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101. 发明申请

US20080293700A1 Compositions and Methods Relating to Novel Compounds and Targets Thereof 审中-公开
标题翻译：与新型化合物及其靶物有关的组合物和方法
公开(公告)号：US20080293700A1
公开(公告)日：2008-11-27
申请号：US11662103
申请日：2005-09-07
申请人： Gary D. Glick
发明人： Gary D. Glick
IPC分类号： C07D243/14 , A61K31/5513 , A61P35/00 , A61P29/00 , A61P11/06 , A61P17/06
CPC分类号： A61K31/05 , A61K31/5513 , C07D243/24 , C07D401/04 , C07D403/04 , C07D403/06 , C07D409/14
摘要： The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and methods of using benzodiazepine derivatives as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, and hyperproliferation, and the like.
摘要翻译：本发明涉及新型化合物，其发现方法及其治疗用途。特别地，本发明提供了苯并二氮杂衍生物和使用苯并二氮杂衍生物作为治疗剂治疗与程序性细胞死亡，自身免疫，炎症和过度增殖等过程的错误调节相关的多种病症的方法。

102. 发明申请

US20080275024A1 CYCLIC MALONAMIDES AS INHIBITORS OF ASS PROTEIN PRODUCTION 有权
标题翻译：作为蛋白质生产的抑制剂的循环马来酸酐
公开(公告)号：US20080275024A1
公开(公告)日：2008-11-06
申请号：US12142145
申请日：2008-06-19
申请人： Richard E. Olson , Michael G. Yang
发明人： Richard E. Olson , Michael G. Yang
IPC分类号： A61K31/55 , C07D223/14 , C07D243/14 , A61K31/5513 , C07D223/08 , A61P25/00
CPC分类号： C07D223/16 , A61K31/4015 , A61K31/445 , A61K31/55 , A61K38/00 , C07D223/10 , C07D223/12 , C07D223/18 , C07D243/14 , C07D243/24 , C07D401/06 , C07D401/12 , C07D403/12 , C07K5/0205 , C07K5/06078 , C07K5/06139 , C07K5/06191 , C07K5/0812
摘要： This invention relates to novel cyclic malonamides having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to β-amyloid production such as Alzheimer's disease and Down's Syndrome.
摘要翻译：本发明涉及具有式（I）的新型环状丙二酰胺：其药物组合物及其使用方法。这些新化合物抑制淀粉样蛋白前体蛋白的加工，更具体地，抑制Aβ肽的产生，从而起到防止淀粉样蛋白质神经沉积的形成的作用。更具体地，本发明涉及治疗与β-淀粉样蛋白产生相关的神经系统疾病，例如阿尔茨海默病和唐氏综合征。

103. 发明申请

US20080090813A1 4-Phenyl-Pyrimidine-2-Carbonitrile Derivatives 失效
标题翻译： 4-苯基 - 嘧啶-2-甲腈衍生物
公开(公告)号：US20080090813A1
公开(公告)日：2008-04-17
申请号：US11628623
申请日：2005-06-09
申请人： Jiaqiang Cai , Zoran Rankovic , Jennifer Moir
发明人： Jiaqiang Cai , Zoran Rankovic , Jennifer Moir
IPC分类号： A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/551 , A61K31/5513 , A61P19/00 , A61P29/00 , A61P37/00 , A61P9/10 , C07D239/28 , C07D243/14 , C07D401/02 , C07D403/02 , C07D413/02
CPC分类号： C07D239/28
摘要： The invention relates to 4-phenyl-pyrimidine-2-carbonitrile derivatives having the general formula I wherein each of the substituents is given the definition as set forth in the specification and claims, or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising the derivatives as well as to the use thereof in the treatment of osteoporosis, atherosclerosis, inflammation and immune disorders, such as rheumatoid arthritis, and chronic pain, such as neuropathic pain.
摘要翻译：本发明涉及具有通式I的4-苯基 - 嘧啶-2-甲腈衍生物，其中每个取代基被给出如说明书和权利要求书中所述的定义，或其药学上可接受的盐。本发明还涉及包含衍生物的药物组合物以及其在治疗骨质疏松症，动脉粥样硬化，炎症和免疫疾病如类风湿性关节炎和慢性疼痛如神经性疼痛中的用途。

104. 发明申请

US20080027042A1 Novel Aminopyridine Derivatives Having Aurora a Selective Inhibitory Action 审中-公开
标题翻译：具有极光选择性抑制作用的新型氨基吡啶衍生物
公开(公告)号：US20080027042A1
公开(公告)日：2008-01-31
申请号：US11666531
申请日：2005-10-25
申请人： Mitsuru Ohkubo , Tetsuya Kato , Nobuhiko Kawanishi , Takashi Mita , Toshiyasu Shimomura
发明人： Mitsuru Ohkubo , Tetsuya Kato , Nobuhiko Kawanishi , Takashi Mita , Toshiyasu Shimomura
IPC分类号： A61K31/496 , A61K31/425 , A61K31/497 , A61K31/5513 , C07D211/72 , C07D243/14 , C07D295/00 , C07D277/04 , C07D241/04 , A61P43/00 , A61K31/5355 , A61K31/44
CPC分类号： A61K38/21 , A61K31/282 , A61K31/337 , A61K31/407 , A61K31/4745 , A61K31/475 , A61K31/496 , A61K31/506 , A61K31/513 , A61K31/519 , A61K31/52 , A61K31/675 , A61K31/704 , A61K31/7048 , A61K31/7068 , A61K31/7076 , A61K33/24 , A61K45/06 , C07D401/12 , C07D403/12 , C07D417/12 , A61K2300/00
摘要： The present invention relates to a compound represented by the general formula (I): wherein m1 and m2 are 1, 2, or 3; n1 and n2 are 0 or 1; i is an integer of any of 1 to m1; j is an integer of 1 to m2; R is aryl, heteroaryl, or cycloalkyl any of which may be substituted; Rai and Rai′ is hydrogen atom, etc. and Rbj and Rbj′ is hydrogen atom, etc.; Rc, Rd, and Re are hydrogen atom, etc; X1 is CH, CX1a, or N; X2 is CH, N, etc.; X3 is CH, N, etc.; X4 is CH or N; Y1, Y2, and Y3 are each independently CH or N; Z1 and Z2 are each independently CH or N; W is a 5-membered aromatic heterocyclic group such as pyrazolyl, thiazolyl, etc., or a pharmaceutically acceptable salt or ester thereof; a pharmaceutical composition or antitumor agent containing the same; and combinations of the antitumor agent with other antitumor agent(s).
摘要翻译：本发明涉及由通式（I）表示的化合物：其中m 1和m 2是1,2或3; n 1和n 2是0或1; i是1〜m1的任一个的整数; j为1〜m 2的整数; R是芳基，杂芳基或环烷基，其中任一个可以被取代; R a a和R a'是氢原子等，R bj和R b'是氢原子等等 R c，R d和R e是氢原子等; X 1是CH，CX 1a，或N; X 2是CH，N等; X 3是CH，N等; X 4是CH或N; Y 1，Y 2和Y 3各自独立地为CH或N; Z 1和Z 2各自独立地为CH或N; W是5元芳族杂环基，例如吡唑基，噻唑基等，或其药学上可接受的盐或酯; 含有它们的药物组合物或抗肿瘤剂; 以及抗肿瘤剂与其它抗肿瘤剂的组合。

105. 发明授权

US07160880B1 Short-acting benzodiazepines 有权
公开(公告)号：US07160880B1
公开(公告)日：2007-01-09
申请号：US09980680
申请日：2000-05-12
申请人： Paul L Feldman , David Kendall Jung , Istvan Kaldor , Gregory J. Pacofsky , Jeffrey A. Stafford , Jeffrey H. Tidwell
发明人： Paul L Feldman , David Kendall Jung , Istvan Kaldor , Gregory J. Pacofsky , Jeffrey A. Stafford , Jeffrey H. Tidwell
IPC分类号： A61P25/20 , A61K31/55 , C07D243/14 , C07D243/18 , C07D243/24
CPC分类号： C07D243/20 , C07D401/04 , C07D401/12 , C07D403/12 , C07D487/04
摘要： The present invention provides a compound of formula (I): wherein all variables are as defined herein, pharmaceutical formulations containing the same, processes for preparing the same and their use therapy.

106. 发明申请

US20050143436A1 Inhibitors of interleukin-1beta converting enzyme 审中-公开
标题翻译：白细胞介素-1β转换酶抑制剂
公开(公告)号：US20050143436A1
公开(公告)日：2005-06-30
申请号：US10999865
申请日：2004-11-29
申请人： Mark Batchelor , David Bebbington , Guy Bemis , Wolf Fridman , Roger Gillespie , Julian Golec , David Lauffer , David Livingston , Saroop Matharu , Michael Mullican , Mark Murcko , Robert Murdoch , Robert Zelle
发明人： Mark Batchelor , David Bebbington , Guy Bemis , Wolf Fridman , Roger Gillespie , Julian Golec , David Lauffer , David Livingston , Saroop Matharu , Michael Mullican , Mark Murcko , Robert Murdoch , Robert Zelle
IPC分类号： C07D243/12 , A61K31/55 , A61K31/551 , A61K31/553 , A61K31/675 , A61K38/00 , A61K38/04 , A61K38/05 , A61K38/06 , A61K38/07 , A61K38/55 , A61P13/12 , A61P19/08 , A61P19/10 , A61P25/00 , A61P25/28 , A61P29/00 , A61P31/00 , A61P31/04 , A61P35/00 , A61P37/00 , A61P37/06 , A61P43/00 , C07D243/10 , C07D243/14 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D473/00 , C07D487/04 , C07D491/048 , C07D495/04 , C07D498/04 , C07D513/04 , C07D519/00 , C07F9/645 , C07F9/6561 , C07K5/02 , C07K5/023 , C07K5/06 , C07K5/078 , C07K5/097 , A61K31/41 , A61K31/195
CPC分类号： C07D243/12 , A61K38/00 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07K5/0202 , C07K5/06139 , C07K5/0821
摘要： The present invention relates to novel classes of compounds which are inhibitors of interleukin-1β converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN-γ-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF- and IFN-γ-mediated diseases and decreasing IGIF and IFN-γ production using the compounds and compositions of this invention. This invention also relates to methods for preparing N-acylamino compounds.
摘要翻译：本发明涉及作为白细胞介素-1β转换酶抑制剂的新型化合物。本发明的ICE抑制剂的特征在于具体的结构和物理化学特征。本发明还涉及包含这些化合物的药物组合物。本发明的化合物和药物组合物特别适用于抑制ICE活性，因此可有利地用作抗IL-1，细胞凋亡，IGIF和IFN-γ介导的疾病，炎性疾病，自身免疫性疾病破坏性骨病，增殖性疾病，感染性疾病，退行性疾病和坏死性疾病。本发明还涉及使用本发明的化合物和组合物来抑制ICE活性，治疗白细胞介素-1，细胞凋亡，IGIF-和IFN-γ介导的疾病以及减少IGIF和IFN-γ产生的方法。本发明还涉及制备N-酰基氨基化合物的方法。

107. 发明申请

US20050113363A1 Hydroxyalkanoylaminolactams and related structures as inhibitors of A beta protein production 有权
标题翻译：羟基烷酰氨基内酰胺和相关结构作为Aβ蛋白生产的抑制剂
公开(公告)号：US20050113363A1
公开(公告)日：2005-05-26
申请号：US11024377
申请日：2004-12-28
申请人： Richard Olson , Hong Liu , Lorin Thompson
发明人： Richard Olson , Hong Liu , Lorin Thompson
IPC分类号： C07D223/18 , C07D243/08 , C07D243/14 , C07D243/24 , C07D401/04 , A61K31/55 , A61K31/4015 , A61K31/445
CPC分类号： C07D223/18 , C07D223/10 , C07D223/12 , C07D223/16 , C07D243/08 , C07D243/14 , C07D243/24 , C07D243/26 , C07D401/04
摘要： This invention relates to novel lactams having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to β-amyloid production such as Alzheimer's disease and Down's Syndrome.
摘要翻译：本发明涉及具有式（I）的新型内酰胺：其药物组合物及其使用方法。这些新化合物抑制淀粉样蛋白前体蛋白的加工，更具体地，抑制Aβ肽的产生，从而起到防止淀粉样蛋白质神经沉积的形成的作用。更具体地，本发明涉及治疗与β-淀粉样蛋白产生相关的神经系统疾病，例如阿尔茨海默病和唐氏综合征。

108. 发明授权

US06878821B2 Modifying chemoselectivity during oxidation of nitrogen compounds 失效
标题翻译：在氮化合物氧化过程中改变化学选择性
公开(公告)号：US06878821B2
公开(公告)日：2005-04-12
申请号：US10240364
申请日：2001-03-22
申请人： Patrick Bernardelli
发明人： Patrick Bernardelli
IPC分类号： C07D487/06 , C07B33/00 , C07B41/02 , C07B61/00 , C07C213/08 , C07C217/18 , C07C403/16 , C07D243/14
CPC分类号： C07B41/02 , C07B33/00
摘要： The invention concerns a method for chemoselective oxidation of an organic compound comprising several potentially oxidizable groups whereof at least one is a nitrogen group. Said method is characterised in that it consists in using at least a protic solvent, which is a good donor of hydrogen bonds, enabling to limit N-oxidation.
摘要翻译：本发明涉及一种用于化学选择性氧化有机化合物的方法，所述有机化合物包括几个潜在的可氧化基团，其中至少一个是氮基团。所述方法的特征在于使用至少一种质子溶剂，其是氢键的良好供体，能够限制N-氧化。

109. 发明申请

US20050009807A1 Cyclic malonamides as inhibitors of A-Beta protein production 有权
标题翻译：循环丙二酰胺作为A-β蛋白生产的抑制剂
公开(公告)号：US20050009807A1
公开(公告)日：2005-01-13
申请号：US10746769
申请日：2003-12-24
申请人： Richard Olson , Michael G. Yang
发明人： Richard Olson , Michael G. Yang
IPC分类号： A61K31/4015 , A61K31/445 , A61K31/55 , A61K31/5513 , A61K38/00 , A61P25/28 , A61P43/00 , C07D223/12 , C07D223/16 , C07D223/18 , C07D243/14 , C07D243/18 , C07D243/24 , C07D401/06 , C07D401/12 , C07D403/12 , C07K5/02 , C07K5/06 , C07K5/065 , C07K5/078 , C07K5/087
CPC分类号： C07D223/16 , A61K31/4015 , A61K31/445 , A61K31/55 , A61K38/00 , C07D223/10 , C07D223/12 , C07D223/18 , C07D243/14 , C07D243/24 , C07D401/06 , C07D401/12 , C07D403/12 , C07K5/0205 , C07K5/06078 , C07K5/06139 , C07K5/06191 , C07K5/0812
摘要： This invention relates to novel cyclic malonamides having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to β-amyloid production such as Alzheimer's disease and Down's Syndrome.
摘要翻译：本发明涉及具有式（I）的新型环状丙二酰胺：其药物组合物及其使用方法。这些新化合物抑制淀粉样蛋白前体蛋白的加工，更具体地，抑制Aβ肽的产生，从而起到防止淀粉样蛋白质神经沉积的形成的作用。更具体地，本发明涉及治疗与β-淀粉样蛋白产生相关的神经系统疾病，例如阿尔茨海默病和唐氏综合征。

110. 发明申请

US20010039340A1 Process for preparing pure crystalline lorazepam 失效
标题翻译：制备纯结晶劳拉西泮的方法
公开(公告)号：US20010039340A1
公开(公告)日：2001-11-08
申请号：US09799318
申请日：2001-03-05
发明人： Igor Lifshitz
IPC分类号： C07D243/14
CPC分类号： C07D243/24
摘要： The present invention provides a process for preparing crystalline lorazepam substantially free of bound solvent from a lorazepam alcohol solvate or hydrate by suspending the lorazepam solvate in an organic medium selected from ethyl acetate, cyclohexane, dichloromethane, toluene and mixtures thereof. This process is useful in producing the anti-anxiety and sedative agent lorazepam in increased yields. A process for converting lorazepam lower alcohol solvates to lorazepam hydrate is also disclosed.
摘要翻译：本发明提供了一种通过将劳拉西泮溶剂化物悬浮在选自乙酸乙酯，环己烷，二氯甲烷，甲苯及其混合物的有机介质中来制备基本上不含结合的溶剂的劳拉西泮醇溶剂化物或水合物的结晶性劳拉西泮的方法。该方法可用于产生抗焦虑和镇静剂劳拉西泮的产量增加。还公开了将劳拉西泮低级醇溶剂化物转化为水合氯雷他平的方法。

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