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41. 发明申请

US20120302602A1 Vanilloid Receptor Ligand Compounds, Pharmaceutical Compositions Containing Them, a Method of Producing Them and the Use Thereof to Treat Pain and Various Other Conditions 失效
标题翻译：香草素受体配体化合物，含有它们的药物组合物，其生产方法及其用途来治疗疼痛和各种其他病症
公开(公告)号：US20120302602A1
公开(公告)日：2012-11-29
申请号：US13557663
申请日：2012-07-25
申请人： Robert Frank , Gregor Bahrenberg , Thomas Christoph , Klaus Schiene , Jean De Vry , Derek Saunders , Jeewoo Lee
发明人： Robert Frank , Gregor Bahrenberg , Thomas Christoph , Klaus Schiene , Jean De Vry , Derek Saunders , Jeewoo Lee
IPC分类号： C07D401/04 , C07D213/70 , A61K31/44 , A61P29/00 , A61P25/00 , A61P25/06 , A61P19/02 , A61P25/24 , A61P25/28 , A61P25/08 , A61P25/16 , A61P11/00 , A61P11/14 , A61P13/00 , A61P13/10 , A61P1/00 , A61P1/04 , A61P17/00 , A61P37/08 , A61P17/06 , A61P31/22 , A61P19/10 , A61P27/02 , A61P3/04 , A61P25/30 , A61P25/32 , A61P9/00 , A61P15/00 , A61P17/02 , A61P23/02 , A61P11/06 , A61P25/22 , A61P11/02 , A61P25/36 , A61K31/4545
CPC分类号： C07D211/08 , C07C311/08 , C07C323/41 , C07C2601/14 , C07D211/14 , C07D213/70 , C07D401/04
摘要： Compounds corresponding to formula I: which act as vanilloid receptor ligands, pharmaceutical composition s containing such compounds, a method for producing the compounds, and the use of such compounds to treat pain and various other conditions.
摘要翻译：对应于式I的化合物：其作为香草素受体配体，含有这些化合物的药物组合物，制备化合物的方法，以及这些化合物用于治疗疼痛和各种其它病症的用途。

42. 发明申请

US20110144347A1 PROCESS FOR THE EPIMERIZATION OF ATOVAQUONE ISOMER, ATOVAQUONE INTERMEDIATES AND MIXTURE THEREOF 审中-公开
标题翻译：异黄酮异构体异构体的方法及其混合物及其混合物
公开(公告)号：US20110144347A1
公开(公告)日：2011-06-16
申请号：US13001156
申请日：2008-06-30
申请人： Fuqiang Zhu , Michel Bekhazi
发明人： Fuqiang Zhu , Michel Bekhazi
IPC分类号： C07D213/70 , C07C46/10
CPC分类号： C07C46/00 , C07C46/10 , C07C2601/14 , C07C2602/10 , C07D213/70 , C07C50/32 , C07C50/24
摘要： Provided is a process for the epimerization of the cis isomer of atovaquone, atovaquone intermediates and isomeric mixtures thereof into their corresponding trans-isomers resulting in higher yield of pure atovaquone.
摘要翻译：提供了将阿托瓦醌，阿托伐醌中间体及其异构体混合物的顺式异构体差向异构化为其相应的反式异构体的方法，导致纯阿托喹醌的较高产率。

43. 发明授权

US07695728B2 2-substituted pyridines, processes for their preparation and their use for controlling harmful fungi 失效
标题翻译： 2-取代的吡啶，其制备方法及其用于控制有害真菌的用途
公开(公告)号：US07695728B2
公开(公告)日：2010-04-13
申请号：US11630569
申请日：2005-06-18
申请人： Joachim Rheinheimer , Frank Schieweck , Thomas Grote , Carsten Blettner , Anja Schwögler , Markus Gewehr , Wassilios Grammenos , Udo Hünger , Bernd Müller , Peter Schäfer , John-Bryan Speakman , Maria Scherer , Siegfried Strathmann , Ulrich Schöfl , Reinhard Stierl
发明人： Joachim Rheinheimer , Frank Schieweck , Thomas Grote , Carsten Blettner , Anja Schwögler , Markus Gewehr , Wassilios Grammenos , Udo Hünger , Bernd Müller , Peter Schäfer , John-Bryan Speakman , Maria Scherer , Siegfried Strathmann , Ulrich Schöfl , Reinhard Stierl
IPC分类号： C07D401/04 , C07D213/61 , C07D417/04 , C07D213/70 , C07D213/86 , C07D213/78 , A01N43/40
CPC分类号： C07D401/04 , A01N43/40 , A01N43/54 , A01N43/56 , A01N43/653 , A01N43/78 , C07D213/61 , C07D213/70 , C07D213/74 , C07D213/78 , C07D213/84 , C07D213/86 , C07D417/04
摘要： The invention relates to 2-substituted pyridines of the formula I in which the index n and the substituents R1 to R4 and L are as defined in the description and in each case one of the two ring members X1, X2 is N, the other is C—H or C-halogen; Y is a group —CH—R1—, —N—R1—, —O— or —S— and is five- or six-membered hetaryl comprising 1 to 3 heteroatoms selected from the group consisting of O, N and S or is phenyl, and to processes for their preparation, intermediates for their preparation, pesticidal compositions and methods for controlling harmful fungi and animal pests using the compounds according to the invention.
摘要翻译：本发明涉及式I中的2-取代吡啶，其中指数n和取代基R 1至R 4和L如说明书中所定义，并且在每种情况下，两个环成员X1，X2中的一个为N，另一个为 C-H或C-卤素; Y是基团-CH-R 1，-N-R 1，-O-或-S-，是包含1至3个选自O，N和S的杂原子的五元或六元杂芳基，或者是苯基，及其制备方法，其制备中间体，杀虫组合物和使用本发明化合物控制有害真菌和动物害虫的方法。

44. 发明申请

US20100041708A1 N-PHENYLARYLSULFONAMIDE COMPOUND, PHARMACEUTICAL COMPOSITION COMPRISING THE COMPOUND AS ACTIVE INGREDIENT, SYNTHETIC INTERMEDIATE FOR THE COMPOUND AND PROCESS FOR IT'S PREPARATION 失效
标题翻译： N-苯基磺酰胺化合物，包含该化合物作为活性成分的药物组合物，该化合物的合成中间体及其制备方法
公开(公告)号：US20100041708A1
公开(公告)日：2010-02-18
申请号：US12603194
申请日：2009-10-21
申请人： Atsushi NAGANAWA , Tetsuji Saito , Kaoru Kobayashi , Takayuki Maruyama , Yoshihiko Nakai , Shinsuke Hashimoto
发明人： Atsushi NAGANAWA , Tetsuji Saito , Kaoru Kobayashi , Takayuki Maruyama , Yoshihiko Nakai , Shinsuke Hashimoto
IPC分类号： A61K31/18 , C07D307/64 , C07D277/36 , C07D213/70 , C07D401/12 , A61K31/341 , A61K31/426 , A61K31/4406 , A61K31/4439 , A61P13/00
CPC分类号： C07D213/70 , C07D277/36 , C07D307/64 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： An N-phenylarylsulfonylamide compound of formula (I) (R1 is COOH etc.; R2 is hydrogen, methyl, etc.; R3 and R4 are a combination of methyl and methyl, etc.; R5 is isopropyl etc.; Ar is thiazolyl, pyridyl, 5-methyl-2-furyl each optionally substituted with methyl; n is zero or 1), a synthetic intermediate for the compound and a process for its preparation. The compound of formula (I) binds to a prostaglandin E2 receptor, especially an EP1 subtype receptor, and antagonizes it. It is less affected by protein binding, so it has a satisfactory in vivo activity. Therefore, it is considered to be useful as an analgesic, an antipyretic agent, an agent for the treatment of pollakiuria (frequent urination) and/or lower urinary tract disease syndrome or an antineoplastic agent.
摘要翻译：式（I）的N-苯基芳基磺酰胺化合物（R1是COOH等; R2是氢，甲基等; R3和R4是甲基和甲基的组合等; R5是异丙基等; Ar是噻唑基，吡啶基，5-甲基-2-呋喃基，各自任选被甲基取代; n为0或1），化合物的合成中间体及其制备方法。式（I）化合物结合前列腺素E2受体，特别是EP1亚型受体，并拮抗它。蛋白质结合的影响较小，因此具有令人满意的体内活性。因此，认为可用作止痛剂，解热剂，治疗尿频（尿频）和/或下尿路疾病综合征或抗肿瘤药物的药剂。

45. 发明申请

US20090227629A1 COMPOUNDS HAVING ACTIVITY AT THE GLYCINE TRANSPORTER GLYT1 AND USES THEREOF 审中-公开
标题翻译：在GLYCINE TRANSPORTER GLYT1中具有活性的化合物及其用途
公开(公告)号：US20090227629A1
公开(公告)日：2009-09-10
申请号：US12158761
申请日：2007-01-08
申请人： Clive Leslie Branch , Jacqueline Anne Macritchie , Howard Marshall , Roderick Alan Porter , Simone Spada
发明人： Clive Leslie Branch , Jacqueline Anne Macritchie , Howard Marshall , Roderick Alan Porter , Simone Spada
IPC分类号： A61K31/4545 , C07D213/70 , A61K31/44 , C07D401/12
CPC分类号： C07D333/38 , C07D213/70 , C07D261/18
摘要： The present invention relates to compounds of formula (I), salts or solvates thereof, their use in the manufacture of medicaments for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof. wherein R1, R2, R3, R4, R5, R6 and n are as defined in the description.
摘要翻译：本发明涉及式（I）化合物，其盐或溶剂合物，它们在制备用于治疗神经和神经精神障碍，特别是精神病，痴呆或注意力缺陷障碍的药物中的用途。本发明还包括制备这些化合物及其药物制剂的方法。其中R1，R2，R3，R4，R5，R6和n如说明书中所定义。

46. 发明申请

US20090171095A1 PRODUCTION METHOD OF HETEROCYCLIC MERCAPTO COMPOUND 有权
标题翻译：杂环化合物的生产方法
公开(公告)号：US20090171095A1
公开(公告)日：2009-07-02
申请号：US12302226
申请日：2007-05-28
申请人： Shinichi Yorozuya , Hidemasa Aoki
发明人： Shinichi Yorozuya , Hidemasa Aoki
IPC分类号： C07D213/70 , C07D307/33 , C07D207/24 , C07D309/30
CPC分类号： C07D307/30 , C07D207/273 , C07D223/10 , C07D333/34
摘要： A method of the invention industrially produces heterocyclic mercapto compounds useful as raw materials or intermediates in the synthesis of medicaments or pesticides, or as permanent wave agent, with a high yield and high productivity using easily available starting materials. A heterocyclic mercapto compound represented by Formula (1) (wherein X represents any structure of —O—, —S—, —NH—, and —NR1—; R1 represents any of an alkyl group, alkoxy group and alkoxyalkyl group each having 1 to 6 carbon atoms; Y represents an oxygen atom, a sulfur atom or —NR2—; R2 represents a hydrogen atom or alkyl group having 1 to 6 carbon atoms; and Z1 represents a divalent organic residue having at least one mercapto group) is produced by reacting a metal sulfide or a metal hydrosulfide with a compound represented by Formula (2) (wherein X and Y are as defined in Formula (1); and Z2 represents a divalent organic residue having at least one halogen group) in the presence of a solvent at a pH of 7.0 to 11.0.
摘要翻译：本发明的工业生产方法是使用容易获得的起始原料工业生产用作合成药物或农药的原料或中间体的杂环巯基化合物，或作为永久挥发剂，以高产率和高生产率。由式（1）表示的杂环巯基化合物（其中X表示-O - ， - S - ， - NH-和-NR 1 - 的任何结构; R 1表示任何烷基，烷氧基和烷氧基烷基， 6个碳原子; Y表示氧原子，硫原子或-NR 2 - ; R 2表示氢原子或碳原子数1〜6的烷基，Z1表示具有至少一个巯基的二价有机残基）通过使金属硫化物或金属氢硫化物与式（2）表示的化合物反应（其中X和Y如式（1）中所定义; Z 2表示具有至少一个卤素基团的二价有机残基） pH 7.0〜11.0的溶剂。

47. 发明申请

US20080255166A1 Dithiocarbamate derivatives and their use as antibacterial agents 审中-公开
标题翻译：二硫代氨基甲酸酯衍生物及其作为抗菌剂的用途
公开(公告)号：US20080255166A1
公开(公告)日：2008-10-16
申请号：US12155604
申请日：2008-06-06
申请人： Ute Mollmann , Vadim Makarov
发明人： Ute Mollmann , Vadim Makarov
IPC分类号： A61K31/505 , C07D239/38 , A61K31/277 , C07C205/56 , C07D213/70 , A61K31/44
CPC分类号： C07D239/56 , C07D213/71 , C07D239/47
摘要： The invention relates to the use of dithiocarbamate derivatives for the therapeutic or prophylactic treatment of infectious diseases in mammals (humans and animals) caused by bacteria, especially diseases like tuberculosis (TB) and lepra caused by mycobacteria and infectious diseases caused by staphylococci. The invention further relates to novel dithiocarbamate derivatives of the formula (I), wherein X is a bivalent residue selected from the group consisting of formulae having excellent antibacterial activities, and to pharmaceutical preparations containing the same.
摘要翻译：本发明涉及二硫代氨基甲酸酯衍生物用于治疗或预防由细菌引起的哺乳动物（人和动物）感染性疾病的治疗，特别是结核分枝杆菌（TB）和由葡萄球菌引起的分枝杆菌和感染性疾病引起的麻风病。本发明还涉及式（I）的新型二硫代氨基甲酸酯衍生物，其中X是选自具有优异抗菌活性的式的二价残基和含有该二价残基的药物制剂。

48. 发明申请

US20080108823A1 Method For Producing Thioether Compound 失效
标题翻译：生产硫醚化合物的方法
公开(公告)号：US20080108823A1
公开(公告)日：2008-05-08
申请号：US11664663
申请日：2005-10-07
申请人： Takahiro Itoh , Toshiaki Mase , Atsushi Akao
发明人： Takahiro Itoh , Toshiaki Mase , Atsushi Akao
IPC分类号： C07D213/70 , C07C327/58 , C07D209/04
CPC分类号： C07D213/32 , B01J31/2457 , B01J2531/824 , C07C319/14 , C07C2601/14 , C07D209/08 , C07D213/70 , C07F17/02 , C07C321/28 , C07C321/30 , C07C323/09 , C07C323/16 , C07C323/20 , C07C323/22 , C07C323/52
摘要： Disclosed is an efficient and widely-applicable method for commercially producing a thioether compound or a thiol compound which is useful as a pharmaceutical compound or a production intermediate of it. Specifically disclosed is a method for producing a thioether compound represented by the general formula [I] below or a salt thereof. This method is characterized in that a compound represented by the following general formula [III]:[III] (wherein X represents a bromine atom, a chlorine atom or a trifluoromethylsulfonyloxy group, and ring A represents an aryl group or a heteroaryl ring group) or a salt thereof is reacted with a thiol compound represented by the following general formula [II]:[II] or a salt thereof in the presence of a palladium compound such as Pd2(dba)3, a base such as i-Pr2NEt and a phosphorus compound represented by the following formula [AA].
摘要翻译：公开了用于商业生产硫醚化合物或硫醇化合物的有效和广泛应用的方法，其可用作药物化合物或其制备中间体。具体公开了由下述通式[I]表示的硫醚化合物或其盐的制备方法。该方法的特征在于由以下通式[III]表示的化合物：[III]（其中X表示溴原子，氯原子或三氟甲基磺酰氧基，环A表示芳基或杂芳基环基）或其盐与下列通式[II]表示的硫醇化合物反应：[II]或其盐在Pd化合物如Pd 2（dba）的存在下进行。碱，例如i-Pr 2 NEt和由下式[AA]表示的磷化合物。

49. 发明授权

US07241782B1 Polymorph V of torasemide 失效
标题翻译：托拉塞米的多晶型V
公开(公告)号：US07241782B1
公开(公告)日：2007-07-10
申请号：US10276881
申请日：2000-09-25
申请人： Darko Filić , Miljenko Dumić , Bo{hacek over (z)}ena Klepić , Aleksandar Danilovski , Marijan Tudja
发明人： Darko Filić , Miljenko Dumić , Bo{hacek over (z)}ena Klepić , Aleksandar Danilovski , Marijan Tudja
IPC分类号： A61K31/44 , C07D213/70
CPC分类号： C07D213/74
摘要： The invention relates to a novel polymorph V of torasemide, to a process for its preparation, to its use as a raw material for the preparation of crystalline modifications I and III of torasemide, to amorphous torasemide modifications and to pharmaceutically acceptable salts of torasemide, to pharmaceutical forms containing the said novel polymorph V of torasemide as the active ingredient as well as to its use.
摘要翻译：本发明涉及托拉塞米的新型多晶型V，其制备方法，其用作制备托拉塞米的晶体修饰I和III的原料，其用于无定形托拉塞米改性和托拉塞米的药学上可接受的盐，含有所述新型多晶型V的托拉塞米作为活性成分的药物形式及其用途。

50. 发明授权

US07166621B2 Pyridyloxyalkanoic acid amide derivatives useful as fungicides 有权
公开(公告)号：US07166621B2
公开(公告)日：2007-01-23
申请号：US10497627
申请日：2002-11-25
申请人： William Guy Whittingham , Kevin Robert Lawson , Paul Anthony Worthington , Charles Adam Russell , Roger Salmon , Leslie Francis May , Mario Jorg , Johannes Paul Pachlatko
发明人： William Guy Whittingham , Kevin Robert Lawson , Paul Anthony Worthington , Charles Adam Russell , Roger Salmon , Leslie Francis May , Mario Jorg , Johannes Paul Pachlatko
IPC分类号： A01N43/00 , C07D213/64 , C07D213/65 , C07D213/70
CPC分类号： C07D213/70 , A01N43/40 , C07D213/65 , C07D213/68 , C07D213/80 , C07D213/82 , C07D213/85
摘要： Fungicidal compounds of the general formula (I): wherein X and Y are independently H, halo, C1-8 alkyl, C3-6 cycloalkyl, C2-8 alkenyl, C2-8 alkynyl, C1-8 alkoxy, C1-8 alkylthio, nitro, amino, mono- or di-(C1-6)alkylamino, mono- or di-(C2-6)alkenylamino, mono- or di-(C2-6)alkynylamino, formylamino, C1-4 alkyl(formyl)amino, C1-4 alkylcarbonylamino, C1-4 alkyl(C1-4 alkylcarbonyl)amino, cyano, formyl, C1-4 alkylcarbonyl, C1-4 alkoxycarbonyl, aminocarbonyl, mono- or di-(C1-4)alkylaminocarbonyl, carboxy, C1-4 alkylcarbonyloxy, aryl(C1-4)alkylcarbonyloxy, C1-4 alkylsulphinyl, C1-4 alkylsulphonyl, C1-4 alkylsulphonyloxy, aryl, heteroaryl, aryloxy, arylthio, heteroaryloxy or heteroarylthio wherein any of the foregoing alkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, groups or moieties are optionally substituted; R1 is phenyl, cyano, C1-4 alkyl, C2-4 alkenyl or C2-4 alkynyl in which the alkyl, alkenyl and alkynyl groups are optionally substituted on their terminal carbon atom with one, two or three halogen atoms, with a cyano group, with a C1-4 alkylcarbonyl group, with a C1-4 alkoxycarbonyl group or with a hydroxy group, or R1 is alkoxyalkyl, alkylthioalkyl, alkylsulphinylalkyl or alkylsulphonylalkyl in which the total number of carbon atoms is 2 or 3; R2 is H, C1-4 alkyl, C1-4 alkoxymethyl or benzyloxymethyl in which the phenyl ring of the benzyl moiety is optionally substituted with C1-4 alkoxy; R3 and R4 are independently H, C1-3 alkyl, C2-3 alkenyl or C2-3 alkynyl provided that both are not H and that when both are other than H their combined total of carbon atoms does not exceed 4, or R3 and R4 join with the carbon atom to which they are attached to form a 3 or 4 membered carbocyclic ring optionally containing one O, S or N atom and optionally substituted with halo or C1-4 alkyl; and R5 is halo, C1-4 alkyl or C3-4 cycloalkyl in which the alkyl or cycloalkyl group is optionally substituted with halo, hydroxy, C1-6 alkoxy, C1-6 alkylthio, cyano, C1-4 alkylcarbonyloxy, aminocarbonyloxy, mono- or di(C1-4)alkylaminocarbonyloxy, or tri(C1-4)alkylsilyloxy. The compounds and compositions containing them are especially useful for combating fungal infections of plants.

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