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1. 发明申请

WO2005116014A1 PROLINE DERIVATIVES AND THEIR USE AS DIPEPTIDYL PEPTIDASE IV INHIBITORS 审中-公开
标题翻译：丙泊酚衍生物及其作为DIPEPTIDYL PEPTIDAS IV抑制剂的用途
公开(公告)号：WO2005116014A1
公开(公告)日：2005-12-08
申请号：PCT/IB2005/001194
申请日：2005-04-29
申请人： PFIZER PRODUCTS INC. , HULIN, Bernard , PIOTROWSKI, David, Walter
发明人： HULIN, Bernard , PIOTROWSKI, David, Walter
IPC分类号： C07D403/14
CPC分类号： C07D207/14 , C07D275/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D498/04
摘要： The invention provides compounds of formula (I), prodrugs and stereoisomers thereof, and the pharmaceutically acceptable salts of the compounds, prodrugs, and stereoisomers, wherein R 1 , R 2 , R 3 , HET, n, Q, X, Y, and Z are as described herein; compositions thereof; and uses thereof in treating diabetic complications including diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, and the like.
摘要翻译：本发明提供式（I）化合物，其前体药物和立体异构体，以及化合物，前药和立体异构体的药学上可接受的盐，其中R 1，R 2，R 3，HET，n，Q X，Y和Z如本文所述; 组合物; 及其用于治疗糖尿病性神经病变，糖尿病性肾病，糖尿病性微血管病变等糖尿病并发症的用途。

2. 发明申请

WO2004085433A3 POSITIVE ALLOSTERIC MODULATORS OF THE NICOTINIC ACETYLCHOLINE RECEPTOR 审中-公开
标题翻译：烟碱型乙酰胆碱受体阳性调节因子
公开(公告)号：WO2004085433A3
公开(公告)日：2004-12-16
申请号：PCT/IB2004000838
申请日：2004-03-15
申请人： UPJOHN CO , ROGERS BRUCE NELSEN , PIOTROWSKI DAVID WALTER , MARGOLIS BRANDON JEROME , MYERS JASON KENNETH , GROPPI VINCENT EDWARD JR , RUDMANN DANIEL GREGORY
发明人： ROGERS BRUCE NELSEN , PIOTROWSKI DAVID WALTER , MARGOLIS BRANDON JEROME , MYERS JASON KENNETH , GROPPI VINCENT EDWARD JR , RUDMANN DANIEL GREGORY
IPC分类号： C07D413/12 , C07D417/12 , G01N33/68 , G01N33/94 , A61K31/42 , A61K31/422 , A61K31/427 , A61K31/433 , A61K31/4439
CPC分类号： C07D417/12 , C07D413/12 , G01N33/6893 , G01N33/944
摘要： The invention provides compounds of Formula (I). These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals used to treat diseases or conditions in which alpha7 nAChR is known to be involved.
摘要翻译：本发明提供了式（I）的化合物。这些化合物可以是药物盐或组合物的形式，可以是纯对映体形式或外消旋混合物，并且可用于用于治疗已知α7nAChR参与的疾病或病症的药物。

3. 发明申请

WO2006067611A1 METHODS OF MODULATING THE ACTIVITIES OF ALPHA7 NICOTINIC ACETYLCHOLINE RECEPTOR 审中-公开
标题翻译：调节ALPHA7 NICOTINIC乙酰胆碱受体活性的方法
公开(公告)号：WO2006067611A1
公开(公告)日：2006-06-29
申请号：PCT/IB2005/003925
申请日：2005-12-14
申请人： PFIZER PRODUCTS INC. , GROPPI, Vincent, Edward, Jr. , HURST, Raymond, Stuart , PIOTROWSKI, David, Walter
发明人： GROPPI, Vincent, Edward, Jr. , HURST, Raymond, Stuart , PIOTROWSKI, David, Walter
IPC分类号： G01N33/48 , A61P25/18 , A61P3/04 , A61K31/17 , A61K31/433 , A61K31/42 , A61K31/44
CPC分类号： A61K31/17 , A61K31/42 , A61K31/433 , A61K31/44 , G01N33/944 , Y02A50/411
摘要： The present invention provides methods for identifying compounds useful in modulating a7 nicotinic acetylcholine receptors. The invention also provides compounds that prevent, suppress or inhibit desensitization of an a7 nicotinic acetylcholine receptor, and which resensitize such receptors. Pharmaceutical compositions, and methods of treatment, particularly in regard of neurological diseases are also described.
摘要翻译：本发明提供鉴定可用于调节烟碱乙酰胆碱受体的化合物的方法。本发明还提供了预防，抑制或抑制a7烟碱乙酰胆碱受体的脱敏作用并使这种受体复敏的化合物。还描述了药物组合物和治疗方法，特别是在神经系统疾病方面。

4. 发明申请

WO2004039815A3 COMPOUNDS HAVING BOTH ALPHA7 NACHR AGONIST AND ANTAGONIST ACTIVITY FOR TREATMENT OF CNS DISEASES 审中-公开
标题翻译：具有两种ALPHA7 NACHR激动剂的化合物和用于治疗CNS疾病的拮抗剂活性
公开(公告)号：WO2004039815A3
公开(公告)日：2004-07-22
申请号：PCT/IB0304681
申请日：2003-10-20
申请人： UPJOHN CO , WONG ERIK HO FONG , CORTES-BURGOS LUZ AMPARO , ROGERS BRUCE NELSEN , PIOTROWSKI DAVID WALTER , WALKER DANIEL PATRICK , JACOBSEN ERIC JON , WISHKA DONN GREGORY , ACKER BRAD ALAN
发明人： WONG ERIK HO FONG , CORTES-BURGOS LUZ AMPARO , ROGERS BRUCE NELSEN , PIOTROWSKI DAVID WALTER , WALKER DANIEL PATRICK , JACOBSEN ERIC JON , WISHKA DONN GREGORY , ACKER BRAD ALAN
IPC分类号： C07D453/02 , C07D487/08 , C07D519/00 , A61K31/439
CPC分类号： C07D487/08 , C07D453/02 , Y02P20/55
摘要： The invention discloses compounds that are selective alpha7 nAChR agonists and 5-HT3 antagonists. The compounds are useful for treating many CNS diseases. The compounds have the following Formula (I): Azabicyclo-N(H)-C(=O)-W wherein Azabicyclo is Formula (2) each R1 is independently H, alkyl, or substituted alkyl; R2 is H, alkyl, or substituted alkyl; k is 1 or 2, provided that one R2 is other than H when k is 2; R3 is H, alkyl, or an amino protecting group; W is Formula (3); W is CH or N; W is O, N(R4), N(C(O)R4), or S; W is O, N(R4), N(C(O)R4), or S; R is H, F, Cl, Br, I, alkyl, substituted alkyl, or alkynyl; Alkyl is both straight- and branched-chain moieties having from 1-6 carbon atoms.
摘要翻译：本发明公开了选择性α7nAChR激动剂和5-HT3拮抗剂的化合物。该化合物可用于治疗许多CNS疾病。化合物具有下式（I）：氮杂双环-N（H）-C（= O）-W 0，其中，氮杂双环是式（2），每个R 1独立地是H，烷基或取代的烷基; R2是H，烷基或取代的烷基; k为1或2，条件是当k为2时，一个R2不为H; R3是H，烷基或氨基保护基; W 0是式（3）; W是CH或N; W 1是O，N（R 4），N（C（O）R 4）或S; W 2是O，N（R 4），N（C（O）R 4）或S; R是H，F，Cl，Br，I，烷基，取代的烷基或炔基; 烷基是具有1-6个碳原子的直链和支链部分。

5. 发明申请

WO2004039815A2 COMPOUNDS HAVING BOTH α7 NICOTINIC AGONIST ACTIVITY AND 5HT3 ANTAGONIST ACTIVITY FOR TREATMENT OF CNS DISEASES 审中-公开
标题翻译：具有两种α7非诺酮激动剂的化合物和5HT3拮抗剂治疗CNS疾病的活性
公开(公告)号：WO2004039815A2
公开(公告)日：2004-05-13
申请号：PCT/IB2003/004681
申请日：2003-10-20
申请人： PHARMACIA & UPJOHN COMPANY , WONG, Erik, Ho Fong , CORTES-BURGOS, Luz, Amparo , ROGERS, Bruce, Nelsen , PIOTROWSKI, David, Walter , WALKER, Daniel, Patrick , JACOBSEN, Eric, Jon , WISHKA, Donn, Gregory , ACKER, Brad, Alan
发明人： WONG, Erik, Ho Fong , CORTES-BURGOS, Luz, Amparo , ROGERS, Bruce, Nelsen , PIOTROWSKI, David, Walter , WALKER, Daniel, Patrick , JACOBSEN, Eric, Jon , WISHKA, Donn, Gregory , ACKER, Brad, Alan
IPC分类号： C07D519/00
CPC分类号： C07D487/08 , C07D453/02 , Y02P20/55
摘要： The invention discloses compounds that are selective α7 nAChR agonists and 5-HT 3 antagonists. The compounds are useful for treating many CNS diseases.
摘要翻译：本发明公开了选择性α7nAChR激动剂和5-HT3拮抗剂的化合物。该化合物可用于治疗许多CNS疾病。

6. 发明申请

WO2010116282A8 4, 5-DIHYDRO-1H-PYRAZOLE COMPOUNDS AND THEIR PHARMACEUTICAL USES 审中-公开
标题翻译： 4,5-二氢-1H-吡唑化合物及其药物用途
公开(公告)号：WO2010116282A8
公开(公告)日：2011-11-03
申请号：PCT/IB2010051337
申请日：2010-03-26
申请人： PFIZER , ARHANCET GRACIELA BARBIERI , CASIMIRO-GARCIA AGUSTIN , CHEN XIANGYANG , HEPWORTH DAVID , MEYERS MARVIN JAY , PIOTROWSKI DAVID WALTER , RAHEJA RAJ KUMAR
发明人： ARHANCET GRACIELA BARBIERI , CASIMIRO-GARCIA AGUSTIN , CHEN XIANGYANG , HEPWORTH DAVID , MEYERS MARVIN JAY , PIOTROWSKI DAVID WALTER , RAHEJA RAJ KUMAR
IPC分类号： C07D401/04 , A61K31/44 , A61P3/04 , A61P9/00 , A61P29/00 , C07D401/14 , C07D413/14
CPC分类号： C07D401/04 , C07D401/14 , C07D413/14
摘要： Mineralocorticoid receptor antagonists (MRa), pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, diabetic nephropathy and hypertension in mammals, including humans.
摘要翻译：皮质激素受体拮抗剂（MRa），含有这些抑制剂的药物组合物，以及这些抑制剂在哺乳动物（包括人）中治疗例如糖尿病肾病和高血压的用途。

7. 发明申请

WO2010116282A1 4, 5-DIHYDRO-LH-PYRAZOLE COMPOUNDS AND THEIR PHARMACEUTICAL USES 审中-公开
标题翻译： 4，5-二氢-2H-吡唑化合物及其药物用途
公开(公告)号：WO2010116282A1
公开(公告)日：2010-10-14
申请号：PCT/IB2010/051337
申请日：2010-03-26
申请人： PFIZER INC. , ARHANCET, Graciela Barbieri , CASIMIRO-GARCIA, Agustin , CHEN, Xiangyang , HEPWORTH, David , MEYERS, Marvin Jay , PIOTROWSKI, David Walter , RAHEJA, Raj Kumar
发明人： ARHANCET, Graciela Barbieri , CASIMIRO-GARCIA, Agustin , CHEN, Xiangyang , HEPWORTH, David , MEYERS, Marvin Jay , PIOTROWSKI, David Walter , RAHEJA, Raj Kumar
IPC分类号： C07D401/04 , C07D401/14 , C07D413/14 , A61K31/44 , A61P3/04 , A61P29/00 , A61P9/00
CPC分类号： C07D401/04 , C07D401/14 , C07D413/14
摘要： Mineralocorticoid receptor antagonists (MRa), pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, diabetic nephropathy and hypertension in mammals, including humans.
摘要翻译：皮质激素受体拮抗剂（MRa），含有这些抑制剂的药物组合物，以及这些抑制剂在哺乳动物（包括人）中治疗例如糖尿病肾病和高血压的用途。

8. 发明申请

WO2007148185A3 SUBSTITUTED 3 -AMINO- PYRROLIDINO-4 -LACTAMS AS DPP INHIBITORS 审中-公开
公开(公告)号：WO2007148185A3
公开(公告)日：2007-12-27
申请号：PCT/IB2007/001588
申请日：2007-06-11
申请人： PFIZER PRODUCTS INC. , BENBOW, John, William , PIOTROWSKI, David, Walter , HUI, Yu
发明人： BENBOW, John, William , PIOTROWSKI, David, Walter , HUI, Yu
IPC分类号： C07D401/14 , C07D403/14 , C07D498/04 , A61K31/506 , A61P3/00 , C07D405/14 , C07D409/14 , C07D417/14 , C07D471/04 , C07D495/04 , C07D513/04 , A61K31/502 , A61K31/53 , A61K31/4025 , A61K31/4427 , A61K31/517 , A61K31/404 , A61K31/52 , C07D473/34
摘要： The invention provides compounds of formula (1), and the pharmaceutically acceptable salt thereof, wherein R 1 , n and R 2 are as described herein; compositions thereof and uses as DPP inhibitors.

9. 发明申请

WO2006008644A1 ANTIDIABETIC COMPOUNDS 审中-公开
标题翻译：抗菌化合物
公开(公告)号：WO2006008644A1
公开(公告)日：2006-01-26
申请号：PCT/IB2005/002159
申请日：2005-07-01
申请人： PFIZER PRODUCTS INC. , CABRAL, Shawn , HULIN, Bernard , PIOTROWSKI, David, Walter
发明人： CABRAL, Shawn , HULIN, Bernard , PIOTROWSKI, David, Walter
IPC分类号： C07D207/16
CPC分类号： C07D207/16 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/12
摘要： The invention provides compounds of formula (I), prodrugs and stereoisomers thereof, and the pharmaceutically acceptable salts of the compounds, prodrugs, and stereoisomers, wherein R 1 is hydrogen, -(C 1 -C 6 )alkyl, -(C 1 -C 6 )alkoxy, -(C 1 -C 6 )arylalkyl, -NR a R b , hydroxy, cyano, arly or heteroaryl, wherein said -(C 1 -C 6 )alkyl, said aryl, or said heteroaryl is optionally substituted independently with one to three -COOH, -C(O)(C 1 -C 6 )alkyl, -C(O)NR a R b cyano, halogen, nitro, trifluoromethyl, -(C 1 -C 6 )alkyl, --(C 1 -C 6 )alkoxy, -(C 3 -C 6 )cycloalkyl or phenyl, wherein: R a and R b are, independently, hydrogen, -(C 1 -C 6 )alkyl, aryl or heteroaryl or R a and R b , taken together with the nitrogen atom to which they are attached, form a four- to six- membered heterocyclic ring, wherein said ring optionally incorporates an additional one or two nitrogen, oxygen or sulfur ring heteroatoms; R 2 and R 3 are, independently, hydrogen, halogen, -(C 1 -C 6 )alkyl, or -(C 3 -C 8 )cycloalkyl; R 4 is (i) hydrogen, (ii) - COOH, (iii) -C(O)(C 1 -C 6 )alkoxy, (iv) -C(O)(C 1 -C 6 )alkyl, (v) -C(O)NR a R b , (vi) cyano or (vii) -(C 1 -C 6 )alkyl, optionally substituted with one to six halogen atoms, -(C 1 -C 6 )alkoxy, cyano, hydroxy, or -NR a R b , (viii) -(C 3 -C 6 )cycloalkyl, (ix) -(C 1 -C 6 )arylalkyl, (x) aryl, or (xi) heteroaryl; Q is a covalent bond, -C(O)-, or -SO 2- ; HET is heterocycloalkyl ring, moiety, optionally substituted independently with: (A) one to four -(C 1 -C 6 )alkyl optionally substituted with one to six halogen atoms, -(C 1 -C 6 )alkoxy, cyano, halogen, hydroxy, or -NR a R b , or (B) -(C 1 -C 6 )aralkyl, optionally substituted with on to six halogen atoms, -(C 1 -C 6 )alkoxy, cyano, halogen, hydroxy, or -NR a R b ; n is zero or one; X is hydrogen or cyano; and Y is -CH 2 -, -S-, -S(O)-, or -SO 2 ; provided that R 2 , R 3 and R 4 are not all hydrogen; compositions thereof; and uses thereof in treating diabetic complications including diabetic neuropathy diabetic nephropathy, diabetic microangiopathy, and the like.
摘要翻译：本发明提供式（I）化合物，其前体药物和立体异构体，以及化合物，前药和立体异构体的药学上可接受的盐，其中R

10. 发明申请

WO2011141848A1 MORPHOLINE COMPOUNDS AS MINERALOCORTICOID RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吗啉化合物作为矿物质受体拮抗剂
公开(公告)号：WO2011141848A1
公开(公告)日：2011-11-17
申请号：PCT/IB2011/051883
申请日：2011-04-28
申请人： PFIZER INC. , CASIMIRO-GARCIA, Agustin , FUTATSUGI, Kentaro , PIOTROWSKI, David Walter
发明人： CASIMIRO-GARCIA, Agustin , FUTATSUGI, Kentaro , PIOTROWSKI, David Walter
IPC分类号： C07D413/04 , C07D417/04 , C07D419/04 , C07D498/04 , A61K31/5377 , A61P9/12
CPC分类号： C07D498/04 , C07D413/04 , C07D417/04 , C07D419/04
摘要： Mineralocorticoid receptor antagonists (MRa), pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, diabetic nephropathy and hypertension in mammals, including humans.
摘要翻译：皮肤激素受体拮抗剂（MRa），含有这些抑制剂的药物组合物以及这些抑制剂在哺乳动物（包括人）中治疗例如糖尿病肾病和高血压的用途。

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