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1. 发明申请

WO2003082828A1 SUBSTITUTED TETRAHYDROISOQUINOLINES AS C5A RECEPTOR MODULATORS 审中-公开
标题翻译：作为C5A受体调节剂的取代的四氢喹啉
公开(公告)号：WO2003082828A1
公开(公告)日：2003-10-09
申请号：PCT/US2003/009046
申请日：2003-03-25
申请人： NEUROGEN CORPORATION , MITCHELL, Scott , OHLIGER, Robert , ZHANG, LuYan , ZHAO, He , CURRIE, Kevin , LEE, Kyungae
发明人： MITCHELL, Scott , OHLIGER, Robert , ZHANG, LuYan , ZHAO, He , CURRIE, Kevin , LEE, Kyungae
IPC分类号： C07D217/04
CPC分类号： C07D221/20 , A61K31/47 , C07D211/14 , C07D211/70 , C07D217/04 , C07D217/14 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/04 , C07D417/12 , C07D495/04
摘要： Substituted tetrahydroisoquinolines of Formula I are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5a receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
摘要翻译：提供式I的取代的四氢异喹啉。这些化合物是可用于在体内或体外调节C5a受体活性的配体，并且特别可用于治疗与人类，驯养的伴侣动物和家畜中的病理性C5a受体激活相关的病症。还提供了用于治疗这些病症的药物组合物和方法，以及使用这些配体进行受体定位研究的方法。

2. 发明申请

WO2003082829A1 NEW ARYL IMIDAZOLES AND RELATED COMPOUNDS AS C5A RECEPTOR MODULATORS 审中-公开
标题翻译：作为C5A受体调节剂的新ARYL咪唑和相关化合物
公开(公告)号：WO2003082829A1
公开(公告)日：2003-10-09
申请号：PCT/US2003/009938
申请日：2003-03-28
申请人： NEUROGEN CORPORATION , LUKE, George, P. , MAYNARD, George , MITCHELL, Scott , THURKAUF, Andrew , XIE, Linghong , ZHANG, LuYan , ZHANG, Suoming , ZHAO, He , CHENARD, Bertrand, L. , GAO, Yang , HAN, Bingsong , HE, Xiao, Shu
发明人： LUKE, George, P. , MAYNARD, George , MITCHELL, Scott , THURKAUF, Andrew , XIE, Linghong , ZHANG, LuYan , ZHANG, Suoming , ZHAO, He , CHENARD, Bertrand, L. , GAO, Yang , HAN, Bingsong , HE, Xiao, Shu
IPC分类号： C07D233/54
CPC分类号： C07D233/64 , A61K31/4164 , C07D233/68 , C07D235/02 , C07D235/30 , C07D237/12 , C07D401/04 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The invention provides Aryl substituted imidazoles, pyrazoles, pyridizines and related compounds of the Formula (I) where the ring system represented by Formula (A) is a 5 membered heteroaryl ring system, in which x is 0, A is chosen from carbon and heteroatoms nitrogen, oxygen, and sulfur, and E and G are independently carbon or nitrogen, provided that the 5 membered heteroaryl ring system does not contain more than 3 heteroatoms or more than 1 oxygen or sulfur atom, or a 6 membered heteroaryl ring system, in which x is 1, A, B, E, and G are independently chosen from carbon and nitrogen, provided that the 6 membered heteroaryl ring system does not contain more than 3 nitrogen atoms. The remaining variables, Ar 1 , Ar 2 , R, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , y and z are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of the invention act bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. This invention also relates to pharmaceutical compositions comprising such compounds. It further relates to the use of such compounds in treating a variety of inflammatory and immune system disorders.
摘要翻译：本发明提供了式（I）的芳基取代的咪唑，吡唑，吡啶和相关化合物，其中由式（A）表示的环系是5元杂芳基环系，其中x是0，A选自碳和杂原子氮，氧和硫，并且E和G独立地为碳或氮，条件是5元杂芳基环系不包含多于3个杂原子或多于1个氧或硫原子或6元杂芳基环系，其中x为1，A，B，E和G独立地选自碳和氮，条件是6元杂芳基环系不含3个以上的氮原子。剩余的变量Ar1，Ar2，R，R1，R2，R3，R4，R5，R6，y和z在本文中定义。这些化合物是C5a受体的配体。本发明优选的化合物作用以高亲和力结合C5a受体，在C5a受体上表现出中性拮抗剂或反向激动剂活性。本发明还涉及包含这些化合物的药物组合物。它还涉及这些化合物在治疗各种炎性和免疫系统疾病中的应用。

3. 发明申请

WO2002050062A3 BENZIMIDAZOLE AND PYRIDYLIMIDAZOLE DERIVATIVES AS LIGANDS FOR GABA RECEPTORS 审中-公开
公开(公告)号：WO2002050062A3
公开(公告)日：2002-06-27
申请号：PCT/US2001/050038
申请日：2001-12-21
申请人： NEUROGEN CORPORATION , PFIZER INC. , LI, Guiying , PETERSON, John, M. , ALBAUGH, Pamela , CURRIE, Kevin, S. , CAI, Guolin , GUSTAVSON, Linda, M. , LEE, Kyungae , HUTCHISON, Alan , SINGH, Vinod , MAYNARD, George, D. , YUAN, Jun , LING HONG, Xie , GHOSH, Manuka , LIU, Nian , LUKE, George, P. , MITCHELL, Scott , ALLEN, Martin, Patrick , LIRAS, Spiros
发明人： LI, Guiying , PETERSON, John, M. , ALBAUGH, Pamela , CURRIE, Kevin, S. , CAI, Guolin , GUSTAVSON, Linda, M. , LEE, Kyungae , HUTCHISON, Alan , SINGH, Vinod , MAYNARD, George, D. , YUAN, Jun , LING HONG, Xie , GHOSH, Manuka , LIU, Nian , LUKE, George, P. , MITCHELL, Scott , ALLEN, Martin, Patrick , LIRAS, Spiros
IPC分类号： C07D401/14
摘要： This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula (I). The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABA A receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABA A receptors in tissue sections.

4. 发明申请

WO2005110416A2 4,5-DISUBSTITUTED-2-ARYL PYRIMIDINES 审中-公开
标题翻译： 4,5-取代的2-芳基吡啶
公开(公告)号：WO2005110416A2
公开(公告)日：2005-11-24
申请号：PCT/US2005/015897
申请日：2005-05-06
申请人： NEUROGEN CORPORATION , MAYNARD, George, D. , GHOSH, Manuka , YUAN, Jun , CURRIE, Kevin, S. , MITCHELL, Scott , GUO, Qin , ZHAO, He
发明人： MAYNARD, George, D. , GHOSH, Manuka , YUAN, Jun , CURRIE, Kevin, S. , MITCHELL, Scott , GUO, Qin , ZHAO, He
IPC分类号： A61K31/505
CPC分类号： A61K31/505 , C07D239/26 , C07D239/28 , C07D239/34 , C07D239/42 , C07D239/47 , C07D239/48 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D417/04 , C07D471/04 , C07D498/04
摘要： 4,5-disubstituted-2-arylpyrimidines of Formula (I) and Formula (II) are provided: wherein R 1 , R 2 , R 3 , R 8 , R 9 , A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I and II bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 4,5-disubstituted-2-arylpyrimidines, which are useful as probes for the localization of C5a receptors.
摘要翻译：提供式（I）和式（II）的4,5-二取代-2-芳基嘧啶：其中R 1，R 2，R 3，R 8，R 9，A和Ar如本文所定义。这些化合物是C5a受体的配体。优选的式I和II化合物以高亲和力结合C5a受体，并在C5a受体上呈现中性拮抗剂或反向活性。本发明还涉及包含这些化合物的药物组合物，以及这些化合物在治疗各种炎性，心血管和免疫系统疾病中的用途。此外，本发明提供标记的4,5-二取代-2-芳基嘧啶，其可用作C5a受体定位的探针。

5. 发明申请

WO2005110991A1 1-ARYL-4-SUBSTITUTED ISOQUINOLINES 审中-公开
标题翻译： 1-ARYL-4取代的异喹啉
公开(公告)号：WO2005110991A1
公开(公告)日：2005-11-24
申请号：PCT/US2005/015959
申请日：2005-05-06
申请人： NEUROGEN CORPORATION , LEE, Kyungae , YUAN, Jun , MAYNARD, George, D. , HUTCHISON, Alan , MITCHELL, Scott
发明人： LEE, Kyungae , YUAN, Jun , MAYNARD, George, D. , HUTCHISON, Alan , MITCHELL, Scott
IPC分类号： C07D217/02
CPC分类号： C07D405/12 , A61K31/47 , C07D217/14 , C07D217/16 , C07D217/22 , C07D401/04 , C07D401/06 , C07D401/14 , C07D413/14
摘要： 1-Aryl-4-substituted isoquinolines analogues of Formula (I) and Formula (II) are provided, as follows : wherein R 1 , R 2 , R 3 , R 8 , R 9 , A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula (I) and (II) bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 1-aryl-4-substituted isoquinolines, which are useful as probes for the localization of C5a receptors.
摘要翻译：提供式（I）和式（II）的1-芳基-4-取代的异喹啉类似物，如下所述：其中R1，R2，R3，R8，R9，A和Ar如本文所定义。这些化合物是C5a受体的配体。式（I）和（II）的优选化合物以高亲和力结合C5a受体，并在C5a受体上呈现中性拮抗剂或反向激动剂活性。本发明还涉及包含这些化合物的药物组合物组合物，以及这些化合物在治疗各种炎性，心血管和免疫系统疾病中的用途。此外，本发明提供标记的1-芳基-4-取代的异喹啉，其可用作C5a受体定位的探针。

6. 发明申请

WO2005005429A1 CERTAIN HETEROCYCLIC SUBSTITUTED IMIDAZO[1,2-A]PYRAZIN-8-YLAMINES AND METHODS OF INHIBITION OF BRUTON’S TYROSINE KINASE BY SUCH COMPOUNDS 审中-公开
标题翻译：某些杂环取代的咪唑并[1,2-A]吡嗪-8-胺和这种化合物抑制BRUTON的酪氨酸激酶的方法
公开(公告)号：WO2005005429A1
公开(公告)日：2005-01-20
申请号：PCT/US2004/021150
申请日：2004-06-30
申请人： CELLULAR GENOMICS, INC. , CURRIE, Kevin, S. , DESIMONE, Robert, W. , MITCHELL, Scott , PIPPIN, Douglas, A.
发明人： CURRIE, Kevin, S. , DESIMONE, Robert, W. , MITCHELL, Scott , PIPPIN, Douglas, A.
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Compounds of formula (I) and all pharmaceutically acceptable forms thereof, are described herein. The variables R 1 , R 2 , R 3 , Z 2 , and Q, shown in Formula I are defined herein. Pharmaceutical compositions containing one or more compounds of Formula I, or a pharmaceutically acceptable form of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents are provided herein. Methods of treating patients suffering from certain diseases responsive to inhibition of tyrosine kinase activity are also given. In certain embodiments the diseases are responsive to inhibition of Btk activity and/or B-cell proliferation. Such methods comprise administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease. These diseases include cancer, an autoimmune and/or inflammatory disease, or an acute inflammatory reaction. Thus methods of treatment include administering a sufficient amount of a compound or salt as provided herein to decrease the symptoms or slow the progression of these diseases. Other embodiments include methods of treating other animals, including livestock and domesticated companion animals, suffering from a disease responsive to inhibition of kinase activity. Methods of treatment include administering a compound of Formula I as a single active agent or administering a compound of Formula I in combination with one or more other therapeutic agent. A method for determining the presence of Btk in a sample, comprising contacting the sample with a compound or form thereof of Formula I under conditions that permit detection of Btk activity, detecting a level of Btk activity in the sample, and therefrom determining the presence or absence of Btk in the sample.
摘要翻译：本文描述式（I）化合物及其所有药学上可接受的形式。式I中所示的变量R1，R2，R3，Z2和Q在本文中定义。本文提供了含有一种或多种式I化合物或此类化合物的药学上可接受的形式的药物组合物，以及一种或多种药学上可接受的载体，赋形剂或稀释剂。还给出了治疗患有某些对抑制酪氨酸激酶活性有响应的疾病的患者的方法。在某些实施方案中，疾病对Btk活性和/或B细胞增殖的抑制有反应。这样的方法包括向这样的患者施用一定量的有效降低疾病体征或症状的式I化合物。这些疾病包括癌症，自身免疫和/或炎性疾病或急性炎症反应。因此，治疗方法包括施用足够量的本文提供的化合物或盐以减少症状或减缓这些疾病的进展。其他实施方案包括治疗其它动物，包括患有对抑制激酶活性有响应的疾病的家畜和驯养的伴侣动物的方法。治疗方法包括给予式I化合物作为单一活性剂或将一种式I化合物与一种或多种其它治疗剂组合施用。一种用于确定样品中Btk的存在的方法，包括在允许检测Btk活性，检测样品中Btk活性水平的条件下使样品与式I化合物或其形式接触的方法，样品中没有Btk。

7. 发明申请

WO2003006471A1 HETEROARYL SUBSTITUTED FUSED BICYCLIC HETEROARYL COMPOUNDS AS GABAA RECEPTOR LIGANDS 审中-公开
标题翻译：作为GABAA受体配体的HETEROARYL取代的双熔体杂环化合物
公开(公告)号：WO2003006471A1
公开(公告)日：2003-01-23
申请号：PCT/US2002/022130
申请日：2002-07-12
申请人： NEUROGEN CORPORATION , HUTCHISON, Alan , MAYNARD, George , ALBAUGH, Pamela , XIE, Linghong , YUAN, Jun , MITCHELL, Scott , SINGH, Vinod , GHOSH, Manuka , LI, Guiying , LIU, Nian
发明人： HUTCHISON, Alan , MAYNARD, George , ALBAUGH, Pamela , XIE, Linghong , YUAN, Jun , MITCHELL, Scott , SINGH, Vinod , GHOSH, Manuka , LI, Guiying , LIU, Nian
IPC分类号： C07D513/04
CPC分类号： C07D487/04 , C07D471/04 , C07D513/04
摘要： This invention relates to heteroaryl substituted fused bicyclic heteroaryl compounds, such as heteroaryl substituted imidazopyridines, imidazopyrazines, imidazopyridizines, imidazopyrimidines, and imidazothiazoles, which may be described by Formula I or Formula II: The invention is particularly relates to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABA A receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Processes for preparing compounds of Formula I and Formula II are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I or Formula II in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABA A receptors in tissue sections.
摘要翻译：本发明涉及可以由式I或式II描述的杂芳基取代的稠合双环杂芳基化合物，例如杂芳基取代的咪唑并吡啶，咪唑并吡嗪，咪唑并吡啶，咪唑并吡啶和咪唑并噻唑。本发明特别涉及以高选择性结合的这类化合物并且对GABA A受体的苯并二氮杂位点具有高亲和力。本发明还涉及包含这些化合物的药物组合物以及这些化合物在治疗某些中枢神经系统（CNS）疾病中的用途。公开了制备式I和式II化合物的方法。本发明还涉及式I或式II的苯并咪唑，吡啶基咪唑和相关双环杂芳基化合物与一种或多种其它CNS剂的组合用于增强其它CNS剂的作用。此外，本发明涉及使用这些化合物作为组织切片中GABA A受体定位的探针。

8. 发明申请

WO2005062802A3 SYSTEM AND METHOD FOR INTERNET BASED MARKETING AND INFORMATION MANAGEMENT FOR MORTGAGE LOANS 审中-公开
公开(公告)号：WO2005062802A3
公开(公告)日：2005-07-14
申请号：PCT/US2004/042524
申请日：2004-12-17
申请人： HOME LOAN DESK CORPORATION , MITCHELL, Scott
发明人： MITCHELL, Scott
IPC分类号： G06Q40/00
摘要： The present invention generally provides systems and methods for processing loans and generating leads for loans. Loans are generally processed by receiving at least one lead relating to one or more individuals interested in obtaining a loan from a registered user, assigning the lead to a loan officer, which may either accept and decline the assignment, and reassigning the lead to another loan officer if a previous assigned loan officer declines the lead. The status of the loan process may be tracked the loan application process. Such leads may be generated by a comparison between at least one term of a closed loan with at least one term of another loan, in which instance, the lead is generated based on a determination as to whether a borrower of the closed loan would benefit from a refinance of the closed loan.

9. 发明申请

WO2011068964A1 INCREASING OCTANE NUMBER OF LIGHT NAPHTHA USING A GERMANIUM-ZEOLITE CATALYST 审中-公开
标题翻译：使用锗 - 沸石催化剂增加光合萘数量
公开(公告)号：WO2011068964A1
公开(公告)日：2011-06-09
申请号：PCT/US2010/058723
申请日：2010-12-02
申请人： SAUDI BASIC INDUSTRIES CORPORATION , STEVENSON, Scott , ELLIS, Paul, E. , MIER, Mike , FARMER, Dustin , KHANMAMEDOVE, Alla , MITCHELL, Scott
发明人： STEVENSON, Scott , ELLIS, Paul, E. , MIER, Mike , FARMER, Dustin , KHANMAMEDOVE, Alla , MITCHELL, Scott
IPC分类号： C07C5/13
CPC分类号： C10G35/065 , B01J29/047 , B01J29/44 , B01J2229/20 , C10G35/085 , C10G2300/1044 , C10G2300/1081 , C10G2300/1096 , C10G2300/202 , C10G2300/305 , C10G2300/4018
摘要： This invention relates to a process for the increasing the octane number of a naphtha hydrocarbon feed having a predominantly paraffin content with a germanium -containing zeolite catalyst. The catalyst is a non-acidic germanium zeolite on which a noble metal, such as platinum, has been deposited. The zeolite structure may be of MTW, MWW, MEL, TON, MRE, FER, MFI, BEA, MOR, LTL or MTT. The zeolite is made non-acidic by being base-exchanged with an alkali metal or alkaline earth metal, such as cesium, potassium, sodium, rubidium, barium, calcium., magnesium and mixtures thereof, to reduce acidity. The catalyst is sulfur tolerant. The hydrocarbon feed may contain sulfur up to 1000 ppm. The present invention could be applicable to a feedstream which is predominantly naphthenes and paraffins.
摘要翻译：本发明涉及一种通过含锗的沸石催化剂提高主要为石蜡含量的石脑油烃进料的辛烷值的方法。催化剂是其上沉积有贵金属如铂的非酸性锗沸石。沸石结构可以是MTW，MWW，MEL，TON，MRE，FER，MFI，BEA，MOR，LTL或MTT。通过与碱金属或碱土金属如铯，钾，钠，铷，钡，钙，镁及其混合物进行碱交换使沸石制成非酸性，以降低酸度。催化剂是耐硫的。烃进料可含有高达1000ppm的硫。本发明可以应用于主要是环烷烃和链烷烃的进料流。

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