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31. 发明授权

US07074819B2 Benzopyran or thiobenzopyran derivatives 失效
标题翻译：苯并吡喃或硫代苯并吡喃衍生物
公开(公告)号：US07074819B2
公开(公告)日：2006-07-11
申请号：US10640696
申请日：2003-08-12
申请人： Jae Chon Jo , Hyun Suk Lim , Jong Min Kim , Ju Su Kim , Kazumi Morikawa , Yoshitake Kanbe , Myung Hwa Kim , Masahiro Nishimoto
发明人： Jae Chon Jo , Hyun Suk Lim , Jong Min Kim , Ju Su Kim , Kazumi Morikawa , Yoshitake Kanbe , Myung Hwa Kim , Masahiro Nishimoto
IPC分类号： A61K31/38 , C07D335/04
CPC分类号： C07D335/06 , C07D311/58 , C07D405/04 , C07D405/06 , C07D407/06 , C07D413/06 , C07D417/06
摘要： The present invention relates to a novel benzopyran or thiobenzopyran derivative represented by formula (1): pharmaceutically acceptable salt or stereoisomer thereof, in which X, R1, R2, R3, R4 and A are defined as described in the specification, and to a process for preparation thereof and a pharmaceutical composition having anti-estrogenic activity which contains the compound (1) as an active component.
摘要翻译：本发明涉及由式（1）表示的新的苯并吡喃或硫代苯并吡喃衍生物：其药学上可接受的盐或立体异构体，其中X，R 1，R 2，R R 3，R 4和A如说明书中所述定义，其制备方法和具有抗雌激素活性的药物组合物含有化合物（1 ）作为活性成分。

32. 发明申请

US20060106233A1 Process for the preparation of disubstituted acetylenes bearing heteroaromatic and heterobicyclic groups 审中-公开
公开(公告)号：US20060106233A1
公开(公告)日：2006-05-18
申请号：US11155847
申请日：2005-06-17
申请人： Bobba Kumar , Shekhar Bhirud , Batchu Chandrasekhar , Changdev Raut
发明人： Bobba Kumar , Shekhar Bhirud , Batchu Chandrasekhar , Changdev Raut
IPC分类号： C07D335/06 , C07D215/60
CPC分类号： C07D335/06
摘要： A process for the preparation of a disubstituted acetylene bearing heteroaromatic and heterobicyclic groups of formula I is provided wherein X is S, O, or NR1 wherein R1 is hydrogen or a C1-C6 straight or branched alkyl group; R is hydrogen or a C1-C6 straight or branched alkyl group; A is a substituted or unsubstituted pyridinyl, thienyl, furyl, pyridazinyl, pyrimidinyl or pyrazinyl group; n is 0-4; and B is H, —COOH, —CH2OH, —CHO or a C1-C6 alkyl acetal derivative, —COR2 or a C1-C6 alkyl ketal derivative where R2 is —(CH2)mCH3 where m is 0-4 or COOR3 wherein R3 is a straight or branched C1-C30 alkyl group, a substituted or unsubstituted C6-C30 aromatic group, a substituted or unsubstituted C3-C30 cycloalkyl, a substituted or unsubstituted C3-C30 cycloalkylalkyl, a substituted or unsubstituted C3-C30 cycloalkenyl, a substituted or unsubstituted C5-C30 aryl, a substituted or unsubstituted C5-C30 arylalkyl, a substituted or unsubstituted C5-C30 heteroaryl, a substituted or unsubstituted C3-C30 heterocyclic ring, a substituted or unsubstituted C4-C30 heterocyclylalkyl, a substituted or unsubstituted C6-C30 heteroarylalkyl, the process comprising a Sonogashira coupling reaction between a compound of formula II wherein X and R have the aforestated meanings, with a compound of formula III X′-A-(CH2)n—B (III) wherein X′ is a halogen and A, n and B have the aforestated meanings, in the presence of a base and a transition metal catalyst and in a polar aprotic solvent.

33. 发明申请

US20060105961A1 Method of using a cox-2 inhibitor and a topoisomerase II inhibitor as a combination therapy in the treatment of neoplasia 审中-公开
标题翻译：在治疗肿瘤中使用cox-2抑制剂和拓扑异构酶II抑制剂作为联合疗法的方法
公开(公告)号：US20060105961A1
公开(公告)日：2006-05-18
申请号：US10539856
申请日：2003-12-17
申请人： Jaime Masferrer
发明人： Jaime Masferrer
IPC分类号： A61K31/7052 , A61K31/50 , A61K31/473 , A61K31/18 , A61K31/415 , A61K31/42
CPC分类号： A61K31/135 , A61K31/18 , A61K31/415 , A61K31/42 , A61K31/445 , A61K31/473 , A61K31/50 , A61K31/505 , A61K31/506 , A61K31/675 , A61K31/7052 , A61K33/24 , A61K41/00 , A61K41/0038 , A61K45/06 , C07D215/54 , C07D311/22 , C07D311/58 , C07D311/92 , C07D335/06 , C07D401/12 , C07D405/04 , C07D407/04 , C07D407/12 , C07D409/04 , C07D471/04 , C07D491/04 , C07D493/04 , A61K2300/00
摘要： The present invention provides compositions and methods to treat, prevent or inhibit a neoplasia or a neoplasia-related disorder in a mammal using a combination of a COX-2 inhibitor and a topoisomerase II inhibitor.
摘要翻译：本发明提供了使用COX-2抑制剂和拓扑异构酶II抑制剂的组合来治疗，预防或抑制哺乳动物中的肿瘤形成或瘤形成相关病症的组合物和方法。

34. 发明授权

US07026487B2 Amines substituted with a dihydronaphthalenyl, chromenyl, or thiochromenyl group, a pyridyl group and an alkyl group, having retinoid-like biological activity 失效
标题翻译：被二氢萘基，色烯基或硫代色烯基取代的胺，吡啶基和烷基，具有类视黄醇样生物活性
公开(公告)号：US07026487B2
公开(公告)日：2006-04-11
申请号：US10612667
申请日：2003-07-02
申请人： Richard L. Beard , Thong Vu , Diana F. Colon , Vidyasagar Vuligonda , Roshantha A. Chandraratna
发明人： Richard L. Beard , Thong Vu , Diana F. Colon , Vidyasagar Vuligonda , Roshantha A. Chandraratna
IPC分类号： C07D213/74 , C07D407/12 , C07D409/12
CPC分类号： C07D335/06 , C07C229/60 , C07C2602/10 , C07D311/20
摘要： Compounds of the formula where the symbols are as defined in the specification, have retinoid agonist, antagonist or negative hormone-like biological activity.
摘要翻译：其中符号如说明书中所定义的式的化合物具有类视黄醇激动剂，拮抗剂或负激素样生物活性。

35. 发明授权

US07015328B2 Substituted coumarins and quinolines and analogs as activators of caspases and inducers of apoptosis and the use thereof 失效
公开(公告)号：US07015328B2
公开(公告)日：2006-03-21
申请号：US10146136
申请日：2002-05-16
申请人： Sui Xiong Cai , Hong Zhang , William E. Kemnitzer , Songchun Jiang , John Drewe , Richard Storer
发明人： Sui Xiong Cai , Hong Zhang , William E. Kemnitzer , Songchun Jiang , John Drewe , Richard Storer
IPC分类号： C07D311/04 , C07D405/00 , C07D217/02 , A61K31/47
CPC分类号： C07D335/06 , A61K31/35 , A61K31/385 , A61K31/47 , C07D215/54 , C07D221/10 , C07D311/16 , C07D311/58 , C07D409/04 , C07D471/04 , C07D491/04 , C07D493/04 , C07D495/04 , C07D513/04
摘要： The present invention is directed to substituted coumarins and quinolines and analogs thereof, represented by the general Formula I: wherein A, B, X, Y, and Z are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

36. 发明申请

US20050261273A1 Substituted urea and carbamate, phenacyl-2-hydroxy-3-diaminoalkane, and benzamide-2-hydroxy-3-diaminoalkane aspartyl-protease inhibitors 审中-公开
标题翻译：取代的脲和氨基甲酸酯，苯甲酰甲基-2-羟基-3-二氨基烷烃和苯甲酰胺-2-羟基-3-二氨基烷烃天冬氨酰蛋白酶抑制剂
公开(公告)号：US20050261273A1
公开(公告)日：2005-11-24
申请号：US11075292
申请日：2005-03-09
申请人： Varghese John , Michel Maillard , John Tucker , Jose Aquino , Roy Hom , Jay Tung , Darren Dressen , Neerav Shah , R. Neitz
发明人： Varghese John , Michel Maillard , John Tucker , Jose Aquino , Roy Hom , Jay Tung , Darren Dressen , Neerav Shah , R. Neitz
IPC分类号： A61K31/16 , A61K31/40 , A61K31/445 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K31/553 , C07C215/28 , C07C229/42 , C07C229/60 , C07C233/40 , C07C235/10 , C07C235/42 , C07C235/74 , C07C235/82 , C07C237/14 , C07C237/30 , C07C239/16 , C07C255/34 , C07C275/06 , C07C275/14 , C07C275/26 , C07C275/28 , C07C311/03 , C07C311/05 , C07C311/07 , C07C311/08 , C07C323/30 , C07C323/59 , C07C327/46 , C07D205/04 , C07D207/16 , C07D207/28 , C07D209/12 , C07D209/18 , C07D211/56 , C07D211/58 , C07D211/94 , C07D213/56 , C07D213/81 , C07D213/82 , C07D231/14 , C07D233/30 , C07D233/46 , C07D233/54 , C07D233/76 , C07D233/90 , C07D239/26 , C07D241/24 , C07D257/04 , C07D261/08 , C07D261/10 , C07D261/14 , C07D261/18 , C07D277/14 , C07D277/28 , C07D277/56 , C07D307/00 , C07D307/24 , C07D307/54 , C07D307/68 , C07D309/14 , C07D311/96 , C07D317/72 , C07D333/20 , C07D333/24 , C07D333/28 , C07D333/38 , C07D335/06 , C07D405/10 , C07D407/12 , C07F9/40
CPC分类号： C07D335/06 , A61K31/16 , C07C215/28 , C07C229/42 , C07C229/60 , C07C233/36 , C07C233/40 , C07C235/10 , C07C235/74 , C07C235/82 , C07C237/30 , C07C239/16 , C07C255/34 , C07C271/20 , C07C271/22 , C07C275/14 , C07C275/26 , C07C311/03 , C07C311/05 , C07C311/07 , C07C311/08 , C07C323/30 , C07C323/59 , C07C327/46 , C07C2601/02 , C07C2601/10 , C07C2601/14 , C07C2602/10 , C07C2603/74 , C07D205/04 , C07D207/16 , C07D207/28 , C07D209/12 , C07D209/18 , C07D209/42 , C07D211/56 , C07D211/58 , C07D211/94 , C07D213/56 , C07D213/81 , C07D213/82 , C07D231/14 , C07D233/30 , C07D233/46 , C07D233/58 , C07D233/64 , C07D233/76 , C07D233/90 , C07D239/26 , C07D241/24 , C07D257/04 , C07D261/08 , C07D261/10 , C07D261/14 , C07D261/18 , C07D277/14 , C07D277/24 , C07D277/28 , C07D277/56 , C07D307/00 , C07D307/24 , C07D307/54 , C07D307/68 , C07D309/14 , C07D311/96 , C07D317/72 , C07D333/18 , C07D333/20 , C07D333/24 , C07D333/28 , C07D333/38 , C07D405/10 , C07D407/12 , C07F9/4006
摘要： The invention relates to acetyl 2-hydroxy-1,3-diaminospirocyclohexanes and derivatives thereof that are useful in treating at least one disease, disorder, and condition associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and condition associated with abnormal deposition of A-beta protein.
摘要翻译：本发明涉及可用于治疗与淀粉样变性相关的至少一种疾病，病症和状况的乙酰基2-羟基-1,3-二氨基螺环己烷及其衍生物。淀粉样变性是指与A-β蛋白异常沉积相关的疾病，病症和病症的集合。

37. 发明申请

US20050240029A1 Process for the preparation of 4,4-dimethyl-6-ethynylthiochroman 失效
标题翻译：制备4,4-二甲基-6-乙炔基二氢苯并噻喃的方法
公开(公告)号：US20050240029A1
公开(公告)日：2005-10-27
申请号：US11158856
申请日：2005-06-22
申请人： Bobba Venkata Kumar , Vishvas Patil , Changdev Raut , Shekhar Bhirud , Batchu Chandrasekhar
发明人： Bobba Venkata Kumar , Vishvas Patil , Changdev Raut , Shekhar Bhirud , Batchu Chandrasekhar
IPC分类号： C07D335/06 , C07D335/04 , A61K31/382
CPC分类号： C07D335/06
摘要： An improved process for the preparation of key intermediates for tazarotene, 4,4-dimethyl-6-ethynylthiochroman, is provided comprising (a) reacting 4,4-dimethyl-6-acetylthiochroman of the formula with an acid chloride and an amido-group containing compound of the general formula wherein R is hydrogen or a hydrocarbyl of from 1 to 15 carbon atoms and R1 and R2 can be the same or different and are hydrocarbyls of from 1 to 15 carbon atoms or R1 and R2 together with the nitrogen atom to which they are bonded are joined together to form a heterocyclic group, optionally containing one or more additional heterocyclic atoms, or one of R1 and R2 together with the nitrogen atom to which it bonded are joined together with the carbonyl radical to form a heterocyclic group, optionally containing one or more additional heterocyclic atoms to form a chloro vinyl carbonyl compound intermediate of the general formula wherein R has the aforestated meanings; and (b) reacting the β-chloro vinyl carbonyl compound intermediate with an alkali metal to provide the 4,4-dimethyl-6-ethynylthiochroman.
摘要翻译：提供了一种用于制备他扎罗汀4,4-二甲基-6-乙炔基二氢苯并噻喃的关键中间体的改进方法，其包括（a）使下式的4,4-二甲基-6-乙酰基二氢苯并二氢吡喃与酰氯和酰氨基其中R是氢或1至15个碳原子的烃基，R 1和R 2可以相同或不同，并且是烃基的通式 1至15个碳原子或R 1和R 2与它们所键合的氮原子一起连接在一起形成杂环基，任选地含有一个或多个另外的杂环原子或R 1和R 2中的一个与其键合的氮原子一起与羰基连接在一起形成杂环基，任选地含有一个或多个另外的杂环原子以形成通式的氯乙烯基羰基化合物中间体，其中R具有af ;意和（b）使β-氯乙烯基羰基化合物中间体与碱金属反应，得到4,4-二甲基-6-乙炔基二氢苯并噻喃。

38. 发明授权

US06905786B2 Light emitting device material, light emitting device using thereof, and amine compound 失效
标题翻译：发光元件材料，使用其的发光元件和胺化合物
公开(公告)号：US06905786B2
公开(公告)日：2005-06-14
申请号：US10308037
申请日：2002-12-03
申请人： Kazumi Nii
发明人： Kazumi Nii
IPC分类号： C07D311/28 , C07D215/22 , C07D215/233 , C07D311/30 , C07D311/60 , C07D311/92 , C07D335/06 , C07D405/04 , C07D405/10 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/06 , C07D417/04 , C07D417/14 , C09K11/06 , H01L51/30 , H01L51/50 , H05B33/12 , H05B33/14 , C07D213/02 , C07D309/34 , C07D335/02
CPC分类号： H01L51/0073 , C07D215/233 , C07D311/30 , C07D311/60 , C07D311/92 , C07D335/06 , C07D405/04 , C07D405/10 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/06 , C07D417/04 , C07D417/14 , C09K11/06 , H01L51/0042 , H01L51/0051 , H01L51/0053 , H01L51/0059 , H01L51/006 , H01L51/0061 , H01L51/0062 , H01L51/0065 , H01L51/0068 , H01L51/0072 , H01L51/0074 , H01L51/0081 , H01L51/50 , H01L2251/308 , Y10S428/917
摘要： A compound represented by the following formula (I): wherein R1, R2 and R3each represents an aryl group, a heterocyclic group or an aliphatic hydrocarbon group, provided that at least one of R1, R2 and R3 represents an aryl group or a heterocyclic group and at least one of the aryl group and heterocyclic group contains a group represented by formula (II), R1, R2 and R3 may be linked to each other to form a ring, wherein R4, R5 and R6, each represents a hydrogen atom or a substituent; X1 represents an oxygen atom, a sulfur atom, N—RX1 or CRX2RX3; RX1, RX2,RX3 each represents a hydrogen atom or a substituent; R4, R5, R6 and X1 may be linked to each other to form a ring; Y represents an oxygen atom, a sulfur atom, or N—RY1; and RY1 represents a hydrogen atom or a substituent.
摘要翻译：由下式（I）表示的化合物：其中R 1，R 2和R 3各自表示芳基，杂环基或脂族烃基，条件是R 1，R 2和R 3中的至少一个表示芳基或杂环基，并且芳基和杂环基中的至少一个含有由式（II）表示的基团，R 1，R 2，R 3和R 3可以彼此连接形成环，其中R 4，R 5和R 6各自表示氢原子或取代基; X 1表示氧原子，硫原子，N-R X 1或X 2 X 3 R 3 X 3; R X1，R X2，R X3各自表示氢原子或取代基; R 4，R 5，R 6和X 1可以彼此连接形成环; Y表示氧原子，硫原子或N-R Y1; R 1表示氢原子或取代基。

39. 发明授权

US06890952B2 Cyclic substituted aminomethyl compounds and medicaments comprising these compounds 失效
标题翻译：环状取代的氨基甲基化合物和包含这些化合物的药物
公开(公告)号：US06890952B2
公开(公告)日：2005-05-10
申请号：US10339671
申请日：2003-01-10
申请人： Oswald Karl Zimmer , Babette-Yvonne Koegel , Wolfgang Werner Alfred Strassburger
发明人： Oswald Karl Zimmer , Babette-Yvonne Koegel , Wolfgang Werner Alfred Strassburger
IPC分类号： A61K31/137 , A61K31/335 , A61K31/38 , A61P1/12 , A61P13/02 , A61P17/04 , A61P25/02 , A61P25/20 , A61P27/16 , A61P29/00 , C07C209/68 , C07C211/29 , C07C211/30 , C07C213/00 , C07C213/08 , C07C215/50 , C07C215/64 , C07C217/74 , C07D311/58 , C07D313/08 , C07D335/06 , C07D337/08 , A61K31/35 , C07D311/04
CPC分类号： C07D335/06 , C07C211/29 , C07C215/64 , C07C217/74 , C07C2602/10 , C07C2602/12 , C07D311/58 , C07D313/08 , C07D337/08
摘要： Cyclic substituted aminomethyl compounds of general formula IA and IB, methods for production thereof, intermediates in said production methods, a medicament containing at least one of said cyclic substituted aminomethyl compounds, the use of said cyclic substituted aminomethyl compounds for the production of a medicament, pharmaceutical compositions containing said compounds, and methods for the treatment of pain, incontinence, pruritis, tinnitus aurium and/or diarrhea using said pharmaceutical compositions.
摘要翻译：通式IA和IB的环状取代的氨基甲基化合物，其制备方法，所述制备方法中的中间体，含有至少一种所述环状取代的氨基甲基化合物的药物，所述环状取代的氨基甲基化合物在制备药物中的用途，含有所述化合物的药物组合物，以及使用所述药物组合物治疗疼痛，失禁，瘙痒，耳鸣耳鸣和/或腹泻的方法。

40. 发明授权

US06872851B1 Substituted cyclic compounds, preparation method and pharmaceutical compositions containing them 失效
标题翻译：取代的环状化合物，制备方法和含有它们的药物组合物
公开(公告)号：US06872851B1
公开(公告)日：2005-03-29
申请号：US09700098
申请日：1999-05-10
申请人： Daniel Lesieur , Frédérique Klupsch , Gérald Guillaumet , Marie-Claude Viaud , Michel Langlois , Caroline Bennejean , Pierre Renard , Philippe Delagrange
发明人： Daniel Lesieur , Frédérique Klupsch , Gérald Guillaumet , Marie-Claude Viaud , Michel Langlois , Caroline Bennejean , Pierre Renard , Philippe Delagrange
IPC分类号： C07D295/12 , A61K31/16 , A61K31/165 , A61K31/166 , A61K31/17 , A61K31/18 , A61K31/19 , A61K31/27 , A61K31/341 , A61K31/343 , A61K31/352 , A61K31/357 , A61K31/381 , A61K31/382 , A61K31/4025 , A61K31/403 , A61K31/404 , A61K31/4045 , A61K31/405 , A61K31/4184 , A61K31/423 , A61K31/435 , A61K31/4355 , A61K31/436 , A61K31/4365 , A61K31/437 , A61K31/4402 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/4453 , A61K31/453 , A61K31/454 , A61K31/473 , A61K31/5355 , A61K31/5375 , A61K31/5377 , A61K31/55 , A61P1/00 , A61P3/06 , A61P3/10 , A61P5/02 , A61P9/00 , A61P15/08 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P35/00 , A61P43/00 , C07C233/36 , C07C233/40 , C07C233/43 , C07C233/62 , C07C233/65 , C07C237/48 , C07C271/20 , C07C271/30 , C07C275/24 , C07C275/40 , C07C311/46 , C07C317/32 , C07C323/40 , C07C323/41 , C07C323/44 , C07C323/62 , C07D207/26 , C07D207/27 , C07D209/08 , C07D209/14 , C07D209/16 , C07D209/18 , C07D209/20 , C07D209/60 , C07D209/90 , C07D213/70 , C07D221/08 , C07D221/10 , C07D233/42 , C07D233/84 , C07D235/06 , C07D235/14 , C07D261/20 , C07D295/18 , C07D307/68 , C07D307/77 , C07D307/81 , C07D307/92 , C07D311/58 , C07D311/60 , C07D311/92 , C07D319/18 , C07D319/20 , C07D333/20 , C07D333/38 , C07D333/40 , C07D333/50 , C07D333/56 , C07D333/58 , C07D333/74 , C07D335/06 , C07D335/08 , C07D401/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D407/12 , C07D409/06 , C07D471/04 , C07D471/14 , C07D491/04 , C07D491/048 , C07D491/052 , C07D493/04 , C07D495/04 , C07D495/14 , C07D521/00 , C07C233/05
CPC分类号： C07D207/27 , C04B35/632 , C07C233/43 , C07C233/62 , C07C233/65 , C07C237/48 , C07C271/20 , C07C275/24 , C07C323/62 , C07C2601/02 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07D209/14 , C07D209/20 , C07D209/60 , C07D213/70 , C07D221/10 , C07D231/12 , C07D233/42 , C07D233/56 , C07D233/84 , C07D235/06 , C07D249/08 , C07D261/20 , C07D307/81 , C07D307/92 , C07D311/58 , C07D311/60 , C07D319/18 , C07D319/20 , C07D333/20 , C07D333/38 , C07D333/58 , C07D333/74 , C07D335/06 , C07D335/08 , C07D401/12 , C07D405/06 , C07D405/12 , C07D407/12 , C07D471/04 , C07D491/04 , C07D495/04 , C07D495/14
摘要： The invention concerns compounds of formula (I): R—A—R′ wherein: A is as defined in the description; R represent, a group (V), wherein R′a and R″a are as defined in the description, or R forms with A a cyclic structure as defined in the description; R′ represents a (CH2)t—R2 group wherein q, t, and R2 are as defined in the description. The invention is useful for preparing medicines.
摘要翻译：本发明涉及式（I）化合物：R-A-R'其中：A如说明书中所定义; R表示基团（V），其中R'a和R'a如说明书中所定义，或R与A形成如说明书中定义的环状结构; R'表示（CH 2）t -R 2基团，其中q，t和R 2如说明书中所定义。本发明可用于制备药物。

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