公开(公告)号：US07608622B2

公开(公告)日：2009-10-27

申请号：US11233725

申请日：2005-09-23

申请人： Jian Liu ,  Raymond J. Patch ,  Mark R. Player ,  Huaping Hu

发明人： Jian Liu ,  Raymond J. Patch ,  Mark R. Player ,  Huaping Hu

IPC分类号： A01N43/58 ,  A61K31/50 ,  A01N43/60 ,  A61K31/495 ,  C07D471/00 ,  C07D487/00 ,  C07D491/00 ,  C07D495/00 ,  C07D497/00

CPC分类号： C07D487/04

摘要： The invention is directed to compounds of Formula I: wherein Q, Y, A are set forth in the specification, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof, that inhibit protein kinases, especially Aurora-1, Aurora-2 and Aurora-3 kinases.

摘要翻译： 本发明涉及式I化合物：其中Q，Y，A在本说明书中列出，以及其抑制蛋白激酶，特别是Aurora-1，Aurora-2的溶剂合物，水合物，互变异构体或其药学上可接受的盐 和Aurora-3激酶。

公开(公告)号：US07790724B2

公开(公告)日：2010-09-07

申请号：US11407605

申请日：2006-04-20

申请人： Mark R. Player ,  Nand Baindur ,  Benjamin Brandt ,  Naresh Chadha ,  Raymond J. Patch ,  Davoud Asgari ,  Taxiarchis M. Georgiadis

发明人： Mark R. Player ,  Nand Baindur ,  Benjamin Brandt ,  Naresh Chadha ,  Raymond J. Patch ,  Davoud Asgari ,  Taxiarchis M. Georgiadis

IPC分类号： A61K31/4439 ,  C07D403/02

CPC分类号： C07D405/12 ,  C07D307/68 ,  C07D409/12

摘要： The invention is directed to compounds of Formula II: wherein A, R1, R2, R3, R4, X, Y and W are set forth in the specification, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase.

摘要翻译： 本发明涉及式II化合物：其中A，R 1，R 2，R 3，R 4，X，Y和W在说明书中列出，以及其抑制蛋白质的溶剂合物，水合物，互变异构体或其药学上可接受的盐 酪氨酸激酶，特别是c-fms激酶。

公开(公告)号：US07427683B2

公开(公告)日：2008-09-23

申请号：US10970865

申请日：2004-10-22

申请人： Mark R. Player ,  Nand Baindur ,  Benjamin Brandt ,  Naresh Chadha ,  Raymond J. Patch ,  Davoud Asgari ,  Taxiarchis Georgiadis

发明人： Mark R. Player ,  Nand Baindur ,  Benjamin Brandt ,  Naresh Chadha ,  Raymond J. Patch ,  Davoud Asgari ,  Taxiarchis Georgiadis

IPC分类号： A61K31/454 ,  C07D401/12

CPC分类号： C07D405/12 ,  C07D207/416 ,  C07D233/90 ,  C07D307/68 ,  C07D409/12

摘要： The invention is directed to compounds of Formulae I: wherein A, R1, R2, R3, R4, X, and W are set forth in the specification, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase.

摘要翻译： 本发明涉及式I的化合物：其中A，R 1，R 2，R 3，R 4， 说明书中列出了SUB，X和W，以及其抑制蛋白酪氨酸激酶，特别是c-fms激酶的溶剂合物，水合物，互变异构体或其药学上可接受的盐。

公开(公告)号：US07429603B2

公开(公告)日：2008-09-30

申请号：US10831216

申请日：2004-04-26

申请人： Mark R. Player ,  Nand Baindur ,  Benjamin Brandt ,  Naresh Chadha ,  Raymond J. Patch ,  Davoud Asgari ,  Taxiarchis M. Georgiadis

发明人： Mark R. Player ,  Nand Baindur ,  Benjamin Brandt ,  Naresh Chadha ,  Raymond J. Patch ,  Davoud Asgari ,  Taxiarchis M. Georgiadis

IPC分类号： C07D405/02 ,  A61K31/445

CPC分类号： C07D213/81 ,  C07D231/38 ,  C07D265/02 ,  C07D307/68 ,  C07D307/71 ,  C07D405/12 ,  C07D491/04

摘要： The invention is directed to compounds of Formulae I, II and III: wherein A, R1, R2, R3, R4, X, Y and W are set forth in the specification, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase.

摘要翻译： 本发明涉及式I，II和III的化合物：其中A，R 1，R 2，R 3，R SUB 说明书中列出了X，Y和W，以及抑制蛋白酪氨酸激酶，特别是c-fms激酶的溶剂合物，水合物，互变异构体或其药学上可接受的盐。

公开(公告)号：US06365625B1

公开(公告)日：2002-04-02

申请号：US09398571

申请日：1999-09-17

申请人： Shyam K. Singh ,  Raymond J. Patch ,  Peter V. Pallai ,  Edith A. Neidhardt ,  Gerard P. Palace ,  Kevin J. Willis ,  Theresa M. Sampo ,  Kevin W. McDonald ,  Zhan Shi

发明人： Shyam K. Singh ,  Raymond J. Patch ,  Peter V. Pallai ,  Edith A. Neidhardt ,  Gerard P. Palace ,  Kevin J. Willis ,  Theresa M. Sampo ,  Kevin W. McDonald ,  Zhan Shi

IPC分类号： A61K31185

CPC分类号： A61K31/795

摘要： This invention pertains to the discovery that condensation polymers of an aldehyde and aromatic sulfonic acids and fractions thereof, such as formaldehyde naphthalenesulfonic acid condensation polymers, can abrogate HIV gp120 binding to CD4, as demonstrated in CD4/gp120 binding assays. In addition to gp120 binding inhibition, the compounds have been shown to inhibit HIV-induced syncytia formation and infectivity of CD+ cells. The use of this compound has been shown to be non-cytotoxic and non-inhibitory to antigen induced T lymphocyte proliferation. Based on these findings, these compounds can be used as a therapeutic agent for the treatment of acquired immunodeficiency syndrome (AIDS), as well as AIDS-related complex (ARC), AIDS-related dementia and non-symptomatic HIV infection. The compounds can also be used to treat blood preparations.

摘要翻译： 本发明涉及如下发现：如在CD4 / gp120结合测定中所证明的，醛和芳族磺酸的缩合聚合物及其部分如甲醛萘磺酸缩聚物可以消除结合CD4的HIV gp120。 除了gp120结合抑制之外，已经显示这些化合物抑制HIV诱导的合胞体形成和CD +细胞的感染性。 这种化合物的使用已被证明是非细胞毒性的，并且对抗原诱导的T淋巴细胞增殖是不抑制的。 基于这些发现，这些化合物可用作治疗获得性免疫缺陷综合征（AIDS）以及艾滋病相关综合征（ARC），AIDS相关性痴呆和无症状性艾滋病毒感染的治疗剂。 该化合物也可用于治疗血液制剂。

公开(公告)号：US5596095A

公开(公告)日：1997-01-21

申请号：US440547

申请日：1995-05-12

申请人： John C. Roberts ,  Raymond J. Patch

发明人： John C. Roberts ,  Raymond J. Patch

IPC分类号： C07C303/02 ,  C07C303/24 ,  C07C309/74 ,  C07D311/72 ,  C07D501/20 ,  C07J31/00 ,  C07J41/00 ,  C07D501/60 ,  A61K31/545

CPC分类号： C07C309/77 ,  C07C303/02 ,  C07C303/28 ,  C07D311/72 ,  C07J31/006 ,  C07J41/0055 ,  Y02P20/55

摘要： The present invention is a method of protecting a sulfonic acid functional group in an organic molecule as a substituted or unsubstituted neopentyl sulfonate ester. The method allows the conversion of R--SO.sub.3 --H to R'--SO.sub.3 --H, wherein R and R' are different organic radicals. Also disclosed is a method of increasing the bioavailability of drugs with a sulfonic acid functional group by protecting the sulfonic acid functional group as a substituted neopentyl sulfonate ester which has a masked heteroatom nucleophile. The masked nucleophile can be liberated in vivo, resulting in removal of the neopentyl protecting group and regeneration of the parent drug.

摘要翻译： 本发明是保护作为取代或未取代的新戊基磺酸酯的有机分子中的磺酸官能团的方法。 该方法允许将R-SO 3 -H转化为R'-SO3-H，其中R和R'是不同的有机基团。 还公开了通过保护磺酸官能团作为具有掩蔽的杂原子亲核试剂的取代的新戊基磺酸酯来提高具有磺酸官能团的药物的生物利用度的方法。 掩蔽的亲核试剂可以在体内释放，导致新戊基保护基的去除和母体药物的再生。

公开(公告)号：US5189046A

公开(公告)日：1993-02-23

申请号：US709948

申请日：1991-06-04

申请人： Ronald M. Burch ,  Raymond J. Patch ,  Barry G. Shearer ,  John J. Perumattam

发明人： Ronald M. Burch ,  Raymond J. Patch ,  Barry G. Shearer ,  John J. Perumattam

IPC分类号： C07D207/09 ,  C07D211/26 ,  C07D211/60 ,  C07D401/12

CPC分类号： C07D401/12 ,  C07D207/09 ,  C07D211/26 ,  C07D211/60

摘要： PKC modulating compounds of the formula ##STR1## Also disclosed are pharmaceutical compositions including these compounds which inhibit PKC activity, methods of using these compounds to inhibit PKC activity in mammals, and intermediates useful in preparing the PKC modulating compounds.

摘要翻译： PKC调节下式化合物（I）还公开了包含抑制PKC活性的这些化合物的药物组合物，使用这些化合物抑制哺乳动物PKC活性的方法，以及可用于制备PKC调节化合物的中间体。

公开(公告)号：US6075050A

公开(公告)日：2000-06-13

申请号：US467728

申请日：1995-06-06

申请人： Shyam K. Singh ,  Raymond J. Patch ,  Peter V. Pallai ,  Edith A. Neidhardt ,  Gerard P. Palace ,  Kevin J. Willis ,  Theresa M. Sampo ,  Kevin W. McDonald ,  Zhan Shi

发明人： Shyam K. Singh ,  Raymond J. Patch ,  Peter V. Pallai ,  Edith A. Neidhardt ,  Gerard P. Palace ,  Kevin J. Willis ,  Theresa M. Sampo ,  Kevin W. McDonald ,  Zhan Shi

IPC分类号： A61K31/795 ,  A61P31/12 ,  A61P31/18 ,  A61K31/185 ,  C07C309/32 ,  C07C309/35

CPC分类号： A61K31/795

摘要： This invention pertains to the discovery that condensation polymers of an aldehyde and aromatic sulfonic acids and fractions thereof, such as formaldehyde naphthalenesulfonic acid condensation polymers, can abrogate HIV gp120 binding to CD4, as demonstrated in CD4/gp120 binding assays. In addition to gp120 binding inhibition, the compounds have been shown to inhibit HIV-induced syncytia formation and infectivity of CD+ cells. The use of this compound has been shown to be non-cytotoxic and non-inhibitory to antigen induced T lymphocyte proliferation. Based on these findings, these compounds can be used as a therapeutic agent for the treatment of acquired immunodeficiency syndrome (AIDS), as well as AIDS-related complex (ARC), AIDS-related dementia and non-symptomatic HIV infection. The compounds can also be used to treat blood preparations.

公开(公告)号：US20110237625A1

公开(公告)日：2011-09-29

申请号：US12899812

申请日：2010-10-07

申请人： Michael Gaul ,  Alexander Kim ,  Lily Lee Searle ,  Raymond J. Patch ,  Dionisios Rentzeperis ,  Guozhang Xu ,  Xizhen Zhu

发明人： Michael Gaul ,  Alexander Kim ,  Lily Lee Searle ,  Raymond J. Patch ,  Dionisios Rentzeperis ,  Guozhang Xu ,  Xizhen Zhu

IPC分类号： A61K31/454 ,  C07D277/34 ,  A61K31/426 ,  C07D263/44 ,  A61K31/421 ,  A61P19/00 ,  A61P11/00 ,  A61P35/00 ,  A61P3/00 ,  A61P9/12

CPC分类号： C07D277/34 ,  C07D263/44

摘要： The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacia, osteoporosis, Paget's disease, periodontal disease, polymyalgia rheumatica, Reiter's syndrome, repetitive stress injury, hyperglycemia, elevated blood glucose level, and insulin resistance.

摘要翻译： 本发明涉及式（I）化合物，制备这些化合物的方法，组合物，中间体及其衍生物，用于治疗包括但不限于强直性脊柱炎，动脉粥样硬化，关节炎（如类风湿性关节炎，感染性关节炎，儿童期 关节炎，牛皮癣关节炎，反应性关节炎），骨相关疾病（包括与骨形成相关的疾病），乳腺癌（包括对抗雌激素治疗无反应的那些），心血管疾病，软骨相关疾病（如软骨损伤/损失， 软骨变性和与软骨形成相关的软骨变性，软骨发育不全，软骨肉瘤，慢性背部损伤，慢性支气管炎，慢性炎症性气道疾病，慢性阻塞性肺病，糖尿病，能量稳态障碍，痛风，假性血糖，脂质障碍，代谢综合征，多发性 骨髓瘤，肥胖症，骨关节炎，成骨不全，骨质溶解骨 骨质疏松症，骨质疏松症，佩吉特氏病，牙周病，风湿性多肌痛，莱特综合征，重复性应激损伤，高血糖症，升高的血糖水平和胰岛素抵抗。

公开(公告)号：US20090111855A1

公开(公告)日：2009-04-30

申请号：US12043269

申请日：2008-03-06

申请人： Michael Gaul ,  Alexander Kim ,  Lily Lee Searle ,  Raymond J. Patch ,  Dionisios Rentzeperis ,  Guozhang Xu ,  Xizhen Zhu

发明人： Michael Gaul ,  Alexander Kim ,  Lily Lee Searle ,  Raymond J. Patch ,  Dionisios Rentzeperis ,  Guozhang Xu ,  Xizhen Zhu

IPC分类号： A61K31/454 ,  C07D277/34 ,  A61K31/426 ,  A61K31/421 ,  C07D263/44 ,  A61P3/04

CPC分类号： C07D277/34 ,  C07D263/44

摘要： The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacia, osteoporosis, Paget's disease, periodontal disease, polymyalgia rheumatica, Reiter's syndrome, repetitive stress injury, hyperglycemia, elevated blood glucose level, and insulin resistance.

摘要翻译： 本发明涉及式（I）化合物，制备这些化合物的方法，组合物，中间体及其衍生物，用于治疗包括但不限于强直性脊柱炎，动脉粥样硬化，关节炎（如类风湿性关节炎，感染性关节炎，儿童期 关节炎，牛皮癣关节炎，反应性关节炎），骨相关疾病（包括与骨形成相关的疾病），乳腺癌（包括对抗雌激素治疗无反应的那些），心血管疾病，软骨相关疾病（如软骨损伤/损失， 软骨变性和与软骨形成相关的软骨变性，软骨发育不全，软骨肉瘤，慢性背部损伤，慢性支气管炎，慢性炎症性气道疾病，慢性阻塞性肺病，糖尿病，能量稳态障碍，痛风，假性血糖，脂质障碍，代谢综合征，多发性 骨髓瘤，肥胖症，骨关节炎，成骨不全，骨质溶解骨 骨质疏松症，骨质疏松症，佩吉特氏病，牙周病，风湿性多肌痛，莱特综合征，重复性应激损伤，高血糖，升高的血糖水平和胰岛素抵抗。