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1. 发明授权

US6013652A Spiro-substituted azacycles as neurokinin antagonists 失效
标题翻译：螺替代的azacycles作为神经激肽拮抗剂
公开(公告)号：US6013652A
公开(公告)日：2000-01-11
申请号：US985338
申请日：1997-12-04
申请人： Malcolm Maccoss , Sander G. Mills , Shrenik K. Shah , Yuan-Ching P. Chiang , Patrick T. Dunn , Hiroo Koyama
发明人： Malcolm Maccoss , Sander G. Mills , Shrenik K. Shah , Yuan-Ching P. Chiang , Patrick T. Dunn , Hiroo Koyama
IPC分类号： C07D471/10 , C07D491/10 , C07D495/10 , A61K31/44 , C07D401/02
CPC分类号： C07D471/10 , C07D491/10 , C07D495/10
摘要： Disclosed are spiro-substituted azacycles of formula I are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, and asthma. In particular compounds of formula I are shown to be neurokinin antagonists.
摘要翻译：公开的式I的螺取代的azacycles是可用于治疗炎性疾病，疼痛或偏头痛和哮喘的速激肽受体拮抗剂。特别地，式I化合物显示为神经激肽拮抗剂。

2. 发明授权

US08513289B2 P38 kinase inhibiting agents 有权
标题翻译： P38激酶抑制剂
公开(公告)号：US08513289B2
公开(公告)日：2013-08-20
申请号：US13266043
申请日：2010-04-26
申请人： Hiroo Koyama , Soumya P. Sahoo , Ginger Xu-Qiang Yang , Daniel J. Miller
发明人： Hiroo Koyama , Soumya P. Sahoo , Ginger Xu-Qiang Yang , Daniel J. Miller
IPC分类号： A61K31/4245 , A61K31/433 , C07D285/08 , C07D207/333
CPC分类号： C07D417/12 , C07D417/14
摘要： Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: Formula (I); are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of asthma, COPD, ARDS, rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and other conditions associated with inflammation.
摘要翻译：由化学式（I）或其药学上可接受的盐描述的化合物：式（I）; 是p38的抑制剂，可用于治疗炎症，例如治疗哮喘，COPD，ARDS，类风湿性关节炎，类风湿性脊椎炎，骨关节炎，痛风性关节炎和其他关节炎病症; 发炎关节，湿疹，牛皮癣或其他炎症皮肤病如晒伤; 炎症性眼病，包括结膜炎; 皮肤炎，疼痛等与炎症有关的病症。

3. 发明申请

US20120040999A1 P38 KINASE INHIBITING AGENTS 有权
标题翻译： P38激酶抑制剂
公开(公告)号：US20120040999A1
公开(公告)日：2012-02-16
申请号：US13266043
申请日：2010-04-26
申请人： Hiroo Koyama , Soumya P. Sahoo , Ginger Xu-Qiang Yang , Daniel J. Miller
发明人： Hiroo Koyama , Soumya P. Sahoo , Ginger Xu-Qiang Yang , Daniel J. Miller
IPC分类号： A61K31/433 , C07D417/14 , A61K31/4439 , A61P19/10 , C07D487/04 , A61K31/519 , A61P29/00 , A61P11/00 , C07D417/12 , A61K31/497
CPC分类号： C07D417/12 , C07D417/14
摘要： Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: Formula (I); are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of asthma, COPD, ARDS, rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and other conditions associated with inflammation.
摘要翻译：由化学式（I）或其药学上可接受的盐描述的化合物：式（I）; 是p38的抑制剂，可用于治疗炎症，例如治疗哮喘，COPD，ARDS，类风湿性关节炎，类风湿性脊椎炎，骨关节炎，痛风性关节炎和其他关节炎病症; 发炎关节，湿疹，牛皮癣或其他炎症皮肤病如晒伤; 炎症性眼病，包括结膜炎; 皮肤炎，疼痛等与炎症有关的病症。

4. 发明授权

US5681951A Metal catalyzed displacement process 失效
标题翻译：金属催化位移过程
公开(公告)号：US5681951A
公开(公告)日：1997-10-28
申请号：US459542
申请日：1995-06-02
申请人： Koichi Hirai , Yuji Iwano , Takahide Nishi , Akira Yoshida , Kozo Oda , Hiroo Koyama
发明人： Koichi Hirai , Yuji Iwano , Takahide Nishi , Akira Yoshida , Kozo Oda , Hiroo Koyama
IPC分类号： C07D205/08 , C07D401/12 , C07D403/12 , C07D477/02 , C07D477/04 , C07D477/20 , C07D499/88 , C07F7/10 , C07F7/18 , C07D499/00 , C07D487/04
CPC分类号： C07D401/12 , C07D205/08 , C07D403/12 , C07D477/02 , C07D477/04 , C07D477/20 , C07D499/88 , C07F7/10 , C07F7/186 , C07F7/1892 , Y02P20/55
摘要： A process for preparing a compound of formula (I'): ##STR1## comprising reacting a compound of formula (II'): ##STR2## with a compound of formula (III'): A'SH (III') wherein the reaction of the compound of formula (II') and the compound of formula (III') are carried out in the presence of a salt of a metal of Group II or III of the Periodic Table of Elements, wherein A' is an alkyl, aryl, aralkyl or heterocyclic, R.sup.1' is hydrogen or a carboxy protecting group, R.sup.2' and R.sup.3' can be hydrogen or alkyl, X' can be sulfur, k' is 1 or 2 and R.sup.4' is alkyl, alkenyl, aryl, aralkyl, cycloalkyl or heterocyclic.
摘要翻译：制备式（I'）化合物的方法：包括使式（II'）的化合物：（II'）与式（III'）的化合物反应：A' SH（III'）其中式（II'）化合物与式（III'）化合物的反应在元素周期表第II或III族金属的盐存在下进行，其中A'是烷基，芳基，芳烷基或杂环，R 1'是氢或羧基保护基，R 2'和R 3'可以是氢或烷基，X'可以是硫，k'是1或2，R 4' 烷基，烯基，芳基，芳烷基，环烷基或杂环基。

5. 发明授权

US5719275A Silyl enol ether alkylation process 失效
标题翻译：甲硅烷基烯醇醚烷基化方法
公开(公告)号：US5719275A
公开(公告)日：1998-02-17
申请号：US460546
申请日：1995-06-02
申请人： Koichi Hirai , Yuji Iwano , Takahide Nishi , Akira Yoshida , Kozo Oda , Hiroo Koyama
发明人： Koichi Hirai , Yuji Iwano , Takahide Nishi , Akira Yoshida , Kozo Oda , Hiroo Koyama
IPC分类号： C07D205/08 , C07D401/12 , C07D403/12 , C07D477/02 , C07D477/04 , C07D477/20 , C07D499/88 , C07F7/10 , C07F7/18 , C07D227/00 , C07D487/04 , C07D499/04
CPC分类号： C07D401/12 , C07D205/08 , C07D403/12 , C07D477/02 , C07D477/04 , C07D477/20 , C07D499/88 , C07F7/10 , C07F7/186 , C07F7/1892 , Y02P20/55
摘要： A method for preparing compounds of formula (I): ##STR1## wherein: R.sup.1 is hydrogen or a hydroxy-protecting group; R.sup.2 is alkyl, alkoxy, halogen, optionally substituted phenyl or optionally substituted phenoxy; R.sup.3 is optionally substituted pyridyl, optionally substituted quinolyl or phenyl group which has a substituent of formula --CYNR.sup.5 R.sup.6, where Y is oxygen or sulfur, and R.sup.5 and R.sup.6 are each alkyl, aryl or aralkyl, or R.sup.5 and R.sup.6 and the nitrogen to which they are attached together form a heterocyclic group; R.sup.4 is hydrogen or an amino-protecting group; and Z is sulfur or oxygen. The process comprises reacting a compound of formula (II): ##STR2## in which R.sup.8, R.sup.9 and R.sup.10 are the same or different and each represents an alkyl group having from 1 to 4 carbon atoms or a phenyl group, with a compound of formula (III): ##STR3## in which R.sup.11 represents an acyloxy, alkylsulfonyl, arylsulfonyl, alkylsulfinyl or arylsulfinyl group.
摘要翻译：制备式（I）化合物的方法：其中：R1是氢或羟基保护基; R 2是烷基，烷氧基，卤素，任选取代的苯基或任选取代的苯氧基; R3是任选取代的吡啶基，任选取代的具有式-CYNR 5 R 6的取代基的喹啉基或苯基，其中Y是氧或硫，R 5和R 6各自是烷基，芳基或芳烷基，或者R 5和R 6以及它们一起形成杂环基; R4是氢或氨基保护基; Z是硫或氧。该方法包括使式（II）化合物：其中R 8，R 9和R 10相同或不同并且各自表示具有1至4个碳原子的烷基或苯基的式（II）化合物与式（III）化合物：其中R 11表示酰氧基，烷基磺酰基，芳基磺酰基，烷基亚磺酰基或芳基亚磺酰基。

6. 发明授权

US5614624A Carbapenem 失效
标题翻译：卡巴培南
公开(公告)号：US5614624A
公开(公告)日：1997-03-25
申请号：US460209
申请日：1995-06-02
申请人： Koichi Hirai , Yuji Iwano , Takahide Nishi , Akira Yoshida , Kozo Oda , Hiroo Koyama
发明人： Koichi Hirai , Yuji Iwano , Takahide Nishi , Akira Yoshida , Kozo Oda , Hiroo Koyama
IPC分类号： C07D205/08 , C07D401/12 , C07D403/12 , C07D477/02 , C07D477/04 , C07D477/20 , C07D499/88 , C07F7/10 , C07F7/18 , C07D487/04
CPC分类号： C07D401/12 , C07D205/08 , C07D403/12 , C07D477/02 , C07D477/04 , C07D477/20 , C07D499/88 , C07F7/10 , C07F7/186 , C07F7/1892 , Y02P20/55
摘要： A compound of the formula ##STR1## in which: R.sup.1' is hydrogen or a carboxy-protecting group;R.sup.41' is hydrogen or a hydroxy-protecting group;R.sup.42' is a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxy, a halogen, an aryl or an aryloxy; R.sup.43' is hydrogen, a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxy, a hydroxy, a halogen, a cyano, a nitro or a group of the formula --NR.sup.8' R.sup.9', where R.sup.8' and R.sup.9' are independently selected from the group consisting of hydrogen, amino-protecting groups, C.sub.1 -C.sub.6 alkyl groups and phenyl groups, or R.sup.8' and R.sup.9' together represent a group --(CH.sub.2).sub.q '--O.sub.r '--(CH.sub.2).sub.s '--, where q' and s' are independently 0 or an integer of from 1 to 5 and r' is 0 or 1, provided that (q'+s') is an integer of at least 2; R.sup.45' and R.sup.46' are independently selected from the group consisting of C.sub.1 -C.sub.6 alkyl groups and aryl groups, or R.sup.45' and R.sup.46' together represent a group --(CH.sub.2).sub.q '--O.sub.r '--(CH.sub.2).sub.s '--, where q' and s' are independently 0 or an integer of from 1 to 5 and r' is 0 or 1; Y' is oxygen or sulfur; and j' is 0, 1 or 2.
摘要翻译：式（IV'）的化合物，其中：R1'是氢或羧基保护基; R 41'是氢或羟基保护基; R 42'是C 1 -C 6烷基，C 1 -C 6烷氧基，卤素，芳基或芳氧基; R 43'是氢，C 1 -C 6烷基，C 1 -C 6烷氧基，羟基，卤素，氰基，硝基或式-NR 8'R 9'基团，其中R 8'和R 9'独立地选自由氢，氨基保护基，C 1 -C 6烷基和苯基组成的组，或者R 8'和R 9'一起表示基团 - （CH 2）q'-Or' - （CH 2）s'，其中q' 和s'独立地为0或1至5的整数，r'为0或1，条件是（q'+ s'）为至少2的整数; R 45'和R 46'独立地选自C 1 -C 6烷基和芳基，或者R 45'和R 46'一起表示基团 - （CH 2）q'-Or' - （CH 2）s - ，其中 q'和s'独立地为0或1至5的整数，r'为0或1; Y'是氧或硫; 并且j'为0,1或2。

7. 发明授权

US5086497A Image output command method for image processing system 失效
标题翻译：图像处理系统的图像输出命令方法
公开(公告)号：US5086497A
公开(公告)日：1992-02-04
申请号：US600280
申请日：1990-10-22
申请人： Hiroshi Horikawa , Akira Watanabe , Hiroo Koyama , Ikuo Mori
发明人： Hiroshi Horikawa , Akira Watanabe , Hiroo Koyama , Ikuo Mori
IPC分类号： G06T11/60
CPC分类号： G06T11/60
摘要： An image output command method, in an image processing system comprising an input controller to dot and compress density or tone data for an image read out by an input unit and for temporarily staying the compressed image data at a buffer; a work station to picture-edit not only a code information edited by an editing input unit but also the image data by the use of an input operating means and a display means; a file server connected to the input controller and the work station by bus lines and for storing the image data, code information and edited data picture-edited by the work station in the file server; and an image setter for reading out the edited data stored in the file server and subjecting the edited data to a required data processing, which comprises the steps of: reading out the stored data from the file server, separating respective image data which constitute one page and commands which edit respective images when the images are transferred to the image output unit via the image setter and are outputted, and separating the data of a unit of one page to blocks and sub-blocks thereby to control image portions by output position and processing method.

8. 发明申请

US20090325953A1 P38 KINASE INHIBITING AGENTS 有权
标题翻译： P38激酶抑制剂
公开(公告)号：US20090325953A1
公开(公告)日：2009-12-31
申请号：US12481614
申请日：2009-06-10
申请人： Soumya P. Sahoo , Meng-Hsin Chen , Kevin D. Dykstra , Hiroo Koyama , Peter T. Meinke , Stephen J. O'Keefe , Ginger Xu-qiang Yang
发明人： Soumya P. Sahoo , Meng-Hsin Chen , Kevin D. Dykstra , Hiroo Koyama , Peter T. Meinke , Stephen J. O'Keefe , Ginger Xu-qiang Yang
IPC分类号： A61K31/437 , C07D471/04 , A61K31/519 , A61K31/5025 , A61K31/5377 , A61P11/06 , A61P19/00
CPC分类号： C07D519/00
摘要： Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of asthma, COPD, ARDS, rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and other conditions associated with inflammation.
摘要翻译：由化学式（I）或其药学上可接受的盐描述的化合物是p38的抑制剂，可用于治疗炎症，例如治疗哮喘，COPD，ARDS，类风湿性关节炎，类风湿性脊椎炎，骨关节炎，痛风性关节炎和其他关节炎病症; 发炎关节，湿疹，牛皮癣或其他炎症皮肤病如晒伤; 炎症性眼病，包括结膜炎; 皮肤炎，疼痛等与炎症有关的病症。

9. 发明授权

US06380191B1 Arylthiazolidinedione and aryloxazolidinedione derivatives 失效
标题翻译：芳基噻唑烷二酮和芳基恶唑烷二酮衍生物
公开(公告)号：US06380191B1
公开(公告)日：2002-04-30
申请号：US09595840
申请日：2000-06-16
申请人： Ranjit C. Desai , Soumya P. Sahoo , Jeffrey P. Bergman , Victoria K. Lombardo , Edward J. Metzger , Hiroo Koyama
发明人： Ranjit C. Desai , Soumya P. Sahoo , Jeffrey P. Bergman , Victoria K. Lombardo , Edward J. Metzger , Hiroo Koyama
IPC分类号： A61K315377
CPC分类号： C07D263/44 , C07D277/34 , C07D413/12
摘要： Substituted 5-aryl-2,4-thiazolidinediones and oxazolidinediones are potent agonists of PPAR, and are therefore useful in the treatment, control or prevention of diabetes, hyperglycemia, hyperlipidemia (including hypercholesterolemia and hypertriglyceridemia), atherosclerosis, obesity, vascular restenosis, and other PPAR &agr; and/or &ggr; mediated diseases, disorders and conditions.
摘要翻译：取代的5-芳基-2,4-噻唑烷二酮和恶唑烷二酮是PPAR的有效激动剂，因此可用于治疗，控制或预防糖尿病，高血糖症，高脂血症（包括高胆固醇血症和高甘油三酯血症），动脉粥样硬化，肥胖症，血管再狭窄和其他PPARα和/或γ介导的疾病，病症和病症。

10. 发明授权

US6090839A Antidiabetic agents 失效
标题翻译：抗糖尿病药
公开(公告)号：US6090839A
公开(公告)日：2000-07-18
申请号：US994123
申请日：1997-12-19
申请人： Alan D. Adams , Derek Von Langen , Richard L. Tolman , Hiroo Koyama
发明人： Alan D. Adams , Derek Von Langen , Richard L. Tolman , Hiroo Koyama
IPC分类号： A61K45/06 , C07D209/08 , C07D307/80 , C07D405/12 , C07D413/12 , A61K31/41 , C07D209/12 , C07D487/04 , C07D493/04
CPC分类号： C07D405/12 , A61K45/06 , C07D209/08 , C07D307/80 , C07D413/12
摘要： The instant invention is concerned with aryl and heteroaryl oxyacetic acid type compounds which are useful antidiabetic compounds. Compositions and methods for the use of the compounds in the treatment of diabetes and related diseases and for lowering triglyceride levels are also disclosed.
摘要翻译：本发明涉及作为有用的抗糖尿病化合物的芳基和杂芳基氧基乙酸型化合物。还公开了用于治疗糖尿病和相关疾病以及降低甘油三酯水平的化合物的组合物和方法。

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