公开(公告)号：US20050227983A1

公开(公告)日：2005-10-13

申请号：US10808210

申请日：2004-03-24

Applicant: Richard Timmer ,  Christopher Alexander ,  Sivaram Pillarisetti ,  Uday Saxena ,  Sesha Alluri ,  Velagala Venkata Krishna Reddy ,  Manojit Pal ,  Jangalgar Reddy ,  Koteswar Yeleswarapu ,  Gaddam Reddy ,  Potlapally Kumar

Inventor： Richard Timmer ,  Christopher Alexander ,  Sivaram Pillarisetti ,  Uday Saxena ,  Sesha Alluri ,  Velagala Venkata Krishna Reddy ,  Manojit Pal ,  Jangalgar Reddy ,  Koteswar Yeleswarapu ,  Gaddam Reddy ,  Potlapally Kumar

IPC: A61K31/53 ,  A61P19/02 ,  A61P29/00 ,  A61P35/00 ,  C07D251/46 ,  C07D251/52 ,  C12M1/34 ,  C07D43/02

CPC classification number: C07D251/46

Abstract: The present invention relates to triazine compounds and their analogs and derivatives, and methods and compositions comprising these compounds. The compounds and compositions of this invention are useful for, among other things, treating pathophysiological conditions arising from inflammatory responses, inhibiting or blocking glycated protein produced induction of the signaling-associated inflammatory response in endothelial cells, inhibiting smooth muscle proliferation, treating vascular occlusive conditions characterized by smooth muscle proliferation such as restenosis and atherosclerosis, and the like.

Abstract translation: 本发明涉及三嗪化合物及其类似物和衍生物，以及包含这些化合物的方法和组合物。 本发明的化合物和组合物尤其可用于治疗由炎症反应引起的病理生理学病症，抑制或阻断糖基化蛋白产生内皮细胞中信号传导相关炎症反应的诱导，抑制平滑肌增生，治疗血管闭塞症状 其特征在于平滑肌增生如再狭窄和动脉粥样硬化等。

公开(公告)号：US20050227979A1

公开(公告)日：2005-10-13

申请号：US11138631

申请日：2005-05-26

Applicant: Richard Apodaca ,  Nicholas Carruthers ,  Curt Dvorak ,  Chandravadan Shah ,  Wei Xiao

Inventor： Richard Apodaca ,  Nicholas Carruthers ,  Curt Dvorak ,  Chandravadan Shah ,  Wei Xiao

IPC: C07D295/08 ,  A61K31/4402 ,  A61K31/445 ,  A61K31/4465 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/551 ,  A61K45/06 ,  A61K51/00 ,  A61P9/00 ,  A61P11/06 ,  A61P25/00 ,  A61P25/06 ,  A61P25/08 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  A61P27/16 ,  A61P37/08 ,  A61P43/00 ,  C07C217/22 ,  C07C323/25 ,  C07C335/32 ,  C07D207/32 ,  C07D207/325 ,  C07D207/335 ,  C07D211/22 ,  C07D211/46 ,  C07D211/58 ,  C07D213/36 ,  C07D213/74 ,  C07D215/06 ,  C07D233/42 ,  C07D233/54 ,  C07D233/84 ,  C07D233/88 ,  C07D235/06 ,  C07D235/26 ,  C07D239/34 ,  C07D257/04 ,  C07D277/36 ,  C07D295/092 ,  C07D295/096 ,  C07D295/112 ,  C07D295/135 ,  C07D295/20 ,  C07D295/205 ,  C07D307/52 ,  C07D317/28 ,  C07D333/20 ,  C07D401/12 ,  C07D401/14 ,  C07D471/08 ,  C07D521/00 ,  C07D413/02 ,  C07D43/02

CPC classification number: C07D207/325 ,  A61K31/4402 ,  A61K31/4465 ,  A61K45/06 ,  C07C217/22 ,  C07C323/25 ,  C07C335/32 ,  C07D207/335 ,  C07D211/22 ,  C07D211/46 ,  C07D211/58 ,  C07D213/36 ,  C07D213/74 ,  C07D215/06 ,  C07D231/12 ,  C07D233/42 ,  C07D233/54 ,  C07D233/56 ,  C07D233/84 ,  C07D233/88 ,  C07D235/06 ,  C07D235/26 ,  C07D239/34 ,  C07D249/08 ,  C07D257/04 ,  C07D277/36 ,  C07D295/088 ,  C07D295/096 ,  C07D295/112 ,  C07D295/135 ,  C07D295/205 ,  C07D307/52 ,  C07D317/28 ,  C07D333/20 ,  C07D401/12 ,  C07D401/14 ,  C07D471/08 ,  A61K2300/00

Abstract: Substituted non-imidazole aryloxypiperidine compounds, compositions containing them, and methods of making and using them to treat or prevent histamine-mediated conditions.

Abstract translation: 取代的非咪唑芳氧基哌啶化合物，含有它们的组合物，以及制备和使用它们来治疗或预防组胺介导的病症的方法。

公开(公告)号：US20050227970A1

公开(公告)日：2005-10-13

申请号：US10514430

申请日：2003-05-06

Applicant: Koichi Araki ,  Tetsuya Murata ,  Koshi Gunjima ,  Norihiko Nakakura ,  Eiichi Shimojo ,  Dale Mitchell ,  Henricus Maria Bastiaans

Inventor： Koichi Araki ,  Tetsuya Murata ,  Koshi Gunjima ,  Norihiko Nakakura ,  Eiichi Shimojo ,  Dale Mitchell ,  Henricus Maria Bastiaans

IPC: A01N43/40 ,  A01N43/74 ,  A01N43/78 ,  A01N43/82 ,  A01N43/824 ,  A01N43/86 ,  A61K31/455 ,  A61K31/541 ,  A61P33/10 ,  A61P33/14 ,  C07D213/82 ,  C07D411/12 ,  C07D413/12 ,  C07D417/12 ,  C07D419/12 ,  C07D417/02 ,  A01N43/54 ,  C07D413/02 ,  C07D43/02

CPC classification number: C07D213/82 ,  A01N43/40 ,  C07D411/12 ,  C07D413/12 ,  C07D417/12 ,  C07D419/12

Abstract: The invention relates to 3-pyridylcarboxamide derivatives of formula (I): wherein the various symbols are as defined in the description, compositions thereof, methods for controlling pests by applying same, and processes for their preparation.

Abstract translation: 本发明涉及式（I）的3-吡啶基甲酰胺衍生物：其中各种符号如说明书中所定义，其组合，通过应用它们控制害虫的方法及其制备方法。

公开(公告)号：US20050227965A1

公开(公告)日：2005-10-13

申请号：US11100983

申请日：2005-04-06

Applicant: Christopher Demerson ,  Silvio Iera ,  Kadum Ali

Inventor： Christopher Demerson ,  Silvio Iera ,  Kadum Ali

IPC: A61K31/55 ,  C07D209/12 ,  C07D403/12 ,  C07D43/02

CPC classification number: C07D209/12 ,  C07D403/12

Abstract: The present invention is directed to a crystalline polymorph of bazedoxifene acetate, compositions containing the same, preparations thereof, and uses thereof.

Abstract translation: 本发明涉及乙酸巴多昔芬的结晶多晶型物，含有它们的组合物，其制备方法及其应用。

公开(公告)号：US20050222210A1

公开(公告)日：2005-10-06

申请号：US10517633

申请日：2003-06-13

Applicant: Keiji Kamiyama ,  Hiroshi Banno ,  Fumihiko Sato

Inventor： Keiji Kamiyama ,  Hiroshi Banno ,  Fumihiko Sato

IPC: A61P1/04 ,  A61P43/00 ,  C07D233/54 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D471/04 ,  A61K31/4439 ,  C07D43/02

CPC classification number: C07D471/04 ,  C07D233/90 ,  C07D401/12 ,  C07D405/04 ,  C07D405/14

Abstract: An imidazole compound represented by the formula (I), a salt thereof and a compound of the formula (V), which is one of the intermediates thereof. wherein each symbol is as defined in the present specification. The compound of the present invention shows a superior anti-ulcer activity, a gastric acid secretion inhibitory action, a mucosa-protecting action, an anti-Helicobacter pylori action and the like. Since it shows low toxicity, the compound is useful as a pharmaceutical product.

Abstract translation: 由式（I）表示的咪唑化合物，其盐和作为其中间体的式（V）化合物。 其中每个符号如本说明书中所定义。 本发明的化合物显示出优异的抗溃疡活性，胃酸分泌抑制作用，粘膜保护作用，抗幽门螺旋杆菌作用等。 由于它显示低毒性，所以该化合物可用作药物产品。

公开(公告)号：US20050222148A1

公开(公告)日：2005-10-06

申请号：US11091885

申请日：2005-03-28

Applicant: Callain Kim ,  Paige Mahaney ,  Eugene Trybulski ,  Puwen Zhang ,  Eugene Terefenko ,  Casey McComas ,  Michael Marella ,  Richard Coghlan ,  Gavin Heffernan ,  Stephen Cohn ,  An Vu ,  Joseph Sabatucci ,  Fei Ye

Inventor： Callain Kim ,  Paige Mahaney ,  Eugene Trybulski ,  Puwen Zhang ,  Eugene Terefenko ,  Casey McComas ,  Michael Marella ,  Richard Coghlan ,  Gavin Heffernan ,  Stephen Cohn ,  An Vu ,  Joseph Sabatucci ,  Fei Ye

IPC: A61K31/4045 ,  C07D209/08 ,  C07D209/30 ,  C07D209/42 ,  C07D235/06 ,  C07D241/42 ,  C07D265/36 ,  C07D471/04 ,  A61K31/5377 ,  A61K31/416 ,  A61K31/4184 ,  A61K31/454 ,  A61K31/496 ,  C07D413/02 ,  C07D43/02

CPC classification number: C07D209/08 ,  C07D209/30 ,  C07D209/42 ,  C07D235/06 ,  C07D241/42 ,  C07D265/36 ,  C07D471/04

Abstract: The present invention is directed to phenylaminopropanol derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.

Abstract translation: 本发明涉及式I的苯基氨基丙醇衍生物：或其药学上可接受的盐，含有这些衍生物的组合物及其用于预防和治疗由单胺再摄取改善的病症的方法，所述方法尤其包括血管舒缩症状（VMS） 特别是选自重度抑郁障碍，血管舒缩症状，压力和急迫性尿失禁，纤维肌痛，疼痛等的那些情况，特别是选自以下的那些病症：血管紧张素转换酶，抑制性功能障碍，性功能障碍，胃肠道和泌尿生殖系统疾病，慢性疲劳综合征，纤维瘤病综合征，神经系统疾病及其组合， 糖尿病性神经病变及其组合。

公开(公告)号：US20050222141A1

公开(公告)日：2005-10-06

申请号：US11018226

申请日：2004-12-22

Applicant: Kazuyuki Sagi ,  Tatsuya Okuzumi ,  Tatsuhiro Yamada ,  Shunsuke Kageyama ,  Yoichiro Shima ,  Tadakiyo Nakagawa ,  Munetaka Tokumasu ,  Masayuki Sugiki ,  Hajime Ito ,  Itsuya Tanabe ,  Tamotsu Suzuki ,  Akira Nakayama ,  Kazuyuki Ubukata ,  Kenji Shinkai ,  Yasuhiro Tanaka ,  Misato Noguchi ,  Ayatoshi Andou ,  Yoriko Yamamoto ,  Noriyasu Kataoka ,  Koichi Fujita

Inventor： Kazuyuki Sagi ,  Tatsuya Okuzumi ,  Tatsuhiro Yamada ,  Shunsuke Kageyama ,  Yoichiro Shima ,  Tadakiyo Nakagawa ,  Munetaka Tokumasu ,  Masayuki Sugiki ,  Hajime Ito ,  Itsuya Tanabe ,  Tamotsu Suzuki ,  Akira Nakayama ,  Kazuyuki Ubukata ,  Kenji Shinkai ,  Yasuhiro Tanaka ,  Misato Noguchi ,  Ayatoshi Andou ,  Yoriko Yamamoto ,  Noriyasu Kataoka ,  Koichi Fujita

IPC: A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  C07D239/70 ,  C07D239/96 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D413/02 ,  C07D417/02 ,  C07D471/04 ,  C07D487/04 ,  C07D43/02

CPC classification number: C07D239/70 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  C07D239/96 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D471/04 ,  C07D487/04

Abstract: Specific phenylalanine derivatives and analogues thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents for various diseases concerning α4 integrin.

Abstract translation: 具体的苯丙氨酸衍生物及其类似物对α4整联蛋白具有拮抗作用。 它们被用作关于α4整联蛋白的各种疾病的治疗剂。

公开(公告)号：US20050222139A1

公开(公告)日：2005-10-06

申请号：US10507595

申请日：2003-03-12

Applicant: Michael Roe ,  Andrzej Batt ,  David Evans ,  Gary Pitt ,  David Rooker

Inventor： Michael Roe ,  Andrzej Batt ,  David Evans ,  Gary Pitt ,  David Rooker

IPC: C07D215/08 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/498 ,  A61K31/538 ,  A61K31/5383 ,  A61P5/04 ,  A61P13/08 ,  A61P15/00 ,  A61P15/08 ,  A61P15/18 ,  A61P35/00 ,  C07D217/02 ,  C07D241/44 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D498/04 ,  A61K31/5415 ,  C07D413/02 ,  C07D417/02 ,  C07D43/02

CPC classification number: C07D413/14 ,  C07D217/02 ,  C07D241/44 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D413/06 ,  C07D417/06

Abstract: Compounds according to general formula 1, wherein A1-A3 are selected from A5 and A6 where A5 is either ═CR13— or ═N— and A6 is —NR14—, —O— or —S—; A4 is either a covalent bond or A5, provided that when A4 is a covalent bond one of A1-A3 must be A6 and the other two must be A5 and when A4 is A5 then all of A1-A3 must be A5; R1 is selected from H, NHY′ and COY2, in which case R2 is H, or R1 and R2 may both be methyl or together represent ═O; R3, R4 and R5 are each independently selected from H and lower alkyl groups; R6, R7, R8, R9, R10, R11 and R12 are each independently selected from H, lower alkyl groups, NH2, halogens (F, CI and Br) O-alkyl, CH2NM2 and CF3; R13 is selected from H, F, CI Br, NO2, NH2, OH, Me, Et, OMe, NMe2 and CF3; R14 is selected from H, methyl and ethyl; W is selected from ═CH— and ═N—; X is selected from CH2, O, S, SO2, NH and N lower alkyl; Y1 is selected from CO-lower alkyl, CO(CH2)bY3, CO(CH2)bCOY3 and CO(CH)NHCOY3, where b is 1-3; Y2 is selected from OR15, NR16R17 and NH(CH2)CCOY3, where c is 1-3; Y3 is selected from OR15 and NR16R17; R15 is selected from H, lower alkyl and (CH2)aR16, where a is 0-4; R16 and R17 are each independently selected from H, lower alkyl and (CH2)aR16 or together are —(CH2)2-Z-(CH2)2—; R18 is OH a phenyl group or an aromatic heterocycle selected from pyridyl, pyrimidinyl, pyrazinyl, furyl, thienyl, pyrrolyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, triazolyl, oxadiazolyl and thiadiazolyl, each of which may optionally have a lower alkyl group substituent; and Z is selected from O, CH2, S, SO2, NH and N-lower alkyl, are new. They are useful in the treatment of breast and prostate cancer, endometriosis and benign prostate hyperplasia, in the regulation of fertility, and in in vitro fertilisation.

公开(公告)号：US20050215784A1

公开(公告)日：2005-09-29

申请号：US11036258

申请日：2005-01-13

Applicant: David Madar ,  Stevan Djuric ,  Melissa Michmerhuizen ,  Hana Kopecka ,  Xiaofeng Li ,  Kenton Longenecker ,  Zhonghua Pei ,  Daisy Pireh ,  Hing Sham ,  Kent Stewart ,  Bruce Szczepankiewicz ,  Paul Wiedeman ,  Hong Yong

Inventor： David Madar ,  Stevan Djuric ,  Melissa Michmerhuizen ,  Hana Kopecka ,  Xiaofeng Li ,  Kenton Longenecker ,  Zhonghua Pei ,  Daisy Pireh ,  Hing Sham ,  Kent Stewart ,  Bruce Szczepankiewicz ,  Paul Wiedeman ,  Hong Yong

IPC: A61K31/551 ,  C07D207/16 ,  C07D207/26 ,  C07D207/27 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D413/02 ,  C07D417/02 ,  C07D417/12 ,  C07D43/02

CPC classification number: C07D207/16 ,  C07D207/27 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D417/12

Abstract: The present invention relates to compounds that inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.

Abstract translation: 本发明涉及抑制二肽基肽酶IV（DPP-IV）并可用于预防或治疗糖尿病，特别是II型糖尿病以及高血糖症，X综合症，高胰岛素血症，肥胖症，动脉粥样硬化和各种免疫调节疾病的化合物 。

公开(公告)号：US20050215598A1

公开(公告)日：2005-09-29

申请号：US11130531

申请日：2005-05-17

Applicant: Sarah Archibald ,  John Head ,  Graham Warrellow ,  John Porter

Inventor： Sarah Archibald ,  John Head ,  Graham Warrellow ,  John Porter

IPC: A61K31/195 ,  A61K31/44 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/455 ,  A61P29/00 ,  A61P37/02 ,  A61P43/00 ,  C07C233/87 ,  C07C235/60 ,  C07C237/30 ,  C07C323/62 ,  C07D213/61 ,  C07D213/81 ,  C07D403/12 ,  C07D213/46 ,  C07D43/02

CPC classification number: C07D213/81 ,  C07C233/87 ,  C07C235/60 ,  C07C237/30 ,  C07C323/62 ,  C07D213/61

Abstract: Phenylalanine derivatives of formula (1) are described: wherein R is a carboxylic acid or a derivative thereof; L1 is a linker atom or group; Ar is an optionally substituted aromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of alpha4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.

Abstract translation: 描述了式（1）的苯丙氨酸衍生物：其中R是羧酸或其衍生物; L 1是连接原子或基团; Ar是任选取代的芳族基团; 及其盐，溶剂合物，水合物和N-氧化物。 该化合物能够抑制α4整联蛋白与其配体的结合，并且可用于预防和治疗免疫或炎症性疾病。