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公开(公告)号：US5589473A
公开(公告)日：1996-12-31
申请号：US407730
申请日：1995-03-20
申请人： J urgen Geiwiz , Erwin G otschi , Paul Hebeisen , Helmut Link , Thomas L ubbers
发明人： J urgen Geiwiz , Erwin G otschi , Paul Hebeisen , Helmut Link , Thomas L ubbers
IPC分类号： A61K31/395 , A61K31/40 , A61K31/41 , A61K31/4245 , A61K31/425 , A61K31/44 , A61K31/535 , A61K31/5377 , A61P31/04 , C07D271/06 , C07D291/08 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D419/04 , C07D419/12 , C07D521/00 , C07F7/18
CPC分类号： C07D271/06 , C07D231/12 , C07D233/56 , C07D249/08 , C07D291/08 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D419/04 , C07D419/12 , C07F7/1856
摘要： The present invention relates to a compound of the formula ##STR1## wherein X.sup.1, R.sup.1, R.sup.2, OP, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.0 are as described herein, and their pharmaceutically acceptable salts thereof carrying an acidic and/or basic substituent.The compound of formula I as well as their pharmaceutically acceptable salts inhibit DNA gyrase activity in bacteria and possess antibiotic, especially antibacterial activity against microorganisms and can be used in the control or prevention of infectious diseases.
摘要翻译： 本发明涉及下式的化合物，其中X1，R1，R2，OP，R3，R4，R5，R6和R0如本文所述，及其药学上可接受的盐携带酸性和/或 碱性取代基。 式I化合物及其药学上可接受的盐抑制细菌中的DNA促旋酶活性，并且具有抗生素，特别是对微生物的抗菌活性，并且可用于控制或预防感染性疾病。
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22.发明授权
公开(公告)号：US5389620A
公开(公告)日：1995-02-14
申请号：US165880
申请日：1993-12-14
申请人： Kiyofumi Ishikawa , Toshio Nagase , Toshiaki Mase , Takashi Hayama , Masaki Ihara , Masaru Nishikibe , Mitsuo Yano
发明人： Kiyofumi Ishikawa , Toshio Nagase , Toshiaki Mase , Takashi Hayama , Masaki Ihara , Masaru Nishikibe , Mitsuo Yano
IPC分类号： C07D221/04 , C07D401/04 , C07D405/04 , C07D405/14 , C07D413/14 , C07D417/14 , C07D419/04 , A61K31/435
CPC分类号： C07D221/04 , C07D401/04 , C07D405/04 , C07D405/14 , C07D413/14 , C07D417/14 , C07D419/04
摘要： A heteroaromatic ring-fused cyclopentene derivative of the formula: ##STR1## wherein the variables are as defined in the specification; or a pharmaceutically acceptable salt thereof.
摘要翻译： 式（I）的杂芳环稠合环戊烯衍生物，其中变量如说明书中所定义; 或其药学上可接受的盐。
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23.发明申请NOVEL SUBSTITUTED PHENYL-OXATHIAZINE DERIVATIVES, METHOD FOR PRODUCING THEM, DRUGS CONTAINING SAID COMPOUNDS AND THE USE THEREOF 有权新型替代苯基 - 氧化氮衍生物，其生产方法，含有化合物的药物及其用途公开(公告)号：US20130338066A1
公开(公告)日：2013-12-19
申请号：US14003329
申请日：2012-03-07
申请人： Thomas Boehme , Christian Engel , Stefan Guessregen , Torsten Haack , Kurt Ritter , Georg Tschank
发明人： Thomas Boehme , Christian Engel , Stefan Guessregen , Torsten Haack , Kurt Ritter , Georg Tschank
IPC分类号： C07D291/06 , A61K45/06 , C07D419/10 , C07D515/10 , A61K31/551 , A61K31/547 , A61K31/541 , C07D419/04 , C07D419/12 , C07D419/14 , A61K31/54 , C07D291/08
CPC分类号： C07D291/06 , A61K31/54 , A61K31/541 , A61K31/547 , A61K31/551 , A61K45/06 , C07D291/08 , C07D419/04 , C07D419/10 , C07D419/12 , C07D419/14 , C07D515/10 , A61K2300/00
摘要： The invention relates to the compounds of formula (I) and to the physiologically acceptable salts thereof. Said compounds are suitable e.g. for the treatment of hyperglycemia.
摘要翻译： 本发明涉及式（I）化合物及其生理上可接受的盐。 所述化合物是合适的。 用于治疗高血糖症。
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公开(公告)号：US08173641B2
公开(公告)日：2012-05-08
申请号：US12654177
申请日：2009-12-11
IPC分类号： C07D291/08 , A01N43/88
CPC分类号： C07D291/08 , A01N37/50 , A01N43/88 , C07D419/04
摘要： The present invention relates to novel benzoxathiazine derivatives of the formula (I) in which R1, R2, R3, R4, R5 and R6 are each as defined in the description, to several processes for preparation thereof and to the use thereof as insecticides and/or acaricides in combination with further compositions such as penetrants and/or ammonium or phosphonium salts.
摘要翻译： 本发明涉及式（I）的新的苯并噻嗪衍生物，其中R 1，R 2，R 3，R 4，R 5和R 6各自如说明书中所定义，其几种制备方法及其作为杀虫剂和/ 或杀螨剂与其它组合物如渗透剂和/或铵或鏻盐的组合。
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公开(公告)号：US20110195936A1
公开(公告)日：2011-08-11
申请号：US12978087
申请日：2010-12-23
IPC分类号： A61K31/661 , C07F9/06 , C07C211/38 , A61K31/135 , C07C229/36 , A61K31/198 , A61P3/10 , A61P19/02 , A61P1/00 , A61P25/28
CPC分类号： C07D271/06 , C07C215/28 , C07C217/64 , C07D333/16 , C07D419/04 , C07F9/091 , C07F9/093
摘要： Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.
摘要翻译： 提供了在一种或多种S1P受体上具有激动剂活性的化合物。 化合物是鞘氨醇类似物，其在磷酸化之后可以作为S1P受体的激动剂。
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公开(公告)号：US20110118240A2
公开(公告)日：2011-05-19
申请号：US12654177
申请日：2009-12-11
CPC分类号： C07D291/08 , A01N37/50 , A01N43/88 , C07D419/04
摘要： The present invention relates to novel benzoxathiazine derivatives of the formula (I) in which R1, R2, R3, R5 and R6 are each as defined in the description, to several processes for preparation thereof and to the use thereof as insecticides and/or acaricides in combination with further compositions such as penetrants and/or ammonium or phosphonium salts.
摘要翻译： 本发明涉及式（I）的新的苯并噻嗪衍生物，其中R1，R2，R3，R5和R6各自如说明书中所定义，其几种制备方法及其作为杀虫剂和/或杀螨剂的用途 与其它组合物如渗透剂和/或铵或鏻盐组合。
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公开(公告)号：US20100331283A1
公开(公告)日：2010-12-30
申请号：US12822066
申请日：2010-06-23
申请人： Jeremy Hans , Eli M. Wallace , Qian Zhao , Shelley Allen , Ellen Laird , Joseph P. Lyssikatos , John E. Robisnson , Christopher P. Corrette , Robert Kirk DeLisle , Walter C. Voegtti
发明人： Jeremy Hans , Eli M. Wallace , Qian Zhao , Shelley Allen , Ellen Laird , Joseph P. Lyssikatos , John E. Robisnson , Christopher P. Corrette , Robert Kirk DeLisle , Walter C. Voegtti
IPC分类号： A61K31/675 , C07D417/04 , C07D513/04 , C07D419/04 , C07D471/04 , C07D487/04 , C07D495/04 , C07F9/06 , C07D417/14 , A61K31/433 , A61K31/437 , A61K31/4439 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/5355 , A61K31/542 , A61K31/4985 , A61K31/5025 , A61K31/519 , A61K31/454 , A61P35/00 , A61P31/10 , A61P37/00 , A61P29/00 , A61P9/00
CPC分类号： C07D513/04 , C07D285/12 , C07D417/04 , C07D417/14 , C07D419/04 , C07D471/04 , C07D487/04 , C07D495/04 , C07D497/04 , C07F9/65395
摘要： This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.
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公开(公告)号：US20080171737A1
公开(公告)日：2008-07-17
申请号：US11954466
申请日：2007-12-12
申请人： Andrew Fensome , Joel Adam Goldberg , Casey Cameron McComas , Charles William Mann , Edward George Melenski , Joseph Peter Sabatucci , Richard Page Woodworth
发明人： Andrew Fensome , Joel Adam Goldberg , Casey Cameron McComas , Charles William Mann , Edward George Melenski , Joseph Peter Sabatucci , Richard Page Woodworth
IPC分类号： A61K31/551 , C07D279/02 , A61K31/5415 , C07D291/08 , A61P1/00 , A61P25/00 , A61P13/00 , A61P15/00 , C07D285/15 , C07D243/08
CPC分类号： C07D279/02 , C07D285/15 , C07D291/08 , C07D417/04 , C07D419/04 , C07D419/06 , C07D487/08
摘要： The present invention is directed to cyclic sulfonamide derivatives of formula I: or a pharmaceutically acceptable salt thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behaviorial disorder, cognitive disorder, diabetic neuropathy, pain, and other diseases or disorders.
摘要翻译： 本发明涉及式I的环状磺酰胺衍生物或其药学上可接受的盐，它们是单胺再摄取抑制剂，含有这些衍生物的组合物，及其用于预防和治疗病症的方法，包括尤其是血管舒缩 症状，性功能障碍，胃肠道疾病和泌尿生殖器疾病，抑郁症，内源性行为障碍，认知障碍，糖尿病性神经病，疼痛和其他疾病或障碍。
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公开(公告)号：US20060247178A1
公开(公告)日：2006-11-02
申请号：US11415455
申请日：2006-05-01
申请人： Jeremy Hans , Eli Wallace , Qian Zhao , Shelley Allen , Ellen Laird , Joseph Lyssikatos , John Robinson , Christopher Corrette , Robert Delisle
发明人： Jeremy Hans , Eli Wallace , Qian Zhao , Shelley Allen , Ellen Laird , Joseph Lyssikatos , John Robinson , Christopher Corrette , Robert Delisle
IPC分类号： A61K38/05 , A61K38/04 , A61K31/53 , A61K31/501 , A61K31/506 , A61K31/4745 , A61K31/4439 , A61K31/433 , C07D417/02 , C07D285/08
CPC分类号： C07D513/04 , C07D285/12 , C07D417/04 , C07D417/14 , C07D419/04 , C07D471/04 , C07D487/04 , C07D495/04 , C07D497/04 , C07F9/65395
摘要： This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.
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公开(公告)号：US20050090533A1
公开(公告)日：2005-04-28
申请号：US10884707
申请日：2004-07-02
申请人： Torsten Hoffmann , Andreas Koblet , Jens-Uwe Peters , Patrick Schnider , Andrew Sleight , Heinz Stadler
发明人： Torsten Hoffmann , Andreas Koblet , Jens-Uwe Peters , Patrick Schnider , Andrew Sleight , Heinz Stadler
IPC分类号： A61K31/44 , A61K31/4418 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/46 , A61K31/496 , A61K31/4995 , A61K31/5377 , A61K31/5386 , A61K31/541 , A61K31/547 , A61K31/551 , A61K31/554 , C07D213/75 , C07D401/04 , C07D413/04 , C07D417/04 , C07D419/04 , C07D451/04 , C07D487/08 , C07D491/10 , C07D495/10 , C07D497/10 , C07D498/08 , C07D513/08
CPC分类号： C07D213/75 , A61K31/44 , A61K31/4418 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/46 , A61K31/496 , A61K31/4995 , A61K31/5377 , A61K31/5386 , A61K31/541 , A61K31/547 , A61K31/551 , A61K31/554 , C07D401/04 , C07D413/04 , C07D417/04 , C07D419/04 , C07D451/04 , C07D487/08 , C07D491/10 , C07D495/10 , C07D497/10 , C07D513/08
摘要： The present invention provides a method for the treatment of schizophrenia which comprises administering a compound of formula wherein the substituents are as described herein or a pharmaceutically active acid-addition salt thereof. In particular, the invention provides methods for treating both positive and negative symptoms of schizophrenia through dual inhibition of NK1 and NK3 receptors. The invention also provides novel compounds with formula I and methods for preparing compounds of the invention.
摘要翻译： 本发明提供了一种治疗精神分裂症的方法，其包括给予下列化合物，其中取代基如本文所述或其药学活性的酸加成盐。 特别地，本发明提供了通过NK1和NK3受体的双重抑制来治疗精神分裂症的正和负症状的方法。 本发明还提供具有式I的新化合物和制备本发明化合物的方法。
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