Compounds derived from boronic acid
    13.
    发明授权
    Compounds derived from boronic acid 失效
    衍生自硼酸的化合物

    公开(公告)号:US5814622A

    公开(公告)日:1998-09-29

    申请号:US807569

    申请日:1997-02-27

    CPC分类号: C07F5/025

    摘要: Compound of formula (I) ##STR1## in which: R.sub.1 and R.sub.2, which are identical or different, represent hydrogen or alkyl or alternatively R.sub.1 and R.sub.2 form, with the carbon atom which bears them, cycloalkyl, R.sub.3 represents hydrogen or alkyl, phenyl or benzyl, R.sub.4 represents: optionally substituted amino, optionally substituted amindino, optionally substituted guanidino, optionally substituted isothioureido, optionally substituted iminomethylamino, mercapto substituted with heterocyclic, or heterocyclic, R.sub.5 and R.sub.6 each represent hydrogen or alkyl, or ##STR2## forms a boronic ester of pinanediol, m represents an integer such that 0.ltoreq.m.ltoreq.6, n represents an integer such that 1.ltoreq.n.ltoreq.6, A represents any one of the following groups: * optionally substituted bicycloalkyl (C.sub.5 -C.sub.10)phenyl, * or a group of formula: ##STR3## A.sub.1 represents --CO--, --CS--, --SO.sub.2 --, the isomers thereof and the addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same are useful as trypsin-like serine proteases.

    摘要翻译: 式(I)化合物其中:R 1和R 2相同或不同,代表氢或烷基,或者R1和R2与带有它们的碳原子形成环烷基,R3代表氢或 烷基,苯基或苄基,R4表示:任选取代的氨基,任选取代的氨基,任选取代的胍基,任选取代的异硫脲基,任选取代的亚氨基甲基氨基,被杂环或杂环取代的巯基,R 5和R 6各自表示氢或烷基, 形成蒎二醇的硼酸酯,m表示0≤n≤6的整数,n表示1≤n≤6的整数,A表示以下基团中的任一个:*任选地 取代的双环烷基(C 5 -C 10)苯基,或下式的基团:A 1表示-CO - , - CS-,-SO 2 - ,其异构体及其与药学上可接受的酸或碱的加成盐,和 使用含有该药物的药用产品 作为胰蛋白酶样丝氨酸蛋白酶。

    Alpha-amino acid sulphonyl compounds
    15.
    发明授权
    Alpha-amino acid sulphonyl compounds 失效
    α-氨基酸磺酰基化合物

    公开(公告)号:US06716843B2

    公开(公告)日:2004-04-06

    申请号:US10109407

    申请日:2002-03-28

    IPC分类号: A61K3140

    摘要: Compound of formula (I): wherein:  represents an optionally substituted, 5-membered, nitrogen-containing heterocycle, R1 represents hydrogen, alkyl, acyl, prolyl, alanyl, histidylprolyl or phenylalanylprolyl, Ak represents an alkylene or heteroalkylene chain, X represents a single bond or optionally substituted phenylene, R2 represents optionally substituted alkyl, (C3-C10)cycloalkyl, or —NR2aR2b wherein R2a and R2b, which may be the same or different, each represent hydrogen or alkyl or, together with the nitrogen atom carrying them, form a nitrogen-containing heterocycle, Y represents R3 represents hydrogen or a group selected from alkyl, (C3-C7) cycloalkyl and aryl, R4, R5 and R6, which may be the same or different, each represent hydrogen or alkyl, or R4 and R6, or R5 and R6, together with the atoms carrying them, form an imidazolidine or dihydrobenzimidazole ring, its optical isomers and addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful as inhibitors of dipeptidyl-peptidase IV.

    摘要翻译: 式(I)化合物:其中:表示任选取代的5元含氮杂环,R 1表示氢,烷基,酰基,脯氨酰基,丙氨酰,组氨酰脯氨酰基或苯丙氨酰脯氨酰基,Ak表示亚烷基或杂亚烷基链,X表示 单键或任选取代的亚苯基,R 2表示任选取代的烷基,(C 3 -C 10)环烷基或-NR 2 a R 2b,其中可以相同或不同的R 2a和R 2b各自代表氢或烷基,或与携带它们的氮原子一起 ,形成含氮杂环,Y表示R 3表示氢或选自烷基,(C 3 -C 7)环烷基和芳基的基团,R 4,R 5和R 6可以相同或不同,各自表示氢或烷基,或R 4 和R6或R5和R6与携带它们的原子一起形成咪唑烷或二氢苯并咪唑环,其光学异构体及其与药学上可接受的酸的加成盐。含有相同的喔 ch可用作二肽基肽酶IV的抑制剂。

    Peptides derived from trifluoromethylketones
    17.
    发明授权
    Peptides derived from trifluoromethylketones 失效
    衍生自三氟甲基酮的肽

    公开(公告)号:US5567804A

    公开(公告)日:1996-10-22

    申请号:US437433

    申请日:1995-05-05

    CPC分类号: C07K5/06191 A61K38/00

    摘要: Compounds of formula (I): ##STR1## in which: R.sub.1 represents alkyl or (C.sub.3 -C.sub.7) cycloalkylR.sub.2 represents alkyl, or (C.sub.3 -C.sub.7) cycloalkyl,R.sub.3 represents hydrogen or alkyl,R.sub.4 represents halogen or alkyl or alkoxy,R.sub.5 represents alkyl,X and Y, which are different, represent CO or SO.sub.2,n represents 1, 2 or 3,p represents 0 or 1,Z represents sulfur or oxygen,A represents any one of the following groups: ##STR2## in which: A.sub.1 represents, with the nitrogen and carbon atoms to which it is attached, a mono- or bicyclic heterocycle,.cndot. or, ##STR3## in which: R.sub.6 represents hydrogen, alkyl or cycloalkyl or 2-indanyl,R.sub.7 represents hydrogen or alkyl,which compounds of formula (I) comprise thereof corresponding hydrates of the ketone function COCF.sub.3,the enantiomers, diastereoisomers and epimers thereof and the addition salts thereof with a pharmaceutically acceptable base and medical products containing the same are useful as HLE inhibitor.

    摘要翻译: 式(I)化合物:其中:R 1表示烷基或(C 3 -C 7)环烷基R 2表示烷基或(C 3 -C 7)环烷基,R 3表示氢或烷基,R 4表示卤素或烷基或 烷氧基,R5表示烷基,X和Y不同,表示CO或SO2,n表示1,2或3,p表示0或1,Z表示硫或氧,A表示以下基团中的任一个:其中:A1表示与其连接的氮和碳原子一一或二环杂环。 或者,其中:R 6表示氢,烷基或环烷基或2-二氢化茚基,R 7表示氢或烷基,式(I)化合物包含其相应的酮官能团COCF 3的水合物,其对映异构体,非对映异构体和差向异构体 并且其与药学上可接受的碱的加成盐和含有它们的医药产品可用作HLE抑制剂。

    Indanyl-piperazine compounds
    18.
    发明授权
    Indanyl-piperazine compounds 失效
    茚基 - 哌嗪化合物

    公开(公告)号:US07442692B2

    公开(公告)日:2008-10-28

    申请号:US11391916

    申请日:2006-03-29

    摘要: A compound selected from those of formula (I): wherein: R3 represents a hydrogen atom, and R1 and R2 together with the carbon atoms carrying them form a benzene, naphthalene or quinoline ring structure, each of the ring structures being optionally substituted, or R1 represents a hydrogen atom, and R2 and R3 together with the carbon atoms carrying them form a benzene, naphthalene or quinoline ring structure, each of the ring structures being optionally substituted, n represents 1 or 2, —X— represents a group selected from —(CH2)m—O-Ak-, —(CH2)m—NR4-Ak-, —(CO)—NR4-Ak- and —(CH2)m—NR4-(CO)—, m represents an integer between 1 and 6 inclusive, Ak represents an optionally substituted alkylene chain, and R4 represents a hydrogen atom or an alkyl group, Ar represents an aryl or heteroaryl group, its enantiomers, diasteroisomers, and addition salts thereof with a pharmaceutically acceptable acid. Medical products containing the same which are useful in the treatment of conditions requiring a serotonin reuptake inhibitor and/or NK1 antagonist.

    摘要翻译: 选自式(I)的化合物的化合物:其中:R 3表示氢原子,R 1和R 2与 带有它们的碳原子形成苯,萘或喹啉环结构,每个环结构任选被取代,或R 1表示氢原子,R 2和R 2 3个与携带它们的碳原子一起形成苯,萘或喹啉环结构,每个环结构可以被取代,n表示1或2,-X-表示选自 - ( CH 2 - (CH 2)n -O - , - (CH 2 CH 2)m -NR 2 -Ak-, - (CO)-NR 4 - 和 - (CH 2)2 -N (CO) - ,m表示1和6之间的整数,包括1和6,Ak表示任选取代的亚烷基链,并且R 4表示氢原子或烷基,Ar 表示芳基或杂芳基,其对映异构体,diastero 异构体及其与药学上可接受的酸的加成盐。 含有该药物的医药产品可用于治疗需要5-羟色胺再摄取抑制剂和/或NK1拮抗剂的病症。

    Indanyl-piperazine compounds
    19.
    发明申请
    Indanyl-piperazine compounds 失效
    茚基 - 哌嗪化合物

    公开(公告)号:US20060223830A1

    公开(公告)日:2006-10-05

    申请号:US11391916

    申请日:2006-03-29

    IPC分类号: A61K31/495 C07D241/04

    摘要: A compound selected from those of formula (I): wherein: R3 represents a hydrogen atom, and R1 and R2 together with the carbon atoms carrying them form a benzene, naphthalene or quinoline ring structure, each of the ring structures being optionally substituted,  or R1 represents a hydrogen atom, and R2 and R3 together with the carbon atoms carrying them form a benzene, naphthalene or quinoline ring structure, each of the ring structures being optionally substituted, n represents 1 or 2, —X— represents a group selected from —(CH2)m—O-Ak-, —(CH2)m—NR4-Ak-, —(CO)—NR4-Ak- and —(CH2)m—NR4-(CO)—,  m represents an integer between 1 and 6 inclusive, Ak represents an optionally substituted alkylene chain, and R4 represents a hydrogen atom or an alkyl group, Ar represents an aryl or heteroaryl group, its enantiomers, diasteroisomers, and addition salts thereof with a pharmaceutically acceptable acid. Medical products containing the same which are useful in the treatment of conditions requiring a serotonin reuptake inhibitor and/or NK1 antagonist.

    摘要翻译: 选自式(I)的化合物的化合物:其中:R 3表示氢原子,R 1和R 2与 带有它们的碳原子形成苯,萘或喹啉环结构,每个环结构任选被取代,或R 1表示氢原子,R 2和R 2 3个与携带它们的碳原子一起形成苯,萘或喹啉环结构,每个环结构可以被取代,n表示1或2,-X-表示选自 - ( CH 2 - (CH 2)n -O - , - (CH 2 CH 2)m -NR 2 -Ak-, - (CO)-NR 4 - 和 - (CH 2)2 -N (CO) - ,m表示1和6之间的整数,包括1和6,Ak表示任选取代的亚烷基链,并且R 4表示氢原子或烷基,Ar 表示芳基或杂芳基,其对映异构体,diastero 异构体及其与药学上可接受的酸的加成盐。 含有该药物的医药产品可用于治疗需要5-羟色胺再摄取抑制剂和/或NK1拮抗剂的病症。