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1. 发明授权

US5543414A Achiral amino acid acyl esters of ganciclovir and its derivatives 失效
标题翻译：更昔洛韦及其衍生物的非手性氨基酸酰基酯
公开(公告)号：US5543414A
公开(公告)日：1996-08-06
申请号：US282142
申请日：1994-07-28
申请人： John J. Nestor , Scott W. Womble , Hans Maag
发明人： John J. Nestor , Scott W. Womble , Hans Maag
IPC分类号： C07D473/16 , A61K31/52 , A61K31/522 , A61P31/12 , A61P31/22 , C07D473/00 , C07D473/18 , C07D473/32 , C07D473/40
CPC分类号： C07D473/00
摘要： Compounds of the Formula I ##STR1## wherein X is hydrogen, chloro, amino or hydroxy; R.sup.1 is an achiral amino acid acyl residue with a tertiary .alpha.-carbon atom. Preferred achiral amino acid acyl residues have the formula ##STR2## wherein each R.sup.2 is alkyl with 1 to 6 carbon atoms, cycloalkyl with 3 to 5 carbon atoms, or benzyl; or the two R.sup.2 groups link together to form a polymethylene group with 3 to 9 carbon atoms, and pharmaceutically acceptable salts thereof are antiviral agents with improved absorption. Intermediates for the preparation of the compounds of Formula I are also described.
摘要翻译：式I的化合物其中X是氢，氯，氨基或羟基; R1是具有叔碳原子的非手性氨基酸酰基残基。优选的非手性氨基酸酰基残基具有式“IMAGE”，其中每个R 2是具有1至6个碳原子的烷基，具有3至5个碳原子的环烷基或苄基; 或两个R 2基团连接在一起形成具有3至9个碳原子的多亚甲基，其药学上可接受的盐是具有改善的吸收的抗病毒剂。还描述了制备式I化合物的中间体。

2. 发明授权

US5807823A Analogs of parathyroid hormone and parathyroid hormone related peptide: synthesis and use for the treatment of osteoporosis 失效
标题翻译：甲状旁腺激素和甲状旁腺激素相关肽的类似物：合成和用于治疗骨质疏松症
公开(公告)号：US5807823A
公开(公告)日：1998-09-15
申请号：US449317
申请日：1995-05-24
申请人： John L. Krstenansky , John J. Nestor , Brian H. Vickery
发明人： John L. Krstenansky , John J. Nestor , Brian H. Vickery
IPC分类号： A61K38/22 , A61K9/00 , A61K38/00 , A61K47/28 , A61K47/40 , A61P3/00 , A61P19/10 , A61P43/00 , C07K1/04 , C07K1/06 , C07K1/113 , C07K14/575 , C07K14/635 , C12N1/21 , C12N15/16 , C12N15/18 , A61K38/29 , A61K38/16
CPC分类号： A61K9/0043 , C07K14/635 , A61K38/00 , A61K47/28 , A61K47/40 , C07K2319/00
摘要： Synthetic polypeptide analogs of parathyroid hormone PTH, parathyroid hormone related peptide PTHrp, and of the physiologically active truncated homologs and analogs of PTH and PTHrp, in which amino acid residues (22-31) form an amphipathic .alpha.-helix, said residues (22-31) selected from hydrophilic amino acids (Haa) and lipophilic amino acids (Laa) ordered in the sequence: Haa(Laa Laa Haa Haa).sub.2 Laa and their pharmaceutically acceptable salts are useful for the prophylaxis and treatment of ostoporosis in mammals. Processes for the production of the polypeptides via solid phase and recombinant methods are provided.
摘要翻译：甲状旁腺激素PTH，甲状旁腺激素相关肽PTHrp和PTH和PTHrp的生理活性截短同源物和类似物的合成多肽类似物，其中氨基酸残基（22-31）形成两亲性α-螺旋，所述残基（22- 选自亲水氨基酸（Haa）和亲脂性氨基酸（Laa）的序列：Haa（Laa Laa Haa）2Laa及其药学上可接受的盐可用于预防和治疗哺乳动物的骨质疏松症。提供了通过固相和重组方法生产多肽的方法。

3. 发明授权

US4581169A Nona-peptide and deca-peptide analogs of LHRH, useful as LHRH antagonists 失效
标题翻译： LHRH的非肽和十肽类似物，可用作LHRH拮抗剂
公开(公告)号：US4581169A
公开(公告)日：1986-04-08
申请号：US472692
申请日：1983-03-07
申请人： John J. Nestor , Brian H. Vickery
发明人： John J. Nestor , Brian H. Vickery
IPC分类号： A61K38/00 , C07K7/23 , A61K37/02
CPC分类号： C07K7/23 , A61K38/00 , Y10S930/13
摘要： Synthetic nona-peptide and deca-peptide LHRH antagonist analogs have a novel guanido-substituted, amidine, tertiary or quaternary aminoacyl residue at position 6.
摘要翻译：合成的十肽和十肽肽LHRH拮抗剂类似物在6位具有新的胍基取代的脒基，叔或季氨基残基。

4. 发明授权

US4234571A Nonapeptide and decapeptide derivatives of luteinizing hormone releasing hormone 失效
标题翻译：促黄体激素释放激素的非肽和十肽衍生物
公开(公告)号：US4234571A
公开(公告)日：1980-11-18
申请号：US47661
申请日：1979-06-11
申请人： John J. Nestor , Gordon H. Jones , Brian H. Vickery
发明人： John J. Nestor , Gordon H. Jones , Brian H. Vickery
IPC分类号： A61K38/04 , A61K38/00 , A61K38/08 , A61K38/22 , A61P5/00 , C07K1/04 , C07K1/06 , C07K7/06 , C07K7/23 , C07K14/00 , C07K14/575 , A61K37/00 , C07C103/52
CPC分类号： C07K7/23 , A61K38/00 , Y10S514/80 , Y10S930/12 , Y10S930/13
摘要： Nonapeptide and decapeptide analogs of LH-RH of the formula(pyro)Glu-His-V-Ser-W-X-Y-Arg-Pro-Z (I)and the pharmaceutically acceptable salts thereof wherein:V is tryptophyl, phenylalanyl or 3-(1-naphthyl)-L-alanyl;W is tyrosyl, phenylalanyl or 3-(1-pentafluorophenyl)-L-alanyl;X is a D-amino acid residue ##STR1## wherein R is (a) a carbocyclic aryl-containing radical selected from the group consisting of naphthyl, anthryl, fluorenyl, phenanthryl, biphenylyl, benzhydryl and phenyl substituted with three or more straight chain lower alkyl groups; or(b) a saturated carbocyclic radical selected from the group consisting of cyclohexyl substituted with three or more straight chain lower alkyl groups, perhydronaphthyl, perhydrobiphenylyl, perhydro-2,2-diphenylmethyl and adamantyl;Y is leucyl, isoleucyl, nor-leucyl or N-methyl-leucyl;Z is glycinamide or --NH--R.sup.1, whereinR.sup.1 is lower alkyl, cycloalkyl, fluoro lower alkyl or ##STR2## wherein R.sup.2 is hydrogen or lower alkyl,are disclosed. These compounds exhibit potent LH-RH agonist properties.
摘要翻译：式（pyro）Glu-His-V-Ser-WXY-Arg-Pro-Z（I）的LH-RH的非肽和十肽类似物及其药学上可接受的盐，其中：V是色氨酸，苯丙氨酰或3-（1 - 萘基）-L-丙氨酰; W是酪氨酰基，苯丙氨酰基或3-（1-五氟苯基）-L-丙氨酰; X是D-氨基酸残基，其中R是（a）选自萘基，蒽基，芴基，菲基，联苯基，二苯甲基和被三个或更多个直链低级取代的苯基的含碳环芳基的基团烷基; 或（b）选自由三个或更多个直链低级烷基取代的环己基，全氢萘基，全氢联苯基，全氢-2,2-二苯基甲基和金刚烷基的饱和碳环基团; Y是亮氨酰基，异亮氨酰基，正亮氨酰基或N-甲基 - 亮氨酰基; Z是甘氨酰胺或-NH-R 1，其中R 1是低级烷基，环烷基，氟低级烷基或其中R 2是氢或低级烷基。这些化合物显示出有效的LH-RH激动剂性质。

5. 发明授权

US5798225A Process for recombinant production of PTH and PTHrp analogs 失效
标题翻译：重组生产PTH和PTHrp类似物的方法
公开(公告)号：US5798225A
公开(公告)日：1998-08-25
申请号：US449500
申请日：1995-05-24
申请人： John L. Krstenansky , John J. Nestor , Teresa H. Ho , Brian H. Vickery , Chinh T. Bach
发明人： John L. Krstenansky , John J. Nestor , Teresa H. Ho , Brian H. Vickery , Chinh T. Bach
IPC分类号： A61K38/22 , A61K9/00 , A61K38/00 , A61K47/28 , A61K47/40 , A61P3/00 , A61P19/10 , A61P43/00 , C07K1/04 , C07K1/06 , C07K1/113 , C07K14/575 , C07K14/635 , C12N1/21 , C12N15/16 , C12N15/18 , C12N15/63
CPC分类号： A61K9/0043 , C07K14/635 , A61K38/00 , A61K47/28 , A61K47/40 , C07K2319/00
摘要： Synthetic polypeptide analogs of parathyroid hormone PTH, parathyroid hormone related peptide PTHrp, and of the physiologically active truncated homologs and analogs of PTH and PTHrp, in which amino acid residues (22-31) form an amphipathic .alpha.-helix, said residues (22-31) selected from hydrophilic amino acids (Haa) and lipophilic amino acids (Laa) ordered in the sequence: Haa(Laa Laa Haa Haa).sub.2 Laa and their pharmaceutically acceptable salts are useful for the prophylaxis and treatment of ostoporosis in mammals. Processes for the production of the polypeptides via solid phase and recombinant methods are provided.
摘要翻译：甲状旁腺激素PTH，甲状旁腺激素相关肽PTHrp和PTH和PTHrp的生理活性截短同源物和类似物的合成多肽类似物，其中氨基酸残基（22-31）形成两亲性α-螺旋，所述残基（22- 选自Haa（Laa Laa Haa）2 Laa及其药学上可接受的盐的亲水性氨基酸（Haa）和亲脂性氨基酸（Laa））可用于预防和治疗哺乳动物的骨质疏松症。提供了通过固相和重组方法生产多肽的方法。

6. 发明授权

US4659693A N,N'-dialkyl substituted guanidino amino acyl residue substituted GRF-analog peptides 失效
标题翻译： N，N'-二烷基取代的胍基氨基酰基残基取代的GRF-类似物肽
公开(公告)号：US4659693A
公开(公告)日：1987-04-21
申请号：US707007
申请日：1985-02-28
申请人： John J. Nestor
发明人： John J. Nestor
IPC分类号： C07K14/60 , A61K37/43 , C07K7/08 , C07K7/10
CPC分类号： C07K14/60 , Y10S930/12
摘要： Peptides which promote the release of growth hormone by the pituitary gland or which inhibit the release of growth hormone by growth hormone releasing factor and which have an N,N'-dialkyl substituted guanidino amino acyl residue at position 1 or 2 are disclosed herein.
摘要翻译：本文公开了促进垂体释放生长激素或通过生长激素释放因子抑制生长激素释放并且在位置1或2处具有N，N'-二烷基取代的胍基氨基酰基残基的肽。

7. 发明授权

US4419347A Nonapeptide and decapeptide analogs of LHRH, useful as LHRH antagonists 失效
标题翻译： LHRH的非肽和十肽类似物，可用作LHRH拮抗剂
公开(公告)号：US4419347A
公开(公告)日：1983-12-06
申请号：US366635
申请日：1982-04-08
申请人： John J. Nestor , Gordon H. Jones , Brian H. Vickery
发明人： John J. Nestor , Gordon H. Jones , Brian H. Vickery
IPC分类号： A61K38/00 , C07K7/23 , A61K37/00 , C07C103/52
CPC分类号： C07K7/23 , A61K38/00 , Y10S514/80 , Y10S930/13
摘要： Nonapeptide and decapeptide analogs of LHRH which have the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein: X is a D-alanyl residue wherein one hydrogen on C-3 is replaced by:(a) a carbocyclic aryl-containing radical selected from the group consisting of phenyl substituted with three or more straight chain lower alkyl groups, naphthyl, anthryl, fluorenyl, phenanthryl, biphenylyl and benzhydryl; or(b) a saturated carbocyclic radical selected from the group consisting of cyclohexyl substituted with three or more straight chain lower alkyl groups, perhydronaphthyl, perhydrobiphenylyl, perhydro-2,2-diphenylmethyl, and adamantyl; or(c) a heterocyclic aryl containing radical selected from the group consisting of radicals represented by the following structural formulas: ##STR2## wherein A" and A' are independently selected from the group consisting of hydrogen, lower alkyl, chlorine, and bromine, and G is selected from the group consisting of oxygen, nitrogen, and sulfur;A is an aminoacyl residue selected from the group consisting of L-pyroglutamyl, D-pyroglutamyl, N-acyl-L-prolyl, N-acyl-D-prolyl, N-acyl-D-tryptophanyl, N-acyl-D-phenylalanyl, N-acyl-D-p-halophenylalanyl, and N-acyl-X wherein X is as defined previously;B is an amino acyl residue selected from the group consisting of D-phenylalanyl, D-p-halophenylalanyl, 2,2-diphenylglycyl, and X wherein X is as defined previously;C is an amino acyl residue selected from the group consisting of L-tryptophanyl, D-tryptophanyl, D-phenylalanyl and X wherein X is as defined above;E is glycinamide or --NH--R.sup.1, wherein R.sup.1 is lower alkyl, cycloalkyl, fluoro lower alkyl or ##STR3## wherein R.sup.2 is hydrogen or lower alkyl;are disclosed. These compounds are LHRH antagonists.
摘要翻译：具有式（I）的LHRH的非肽和十肽类似物及其药学上可接受的盐，其中：X是D-丙氨酰残基，其中C-3上的一个氢被：（a）碳环芳基 - 含有选自被三个或多个直链低级烷基取代的苯基的萘基，萘基，蒽基，芴基，菲基，联苯基和二苯甲基; 或（b）饱和碳环基团，其选自由三个或更多个直链低级烷基取代的环己基，全氢萘基，全氢联苯基，全氢-2,2-二苯基甲基和金刚烷基; 或（c）含有选自下列结构式的基团的杂环芳基基团：其中A“和A'独立地选自氢，低级烷基，氯和溴，G选自氧，氮和硫; A是选自L-焦谷氨酰基，D-焦谷氨酰基，N-酰基-L-脯氨酰基，N-酰基-D-脯氨酰基，N-酰基-D-色氨酸基，N-酰基-D-苯丙氨酰基，N-酰基-Dp-卤代苯丙氨酰基和N-酰基-X，其中X如前所定义; B是选自D-苯丙氨酰，D-p-卤苯丙氨酰，2,2-二苯基甘氨酰和X的氨基酰基残基，其中X如前所定义; C是选自L-色氨酰基，D-色氨酸基，D-苯丙氨酰基和X的氨基酰基残基，其中X如上定义; E是甘氨酰胺或-NH-R 1，其中R 1是低级烷基，环烷基，氟低级烷基或者其中R 2是氢或低级烷基; 被披露。这些化合物是LHRH拮抗剂。

8. 发明授权

US4341767A Nonapeptide and decapeptide analogs of LHRH, useful as LHRH antagonists 失效
标题翻译： LHRH的非肽和十肽类似物，可用作LHRH拮抗剂
公开(公告)号：US4341767A
公开(公告)日：1982-07-27
申请号：US194180
申请日：1980-10-06
申请人： John J. Nestor , Gordon H. Jones , Brian H. Vickery
发明人： John J. Nestor , Gordon H. Jones , Brian H. Vickery
IPC分类号： A61K38/00 , C07K7/23 , A61K37/00 , C07C103/52
CPC分类号： C07K7/23 , A61K38/00 , Y10S514/80 , Y10S930/13
摘要： Nonapeptide and decapeptide analogs of LHRH which have the formula: ##STR1## and the pharmaceutically acceptable salts thereof, wherein: X is a D-alanyl residue wherein one hydrogen on C-3 is replaced by:(a) a carbocyclic aryl-containing radical selected from the group consisting of phenyl substituted with three or more straight chain lower alkyl groups, naphthyl, anthryl, fluorenyl, phenanthryl, biphenylyl and benzhydryl; or(b) a saturated carbocyclic radical selected from the group consisting of cyclohexyl substituted with three or more straight chain lower alkyl groups, perhydronaphthyl, perhydrobiphenylyl, perhydro-2,2-diphenylmethyl, and adamantyl; or(c) a heterocyclic aryl containing radical selected from the group consisting of radicals represented by the following structural formulas: ##STR2## wherein A" and A' are independently selected from the group consisting of hydrogen, lower alkyl, chlorine, and bromine, and G is selected from the group consisting of oxygen, nitrogen, and sulfur;A is an aminoacyl residue selected from the group consisting of L-pyroglutamyl, D-pyroglutamyl, N-acyl-L-prolyl, N-acyl-D-prolyl, N-acyl-D-tryptophanyl, N-acyl-D-phenylalanyl, N-acyl-D-p-halophenylalanyl, and N-acyl-X wherein X is as defined previously;B is an amino acyl residue selected from the group consisting of D-phenylalanyl, D-p-halophenylalanyl, 2,2-diphenylglycyl, and X wherein X is as defined previously;C is an amino acyl residue selected from the group consisting of L-tryptophanyl, D-tryptophanyl, D-phenylalanyl and X wherein X is as defined above;E is glycinamide or --NH--R.sup.1, wherein R.sup.1 is lower alkyl, cycloalkyl, fluoro lower alkyl or ##STR3## wherein R.sup.2 is hydrogen or lower alkyl; are disclosed. These compounds are LHRH antagonists.
摘要翻译：具有下式的LHRH的非肽和十肽类似物及其药学上可接受的盐，其中：X是D-丙氨酰残基，其中C-3上的一个氢被：（a）碳环芳基选自由三个或更多个直链低级烷基取代的苯基的萘基，萘基，蒽基，芴基，菲基，联苯基和二苯甲基; 或（b）饱和碳环基团，其选自由三个或更多个直链低级烷基取代的环己基，全氢萘基，全氢联苯基，全氢-2,2-二苯基甲基和金刚烷基; 或（c）含有杂环芳基的基团，其选自由以下结构式表示的基团：其中A“和A'独立地选自氢，低级烷基，氯和溴，G选自氧，氮和硫; A是选自L-焦谷氨酰基，D-焦谷氨酰基，N-酰基-L-脯氨酰基，N-酰基-D-脯氨酰基，N-酰基-D-色氨酸基，N-酰基-D-苯丙氨酰基，N-酰基-Dp-卤代苯丙氨酰基和N-酰基-X，其中X如前所定义; B是选自D-苯丙氨酰，D-p-卤苯丙氨酰，2,2-二苯基甘氨酰和X的氨基酰基残基，其中X如前所定义; C是选自L-色氨酰基，D-色氨酸基，D-苯丙氨酰基和X的氨基酰基残基，其中X如上定义; E是甘氨酰胺或-NH-R 1，其中R 1是低级烷基，环烷基，氟低级烷基或者其中R 2是氢或低级烷基; 被披露。这些化合物是LHRH拮抗剂。

9. 发明授权

US4530920A Nonapeptide and decapeptide analogs of LHRH, useful as LHRH agonist 失效
标题翻译： LHRH的非肽和十肽类似物，可用作LHRH激动剂
公开(公告)号：US4530920A
公开(公告)日：1985-07-23
申请号：US549355
申请日：1983-11-07
申请人： John J. Nestor , Brian H. Vickery
发明人： John J. Nestor , Brian H. Vickery
IPC分类号： A61K38/04 , A61K38/00 , A61K38/22 , A61P5/00 , A61P13/02 , A61P15/00 , C07K1/113 , C07K7/23 , C07K14/575 , C07C103/52 , A61K37/02
CPC分类号： C07K7/23 , A61K38/00 , Y10S514/80 , Y10S930/13
摘要： Synthetic nonapeptide and decapeptide LHRH agonists analogs having a novel gaunadino-substituted, amidine, tertiary or quatrinary aminoacyl residue at position 6 are disclosed herein.
摘要翻译：本文公开了在6位具有新的高甘氨酸取代的，脒基，叔或氨基酰基残基的合成的单肽和十肽LHRH激动剂类似物。

10. 发明授权

US4318905A Nonapeptide and decapeptide agonists of luteinizing hormone releasing hormone containing heterocyclic amino acid residues 失效
标题翻译：含有杂环氨基酸残基的促黄体激素释放激素的非肽和十肽激动剂
公开(公告)号：US4318905A
公开(公告)日：1982-03-09
申请号：US162455
申请日：1980-06-23
申请人： John J. Nestor , Gordon H. Jones , Brian H. Vickery
发明人： John J. Nestor , Gordon H. Jones , Brian H. Vickery
IPC分类号： C07D235/16 , C07D277/64 , C07K7/23 , A61K37/00 , C07C103/52
CPC分类号： C07D277/64 , C07D235/16 , C07K7/23 , Y10S514/80 , Y10S930/13
摘要： Nonapeptide and decapeptide analogs of LH-RH of the formula ##STR1## and the pharmaceutically acceptable salts thereof wherein: V is tryptophyl, phenylalanyl or 3-(1-naphthyl)-L-alanyl;W is tyrosyl, phenylalanyl or 3-(1-pentafluorophenyl)-L-alanyl;X is a D-amino acid residue of the formula: ##STR2## wherein R is a heterocyclic aryl containing radical selected from the group consisting of radicals represented by the following structural formulas: ##STR3## wherein A and A' are independently selected from the group consisting of hydrogen, lower alkyl, chlorine, and bromine, and G is selected from the group consisting of oxygen, nitrogen, and sulfur;Y is leucyl, isoleucyl, nor-leucyl or N-methyl-leucyl;Z is glycinamide or --NH--R.sup.1, wherein:R.sup.1 is lower alkyl, cycloalkyl, fluoro lower alkyl or ##STR4## wherein R.sup.2 is hydrogen or lower alkyl,are disclosed. These compounds exhibit potent LH-RH agonist properties.
摘要翻译：式（I）的LH-RH的非肽和十肽类似物及其药学上可接受的盐，其中：V是色氨酸，苯丙氨酰基或3-（1-萘基）-L-丙氨酰; W是酪氨酰基，苯丙氨酰基或3-（1-五氟苯基）-L-丙氨酰; X是下式的D-氨基酸残基：其中R是含有基团的杂环芳基，其选自由以下结构式表示的基团：其中A 和A'独立地选自氢，低级烷基，氯和溴，并且G选自氧，氮和硫; Y是亮氨酰基，异亮氨酰基，正亮氨酰基或N-甲基 - 亮氨酰基; Z是甘氨酰胺或-NH-R 1，其中：R 1是低级烷基，环烷基，氟低级烷基或其中R 2是氢或低级烷基。这些化合物显示出有效的LH-RH激动剂性质。

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