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1. 发明专利

JP2003261565A NEW POLYMORPH 审中-公开
公开(公告)号：JP2003261565A
公开(公告)日：2003-09-19
申请号：JP2003101700
申请日：2003-04-04
申请人： PFIZER PROD INC
发明人： BUSCH FRANK ROBERT , CHIU CHARLES KWOK-FUNG , MELTZ CLIFFORD NATHANIEL , POST RONALD JAMES , ROSE PETER ROBERT
IPC分类号： C07K5/00 , A61K31/437 , A61K38/00 , A61P5/00 , A61P19/10 , C07B57/00 , C07D20060101 , C07D471/04 , C07K5/02 , C07K5/06
摘要： PROBLEM TO BE SOLVED: To provide a new polymorph used for producing a growth hormone secretion promoter in an improved chemical and optical yield. SOLUTION: This polymorph comprises a dihydrate of the formula (XX) (Chinese characteristics in the formula mean 'L-tartrate salt'). COPYRIGHT: (C)2003,JPO

2. 发明专利

JP2003327585A Method for producing growth hormone secretion- promoting drug 有权
标题翻译：生产生长激素分泌促进药物的方法
公开(公告)号：JP2003327585A
公开(公告)日：2003-11-19
申请号：JP2003101688
申请日：2003-04-04
申请人： Pfizer Prod Inc , ファイザー・プロダクツ・インク
发明人： BUSCH FRANK ROBERT , CHIU CHARLES KWOK-FUNG , MELTZ CLIFFORD NATHANIEL , POST RONALD JAMES , ROSE PETER ROBERT
IPC分类号： C07K5/00 , A61K31/437 , A61K38/00 , A61P5/00 , A61P19/10 , C07B57/00 , C07D20060101 , C07D471/04 , C07K5/02 , C07K5/06
CPC分类号： C07K5/0202 , A61K38/00 , C07D471/04 , C07K5/06191 , Y02P20/55
摘要： PROBLEM TO BE SOLVED: To provide a method for producing a growth hormone secretion- promoting drug in improved chemical and optical yields.
SOLUTION: The improved method for producing a compound of formula II and a compound of formula III is provided (in these formulae II and III, R
1 , R
2 and R
3 and Rrt are the same as described in the Specification).
COPYRIGHT: (C)2004,JPO
摘要翻译：待解决的问题：提供一种以提高的化学和光学产率生产生长激素分泌促进药物的方法。解决方案：提供了制备式II化合物和式III化合物的改进方法（在这些式II和III中，R 1，R 2，R 2，和R 3 和Rrt与说明书中描述的相同）。版权所有（C）2004，JPO

3. 发明专利

JP2000247974A PRODUCTION OF GROWTH HORMONE SECRETION PROMOTIVE AGENT 失效
公开(公告)号：JP2000247974A
公开(公告)日：2000-09-12
申请号：JP2000047626
申请日：2000-02-24
申请人： PFIZER PROD INC
发明人： BUSCH FRANK ROBERT , CHIU CHARLES KWOK-FUNG , MELTZ CLIFFORD NATHANIEL , POST RONALD JAMES , ROSE PETER ROBERT
IPC分类号： C07K5/00 , A61K31/437 , A61K38/00 , A61P5/00 , A61P19/10 , C07B57/00 , C07D20060101 , C07D471/04 , C07K5/02 , C07K5/06
摘要： PROBLEM TO BE SOLVED: To obtain an intermediate for producing the subject medicament in high yield by mixing a specific chiral tartaric acid salt with an organic amine in an inert solvent within a specific temperature range and then adding a specific carboxylic acid compound and a coupling reagent successively to the slurry formed above so as to avoid any cryogenic filtration operation. SOLUTION: This intermediate of formula III is obtained by mixing a chiral tartaric acid salt of formula I (R1 is a 1-10C alkyl substitutable

4. 发明申请

WO0189570A3 COMBINATION OF GROWTH HORMONE SECRETAGOGUES AND ANTIDEPRESSANTS 审中-公开
标题翻译：生长激素分泌素和抗生素的组合
公开(公告)号：WO0189570A3
公开(公告)日：2002-06-20
申请号：PCT/IB0100815
申请日：2001-05-10
申请人： PFIZER PROD INC , BUSCH FRANK ROBERT , WELCH WILLARD MCKOWAN JR
发明人： BUSCH FRANK ROBERT , WELCH WILLARD MCKOWAN JR
IPC分类号： A61K45/06 , A61K31/135 , A61K31/136 , A61K31/343 , A61K31/437 , A61K31/438 , A61K31/4406 , A61K31/445 , A61K31/454 , A61K31/4745 , A61K31/4985 , A61K31/55 , A61K38/05 , A61K38/22 , A61P1/02 , A61P3/00 , A61P5/10 , A61P9/00 , A61P19/00 , A61P21/00 , A61P25/00 , A61P25/24 , A61P43/00
CPC分类号： A61K45/06 , A61K31/135 , A61K31/438 , A61K38/08 , A61K2300/00
摘要： This invention is directed to combinations comprising a growth hormone secretagogue, a prodrug thereof or a pharmaceutically acceptable salt of said growth hormone secretagogue or said prodrug and an antidepressant, a prodrug thereof or a pharmaceutically acceptable salt of said antidepressant or said prodrug and to pharmaceutical compositions and kits comprising such combinations. Antidepressants within the scope of this invention include norepinephrine reuptake inhibitors (e.g., secondary and tertiary amine tricyclics), selective sertraline reuptake inhibitors, agents which are combined norepinephrine/sertraline reuptake inhibitors, monoamine oxidase inhibitors and atypical antidepressants. This invention is also directed to methods of improving the physical and/or psychological condition of a patient undergoing a medical procedure, to methods of treating musculoskeletal frailty, to methods of treating congestive heart failure and to methods of attenuating protein catabolic response after a major operation comprising administering such a combination. In particular, this invention relates to such compositions and kits that improve the cardiac function, metabolism, muscle tone and/or mental state of patients undergoing a medical procedure. The compositions and kits of this invention are also useful in treating central nervous system disorders of patients undergoing a medical procedure.
摘要翻译：本发明涉及包含生长激素促分泌素，其前药或所述生长激素促分泌素或所述前药的药学上可接受的盐和抗抑郁药，其前药或所述抗抑郁药或所述前药的药学上可接受的盐和药物组合物和包含这种组合的试剂盒。本发明范围内的抗抑郁药包括去甲肾上腺素再摄取抑制剂（例如仲胺和叔胺三环素），选择性舍曲林再摄取抑制剂，联合去甲肾上腺素/舍曲林再摄取抑制剂，单胺氧化酶抑制剂和非典型抗抑郁药。本发明还涉及改善接受医学过程的患者的身体和/或心理状况，治疗肌肉骨骼虚弱的方法，治疗充血性心力衰竭的方法以及在主要手术后减弱蛋白质分解代谢反应的方法的方法包括施用这样的组合。特别地，本发明涉及这样的组合物和试剂盒，其改善了经历医疗程序的患者的心脏功能，代谢，肌肉紧张度和/或精神状态。本发明的组合物和试剂盒也可用于治疗经历医疗过程的患者的中枢神经系统疾病。

5. 发明申请

WO2007110730A3 VARENICLINE STANDARDS AND IMPURITY CONTROLS 审中-公开
标题翻译： VARENICLINE标准和污染控制
公开(公告)号：WO2007110730A3
公开(公告)日：2007-12-13
申请号：PCT/IB2007000722
申请日：2007-03-15
申请人： PFIZER PROD INC , BRONK KAREN SROUR , BUSCH FRANK ROBERT , SINAY TERRY GENE , WITHBROE GREGORY JOHN
发明人： BRONK KAREN SROUR , BUSCH FRANK ROBERT , SINAY TERRY GENE , WITHBROE GREGORY JOHN
IPC分类号： A61K31/439 , A61K31/498 , A61P1/00 , A61P3/00 , A61P9/00 , A61P25/00 , A61P25/34
CPC分类号： A61K31/439 , A61K31/498 , Y10T436/147777
摘要： The subject invention provides a varenicline composition that comprises varenicline, or a pharmaceutically acceptable salt thereof, and an amount of a compound selected from one or more of several mononitro, monoamine mixed aminonitro, diamino or dinitro intermediates, and the concentration of said compound is greater than 0 ppm and not greater than about 500 ppm, not greater than about 100 ppm or not greater than about 10 ppm. Methods for synthesizing and using such varenicline compositions are also provided.
摘要翻译：本发明提供一种伐伦赛克组合物，其包含伐伦克林或其药学上可接受的盐和一定量的选自几个单硝基，单胺混合氨基硝基，二氨基或二硝基中间体中的一种或多种的化合物，并且所述化合物的浓度更大不超过约0ppm，不大于约500ppm，不大于约100ppm或不大于约10ppm。还提供了合成和使用这种伐伦尼克组合物的方法。

6. 发明专利

BRPI0000967B8 processos para preparação de compostos secretagogos de hormônio de crescimento 未知
公开(公告)号：BRPI0000967B8
公开(公告)日：2021-07-06
申请号：BRPI0000967
申请日：2000-02-28
申请人： PFIZER PROD INC
发明人： BUSCH FRANK ROBERT , CHIU CHARLES KWOK-FUNG , MELTZ CLIFFORD NATHANIEL , POST RONALD JAMES , ROSE PETER ROBERT
IPC分类号： C07K5/00 , A61K31/437 , A61K38/00 , A61P5/00 , A61P19/10 , C07B57/00 , C07D20060101 , C07D471/04 , C07K5/02 , C07K5/06

7. 发明专利

BRPI0607838A2 未知
公开(公告)号：BRPI0607838A2
公开(公告)日：2009-06-13
申请号：BRPI0607838
申请日：2006-02-21
申请人： PFIZER PROD INC
发明人： BUSCH FRANK ROBERT , HAWKINS JOEL MICHAEL , MUSTAKIS LANSON GEORGIOS , SINAY TERRY GENE JR , WATSON TIMOTHY JAMES NORMAN , WITHBROE GREGORY JOHN
IPC分类号： C07D471/08
摘要： The present invention comprises an improved process for the preparation of substituted quinoxaline I by cyclization of the corresponding dianiline.

8. 发明专利

SI1476162T1 Nadzirana sinteza ziprasidona 未知
公开(公告)号：SI1476162T1
公开(公告)日：2007-08-31
申请号：SI200330811
申请日：2003-02-17
申请人： PFIZER PROD INC
发明人： BUSCH FRANK ROBERT , GROBIN ADAM WORTH , HOWARD HARRY RALPH JR , LEEMAN KYLE ROBERT
IPC分类号： A61K31/00 , C07D417/12 , A61K20060101 , A61K31/496 , A61P20060101 , A61P25/00 , A61P25/06 , A61P25/14 , A61P25/22 , A61P25/28 , A61P27/06

9. 发明专利

PL195209B1 Środek farmaceutyczny i zastosowanie krystalicznego zyprazydonu 未知
公开(公告)号：PL195209B1
公开(公告)日：2007-08-31
申请号：PL33373799
申请日：1999-06-14
申请人： PFIZER PROD INC
发明人： BUSCH FRANK ROBERT , HAUSBERGER ANGELA CAROL GATLIN , RASADI BIJAN , ARENSON DANIEL RAY
IPC分类号： A61K31/495 , A61K31/496 , A61K9/00 , A61K9/14 , A61K9/16 , A61K9/48 , A61K31/00 , A61K31/54 , A61K47/26 , A61P25/18 , C07D417/12

10. 发明专利

CZ297954B6 Farmaceutická kompozice na bázi ziprasidonu a zpusob výroby velkých krystalu monohydrátu hydrochloridu ziprasidonu 未知
公开(公告)号：CZ297954B6
公开(公告)日：2007-05-09
申请号：CZ212799
申请日：1999-06-14
申请人： PFIZER PROD INC
发明人： BUSCH FRANK ROBERT , HAUSBERGER ANGELA CAROL GATLIN , RASADI BIJAN , ARENSON DANIEL RAY
IPC分类号： A61K31/495 , A61K31/496 , A61K9/00 , A61K9/14 , A61K9/16 , A61K9/48 , A61K31/00 , A61K31/54 , A61K47/26 , A61P25/18 , C07D417/12
摘要： Farmaceutická kompozice obsahující cástice krystalické volné báze ziprasidonu nebo krystalického hydrochloridu ziprasidonu, jejichz strední velikost je 85 .mi.m nebo mensí, a farmaceuticky vhodné redidlo nebo nosic. Zpusob výroby velkých krystalu monohydrátu hydrochloridu ziprasidonu, pri nemz se 1) volná báze ziprasidonu rozpustí v rozpoustedle obsahujícím tetrahydrofuran a vodu v objemovém pomeru 22 az 35 objemových jednotek tetrahydrofuranu na 1,5 az 8 objemových jednotek vody; 2) roztok pripravený ve stupni 1 se zahrívá; 3) k roztoku pripravenému ve stupni 2 se pridá chlorovodík; a 4) roztok pripravený ve stupni 3 se ochladí.

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