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1. 发明授权

US5380727A Synergistic combination for treating herpes infections 失效
标题翻译：协同治疗疱疹感染的组合
公开(公告)号：US5380727A
公开(公告)日：1995-01-10
申请号：US809611
申请日：1991-12-17
申请人： Robert Deziel , Yvan Guindon
发明人： Robert Deziel , Yvan Guindon
IPC分类号： A61K8/49 , A61K8/60 , A61K8/64 , A61K31/52 , A61K31/522 , A61K31/70 , A61K38/00 , A61K38/55 , A61P31/12 , A61P31/22 , A61P43/00 , A61Q19/00 , A61K37/00
CPC分类号： A61Q19/00 , A61K38/005 , A61K8/606 , A61K8/64 , A61K2800/782
摘要： Disclosed herein is a combination of an antiviral nucleoside analog and a ribonucleotide reductase inhibiting peptide derivative. The combination is useful for treating herpes infections.
摘要翻译：本文公开了抗病毒核苷类似物和抑制核糖核苷酸还原酶的肽衍生物的组合。该组合可用于治疗疱疹感染。

2. 发明授权

US5126326A Enzyme inhibiting peptide derivatives 失效
标题翻译：酶抑制肽衍生物
公开(公告)号：US5126326A
公开(公告)日：1992-06-30
申请号：US361895
申请日：1989-06-06
申请人： Paul C. Anderson , Yvan Guindon , Christiane Yoakim
发明人： Paul C. Anderson , Yvan Guindon , Christiane Yoakim
IPC分类号： C12N9/99 , A61K38/55 , A61P9/00 , A61P9/12 , A61P43/00 , C07K1/06 , C07K1/113 , C07K5/02 , C07K5/06 , C07K14/81
CPC分类号： C07K5/0227
摘要： Disclosed herein are peptide derivatives which inhibit the activities of human immunodeficiency virus (HIV) protease and renin. The peptide derivatives can be represented by general formula R.sup.1 --R.sup.2 --Y--R.sup.3 --R.sup.4 wherein R.sup.1 is a derived amino acid based on an O.sup.4 -(carboxymethyl)-tyrosyl residue, R.sup.2 and are amino acid or analogous amino acid residues (R.sup.3 may optionally be absent), Y is a non-peptide linking unit, e.g. statyl, and R.sup.4 is [--NR.sup.17 CHR.sup.18 --C(O)].sub.p --Z wherein R.sup.17 is hydrogen or lower alkyl, R.sup.18 is an amino acid or analogous amino acid side chain, p is zero or one and Z is a terminal group (e.g. hydroxy or amino), or R.sup.4 is --NR.sup.17 CR.sup.18 (R.sup.21)CH.sub.2 OH wherein R.sup.17 and R.sup.18 are as noted hereinabove and R.sup.21 is hydrogen, lower alkyl or hydroxy(lower)alkyl. The derivatives are useful as agents for combatting HIV infections and for treating renin-associated hypertension and congestive heart failure.
摘要翻译：本文公开了抑制人免疫缺陷病毒（HIV）蛋白酶和肾素的活性的肽衍生物。肽衍生物可以由通式R 1 -R 2 -Y-R 3 -R 4表示，其中R 1是基于O 4 - （羧甲基） - 酪氨酰残基R2的衍生氨基酸，并且是氨基酸或类似氨基酸残基（R3可以任选地不存在），Y是非肽连接单元，例如辛基，R4是[-NR17CHR18-C（O）] pZ，其中R17是氢或低级烷基，R18是氨基酸或类似的氨基酸侧链，p是0或1，Z是末端基团（例如羟基或氨基），或R 4是-NR 17 CR 18（R 21）CH 2 OH，其中R 17和R 18如上所述，R 21是氢，低级烷基或羟基（低级）烷基。该衍生物可用作抗艾滋病毒感染和治疗肾素相关性高血压和充血性心力衰竭的药剂。

3. 发明授权

US5095004A Fluorine containing atrial natriuretic peptides 失效
标题翻译：含有含氟的ATRIAL NATRIURETIC PEPTIDES
公开(公告)号：US5095004A
公开(公告)日：1992-03-10
申请号：US166526
申请日：1988-03-14
申请人： Sumanas Rakhit , Mahesh H. Goghari
发明人： Sumanas Rakhit , Mahesh H. Goghari
IPC分类号： A61K38/00 , A61P7/10 , A61P9/12 , C07K1/04 , C07K1/06 , C07K1/113 , C07K7/08 , C07K14/00 , C07K14/575 , C07K14/58
CPC分类号： C07K14/58 , A61K38/00
摘要： Disclosed herein are derivatives of atrial natriuretic peptides which are characterized by having (at position 124 or at positions 106 and 124) a phenylalanyl residue bearing a fluoro or trifluoromethyl substituent on the aromatic portion thereof. Optionally, the exocyclic N-terminal peptide segment and the first cystienyl residue (at position 105) are replaced by an optionally substituted thioalkanoyl residue. The derivatives possess useful diuretic, natriuretic and antihypertensive activities.

4. 发明授权

US5354767A Renin inhibiting polyhydroxy-monoamides 失效
标题翻译：肾素抑制多羟基 - 单酰胺
公开(公告)号：US5354767A
公开(公告)日：1994-10-11
申请号：US990779
申请日：1992-12-10
申请人： Paul C. Anderson , Gary W. Bantle , Grace L. Jung , Pierre Lavallee , Bruno Simoneau
发明人： Paul C. Anderson , Gary W. Bantle , Grace L. Jung , Pierre Lavallee , Bruno Simoneau
IPC分类号： C07C235/08 , C07C235/26 , C07C235/34 , C07D233/54 , C07D233/88 , C07D277/36 , C07D307/58 , A61K31/16
CPC分类号： C07D233/64 , C07C235/08 , C07C235/26 , C07C235/34 , C07D233/88 , C07D277/36 , C07D307/58 , C07C2101/02 , C07C2101/08 , C07C2101/14
摘要： Disclosed herein are compounds of the formula:R.sup.1 CH.sub.2 CH(X)CH(Y)CH(Z)CHR.sup.2 C(O)NHCHR.sup.3 CH(OH)CH(OH)R.sup.4wherein R.sup.1 is a terminal unit, for example lower cycloalkyl or phenyl; R.sup.2 is, for example, an optionally substituted alkyl, cycloalkylmethyl, benzyl, 4-imidazolylmethyl, 2-thienylmethyl or 4-thiazolylmethyl; R.sup.3 is alkyl, cycloalkylmethyl or an optionally substituted benzyl; R.sup.4 is alkyl or cycloalkyl; and X and Y each is hydroxy and Z is hydrogen, or X and Z each is hydroxy and Y is hydrogen; with the provisos that (a) the carbon atom bearing R.sup.2 has the "R" configuration except when R.sup.2 is 2-thienylmethyl or 2-thiazolylmethyl, X and Y each is hydroxy and Z is hydrogen, then the carbon atom bearing R.sup.2 has the "S" configuration; (b) the carbon atoms bearing R.sup.3 and R.sup.4 each has the "S" configuration; and (c) the carbon atom located between the last-said two carbon atoms has the "R" configuration. The compounds inhibit renin activity and are indicated for the treatment of hypertension and congestive heart failure.
摘要翻译：本文公开的是下式的化合物：R1CH2CH（X）CH（Y）CH（Z）CHR2C（O）NHCHR3CH（OH）CH（OH）R4其中R1是末端单元，例如低级环烷基或苯基; R2是例如任选取代的烷基，环烷基甲基，苄基，4-咪唑基甲基，2-噻吩基甲基或4-噻唑基甲基; R3是烷基，环烷基甲基或任选取代的苄基; R4是烷基或环烷基; X和Y各自为羟基，Z为氢，或X和Z各自为羟基，Y为氢; 条件是（a）带有R2的碳原子具有“R”构型，除非R2是2-噻吩基甲基或2-噻唑基甲基，X和Y各自为羟基，Z为氢，则带有R2的碳原子具有“ S“配置; （b）含有R 3和R 4的碳原子各自具有“S”构型; 和（c）位于最后所述两个碳原子之间的碳原子具有“R”构型。该化合物抑制肾素活性，并被指示用于治疗高血压和充血性心力衰竭。

5. 发明授权

US5198425A Inhibitors of bacterial ribonucleotide reductase 失效
标题翻译：细菌核糖核苷酸还原酶抑制剂
公开(公告)号：US5198425A
公开(公告)日：1993-03-30
申请号：US900366
申请日：1992-06-18
申请人： Sumanas Rakhit , Raymond Plante , Gregory P. Cosentino
发明人： Sumanas Rakhit , Raymond Plante , Gregory P. Cosentino
IPC分类号： A61K38/00 , C07K7/06
CPC分类号： C07K7/06 , A61K38/00
摘要： Disclosed herein are peptides of the formulaY--R.sup.1 --R.sup.2 --R.sup.3 --R.sup.4 --R.sup.5 --R.sup.6 --R.sup.7 --R.sup.8 --R.sup.9 --Zwherein R.sup.1 to R.sup.9 are designated amino acid residues; Y is hydrogen or lower alkanoyl, or Y is the hexapeptide radical W-lle-R.sup.10 -Ser-R.sup.11 -Val-R.sup.12 wherein W is hydrogen or lower alkanoyl and R.sup.10, R.sup.11 and R.sup.12 are designated amino acid residues, or Y is a fragment of the hexapeptide radical wherein from one to five of the amino acid residues (i.e. Ile to Val) may be deleted serially from the amino terminus of the hexapeptide radical; and Z is hydroxy, amino, lower alkylamino or di(lower alkyl)amino. The peptides inhibit bacterial ribonucleotide reductase and are indicated for preventing or ameliorating bacterial infections.
摘要翻译：本文公开的是式Y-R1-R2-R3-R4-R5-R6-R7-R8-R9-Z的肽，其中R1至R9被指定为氨基酸残基; Y为氢或低级烷酰基，或Y为六肽基团W-Lle-R10-Ser-R11-Val-R12，其中W为氢或低级烷酰基，R10，R11和R12为氨基酸残基，或Y为片段的六肽基团，其中一至五个氨基酸残基（即Ile至Val）可以从六肽基团的氨基末端连续缺失; 和Z是羟基，氨基，低级烷基氨基或二（低级烷基）氨基。肽抑制细菌核糖核苷酸还原酶，并且用于预防或改善细菌感染。

6. 发明授权

US5149778A Cyclic peptides for treating herpes infections 失效
标题翻译：用于治疗疱疹感染的循环肽
公开(公告)号：US5149778A
公开(公告)日：1992-09-22
申请号：US547721
申请日：1990-07-03
申请人： Julian Adams , John DiMaio , Raymond Plante
发明人： Julian Adams , John DiMaio , Raymond Plante
IPC分类号： A61K38/00 , C07K7/56
CPC分类号： C07K7/56 , A61K38/00 , Y10S514/934 , Y10S930/27
摘要： Disclosed herein are cyclic peptide derivatives of the formula ##STR1## wherein A is absent or the tripeptide radical Thr.rarw.Gly.rarw.Ala, R.sup.1 is benzyl or benzyl monosubstituted at position 4 of the aromatic ring with halo, hydroxy, lower alkyl or lower alkoxy, R.sup.2 and R.sup.4 each independently is hydrogen or lower alkyl, R.sup.3 is lower alkyl or lower alkyl monosubstituted with a hydroxy, R.sup.5 is lower alkyl, Y is oxo or thioxo and Z is hydroxy or NR.sup.6 R.sup.7 wherein R.sup.6 and R.sup.7 each independently is hydrogen or lower alkyl. The derivatives are useful for treating herpes infections.
摘要翻译：本文公开了具有下式的环肽衍生物：其中A不存在或三肽基Thr <-Gly <-Ala，R1是苄基或在芳环的4位被卤素单取代的苄基的环肽衍生物，羟基，低级烷基或低级烷氧基，R 2和R 4各自独立地为氢或低级烷基，R 3为低级烷基或被羟基单取代的低级烷基，R 5为低级烷基，Y为氧代或硫代，Z为羟基或NR 6 R 7，其中R 6 和R 7各自独立地为氢或低级烷基。该衍生物可用于治疗疱疹感染。

7. 发明授权

US4891358A ANE derivatives with novel bridging 失效
标题翻译： ANE衍生物与新桥接
公开(公告)号：US4891358A
公开(公告)日：1990-01-02
申请号：US284555
申请日：1988-12-15
申请人： John DiMaio , Dominik M. Wernic , Jorge Jaramillo
发明人： John DiMaio , Dominik M. Wernic , Jorge Jaramillo
IPC分类号： A61K38/22 , A61K38/00 , A61P3/00 , A61P7/10 , A61P9/08 , A61P9/12 , C07K1/06 , C07K1/10 , C07K7/08 , C07K14/00 , C07K14/575 , C07K14/58
CPC分类号： C07K14/58 , A61K38/00
摘要： Disclosed herein are derivatives of atrial natriuretic peptides wherein the exocyclic N-terminal peptide segment is deleted and the two cysteinyl residues (at positions 105 and 121) of the natural sequence are replaced with a trivalent unit, --NHCH(CO--)--Q--X--Y--CH.sub.2 CH.sub.2 CO-- wherein Q is methylene, ethylene or CR'R" wherein R' and R" each independently is lower alkyl, X is oxy or thio, and Y is methylene or des-Y. The derivatives may be optionally substituted at various positions including positions 106, 107 and 124. The derivatives possess ANF-like activity and are indicated for treating hypertension and for treating pathological conditions resulting from an imbalance of body fluids and electrolytes.

8. 发明授权

US5212157A Enzyme inhibitors 失效
标题翻译：酶抑制剂
公开(公告)号：US5212157A
公开(公告)日：1993-05-18
申请号：US362171
申请日：1989-06-06
申请人： Paul C. Anderson , Yvan Guindon , Christiane Yoakim
发明人： Paul C. Anderson , Yvan Guindon , Christiane Yoakim
IPC分类号： C12N9/99 , A61K38/00 , A61K38/55 , A61P9/00 , A61P9/12 , A61P31/12 , A61P31/18 , A61P43/00 , C07D217/26 , C07K1/06 , C07K1/113 , C07K5/02 , C07K5/06 , C07K5/08 , C07K14/81
CPC分类号： C07K5/0205 , C07D217/26 , C07K5/0207 , A61K38/00
摘要： Disclosed herein are peptide derivatives which inhibit the activity of human immunodeficiency virus (HIV) protease. The peptide derivatives can be represented by general formula R.sup.1 --R.sup.2 --Y--R.sup.3 --R.sup.4 wherein R.sup.1 is an optionally substituted 3-(1,2,3,4-tetrahydroisoquinolyl)carbonyl residue, R.sup.2 and R.sup.3 are amino acid or analogous amino acid residues (R.sup.3 may optionally be absent), Y is a non-peptide linking unit, e.g. statyl, and R.sup.4 is [--NR.sup.17 CH(R.sup.18)C(O)].sub.p --Z wherein R.sup.17 is hydrogen or lower alkyl, R.sup.18 is an amino acid or analogous amino acid side chain, p is zero or 1 and Z is a terminal group (e.g. hydroxy or amino), or R.sup.4 is --NR.sup.17 CR.sup.18 (R.sup.21)CH.sub.2 --OH wherein R.sup.17 and R.sup.18 are as noted hereinabove and R.sup.21 is hydrogen, lower alkyl or hydroxy(lower)alkyl. The derivatives also inhibit renin activity. Accordingly, the derivatives can be used for combating HIV infections or for treating hypertension or congestive heart failure.

9. 发明授权

US5071835A Ribonucleotide reductase inhibitors 失效
标题翻译： RIBONUCLEOTIDE还原抑制剂
公开(公告)号：US5071835A
公开(公告)日：1991-12-10
申请号：US474589
申请日：1990-02-01
申请人： Yvan Guindon , Pierre Lavallee , Sumanas Rakhit , Gregory P. Cosentino
发明人： Yvan Guindon , Pierre Lavallee , Sumanas Rakhit , Gregory P. Cosentino
IPC分类号： C12N9/99 , A61K38/00 , A61K38/55 , A61P35/00 , C07K1/04 , C07K1/06 , C07K7/06 , C07K7/08 , C12Q1/26
CPC分类号： C07K7/06 , C07K7/08 , C12Q1/26 , A61K38/00
摘要： Disclosed herein are peptides of the formulaY--R.sup.1 --R.sup.2 --R.sup.3 --R.sup.4 --R.sup.5 --R.sup.6 --Zwherein R.sup.1 to R.sup.5 are designated amino acid residues; R.sup.6 is Phe, homoPhe or an amino acid residue derived from 2-amino-3-cyclohexylpropionic acid, 2-amino-3-(4-(lower alkoxy)phenyl) propionic acid or 2-amino-3-(4-halophenyl)propionic acid; Y is Phe, desamino-Phe, (lower alkanoyl)-Phe, p-haloPhe, Tyr, desamino-Tyr or (lower alkanoyl)-Tyr, or Y is the decapeptide radical W--Val--R.sup.7 --Ser--R.sup.8 --R.sup.9 --Thr--Glu--R.sup.10 --Ser--Phe wherein W is hydrogen or lower alkanoyl and R.sup.7 to R.sup.10 are designated amino acids residues, or Y is a fragment of the decapeptide radical wherein from one to nine of the amino acid residues (i.e. Val to Ser) may be deleted serially from the amino terminus of the decapeptide radical; and Z is hydroxy, amino, lower alkylamino or di(lower alkyl)amino. The peptides inhibit mammalian ribonucleotide reductase and are indicated for preventing or ameliorating abnormal cell proliferation.

10. 发明授权

US5242946A Treating herpes Viral infections 失效
标题翻译：治疗疱疹病毒感染
公开(公告)号：US5242946A
公开(公告)日：1993-09-07
申请号：US830019
申请日：1992-01-31
申请人： Yvan Guindon
发明人： Yvan Guindon
IPC分类号： A61K31/22
CPC分类号： A61K31/22 , Y10S514/934
摘要： A group of known naphthalene derivatives have been found to be useful for preventing or relieving herpes viral infections.
摘要翻译：已经发现一组已知的萘衍生物可用于预防或缓解疱疹病毒感染。

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