公开(公告)号：US5395827A

公开(公告)日：1995-03-07

申请号：US171629

申请日：1993-12-22

申请人： Waclaw J. Rzeszotarski ,  Suzanne R. Ellenberger ,  Maria E. Guzewska ,  John W. Ferkany ,  Gregory S. Hamilton ,  Raymond J. Patch ,  Edward W. Karbon, Jr

发明人： Waclaw J. Rzeszotarski ,  Suzanne R. Ellenberger ,  Maria E. Guzewska ,  John W. Ferkany ,  Gregory S. Hamilton ,  Raymond J. Patch ,  Edward W. Karbon, Jr

IPC分类号： A61K31/66 ,  C07F9/38

CPC分类号： C07F9/3882 ,  A61K31/66 ,  C07F9/3834

摘要： The present invention pertains to antagonists of excitatory amino acid neurotransmitter receptor antagonists, their method of preparation as well as compositions containing them which have the general formula: ##STR1## wherein n and m independently are 0, 1, 2, or 3; R.sub.1 is selected from the group consisting of hydrogen and R.sub.2 ; R.sub.2 is selected from the group consisting of hydrogen, halogen, halomethyl, nitro, amino, alkoxy, hydroxyl, hydroxymethyl, C.sub.1 to C.sub.6 lower alkyl, C.sub.7 to C.sub.12 higher alkyl, aryl and aralkyl, wherein if R.sub.2 is hydrogen, R.sub.1 is not hydrogen; R.sub.3 is selected from the group consisting of hydrogen and C.sub.1 to C.sub.6 lower alkyl; the stereoisomers thereof in their resolved or racemic form, and pharmaceutically acceptable salts thereof.

摘要翻译： 本发明涉及兴奋性氨基酸神经递质受体拮抗剂的拮抗剂，它们的制备方法以及含有它们的组合物，它们具有以下通式：其中n和m独立地是0,1,2或3; R1选自氢和R2; R2选自氢，卤素，卤代甲基，硝基，氨基，烷氧基，羟基，羟甲基，C1至C6低级烷基，C7至C12高级烷基，芳基和芳烷基，其中如果R2是氢，R1不是氢 ; R3选自氢和C1至C6低级烷基; 其立体异构体以其分辨或外消旋形式，及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：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：US07247438B1

公开(公告)日：2007-07-24

申请号：US08948124

申请日：1997-10-09

申请人： Ellis Reinherz ,  Linda Clayton ,  Timothy D. Ocain ,  Raymond J. Patch

发明人： Ellis Reinherz ,  Linda Clayton ,  Timothy D. Ocain ,  Raymond J. Patch

IPC分类号： G01N33/53

CPC分类号： C12N9/6475 ,  A61K38/00

摘要： Methods for identifying agents which enhance the activity of a caspase according to the invention are described, as well as methods for enhancing caspase activity and methods for enhancing apoptosis in a lymphocyte.

摘要翻译： 本发明描述了提高半胱天冬酶活性的试剂的方法，以及增强半胱天冬酶活性的方法和增强淋巴细胞凋亡的方法。

公开(公告)号：US5677343A

公开(公告)日：1997-10-14

申请号：US467725

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 naphthalene-sulfonic 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：US5614559A

公开(公告)日：1997-03-25

申请号：US245619

申请日：1994-05-19

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 naphthalene-sulfonic 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合聚合物可以消除结合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：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：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.