公开(公告)号：US20090298833A1

公开(公告)日：2009-12-03

申请号：US12505724

申请日：2009-07-20

申请人： Percy H. Carter ,  Cullen L. Cavallaro ,  John V. Duncia ,  Daniel S. Gardner ,  John Hynes ,  Rui-Qin Liu ,  Joseph B. Santella ,  Dharmpal S. Dodd

发明人： Percy H. Carter ,  Cullen L. Cavallaro ,  John V. Duncia ,  Daniel S. Gardner ,  John Hynes ,  Rui-Qin Liu ,  Joseph B. Santella ,  Dharmpal S. Dodd

IPC分类号： A61K31/445 ,  C07D211/40 ,  C07D417/12 ,  C07D401/12 ,  C07D413/14 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61P9/00 ,  A61P35/00 ,  A61P19/00 ,  A61P31/18

CPC分类号： C07D211/52 ,  C07D211/18 ,  C07D211/38 ,  C07D211/58 ,  C07D211/70 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/10 ,  C07D491/107

摘要： The present application describes substituted piperidinyl modulators of MIP-1α or CCR-1 or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using said modulators are disclosed.

摘要翻译： 本申请描述了MIP-1α或CCR-1的取代的哌啶基调节剂或其立体异构体或其药学上可接受的盐。 此外，公开了使用所述调节剂治疗和预防炎症性疾病如哮喘和过敏性疾病以及自身免疫性病症如类风湿性关节炎和移植排斥的方法。

公开(公告)号：US20090239829A1

公开(公告)日：2009-09-24

申请号：US12309701

申请日：2007-07-25

申请人： Armando Rossello ,  Elisabetta Orlandini ,  Aldo Balsamo ,  Laura Panelli ,  Elisa Nuti

发明人： Armando Rossello ,  Elisabetta Orlandini ,  Aldo Balsamo ,  Laura Panelli ,  Elisa Nuti

IPC分类号： A61K31/662 ,  C07C233/64 ,  A61K31/165 ,  C07D333/06 ,  A61K31/381 ,  C07F9/38 ,  C07D207/00 ,  A61K31/40 ,  C07D239/02 ,  A61K31/515 ,  C07D211/40 ,  A61K31/445 ,  A61P35/00

CPC分类号： C07C317/44 ,  C07C317/14 ,  C07C317/22 ,  C07C323/62 ,  C07D207/46 ,  C07D209/48 ,  C07D211/76 ,  C07D239/60 ,  C07F9/3882

摘要： There are described compounds having the general formula (I) below and their pharmaceutically acceptable salts thereof, wherein E, X, m, q, R1, R2, n and ZBG have the meanings reported in the description useful, in therapy, as inhibitors of zinc metalloproteinases.

摘要翻译： 描述了具有下面通式（I）的化合物及其药学上可接受的盐，其中E，X，m，q，R 1，R 2，n和ZBG具有在本说明书中报道的含义，在治疗中作为抑制剂 锌金属蛋白酶。

公开(公告)号：US07531535B2

公开(公告)日：2009-05-12

申请号：US11955678

申请日：2007-12-13

申请人： Donald J. P. Pinto ,  Jennifer X. Qiao

发明人： Donald J. P. Pinto ,  Jennifer X. Qiao

IPC分类号： C07D413/00 ,  C07D401/00 ,  C07D241/04 ,  C07D215/38 ,  C07D405/00 ,  C07D211/40 ,  C07D211/54 ,  C07D409/00 ,  C07D213/78 ,  A61K31/535 ,  A61K31/495 ,  A61K31/47 ,  A61P7/02

CPC分类号： C07D471/04 ,  A61J1/00 ,  A61J1/03 ,  A61J1/05 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/444 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/513 ,  A61K31/55 ,  A61K45/06 ,  B65D81/3216 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D409/12 ,  C07D413/14 ,  C07D417/14

摘要： The present application describes lactam-containing compounds and derivatives thereof of Formula I: or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.

摘要翻译： 本申请描述了含有式I的化合物及其衍生物或其药学上可接受的盐形式，其中环P（如果存在）为5-7元碳环或杂环，且环M为5-7元碳环或杂环。 本发明的化合物可用作胰蛋白酶样丝氨酸蛋白酶的抑制剂，特别是因子Xa。

公开(公告)号：US20080260651A1

公开(公告)日：2008-10-23

申请号：US12103032

申请日：2008-04-15

申请人： Veronique Morisson-Iveson ,  Joanna Marie Passmore

发明人： Veronique Morisson-Iveson ,  Joanna Marie Passmore

IPC分类号： A61K49/04 ,  C07D207/12 ,  C07D211/40

CPC分类号： C07D211/46 ,  A61K49/0438 ,  C07D207/12

摘要： The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds. More specifically the iodine containing compounds are chemical compounds containing an aliphatic N-heterocyclic central moiety such as pyrrolidine or piperidine heterocycles allowing for the arrangement of three iodinated phenyl groups bound thereto.The invention also relates to the use of such diagnostic compositions as contrast agents in diagnostic imaging, in particular in X-ray imaging, and to contrast media containing such compounds.

摘要翻译： 本发明涉及一类化合物和含有这些化合物的诊断组合物，其中化合物是含碘化合物。 更具体地说，含碘化合物是含有脂族N-杂环中心部分如吡咯烷或哌啶杂环的化合物，其允许与其结合的三个碘化苯基的排列。 本发明还涉及这样的诊断组合物作为造影剂在诊断成像，特别是X射线成像中的用途，以及含有这些化合物的造影剂。

公开(公告)号：US20080255362A1

公开(公告)日：2008-10-16

申请号：US12157573

申请日：2008-06-11

申请人： Keiji Kubo ,  Yasuhiro Imaeda

发明人： Keiji Kubo ,  Yasuhiro Imaeda

IPC分类号： C07D211/40

CPC分类号： C07D211/76 ,  C07D401/04 ,  C07D403/04 ,  C07D413/04 ,  C07D417/04

摘要： The present invention provides a cyclic amide derivative useful as a drug for treating thrombosis, which is represented by the formula (I): wherein R1 represents an optionally substituted cyclic hydrocarbon group or an optionally substituted heterocyclic group, W represents a bond or an optionally substituted divalent chain hydrocarbon group, a represents 0, 1, or 2, X1 represents an optionally substituted lower alkylene or an optionally substituted lower alkenylene, Y1 represents —C(O)—, —S(O)— or —S(O)2—, A represents a piperazine ring which may be further substituted or a piperidine ring which may be further substituted, X2 represents a bond or an optionally substituted lower alkylene, Y2 represents —C(O)—, —S(O)—, —S(O)2— or —C(═NR7)—, X3 represents an optionally substituted C1-4 alkylene or an optionally substituted C2-4 alkenylene, Z3 represents —N(R4)—, —O— or a bond, Z1 represents —C(R2)(R2′)—, —N(R2)—, etc., and Z2 represents —C(R3)(R3′)—, —N(R3)—, etc., or a salt thereof.

公开(公告)号：US20080139625A1

公开(公告)日：2008-06-12

申请号：US11632675

申请日：2005-04-29

申请人： Libuse Jaroskova ,  Joannes Theodorus Maria Linders ,  Christophe Francis Robert Nestor Buyck ,  Louis Jozef Elizabeth Van Der Veken ,  Vladimir Dimichev Dimitrov ,  Theo Teofanov Nikiforov

发明人： Libuse Jaroskova ,  Joannes Theodorus Maria Linders ,  Christophe Francis Robert Nestor Buyck ,  Louis Jozef Elizabeth Van Der Veken ,  Vladimir Dimichev Dimitrov ,  Theo Teofanov Nikiforov

IPC分类号： A61K31/4015 ,  C07D207/12 ,  C07D405/10 ,  A61P3/00 ,  A61K31/4412 ,  C07D211/40

CPC分类号： C07D211/76 ,  C07D207/26 ,  C07D207/267 ,  C07D405/06

摘要： Formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 1 or 2; L represents a C1-3alkyl linker optionally substituted with one or two substituents selected from C1-4alkyl, C1-3alkyloxy-C1-4alkyl-, hydroxy-C1-4alkyl, hydroxy, C1-3alkyloxy- or phenyl-C1-4alkyl; M represents a direct bond or a C1-3alkyl linker optionally substituted with one or two substituents selected from hydroxy, C1-4alkyl or C1-4alkyloxy; R1 and R2 each independently represent hydrogen, halo, cyano, hydroxy, C1-4alkyl optionally substituted with halo, C1-4alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy, Ar1 and halo; or R1 and R2 taken together with the phenyl ring to which they are attached form naphtyl or 1,3-benzodioxolyl, wherein said naphtyl or 1,3-benzodioxolyl are optionally substituted with halo; R3 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R4 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R5 represents hydrogen, C1-4alkyl or Ar2-C1-4alky-; R6 represents hydrogen, halo, C1-4alkyl Or C1-4alkyoxy-; Ar1 and Ar2 each independently represent phenyl or naphtyl wherein said phenyl and naphtyl are optionally substituted with C1-4alkyl, C1-4alkyloxy-, or phenyl-C1-4alkyl; for use as a medicine.

公开(公告)号：US20070173647A1

公开(公告)日：2007-07-26

申请号：US11606527

申请日：2006-11-29

申请人： Thomas Landmesser ,  Hans Bonnier

发明人： Thomas Landmesser ,  Hans Bonnier

IPC分类号： C07D403/02 ,  C07D211/40

CPC分类号： C07D211/88

摘要： The present invention relates to a method for the preparation of a carboxylic imide having the general formula R1—(CO)—(NR3)—(CO)—R2 ,   (I) wherein a carboxylic anhydride having the general formula R1—(CO)—O—(CO)—R2   (II) is reacted with urea or a urea derivative of the form (R3HN)—(CO)—(NR3H) in a solvent. In particular, the method can be used for the preparation of thalidomide.

摘要翻译： 本发明涉及一种制备具有通式为 - （CO） - （NR.sup.3） - （CO） - R 2的羧酰亚胺的方法， （I）其中具有通式为R 1 - （CO）-O - （CO）-R 2（II）的羧酸酐与脲或形式的脲衍生物反应 （R.sup.3HN） - （CO） - （NR.s.3.3H）在溶剂中。 特别地，该方法可用于制备沙利度胺。

公开(公告)号：US20070167458A1

公开(公告)日：2007-07-19

申请号：US10574122

申请日：2004-09-22

申请人： Axel Bouchon ,  Nicole Diedrichs ,  Achim Hermann ,  Klemens Lustig ,  Heinrich Meier ,  Josef Pernerstorfer ,  Elke Reissmuller ,  Jean De Vry ,  Muneto Mogi ,  Klaus Urbahns ,  Takeshi Yura ,  Hiroshi Fujishima ,  Masaomi Tajimi ,  Noriyuki Yamamoto ,  Hiroaki Yuasa ,  Jang Gupta ,  Yasuhiro Tsukimi ,  Fumihiko Hayashi

发明人： Axel Bouchon ,  Nicole Diedrichs ,  Achim Hermann ,  Klemens Lustig ,  Heinrich Meier ,  Josef Pernerstorfer ,  Elke Reissmuller ,  Jean De Vry ,  Muneto Mogi ,  Klaus Urbahns ,  Takeshi Yura ,  Hiroshi Fujishima ,  Masaomi Tajimi ,  Noriyuki Yamamoto ,  Hiroaki Yuasa ,  Jang Gupta ,  Yasuhiro Tsukimi ,  Fumihiko Hayashi

IPC分类号： A61K31/495 ,  C07D211/40 ,  C07D241/04

CPC分类号： C07D295/215 ,  C07D211/62 ,  C07D401/04

摘要： This invention relates to a hydroxy-tetrahydro-naphthalene or an urea derivative formula (I) and salts thereof which are useful as active ingredients of pharmaceutical preparations, wherein A represents formula (II) or (III) wherein # represents the connection position to the molecule and Q1a, Q2a, Q3a and Q4a are defined, and E represents formula (IV) or (V) wherein # represents the connection position to the molecule and Q1b, Q2b, Q3b, Q4b, Q5b, R1b, na, ma, Xa and Ra are defined.

摘要翻译： 本发明涉及用作药物制剂活性成分的羟基 - 四氢 - 萘或脲衍生物式（I）及其盐，其中A表示式（II）或（III），其中＃表示与 分子和Q 1a，Q 2a，Q 3a和Q 4a定义，E表示式（IV ）或（V）其中＃表示与分子的连接位置和Q 1b，Q 2b，Q 3b，Q 4b α，α，α，α，α，α，α，α，α和R a a都被定义 。

公开(公告)号：US07223779B2

公开(公告)日：2007-05-29

申请号：US10504777

申请日：2003-06-26

申请人： Takahiro Tsukida ,  Hideki Moriyama ,  Koichi Yokota ,  Mariko Hatakeyama ,  Shinichiro Nishimura

发明人： Takahiro Tsukida ,  Hideki Moriyama ,  Koichi Yokota ,  Mariko Hatakeyama ,  Shinichiro Nishimura

IPC分类号： A61K31/44 ,  C07D211/40

CPC分类号： C07D491/04 ,  A61K31/445 ,  C07D211/96

摘要： A novel azasugar derivative, and a drug containing the same as an active ingredient are disclosed. The drug is useful for treatment of keratinocyte-proliferative diseases.

摘要翻译： 公开了一种新型的azasagar衍生物和含有其作为活性成分的药物。 该药物可用于治疗角化细胞增生性疾病。

公开(公告)号：US20060205779A1

公开(公告)日：2006-09-14

申请号：US11372294

申请日：2006-03-09

申请人： YongQi Mu ,  Yu-Hua Ji ,  Mathai Mammen ,  Eric Stangeland

发明人： YongQi Mu ,  Yu-Hua Ji ,  Mathai Mammen ,  Eric Stangeland

IPC分类号： A61K31/445 ,  C07D211/54 ,  C07D211/40

CPC分类号： C07D211/46 ,  C07D405/12

摘要： The invention provides compounds of formula I: wherein a, b, c, p, W, A, X1, R1, R2, R3, R6, R7, and R8 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.

摘要翻译： 本发明提供式I化合物：其中a，b，c，p，W，A，X 1，R 1，R 2， R 3，R 6，R 7和R 8如本说明书中所定义。 式I化合物是毒蕈碱受体拮抗剂。 本发明还提供含有这些化合物的药物组合物，用于制备这些化合物的方法和中间体以及使用这些化合物治疗肺部疾病的方法。