供具有生长激素促分泌作用并且能够增加内源性生长激素水平的化合物，以提供其药学上可接受的盐，并提供含有其的药物组合物。解决方案：该化合物包含具有特定结构的二肽衍生物，增加人或其他动物的生长激素的内源性产生或释放，并且对于治疗和预防骨质疏松症和/或虚弱是有效的。通过将二肽衍生物与二膦酸盐化合物如阿仑膦酸盐进一步组合并进一步与雌激素，雌激素，降钙素等组合而成的药物组合物对于治疗疾病是有效的。版权所有（C）2004，JPO

9. 发明专利

JP2004043476A Dipeptide derivative as growth hormone secretion-accelerating agent 有权
标题翻译：作为生长激素分泌促进剂的二氢睾酮衍生物
公开(公告)号：JP2004043476A
公开(公告)日：2004-02-12
申请号：JP2003271589
申请日：2003-07-07
申请人： Pfizer Inc , ファイザー・インク
发明人： CARPINO PHILIP ALBERT , GRIFFITH DAVID ANDREW , LEFKER BRUCE ALLEN
IPC分类号： A61K31/138 , A61K31/40 , A61K31/4168 , A61K31/4174 , A61K31/437 , A61K31/4439 , A61K31/4453 , A61K31/4535 , A61K31/4725 , A61K31/4985 , A61K31/565 , A61K31/663 , A61K38/00 , A61K38/04 , A61K38/22 , A61K38/23 , A61K38/27 , A61K45/00 , A61P3/00 , A61P3/02 , A61P3/04 , A61P3/08 , A61P3/10 , A61P5/06 , A61P5/10 , A61P7/00 , A61P9/04 , A61P13/12 , A61P15/00 , A61P15/14 , A61P17/00 , A61P17/02 , A61P19/00 , A61P19/08 , A61P19/10 , A61P21/00 , A61P25/02 , A61P25/20 , A61P43/00 , C07D471/04 , C07D487/04 , C07D491/04 , C07D498/04 , C07D513/04 , C07K1/02 , C07K5/02 , C07K5/023 , C07K5/06 , C07K5/062
CPC分类号： C07D487/04 , A61K38/00 , C07D471/04 , C07D491/04 , C07D513/04 , C07K5/0202 , C07K5/0205 , C07K5/0207 , C07K5/021 , C07K5/06026
摘要： PROBLEM TO BE SOLVED: To provide a dipeptide compound as a growth hormone secretion-accelerating agent and useful as the treatment and prevention of osteoporosis and weakness. SOLUTION: This dipeptide derivative as the growth hormone secretion-accelerating agent is a compound expressed by formula 1 (wherein, HET is a heterocycle residue: R 3 is an alkyl, a cycloalkyl or the like: R 4 is H, an alkyl, a cycloalkyl or the like; R 6 is a group having a 3 to 7-membered ring or the like containing an element selected from oxygen, sulfur and nitrogen; and R 7 , R 8 are each independently H or a substituted alkyl), a mixture of its stereo isomers or a pharmaceutically permissible salt as its prodrug. COPYRIGHT: (C)2004,JPO
摘要翻译：要解决的问题：提供二肽化合物作为生长激素分泌促进剂，并且可用作治疗和预防骨质疏松和虚弱。解决方案：作为生长激素分泌促进剂的二肽衍生物是由式1表示的化合物（其中，HET是杂环残基：R 3是烷基，环烷基等：R 4是H，烷基，环烷基等; R 6是具有3〜7元环等的基团，其含有选自以下的元素：氧，硫和氮;以及R“SP”，R“SP”8各自独立地为H或取代的烷基），其立体异构体的混合物或其药学上可允许的盐作为其前药。版权所有（C）2004，JPO

10. 发明申请

WO2011058474A8 N1-PYRAZOLOSPIROKETONE ACETYL-COA CARBOXYLASE INHIBITORS 审中-公开
标题翻译： N1-PYRAZOLOSPIROKETONE乙酰辅酶C羧酸酶抑制剂
公开(公告)号：WO2011058474A8
公开(公告)日：2012-04-26
申请号：PCT/IB2010054908
申请日：2010-10-29
申请人： PFIZER , BAGLEY SCOTT WILLIAM , GRIFFITH DAVID ANDREW , KUNG DANIEL WEI-SHUNG
发明人： BAGLEY SCOTT WILLIAM , GRIFFITH DAVID ANDREW , KUNG DANIEL WEI-SHUNG
IPC分类号： C07D471/10 , A61K31/438 , A61P1/16 , A61P3/10
CPC分类号： C07D471/10 , C07D519/00
摘要： The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3 and R4 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl- CoA carboxylase enzyme(s) in an animal.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐，其中R 1，R 2，R 3和R 4如本文所述; 其药物组合物; 以及其用于治疗通过抑制动物体内的乙酰辅酶A羧化酶调节的疾病，病症或病症的用途。

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