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1. 发明授权

US5908846A Topical compositions for transdermal delivery of prodrug derivatives of morphine 失效
标题翻译：用于经皮递送吗啡前药衍生物的局部组合物
公开(公告)号：US5908846A
公开(公告)日：1999-06-01
申请号：US50336
申请日：1993-08-17
申请人： Hans Bundgaard, deceased , Lona Christrup , Jorn Drustrup , Ann Fullerton , Martin Nicklasson
发明人： Hans Bundgaard, deceased , Lona Christrup , Jorn Drustrup , Ann Fullerton , Martin Nicklasson
IPC分类号： A61K9/00 , A61K20060101 , A61K31/485 , A61P25/04 , C07D489/02 , A61K9/70 , A61K47/00
CPC分类号： A61K31/485 , Y10S514/817 , Y10S514/946 , Y10S514/947
摘要： Topical composition for transdermal delivery of morphine. The composition contains certain morphine esters in association with a carrier. The compositions relieved pain or tranquilize a mammal when delivered transdermally.
摘要翻译： PCT No.PCT / SE91 / 00760 Sec。 371日期：1993年8月17日 102（e）日期1993年8月17日PCT 1991年11月11日PCT PCT。公开号WO92 / 08459 日期1992年5月29日吗啡经皮给药吗？该组合物含有与载体结合的某些吗啡酯。当经皮递送时，该组合物可缓解疼痛或使哺乳动物平静化。

2. 发明授权

US5405834A Prodrug derivatives of thyrotropin-releasing hormone (TRH) 失效
标题翻译：促甲状腺激素释放激素（TRH）的前药衍生物
公开(公告)号：US5405834A
公开(公告)日：1995-04-11
申请号：US842181
申请日：1992-03-20
申请人： Hans Bundgaard , Judi Moss
发明人： Hans Bundgaard , Judi Moss
IPC分类号： A61K38/22 , A61K38/00 , A61K38/04 , A61P5/00 , A61P5/12 , C07K1/113 , C07K5/08 , C07K5/097 , C07K7/04 , A61K37/24 , A61K37/43
CPC分类号： C07K5/0825 , A61K38/00
摘要： Compounds of formula (I), wherein R.sub.1 is selected from the group consisting of an alkyl group, an aralkyl group, an alkenyl group, a cycloalkyl group, in which the alkyl, aralkyl, alkenyl or cycloalkyl group is unsubstituted or substituted with one or more substituents selected from the group consisting of a halogen atom, e.g. Cl or Br, a hydroxyl group or a straight or branched-chain alkoxy group containing from 1 to 6 carbon atoms; and the pharmaceutically acceptable acid addition salts thereof. Such compounds are prodrugs of TRH and are characterized by having a higher lipophilicity than TRH and possessing a high resistance toward degradation by TRH-inactivating enzymes. Such compounds will after administration be converted into TRH.
摘要翻译： PCT No.PCT / DK90 / 00228 Sec。 371日期：1992年3月20日 102（e）1992年3月20日PCT PCT 1990年9月3日PCT公布。第WO91 / 03487号公报 1991年3月21日。式（I）化合物，其中R 1选自烷基，芳烷基，烯基，环烷基，其中烷基，芳烷基，烯基或环烷基是未取代的或被一个或多个选自以下的取代基取代：卤素原子，例如， Cl或Br，含有1至6个碳原子的羟基或直链或支链烷氧基; 及其药学上可接受的酸加成盐。这些化合物是TRH的前药，其特征在于具有比TRH更高的亲油性，并且通过TRH灭活酶具有高度降解的抗性。给药后，这些化合物转化为TRH。

3. 发明授权

US5306841A Derivatives of inositol, preparations containing them and their use 失效
标题翻译：肌醇的衍生物，含有它们的制剂及其用途
公开(公告)号：US5306841A
公开(公告)日：1994-04-26
申请号：US955708
申请日：1993-07-02
申请人： Hans Bundgaard, deceased , by Charlotte Bundgaard, legal representative
发明人： Hans Bundgaard, deceased , by Charlotte Bundgaard, legal representative
IPC分类号： A61K31/66 , A61K31/661 , A61K31/6615 , A61P43/00 , C07F9/117 , C07F9/40 , C07F9/144
CPC分类号： C07F9/117 , C07F9/4075
摘要： A compound having the formula ##STR1## where X is a radical of myo-inositol or a radical of a configuration isomer thereof where at least one R is ##STR2## where Y is (1) oxygen, (2) a straight or branched alkyl with 1-10 carbon atoms, where Z is ##STR3## where A.sup.1 and A.sup.2 are the same or different and are hydrogen or methyl and n is 3-10, or ##STR4## where A.sup.1 and A.sup.2 are hydrogen or methyl and where m is 1-5, where R.sup.1 is hydrogen, straight or branched alkyl, aryl or alkaryl, alkoxy or aryloxy, where R.sup.2 is(1) R.sup.1,(2) hydroxyl, or(3) OZOCOR.sup.1,and where the remaining R is/are hydroxyl.
摘要翻译： PCT No.PCT / SE92 / 00489 Sec。 371日期：1993年7月2日 102（e）日期1993年7月2日PCT提交1992年6月30日PCT公布。公开号WO93 / 01197 日本1993年1月21日。具有式（*化学结构*）的化合物，其中X是肌醇的基团或其构型异构体的基团，其中至少一个R是（*化学结构*），其中Y是（1）氧，（2）具有1-10个碳原子的直链或支链烷基，其中Z是（* CHEMICAL STRUCTURE *），其中A1和A2相同或不同，为氢或甲基，n为3-10，或（*化学结构*）其中A1和A2是氢或甲基，其中m是1-5，其中R1是氢，直链或支链烷基，芳基或烷芳基，烷氧基或芳氧基，其中R2是（1）R1，（ 2）羟基或（3）OZOCOR1，其中R为羟基。

4. 发明授权

US5017571A Carbamic acid ester of substituted 7-hydroxy-2,3,4,5-tetrahydro-1H-3-benzazepines 失效
标题翻译：取代的7-羟基-2,3,4,5-四氢-1H-3-苯并吖庚因的氨基甲酸酯
公开(公告)号：US5017571A
公开(公告)日：1991-05-21
申请号：US317016
申请日：1989-02-28
申请人： Kristian T. Hansen , Hans Bundgaard , Peter Faarup
发明人： Kristian T. Hansen , Hans Bundgaard , Peter Faarup
IPC分类号： C07D223/16 , A61K31/55 , A61P25/00 , C07D401/04 , C07D403/12 , C07D405/04 , C07D409/04
CPC分类号： C07D401/04 , C07D405/04 , C07D409/04
摘要： Compounds having the formula ##STR1## wherein R.sup.1, R.sup.4, R.sup.6, R.sup.7, and R.sup.8 are hydrogen or a substituent, R.sup.2 is a substituent, R.sup.5 is an optionally-substituted bicyclic ring system, especially a 7-benzofuranyl or 2,3-dihydrobenzofuran-7-yl substituent, R.sup.9 is hydrogen, alkyl, alkoxycarbonyl or, together with R.sup.8, forms the remainder of a heterocyclic ring, their pharmaceutically-accceptable salts, as well as their pharmaceutical compositions and use as prodrugs for compounds active for the treatment of mental disorders, are disclosed.

5. 发明授权

US4482722A Ester of metronidazole with N,N-dimethylglycine and acid addition salt thereof 失效
标题翻译：甲硝唑酯与N，N-二甲基甘氨酸及其酸加成盐
公开(公告)号：US4482722A
公开(公告)日：1984-11-13
申请号：US502210
申请日：1983-06-08
申请人： Pia Thorbek , Hans Bundgaard , Claus Larsen
发明人： Pia Thorbek , Hans Bundgaard , Claus Larsen
IPC分类号： C07D233/94 , C07D233/95
CPC分类号： C07D233/94
摘要： N,N-dimethylglycine ester of metronidazole, acid addition salt thereof and method of preparing such ester or acid addition salt. The novel compounds exhibit favorable solubility in water and are especially useful for the parenteral treatment of certain anaerobic infections.
摘要翻译：甲硝唑的N，N-二甲基甘氨酸酯，其酸加成盐和制备这种酯或酸加成盐的方法。新型化合物在水中表现出良好的溶解性，特别适用于肠胃外处理某些厌氧菌感染。

6. 发明授权

US5073641A Prodrug derivatives of carboxylic acid drugs 失效
标题翻译：羧甲基纤维素的制剂衍生物
公开(公告)号：US5073641A
公开(公告)日：1991-12-17
申请号：US188407
申请日：1988-04-26
申请人： Hans Bundgaard , Niels M. Nielsen
发明人： Hans Bundgaard , Niels M. Nielsen
IPC分类号： A61K31/00 , A61K31/395 , A61K31/397 , A61K31/40 , A61K31/495 , A61P43/00 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/12 , C07C313/00 , C07C325/00 , C07C401/00 , C07D205/04 , C07D207/00 , C07D207/16 , C07D207/26 , C07D207/263 , C07D207/34 , C07D209/28 , C07D211/00 , C07D211/16 , C07D211/46 , C07D295/12 , C07D295/13 , C07D295/18 , C07D295/185 , C07D307/52 , C07D499/00
CPC分类号： C07D207/27 , C07D207/16 , C07D207/34 , C07D209/28 , C07D211/46 , C07D295/13 , C07D295/185 , C07D307/52 , C07D499/00
摘要： Novel ester derivatives of carboxylic acid medicaments of formula (I), wherein R--COO--represents the acyloxy residue of a carboxylic acid drug or medicament, n is an integrer from 1 to 3, and R.sub.1 and R.sub.2 are the same or different and are selected from a group consisting of an alkyl, an alkenyl, an aryl, an aralkyl, a cycloalkyl and which group may be unsubstituted or substituted, or R.sub.1 and R.sub.2 together with the N forms a 4-, 5-, 6- or 7-membered heterocyclic ring, which in addition to the nitrogen atom may contain one or two further heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur and which heterocyclic group may be substituted. These compounds are highly biolabile prodrug forms of the corresponding carboxylic acid compounds and are highly susceptible to undergoing enzymatic hydrolysis in vivo whereas they are highly stable in aqueous solution. The novel derivatives are less irritating to mucosa than the parent carboxylic acids and may provide an improved bio-availability of the drugs.
摘要翻译： PCT No.PCT / DK87 / 00104 Sec。 371日期：1988年4月26日 102（e）日期1988年4月26日PCT提交1987年8月25日PCT公布。出版物WO88 / 01615 （I）式（I）的羧酸药物的新型酯衍生物，其中R-COO-代表羧酸药物或药物的酰氧基残基，n是1至 3，并且R 1和R 2相同或不同，并且选自烷基，烯基，芳基，芳烷基，环烷基，该基团可以是未取代的或取代的，或者R 1和R 2与N 形成4-，5-，6-或7-元杂环，其除了氮原子可以含有一个或两个另外的选自氮，氧和硫的杂原子，哪些杂环基可以被取代。这些化合物是相应的羧酸化合物的高度不可逆的前药形式，并且在体内经历酶水解高度敏感，而在水溶液中它们是高度稳定的。新型衍生物比母体羧酸对粘膜的刺激性较小，并且可提供药物的改善的生物利用度。

7. 发明授权

US4742073A Pilocarpine prodrugs 失效
公开(公告)号：US4742073A
公开(公告)日：1988-05-03
申请号：US533646
申请日：1983-09-16
申请人： Hans Bundgaard , Erik Falch , Claus S. Larsen , Thomas J. Mikkelson
发明人： Hans Bundgaard , Erik Falch , Claus S. Larsen , Thomas J. Mikkelson
IPC分类号： A61K31/415 , A61P27/02 , A61P27/06 , C07D233/54 , C07D233/64 , C07D263/04
CPC分类号： C07D233/64
摘要： Compounds are disclosed of the general formula I ##STR1## wherein R.sub.1 is a group of the formula IIR.sub.3 --X-- IIwherein R.sub.3 is alkyl; phenyl; phenyl substituted with halogen, lower alkyl, hydroxy, lower alkoxy, or phenoxy; phenyl-lower alkyl in which the phenyl group may be substituted with halogen, lower alkyl, hydroxy, lower alkoxy, or phenoxy; phenyl-lower alkenyl in which the phenyl group may be substituted with halogen, lower alkyl, hydroxy, lower alkoxy or phenoxy; and X is oxygen or sulfur; or R.sub.1 is a group of the formula III ##STR2## wherein R.sub.4 has the same meaning as R.sub.3 as defined above; or R.sub.4 is a group of the formula IV ##STR3## wherein R.sub.7 has the same meaning as R.sub.3 as defined above; or R.sub.7 is an aromatic 5- or 6-membered heterocyclic ring containing one or two heteroatoms selected from the group consisting of nitrogen, oxygen, and sulfur; and wherein R.sub.5 and R.sub.6 are the same or different and each represent hydrogen or have the same meaning as R.sub.3 as defined above;or R.sub.1 is a group of the formula V ##STR4## wherein R.sub.5 and R.sub.6 are as defined above and R.sub.8 is polyhalogenated lower alkyl or a group of the formula VI ##STR5## wherein R.sub.3 is as defined above; or R.sub.1 is a group of the formula VII ##STR6## wherein R.sub.10 and R.sub.11 together with the adjacent nitrogen atom form a 5- or 6-membered heterocyclic ring, which in addition to the nitrogen may contain one or two further heteroatoms selected from the group consisting of nitrogen, oxygen, and sulfur;or R.sub.1 is a group of the formula VIII ##STR7## wherein R.sub.13 is a group of the formula II, wherein R.sub.3 and X are as defined above; or R.sub.13 is a group of the formula VIIa ##STR8## wherein R.sub.16 and R.sub.17 are the same or different and each represent hydrogen or have the same meaning as R.sub.3 as defined above; or R.sub.13 is a group of the formula VII, wherein R.sub.10 and R.sub.11 are as defined above;or R.sub.1 is a group of the formula IX ##STR9## wherein R.sub.13 is as defined above; and R.sub.2 is hydrogen or a group of the formula IV, wherein R.sub.7 is as defined above; or R.sub.2 is a group of the formula VI, wherein R.sub.3 is as defined above; and salts thereof.The compounds of the formula I are prodrugs of pilocarpine. When administered ophthalmically to a warm-blooded animal, such as a human, compounds of formula I, due to their high lipophilicity, will penetrate the cornea in an extent greater than pilocarpine itself, and will thereafter be converted into pilocarpine in a slow and controlled manner.

8. 发明授权

US4694006A Acyl- or acyloxymethyl-allopurinol prodrugs 失效
标题翻译：酰基或酰氧基甲基别嘌呤醇前药
公开(公告)号：US4694006A
公开(公告)日：1987-09-15
申请号：US711583
申请日：1985-02-26
申请人： Hans Bundgaard , Erik Falch
发明人： Hans Bundgaard , Erik Falch
IPC分类号： C07F9/6561 , A61K31/505 , A61P19/06 , A61P43/00 , C07D487/00 , C07D487/04
CPC分类号： C07D487/04
摘要： Compounds of the formula Ia and Ib ##STR1## are prodrugs of allopurinol and have i.a. a much higher solubility in water and/or a higher lipophilicity than allopurinol, which makes such compounds useful for oral, parenteral and rectal administration to a warm-blooded animal such as a human. Such compounds will after administration be converted into allopurinol.
摘要翻译： PCT No.PCT / DK84 / 00057 Sec。 371日期1985年2月26日第 102（e）日期1985年2月26日PCT Filed 1984年6月19日PCT公布。公开号WO85 / 00368 日期：1985年1月31日。式Ia和Ib的化合物是别嘌呤醇的前药，具有i.a. 在水中的溶解度高于和/或比别嘌呤醇更高的亲脂性，这使得这些化合物可用于口服，肠胃外和直肠给予温血动物例如人。给药后的这些化合物被转化为别嘌呤醇。

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