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1. 发明申请

WO1994025046A1 METHOD OF COMBATING ACYCLOVIR-RESISTANT HERPES SIMPLEX VIRAL INFECTIONS 审中-公开
标题翻译：组合抗胆碱酯酶复合病毒感染的方法
公开(公告)号：WO1994025046A1
公开(公告)日：1994-11-10
申请号：PCT/CA1994000242
申请日：1994-04-29
申请人： BIO-MEGA/BOEHRINGER INGELHEIM RESEARCH INC.
发明人： BIO-MEGA/BOEHRINGER INGELHEIM RESEARCH INC. , CHAFOULEAS, James, Gus , DEZIEL, Robert
IPC分类号： A61K37/02
CPC分类号： A61K31/70 , A61K31/195 , A61K31/52 , A61K38/04 , A61K2300/00
摘要： Disclosed herein is a method for treating acyclovir-resistant herpes infections in a mammal. The method comprises administering a peptide derivative or a combination of the peptide derivative and an antiviral nucleoside analog to the infected mammal. The peptide derivative used for the method is represented by the formula A-B-D-CH2CH{CH2C(O)R }C(O)-NHCH{CR (R )COOH}C(O)-E wherein A is a terminal group, for example an optionally substituted phenylalkanoyl, and B is an N-methyl amino acid residue; or A and B together form a saturated alkylaminocarbonyl; D is an amino acid residue; R is, for example, an alkyl, cycloalkyl, or a monosubstituted or a disubstituted amino; R is, for example, hydrogen or alkyl and R is alkyl, or R is hydrogen and R is phenylalkyl, or R and R are joined to form a cycloalkyl; and E is a terminal unit, for example, an alkylamino or a monovalent amino acid radical such as NHCH(alkyl)C(O)OH.
摘要翻译：本文公开了一种在哺乳动物中治疗阿昔洛韦耐药性疱疹感染的方法。该方法包括给受感染的哺乳动物施用肽衍生物或肽衍生物与抗病毒核苷类似物的组合。用于该方法的肽衍生物由式ABD-CH 2 CH（CH 2 C（O）R）C（O）-NHCH（CR 2）（R 3）COOH）C（O）其中A为末端基团，例如任选取代的苯基烷酰基，B为N-甲基氨基酸残基; 或A和B一起形成饱和的烷基氨基羰基; D是氨基酸残基; R 1是例如烷基，环烷基或单取代或二取代的氨基; R 2为例如氢或烷基，R 3为烷基，或R 2为氢，R 3为苯基烷基，或R 2和R 3连接形成环烷基; 并且E是末端单元，例如烷基氨基或单价氨基酸基团，例如NHCH（烷基）C（O）OH。

2. 发明申请

WO1994020528A1 INHIBITORS OF HERPES VIRAL RIBONUCLEOTIDE REDUCTASE 审中-公开
标题翻译： HERPES VIRAL RIBONUCLEOTIDE REDUCTASE的抑制剂
公开(公告)号：WO1994020528A1
公开(公告)日：1994-09-15
申请号：PCT/CA1994000106
申请日：1994-02-28
申请人： BIO-MEGA/BOEHRINGER INGELHEIM RESEARCH INC.
发明人： BIO-MEGA/BOEHRINGER INGELHEIM RESEARCH INC. , DEZIEL, Robert , MOSS, Neil
IPC分类号： C07K05/10
CPC分类号： C07K5/101 , A61K38/00 , C07K14/005 , C12N2710/16622
摘要： Disclosed herein are peptide derivatives of the formula A-B-D-NHCH{CH2C(O)R }C(O)-NHCH{CR (R )-COOH}C(O)-E wherein A is a lower alkanoyl bearing two substituents, each substituent selected independently from phenyl or a monosubstituted phenyl wherein the monosubstituent is alkyl, halo, hydroxy or alkoxy; B is an N-methyl amino acid residue; D is an amino acid residue; R is alkyl, cycloalkyl, a monosubstituted amino or a disubstituted amino; R is hydrogen or alkyl and R is alkyl, or R and R are joined to form a cycloalkyl; and E is a terminal unit, for example, an alkylamino or a monovalent amino acid radical such as NHCH(alkyl)C(O)OH. The derivatives are useful for treating herpes infections.
摘要翻译：本文公开的是式ABD-NHCH（CH 2 C（O）R 1）C（O）-NHCH（CR 2）（R 3）-COOH）C（O）-E的肽衍生物，其中A是具有两个取代基的低级烷酰基，每个取代基独立地选自苯基或单取代的苯基，其中单取代基是烷基，卤素，羟基或烷氧基; B是N-甲基氨基酸残基; D是氨基酸残基; R 1是烷基，环烷基，单取代的氨基或二取代的氨基; R 2是氢或烷基，R 3是烷基，或R 2和R 3连接形成环烷基; 并且E是末端单元，例如烷基氨基或单价氨基酸基团，例如NHCH（烷基）C（O）OH。该衍生物可用于治疗疱疹感染。

3. 发明申请

WO1996020171A1 ANTIHERPES PEPTIDOMIMETIC COMPOUNDS 审中-公开
标题翻译：抗生素化合物
公开(公告)号：WO1996020171A1
公开(公告)日：1996-07-04
申请号：PCT/CA1995000626
申请日：1995-10-31
申请人： BIO-MEGA/BOEHRINGER INGELHEIM RESEARCH INC.
发明人： BIO-MEGA/BOEHRINGER INGELHEIM RESEARCH INC. , DEZIEL, Robert , BRUNET, Montse, Llinas , MOSS, Neil , PLANTE, Raymond
IPC分类号： C07C275/16
CPC分类号： C07C275/16 , C07C271/22 , C07C2601/08 , C07C2601/14 , Y02P20/55
摘要： Disclosed herein are compounds of formula (1), wherein R is (1-3C)alkyl, R is hydrogen or (1-3C)alkyl and R is (1-3C)alkyl, or a therapeutically acceptable salt thereof. The compounds are useful for treating herpes infections.
摘要翻译：本文公开的是式（1）的化合物，其中R 1是（1-3C）烷基，R 2是氢或（1-3C）烷基，R 3是（1-3C）烷基，或其治疗上可接受的盐。该化合物可用于治疗疱疹感染。

4. 发明申请

WO1994007846A1 RENIN INHIBITING N-(2-AMINO-2-OXOETHYL)BUTANEDIAMIDE DERIVATIVES 审中-公开
标题翻译：雷宁抑制N-（2-氨基-2-氧代乙基）丁二酰胺衍生物
公开(公告)号：WO1994007846A1
公开(公告)日：1994-04-14
申请号：PCT/CA1993000380
申请日：1993-09-15
申请人： BIO-MEGA/BOEHRINGER INGELHEIM RESEARCH INC.
发明人： BIO-MEGA/BOEHRINGER INGELHEIM RESEARCH INC. , LAVALLEE, Pierre , SIMONEAU, Bruno
IPC分类号： C07C237/22
CPC分类号： C07D295/185 , C07C237/22 , C07D295/215
摘要： Disclosed herein are compounds of the formula: A-N(R1)C(O)CH2CHR2C(O)-B, wherein A is R3R4NC(O)CH2 wherein, for example, R3 is hydrogen or alkyl and R4 is hydrogen, alkyl or a substituted alkyl such as 2-(2-pyridinyl)ethyl, or R3 and R4 together with the nitrogen atom to which they are attached form a pyrrolidino, piperidino, morpholino or thiomorpholino; R1 is, for example, benzyl, alkyl or a substituted alkyl such as cyclohexylmethyl; R2 is, for example, alkyl, cycloalkylmethyl, 1(H)-imidazol-4-ylmethyl, 4-thiazolylmethyl or (2-amino-4-thiazolyl)methyl; and B is a renin substrate transition state analog, for example, (1(S)-(cyclohexylmethyl)-2(R),3(S)-dihydroxy-5-methylhexyl)amino. 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：AN（R 1）C（O）CH 2 CHR 2 C（O）-B，其中A是R 3 R 4 NC（O）CH 2，其中例如R 3是氢或烷基，R 4是氢，烷基或取代的烷基如2-（2-吡啶基）乙基或R3和R4与它们所连接的氮原子一起形成吡咯烷子基，哌啶子基，吗啉代或硫代吗啉代; R1是例如苄基，烷基或取代的烷基，例如环己基甲基; R2是例如烷基，环烷基甲基，1（H） - 咪唑-4-基甲基，4-噻唑基甲基或（2-氨基-4-噻唑基）甲基; （1）（S） - （环己基甲基）-2（R），3（S） - 二羟基-5-甲基己基）氨基。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. 发明申请

WO1996017821A1 PROCESS FOR THE PREPARATION OF ENANTIOMERICALLY PURE (S,S) AMINOEPOXIDES, KEY INTERMEDIATES FOR HIV PROTEASE INHIBITORS, VIA THEIR CHLOROHYDRINES 审中-公开
标题翻译：制备纯化（S，S）氨基氧化物的方法，艾滋病病毒蛋白酶抑制剂的主要中间体，通过其氯林酯
公开(公告)号：WO1996017821A1
公开(公告)日：1996-06-13
申请号：PCT/CA1995000625
申请日：1995-10-31
申请人： BIO-MEGA/BOEHRINGER INGELHEIM RESEARCH INC.
发明人： BIO-MEGA/BOEHRINGER INGELHEIM RESEARCH INC. , BEAULIEU, Pierre, Louis , GUINDON, Yvan , WERNIC, Dominik, Marek
IPC分类号： C07C213/00
CPC分类号： C07C213/08 , Y02P20/55
摘要： Disclosed herein is a stereospecific synthesis amenable to the large scale preparation of a hydrochloric acid addition salt of a chlorohydrin of formula (1) wherein R and R are amino protective groups and R is an amino acid side chain or a protected amino acid side chain. The synthesis involves reacting an aldehyde of formula (2) wherein R , R and R are as defined hereinbefore with (chloromethyl)lithium at -20 DEG C or below and contacting the resulting diastereoisomeric mixture of lithium alcoholates with aqueous hydrochloric acid to obtain a separable mixture of the hydrochloric acid addition salts of the chlorohydrin and its corresponding hydroxy diastereoisomer. The hydrochloric acid addition salt of the chlorohydrin is transformed readily into corresponding optionally amino-protected aminoepoxides; for example, 3(S)-(tert-butyloxycarbonylamino)-1,2(S)-epoxy-4-phenyl-butane.
摘要翻译：本文公开了适于大规模制备式（1）的氯醇的盐酸加成盐的立体特异性合成，其中R 1和R 2是氨基保护基，R 3是氨基酸侧链或被保护的氨基酸侧链。该合成包括使式（2）的醛（其中R 1，R 2和R 3如上定义）与（氯甲基）锂在-20℃或更低的温度下反应，并使所得的非对映异构体混合物与盐酸水溶液混合，得到氯醇的盐酸加成盐及其相应的羟基非对映异构体的可分离混合物。氯代醇的盐酸加成盐容易地转化成相应的任选氨基保护的氨基环氧化物; 例如，3（S） - （叔丁氧基羰基氨基）-1,2（S） - 环氧-4-苯基 - 丁烷。

6. 发明申请

WO1993018056A1 ISOSTERIC ANTIHERPES PEPTIDE DERIVATIVES 审中-公开
标题翻译：异构抗原肽衍生物
公开(公告)号：WO1993018056A1
公开(公告)日：1993-09-16
申请号：PCT/CA1993000095
申请日：1993-03-12
申请人： BIO-MEGA/BOEHRINGER INGELHEIM RESEARCH INC.
发明人： BIO-MEGA/BOEHRINGER INGELHEIM RESEARCH INC. , BEAULIEU, Pierre-Louis , DEZIEL, Robert , MOSS, Neil , PLANTE, Raymond
IPC分类号： C07K05/02
CPC分类号： C07D295/185 , A61K38/04 , C07C237/22 , C07C271/22 , C07C2601/08 , C07C2601/14 , C07K5/0207 , C07K5/06104 , A61K31/70 , A61K2300/00
摘要： Disclosed herein are peptide derivatives of the formula A-B-D-CH2CH{CH2C(O)R1}C(O)-NHCH{CR2(R3)COOH}C(O)-E wherein A is a terminal group, for example an optionally substituted phenylalkanoyl, and B is an N-methyl amino acid residue; or A and B together form a saturated or unsaturated alkylaminocarbonyl; D is an amino acid residue; R1 is alkyl, cycloalkyl, a monosubstituted or a disubstituted amino; R2 is hydrogen or alkyl and R3 is alkyl, or R2 is hydrogen and R3 is phenylalkyl, or R?2 and R3¿ are joined to form a cycloalkyl; and E is a terminal unit, for example, an alkylamino or a monovalent amino acid radical such as NHCH(alkyl)C(O)OH. The derivatives are useful for treating herpes infections.

7. 发明申请

WO1993018003A1 SUBSTITUED PIPECOLINIC ACID DERIVATIVES AS HIV PROTEASE INHIBITORS 审中-公开
标题翻译：作为艾滋病病毒蛋白酶抑制剂的替代的磷脂酸衍生物
公开(公告)号：WO1993018003A1
公开(公告)日：1993-09-16
申请号：PCT/CA1993000096
申请日：1993-03-12
申请人： BIO-MEGA/BOEHRINGER INGELHEIM RESEARCH INC.
发明人： BIO-MEGA/BOEHRINGER INGELHEIM RESEARCH INC. , ANDERSON, Paul, Cates , SOUCY, François , YOAKIM, Christiane , LAVALLEE, Pierre , BEAULIEU, Pierre, Louis
IPC分类号： C07D211/60
CPC分类号： C07D401/12 , C07D211/60 , C07D401/14
摘要： Disclosed herein are compounds of formula (1) wherein X is a terminal group, for exemple, an aryloxycarbonyl, an alkanoyl or an optionally mono- or disubstituted carbamoyl; B is absent or an amino acid residue, for example, Val or Asn; R1 is hydrogen or a ring substituent, for example, fluoro or methyl; R2 is alkyl; and Y is a ring substituent, for example, phenoxy, 2-pyridinylmethoxy, phenylthio or 2-pyridinylthio. The compounds inhibit the activity of human immunodeficiency virus (HIV) protease and interfere with HIV induced cytopathogenic effects in human cells. These properties render the compounds useful for combating HIV infections.

8. 发明申请

WO1994007845A1 N-(HYDROXYETHYL)BUTANEDIAMIDE DERIVATIVES AS RENIN INHIBITORS 审中-公开
标题翻译：作为瑞宁抑制剂的N-（羟基乙基）丁二酰胺衍生物
公开(公告)号：WO1994007845A1
公开(公告)日：1994-04-14
申请号：PCT/CA1993000379
申请日：1993-09-15
申请人： BIO-MEGA/BOEHRINGER INGELHEIM RESEARCH INC.
发明人： BIO-MEGA/BOEHRINGER INGELHEIM RESEARCH INC. , ANDERSON, Paul, Cates , HALMOS, Teddy , JUNG, Grace, Lorena , POUPART, Marc-André , SIMONEAU, Bruno
IPC分类号： C07C233/19
CPC分类号： C07D207/27 , C07C233/18 , C07C233/19 , C07C2601/02 , C07C2601/14 , C07D213/40 , C07D233/64 , C07D277/30 , C07D277/40 , C07D317/58
摘要： Disclosed herein are compounds of the formula: A-N(R1)C(O)CH2CHR2C(O)-B, wherein A is an oxygen-bearing radical selected from the group consisting of: (a) HO-CH(R3)CH2 wherein R3 is, for example, hydrogen, lower alkyl, lower cycloalkyl, phenyl or an unsubstituted five- or six-membered heterocyclic ring containing one or two hereroatoms selected from the group of N, O or S; (b) HO-CH2CH(R4) wherein R4 is, for example, lower alkyl or phenyl(lower)alkyl; and (c) HO-CR5(R6)CH2 wherein each of R5 and R6 is lower alkyl; or R5 and R6 together with the carbon atom to which they are attached form a 1,1-(lower cycloalkanediyl), 1,1-(4-hydroxycyclohexanediyl) or 1,1-(4-oxocyclohexanediyl); (d) (lower alkoxy)CR5A(R6A)CH2 wherein each of R5A and R6A is lower alkyl; or R5A and R6A together with the carbon atom to which they are attached form a 1,1-(lower cycloalkanediyl); and (e) (lower alkyl)C(O)CH2; R1 is, for example, benzyl, alkyl, a substituted alkyl such as cyclohexylmethyl, or R7R8NC(O)CH2 wherein R7 and R8 are alkyl such as methyl or ethyl; R2 is, for example, alkyl, cycloalkylmethyl, 1(H)-imidazol-4-ylmethyl, 4-thiazolylmethyl or (2-amino-4-thiazolyl)methyl; and B is a renin substrate transition state mimic, for example, (1(S)-(cyclohexylmethyl)-2(R),3(S)-dihydroxy-5-methylhexyl)amino. 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：AN（R 1）C（O）CH 2 CHR 2 C（O）-B，其中A是选自以下的含氧基团：（a）HO-CH（R3）CH2其中R3 是例如氢，低级烷基，低级环烷基，苯基或含有选自N，O或S的一个或两个天然原子的未取代的五元或六元杂环; （b）HO-CH2CH（R4）其中R4为例如低级烷基或苯基（低级）烷基; 和（c）HO-CR5（R6）CH2，其中R5和R6各自为低级烷基; 或R 5和R 6与它们所连接的碳原子一起形成1,1-（低级环烷二基），1,1-（4-羟基环己烷基）或1,1-（4-氧代环己烷二基）; （d）（低级烷氧基）CR5A（R6A）CH2，其中R5A和R6A各自为低级烷基; 或R5A和R6A与它们所连接的碳原子一起形成1,1-（低级环烷二基）; 和（e）（低级烷基）C（O）CH 2; R1是例如苄基，烷基，取代的烷基如环己基甲基或R7R8NC（O）CH2，其中R7和R8是烷基，例如甲基或乙基; R2是例如烷基，环烷基甲基，1（H） - 咪唑-4-基甲基，4-噻唑基甲基或（2-氨基-4-噻唑基）甲基; （1）（S） - （环己基甲基）-2（R），3（S） - 二羟基-5-甲基己基）氨基。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。

9. 发明授权

US5565476A N-(hydroxyethyl)butanediamide derivatives 失效
标题翻译： N-（羟乙基）丁二酰胺衍生物
公开(公告)号：US5565476A
公开(公告)日：1996-10-15
申请号：US432409
申请日：1995-05-01
申请人： Paul C. Anderson , Teddy Halmos , Grace L. Jung , Marc-Andr e Poupart , Bruno Simoneau
发明人： Paul C. Anderson , Teddy Halmos , Grace L. Jung , Marc-Andr e Poupart , Bruno Simoneau
IPC分类号： A61K31/16 , A61K31/165 , A61K31/40 , A61K31/4015 , A61K31/415 , A61K31/42 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4418 , A61P9/12 , A61P43/00 , C07C233/18 , C07C233/19 , C07C237/22 , C07D207/26 , C07D207/27 , C07D213/40 , C07D233/54 , C07D233/64 , C07D277/28 , C07D277/30 , C07D277/40 , C07D317/58 , C07D417/12
CPC分类号： C07D207/27 , C07C233/18 , C07C233/19 , C07D213/40 , C07D233/64 , C07D277/30 , C07D277/40 , C07D317/58 , C07C2101/02 , C07C2101/14
摘要： Disclosed herein are compounds of the formula:A'--N(R.sup.1')C(O)CH.sub.2 CHR.sup.2 C(O)--Bwherein A' is, for example, HO--CR.sup.5 (R.sup.6)CH.sub.2 wherein R.sup.5 and R.sup.6 together with the carbon atom to which they are attached form a 1,1-(lower cycloalkanediyl); R.sup.1' is R.sup.7 R.sup.8 NC(O)CH.sub.2 wherein R.sup.7 is lower alkyl and R.sup.8 is pyridinyl-(CH.sub.2).sub.n wherein n is the integer one or two; R.sup.2 is, for example, 4-thiazolylmethyl or (2-amino-4-thiazolyl)methyl; and B is a renin substrate transition state mimic, for example, [1(S)-(cyclohexylmethyl)-2(R), 3(S)-dihydroxy-5-methylhexyl]amino. 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：A'-N（R 1'）C（O）CH 2 CHR 2 C（O）-B，其中A'是例如HO-CR 5（R 6）CH 2，其中R 5和R 6与碳原子它们连接形成1,1-（低级环烷二基）; R 1'是R 7 R 8 NC（O）CH 2，其中R 7是低级烷基，R 8是吡啶基 - （CH 2）n，其中n是整数1或2; R2是例如4-噻唑基甲基或（2-氨基-4-噻唑基）甲基; B是肾素底物过渡态模拟物，例如[1（S） - （环己基甲基）-2（R），3（S） - 二羟基-5-甲基己基]氨基。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。

10. 发明授权

US5550291A Process for key intermediates for HIV protease inhibitors 失效
标题翻译： HIV蛋白酶抑制剂关键中间体的方法
公开(公告)号：US5550291A
公开(公告)日：1996-08-27
申请号：US434691
申请日：1995-05-04
申请人： Pierre L. Beaulieu , Yvan Guindon , Dominik M. Wernic
发明人： Pierre L. Beaulieu , Yvan Guindon , Dominik M. Wernic
IPC分类号： C07D303/36 , C07B53/00 , C07C213/00 , C07C213/08 , C07C215/28 , C07C217/60 , C07C209/26 , C07C209/54 , C07C209/68 , C07C209/82
CPC分类号： C07C213/08 , Y02P20/55
摘要： Disclosed herein is a stereospecific synthesis amenable to the large scale preparation of a hydrochloric acid addition salt of a chlorohydrin of the formula ##STR1## wherein R.sup.1 and R.sup.2 are amino protective groups and R.sup.3 is an amino acid side chain or a protected amino acid side chain. The synthesis involves reacting an aldehyde of the formula ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined hereinbefore with (chloromethyl)lithium at -20.degree. C. or below and contacting the resulting diastereoisomeric mixture of lithium alcoholates with aqueous hydrochloric acid to obtain a separable mixture of the hydrochloric acid addition salts of the chlorohydrin and its corresponding hydroxy diastereoisomer. The hydrochloric acid addition salt of the chlorohydrin is transformed readily into corresponding optionally amino-protected aminoepoxides; for example, 3(S)-(tert-butyloxycarbonylamino)-l,2(S)-epoxy-4-phenyl-butane.
摘要翻译：本文公开了一种立体特异性合成，其可以大规模制备下式的氯醇的盐酸加成盐：其中R1和R2是氨基保护基，R3是氨基酸侧链或被保护的氨基酸侧链。该合成包括使式（Ia）的醛，其中R 1，R 2和R 3如上文所定义，与（氯甲基）锂在-20℃或更低的温度下反应，并使所得到的醇锂与盐酸水溶液的非对映异构体混合物接触，得到氯代醇的盐酸加成盐及其相应的羟基非对映异构体的可分离的混合物。氯代醇的盐酸加成盐容易地转化成相应的任选氨基保护的氨基环氧化物; 例如，3（S） - （叔丁氧基羰基氨基）-1,2（S） - 环氧-4-苯基 - 丁烷。

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