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51. 发明授权

US06855512B2 Methods for identifying inhibitors of cytochrome P450RAI 失效
标题翻译：鉴定细胞色素P450RAI抑制剂的方法
公开(公告)号：US06855512B2
公开(公告)日：2005-02-15
申请号：US10212533
申请日：2002-08-05
申请人： Jayasree Vasudevan , Alan T. Johnson , Liming Wang , Dehua Huang , Roshantha A. Chandraratna
发明人： Jayasree Vasudevan , Alan T. Johnson , Liming Wang , Dehua Huang , Roshantha A. Chandraratna
IPC分类号： C07D233/60 , A61K31/167 , A61K31/192 , A61K31/195 , A61K31/196 , A61K31/216 , A61K31/232 , A61K31/24 , A61K31/353 , A61K31/381 , A61K31/382 , A61K31/4174 , A61K31/47 , A61K31/472 , A61K31/4747 , A61P1/04 , A61P3/02 , A61P3/06 , A61P3/10 , A61P5/06 , A61P5/10 , A61P5/38 , A61P7/00 , A61P9/00 , A61P9/10 , A61P11/00 , A61P15/00 , A61P17/00 , A61P17/02 , A61P17/06 , A61P17/10 , A61P17/12 , A61P17/14 , A61P17/16 , A61P25/16 , A61P25/28 , A61P27/02 , A61P29/00 , A61P31/12 , A61P31/20 , A61P35/00 , A61P37/02 , A61P37/04 , A61P37/06 , A61P39/00 , A61P43/00 , C07C59/64 , C07C59/72 , C07C59/86 , C07C65/28 , C07C65/38 , C07C69/757 , C07C229/34 , C07C229/38 , C07C229/46 , C07C229/50 , C07C403/20 , C07D215/14 , C07D217/04 , C07D221/20 , C07D311/58 , C07D311/70 , C07D311/96 , C07D333/40 , C07D335/04 , C07D335/06 , C07D409/06 , C07D521/00 , C12Q1/26
CPC分类号： C07D221/20 , A61K31/192 , A61K31/195 , A61K31/353 , A61K31/382 , A61K31/47 , A61K31/472 , A61K31/4747 , C07C59/72 , C07C65/28 , C07D215/14 , C07D217/04 , C07D231/12 , C07D233/56 , C07D249/08 , C07D311/70 , C07D311/96 , C07D333/40 , C07D335/04 , C07D335/06 , C07D409/06
摘要： A method of identifying a compound which is an inhibitor of the enzyme cytochrome P450RAI is performed by selecting a compound that has retinoid activity in an art recognized assay and includes a benzoic acid, benzoic acid ester, naphthoic acid ester or heteroaryl carboxylic acid or ester moiety, with a partial structure of —A(R2)—(CH2)n—COOR8 where n is 0 and the remaining variables are as described in the specification and claims. Thereafter, a compound having the cytochrome P450RAI inhibitory activity is identified and selected where the compound has the —A(R2)—(CH2)2—COOR8 partial structure wherein the variable n is 1 or 2.
摘要翻译：鉴定作为细胞色素P450RAI酶的抑制剂的化合物的方法通过在本领域公认的测定中选择具有类视黄醇活性的化合物进行，并且包括苯甲酸，苯甲酸酯，萘甲酸酯或杂芳基羧酸或酯部分，其具有-A（R2） - （CH2）n-COOR8的部分结构，其中n为0，其余变量如说明书和权利要求中所述。此后，鉴定并选择具有细胞色素P450RAI抑制活性的化合物，其中化合物具有其中n为1或2的-A（R 2） - （CH 2）2 -COOR 8部分结构。

52. 发明授权

US06852229B2 Method for preparing high-purity ionic liquids 失效
标题翻译：制备高纯度离子液体的方法
公开(公告)号：US06852229B2
公开(公告)日：2005-02-08
申请号：US10277420
申请日：2002-10-22
申请人： Christian P. Mehnert , Nicholas C. Dispenziere , Raymond A. Cook
发明人： Christian P. Mehnert , Nicholas C. Dispenziere , Raymond A. Cook
IPC分类号： B01J31/02 , C07C45/50 , C07D213/20 , C07D521/00 , B01D11/04
CPC分类号： C07D213/20 , B01J31/0234 , C07D231/12 , C07D233/56 , C07D249/08
摘要： A method for preparing a high-purity ionic liquid having a pH value of 7 and an elemental analysis deviation of less than 0.5 wt % between a calculated elemental analysis and a found elemental analysis for each of carbon, hydrogen and nitrogen, wherein the method comprises forming a monophasic or biphasic mixture of an ionic liquid and an inert liquid. When the monophasic mixture is formed, it is filtered to yield a filtrate from which the high-purity ionic liquid is recovered. When the biphasic mixtures is formed, it is separated into an aqueous phase and ionic liquid phase, whereby the ionic liquid phase is filtered to yield a filtrate from which the high-purity ionic liquid is recovered. Furthermore, the present purification procedure can be used for the clean-up of a contaminated ionic liquid by extracting it into a polar extractant to form an extract containing the ionic liquid. Water traces are removed from the extract. Then, the extract is filtered and the high-purity ionic liquid is recovered from the filtered extract.
摘要翻译：在计算的元素分析和针对碳，氢和氮各自的元素分析中，制备pH值为7并且元素分析偏差小于0.5重量％的高纯度离子液体的方法，其中所述方法包括形成离子液体和惰性液体的单相或双相混合物。当形成单相混合物时，将其过滤以产生从其中回收高纯度离子液体的滤液。当形成双相混合物时，将其分离成水相和离子液相，由此过滤离子液相以产生从其中回收高纯度离子液体的滤液。此外，本纯化方法可用于通过将污染的离子液体提取到极性萃取剂中以形成含有离子液体的提取物来清理污染的离子液体。从提取物中除去水迹。然后，将提取物过滤并从过滤的提取物中回收高纯度离子液体。

53. 发明申请

US20050027121A1 Aroyl-piperazine derivatives, their preparation and their use as tachykinin antagonists 失效
公开(公告)号：US20050027121A1
公开(公告)日：2005-02-03
申请号：US10720021
申请日：2003-11-24
申请人： Hiroshi Miyake , Kazuhiko Take , Shinji Shigenaga , Hidenori Azami , Hiroshi Sasaki , Yoshiteru Eikyu , Kazuo Nakai , Junya Ishida , Takashi Manabe , Nobukiyo Konishi , Tadashi Terasaka
发明人： Hiroshi Miyake , Kazuhiko Take , Shinji Shigenaga , Hidenori Azami , Hiroshi Sasaki , Yoshiteru Eikyu , Kazuo Nakai , Junya Ishida , Takashi Manabe , Nobukiyo Konishi , Tadashi Terasaka
IPC分类号： A61K31/496 , A61K31/5377 , A61K31/541 , A61K31/55 , A61P1/00 , A61P9/00 , A61P11/00 , A61P11/06 , A61P25/00 , A61P25/04 , A61P27/02 , A61P29/00 , A61P43/00 , C07D241/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/06 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/08 , C07D417/14 , C07D521/00 , C07D413/02 , C07
CPC分类号： C07D231/12 , C07D233/56 , C07D241/04 , C07D249/08 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/06 , C07D413/06 , C07D417/14
摘要： This invention relates to piperazine derivatives of the formula: wherein each symbol is as defined in the description, and its pharmaceutically acceptable salt, to processes for preparation thereof, to pharmaceutical composition comprising the same, and to a use of the same for treating or preventing Tachykinin-mediated diseases in human being or animals.

54. 发明授权

US06846829B2 N-heterocyclic derivatives as NOS inhibitors 失效
公开(公告)号：US06846829B2
公开(公告)日：2005-01-25
申请号：US10121758
申请日：2002-04-12
申请人： Damian O. Arnaiz , John J. Baldwin , David D. Davey , James J. Devlin , Roland Ellwood Dolle, III , Shawn David Erickson , Kirk McMillan , Michael M. Morrissey , Michael H. J. Ohlmeyer , Gonghua Pan , Vidyadhar Madhav Paradkar , John Parkinson , Gary B. Phillips , Bin Ye , Zuchun Zhao
发明人： Damian O. Arnaiz , John J. Baldwin , David D. Davey , James J. Devlin , Roland Ellwood Dolle, III , Shawn David Erickson , Kirk McMillan , Michael M. Morrissey , Michael H. J. Ohlmeyer , Gonghua Pan , Vidyadhar Madhav Paradkar , John Parkinson , Gary B. Phillips , Bin Ye , Zuchun Zhao
IPC分类号： C07D403/14 , A61K31/506 , A61K31/5377 , A61K31/547 , A61P1/04 , A61P3/10 , A61P9/00 , A61P9/02 , A61P9/04 , A61P9/08 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/02 , A61P17/06 , A61P19/02 , A61P21/00 , A61P25/00 , A61P25/16 , A61P25/28 , A61P29/00 , A61P35/00 , A61P37/00 , A61P37/02 , A61P37/06 , A61P43/00 , C07D213/00 , C07D233/00 , C07D239/00 , C07D241/02 , C07D265/00 , C07D279/00 , C07D317/44 , C07D319/00 , C07D333/02 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： N-Heterocyclic derivatives of the formula (I): are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.

55. 发明申请

US20050009815A1 4-Aminoquinoline compounds 审中-公开
标题翻译： 4-氨基喹啉化合物
公开(公告)号：US20050009815A1
公开(公告)日：2005-01-13
申请号：US10496614
申请日：2002-11-22
申请人： Robert DeVita , Lehua Chang , MyLe Hoang , JinLong Jiang , Peter Lin , Andreas Sailer
发明人： Robert DeVita , Lehua Chang , MyLe Hoang , JinLong Jiang , Peter Lin , Andreas Sailer
IPC分类号： A61K31/4706 , A61K31/4709 , A61K31/473 , A61K31/496 , A61K31/519 , A61P1/16 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P13/02 , A61P13/12 , A61P15/00 , A61P19/02 , A61P25/02 , A61P25/08 , A61P25/14 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/28 , A61P25/30 , A61P31/18 , A61P35/00 , A61P43/00 , C07D215/42 , C07D215/48 , C07D219/10 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D413/04 , C07D487/04 , C07D521/00 , C07F7/22 , A61K31/541 , A61K31/5377
CPC分类号： C07D231/12 , C07D215/42 , C07D219/10 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D413/04 , C07D487/04 , C07F7/2208
摘要： The present invention is concerned with compounds of the general Formula I: and pharmaceutically acceptable salts thereof, which are useful as melanin concentrating hormone receptor antagonists, particularly MCH-1R antagonists. As such, compounds of the present invention are useful for the treatment or prevention of obesity or eating disorders associated with excessive food intake and complications thereof, osteoarthritis, certain cancers, AIDS wasting, cachexia, frailty (particularly in elderly), mental disorders stress, cognitive disorders, sexual function, reproductive function, kidney function, locomotor disorders, attention deficit disorder (ADD), substance abuse disorders and dyskinesias, Huntington's disease, epilepsy, memory function, and spinal muscular atrophy. Compounds of formula I may therefore be used in the treatment of these conditions, and in the manufacture of a medicament useful in treating these conditions. Pharmaceutical formulations comprising one of the compounds of formula (I) as an active ingredient are disclosed, as are processes for preparing these compounds.
摘要翻译：本发明涉及通式I的化合物及其药学上可接受的盐，其可用作黑色素浓缩激素受体拮抗剂，特别是MCH-1R拮抗剂。因此，本发明的化合物可用于治疗或预防与食物过量摄取及其并发症，骨关节炎，某些癌症，艾滋病消瘦，恶病质，虚弱（特别是老年人）相关的肥胖或进食障碍，精神障碍压力，认知障碍，性功能，生殖功能，肾功能，运动障碍，注意力缺陷障碍（ADD），药物滥用障碍和运动障碍，亨廷顿病，癫痫，记忆功能和脊髓性肌肉萎缩。因此，式I化合物可用于治疗这些病症，以及制备用于治疗这些病症的药物。作为制备这些化合物的方法，公开了包含式（I）化合物之一作为活性成分的药物制剂。

56. 发明授权

US06841674B2 N-heterocyclic derivatives as NOS inhibitors 失效
标题翻译： N-杂环衍生物作为NOS抑制剂
公开(公告)号：US06841674B2
公开(公告)日：2005-01-11
申请号：US10122072
申请日：2002-04-12
申请人： Damian O. Arnaiz , John J. Baldwin , David D. Davey , James J. Devlin , Roland Ellwood Dolle, III , Shawn David Erickson , Kirk McMillan , Michael M. Morrissey , Michael H. J. Ohlmeyer , Gonghua Pan , Vidyadhar Madhav Paradkar , John Parkinson , Gary B. Phillips , Bin Ye , Zuchun Zhao
发明人： Damian O. Arnaiz , John J. Baldwin , David D. Davey , James J. Devlin , Roland Ellwood Dolle, III , Shawn David Erickson , Kirk McMillan , Michael M. Morrissey , Michael H. J. Ohlmeyer , Gonghua Pan , Vidyadhar Madhav Paradkar , John Parkinson , Gary B. Phillips , Bin Ye , Zuchun Zhao
IPC分类号： C07D403/14 , A61K31/506 , A61K31/5377 , A61K31/547 , A61P1/04 , A61P3/10 , A61P9/00 , A61P9/02 , A61P9/04 , A61P9/08 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/02 , A61P17/06 , A61P19/02 , A61P21/00 , A61P25/00 , A61P25/16 , A61P25/28 , A61P29/00 , A61P35/00 , A61P37/00 , A61P37/02 , A61P37/06 , A61P43/00 , C07D213/00 , C07D233/00 , C07D239/00 , C07D241/02 , C07D265/00 , C07D279/00 , C07D317/44 , C07D319/00 , C07D333/02 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： N-Heterocyclic derivatives of the formula (I): are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.
摘要翻译：式（I）的N-杂环衍生物：本文描述以及其它N-杂环作为一氧化氮合酶的抑制剂。含有这些化合物的药物组合物，使用这些化合物作为一氧化氮合酶抑制剂的方法以及合成这些化合物的方法也在本文中描述。

57. 发明授权

US06838414B2 Substituted aryl sulphonyl(thio)ureas used as herbicides 失效
标题翻译：用作除草剂的取代的芳基磺酰基（硫代）脲
公开(公告)号：US06838414B2
公开(公告)日：2005-01-04
申请号：US10195979
申请日：2002-07-16
申请人： Ernst Rudolf F. Gesing , Rolf Kirsten , Joachim Kluth , Klaus-Helmut Müller , Mark Wilhelm Drewes , Johannes Rudolf Jansen , Ulrich Philipp , Hans-Jochem Riebel , Otto Schallner , Markus Dollinger , Hans-Joachim Santel
发明人： Ernst Rudolf F. Gesing , Rolf Kirsten , Joachim Kluth , Klaus-Helmut Müller , Mark Wilhelm Drewes , Johannes Rudolf Jansen , Ulrich Philipp , Hans-Jochem Riebel , Otto Schallner , Markus Dollinger , Hans-Joachim Santel
IPC分类号： A01N47/36 , C07D239/42 , C07D239/46 , C07D239/52 , C07D251/16 , C07D251/46 , C07D521/00 , A01N43/54 , C07D239/697
CPC分类号： C07D239/42 , A01N47/36 , C07D239/47 , C07D239/52 , C07D251/16 , C07D251/46 , C07D521/00
摘要： The invention relates to novel substituted arylsulphonyl(thio)ureas in which A represents nitrogen or a CH grouping, Q represents oxygen or sulphur, R1 represents hydrogen, halogen or respectively optionally substituted alkyl, alkoxy, alkylthio, alkylamino, dialkylamino, cycloalkyl, cycloalkyloxy or heterocyclyloxy, R2 represents hydrogen, halogen or respectively optionally substituted alkyl, alkoxy, alkylthio, alkylamino, dialkylamino, cycloalkyl, cycloalkyloxy or heterocyclyloxy, R3 represents hydrogen or optionally substituted alkyl, R4 represents respectively optionally substituted alkyl, alkoxy, alkenyl, alkinyl, alkenyloxy, alkinyloxy, cycloalkyl, cycloalkyloxy or cycloalkylalkyl, and R5 represents hydrogen, formyl or respectively optionally substituted alkyl, alkylcarbonyl, alkoxycarbonyl, alkylsulphonyl, alkenyl, alkinyl, cycloalkyl, cycloalkylcarbonyl, cycloalkylsulphonyl or heterocyclyl, and to salts of compounds of the formula (I), except for the compound N-(4,6-dimethyl-pyrimidin-2-yl)-N′-[2-(1,1,2,2-tetrafluoro-ethoxy)-6-methyl-phenylsulphonyl]-urea, to processes for preparing the novel compounds and to their use as herbicides.
摘要翻译：本发明涉及A代表氮或CH基的新型取代芳基磺酰基（硫代）脲脲，Q表示氧或硫，R 1表示氢，卤素或分别任意取代的烷基，烷氧基，烷硫基，烷基氨基，二烷基氨基，环烷基，环烷氧基或杂环氧基，R 2表示氢，卤素或分别任选取代的烷基，烷氧基，烷硫基，烷基氨基，二烷基氨基，环烷基，环烷氧基或杂环氧基，R 3表示氢或任选取代的烷基，烷基，烷氧基，烯基，炔基，烯氧基，烷氧基，环烷基，环烷基氧基或环烷基烷基，R 5表示氢，甲酰基或分别任选取代的烷基，烷基羰基，烷氧基羰基，烷基磺酰基，烯基，炔基，环烷基，环烷基羰基，环烷基磺酰基或杂环基，和式（I）化合物的盐，除了化合物N-（4,6-二甲基 - 吡啶-2-基）亚氨基-2-基）-N' - [2-（1,1,2,2-四氟 - 乙氧基）-6-甲基 - 苯基磺酰基] - 脲，用于制备新化合物及其作为除草剂的用途。

58. 发明授权

US6159941A Use of somatostatin agonists and antagonists for treating diseases related to the eye 失效
标题翻译：生长抑素激动剂和拮抗剂用于治疗与眼睛有关的疾病
公开(公告)号：US6159941A
公开(公告)日：2000-12-12
申请号：US97907
申请日：1998-06-16
申请人： Michael Ankersen , Carsten Enggaard Stidsen , Michael Albert Crider
发明人： Michael Ankersen , Carsten Enggaard Stidsen , Michael Albert Crider
IPC分类号： A61K31/4439 , A61K31/4709 , A61K31/506 , A61K31/5377 , C07D213/74 , C07D401/12 , C07D521/00 , A61K38/00
CPC分类号： C07D213/74 , A61K31/4439 , A61K31/4709 , A61K31/501 , A61K31/506 , A61K31/5377 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , Y10S514/913
摘要： The invention relates to the use of a somatostatin receptor ligand of nonpeptide origin, e.g. of the general formula Ia or Ib ##STR1## or a pharmaceutically acceptable salt thereof, which has high and/or selective affinity to the somatostatin receptor protein designated SSTR4 and, for the preparation of a medicament for the treatment of a disease associated with an adverse condition in the retina and/or iris-ciliary body of a mammal. Such conditions are high intraocular pressure (IOP) and/or deep ocular infections. The diseases which may be treated are e.g. glaucoma, stromal keratitis, iritis, retinitis, cataract and conjunctivitis.
摘要翻译：本发明涉及使用非肽来源的生长抑素受体配体，例如，具有对命名为SSTR4的生长抑素受体蛋白具有高和/或选择性亲和力的通式Ia或Ib或其药学上可接受的盐，并且用于制备用于治疗与不良状况相关的疾病的药物视网膜和/或虹膜睫状体。这种情况是高眼内压（IOP）和/或深部眼部感染。可以治疗的疾病是例如青光眼，基质角膜炎，虹膜炎，视网膜炎，白内障和结膜炎。

59. 发明授权

US6150385A 1,3,4-thiadiazoles useful for the treatment of CMV infections 失效
标题翻译：可用于治疗CMV感染的1,3,4-噻二唑
公开(公告)号：US6150385A
公开(公告)日：2000-11-21
申请号：US270429
申请日：1999-03-16
申请人： Suvit Thaisrivongs , Steven Ronald Turner
发明人： Suvit Thaisrivongs , Steven Ronald Turner
IPC分类号： A61K31/433 , A61K31/496 , A61K31/5377 , A61P31/12 , A61P31/22 , C07D285/12 , C07D285/135 , C07D417/12 , C07D417/14 , C07D521/00
CPC分类号： C07D285/135 , C07D231/12 , C07D233/56 , C07D249/08 , C07D417/12 , C07D417/14
摘要： The present invention presents novel 1,3,4-thiadiazole derivatives of formula I ##STR1## which have useful antiviral activity against herpes virus, cytomegalovirus (CMV).
摘要翻译：本发明提出了具有抗疱疹病毒，巨细胞病毒（CMV）的有效抗病毒活性的式I的新的1,3,4-噻二唑衍生物。

60. 发明授权

US6136826A Peripheral vasodilating agent containing piperidine derivative as active ingredient 失效
标题翻译：含有哌啶衍生物作为活性成分的外周血管舒张剂
公开(公告)号：US6136826A
公开(公告)日：2000-10-24
申请号：US066930
申请日：1998-04-28
申请人： Takafumi Fujioka , Shuji Teramoto , Michinori Tanaka , Hiroshi Shimizu , Fujio Tabusa , Michiaki Tominaga
发明人： Takafumi Fujioka , Shuji Teramoto , Michinori Tanaka , Hiroshi Shimizu , Fujio Tabusa , Michiaki Tominaga
IPC分类号： C07D211/58 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/10 , C07D417/06 , C07D521/00 , A61K31/445
CPC分类号： C07D231/12 , C07D211/58 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/10 , C07D417/06
摘要： The present invention relates to novel peripheral vasodilating agents characterized by each containing as an active ingredient, a piperidine derivative or pharmaceutically acceptable salt thereof having excellent peripheral vasodilating activity.Said piperidine derivative or pharmaceutically acceptable salt thereof is represented by the general formula (1): ##STR1## (wherein R, R.sup.1 and R.sup.2 are the same as defined above.
摘要翻译：本发明涉及新颖的外周血管扩张剂，其特征在于每种含有作为活性成分的哌啶衍生物或其药学上可接受的盐具有优异的外周血管扩张活性。所述哌啶衍生物或其药学上可接受的盐由通式（1）表示：（其中R，R 1和R 2与上述定义相同。

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