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71. 发明申请

US20060135561A1 4-Aminopiperidine derivatives 失效
标题翻译： 4-氨基哌啶衍生物
公开(公告)号：US20060135561A1
公开(公告)日：2006-06-22
申请号：US11300206
申请日：2005-12-14
申请人： Markus Boehringer , Daniel Hunziker , Bernd Kuhn , Bernd Loeffler , Thomas Luebbers , Fabienne Ricklin
发明人： Markus Boehringer , Daniel Hunziker , Bernd Kuhn , Bernd Loeffler , Thomas Luebbers , Fabienne Ricklin
IPC分类号： A61K31/4545 , A61K31/454 , C07D211/68 , A61K31/445 , C07D401/02
CPC分类号： C07D211/58 , C07D211/60 , C07D277/04
摘要： The present invention relates to compounds of the formula (I) wherein R1 and R2 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP-IV, such as diabetes, non-insulin dependent diabetes mellitus and/or impaired glucose tolerance, obesity, and/or metabolic syndrome or β-cell protection.
摘要翻译：本发明涉及式（I）的化合物，其中R 1和R 2如在说明书和权利要求书中所定义，及其药学上可接受的盐。该化合物可用于治疗和/或预防与DPP-IV相关的疾病，例如糖尿病，非胰岛素依赖性糖尿病和/或葡萄糖耐量异常，肥胖症和/或代谢综合征或β细胞保护。

72. 发明授权

US06984649B1 Pyridine derivatives 失效
标题翻译：吡啶衍生物
公开(公告)号：US06984649B1
公开(公告)日：2006-01-10
申请号：US10402500
申请日：2003-03-28
申请人： Toshiki Murata , Masaomi Umeda , Sachiko Sakakibara , Takashi Yoshino , Hiroki Sato , Tsutomu Masuda , Yuji Koriyama , Mitsuyuki Shimada , Takuya Shintani , Hiroshi Kadono , Timothy B. Lowinger , Karl B. Ziegelbauer , Kinji Fuchikami , Hiroshi Komura
发明人： Toshiki Murata , Masaomi Umeda , Sachiko Sakakibara , Takashi Yoshino , Hiroki Sato , Tsutomu Masuda , Yuji Koriyama , Mitsuyuki Shimada , Takuya Shintani , Hiroshi Kadono , Timothy B. Lowinger , Karl B. Ziegelbauer , Kinji Fuchikami , Hiroshi Komura
IPC分类号： A61K31/4545 , C07D409/14 , C07D211/68 , C07D213/73
CPC分类号： C07D213/08 , C07D213/10 , C07D213/73 , C07D213/80 , C07D213/85 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/14 , C07D471/04 , C07D471/08 , C07D513/04 , C07D515/04
摘要： Pyridine compounds of general formula: wherein —R1 represents in which R11 is hydrogen, C1-6 alkyl, halogen, hydroxy, C1-12 alkoxy, nitro, amino, C1-6 alkylsulfonylamino, C1-6 alkoxycarbonyl, C1-6 alkylamino, di (C1-6 alkyl)amino, C1-6 alkanoylamino, phenyl C1-6 alkylamino, phenylsulfonylamino, or —O—(CH2)n—R111; R2 represents hydrogen or halogen; R3 represents 1.2.3.6-tetrahydro-pyridine, or —CR31R32R33 wherein R31 represents H or C1-6 alkyl and R32 and R33 are joined to form a 5-8 membered saturated ring optionally containing up to three heteroatoms; R4 is carbamoyl, CN, carboxyl, etc.; R5 is amino, C1-6 alkylamino, di C1-6 alkylamino, etc. or salt thereof. The compound has an excellent anti-inflammatory activity, and other biological activity.
摘要翻译：吡啶化合物，其通式如下：其中R 1表示其中R 11为氢，C 1-6烷基，卤素，羟基，C 1-12烷氧基，硝基，氨基，C 1-6烷基磺酰基氨基，C 1-6烷氧基羰基，C 1-6烷基，（C 1-6烷基）氨基，C 1-6烷酰基氨基，苯基C 1-6烷基氨基，苯基磺酰基氨基，C 1 -C 6烷基氨基，，或-O-（CH 2）n - n - R 111; R 2表示氢或卤素; R 3表示1.2.3.6-四氢 - 吡啶或-CR 31，其中R 1，R 2，R 3， SUP> 31表示H或C 1-6烷基，R 32和R 33连接形成5-8 任选地含有至多三个杂原子的饱和环; R 4是氨基甲酰基，CN，羧基等; R 5是氨基，C 1-6烷基氨基，C 1-6烷基氨基等，或其盐。该化合物具有优异的抗炎活性和其他生物活性。

73. 发明申请

US20040138259A1 4-(phenyl-piperdin-4-ylidene-methyl)-benzamide derivatives and their use for the treatment of pain, anxiety or gastrointestinal disorders 审中-公开
标题翻译： 4-（苯基 - 哌啶-4-亚基 - 甲基） - 苯甲酰胺衍生物及其用于治疗疼痛，焦虑或胃肠道疾病的用途
公开(公告)号：US20040138259A1
公开(公告)日：2004-07-15
申请号：US10477854
申请日：2003-11-13
发明人： William Brown , Christopher Walpole , Zhongyong Wei
IPC分类号： C07D211/68 , A61K031/445
CPC分类号： C07D401/06 , C07D211/70 , C07D405/06 , C07D409/06 , C07D417/06
摘要： Compounds of general formula I R1 is selected from any one of phenyl, pyridinyl, pyrrolyl, thienyl, furanyl, imidazolyl, triazolyl, thiazolyl, and pyridine N-oxide; where each R1 phenyl ring and R1 heteroaromatic ring may optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C1-C6 alkyl, NO2, CF3, C1-C6 alkoxy, chloro, fluoro, bromo, and iodo. The substitutions on the phenyl ring and on the heteroaromatic ring may take place in any position on said ring systems; are disclosed and claimed in the present application, as well as salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain, anxiety, and functional gastrointestinal disorders. 1
摘要翻译：通式I R1的化合物选自苯基，吡啶基，吡咯基，噻吩基，呋喃基，咪唑基，三唑基，噻唑基和吡啶N-氧化物中的任一种; 其中每个R 1苯基环和R 1杂芳环可以任选和独立地被1,2或3个选自直链和支链C 1 -C 6烷基，NO 2，CF 3，C 1 -C 6烷氧基，氯，氟，溴和碘的取代基取代。。苯环上和杂芳环上的取代可以在所述环体系上的任何位置进行; 在本申请中公开和要求保护，以及包含新化合物的盐和药物组合物及其在治疗中的用途，特别是在治疗疼痛，焦虑和功能性胃肠道疾病中的用途。

74. 发明申请

US20030120081A1 Process for the preparation of non-steroidal glucocorticoid receptor modulators 失效
公开(公告)号：US20030120081A1
公开(公告)日：2003-06-26
申请号：US10271309
申请日：2002-10-15
发明人： Jerry A. Murry , Timothy D. White
IPC分类号： C07D211/68
CPC分类号： C07D213/40 , C07B2200/07 , C07C41/01 , C07C41/26 , C07C43/192 , C07C43/196 , C07C49/747 , C07C51/08 , C07C65/17 , C07C255/53 , C07C255/54 , C07C255/56 , C07C269/00 , C07C2603/26 , C07C271/52
摘要： A process for preparing a compound of the formula 1 useful as a non-steroidal glucocorticoid receptor modulator.

75. 发明申请

US20020151714A1 PROCESS FOR PREPARING 1,4-DISUBSTITUTED PIPERIDINE COMPOUNDS 审中-公开
标题翻译：制备1,4-取代的哌啶化合物的方法
公开(公告)号：US20020151714A1
公开(公告)日：2002-10-17
申请号：US09380835
申请日：2000-01-31
发明人： MAX REY , STEFAN GLADOW
IPC分类号： C07D211/68 , C07D211/80 , C07D213/02
CPC分类号： C07D401/04
摘要： The invention concerns a process for preparing 1,4-disubstituted piperidine compounds of formula (I), in which Y null-(CH2) n , n being 0. 1. 2 or 3; oxygen; sulphur; vinyl, -CH 2 -0-; -0-CH 2; -CH 2 -S- or -S-CH 2 , and R and Z mean substituents known per se. Compounds in which Z means -CH 2 -CH 2 - are produced in that the correspondingly substituted 5,6-dihydro- 11 H -benzonull5,6null-cyclohepta-null1,2-bnull pyridin-11-one compound is reacted with the corresponding 1-substituted 4-piperidone in a single process step by means of reductive dimerization in the presence of a finely dispersed metal of the IVth and/or Vth and/or VIth subgroup of the periodic table of elements or a low-valent oxidation stage of a corresponding metal compound of this type, the finely dispersed metal or the low-valent oxidation stage being produced in situ by means of a reducing agent and in the presence of an inert solvent. Preferably 4-(5.6-dihydro- 11 H -benzo-null5,6null cycloheptanull1 ,2-bnull pyridin-11-ylidene)-1-piperidine compounds are produced.
摘要翻译：本发明涉及制备式（I）的1,4-二取代哌啶化合物的方法，其中Y = - （CH 2）n，n为0,1.2或3; 氧; 硫; 乙烯基，-CH 2 -O-; -O-CH 2; -CH 2 -S-或-S-CH 2，R和Z表示本身已知的取代基。其中Z表示-CH 2 -CH 2 - 的化合物是由相应取代的5,6-二氢-11H-苯并[5,6] - 环庚烯并[1,2-b]吡啶-11-酮化合物在单一工艺步骤中通过还原二聚化在元素周期表的IV和/或Vth和/或VI族亚组的精细分散的金属的存在下与相应的1-取代的4-哌啶酮反应或低这种类型的相应的金属化合物的高价氧化阶段，微细分散的金属或低价氧化阶段是通过还原剂在原位制备的，并且在惰性溶剂的存在下制备。优选制备4-（5.6-二氢-11H-苯并[5,6]环庚并[1,2-b]吡啶-11-亚基）-1-哌啶化合物。

76. 发明申请

US20010044440A1 Modulators of p38 MAP kinase 失效
标题翻译： p38 MAP激酶的调节剂
公开(公告)号：US20010044440A1
公开(公告)日：2001-11-22
申请号：US09792876
申请日：2001-02-23
发明人： David J. Morgans JR. , Silke Thode , Dongxu Sun
IPC分类号： C07D211/68 , A61K031/513 , A61K031/506 , A61K031/4545 , A61K031/44
CPC分类号： C07D213/78 , C07D239/28
摘要： Compounds of formula I are effective modulators of p38 MAP kinase. 1 wherein R1 is H, lower alkyl, or OR5, where R5 is aryl, heterocyclyl, acyl, NnullR6-4-piperidinyl, NnullR6-4-piperidinylmethyl, or NnullR6-4-pipelidinylethyl, where aryl and heterocyclyl are substituted with 1-3 R6 substituents selected from the group consisting of H, lower alkyl, lower alkenyl, OH, NO2, NH2, halo, trihalomethyl, nullCN, SH, SO, SO2, SO3H, nullOR, nullCOR, nullCOOR, nullCONHR, nullOCOR, and nullNCOR, where R is lower alkyl; R2 is H or lower alkyl; R3 is aryl substituted with 1-3 R6 substituents; R4 is H, lower alkyl, aryl, aralkyl, nullOH, nullNH2, nullNHR, or nullOR, where R is lower alkyl or aryl-lower alkyl; and A is nullCHnull or nullNnull; and pharmaceutically acceptable salts thereof.
摘要翻译：式I化合物是p38 MAP激酶的有效调节剂。其中R 1是H，低级烷基或OR 5，其中R 5是芳基，杂环基，酰基，N-R6-4-哌啶基，N-R6-4-哌啶基甲基或N-R6-4-哌啶基乙基，其中芳基和杂环基是被选自H，低级烷基，低级烯基，OH，NO 2，NH 2，卤素，三卤甲基，-CN，SH，SO，SO 2，SO 3 H，-OR，-COR，-COOR的1-3个R 6取代基取代，-CONHR，-OCOR和-NCOR，其中R是低级烷基; R2是H或低级烷基; R3是被1-3个R6取代基取代的芳基; R4是H，低级烷基，芳基，芳烷基，-OH，-NH2，-NHR或-OR，其中R是低级烷基或芳基 - 低级烷基; A是-CH-或-N-; 及其药学上可接受的盐

77. 发明授权

US6043366A 1,3,8,-triaza spiro (4,5)decan-4-on derivatives 失效
标题翻译： 1,3,5， - 三氮螺（4,5）癸-4-酮衍生物
公开(公告)号：US6043366A
公开(公告)日：2000-03-28
申请号：US204184
申请日：1998-12-03
申请人： Geo Adam , Andrea Cesura , Caido Galley , Fran.cedilla.ois Jenck , Stephan Rover , Jurgen Wichmann
发明人： Geo Adam , Andrea Cesura , Caido Galley , Fran.cedilla.ois Jenck , Stephan Rover , Jurgen Wichmann
IPC分类号： C07D235/02 , A61K31/00 , A61K31/41 , A61K31/435 , A61K31/438 , A61P3/00 , A61P3/04 , A61P9/00 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P43/00 , C07D207/04 , C07D233/30 , C07D471/10 , C07D215/20 , C07D211/56 , C07D211/68
CPC分类号： C07D471/10
摘要： The present invention relates to compounds of formula I and pharmaceutically acceptable acid addition salts thereof.
摘要翻译：本发明涉及式I化合物及其药学上可接受的酸加成盐。

78. 发明授权

US5994377A Piperidine compounds 失效
标题翻译：哌啶化合物
公开(公告)号：US5994377A
公开(公告)日：1999-11-30
申请号：US955564
申请日：1997-10-17
申请人： Choung U. Kim , Matthew A. Williams
发明人： Choung U. Kim , Matthew A. Williams
IPC分类号： A61K31/44 , C07D211/72 , C07D211/74 , C07D211/68 , A61K31/435
CPC分类号： C07D211/74 , A61K31/44 , C07D211/72
摘要： Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.
摘要翻译：描述了新的化合物。化合物通常包含酸性基团，碱性基团，取代的氨基或N-酰基和具有任选羟基化的烷烃部分的基团。还描述了包含本发明抑制剂的药物组合物。还描述了怀疑含有神经氨酸酶的样品中抑制神经氨酸酶的方法。还描述了抗原物质，聚合物，抗体，本发明化合物与标记物的缀合物，以及用于检测神经氨酸酶活性的测定方法。

79. 发明授权

US5756519A Fibrinogen receptor antagonists 失效
标题翻译：纤维蛋白原受体拮抗剂
公开(公告)号：US5756519A
公开(公告)日：1998-05-26
申请号：US619589
申请日：1997-06-20
申请人： William E. Bondinell , James M. Samanen
发明人： William E. Bondinell , James M. Samanen
IPC分类号： A61K31/445 , A61K31/4465 , A61P7/02 , C07D211/26 , C07D213/36 , C07D213/74 , C07D211/00 , C07D211/68 , C07D401/00
CPC分类号： C07D211/26
摘要： The following invention relates to compounds which are effective for inhbiting platelet aggregation, pharmaceutical compositions for effecting such activity and a method for inhibiting platelet aggregation.
摘要翻译： PCT No.PCT / US95 / 16262 Sec。 371日期：1997年6月20日 102（e）日期1997年6月20日PCT提交1995年12月7日PCT公布。 WO96 / 19222 PCT公开号日期1996年6月27日以下发明涉及对血小板聚集有效的化合物，用于实现这种活性的药物组合物和抑制血小板聚集的方法。

80. 发明授权

US5663349A Preparation of substituted piperidenes 失效
标题翻译：取代的哌啶的制备
公开(公告)号：US5663349A
公开(公告)日：1997-09-02
申请号：US273662
申请日：1994-07-12
申请人： Terry J. Rosen , Dennis M. Godek , Sally Gut , Lewin Wint
发明人： Terry J. Rosen , Dennis M. Godek , Sally Gut , Lewin Wint
IPC分类号： A61K31/4418 , A61K31/445 , A61K31/451 , A61P1/00 , A61P11/00 , A61P25/00 , A61P29/00 , A61P43/00 , C07D211/56 , C07D213/73 , C07D213/74 , C07D213/75 , C07D215/12 , C07D211/02 , C07D211/68 , C07D215/04
CPC分类号： C07D213/73 , C07D211/56 , C07D213/74
摘要： Novel processes are disclosed for the preparation and resolution of substituted piperidines of the formula ##STR1## wherein R.sup.1 and R.sup.2 are defined as below, and related compounds, as well as novel intermediates used in such processes.
摘要翻译：公开了用于制备和拆分式（I）的取代哌啶的方法，其中R 1和R 2如下定义，以及相关化合物以及在这些方法中使用的新型中间体。

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