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1. 发明授权

US5670501A N-substituted 9-alkyladenines 失效
标题翻译： N-取代的9-烷基腺嘌呤
公开(公告)号：US5670501A
公开(公告)日：1997-09-23
申请号：US299992
申请日：1994-09-01
申请人： James V. Peck , Ronald J. Wysocki , Ibrahim M. Uwaydah , Noel J. Cusack
发明人： James V. Peck , Ronald J. Wysocki , Ibrahim M. Uwaydah , Noel J. Cusack
IPC分类号： A61K31/52 , A61P7/10 , A61P9/00 , A61P13/02 , A61P15/00 , A61P25/02 , C07D473/34 , A61K31/535 , C07D317/72
CPC分类号： C07D473/34
摘要： Optically active or racemic compounds represented by the formula ##STR1## where R.sub.1 is C.sub.1 to C.sub.4 straight chain or branched alkyl; R.sub.2 is selected from the group consisting of H, --OR.sub.1, --SR.sub.1, --NH(R.sub.1), --N(R.sub.4)(R.sub.5), aminocarbonyl, halogen, and --CN, where R.sub.4 and R.sub.5 are independently C.sub.1 to C.sub.6 straight chain or branched alkyl, or taken together form a 3- to 7-membered heterocycloalkyl substituent, such heteroatom selected from the group consisting of oxygen, nitrogen and sulfur, optionally including an additional heteroatom which is selected from the group consisting of nitrogen, oxygen, and sulfur; R.sub.3 is cyclopentyl or: ##STR2## where R' and R" are independently H, .dbd.O, --OH, or --NH.sub.2, with the proviso that R' and R" can be taken together form the following structure as R.sub.3 : ##STR3## where R'" is --OH or --NH.sub.2 ; and with the further proviso that when R.sub.3 is cyclopentyl or norbornyl, then R.sub.2 cannot be H or halogen; and pharmaceutically-acceptable salts thereof. These compounds are useful as diuretics, renal protectives against acute or chronic renal failure, as well as agents to facilitate recovery from coma, to improve the therapeutic outcome resulting from defibrillation or cardiopulmonary resuscitation by preventing post-resuscitation bradycardia, bradyarrhythmia and cardioplegia, to restore cardiac function following a cardioplegic procedure, and to treat or prevent intermittent claudication.
摘要翻译：其中R 1为C 1至C 4直链或支链烷基的式（ⅩⅧ）表示的光学活性或外消旋化合物; R2选自H，-OR1，-SR1，-NH（R1），-N（R4）（R5），氨基羰基，卤素和-CN，其中R4和R5独立地为C1-C6直链或支链烷基，或一起形成3-至7-元杂环烷基取代基，这种选自氧，氮和硫的杂原子，任选地包括另外的杂原子，其选自氮，氧和硫; R3是环戊基或：其中R'和R“独立地是H，= O，-OH或-NH 2，条件是R'和R”可以一起形成如下结构：R3：其中R“是-OH或-NH 2; 并且进一步的条件是当R 3是环戊基或降冰片基时，则R 2不能是H或卤素; 及其药学上可接受的盐。这些化合物可用作利尿剂，抗急性或慢性肾功能衰竭的肾脏保护剂，以及促进从昏迷恢复的药剂，以改善由除颤或心肺复苏引起的治疗结果，通过防止复苏后心动过缓，缓慢心律失常和心脏停搏恢复心脏停搏手术后的心脏功能，治疗或预防间歇性跛行。

2. 发明授权

US5981524A Substituted 9-alkyladenines 失效
标题翻译：取代的9-烷基腺嘌呤
公开(公告)号：US5981524A
公开(公告)日：1999-11-09
申请号：US904553
申请日：1997-08-04
申请人： James V. Peck , Ronald J. Wysocki , Ibrahim M. Uwaydah , Noel J. Cusack
发明人： James V. Peck , Ronald J. Wysocki , Ibrahim M. Uwaydah , Noel J. Cusack
IPC分类号： A61K31/52 , A61P7/10 , A61P9/00 , A61P13/02 , A61P15/00 , A61P25/02 , C07D473/34 , A61K31/535 , C07D317/72
CPC分类号： C07D473/34
摘要： Optically active or racemic compounds represented by the formula ##STR1## where R.sub.1 is C.sub.1 to C.sub.4 straight chain or branched alkyl; R.sub.2 is selected from the group consisting of H, --OR.sub.1, --SR.sub.1, --NH(R.sub.1), --N(R.sub.4)(R.sub.5), aminocarbonyl, halogen, and --CN, where R.sub.4 and R.sub.5 are independently C.sub.1 to C.sub.6 straight chain or branched alkyl, or taken together form a 3- to 7-membered heterocycloalkyl substituent, such heteroatom selected from the group consisting of oxygen, nitrogen and sulfur, optionally including an additional heteroatom which is selected from the group consisting of nitrogen, oxygen, and sulfur; R.sub.3 is cyclopentyl or: ##STR2## where R' and R" are independently H, .dbd.O, --OH, or --NH.sub.2, with the proviso that R' and R" can be taken together form the following structure as R.sub.3 : ##STR3## where R'" is --OH or --NH.sub.2 ; and with the further proviso that when R.sub.3 is cyclopentyl or norbornyl, then R.sub.2 cannot be H or halogen; and pharmaceutically-acceptable salts thereof.These compounds are useful as diuretics, renal protectives against acute or chronic renal failure, as well as agents to facilitate recovery from coma, to improve the therapeutic outcome resulting from defibrillation or cardiopulmonary resuscitation by preventing post-resuscitation bradycardia, bradyarrhythmia and cardioplegia, to restore cardiac function following a cardioplegic procedure, and to treat or prevent intermittent claudication.
摘要翻译：由下式表示的光学活性或外消旋化合物，其中R 1为C 1至C 4直链或支链烷基; R2选自H，-OR1，-SR1，-NH（R1），-N（R4）（R5），氨基羰基，卤素和-CN，其中R4和R5独立地为C1-C6直链或支链烷基，或一起形成3-至7-元杂环烷基取代基，该杂原子选自氧，氮和硫，任选地包括另外的杂原子，其选自氮，氧和硫; R 3是环戊基或：其中R'和R“独立地是H，= O，-OH或-NH 2，条件是R'和R”可以一起形成如下R3的结构：其中R' “是-OH或-NH 2; 并且进一步的条件是当R 3是环戊基或降冰片基时，则R 2不能是H或卤素; 及其药学上可接受的盐。这些化合物可用作利尿剂，抗急性或慢性肾功能衰竭的肾脏保护剂，以及促进从昏迷恢复的药剂，以改善由除颤或心肺复苏引起的治疗结果，通过防止复苏后心动过缓，缓慢心律失常和心脏停搏恢复心脏停搏手术后的心脏功能，治疗或预防间歇性跛行。

3. 发明授权

US5444075A Penetration enhancers for transdermal delivery of systemic agents 失效
标题翻译：用于透皮递送全身药物的渗透增强剂
公开(公告)号：US5444075A
公开(公告)日：1995-08-22
申请号：US326353
申请日：1994-10-20
申请人： Gevork Minaskanian , James V. Peck
发明人： Gevork Minaskanian , James V. Peck
IPC分类号： A01N37/44 , A01N43/36 , A01N43/40 , A01N43/46 , A61K47/22 , C05G3/00 , C07C233/47 , C07D207/16 , C07D207/26 , C07D207/27 , C07D207/28 , C07D223/10 , C07D263/22 , C07D295/15 , D06P1/642 , A61K31/445 , A61K31/135 , A61K31/155 , A61K31/195 , A61K31/34 , A61K31/40 , A61K31/44 , A61K31/56 , A61K47/00
CPC分类号： C07D207/27 , A01N37/44 , A01N43/36 , A01N43/40 , A01N43/46 , A61K47/22 , A61K9/0014 , C05G3/00 , C07C233/47 , C07D207/16 , C07D207/28 , C07D223/10 , C07D263/22 , C07D295/15 , D06P1/6426 , Y10S514/947
摘要： This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals and into the blood stream in a transdermal device or formulation comprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer.
摘要翻译：本发明涉及一种通过人和动物的皮肤或粘膜施用全身活性剂，包括治疗剂的方法，并且在透皮装置或制剂中进入血流中，该方法包括与所述全身药剂局部施用有效量的膜渗透增强剂。

4. 发明授权

US5283343A 2-aryl substituted N-acetyltryptamines and process of preparing such 失效
标题翻译： 2-芳基取代的N-乙酰基色胺及其制备方法
公开(公告)号：US5283343A
公开(公告)日：1994-02-01
申请号：US718342
申请日：1991-06-18
申请人： Margarita L. Dubocovich , Vithal J. Rajadhyaksha , James V. Peck , Atef A. Helmy
发明人： Margarita L. Dubocovich , Vithal J. Rajadhyaksha , James V. Peck , Atef A. Helmy
IPC分类号： A61K31/40 , C07D209/16
CPC分类号： A61K31/40
摘要： This invention relates to novel melatonin derivatives, such as 2-aryl substituted N-acetyltryptamines, having pharmacological activity, e.g., melatonin antagonist activity, and methods for the synthesis thereof.
摘要翻译：本发明涉及具有药理学活性的新的褪黑激素衍生物，例如具有药理学活性的2-芳基取代的N-乙酰基色胺，例如褪黑激素拮抗剂活性，及其合成方法。

5. 发明授权

US5234959A Penetration enhancers for transdermal delivery of systemic agents 失效
标题翻译：渗透增强剂用于系统性试剂的转运
公开(公告)号：US5234959A
公开(公告)日：1993-08-10
申请号：US611613
申请日：1990-11-13
申请人： Gevork Minaskanian , James V. Peck
发明人： Gevork Minaskanian , James V. Peck
IPC分类号： A01N37/44 , A01N43/36 , A01N43/40 , A01N43/46 , A61K47/22 , C05G3/00 , C07C233/47 , C07D207/16 , C07D207/26 , C07D207/27 , C07D207/28 , C07D223/10 , C07D263/22 , C07D295/15 , D06P1/642
CPC分类号： C07D207/27 , A01N37/44 , A01N43/36 , A01N43/40 , A01N43/46 , A61K47/22 , A61K9/0014 , C05G3/00 , C07C233/47 , C07D207/16 , C07D207/28 , C07D223/10 , C07D263/22 , C07D295/15 , D06P1/6426 , Y10S514/947
摘要： This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals and into the blood stream in a transdermal device or formulation comprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer being a carboxylic acid derivative or a salt thereof represented in one embodiment by the general formula ##STR1## wherein W represents oxygen, sulfur, or two hydrogen radicals; wherein Z represents oxygen, sulfur, or --CH.sub.2 --;wherein R represents alkyl optionally substituted with one to three double or triple bonds, --SR'", --OR'", --NHR'", --CH.sub.3, or COOR.sub.1, and wherein R.sub.1 represents hydrogen or lower alkyl;wherein R'" represents alkyl, alkylthioalkyl, alkoxyalkyl, substituted aminoalkyl, optionally substituted with a phenyl, benzoyl or heterocyclic group;wherein R' represents hydrogen, alkyl, alkoxy, acyloxy, alkylthio, hydroxy, --(CH2).sub.y COOR.sub.1 and with y being between zero and 3, inclusive;and wherein R" represents hydrogen or --(CH2).sub.y COOR.sub.1 such that when R" is hydrogen, then W is two hydrogen radicals and R' is not hydrogen; and when R' is hydrogen, then R" is not hydrogen;and wherein m is between one and 5, preferably 2, 3, or 4, while n is between 1 and 24, preferably between 5 and 12, and x is zero or 1, inclusive.It has been found that both open and closed-chain embodiments of the penetration enhancer are sufficient to carry physiologically active agents through body membranes and into the bloodstream.
摘要翻译：本发明涉及一种通过人和动物的皮肤或粘膜施用全身活性剂，包括治疗剂的方法，并且在透皮装置或制剂中进入血流中，该方法包括与所述全身药剂局部施用有效量的膜渗透增强剂在一个实施方案中通过通式“IMAGE”表示的羧酸衍生物或其盐，其中W表示氧，硫或两个氢原子; 其中Z表示氧，硫或-CH 2 - ; 其中R表示任选被一至三个双键或三键-SR“，-OR”'，-NHR“'，-CH 3或COOR 1取代的烷基，并且其中R 1表示氢或低级烷基; 其中R“表示任选被苯基，苯甲酰基或杂环基取代的烷基，烷硫基烷基，烷氧基烷基，取代氨基烷基; 其中R'表示氢，烷基，烷氧基，酰氧基，烷硫基，羟基， - （CH2）yCOOR1，y在0和3之间，并且其中R“表示氢或 - （CH 2）y COOR 1，使得当R”为氢时，则W为两个氢原子并且R'不为氢; 当R'为氢时，R“不为氢; 并且其中m为1至5，优选2,3或4，而n为1至24，优选5至12，x为0或1，包括端值。已经发现穿透增强剂的开放和闭合两个实施方案足以将生理活性剂携带通过体膜并进入血流。

6. 发明授权

US4920101A Compositions comprising 1-oxo- or thiohydrocarbyl substituted azacycloaklkanes 失效
标题翻译：包含1-氧代或硫代烃基取代的氮杂环丁烷的组合物
公开(公告)号：US4920101A
公开(公告)日：1990-04-24
申请号：US103445
申请日：1987-09-30
申请人： Gevork Minaskanian , James V. Peck
发明人： Gevork Minaskanian , James V. Peck
IPC分类号： C07D295/18 , A61K31/12 , A61K31/16 , A61K31/33 , A61K31/505 , A61K31/55 , A61K45/00 , A61K47/22 , A61P31/00 , A61P31/04 , C07D225/02
CPC分类号： A61K47/22 , A61K9/0014 , Y10S514/946 , Y10S514/947
摘要： This invention provides compositions comprising a physiologically-active agent and a compound represented by the general formula ##STR1## wherein X may represent sulfur, oxygen or 2 hydrogen radicals; Y may represent --CH.sub.2 --, --NH-- or oxygen; n and m are integers of from 1 to 3; p is an integer of from 3 to 17; q is 2, 4, 6 or 8; wherein p.gtoreq.9; and R' is selected from the group consisting of H, a lower alkyl group having from 1 to 4 carbon atoms, phenyl, lower alkyl or halogen substituted phenyl, acetamido, halogen, piperidinyl, lower alkyl or halogen substituted piperidinyl, carbalkoxy, carboxamide, and alkanoyl. These compositions are useful in topical or transdermal applications of the physiologically-active agent.
摘要翻译：本发明提供了包含生理活性剂和由通式“IMAGE”表示的化合物的组合物，其中X可以表示硫，氧或2个氢原子; Y可以表示-CH 2 - ， - NH-或氧; n和m为1〜3的整数; p为3〜17的整数。 q是2,4,6或8; 其中p> / = 9; R'选自H，具有1至4个碳原子的低级烷基，苯基，低级烷基或卤素取代的苯基，乙酰氨基，卤素，哌啶基，低级烷基或卤素取代的哌啶基，烷氧羰基，羧酰胺，和烷酰基。这些组合物可用于生理活性剂的局部或透皮应用。

7. 发明授权

US4886783A Penetration enhancers for transdermal delivery of systemic agents 失效
标题翻译：用于透皮递送全身药物的渗透增强剂
公开(公告)号：US4886783A
公开(公告)日：1989-12-12
申请号：US233551
申请日：1988-08-17
申请人： Gevork Minaskanian , James V. Peck
发明人： Gevork Minaskanian , James V. Peck
IPC分类号： A01N25/02 , A01N37/32 , A01N43/46 , A61K47/22 , C05G3/00
CPC分类号： A61K47/22 , A01N25/02 , A01N37/32 , A01N43/46 , A61K9/0014 , C05G3/00 , Y10S514/919 , Y10S514/946 , Y10S514/947
摘要： This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals in a transdermal device or formulation comprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer having the structural formula ##STR1## wherein each X, Y and Z may represent oxygen, sulfur or two hydrogen atoms, provided however that, when Z represents two hydrogen atoms, both X and Y represent oxygen or sulfur and when Z represents oxygen or sulfur at least one of X and Y must represent oxygen or sulfur; m is 2-6; R' is H or a lower alkyl group having 1-4 carbon atoms; n is 0-16 and R is --CH.sub.3, ##STR2## wherein R" is H or halogen.
摘要翻译：本发明涉及一种通过透皮装置或制剂的人和动物的皮肤或粘膜施用全身活性剂的方法，所述方法包括与所述全身药剂局部施用有效量的具有结构式的膜渗透增强剂，其中每个X，Y和Z可以表示氧，硫或两个氢原子，但是当Z表示两个氢原子时，X和Y都表示氧或硫，并且当Z表示氧或硫时，X， Y必须代表氧或硫; m为2-6; R'是H或具有1-4个碳原子的低级烷基; n为0-16且R为-CH 3，其中R“为H或卤素。

8. 发明授权

US4870173A Lactam formation by a selective cyclization process 失效
标题翻译：通过选择性环化过程形成内酰胺
公开(公告)号：US4870173A
公开(公告)日：1989-09-26
申请号：US847464
申请日：1986-04-03
申请人： Gevork Minaskanian , James V. Peck
发明人： Gevork Minaskanian , James V. Peck
IPC分类号： C07D205/08 , C07D207/26 , C07D207/277 , C07D211/78 , C07D223/10
CPC分类号： C07D207/277 , C07D205/08 , C07D211/78 , C07D223/10
摘要： This invention provides a process for preparing lactams, by selectively reacting a novel 1-hydrocarbyl-amino (or heteroatom-substituted hydrocarbylamino); 1,1-dicarboxylic acid, alkylesters; 1-hydrocarbyl (or heteroatom-substituted hydrocarbyl) carboxylic acid, alkyl ester methane, as the salt of an acid having a pKa of 0 or more, in the absence or presence of a base, whereby novel lactams wherein one or both hydrocarbyl moieties are incorporated into the lactam ring are obtained. That is, the acid moiety of said novel salt promotes the reaction whereby both hydrocarbyl moieties are incorporated into the ring, while the presence of a base, in an amount substantially equivalent to said acid promotes the reaction whereby only one hydrocarbyl is incorporated into the ring.
摘要翻译：本发明提供了一种制备内酰胺的方法，通过选择性地使新的1-烃基 - 氨基（或杂原子取代的烃基氨基） 1,1-二羧酸，烷基酯; 1-烷基（或杂原子取代的烃基）羧酸烷基酯甲烷，作为pKa为0或更大的酸的盐，在不存在或存在碱的情况下，其中新的内酰胺，其中一个或两个烃基部分是加入内酰胺环。也就是说，所述新型盐的酸部分促进反应，由此将两个烃基部分并入环中，而碱的存在量基本上等于所述酸促进反应，从而仅将一个烃基引入环中。

9. 发明授权

US10251844B2 Transdermal therapeutic system and method of use thereof for treating parkinsonism 有权
公开(公告)号：US10251844B2
公开(公告)日：2019-04-09
申请号：US11931762
申请日：2007-10-31
申请人： Walter Müller , James V. Peck
发明人： Walter Müller , James V. Peck
IPC分类号： A61K9/70 , A61K31/381
摘要： A substantially solvent-free matrix layer containing (−)-5,6,7,8-tetrahydro-6-[propyl-[2-(2-thienyl)ethyl]amino]-1-naphthalenol is produced by adding an active substance to an adhesive solution, coating the resultant active substance-containing adhesive solution onto a suitable sheet, and removing the solvents in a drying process to give said substantially solvent-free matrix layer.

10. 发明授权

US6086905A Topical compositions useful as skin penetration barriers 失效
标题翻译：用作皮肤渗透屏障的局部组合物
公开(公告)号：US6086905A
公开(公告)日：2000-07-11
申请号：US102176
申请日：1993-08-04
申请人： James V. Peck , Gevork Minaskanian , Jonathan Hadgraft
发明人： James V. Peck , Gevork Minaskanian , Jonathan Hadgraft
IPC分类号： A61K8/49 , A61K31/17 , A61K31/4164 , A61K31/4166 , A61K31/421 , A61K31/426 , A61K31/535 , A61K31/55 , A61K31/553 , A61Q17/00 , A01N25/32
CPC分类号： A61K31/553 , A61K31/17 , A61K31/4164 , A61K31/4166 , A61K31/421 , A61K31/426 , A61K31/535 , A61K31/55 , A61K8/49 , A61Q17/00
摘要： Methods for preventing the penetration of toxic chemicals through the stratum corneum of the skin of a mammal are disclosed which employ, as a penetration prevention agent, at least one compound selected from the group consisting of compounds represented by the formula: ##STR1## wherein W.sub.1 is a divalent oxygen, sulfur or nitrogen radical, W.sub.2 and W.sub.3 are independently a divalent oxygen or sulfur radical, R' is an alkyl radical comprising from 1 to 4 carbon atoms, y is 0 or 1, R.sub.1 and R.sub.2 are alkyl radicals comprising from 1 to 10 carbon atoms and R and R.sub.3 are individually a hydrocarbyl radical containing from 1 to 20 carbon atoms or a heteroatom-substituted derivative thereof wherein at least one but not two adjacent carbon atoms may be replaced by a divalent oxygen or sulfur radical or by NR", wherein R" is hydrogen or R', n is an integer from 2 to 5 and compounds represented by the above formula in which the ring and/or R includes one to three carbon carbon double bonds.
摘要翻译：公开了防止有毒化学物质穿过哺乳动物皮肤角质层渗透的方法，其中使用至少一种选自由下式表示的化合物的化合物作为防渗剂，其中W1为二价氧，硫或氮基团，W2和W3独立地是二价氧或硫基团，R'是包含1至4个碳原子的烷基，y是0或1，R 1和R 2是包含1至10个的烷基碳原子，R和R 3分别是含有1至20个碳原子的烃基或其杂原子取代的衍生物，其中至少一个但不是两个相邻的碳原子可被二价氧或硫基取代，或被NR“ 其中R“为氢或R'，n为2至5的整数和由上式表示的化合物，其中环和/或R包括一至三个碳碳双键。

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