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1. 发明申请

US20060199796A1 Substituted benzofused heterocycles 有权
公开(公告)号：US20060199796A1
公开(公告)日：2006-09-07
申请号：US11203562
申请日：2005-08-12
申请人： Xi Chen , Xiaoqi Chen , Richard Connors , Kang Dai , Ying Fu , Juan Jaen , Yong-Jae Kim , Leping Li , Mike Lizarzaburu , Jeffrey Mihalic , Stephen Shuttleworth
发明人： Xi Chen , Xiaoqi Chen , Richard Connors , Kang Dai , Ying Fu , Juan Jaen , Yong-Jae Kim , Leping Li , Mike Lizarzaburu , Jeffrey Mihalic , Stephen Shuttleworth
IPC分类号： A61K31/553 , A61K31/5513 , A61K31/4709
CPC分类号： C07D417/06 , C07D217/24 , C07D223/16 , C07D243/14 , C07D401/06 , C07D401/12 , C07D487/04 , C07D491/10
摘要： The present invention relates to the compounds of Formula I, their preparation and pharmaceutical compositions comprising them. The compounds and pharmaceutical compositions are useful, for example, for the treatment and prevention of obesity, obesity-related disorders and eating disorders.

2. 发明申请

US20060040943A1 3-Furanyl analogs of toxoflavine as kinase inhibitors 失效
公开(公告)号：US20060040943A1
公开(公告)日：2006-02-23
申请号：US10520641
申请日：2003-07-08
申请人： Jean Fernand LaCrampe , Richard Connors , Chih Ho , Alan Richardson , Eddy Freyne , Peter Buijnsters , Annette Bakker
发明人： Jean Fernand LaCrampe , Richard Connors , Chih Ho , Alan Richardson , Eddy Freyne , Peter Buijnsters , Annette Bakker
IPC分类号： C07D487/04 , A61K31/53
CPC分类号： C07D487/04
摘要： The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein m represents an integer being 0 or 1; n represents an integer being 0, 1 or 2; R1 represents C1-4alkyl, C1-4alkyl substituted with pyridinyl, phenyl, piperidinyl or piperidinyl substituted with C1-4alkyloxycarbonyl; R2 represents hydrogen or C1-4alkyl; R3 represents hydrogen or C1-4alkyl; or R2 and R3 taken together with the carbon atom to which they are attached form cyclopentyl or piperidinyl wherein said cyclopentyl or piperidinyl each independently may optionally be substituted with one, or where possible, two or three substituents each independently selected from C1-4alkyloxycarbonyl, phenylcarbonyl or —C(═NH)—NH2; R4 represents halo or C1-4alkyloxy; R5 represents Het2, C1-4alkyl substituted with one or where possible more substituents being selected from hydroxy, halo, Het3 or NR6R7, or C1-4alkyloxy substituted with one or where possible more substituents being selected from Het4 or —C(═O)-Het4; R6 and R7 are each independently selected from hydrogen, C1-4alkyl, Het5 or C1-4alkyl substituted with one or where possible more substituents being selected from hydroxy or Het5; Het2 represents piperazinyl; Het3 represents a heterocycle selected from morpholinyl, pyrrolidinyl, piperidinyl, or piperazinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from C1-4alkyl preferably methyl, aminosulfonyl, mono- or di(C1-4alkyl)aminosulfonyl, hydroxyC1-4alkyloxyC1-4alkyl, C1-4alkyloxyC1-4alkyl or C1-4alkyloxy; Het4 represents a heterocycle selected from morpholinyl or piperazinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three C1-4alkyl substituents, preferably methyl; Het5 represents a heterocycle selected from pyridinyl, pyrrolidinyl or piperidinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from aminosulfonyl, C1-4alkyloxycarbonyl or mono- or di(C1-4alkyl)aminosulfonyl.

3. 发明申请

US20070203136A1 TRIAZOLOPYRIDAZINES AS KINASE MODULATORS 有权
标题翻译：三唑吡啶作为激酶调节剂
公开(公告)号：US20070203136A1
公开(公告)日：2007-08-30
申请号：US11612020
申请日：2006-12-18
申请人： Tianbao Lu , Richard Alexander , Richard Connors , Maxwell Cummings , Robert Galemmo , Heather Rae Hufnagel , Dana Johnson , Ehab Khalil , Kristi Leonard , Thomas Markotan , Anna Maroney , Jan Sechler , Jeremy Travins , Robert Tuman
发明人： Tianbao Lu , Richard Alexander , Richard Connors , Maxwell Cummings , Robert Galemmo , Heather Rae Hufnagel , Dana Johnson , Ehab Khalil , Kristi Leonard , Thomas Markotan , Anna Maroney , Jan Sechler , Jeremy Travins , Robert Tuman
IPC分类号： A61K31/503 , A61K31/5377 , C07D487/04
CPC分类号： C07D487/04 , C07D519/00
摘要： The invention is directed to triazolopyridazine compounds of Formula I: where R1, R5, R6, R7, R8, and A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.
摘要翻译：本发明涉及式I的三唑并哒嗪化合物：其中R 1，R 5，R 6，R 7， >，R 8和A如本文所定义，使用这些化合物作为蛋白质酪氨酸激酶调节剂，特别是c-Met的抑制剂，以及这些化合物用于降低或抑制激酶活性的用途 c-Met在细胞或受试者中的调节，并调节细胞或受试者中的c-Met表达，以及这些化合物在受试者中预防或治疗细胞增殖性疾病和/或与c-Met有关的障碍的用途。本发明进一步涉及包含本发明化合物的药物组合物和治疗诸如癌症和其它细胞增殖性疾病的病症的方法。

4. 发明申请

US20050032084A1 Method of attaching a biopolymer to a solid support 审中-公开
标题翻译：将生物聚合物连接到固体支持物上的方法
公开(公告)号：US20050032084A1
公开(公告)日：2005-02-10
申请号：US10752493
申请日：2004-01-08
申请人： Michael Pirrung , Amy Odenbaugh , Richard Connors , Janice Worden
发明人： Michael Pirrung , Amy Odenbaugh , Richard Connors , Janice Worden
IPC分类号： G01N33/543 , G01N33/552 , B05D3/00 , C12M1/34 , C12Q1/68
CPC分类号： G01N33/54353 , G01N33/552
摘要： The present invention relates, in general, to a method of attaching a biopolymer to a solid support and, in particular, to a method of attaching a nucleic acid to a glass surface, and to reagents suitable for use in such a method. The invention further relates to the product produced by the present method and to kits comprising same.
摘要翻译：本发明一般涉及将生物聚合物连接到固体支持物的方法，特别是涉及将核酸附着到玻璃表面的方法以及适用于这种方法的试剂。本发明还涉及通过本发明方法生产的产品和包含该产品的试剂盒。

5. 发明申请

US20050239784A1 3-Phenyl analogs of toxoflavine as kinase inhibitors 审中-公开
公开(公告)号：US20050239784A1
公开(公告)日：2005-10-27
申请号：US10520768
申请日：2003-07-08
申请人： Jean LaCrampe , Richard Connors , Chih Ho , Alan Ricardson , Eddy Freyne , Peter Jacobus Buijnsters , Annette Bakker
发明人： Jean LaCrampe , Richard Connors , Chih Ho , Alan Ricardson , Eddy Freyne , Peter Jacobus Buijnsters , Annette Bakker
IPC分类号： A61K31/53 , A61K31/5377 , A61P9/10 , A61P35/00 , A61P43/00 , C07D487/04 , C07D519/00 , C07D487/02
CPC分类号： C07D487/04
摘要： The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereo-chemically isomeric forms thereof, wherein n represents an integer being 0, 1 or 2; m represents an integer being 0 or 1; R represents C1-4alkyl; R represents C1-4alkyl; R3 represents C1-4alkyl; or R2 and R3 taken together with the carbon atom to which they are attached form a C3-8cycloalkyl or Het1 wherein said C3-8cycloalkyl or Het1 each independently may optionally be substituted with C1-4alkyloxycarbonyl; R4 represents halo or C1-4alkyloxy; R5 represents C1-4alkyloxycarbonyl, —O-(mono- or di(C1-4alkyl)aminosulfonyl), C1-4alkyl substituted with one or where possible more substituent being selected from Het3 or NR6R7, C1-4alkyloxy substituted with one or where possible more substituents being selected from amino, Het4 or NR8R9; R6 and R7 are each independently selected from hydrogen, C1-4alkyl, C1-4alkyloxyC1-4alkyl, -Het5 or C1-4alkyl substituted with one or where possible more substituents being selected from hydroxy, or Het5; R8 and R9 are each independently selected from hydrogen, C1-4alkyl, -Het7 or mono- or di(C1-4alkyl)aminosulphonyl; Het3 represents a heterocycle selected from piperidinyl, or piperazinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from hydroxy, aminosulfonyl, amino, mono- or di(C1-4alkyl)aminosulfonyl, hydroxyC1-4alkyloxyC1-4alkyl or C1-4alkyloxy; Het4 represents a heterocycle selected from morpholinyl, piperidinyl or piperazinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from C1-4alkyl, C1-4alkyloxycarbonyl or mono- or di(C1-4alkyl)aminosulfonyl; Het5 represents a heterocycle selected from pyridinyl or piperidinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from aminosulfonyl, or mono- or di(C1-4alkyl)aminosulfonyl; Het7 represents piperidinyl.

6. 发明申请

US20080096208A1 BIOMARKERS FOR ASSESSING RESPONSE TO C-MET TREATMENT 审中-公开
标题翻译：评估对C-MET治疗反应的生物标志物
公开(公告)号：US20080096208A1
公开(公告)日：2008-04-24
申请号：US11846684
申请日：2007-08-29
申请人： Richard CONNORS
发明人： Richard CONNORS
IPC分类号： C12Q1/68 , C07H21/00 , C07K2/00 , C12Q1/02
CPC分类号： C12Q1/6886 , C12Q2600/106 , C12Q2600/136 , G01N33/5011 , G01N33/57484 , G01N2333/52 , G01N2333/70585 , G01N2800/52
摘要： Biomarkers that correlate to treatment with drugs that inhibit c-met are disclosed. These biomarkers have been shown to have utility in assessing response to the compounds. The expression level of the biomarkers is reduced upon treatment with c-met inhibitor compounds, thus indicating that these biomarkers are involved in c-met activity.
摘要翻译：公开了与抑制c-met的药物治疗相关的生物标志物。这些生物标志物已被证明可用于评估对化合物的反应。在用c-met抑制剂化合物治疗时，生物标志物的表达水平降低，从而表明这些生物标志物参与c-met活性。

7. 发明申请

US20070015207A1 Triazolopyrimidine derivatives 有权
标题翻译：三唑并嘧啶衍生物
公开(公告)号：US20070015207A1
公开(公告)日：2007-01-18
申请号：US11329642
申请日：2006-01-11
申请人： Donald Ludovici , Richard Connors , Steven Coats , Li Liu , Bart De Corte , Dana Johnson , Mark Schulz
发明人： Donald Ludovici , Richard Connors , Steven Coats , Li Liu , Bart De Corte , Dana Johnson , Mark Schulz
IPC分类号： G01N33/53 , C07H21/04 , C12P21/06 , C12N5/06 , C07D487/02 , C07K16/40 , C12N9/12
CPC分类号： C07K14/4738 , C07D487/04 , C12N9/1205 , C12Q1/485 , G01N2500/02
摘要： The invention relates to the discovery of triazolopyrimidine derivatives of formula (I), which have been found to exhibit inhibitory activity against the serine-tyrosine and tyrosine kinases.
摘要翻译：本发明涉及已发现对丝氨酸 - 酪氨酸和酪氨酸激酶具有抑制活性的式（I）三唑并嘧啶衍生物的发现。

8. 发明申请

US20070066610A1 Acylhydrazones as kinase modulators 有权
标题翻译：酰腙作为激酶调节剂
公开(公告)号：US20070066610A1
公开(公告)日：2007-03-22
申请号：US11377077
申请日：2006-03-16
申请人： Kristi Leonard , Tianbao Lu , Robert Tuman , Dana Johnson , Anna Maroney , Jan Sechler , Richard Connors , Richard Alexander , Maxwell Cummings , Robert Galemmo , Thomas Markotan
发明人： Kristi Leonard , Tianbao Lu , Robert Tuman , Dana Johnson , Anna Maroney , Jan Sechler , Richard Connors , Richard Alexander , Maxwell Cummings , Robert Galemmo , Thomas Markotan
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/404 , C07D413/14 , C07D405/14
CPC分类号： C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12
摘要： The invention is directed to acylhydrazones compounds of Formula I: where R1, R2 and A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.
摘要翻译：本发明涉及式I的酰腙化合物：其中R 1，R 2和A如本文所定义，使用这些化合物作为蛋白质酪氨酸激酶调节剂，特别是 c-Met的抑制剂以及这些化合物在细胞或受试者中降低或抑制c-Met的激酶活性并调节细胞或受试者中的c-Met表达的用途，以及这些化合物用于预防或在受试者中治疗与c-Met相关的细胞增殖性疾病和/或障碍。本发明进一步涉及包含本发明化合物的药物组合物和治疗诸如癌症和其它细胞增殖性疾病的病症的方法。

9. 发明申请

US20050130910A1 Immobilized N-substituted tricyclic 3-aminopyrazoles for the identification of biomolecular targets 审中-公开
标题翻译：固定的N-取代三环3-氨基吡唑，用于鉴定生物分子靶标
公开(公告)号：US20050130910A1
公开(公告)日：2005-06-16
申请号：US10986500
申请日：2004-11-10
申请人： Chih Ho , Robert Galemmo , Dana Johnson , Jay Mei , Stanley Belkowski , Richard Connors
发明人： Chih Ho , Robert Galemmo , Dana Johnson , Jay Mei , Stanley Belkowski , Richard Connors
IPC分类号： A61K31/4162 , A61K31/422 , A61K31/427 , A61K31/7056 , C07D231/54 , C07D231/56 , C07D401/12 , C07D403/12 , C07D413/02 , C07D417/02 , C07D495/04 , C07H17/00 , G01N33/543 , G01N33/574
CPC分类号： C07D403/12 , C04B35/632 , C07D231/54 , C07D231/56 , C07D401/12 , C07D495/04 , G01N33/574 , G01N2333/71 , G01N2500/00
摘要： The present invention relates to immobilized N-substituted tricyclic 3-aminopyrazole compounds of Formula 1 as tools for the identification of bimolecular targets in cells of therapeutic significance, profiling the selectivity of compounds, prediction of possible related toxicities and exploration of mechanisms of action in biological systems for therapeutic indications related to compounds. These agents can be used to identify biomolecules with the potential to interact with the immobilized reagent. The identified biomolecule may be then be used as a therapeutic target, serve as a marker of drug action, or alternatively describe an untoward or toxic potential of the immobilized agent.
摘要翻译：本发明涉及式1的固定化N-取代三环3-氨基吡唑化合物，作为用于鉴定细胞中双分子靶标的具有治疗意义的工具，分析化合物的选择性，预测可能的相关毒性和探索生物学作用机制与化合物相关的治疗适应症系统。这些试剂可用于鉴定具有与固定化试剂相互作用的潜力的生物分子。所鉴定的生物分子然后可以用作治疗靶，用作药物作用的标记，或者替代地描述固定化剂的不利或有毒的潜力。

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