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41. 发明授权

US07351825B2 Cyclopropane compounds and pharmaceutical use thereof 失效
标题翻译：环丙烷化合物及其药物用途
公开(公告)号：US07351825B2
公开(公告)日：2008-04-01
申请号：US11011773
申请日：2004-12-15
申请人： Takashi Inaba , Julia Haas , Makoto Shiozaki , Nicole M. Littmann , Katsutaka Yasue , Steven W. Andrews , Atushi Sakai , Andrew M. Fryer , Takafumi Matsuo , Ellen R. Laird , Akira Suma , Yuichi Shinozaki , Yoshikazu Hori , Hiroto Imai , Tamotsu Negoro
发明人： Takashi Inaba , Julia Haas , Makoto Shiozaki , Nicole M. Littmann , Katsutaka Yasue , Steven W. Andrews , Atushi Sakai , Andrew M. Fryer , Takafumi Matsuo , Ellen R. Laird , Akira Suma , Yuichi Shinozaki , Yoshikazu Hori , Hiroto Imai , Tamotsu Negoro
IPC分类号： C07D265/00 , C07D295/00 , C07D237/00 , C07D409/00 , C07D411/00 , C07D217/00 , C07D211/00 , C07D213/00 , C07D271/00 , C07D413/00 , C07D498/00 , C07D277/00 , C07D257/00 , C07D233/00 , C07D231/00 , C07D207/00 , C07D333/00 , C07D307/00 , C07D303/00 , C07D309/00 , C07D311/00
CPC分类号： C07C311/29 , C07C311/13 , C07C311/20 , C07C311/22 , C07C311/46 , C07C2601/02 , C07C2601/14 , C07C2603/08 , C07C2603/18 , C07C2603/30 , C07D205/04 , C07D207/48 , C07D209/44 , C07D211/58 , C07D211/96 , C07D213/18 , C07D213/65 , C07D213/71 , C07D213/74 , C07D213/81 , C07D213/82 , C07D217/08 , C07D231/12 , C07D233/64 , C07D237/12 , C07D239/22 , C07D243/08 , C07D257/04 , C07D261/08 , C07D271/06 , C07D271/107 , C07D277/26 , C07D277/36 , C07D277/82 , C07D295/26 , C07D307/79 , C07D307/91 , C07D333/18 , C07D333/34 , C07D333/36 , C07D333/38 , C07D333/62 , C07D401/04 , C07D409/04 , C07D409/12 , C07D413/04 , C07D417/04 , C07D417/12 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1—(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.; or a prodrug thereof or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供具有聚集蛋白聚糖蛋白聚糖酶抑制活性和MMP-13抑制活性的化合物，可用作骨关节炎，类风湿性关节炎等的治疗剂，更具体而言，可以使用式（1）的环丙烷化合物：其中R 1 是 - （CH 2）2 -X-（CH 2）n - SUP> 1等，其中m和n相同或不同，并且各自为0至6，X为单键等，而A 1为取代的C _{3-14个烃环基等; R 2和R 3相同或不同，并且各自为氢原子， - （CH 2）2 N 其中p和q为 - （CH 2）2 - - - - CH 2 - 相同或不同，并且各自为0至6，X 1为单键等，而A 2为任选取代的C 3-14烷基，烃环等; R 4是-CO 2 R 9等，其中R 9是氢原子等。 ; 和R 20和R 21相同或不同，各自为氢原子， - （CH 2 CH 2）m 12 其中m12和m12（其中m12和m12）相同或不同，各自为0至6，X 12为单键等，R 30为氢原子等; 或其前药或其药学上可接受的盐。}

42. 发明申请

US20080045470A1 Ceramides and Apoptosis-Signaling Ligand 有权
标题翻译：神经酰胺和细胞凋亡信号配体
公开(公告)号：US20080045470A1
公开(公告)日：2008-02-21
申请号：US11666519
申请日：2005-10-31
申请人： Alicja Bielawska , Yusuf Hannun , James Norris , Zdzislaw Szulc , Jian-yun Dong , Jacek Bielawski , David Schwartz , David Holman , Ahmed El-Zawahry , John McKillop
发明人： Alicja Bielawska , Yusuf Hannun , James Norris , Zdzislaw Szulc , Jian-yun Dong , Jacek Bielawski , David Schwartz , David Holman , Ahmed El-Zawahry , John McKillop
IPC分类号： A61K31/40 , A61K31/415 , A61K31/44 , A61K31/445 , A61K31/497 , A61K31/535 , A61K31/70 , A61P43/00 , C07D207/00 , C07D211/00 , C07D233/00 , C07D241/04 , C07D265/30
CPC分类号： C07D213/56 , C07C215/18 , C07C215/28 , C07C275/24
摘要： The invention provides the compounds of formula ( ): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, A, X, Y, a, b and n are as defined herein. Also disclosed are methods for making the compounds of formula (I) and their use in treating or preventing diseases associated with cell overproliferation and dysfunctional sphingolipid signal transduction. The invention also encompasses the use of the compounds in combination with an apoptosis-signaling ligand, such as Fas ligand. Preferably, the Fas ligand is administered in the form of a gene therapy agent.
摘要翻译：本发明提供式（I）化合物及其药学上可接受的盐，其中R 1，R 2，R 3，R 3 > 4，A，X，Y，a，b和n如本文所定义。还公开了制备式（I）化合物及其用于治疗或预防与细胞过度增生和功能失调的鞘脂信号转导相关的疾病的方法。本发明还包括与凋亡信号传导配体如Fas配体组合的化合物的用途。优选地，Fas配体以基因治疗剂的形式施用。

43. 发明申请

US20080015195A1 Novel Heteroaromatic Inhibitors of Fructose-1,6-Bisphosphatase 审中-公开
标题翻译：果糖-1,6-二磷酸酶的新型杂芳族抑制剂
公开(公告)号：US20080015195A1
公开(公告)日：2008-01-17
申请号：US11842035
申请日：2007-08-20
申请人： Qun Dang , Srinivas Kasibhatla , K. Reddy , Mark Erion , M. Reddy , Atul Agarwal
发明人： Qun Dang , Srinivas Kasibhatla , K. Reddy , Mark Erion , M. Reddy , Atul Agarwal
IPC分类号： A61K31/53 , A61K31/33 , A61K31/341 , A61K31/41 , A61K31/4155 , A61K31/4164 , A61K31/421 , A61P3/10 , C07D213/02 , C07D277/62 , C07D277/02 , C07D263/02 , C07D257/04 , C07D253/02 , C07D241/00 , C07D239/00 , C07D233/00 , C07D231/00 , C07D307/02 , C07D293/06 , C07D285/12 , A61P9/00 , A61K31/426 , A61K31/428 , A61K31/433 , A61K31/44 , A61K31/4965 , A61K31/505
CPC分类号： C07F9/4006 , C07F9/5728 , C07F9/58 , C07F9/650952 , C07F9/6512 , C07F9/653 , C07F9/65324 , C07F9/6539 , C07F9/65395 , C07F9/6541 , C07F9/65515 , C07F9/65517 , C07F9/655345 , C07F9/65583 , C07F9/65586 , C07F9/657181 , C07F9/6578 , C07F9/65846
摘要： Novel FBPase inhibitors of the formula I and X are useful in the treatment of diabetes and other conditions associated with elevated blood glucose.
摘要翻译：式I和X的新型FBPase抑制剂可用于治疗与血糖升高相关的糖尿病和其它病症。

44. 发明授权

US07304083B2 2-iminoimidazole derivatives (2) 失效
标题翻译： 2-亚氨基咪唑衍生物（2）
公开(公告)号：US07304083B2
公开(公告)日：2007-12-04
申请号：US10475118
申请日：2002-04-19
申请人： Shuichi Suzuki , Makoto Kotake , Mitsuaki Miyamoto , Tetsuya Kawahara , Akiharu Kajiwara , Ieharu Hishinuma , Kazuo Okano , Syuhei Miyazawa , Richard Clark , Fumihiro Ozaki , Nobuaki Sato , Masanobu Shinoda , Atsushi Kamada , Itaru Tsukada , Fumiyoshi Matsuura , Yoshimitsu Naoe , Taro Terauchi , Yoshiaki Oohashi , Osamu Ito , Hiroshi Tanaka , Takashi Musha , Motoji Kogushi , Tsutomu Kawata , Toshiyuki Matsuoka , Hiroko Kobayashi , Ken-ichi Chiba , Akifumi Kimura , Naoto Ono
发明人： Shuichi Suzuki , Makoto Kotake , Mitsuaki Miyamoto , Tetsuya Kawahara , Akiharu Kajiwara , Ieharu Hishinuma , Kazuo Okano , Syuhei Miyazawa , Richard Clark , Fumihiro Ozaki , Nobuaki Sato , Masanobu Shinoda , Atsushi Kamada , Itaru Tsukada , Fumiyoshi Matsuura , Yoshimitsu Naoe , Taro Terauchi , Yoshiaki Oohashi , Osamu Ito , Hiroshi Tanaka , Takashi Musha , Motoji Kogushi , Tsutomu Kawata , Toshiyuki Matsuoka , Hiroko Kobayashi , Ken-ichi Chiba , Akifumi Kimura , Naoto Ono
IPC分类号： A61K31/415 , C07D233/00 , C07D233/44 , C07D233/66
CPC分类号： C07D209/44
摘要： A 2-iminoimidazole derivative represented by the formula: {wherein R1, R2 and R3 represent hydrogen, optionally substituted C1-6 alkyl, etc.; R6 represents hydrogen, C1-6 alkyl, C1-6 alkyloxycarbonyl, etc.; Y1 represents a single bond, —CH2—, etc.; Y2 represents a single bond, —CO—, etc.; and Ar represents hydrogen, a group represented by the formula: [wherein R10–R14 represent hydrogen, C1-6 alkyl, hydroxyl, C1-6 alkoxy, etc., and R11 and R12 or R12 and R13 may bond together to form a 5- to 8-membered heterocycle], etc.}or salt thereof.
摘要翻译：由下式表示的2-亚氨基咪唑衍生物：

45. 发明授权

US07253289B2 One-step process for the preparation of halide-free hydrophobic salts 失效
公开(公告)号：US07253289B2
公开(公告)日：2007-08-07
申请号：US10250801
申请日：2002-01-22
申请人： Rex Xiaofeng Ren , Victor R. Koch
发明人： Rex Xiaofeng Ren , Victor R. Koch
IPC分类号： C07D233/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07F9/28
摘要： This invention describes a one pot, single-step process for the preparation of halide-free hydrophobic salts comprising polyalkylated imidazolium cations and various anions in accordance with the following structure, where R1 and R3 represent the either the same or different alkyl groups, and R2, R4, and R5 represent either hydrogen atoms, or the same or different alkyl group substituents; X represents a polyatomic anion that is the conjugate base of an acid. By simply mixing aqueous formaldehyde with an alkyl amine such as methylanune, ethylamine, n-propyl oriso-propylamine, or n-butyl-, iso-butyl, or t-butylamine, or by mixing aqueous formaldehyde with two alkyl amines (preferably one being methylamine, ethylamine, n-propyl- or iso-propylamine, or n-butyl-, isobutyl, or t-butylamine) and another being n-propyl- or isopropylaine, or n-butyl-, isbutyl, or t-butylamine), an acid (such as hexafluorophosphoric acid, trifluoroacetic acid, pentafluoropropionic, heptafluorobutyric acid, or the free acid of a bis(perfluoroalkylsulfonyprnide or tris(perfluoroalkylsulfonyl)methide as the source of the anion) and aqueous glyoxal solution, the hydrophobic ionic salts or mixtures thereof thus formed may be conveniently separated directly from the aqueous byproduct layer. Like the single cation hydrophobic salts, these mixed hydrophobic ionic liquids are non-flammable and manifest no detectable vapor pressure up to their decomposition temperature of greater than 300° C. We have also discovered that, surprisingly, ternary mixtures of dialkylated ionic liquids manifest higher ionic conductivities than a single ionic liquid of the mixture alone. This property benefits electrochemical power source applications such as batteries and capacitors. Furthermore, we have discovered that ternary mixtures of dialkylated ionic liquids absorb microwave radiation more efficiently than a single ionic liquid of the mixture alone. This property benefits microwave-induced synthetic reactions. Such physical and chemical properties make it possible to employ inexpensive mixtures of polyalkylated imidazolium cations in an advantageous manner as thermal transfer fluids, high temperature lubricants, and plasticizers, and as solvents in the areas of electrochemistry, synthetic chemistry, catalysis, and separations chemistry.

46. 发明授权

US07041693B2 Hydantoin derivatives as inhibitors of matrix metalloproteinases and/or TNF-α converting enzyme (TACE) 有权
标题翻译：乙内酰脲衍生物作为基质金属蛋白酶和/或TNF-α转化酶（TACE）的抑制剂
公开(公告)号：US07041693B2
公开(公告)日：2006-05-09
申请号：US10677988
申请日：2003-10-02
申请人： James Sheppeck
发明人： James Sheppeck
IPC分类号： A61K31/415 , C07D233/00 , C07D453/02
CPC分类号： C07D405/14 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D417/12 , C07D417/14
摘要： The present application describes novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein L, Z0, R1, R4, R5, and R11 are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-α converting enzyme (TACE), aggrecanase, or a combination thereof.
摘要翻译：本申请描述了式（I）的新型乙内酰脲衍生物或其药学上可接受的盐或前药形式，其中L，Z 0，R 1，R 4，本说明书中定义了R 5，R 5和R 11，其可用作基质金属蛋白酶（MMP），TNF-α转换酶（ TACE），聚集蛋白聚糖蛋白聚糖酶或其组合。

47. 发明授权

US06864368B2 N-heterocyclic derivatives as NOS inhibitors 失效
公开(公告)号：US06864368B2
公开(公告)日：2005-03-08
申请号：US10122006
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.

48. 发明授权

US06864263B2 N-heterocyclic derivatives as NOS inhibitors 失效
公开(公告)号：US06864263B2
公开(公告)日：2005-03-08
申请号：US10121659
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.

49. 发明申请

US20020198115A1 Combination of additives for lubricating oils 失效
标题翻译：润滑油添加剂的组合
公开(公告)号：US20020198115A1
公开(公告)日：2002-12-26
申请号：US10166413
申请日：2002-06-10
发明人： Ravindranath Mukkamala
IPC分类号： C10M141/00 , C07D233/00
CPC分类号： C07D235/02 , C07D233/42 , C10M135/32 , C10M2219/09 , C10N2230/06 , C10N2230/12 , C10N2240/10 , C10N2240/101 , C10N2240/104 , C10N2240/106
摘要： A composition comprising a compound of formula I: 1 wherein W represents O, SnullA2, or two groups, R3 and R4; bonds a and b are single or double bonds, provided that one of a and b is a single bond and the other is a double bond; c is a single or double bond, and d is a single bond, double bond, or two single bonds, provided that d is a single bond when c is a double bond, d is not a single bond when c is a single bond, and W is R3 and R4 when d is two single bonds; A1, A2, B1 and B2 are independently hydrogen, alkyl, alkenyl, aralkyl or one of the groups depicted in Scheme 1: 2 and a dithiophosphate.
摘要翻译：一种组合物，其包含式I化合物：其中W表示O，S-A2或两个基团，R 3和R 4; 键a和b是单键或双键，条件是a和b之一是单键，另一个是双键; c是单键或双键，d是单键，双键或两个单键，条件是当c是双键时d是单键，当c是单键时d不是单键，当d为2个单键时，W为R3和R4; A1，A2，B1和B2独立地是氢，烷基，烯基，芳烷基或方案1中所示的基团之一：和二硫代磷酸酯。

50. 发明授权

US6103717A Halogen pyrimidines and its use thereof as parasite abatement means 失效
标题翻译：卤素嘧啶及其作为减少寄生虫的手段
公开(公告)号：US6103717A
公开(公告)日：2000-08-15
申请号：US101791
申请日：1998-07-16
申请人： Ulrich Heinemann , Herbert Gayer , Peter Gerdes , Bernd-Wieland Kruger , Bernd Gallenkamp , Uwe Stelzer , Albrecht Marhold , Ralf Tiemann , Stefan Dutzmann , Gerd Hanssler , Klaus Stenzel
发明人： Ulrich Heinemann , Herbert Gayer , Peter Gerdes , Bernd-Wieland Kruger , Bernd Gallenkamp , Uwe Stelzer , Albrecht Marhold , Ralf Tiemann , Stefan Dutzmann , Gerd Hanssler , Klaus Stenzel
IPC分类号： C07D239/34 , A01N43/72 , A01N43/88 , A01P3/00 , C07D233/00 , C07D239/00 , C07D239/80 , C07D249/00 , C07D271/00 , C07D273/00 , C07D273/01 , C07D413/12 , C07D413/14
CPC分类号： C07D273/00 , C07D413/12 , C07D413/14
摘要： Compounds of the formula (I) ##STR1## in which A represents optionally substituted alkanediyl,R represents in each case optionally substituted cycloalkyl, aryl or benzo-fused heterocyclyl,E represents --CH.dbd. or nitrogen,Q represents oxygen, sulphur, --CH.sub.2 --O--, a single bond, or a nitrogen atom which is optionally substituted by alkyl, andX represents halogen.
摘要翻译： PCT No.PCT / EP97 / 00151 Sec。 371日期：1998年7月16日 102（e）日期1998年7月16日PCT 1997年1月15日PCT PCT。公开号WO97 / 27189 日期1997年7月31日，式（I）的化合物，其中A表示任选取代的烷二基，R表示在各自情况下为任选取代的环烷基，芳基或苯并稠合的杂环基，E表示-CH =或氮，Q表示氧， -CH 2 -O-，单键或任选被烷基取代的氮原子，X表示卤素。

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