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1. 发明申请

WO2006081332A1 SUBSTITUTED ARYLAMINE COMPOUNDS AND THEIR USE AS 5-HT6 MODULATORS 审中-公开
标题翻译：取代的芳基胺化合物及其作为5-HT6调节剂的用途
公开(公告)号：WO2006081332A1
公开(公告)日：2006-08-03
申请号：PCT/US2006/002718
申请日：2006-01-25
申请人： PREDIX PHARMACEUTICALS HOLDINGS, INC. , BECKER, Oren , LOBERA, Mercedes , MELENDEZ, Rosa E. , SHARADENDU, Anurag , WU, Laurence , YU, Xiang, Y. , DHANOA, Dale, S. , CHERUKU, Srinivasa, Rao , MARANTZ, Yael , NOIMAN, Silvia , FICHMAN, Merav , SENDEROWITZ, Hanoch , SHACHAM, Sharon , SAHA, Ashis , ORBACH, Pini
发明人： BECKER, Oren , LOBERA, Mercedes , MELENDEZ, Rosa E. , SHARADENDU, Anurag , WU, Laurence , YU, Xiang, Y. , DHANOA, Dale, S. , CHERUKU, Srinivasa, Rao , MARANTZ, Yael , NOIMAN, Silvia , FICHMAN, Merav , SENDEROWITZ, Hanoch , SHACHAM, Sharon , SAHA, Ashis , ORBACH, Pini
IPC分类号： C07D295/12 , A61K31/495 , A61K31/496 , C07D243/08 , C07D311/68 , C07D317/62 , C07D319/18 , C07D333/66
CPC分类号： C07D295/135 , C07D207/14 , C07D211/58 , C07D243/08 , C07D311/68 , C07D317/62 , C07D319/18 , C07D333/66 , C07D405/12
摘要： The invention relates to 5-HT 6 receptor antagonists. Novel arylamine compounds having the formula: (see formula I) and pharmaceutically acceptable salts and/or esters thereof, wherein - n is 0, 1, 2, 3, or 4; - A, when present is a lower alkyl group; - R 1 is hydrogen or substituted or unsubstituted alkyl or aryl; - R 2 is hydrogen; halo; nitro; cyano, lower alkoxy; carboxylate salt acid or alkyl ester thereof; a sulfone; haloalkyl or haloalkoxy; acetaldehyde; carboxamide; carbomyl; alkoxyaminocarbonyl; or substituted arylalkylamino; - R 3 and R 4 independently are hydrogen, substituted or unsubstituted alkyl, aryl, alkylaryl, heteroaryl or alkylheteroaryl, or, taken together, R 3 and R 4 form one substituted or unsubstituted aryl, alkylaryl, heteroaryl or alkylheteroaryl group; - B, when present, is lower alkyl; and - X and Y are independently C or N; and use of these compounds and their pharmaceutical compositions, e.g. , in the treatment, modulation and/or prevention of physiological conditions associated with serotonin action, such as in treating obesity, and obesity-related disorders, e.g. , cardiovascular disease, digestive disease, respiratory disease, cancer and type II diabetes; and psychological disorders such as schizophrenia, are disclosed.
摘要翻译：本发明涉及5-HT 6受体拮抗剂。具有下式的新型芳基胺化合物（参见式I）及其药学上可接受的盐和/或酯，其中n为0,1,2,3或4; A存在时为低级烷基; R 1是氢或取代或未取代的烷基或芳基; R 2是氢; 光环; 硝基; 氰基，低级烷氧基; 羧酸盐酸或其烷基酯; 一个砜; 卤代烷基或卤代烷氧基; 乙醛; 甲酰胺; carbomyl; 烷氧基氨基羰; 或取代的芳烷基氨基; R 3和R 4独立地是氢，取代或未取代的烷基，芳基，烷基芳基，杂芳基或烷基杂芳基，或者一起是R 3 >和R 4形成一个取代或未取代的芳基，烷基芳基，杂芳基或烷基杂芳基; 当存在时，B是低级烷基; 且X和Y独立地为C或N; 以及这些化合物及其药物组合物的用途，例如用于治疗，调节和/或预防与5-羟色胺作用相关的生理条件，例如治疗肥胖症和肥胖相关疾病，例如心血管疾病，消化系统疾病，呼吸系统疾病疾病，癌症和II型糖尿病; 和精神分裂症等心理障碍。

2. 发明申请

WO2002048312A3 BACKBONE CYCLIZED INHIBITORS OF HEAT SHOCK PROTEINS 审中-公开
公开(公告)号：WO2002048312A3
公开(公告)日：2002-06-20
申请号：PCT/IL2001/001144
申请日：2001-12-11
申请人： PEPTOR LTD. , ELIAS, Dana , AVRON, Ann , SENDEROWITZ, Hanoch
发明人： ELIAS, Dana , AVRON, Ann , SENDEROWITZ, Hanoch
IPC分类号： A61K38/12
摘要： Novel peptide analogs which are backbone cyclized peptide antagonists of heat shock proteins are disclosed as well as methods for synthesizing them. Pharmaceutical compositions comprising backbone cyclized peptide antagonists of heat shock protein 60, and methods of using such compositions for treatment, prevention and diagnosis of inflammatory, antoimmune and infectious disorders are also disclosed.

3. 发明申请

WO0248312A2 BACKBONE CYCLIZED INHIBITORS OF HEAT SHOCK PROTEINS 审中-公开
标题翻译：背部循环抑制剂的热休克蛋白
公开(公告)号：WO0248312A2
公开(公告)日：2002-06-20
申请号：PCT/IL0101144
申请日：2001-12-11
申请人： PEPTOR LTD , ELIAS DANA , AVRON ANN , SENDEROWITZ HANOCH
发明人： ELIAS DANA , AVRON ANN , SENDEROWITZ HANOCH
IPC分类号： A61K38/00 , C07K14/195 , C07K14/35 , C07K14/47 , C12N
CPC分类号： C07K14/4713 , A61K38/00 , C07K14/195 , C07K14/35
摘要： Novel peptide analogs which are backbone cyclized peptide antagonists of heat shock proteins are disclosed as well as methods for synthesizing them. Pharmaceutical compositions comprising backbone cyclized peptide antagonists of heat shock protein 60, and methods of using such compositions for treatment, prevention and diagnosis of inflammatory, antoimmune and infectious disorders are also disclosed.
摘要翻译：公开了作为热休克蛋白的骨架环化肽拮抗剂的新型肽类似物以及合成它们的方法。还公开了包含热休克蛋白60的骨架环化肽拮抗剂的药物组合物，以及使用这些组合物治疗，预防和诊断炎性，免疫和感染性疾病的方法。

4. 发明申请

WO2003010281A3 PROTEIN KINASE INHIBITORS COMPRISING ATP MIMETICS CONJUGATED TO PEPTIDES OR PEPTIDOMIMETICS 审中-公开
公开(公告)号：WO2003010281A3
公开(公告)日：2003-02-06
申请号：PCT/IL2002/000618
申请日：2002-07-25
申请人： PEPTOR LTD. , LIVNAH, Nurit , YECHEZKEL, Tamar , SALITRA, Yosef , PERLMUTTER, Boris , OHNE, Onsat , COHEN, Ilana , LITMAN, Pninit , SENDEROWITZ, Hanoch
发明人： LIVNAH, Nurit , YECHEZKEL, Tamar , SALITRA, Yosef , PERLMUTTER, Boris , OHNE, Onsat , COHEN, Ilana , LITMAN, Pninit , SENDEROWITZ, Hanoch
IPC分类号： A61K31/47
摘要： The present invention provides small molecules having high affinity to the ATP binding site of protein kinases, which are conjugated to apeptide or peptidomimetic moiety which mimics the substrate of PKB. The chimeric compounds according to the present invention preferably serve as PKB inhibitors with improved activity and selectivity. Novel ATP mimetic compounds , particularly isoquinoline derivatives, conjugated with peptides or peptidomimetics are useful as inhibitors of protein kinases for experimental, medical, and drug design purposes. Furthermore, pharmaceutical compositions comprising these protein kinase inhibitors, and methods of using such compositions for treatment and diagnosis of cancers, diabetes, cardiovascular pathologies, hemorrhagic shock, obesity, inflammatory diseases, diseases of the central nervous system, and autoimmune disease, are disclosed.

5. 发明申请

WO2003010281A2 PROTEIN KINASE INHIBITORS COMPRISING ATP MIMETICS CONJUGATED TO PEPTIDES OR PEPTIDOMIMETICS 审中-公开
标题翻译：蛋白激酶抑制剂，包含ATP模拟物与肽或多肽的结合物
公开(公告)号：WO2003010281A2
公开(公告)日：2003-02-06
申请号：PCT/IL2002/000618
申请日：2002-07-25
申请人： PEPTOR LTD. , LIVNAH, Nurit , YECHEZKEL, Tamar , SALITRA, Yosef , PERLMUTTER, Boris , OHNE, Onsat , COHEN, Ilana , LITMAN, Pninit , SENDEROWITZ, Hanoch
发明人： LIVNAH, Nurit , YECHEZKEL, Tamar , SALITRA, Yosef , PERLMUTTER, Boris , OHNE, Onsat , COHEN, Ilana , LITMAN, Pninit , SENDEROWITZ, Hanoch
IPC分类号： C12N
CPC分类号： C07K7/06 , A61K38/00 , A61K47/64
摘要： The present invention provides small molecules having high affinity to the ATP binding site of protein kinases, which are conjugated to apeptide or peptidomimetic moiety which mimics the substrate of PKB. The chimeric compounds according to the present invention preferably serve as PKB inhibitors with improved activity and selectivity. Novel ATP mimetic compounds , particularly isoquinoline derivatives, conjugated with peptides or peptidomimetics are useful as inhibitors of protein kinases for experimental, medical, and drug design purposes. Furthermore, pharmaceutical compositions comprising these protein kinase inhibitors, and methods of using such compositions for treatment and diagnosis of cancers, diabetes, cardiovascular pathologies, hemorrhagic shock, obesity, inflammatory diseases, diseases of the central nervous system, and autoimmune disease, are disclosed.
摘要翻译：本发明提供对蛋白激酶的ATP结合位点具有高亲和力的小分子，其与模拟PKB底物的肽或拟肽部分缀合。根据本发明的嵌合化合物优选用作具有改善的活性和选择性的PKB抑制剂。与肽或肽模拟物缀合的新型ATP模拟化合物，特别是异喹啉衍生物可用作实验，医学和药物设计目的的蛋白激酶抑制剂。此外，公开了包含这些蛋白激酶抑制剂的药物组合物，以及使用这些组合物治疗和诊断癌症，糖尿病，心血管病变，失血性休克，肥胖症，炎性疾病，中枢神经系统疾病和自身免疫性疾病的方法。

6. 发明申请

WO1996012168A2 A RAPIDLY CONVERGENT METHOD FOR BOLTZMANN-WEIGHTED ENSEMBLE GENERATION IN FREE ENERGY SIMULATIONS 审中-公开
标题翻译：一种用于自由能量模拟中的BOLTZMANN-WEIGHTING ENSEMBLE GENERATION的快速融合方法
公开(公告)号：WO1996012168A2
公开(公告)日：1996-04-25
申请号：PCT/US1995012926
申请日：1995-10-06
申请人： THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK , STILL, W., Clark , GUARNIERI, Frank , SENDEROWITZ, Hanoch
发明人： THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK
IPC分类号： G01N00/00
CPC分类号： C07K1/00 , G06F19/701
摘要： The invention is directed to a method for generating possible conformations of a molecule comprising the steps of: a) selecting a first conformation of the molecule characterized by a first set of coordinates associated with each atom in the molecule by the presence of a pattern of forces among such atoms and by a series of intrinsic forces associated with each atom; b) varying the pattern of forces among such atoms in a non-random manner and randomly varying the series of intrinsic forces associated with each atom so as to generate a second conformation of the molecule characterized by a second set of coordinates associated with each atom in the molecule, by a second pattern of forces among each atom and by a second series of intrinsic forces associated with each atom; and c) randomly varying the second set of coordinates so as to obtain a third set of coordinates and thereby generating such possible conformations of the molecule.
摘要翻译：本发明涉及一种用于产生分子的可能构象的方法，包括以下步骤：a）选择分子的第一构象，所述第一构象的特征在于通过存在力图形的分子中与每个原子相关联的第一组坐标在这些原子之间以及与每个原子相关联的一系列内在力; b）以非随机方式改变这些原子之间的力的模式并且随机地改变与每个原子相关联的一系列内在力，以便产生分子的第二构象，其特征在于与每个原子相关联的第二组坐标分子，通过每个原子之间的第二个力图案和与每个原子相关联的第二系列内在力; 以及c）随机地改变所述第二组坐标以获得第三组坐标，从而产生所述分子的这种可能的构象。

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