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11. 发明申请

WO2007148185A2 SUBSTITUTED 3 -AMINO- PYRR0LIDIN0-4 -LACTAMS AS DPP INHIBITORS 审中-公开
标题翻译：作为DPP抑制剂取代3 -AMINO- PYRR0LIDIN0-4 -LACTAMS
公开(公告)号：WO2007148185A2
公开(公告)日：2007-12-27
申请号：PCT/IB2007001588
申请日：2007-06-11
申请人： PFIZER PROD 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 , A61K31/4025 , A61K31/404 , A61K31/4427 , A61K31/502 , A61K31/506 , A61K31/517 , A61K31/52 , A61K31/53 , A61P3/00 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D471/04 , C07D473/34 , C07D495/04 , C07D498/04 , C07D513/04
CPC分类号： C07D401/04 , C07D207/27 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D473/34 , C07D498/04
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.
摘要翻译：本发明提供式（1）化合物及其药学上可接受的盐，其中R 1，n和R 2如本文所述; 其组合物和用作DPP抑制剂。

12. 发明申请

WO2004039815A8 COMPOUNDS HAVING BOTH ALPHA7 NACHR AGONIST AND 5HT ANTAGONIST ACTIVITY FOR TREATMENT OF CNS DISEASES 审中-公开
标题翻译：具有两种ALPHA7 NACHR激动剂和5HT拮抗剂活性以治疗CNS疾病的化合物
公开(公告)号：WO2004039815A8
公开(公告)日：2004-09-23
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。

13. 发明申请

WO1992020682A1 ARTHROPODICIDAL ANILIDES 审中-公开
标题翻译：抗抑郁药
公开(公告)号：WO1992020682A1
公开(公告)日：1992-11-26
申请号：PCT/US1992003880
申请日：1992-04-30
申请人： E.I. DU PONT DE NEMOURS AND COMPANY , BARNETTE, William, Eldo , HARRISON, Charles, Richard , LAHM, George, Philip , PIOTROWSKI, David, Walter , WING, Keith, Dumont
发明人： E.I. DU PONT DE NEMOURS AND COMPANY
IPC分类号： C07D491/052
CPC分类号： C07D253/10 , C07C281/12 , C07C2602/08 , C07D237/26 , C07D273/04 , C07D491/04
摘要： Substituted anilides of formula (I), wherein Q is one of (Q-1), (Q-2) and (Q-3), and R to R , Y, Z and Z are as defined in the text, arthropodicidal compositions containing such compounds; and a method for controlling arthropods by use of such compounds.
摘要翻译：取代的式（I）的酰苯胺，其中Q是（Q-1），（Q-2）和（Q-3）之一，R 1至R 5，Y，Z和Z 1 如本文所定义的含有这些化合物的节肢动物杀伤组合物; 以及通过使用这些化合物来控制节肢动物的方法。

14. 发明申请

WO2005100334A1 DIPEPTIDYL PEPTIDASE-IV INHIBITORS 审中-公开
标题翻译： DIPEPTIDYL PEPTIDASE-IV抑制剂
公开(公告)号：WO2005100334A1
公开(公告)日：2005-10-27
申请号：PCT/IB2005/000907
申请日：2005-04-01
申请人： PFIZER PRODUCTS INC. , HULIN, Bernard , PARKER, Janice, Catherine , PIOTROWSKI, David, Walter
发明人： HULIN, Bernard , PARKER, Janice, Catherine , PIOTROWSKI, David, Walter
IPC分类号： C07D295/185
CPC分类号： C07D207/10 , C07D207/08 , C07D207/12 , C07D207/16 , C07D207/28 , C07D209/46 , C07D213/82 , C07D231/38 , C07D233/38 , C07D241/24 , C07D241/26 , C07D263/16 , C07D263/18 , C07D263/24 , C07D263/44 , C07D275/06 , C07D295/185 , C07D401/12 , C07D403/12 , C07D417/08 , C07D417/12 , C07D471/04 , C07D487/04 , C07D493/04 , C07D495/04
摘要： The invention provides compounds of Formula (I) or prodrugs thereof, or pharmaceutically acceptable salts of said compounds or prodrugs, or solvates of said compounds, prodrugs or salts, wherein A, N, X and R 1 are as defined herein; pharmaceutical compositions thereof; and methods of using the pharmaceutical compositions for the treatment of diseases, including Type 2 diabetes, Type 1 diabetes, impaired glucose tolerance, hyperglycemia, metabolic syndrome (syndrome X and/or insulin resistance syndrome), glucosuria, metabolic acidosis, arthritis, cataracts, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic cardiomyopathy, obesity, conditions exacerbated by obesity, hypertension, hyperlipidemia, atherosclerosis, osteoporosis, osteopenia, frailty, bone loss, bone fracture, acute coronary syndrome, short stature due to growth hormone deficiency, infertility due to polycystic ovary syndrome, anxiety, depression, insomnia, chronic fatigue, epilepsy, eating disorders, chronic pain, alcohol addiction, diseases associated with intestinal motility, ulcers, irritable bowel syndrome, inflammatory bowel syndrome; short bowel syndrome; and the prevention of disease progression in Type 2 diabetes.
摘要翻译：本发明提供式（I）化合物或其前药，或所述化合物或前药的药学上可接受的盐，或所述化合物，前药或盐的溶剂合物，其中A，N，X和R 1如本文所定义; 其药物组合物; 以及使用该药物组合物治疗疾病的方法，包括2型糖尿病，1型糖尿病，葡萄糖耐量降低，高血糖症，代谢综合征（X综合征和/或胰岛素抵抗综合征），糖尿病，代谢性酸中毒，关节炎，白内障，糖尿病性肾病，糖尿病性肾病，糖尿病性视网膜病变，糖尿病性心肌病，肥胖症，肥胖症，高血压，高脂血症，动脉粥样硬化，骨质疏松症，骨质减少症，虚弱，骨质疏松，骨折，急性冠状动脉综合征，生长激素缺乏引起的身材矮小，不育症由于多囊卵巢综合征，焦虑症，抑郁症，失眠症，慢性疲劳，癫痫，进食障碍，慢性疼痛，酒精成瘾，与肠蠕动相关的疾病，溃疡，肠易激综合征，炎性肠综合征; 短肠综合征并预防2型糖尿病的疾病进展。

15. 发明申请

WO2004085433A2 POSITIVE ALLOSTERIC MODULATORS OF THE NICOTINIC ACETYLCHOLINE RECEPTOR 审中-公开
标题翻译： NICOTINIC乙酰胆碱受体的阳性免疫调节剂
公开(公告)号：WO2004085433A2
公开(公告)日：2004-10-07
申请号：PCT/IB2004/000838
申请日：2004-03-15
申请人： PHARMACIA & UPJOHN COMPANY , 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： C07D413/00
CPC分类号： C07D417/12 , C07D413/12 , G01N33/6893 , G01N33/944 , Y02A50/58
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 α7 nAChR is known to be involved.
摘要翻译：本发明提供式（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其中已知α7nAChR涉及的疾病或病症的药物。

16. 发明申请

WO2004052889A1 COMPOUNDS AS RADIOLIGANDS FOR THE DIAGNOSIS OF DISEASE 审中-公开
标题翻译：化合物作为疾病诊断的放射性物质
公开(公告)号：WO2004052889A1
公开(公告)日：2004-06-24
申请号：PCT/IB2003/005521
申请日：2003-11-24
申请人： PHARMACIA & UPJOHN COMPANY , ROGERS, Bruce, Nelsen , PIOTROWSKI, David, Walter , GROPPI, Vincent, Edward, Jr. , JACOBSEN, Eric, Jon , MYERS, Jason, Kenneth , WALKER, Daniel, Patrick , WISHKA, Donn, Gregory , SKADDAN, Marc, Bradley
发明人： ROGERS, Bruce, Nelsen , PIOTROWSKI, David, Walter , GROPPI, Vincent, Edward, Jr. , JACOBSEN, Eric, Jon , MYERS, Jason, Kenneth , WALKER, Daniel, Patrick , WISHKA, Donn, Gregory , SKADDAN, Marc, Bradley
IPC分类号： C07D453/02
CPC分类号： C07D471/08 , C07B2200/05 , C07D453/02 , C07D487/08
摘要： Radiolabeled ligands useful as probes for determining the relative abundance, receptor occupancy, and/or function of nicotinic acetylcholine receptors. The compounds of Formula I as described herein are labeled with a radioactive isotopic moiety such as 11 C, 18 F, 76 Br, 123 I or 125 I. Disorders are diagnosed by administering to a mammal a detectably labeled compound and detecting the binding of that compound to the nAChR. The compounds that have been administered are detected using methods including, but not limited to, position emission topography and single-photon to emission computed tomography. The present invention is useful in diagnosing a wide variety of diseases and disorders as discussed herein.
摘要翻译：用作确定烟碱乙酰胆碱受体的相对丰度，受体占有率和/或功能的探针的放射性标记配体。如本文所述的式I化合物用放射性同位素部分（例如11 C，18 F，76 Br，123 I或125 I）进行标记。通过向哺乳动物施用可检测标记的化合物并检测该化合物与nAChR的结合来诊断疾病。使用包括但不限于位置发射形貌和单光子到发射计算机断层摄影的方法检测已经施用的化合物。本发明可用于诊断本文所讨论的多种疾病和病症。

17. 发明申请

WO2004052461A1 COMBINATION FOR THE TREATMENT OF ADHD 审中-公开
标题翻译：组合治疗ADHD
公开(公告)号：WO2004052461A1
公开(公告)日：2004-06-24
申请号：PCT/IB2003/005542
申请日：2003-11-28
申请人： PHARMACIA & UPJOHN COMPANY , GROPPI, Vincent, Edward, Jr. , JACOBSEN, Eric, Jon , MYERS, Jason, Kenneth , PIOTROWSKI, David, Walter , ROGERS, Bruce, Nelsen , WALKER, Daniel, Patrick , WISHKA, Donn, Gregory
发明人： GROPPI, Vincent, Edward, Jr. , JACOBSEN, Eric, Jon , MYERS, Jason, Kenneth , PIOTROWSKI, David, Walter , ROGERS, Bruce, Nelsen , WALKER, Daniel, Patrick , WISHKA, Donn, Gregory
IPC分类号： A61P25/00
CPC分类号： A61K45/06 , A61K31/46 , A61K2300/00
摘要： The present invention relates to compositions and methods to treat ADHD with an α7 nAChR full agonist and psychostimulants and/or monoamine reuptake inhibitors.
摘要翻译：本发明涉及用α7nAChR全激动剂和精神兴奋剂和/或单胺再摄取抑制剂治疗ADHD的组合物和方法。

18. 发明申请

WO0222583A3 PYRIDINYL AMIDES AND IMIDES FOR USE AS FUNGICIDES 审中-公开
标题翻译：吡啶酰胺和酰胺用作杀真菌剂
公开(公告)号：WO0222583A3
公开(公告)日：2002-07-18
申请号：PCT/US0128971
申请日：2001-09-17
申请人： DU PONT , NEUBERT TIMOTHY DONALD , PIOTROWSKI DAVID WALTER , WALKER MICHAEL PAUL
发明人： NEUBERT TIMOTHY DONALD , PIOTROWSKI DAVID WALTER , WALKER MICHAEL PAUL
IPC分类号： A01N43/40 , C07D213/82
CPC分类号： C07D213/82 , A01N43/40
摘要： Compounds of Formula (I), their N-oxides and agriculturally suitable salts are disclosed which are useful as fungicides formula (I), (II) wherein A is a substituted pyridinyl ring; B is a substituted pyridinyl ring; W is C=L or SOn is O or S; R and R are each independently H; or C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl or C3-C6 cycloalkyl, each optionally substituted; R is H; or C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl or C3-C6 cycloalkyl, C2-C6 alkylcarbonyl, C2-C6 alkoxycarbonyl, C2-C6 alkylaminocarbonyl or C3-C8 dialkylaminocarbonyl; R is C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl or C3-C6 cycloalkyl, each optionally substituted; X is O or S; and n is 1 or 2; provided that when W is C=O and R , R and R are H; then B is other than 4-trifluoromethyl-3-pyridinyl, 2-chloro-4-pyridinyl and 2,6-dihalo-4-pyridinyl.Also disclosed are compositions containing the compounds of Formula (I) and a method for controlling plant diseases caused by fungal plant pathogens that involves applying an effective amount of a compound of Formula (I).
摘要翻译：公开了式（I）化合物，其N-氧化物和农业上合适的盐，其可用作式（I），（II）的杀真菌剂，其中A是取代的吡啶基环; B是取代的吡啶基环; W是C = L或SOn是O或S; R 1和R 2各自独立地为H; 或各自任选被取代的C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基或C 3 -C 6环烷基; R 3是H; 或C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基或C 3 -C 6环烷基，C 2 -C 6烷基羰基，C 2 -C 6烷氧基羰基，C 2 -C 6烷基氨基羰基或C 3 -C 8二烷基氨基羰基; R 4是各自任选被取代的C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基或C 3 -C 6环烷基; X是O或S; 并且n是1或2; 条件是当W是C = O并且R 1，R 2和R 3是H时; 那么B不是4-三氟甲基-3-吡啶基，2-氯-4-吡啶基和2,6-二卤代-4-吡啶基。还公开了含有式（I）化合物的组合物和防治植物病害的方法由真菌植物病原体引起，涉及施用有效量的式（I）化合物。

19. 发明申请

WO1995003306A1 ARTHROPODICIDAL AZACYCLIC HETEROCYCLES 审中-公开
标题翻译：抗坏血酸菌素杂合物
公开(公告)号：WO1995003306A1
公开(公告)日：1995-02-02
申请号：PCT/US1994008404
申请日：1994-07-21
申请人： E.I. DU PONT DE NEMOURS AND COMPANY , PIOTROWSKI, David, Walter
发明人： E.I. DU PONT DE NEMOURS AND COMPANY
IPC分类号： C07D487/08
CPC分类号： C07D401/04 , A01N43/40 , A01N43/42 , A01N43/82 , A01N43/90 , C07D453/02 , C07D453/06 , C07D487/08
摘要： Arthropodicidal compounds having formula (I) and compositions comprising compounds of formula (II) and use of said compounds to control arthropods, wherein Q is selected from the group Q-1, Q-2, Q-3 and Q-4; and Q is selected from the group Q-5, Q-6 and Q-7.
摘要翻译：具有式（I）的组合节肢动物化合物和包含式（II）化合物的组合物和所述化合物用于控制节肢动物的组合物，其中Q选自Q-1，Q-2，Q-3和Q-4组; Q 1选自Q-5，Q-6和Q-7。

20. 发明申请

WO1993005024A1 ARTHROPODICIDAL ANILIDES 审中-公开
标题翻译：抗抑郁药
公开(公告)号：WO1993005024A1
公开(公告)日：1993-03-18
申请号：PCT/US1992007145
申请日：1992-08-28
申请人： E.I. DU PONT DE NEMOURS AND COMPANY , BARNETTE, William, Eldo , HARRISON, Charles, Richard , LAHM, George, Philip , PIOTROWSKI, David, Walter , WING, Keith, Dumont
发明人： E.I. DU PONT DE NEMOURS AND COMPANY
IPC分类号： C07D231/06
CPC分类号： C07D231/06 , A01N47/38
摘要： Arthropodicidal anilides of formula (I) wherein R to R are as defined in the text; arthropodicidal compositions containing such compounds and a method of using the compounds to control arthropods.
摘要翻译：其中R 1至R 5的式（I）的节肢动物杀虫辅剂如文中所定义; 含有这些化合物的节肢动物杀伤组合物以及使用该化合物控制节肢动物的方法。

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