公开(公告)号：US20060063787A1

公开(公告)日：2006-03-23

申请号：US11212407

申请日：2005-08-26

申请人： Seiji Yoshikawa ,  Eita Emori ,  Fumiyoshi Matsuura ,  Richard Clark ,  Hironori Ikuta ,  Kazunobu Kira ,  Nobuyuki Yasuda ,  Tadashi Nagakura ,  Kazuto Yamazaki

发明人： Seiji Yoshikawa ,  Eita Emori ,  Fumiyoshi Matsuura ,  Richard Clark ,  Hironori Ikuta ,  Kazunobu Kira ,  Nobuyuki Yasuda ,  Tadashi Nagakura ,  Kazuto Yamazaki

IPC分类号： A61K31/522 ,  C07D473/02 ,  A61K31/4745 ,  C07D471/02

CPC分类号： C07D473/30 ,  C07D471/04 ,  C07D473/04 ,  C07D473/06 ,  C07D473/18 ,  C07D473/36 ,  C07D473/40 ,  C07D487/04 ,  C07D491/14

摘要： The present invention is related to compounds represented by the following formula, or salts or hydrates thereof wherein, T1 represents a 4- to 12-membered heterocyclic group containing one or two nitrogen atoms in the ring, which is a monocyclic or bicyclic structure that may have one or more substituents; X represents a C1-6 alkyl group which may have one or more substituents, or such; Z1 and Z2 each independently represent a nitrogen atom or a group represented by the formula —CR2—; R1 and R2 independently represent a hydrogen atom, a C1-6 alkyl group which may have one or more substituents, or a C1-6 alkoxy group which may have one or more substituents, or such. These are novel compounds that exhibit an excellent DPPIV-inhibiting activity.

摘要翻译： 本发明涉及由下式表示的化合物或其盐或水合物

公开(公告)号：US20060052602A1

公开(公告)日：2006-03-09

申请号：US11190751

申请日：2005-07-26

申请人： Choung Kim ,  Johan Neyts ,  David Oare ,  Gerhard Puerstinger

发明人： Choung Kim ,  Johan Neyts ,  David Oare ,  Gerhard Puerstinger

IPC分类号： C07D473/02

CPC分类号： C07D471/04 ,  C07D473/00 ,  C07D473/30

摘要： The present invention relates to pharmaceutical compositions for the treatment or prevention of viral infections comprising as an active principle at least one imidazo[4,5-c]pyrimidine having the general formula (A): wherein the substituents are described in the specification. The invention also relates to processes for the preparation of compounds according to the invention having above mentioned general formula, their pharmaceutically acceptable formulations and their use as a medicine or to treat or prevent viral infections.

摘要翻译： 本发明涉及用于治疗或预防病毒感染的药物组合物，其包含作为活性成分的至少一种具有通式（A）的咪唑并[4,5-c]嘧啶：

公开(公告)号：US20050250785A1

公开(公告)日：2005-11-10

申请号：US11182977

申请日：2005-07-15

申请人： Sung Kim ,  Hyunil Lee ,  Jong Lim ,  Hoon Choi ,  Jae Jeon ,  Sang Ahn ,  Sung Lee ,  Won Yoon

发明人： Sung Kim ,  Hyunil Lee ,  Jong Lim ,  Hoon Choi ,  Jae Jeon ,  Sang Ahn ,  Sung Lee ,  Won Yoon

IPC分类号： C12N15/09 ,  A61K31/513 ,  A61K31/52 ,  C07D277/80 ,  C07D405/12 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D473/02 ,  C07D473/18 ,  C07D473/32 ,  C07D473/34 ,  A61K31/506

CPC分类号： C07D417/04 ,  C07B2200/11 ,  C07D277/80 ,  C07D417/12 ,  C07D417/14 ,  Y02P20/55

摘要： This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is nitrogen or C—R′; J is sulfur or oxygen; R′, R1, R2, R3, R4 is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy, phenyl or halogenated phenyl, R5 is H or protected or unprotected side chain of natural or unnatural α-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases in the presence of thiol.

公开(公告)号：US20050245523A1

公开(公告)日：2005-11-03

申请号：US11152599

申请日：2005-06-14

申请人： Peter Emig ,  Eckhard Gunther ,  Jurgen Schmidt ,  Bernd Nickel ,  Bernhard Kutscher

发明人： Peter Emig ,  Eckhard Gunther ,  Jurgen Schmidt ,  Bernd Nickel ,  Bernhard Kutscher

IPC分类号： C07D401/06 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/513 ,  A61K31/53 ,  A61P35/00 ,  C07D215/50 ,  C07D219/04 ,  C07D473/02 ,  C07D43/14

CPC分类号： C07D401/06 ,  C07D215/50

摘要： The invention relates to novel quinoline derivatives of the formula 1, to their preparation and to their use as medicaments, in particular for treating tumors.

摘要翻译： 本发明涉及式1的新型喹啉衍生物，其制备方法及其用作药物，特别是用于治疗肿瘤。

公开(公告)号：US20050169982A1

公开(公告)日：2005-08-04

申请号：US10716976

申请日：2003-11-19

申请人： Om Almarssoo ,  Julius Remenar ,  Matthew Peterson

发明人： Om Almarssoo ,  Julius Remenar ,  Matthew Peterson

IPC分类号： C07D473/12 ,  A61K9/00 ,  A61K9/16 ,  A61K31/19 ,  A61K31/195 ,  A61K31/4015 ,  A61K31/4166 ,  A61K31/522 ,  A61K31/53 ,  A61K31/55 ,  A61K31/7028 ,  A61K47/10 ,  A61K47/32 ,  A61P1/08 ,  A61P1/14 ,  A61P3/04 ,  A61P9/12 ,  A61P11/02 ,  A61P15/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P25/34 ,  A61P27/02 ,  A61P43/00 ,  C07H5/04 ,  C07H5/06 ,  C07H11/00 ,  G01N33/15 ,  A61K9/48 ,  C07D473/02

CPC分类号： A61K9/1652 ,  A61K9/0014 ,  A61K9/0019 ,  A61K47/10 ,  A61K47/32 ,  C07H5/04 ,  C07H5/06

摘要： The invention encompasses novel salts of topiramate, and pharmaceutically acceptable polymorphs, solvates, hydrates, dehydrates, co-crystals, anhydrous, or amorphous forms thereof, as well as pharmaceutical compositions and pharmaceutical unit dosage forms containing the same. In particular, the invention encompasses pharmaceutically acceptable salts of topiramate, including without limitation topiramate sodium, topiramate lithium, topiramate potassium, or polymorphs, solvates, hydrates, dehydrates, co-crystals, anhydrous, and amorphous forms thereof. The invention further encompasses novel co-crystals or complexes of topiramate, as well as pharmaceutical compositions comprising them. The invention also encompasses methods of treating or preventing a variety of diseases and conditions including, but not limited to, seizures, epileptic conditions, tremors, cerebral function disorders, obesity, neuropathic pain, affective disorders, tobacco cessation, migraines, and cluster headache.

摘要翻译： 本发明包括托吡酯及其药学上可接受的多晶型物，溶剂合物，水合物，脱水剂，共晶体，无水或无定形形式的新型盐以及含有该盐的药物组合物和药物单位剂型。 特别地，本发明包括托吡酯的药学上可接受的盐，包括但不限于托吡酯钠，托吡酯锂，托吡酯钾或多晶型物，溶剂合物，水合物，脱水剂，共晶体，无水和无定形形式。 本发明还包括托吡酯的新型共晶体或络合物，以及包含它们的药物组合物。 本发明还包括治疗或预防各种疾病和病症的方法，包括但不限于癫痫发作，癫痫病症，震颤，脑功能障碍，肥胖症，神经性疼痛，情感障碍，戒烟，偏头痛和丛集性头痛。

公开(公告)号：US20050070534A1

公开(公告)日：2005-03-31

申请号：US10949055

申请日：2004-09-24

申请人： Nicholas Carruthers ,  Wenying Chai ,  Scott Dax ,  Jill Jablonowski ,  Xiaobing Li ,  Timothy Lovenberg ,  William Murray ,  Dale Rudolph ,  Mark Seierstad ,  Mark Youngman

发明人： Nicholas Carruthers ,  Wenying Chai ,  Scott Dax ,  Jill Jablonowski ,  Xiaobing Li ,  Timothy Lovenberg ,  William Murray ,  Dale Rudolph ,  Mark Seierstad ,  Mark Youngman

IPC分类号： A61K31/404 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/497 ,  A61K31/52 ,  A61K31/5377 ,  A61K31/541 ,  A61P3/04 ,  A61P15/08 ,  A61P25/22 ,  A61P25/24 ,  C07D401/12 ,  C07D401/14 ,  C07D409/14 ,  C07D413/02 ,  C07D417/02 ,  C07D473/02 ,  C07D43/02

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D409/14

摘要： The invention provides novel non-peptidic NPY Y2 receptor inhibitors useful in treating or preventing: anxiolytic disorders or depression; injured mammalian nerve tissue; conditions responsive to treatment through administration of a neurotrophic factor; neurological disorders; bone loss; substance related disorders; obesity; or an obesity-related disorder. Compounds of the invention are also useful in modulating endocrine functions, particularly endocrine functions controlled by the pituitary and hypothalamic glands, and are therefore useful in the treatment or prevention of inovulation and infertility.

摘要翻译： 本发明提供了用于治疗或预防：抗焦虑障碍或抑郁症的新型非肽性NPY Y2受体抑制剂; 受伤的哺乳动物神经组织; 通过施用神经营养因子治疗反应的病症; 神经系统疾病; 骨质疏松 物质相关疾病; 肥胖; 或肥胖相关疾病。 本发明的化合物还可用于调节内分泌功能，特别是由垂体和下丘脑腺体控制的内分泌功能，因此可用于治疗或预防排卵和不育症。

公开(公告)号：US20050032738A1

公开(公告)日：2005-02-10

申请号：US10943429

申请日：2004-09-17

申请人： Sai Sunkara

发明人： Sai Sunkara

IPC分类号： C07D239/54 ,  A61K31/475 ,  A61K31/505 ,  A61K31/513 ,  A61K31/7068 ,  A61P35/00 ,  A61P35/02 ,  C07D405/04 ,  C07D473/02 ,  C07H19/04 ,  C07H19/06 ,  A61K31/7076 ,  A61K31/519 ,  A61K31/522 ,  A61K31/7072

CPC分类号： A61K31/475 ,  A61K31/505 ,  A61K31/70 ,  C07H19/04 ,  C07H19/06 ,  A61K31/415 ,  A61K2300/00

摘要： The present invention relates to a method of treating a patient suffering from a neoplastic disease state comprising administering to said patient an effective antineoplastic amount of a 2′-halomethylidene derivative in conjunctive therapy with an effective antineoplastic amount of a S phase or M-phase specific agent.

摘要翻译： 本发明涉及一种治疗患有肿瘤疾病状态的患者的方法，其包括向所述患者施用有效的抗肿瘤剂量的联合治疗中的2'-卤代亚甲基衍生物，其有效抗肿瘤剂量为S期或M期特异性 代理商

公开(公告)号：US20050009829A1

公开(公告)日：2005-01-13

申请号：US10849436

申请日：2004-05-19

申请人： Marc Nazare ,  Michael Wagner ,  Volkmar Wehner ,  Hans Matter ,  Matthias Urmann ,  Kurt Ritter

发明人： Marc Nazare ,  Michael Wagner ,  Volkmar Wehner ,  Hans Matter ,  Matthias Urmann ,  Kurt Ritter

IPC分类号： C07D235/24 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D473/08 ,  C07D495/04 ,  A61K31/52 ,  A61K31/4709 ,  A61K31/513 ,  A61K31/517 ,  C07D473/02 ,  C07

CPC分类号： C07D235/24 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D473/08 ,  C07D495/04

摘要： The present invention relates to compounds of the formula I, wherein R0, R1, R2, Q, V, G and M are as defined herein. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

摘要翻译： 本发明涉及式I化合物，其中R 0，R 1，R 2，Q，V，G和M如本文所定义。 式I的化合物是有价值的药理活性化合物。 它们具有强烈的抗血栓形成作用，并且适用于例如治疗和预防心血管疾病如血栓栓塞性疾病或再狭窄。 它们是血液凝固酶因子Xa（FXa）和/或因子VIIa（FVIIa）的可逆抑制剂，并且通常可用于存在因子Xa和/或因子VIIa的不期望活性或用于治愈 或预防因子Xa和/或因子VIIa的抑制。 本发明还涉及式I化合物的制备方法，其用途，特别是作为药物中的活性成分，以及包含它们的药物制剂。

公开(公告)号：US20050009823A1

公开(公告)日：2005-01-13

申请号：US10762742

申请日：2004-01-22

申请人： Yuhpyng Chen

发明人： Yuhpyng Chen

IPC分类号： C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04 ,  A61K31/519 ,  A61K31/52 ,  A61K31/53 ,  C07D473/02

CPC分类号： C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04 ,  C07D513/04

摘要： This invention relates to compounds of the formula wherein A, B, D, E, K, T, G, R3 and R5 are defined as in the specification, and to the pharmaceutically acceptable salts of such compounds.

摘要翻译： 本发明涉及下式的化合物，其中A，B，D，E，K，T，G，R 3和R 5如说明书中所定义，以及这些化合物的药学上可接受的盐。

公开(公告)号：US20040241683A1

公开(公告)日：2004-12-02

申请号：US10483038

申请日：2004-06-14

发明人： Stephen C Ekker ,  Aidas Nasevicius ,  Eleanor Y Chen

IPC分类号： C12Q001/68 ,  A01K067/027 ,  C07D473/02 ,  C07D413/14 ,  C07K016/18

CPC分类号： C07K14/461 ,  C07K14/47

摘要： The invention provides methods and materials related to modulating angiogenesis in an animal. The invention provides polynucleotides and modified polynucleotides such as morpholino-modified polynucleotides for modulating angiogenesis, as well as cells and embryos containing these polynucleotides. The invention also provides methods for identifying HSST- and angiogenesis-modulating agents.

摘要翻译： 本发明提供了与动物调节血管生成相关的方法和材料。 本发明提供了多核苷酸和修饰的多核苷酸，例如用于调节血管发生的吗啉代修饰的多核苷酸，以及含有这些多核苷酸的细胞和胚胎。 本发明还提供鉴定HSST-和血管生成调节剂的方法。