公开(公告)号：US07452905B2

公开(公告)日：2008-11-18

申请号：US10402006

申请日：2003-03-31

Applicant: Nobuyasu Suzuki ,  Toshihiko Yoshimura ,  Eiji Nakanishi ,  Masahiro Murata ,  Takashi Tsuji

Inventor： Nobuyasu Suzuki ,  Toshihiko Yoshimura ,  Eiji Nakanishi ,  Masahiro Murata ,  Takashi Tsuji

IPC: A61K31/47 ,  C07D471/10 ,  C07D221/04

CPC classification number: C07D207/452 ,  A61K31/395 ,  A61K31/4015 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/435 ,  A61K31/4355 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/438 ,  A61K31/4412 ,  A61K31/45 ,  A61K31/472 ,  A61K31/48 ,  A61K31/4985 ,  A61K31/55 ,  C07D207/38 ,  C07D209/46 ,  C07D209/48 ,  C07D209/52 ,  C07D209/66 ,  C07D209/76 ,  C07D211/88 ,  C07D217/24 ,  C07D217/26 ,  C07D221/14 ,  C07D221/20 ,  C07D223/10 ,  C07D223/18 ,  C07D403/12 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

Abstract: Specific phenylalanine derivatives or pharmaceutically acceptable salts thereof have an antagonistic effect on the α 4 integrins and, therefore, are usable as therapeutic agents or preventive agents for diseases in which α 4 integrin-depending adhesion process participates in the pathology, such as inflammatory diseases, rheumatoid arthritis, inflammatory bowel diseases, systemic lupus erythematosus, multiple sclerosis, Sjögren's syndrome, asthma, psoriasis, allergy, diabetes, cardiovascular diseases, arterial sclerosis, restenosis, tumor proliferation, tumor metastasis and transplantation rejection.

Abstract translation: 特定的苯丙氨酸衍生物或其药学上可接受的盐对α4整联蛋白具有拮抗作用，因此可用作治疗剂或其中α4整联蛋白依赖性粘附过程参与病理学的疾病的预防剂，例如炎性疾病， 类风湿关节炎，炎性肠病，系统性红斑狼疮，多发性硬化症，Sjögren综合征，哮喘，牛皮癣，过敏，糖尿病，心血管疾病，动脉硬化，再狭窄，肿瘤增生，肿瘤转移和移植排斥。

公开(公告)号：US07425551B2

公开(公告)日：2008-09-16

申请号：US11726639

申请日：2007-03-22

Applicant: Alexander Flohr ,  Roland Jakob-Roetne ,  Wolfgang Wostl

Inventor： Alexander Flohr ,  Roland Jakob-Roetne ,  Wolfgang Wostl

IPC: C07D223/18 ,  A61K31/55

CPC classification number: C07D223/18

Abstract: The invention relates to malonamide derivatives of formula wherein A1, A2, R1, R2, R3, and R4 are as defined herein and to pharmaceutically acceptable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof for the treatment of Alzheimer's disease.

Abstract translation: 本发明涉及下式的丙二酰胺衍生物：其中A 1，S 2，R 1，R 2，R 2，R 2， R 4和R 4如本文所定义，以及用于治疗阿尔茨海默病的药学上可接受的酸加成盐，光学纯对映异构体，外消旋物或非对映体混合物。

公开(公告)号：US20080188463A1

公开(公告)日：2008-08-07

申请号：US12019667

申请日：2008-01-25

Applicant: Alexander Flohr ,  Roland Jakob-Roetne ,  Wolfgang Wostl

Inventor： Alexander Flohr ,  Roland Jakob-Roetne ,  Wolfgang Wostl

IPC: A61K31/55 ,  C07D223/18

CPC classification number: C07D223/18

Abstract: The invention relates to 6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl derivatives of formula I wherein R1, R2 and R3 are as defined herein. The compounds are γ-secretase inhibitors useful in the treatment of Alzheimer's disease or common cancer, including, but not limited to, cervical carcinomas and breast carcinomas and malignancies of the hematopoietic system.

Abstract translation: 本发明涉及式I的6-氧代-6,7-二氢-5H-二苯并[b，d]吖庚因-7-基衍生物，其中R 1，R 2， >和R 3'如本文所定义。 该化合物是可用于治疗阿尔茨海默病或常见癌症的γ-分泌酶抑制剂，包括但不限于宫颈癌和乳腺癌以及造血系统的恶性肿瘤。

公开(公告)号：US06949291B2

公开(公告)日：2005-09-27

申请号：US10381583

申请日：2001-09-26

Applicant: Andrew Holmes ,  Rainer Martin ,  Ian Rees ,  Cedric Fischmeister ,  Yuguang Ma ,  Franco Cacialli

Inventor： Andrew Holmes ,  Rainer Martin ,  Ian Rees ,  Cedric Fischmeister ,  Yuguang Ma ,  Franco Cacialli

IPC: H01L51/50 ,  C07D223/18 ,  C07D313/10 ,  C07D321/10 ,  C07D337/10 ,  C07F5/02 ,  C08G61/00 ,  C08G61/02 ,  C08G61/12 ,  C09K11/06 ,  H01B1/12 ,  H01L51/00 ,  H01L51/30 ,  B32B27/00 ,  C08G83/00

CPC classification number: H01L51/0035 ,  C07D223/18 ,  C07D313/10 ,  C07D321/10 ,  C07D337/10 ,  C07F5/025 ,  C08G61/02 ,  C08G61/12 ,  H01B1/128 ,  H01L51/0037 ,  H01L51/0038 ,  H01L51/0039 ,  H01L51/0043 ,  H01L51/0055 ,  H01L51/0059 ,  H01L51/5012 ,  Y10T428/31504

Abstract: The invention relates to optical devices comprising a substrate and at least one semiconductive polymer supported by said substrate, wherein said semiconductive polymer is a copolymer in which one of the repeat units is a group of formula (I) or a homopolymer in which the repeat unit is a group of formula (I): wherein: A and B are the same or different and each comprises wholly or partially an aryl moiety or a heteroaryl moiety, said moiety in A being fused to the bond a-b and said moiety in B being fused to the bond c-d, and X is a linking unit, X being such that there is a torsion angle of at least 5° between the bond a-b and the bond c-d about the bond b-d.The invention also relates to semiconductive polymers, monomers for preparing same, and methods for preparing random statistical conjugated polymers.

Abstract translation: 本发明涉及包括基材和由所述基材支持的至少一种半导体聚合物的光学装置，其中所述半导电聚合物是共聚物，其中一个重复单元是式（I）的基团或其中重复单元 是式（I）的基团：其中：A和B相同或不同，并且各自包括全部或部分芳基部分或杂芳基部分，A中的所述部分与键ab融合，并且B中的部分被稠合 键合键，X是连接单元，X使得在键合b 1和键cd之间存在至少5°的扭转角。 本发明还涉及半导体聚合物，制备它的单体和制备随机统计共轭聚合物的方法。

公开(公告)号：US20050119432A1

公开(公告)日：2005-06-02

申请号：US10945697

申请日：2004-09-21

Applicant: Katsuya Sakayori

Inventor： Katsuya Sakayori

IPC: C07D223/18 ,  C08F2/50 ,  C08F10/00 ,  C08F210/00 ,  C07D221/06 ,  C07F7/02

CPC classification number: C07D223/18 ,  C08F2/50 ,  C08F10/00 ,  C08F4/04

Abstract: A photoradical generator which produces no low-molecular decomposition material but a radical during a photoradical generating process, does not generate a radical during a heating process, exists in a chemically stable state in a resulting product of a radical reaction such as a cured coating layer or the like, has high heat resistance, stability and preserving ability, and is excellent in compatibility or solubility is provided. The photoradical generator is comprised of a compound (a) having a seven-membered ring imide structure-containing group represented by the following formula (1), wherein, R1 to R8 respectively represent a hydrogen atom or a substituent and may be a cyclic structure in which they are bonded to each other.

Abstract translation: 在光自由基产生过程中不产生低分子分解物质而不产生自由基的光自发生成器在加热过程中不产生自由基，在所得到的自由基反应产物如固化涂层中以化学稳定的状态存在 具有高的耐热性，稳定性和保存能力，并且具有优异的相容性或溶解性。 光自由基发生器由具有由下式（1）表示的含有七元环酰亚胺结构的基团的化合物（a）组成，其中R 1至R 8， SUP>分别表示氢原子或取代基，可以是它们彼此结合的环状结构。

公开(公告)号：US20030166636A1

公开(公告)日：2003-09-04

申请号：US10287117

申请日：2002-11-04

Inventor： Richard E. Olson ,  Hong Liu ,  Lorin A. Thompson

IPC: A61K031/55 ,  A61K031/541 ,  A61K031/5377 ,  A61K031/496 ,  A61K031/4545 ,  A61K031/454 ,  C07D417/02 ,  C07D413/02 ,  C07D43/02 ,  C07D41/02

CPC classification number: C07D223/18 ,  C07D223/10 ,  C07D223/12 ,  C07D223/16 ,  C07D243/08 ,  C07D243/14 ,  C07D243/24 ,  C07D243/26 ,  C07D401/04

Abstract: This invention relates to novel lactams having the formula (I): 1 to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Anull-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to null-amyloid production such as Alzheimer's disease and Down's Syndrome.

Abstract translation: 本发明涉及具有式（I）的新型内酰胺：其药物组合物及其使用方法。 这些新化合物抑制淀粉样蛋白前体蛋白的加工，更具体地，抑制Aβ肽的产生，从而起到防止淀粉样蛋白质神经沉积的形成的作用。 更具体地，本发明涉及治疗与β-淀粉样蛋白产生相关的神经系统疾病，例如阿尔茨海默病和唐氏综合征。

公开(公告)号：US06509331B1

公开(公告)日：2003-01-21

申请号：US09337484

申请日：1999-06-21

Applicant: James E. Audia ,  Richard C. Thompson ,  Stephen C. Wilkie ,  Thomas C. Britton ,  Warren J. Porter ,  George W. Huffman ,  Lee H. Latimer

Inventor： James E. Audia ,  Richard C. Thompson ,  Stephen C. Wilkie ,  Thomas C. Britton ,  Warren J. Porter ,  George W. Huffman ,  Lee H. Latimer

IPC: C07D48700

CPC classification number: C07D401/04 ,  A61K31/551 ,  A61K31/5513 ,  A61K31/553 ,  A61K31/655 ,  C07D221/22 ,  C07D223/18 ,  C07D243/12 ,  C07D243/14 ,  C07D243/24 ,  C07D409/04 ,  C07D409/12 ,  C07D417/04 ,  C07D471/06

Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

公开(公告)号：US20020173504A1

公开(公告)日：2002-11-21

申请号：US09915519

申请日：2001-07-27

Inventor： Jing Wu ,  Jay S. Tung ,  Eugene D. Thorsett ,  Michael A. Pleiss ,  Jeffrey S. Nissen ,  Jeffrey Neitz ,  Lee H. Latimer ,  Varghese John ,  Stephen Freedman ,  Thomas C. Britton ,  James E. Audia ,  Jon K. Reel ,  Thomas E. Mabry ,  Bruce A. Dressman ,  Cynthia L. Cwi ,  James J. Droste ,  Steven S. Henry ,  Stacey L. McDaniel ,  William Leonard Scott ,  Russell D. Stucky ,  Warren J. Porter

IPC: A61K031/55 ,  A61K031/445 ,  A61K031/4015 ,  A61K031/13

CPC classification number: C07D471/04 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/445 ,  A61K31/5513 ,  A61K38/05 ,  C07C237/22 ,  C07C2603/32 ,  C07D223/18 ,  C07D307/33 ,  C07D311/76 ,  C07D471/06 ,  C07D471/08

Abstract: Disclosed are compounds which inhibit null-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits null-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

Abstract translation: 公开了抑制β-淀粉样蛋白肽释放和/或其合成的化合物，因此具有治疗阿尔茨海默病的效用。 还公开了包含抑制β-淀粉样蛋白肽释放和/或其合成的化合物的药物组合物以及用这种药物组合物预防性和治疗性地治疗阿尔茨海默病的方法。

公开(公告)号：US20020103184A1

公开(公告)日：2002-08-01

申请号：US09825211

申请日：2001-04-03

Inventor： Richard E. Olson ,  Michael G. Yang

IPC: A61K031/55 ,  A61K031/445 ,  A61K031/4015 ,  C07D223/12

CPC classification number: C07D223/16 ,  A61K31/4015 ,  A61K31/445 ,  A61K31/55 ,  A61K38/00 ,  C07D223/10 ,  C07D223/12 ,  C07D223/18 ,  C07D243/14 ,  C07D243/24 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07K5/0205 ,  C07K5/06078 ,  C07K5/06139 ,  C07K5/06191 ,  C07K5/0812

Abstract: This invention relates to novel cyclic malonamides having the formula (I): 1 to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Anull-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to null-amyloid production such as Alzheimer's disease and Down's Syndrome.

Abstract translation: 本发明涉及具有式（I）的新型环状丙二酰胺：其药物组合物及其使用方法。 这些新化合物抑制淀粉样蛋白前体蛋白的加工，更具体地，抑制Aβ肽的产生，从而起到防止淀粉样蛋白质神经沉积的形成的作用。 更具体地，本发明涉及治疗与β-淀粉样蛋白产生相关的神经系统疾病，例如阿尔茨海默病和唐氏综合征。

公开(公告)号：US20020061874A1

公开(公告)日：2002-05-23

申请号：US09824945

申请日：2001-04-03

Inventor： Michael G. Yang ,  Hong Liu

IPC: A61K031/5513 ,  A61K031/55 ,  C07D243/24 ,  C07D223/16 ,  C07D223/18

CPC classification number: C07D407/12 ,  A61K38/00 ,  C07D223/18 ,  C07D243/14 ,  C07D243/24 ,  C07K5/06078

Abstract: This invention relates to novel lactams having the Formula (I): 1 to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Anull-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to null-amyloid production such as Alzheimer's disease and Down's Syndrome.

Abstract translation: 本发明涉及具有式（I）的新型内酰胺：其药物组合物及其使用方法。 这些新化合物抑制淀粉样蛋白前体蛋白的加工，更具体地，抑制Aβ肽的产生，从而起到防止淀粉样蛋白质神经沉积的形成的作用。 更具体地，本发明涉及治疗与β-淀粉样蛋白产生相关的神经系统疾病，例如阿尔茨海默病和唐氏综合征。