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1. 发明申请

US20060229298A1 Melanin concentrating hormone receptor ligands: substituted 1-benzyl-4-aryl piperazine analogues 失效
公开(公告)号：US20060229298A1
公开(公告)日：2006-10-12
申请号：US11436099
申请日：2006-05-17
申请人： Alan Hutchison , Linda Gustavson , John Peterson , Dario Dollar , Timothy Caldwell , Taeyoung Yoon , Wallace Pringle , Rajagopal Bakthavatchalam , Yiping Shen , Cheryl Steenstra , Helen Yin , Robert DeSimone , Xiao-shu He
发明人： Alan Hutchison , Linda Gustavson , John Peterson , Dario Dollar , Timothy Caldwell , Taeyoung Yoon , Wallace Pringle , Rajagopal Bakthavatchalam , Yiping Shen , Cheryl Steenstra , Helen Yin , Robert DeSimone , Xiao-shu He
IPC分类号： A61K31/496 , A61K31/551 , A61K31/495 , C07D403/02
CPC分类号： C07D513/04 , C07D209/86 , C07D211/52 , C07D213/64 , C07D213/74 , C07D215/12 , C07D215/20 , C07D243/08 , C07D295/096 , C07D295/108 , C07D311/18 , C07D317/58 , C07D401/12 , C07D471/04 , C07D487/04 , C07D487/08
摘要： Melanin concentrating hormone receptor ligands (especially 1-benzyl-4-aryl-piperazines, 1-benzyl-4-aryl-piperidines and related compounds), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).

2. 发明授权

US06509366B2 Substituted imidazoles as selective modulators of Bradykinin B2 receptors 失效
标题翻译：取代的咪唑作为缓激肽B2受体的选择性调节剂
公开(公告)号：US06509366B2
公开(公告)日：2003-01-21
申请号：US09764805
申请日：2001-01-17
申请人： Stanislaw Rachwal , Alan Hutchison , Kenneth Shaw , George D. Maynard , Xiao-shu He , Robert DeSimone , Kevin Hodgetts
发明人： Stanislaw Rachwal , Alan Hutchison , Kenneth Shaw , George D. Maynard , Xiao-shu He , Robert DeSimone , Kevin Hodgetts
IPC分类号： A61K314174
CPC分类号： C07D233/64 , C07D233/68 , C07D401/06
摘要： Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein Y, R1, R2, R3, R4, R5, R6, R7 R7′ are variables defined herein, which compounds are modulators of Bradykinin B2 receptors. These compounds are therefore useful in the diagnosis and treatment of renal diseases, heart failure, hypertension, Meniere's disease, vaginal inflammation and pain, peripheral circulatory disorders, climacteric disturbance, retinochoroidal circulatory disorders, myocardial ischemia, myocardial infarction, postmyocardial infarction syndrome, angina pectoris, restenosis after percutaneous transluminal coronary angioplasty, hepatitis, liver cirrhosis, pancreatitis, ileus, diabetes, diabetic complications, male infertility, glaucoma, pain, asthma, and rhinitis, and for the increase of permeability of the blood-brain barrier or the blood-brain-tumor barrier.
摘要翻译：公开了下式的化合物或其药学上可接受的无毒盐，其中Y，R 1，R 2，R 3，R 4，R 5，R 6，R 7 R 7'是本文定义的变量，该化合物是缓激肽B2受体的调节剂。因此，这些化合物可用于诊断和治疗肾脏疾病，心力衰竭，高血压，梅尼埃病，阴道炎症和疼痛，外周循环障碍，更年期障碍，视网膜循环障碍，心肌缺血，心肌梗死，心肌梗死后综合征，心绞痛经皮腔内冠状动脉血管成形术，肝炎，肝硬化，胰腺炎，肠梗阻，糖尿病，糖尿病并发症，男性不育症，青光眼，疼痛，哮喘和鼻炎的再狭窄，以及增加血脑屏障或血液 - 脑肿瘤屏障。

3. 发明授权

US06482844B1 1-benzylimidazole derivatives 失效
标题翻译： 1-苄基咪唑衍生物
公开(公告)号：US06482844B1
公开(公告)日：2002-11-19
申请号：US09827565
申请日：2001-04-06
申请人： Xiao-Shu He , Xiaoyan Zhang , He Zhao , Robert DeSimone , Andrew Thurkauf
发明人： Xiao-Shu He , Xiaoyan Zhang , He Zhao , Robert DeSimone , Andrew Thurkauf
IPC分类号： A61K31415
CPC分类号： C07D233/64
摘要： Provided are compounds (and pharmaceutically acceptable non-toxic salt of such compounds) of the formula: in which A and B are C1-C3 alkylene; R1 is C1-C6 alkyl; R2 and R3 are hydrogen or C1-C6 alkyl; U and V are C1-C6 alkyl or halogen; X, Y and Z are hydrogen, C1-C6 alkyl, trifluoromethyl, C1-C6 alkoxy, trifluoromethoxy, halogen, or cyano; and W represents up to three substituents which are C1-C6 alkyl, trifluoromethyl, C1-C6 alkoxy, trifluoromethoxy, halogen, hydroxy, amino, or cyano. These compounds act as modulators of blood glucose levels and are useful for the treatment of diabetes, eating disorders, and obesity. Pharmaceutical compositions and methods of use of the compounds as pharmaceutical agents are also provided.
摘要翻译：本发明提供下式的化合物（和这些化合物的药学上可接受的无毒盐）：其中A和B是C1-C3亚烷基; R1是C1-C6烷基; R2和R3是氢或C1-C6烷基; U和V是C 1 -C 6烷基或卤素; X，Y和Z是氢，C 1 -C 6烷基，三氟甲基，C 1 -C 6烷氧基，三氟甲氧基，卤素或氰基; W代表最多三个取代基，它们是C1-C6烷基，三氟甲基，C1-C6烷氧基，三氟甲氧基，卤素，羟基，氨基或氰基。这些化合物作为血糖水平的调节剂，可用于治疗糖尿病，进食障碍和肥胖症。还提供了药物组合物和化合物作为药剂的使用方法。

4. 发明授权

US6133265A Certain amido- and amino- substituted benzylamine derivatives; a new class of neuropeptide Y1 specific ligands 失效
标题翻译：某些酰氨基和氨基取代的苄胺衍生物; 一类新的神经肽Y1特异性配体
公开(公告)号：US6133265A
公开(公告)日：2000-10-17
申请号：US897046
申请日：1997-07-18
申请人： Charles A. Blum , Robert DeSimone , Alan Hutchison , John M. Peterson
发明人： Charles A. Blum , Robert DeSimone , Alan Hutchison , John M. Peterson
IPC分类号： C07D295/12 , A61K31/415 , A61K31/416 , A61K31/42 , A61K31/444 , A61K31/472 , A61K31/495 , A61K31/496 , A61K31/502 , A61P3/00 , A61P9/04 , A61P9/12 , A61P43/00 , C07D209/42 , C07D211/76 , C07D213/81 , C07D213/82 , C07D215/48 , C07D215/50 , C07D215/54 , C07D217/26 , C07D231/14 , C07D231/56 , C07D237/28 , C07D261/20 , C07D295/02 , C07D295/135 , C07D295/14 , C07D295/155 , C07D333/24 , C07D333/40 , A61K31/5355 , C07D487/04
CPC分类号： C07D231/56 , C07D237/28 , C07D295/02 , C07D295/135 , C07D295/155
摘要： Amido, amino and sulfonamide substituted benzylamine derivatives useful in treating eating disorders have the formula ##STR1## where X.sub.1, X.sub.2, and X.sub.3, independently represent substituents of formula ##STR2## D=H, lower straight or branched chain alkyl having 1-6 carbon atoms, a methylene unit incorporated into a ring connected with G as in the cases of pyrrolidine, pyrrolidone, piperidine, and piperidone;E=O or H.sub.2 ;O=0 or 1;G=straight or branched chain lower alkyl having 1-6 carbon atoms, aryl, aryl substituted with halogen, straight or branched chain lower alkyl having 1-6 carbon atoms, heteroaryl--selected from the group consisting of 2-, 3-, or 4-pyridyl, 2-pyrazyl, 2-, or 3-thienyl, 2-pyrazinyl, 2-, 3-, or 4-quinolyl, 1-, 3-, or 4-isoquinolyl, 2-quinoxalyl, 3-, or 4-cinnolyl, said heteroaryl substituted with halogen, hydroxy, straight or branched chain lower alkyl having 1-6 carbon atoms, straight or branched chain lower alkoxy having 1-6 carbon atoms;and A, T and R.sub.1 -R.sub.4 are hydrogen or organic substituents.
摘要翻译：可用于治疗进食障碍的酰氨基，氨基和磺酰胺取代的苄基胺衍生物具有下式，其中X1，X2和X3独立地表示式D = H的取代基，具有1-6个碳原子的低级直链或支链烷基，如吡咯烷，吡咯烷酮，哌啶和哌啶酮的情况下与G连接的环; E = O或H2; O = 0或1; G =具有1-6个碳原子的直链或支链低级烷基，芳基，被卤素取代的芳基，具有1-6个碳原子的直链或支链低级烷基，杂芳基 - 选自2-，3-或 4-吡啶基，2-吡嗪基，2-或3-噻吩基，2-吡嗪基，2-，3-或4-喹啉基，1-，3-或4-异喹啉基，2-喹喔啉基，3-或所述杂芳基被卤素取代，羟基，具有1-6个碳原子的直链或支链低级烷基，具有1-6个碳原子的直链或支链低级烷氧基; 并且A，T和R 1 -R 4是氢或有机取代基。

5. 发明授权

US06316617B1 Certain amido-and amino-substituted benzylamine derivatives; a new class of Neuropeptide Y1 specific ligands 失效
标题翻译：某些酰氨基和氨基取代的苄胺衍生物; 一类新的神经肽Y1特异性配体
公开(公告)号：US06316617B1
公开(公告)日：2001-11-13
申请号：US09633055
申请日：2000-08-08
申请人： Charles A. Blum , Robert DeSimone , Alan Hutchison , John M. Peterson
发明人： Charles A. Blum , Robert DeSimone , Alan Hutchison , John M. Peterson
IPC分类号： C07D41710
CPC分类号： C07D231/56 , C07D237/28 , C07D295/02 , C07D295/135 , C07D295/155
摘要： This invention encompasses compounds of the formula where X1, X2, and X3, independently represent substituents of formula and the pharmaceutically acceptable salts thereof wherein the remaining variables are as defined herein and wherein said compounds are useful in the diagnosis and treatment of feeding disorders such as obesity and bulimia and cardiovascular diseases such as essential hypertension and congestive heart failure due to the binding of these compounds to human Neuropeptide Y1 receptors.
摘要翻译：本发明包括式X 1，X 2和X 3的化合物独立地表示下式的取代基及其药学上可接受的盐，其中其余变量如本文所定义，并且其中所述化合物可用于诊断和治疗哺乳障碍如肥胖症和贪食症以及由于这些化合物与人神经肽Y1受体的结合导致的心血管疾病如原发性高血压和充血性心力衰竭。

6. 发明授权

US07348326B2 Heteroaryl fused aminoalkyl imidazole derivatives: selective modulators of GABAa receptors 失效
标题翻译：杂芳基稠合氨基烷基咪唑衍生物：GABAa受体的选择性调节剂
公开(公告)号：US07348326B2
公开(公告)日：2008-03-25
申请号：US11295173
申请日：2005-12-06
申请人： Robert DeSimone , Alan Hutchison , Kenneth Shaw , Daniel Rosewater
发明人： Robert DeSimone , Alan Hutchison , Kenneth Shaw , Daniel Rosewater
IPC分类号： A01N43/58 , A01N43/60 , C07D237/00 , C07D237/02 , C07D513/02
CPC分类号： C07D235/14 , C07D401/06 , C07D405/06 , C07D405/12 , C07D409/12 , C07D471/04
摘要： Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein the A, B, C, D, X, R1, R2, R3, R4, R5, and R6, are variables defined herein, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors, and are therefore useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, depression, overdose with benzodiazepine drugs, and enhancement of memory and alertness.
摘要翻译：公开了下式的化合物或其药学上可接受的无毒盐，其中A，B，C，D，X，R 1，R 2， R 3，R 4，R 5和R 6是本文定义的变量，这些化合物是高度选择性的激动剂，GABAa脑受体的拮抗剂或反向激动剂或GABAa脑受体的激动剂，拮抗剂或反向激动剂的前药，因此可用于诊断和治疗焦虑症，唐氏综合征，睡眠，认知和癫痫发作障碍，抑郁症，苯并二氮卓过量药物，提高记忆力和警觉性。

7. 发明申请

US20060160842A1 Heteroaryl fused aminoalkyl imidazole derivates: selective modulators of GABAA receptors 失效
标题翻译：杂芳基稠合氨基烷基咪唑衍生物：GABA A受体的选择性调节剂
公开(公告)号：US20060160842A1
公开(公告)日：2006-07-20
申请号：US11295173
申请日：2005-12-06
申请人： Robert DeSimone , Alan Hutchison , Kenneth Shaw , Daniel Rosewater
发明人： Robert DeSimone , Alan Hutchison , Kenneth Shaw , Daniel Rosewater
IPC分类号： C07D471/02 , A61K31/4745
CPC分类号： C07D235/14 , C07D401/06 , C07D405/06 , C07D405/12 , C07D409/12 , C07D471/04
摘要： Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein the A, B, C, D, X, R1, R2, R3, R4, R5, and R6, are variables defined herein, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors, and are therefore useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, depression, overdose with benzodiazepine drugs, and enhancement of memory and alertness.
摘要翻译：公开了下式的化合物或其药学上可接受的无毒盐，其中A，B，C，D，X，R 1，R 2， R 3，R 4，R 5和R 6是本文定义的变量，这些化合物是高度选择性的激动剂，GABAa脑受体的拮抗剂或反向激动剂或GABAa脑受体的激动剂，拮抗剂或反向激动剂的前药，因此可用于诊断和治疗焦虑症，唐氏综合征，睡眠，认知和癫痫发作障碍，抑郁症，苯并二氮卓过量药物，提高记忆力和警觉性。

8. 发明申请

US20050288295A1 Certain imidazo[1,2-a]pyrazin-8-ylamines, method of making, and method of use thereof 审中-公开
标题翻译：某些咪唑并[1,2-a]吡嗪-8-基胺，制备方法及其使用方法
公开(公告)号：US20050288295A1
公开(公告)日：2005-12-29
申请号：US10985023
申请日：2004-11-10
申请人： Kevin Currie , Robert DeSimone , Douglas Pippin , James Darrow , Scott Mitchell
发明人： Kevin Currie , Robert DeSimone , Douglas Pippin , James Darrow , Scott Mitchell
IPC分类号： A61K31/498 , C07D487/04
CPC分类号： C07D487/04
摘要： At least one chemical entity chosen from compounds of Formula 1 and pharmaceutically acceptable pharmaceutically acceptable salts, hydrates, solvates, crystal forms, diastereomers, and prodrugs thereof. Methods of treating or preventing disorders in which aberrant kinase activity is implicated, pharmaceutically compositions, and methods for detecting the presence kinases in cells or biological preparations and for identifying kinases of therapeutic interest.
摘要翻译：至少一种选自式1化合物的化学实体及其药学上可接受的药学上可接受的盐，水合物，溶剂化物，晶型，非对映异构体和前药。治疗或预防涉及异常激酶活性的病症的方法，药物组合物和用于检测细胞或生物制剂中存在的激酶以及鉴定治疗感兴趣的激酶的方法。

9. 发明申请

US20060199846A1 Certain substituted ureas as modulators of kinase activity 审中-公开
标题翻译：某些取代的脲类作为激酶活性的调节剂
公开(公告)号：US20060199846A1
公开(公告)日：2006-09-07
申请号：US11331346
申请日：2006-01-13
申请人： Scott Mitchell , Mihaela Danca , Peter Blomgren , Robert DeSimone , Douglas Pippin , David Brittelli
发明人： Scott Mitchell , Mihaela Danca , Peter Blomgren , Robert DeSimone , Douglas Pippin , David Brittelli
IPC分类号： A61K31/4439 , C07D403/02
CPC分类号： C07D401/14 , C07D401/06
摘要： Certain chemical entities chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, crystal forms, chelates, non-covalent complexes, prodrugs, and mixtures thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are also provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to angiogenic kinase modulation, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer, including breast neoplasia, endometrial cancer, colon cancer, and neck squamous cell carcinoma. Methods of treatment include administering at least one chemical entity as a single active agent or administering such at least one chemical entity in combination with one or more other therapeutic agents. A method for determining the presence or absence of an angiogenic kinase in a sample comprising contacting the sample with at least one chemical entity under conditions that permit detection of activity of the angiogenic kinase, detecting a level of the activity of the angiogenic kinase, and therefrom determining the presence or absence of the angiogenic kinase in the sample.
摘要翻译：本文提供了选自式1化合物的某些化学实体及其药学上可接受的盐，溶剂合物，结晶形式，螯合物，非共价复合物，前药及其混合物。本文还提供了包含至少一种化学实体和一种或多种药学上可接受的载体的药物组合物，其选自载体，佐剂和赋形剂。公开了治疗患有对血管生成激酶调节反应的某些疾病和病症的患者的方法，其包括向这些患者施用一定量的至少一种有效减少疾病或病症体征或症状的化学实体。这些疾病包括癌症，包括乳腺肿瘤，子宫内膜癌，结肠癌和颈部鳞状细胞癌。治疗方法包括给予至少一种化学实体作为单一活性剂或者与一种或多种其它治疗剂组合施用这样的至少一种化学实体。一种用于确定样品中存在或不存在血管生成激酶的方法，包括在允许检测血管生成激酶活性，检测血管生成激酶活性水平的条件下将样品与至少一种化学实体接触确定样品中存在或不存在血管生成激酶。

10. 发明申请

US20050054649A1 Certain 8-heteroaryl-6-phenyl-imidazo[1,2-A]pyrazines as modulators of Hsp90 complex activity 有权
标题翻译：某些8-杂芳基-6-苯基 - 咪唑并[1,2-A]吡嗪作为Hsp90复合物活性的调节剂
公开(公告)号：US20050054649A1
公开(公告)日：2005-03-10
申请号：US10776631
申请日：2004-02-10
申请人： Kevin Currie , Robert DeSimone , Douglas Pippin , James Darrow , Scott Mitchell
发明人： Kevin Currie , Robert DeSimone , Douglas Pippin , James Darrow , Scott Mitchell
IPC分类号： A61P35/02 , A61P37/00 , C07D487/04 , A61K31/498
CPC分类号： C07D487/04
摘要： This invention pertains to compounds of Formula I: and the pharmaceutically-acceptable forms thereof. The variables R1, R2, R3, Z1, Z2, W, and X shown in Formula I are defined herein. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or pharmaceutically acceptable form of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain diseases and disorders responsive to Hsp90 complex modulation, which comprise administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These diseases include cancer, including chronic myeloid leukemia, melanoma, breast, ovarian, brain, thyroid, colorectal, prostate, and bladder cancer, heart disease, stroke, autoimmune/inflammatory diseases, and neurodegenerative diseases. Thus methods of treatment include administering a sufficient amount of a compound of Formula I or form thereof to decrease the symptoms or slow the progression of these diseases or disorders. The invention also encompasses methods of treating non-human patients, including livestock and domesticated companion animals, suffering from a disease or disorder responsive to Hsp90 complex modulation. 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. The invention also includes a method for determining the presence of certain kinases or Hsp90 complex in a sample, comprising contacting the sample with a compound of Formula I or form thereof, and detecting Hsp9O complex activity in the sample.
摘要翻译：本发明涉及式I化合物及其药学上可接受的形式。本文定义了式I中所示的变量R1，R2，R3，Z1，Z2，W和X. 本发明还提供含有一种或多种式I化合物或这些化合物的药学上可接受的形式的药物组合物和一种或多种药学上可接受的载体，赋形剂或稀释剂。本发明还包括治疗患有对Hsp90复合物调节有反应的某些疾病和病症的患者的方法，其包括向所述患者施用一定量的有助于减少疾病或病症的体征或症状的式I化合物。这些疾病包括癌症，包括慢性骨髓性白血病，黑素瘤，乳腺癌，卵巢癌，脑，甲状腺，结肠直肠癌，前列腺癌和膀胱癌，心脏病，中风，自身免疫/炎性疾病和神经变性疾病。因此，治疗方法包括施用足量的式I化合物或其形式以减少症状或减缓这些疾病或病症的进展。本发明还包括治疗患有针对Hsp90复合调节的疾病或病症的非人类患者，包括家畜和驯养伴侣动物的方法。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。本发明还包括用于测定样品中某些激酶或Hsp90复合物的存在的方法，包括使样品与式I化合物或其形式接触并检测样品中的Hsp9O复合物活性。

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