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1. 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。

2. 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。

3. 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。

4. 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。

5. 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。

6. 发明授权

US5470848A 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：US5470848A
公开(公告)日：1995-11-28
申请号：US139684
申请日：1993-10-22
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 , A61K31/56 , A61K31/04 , A61K31/40 , A61K31/445
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 through the skin or mucosal membranes of humans and animals and into the bloodstream in a transdermal device or formulation comprising topically administrating with said systemic agent an effective amount of a membrane penetration enhancer having the structural formula ##STR1## or the pharmaceutically acceptable salt thereof wherein W represents oxygen, sulfur or two hydrogen radicals; Z represents --CH.sub.2 --; R represents alkyl optionally substituted with one to three double or triple bonds, --SR"', --OR"', --NHR"', or --COOR.sub.1 ; R"' represents alkyl, alkylthioalkyl, alkoxyalkyl, amino alkyl, optionally substituted with a phenyl, or benzoyl; R' represents hydrogen, alkyl, alkoxy, acyloxy, alkylthio, hydroxy or --(CH.sub.2).sub.y COOR.sub.1 ; R" represents hydrogen or --(CH.sub.2).sub.y COOR.sub.1 ; R.sub.1, in each instance, independently represents hydrogen or lower alkyl; y, in each instance, is between zero and 3, inclusive; m is between one and 3, inclusive; n is between one and 24, inclusive; and x is zero or one, inclusive;with the provisos 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. It has been found that the penetration enhancers 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并以透皮装置或制剂进入血流的方法，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W表示氧，硫或两个氢原子; Z表示-CH 2 - ; R代表任选被一至三个双键或三键-SR“，-OR”'，-NHR“'或-COOR 1取代的烷基; R“表示任选被苯基或苯甲酰基取代的烷基，烷硫基烷基，烷氧基烷基，氨基烷基; R'表示氢，烷基，烷氧基，酰氧基，烷硫基，羟基或 - （CH2）yCOOR1; R“表示氢或 - （CH 2）y COOR 1; 在每种情况下，R 1独立地表示氢或低级烷基; 在每种情况下，y在0和3之间，包括0和3之间; m在1和3之间，包括1和3; n在1到24之间，包括1和24; x为0或1（含）; 条件是当R“是氢时，则W是两个氢原子并且R'不是氢; 当R'为氢时，R“不为氢。已经发现穿透增强剂足以携带生理活性剂通过体膜并进入血流。

7. 发明授权

US5430056A Substituted 2-aminotetralins 失效
标题翻译：取代的2-氨基鸟嘌呤
公开(公告)号：US5430056A
公开(公告)日：1995-07-04
申请号：US200338
申请日：1994-02-23
申请人： James V. Peck , Gevork Minaskanian
发明人： James V. Peck , Gevork Minaskanian
IPC分类号： C07C215/64 , C07C217/16 , C07C217/74 , C07D307/88 , A61K31/34 , C07D307/81 , C07D307/83
CPC分类号： C07C217/16 , C07C215/64 , C07C217/74 , C07D307/88 , C07C2102/08 , C07C2102/10
摘要： Optically active or racemic compounds are provided having the formula ##STR1## where R.sub.1 is ##STR2## where Y is hydrogen, halogen or C.sub.1 to C.sub.6 linear or branched alkyl; R.sub.6 is C.sub.1 to C.sub.4 linear or branched alkyl; X is oxygen or sulfur; a is an integer from zero to 3; and n is an integer from 1 to 4. The compounds are capable of binding selectively to dopamine D.sub.2 receptors and are useful in treatment of disorders of the central nervous, cardiovascular and endocrine systems, such as intraocular pressure, schizophrenia and Parkinsonism, and for inducing anorexia and weight loss in humans and other mammals.
摘要翻译：提供具有式（IMAGE）的光学活性或外消旋化合物，其中R1是或者IMA图，其中Y是氢，卤素或C1-C6直链或支链烷基; R6是C1-C4直链或支链烷基; X是氧或硫; a是从零到3的整数; 并且n是1至4的整数。化合物能够选择性结合多巴胺D2受体，并且可用于治疗中枢神经，心血管和内分泌系统的疾病，例如眼内压，精神分裂症和帕金森综合征，以及诱导人类和其他哺乳动物的厌食和体重减轻。

8. 发明授权

US5358971A Substituted 2-aminotetralins 失效
标题翻译：取代的2-氨基鸟嘌呤
公开(公告)号：US5358971A
公开(公告)日：1994-10-25
申请号：US131845
申请日：1993-10-04
申请人： James V. Peck , Gevork Minaskanian
发明人： James V. Peck , Gevork Minaskanian
IPC分类号： C07C215/64 , C07C217/16 , C07C217/74 , C07D307/88 , A61K31/135 , C07C217/10
CPC分类号： C07C215/64 , C07C217/16 , C07C217/74 , C07D307/88 , C07C2102/08 , C07C2102/10
摘要： Optically active or racemic compounds are provided having the formula ##STR1## where R.sub.2, R.sub.3 and R.sub.4 are selected from the group consisting of H and OA with the provision that at least one of R.sub.2, R.sub.3 and R.sub.4 is H, that R.sub.2 and R.sub.4 are not both OA; A is H or is selected from the group consisting of hydrocarbyl radicals, said hydrocarbyl radicals being further optionally substituted with radicals selected from the group consisting of ##STR2## R.sub.5 is selected from the group consisting of alkyl and aromatic residues, preferably radicals having between 1 and 12 carbon atoms, including alkyl, alkyl substituted with aryl radicals, and aryl radicals substituted with alkyl radicals; n is an integer between 1 and 4; R.sub.6 is an alkyl chain comprising between 1 and 4 carbon atoms; X is oxygen; and R.sub.1 is selected from the group consisting of ##STR3## wherein Y is as defined in the specification, and a is an integer of from zero to 3.These compounds are useful in treatment of disorders of the central nervous, cardiovascular, and endocrine systems, such as for inducing anorexia and weight loss in humans.
摘要翻译：提供具有式“IMAGE”的光学活性或外消旋化合物，其中R2，R3和R4选自H和OA，条件是R2，R3和R4中的至少一个为H，R2和R4为不是OA; A是H或选自烃基，所述烃基进一步任选被选自以下的基团取代：R 5选自烷基和芳族残基，优选具有1个和12个碳原子，包括烷基，被芳基取代的烷基和被烷基取代的芳基; n是1到4之间的整数; R6是包含1至4个碳原子的烷基链; X是氧; 并且R 1选自，其中Y如说明书中所定义，a是0-3的整数。这些化合物可用于治疗中枢神经，心血管和内分泌系统的病症，例如用于诱导人类的厌食和体重减轻。

9. 发明授权

US5274003A Substituted 2-aminotetralins 失效
标题翻译：取代的2-氨基鸟嘌呤
公开(公告)号：US5274003A
公开(公告)日：1993-12-28
申请号：US837229
申请日：1992-02-18
申请人： James V. Peck , Gevork Minaskanian
发明人： James V. Peck , Gevork Minaskanian
IPC分类号： C07C215/64 , C07C217/16 , C07C217/74 , C07D307/88 , A61K31/135 , C07C217/14 , C07C217/24
CPC分类号： C07C217/16 , C07C215/64 , C07C217/74 , C07D307/88 , C07C2102/08 , C07C2102/10
摘要： Optically active or racemic compounds are provided having the formula ##STR1## where R.sub.2, R.sub.3 and R.sub.4 are each selected from the group consisting of H and OH with the provision that at least one of R.sub.2, R.sub.3 and R.sub.4 is H, that R.sub.2 and R.sub.4 are not both OH; X is oxygen; and R.sub.1 is selected from the group consisting of ##STR2## wherein Z is oxygen, nitrogen or sulfur, wherein Y is selected from the group consisting of hydroxy, nitro, cyano, azido, amino, acylamino, carboxyamido, trifluoromethyl, sulfate, sulfonamido, halogen, hydrocarbyl and heteroatom-substituted hydrocarbyl radicals, wherein said heteroatoms are selected from the group consisting of halogen, nitrogen, oxygen, sulfur and phosphorus and said hydrocarbyl radicals comprise from 1 to 12 carbon atoms, and a is an integer of from zero to 3. These compounds are capable of binding selectivity of one or more dopamine D.sub.2 receptors, for instance, in humans. They are useful in treatment of disorders of the central nervous, cardiovascular, and endocrine systems, such as elevated intraocular pressure, schizophrenia and Parkinsonism, and for inducing anorexia and weight loss in humans and other mammals.
摘要翻译：提供具有式“IMAGE”的光学活性或外消旋化合物，其中R2，R3和R4各自选自H和OH，条件是R2，R3和R4中的至少一个为H，R2和R4 不是OH; X是氧; 其中Z是氧，氮或硫，其中Y选自羟基，硝基，氰基，叠氮基，氨基，酰基氨基，羧酰胺基，三氟甲基，硫酸根，亚磺酰氨基，卤素，烃基和杂原子取代的烃基，其中所述杂原子选自卤素，氮，氧，硫和磷，所述烃基包含1至12个碳原子，并且a是0至3的整数。这些化合物能够结合一种或多种多巴胺D2受体的选择性，例如在人中。它们可用于治疗中枢神经，心血管和内分泌系统的疾病，例如眼内压升高，精神分裂症和帕金森综合征，以及诱导人类和其他哺乳动物的厌食和体重减轻。

10. 发明授权

US5256647A Compositions comprising 1-substituted azacycloalkanes 失效
标题翻译：包含1-取代的氮杂环烷烃的组合物
公开(公告)号：US5256647A
公开(公告)日：1993-10-26
申请号：US611612
申请日：1990-11-13
申请人： Gevork Minaskanian , James V. Peck , Eric L. Nelson
发明人： Gevork Minaskanian , James V. Peck , Eric L. Nelson
IPC分类号： A01N25/02 , A01N43/36 , A01N43/40 , A01N43/62 , A61K9/00 , A61K47/22 , B01J31/02 , C05G3/00 , C07D223/10 , D06P1/642 , A01N43/04 , A61K7/42 , A61K7/44 , A61K9/02 , A61K9/06 , A61K9/10 , A61K9/12 , A61K31/70
CPC分类号： A61K9/0014 , A01N25/02 , A01N43/36 , A01N43/40 , A01N43/62 , A61K47/22 , C05G3/00 , C07D223/10 , D06P1/6426 , Y10S424/05 , Y10S424/10 , Y10S424/13 , Y10S514/844 , Y10S514/846 , Y10S514/858 , Y10S514/859 , Y10S514/861 , Y10S514/862 , Y10S514/863 , Y10S514/864 , Y10S514/88
摘要： This invention provides compositions comprising a physiologically-active agent and a compound having the structural formula ##STR1## wherein X may represent sulfur or two hydrogen atoms; R' is H or a lower alkyl group having 1-4 carbon atoms; m is 2-6; n is 0-18 and R is --CH.sub.3, ##STR2## wherein R" is H or halogen, in an amount effective to enhance the penetration of the physiologically-active agent through the skin or other membrane of the body of an animal.
摘要翻译：本发明提供了包含生理活性剂和具有结构式的化合物的组合物，其中X可以表示硫或两个氢原子; R'是H或具有1-4个碳原子的低级烷基; m为2-6; n是0-18，R是-CH 3，或者，其中R“是H或卤素，其量可以有效地增强生理活性剂通过身体的皮肤或其他膜的渗透的动物

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