Hepatitis C inhibitor tri-peptides
    1.
    再颁专利
    Hepatitis C inhibitor tri-peptides 有权
    丙型肝炎抑制剂三肽

    公开(公告)号:USRE42164E1

    公开(公告)日:2011-02-22

    申请号:US12119609

    申请日:2008-05-13

    Abstract: Racemates, diastereoisomers and optical isomers of a compound of formula (I): wherein B is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of which optionally substituted with C1-6 alkyl; C1-6 alkoxy; C1-6 alkanoyl; hydroxy; hydroxyalkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with C1-6 alkyl; amido; or (lower alkyl)amide; or B is an acyl derivative of formula R4—C(O)—; a carboxyl of formula R4—O—C(O)—; an amide of formula R4—N(R5)—C(O)—; a thioamide of formula R4—N(R5)—C(S)—; or a sulfonyl of formula R4—SO2; R5 is H or C1-6 alkyl; and Y is H or C1-6 alkyl; R3 is C1-8 alkyl, C3-7 cycloalkyl, or C4-10 alkylcycloalkyl, all optionally substituted with hydroxy, C1-6 alkoxy, C1-6 thioalkyl, amido, (lower alkyl)amido, C6 or C10 aryl, or C7-16 aralkyl; R2 is CH2—R20, NH—R20, O—R20 or S—R20, wherein R20 is a saturated or unsaturated C3-7 cycloalkyl or C4-10 (alkylcycloalkyl), all of which being optionally mono-, di- or tri-substituted with R21, or R20 is a C6 or C10 aryl or C7-14 aralkyl optionally substituted, or R20 is Het or (lower alkyl)-Het, both optionally substituted, Het or (lower alkyl)-Het; carboxyl; carboxy(lower alkyl); C6 or C10 aryl, C7-14 aralkyl or Het, said aryl, aralkyl or Het being optionally substituted; and R1 is H; C1-6 alkyl, C3-7 cycloalkyl, C2-6 alkenyl, or C2-6 alkynyl, all optionally substituted with halogen; or a pharmaceutically acceptable salt or ester thereof.

    Abstract translation: 式(I)化合物的外消旋体,非对映异构体和光学异构体:其中B是H,C6或C10芳基,C7-16芳烷基; Het或(低级烷基)-Het,其全部任选被C 1-6烷基取代; C 1-6烷氧基 C 1-6烷酰基; 羟基; 羟烷基 光环; 卤代烷基 硝基 氰基; 氰基烷基; 任选被C 1-6烷基取代的氨基; 氨基酸 或(低级烷基)酰胺; 或B是式R4-C(O) - 的酰基衍生物; 式R4-O-C(O) - 的羧基; 式R 4 -N(R 5)-C(O) - 的酰胺; 式R 4 -N(R 5)-C(S) - 的硫代酰胺; 或式R4-SO2的磺酰基; R5是H或C1-6烷基; Y为H或C 1-6烷基; R 3是C 1-8烷基,C 3-7环烷基或C 4-10烷基环烷基,全部任选被羟基,C 1-6烷氧基,C 1-6硫烷基,酰氨基,(低级烷基)酰氨基,C 6或C 10芳基或C 7〜 16芳烷基; R2是CH2-R20,NH-R20,O-R20或S-R20,其中R20是饱和或不饱和的C3-7环烷基或C4-10(烷基环烷基),它们都是任选的单 - ,二 - 或三 - 或R 20为任选取代的C 6或C 10芳基或C 7-14芳烷基,或R 20为Het或(低级烷基)-Het,均为任选取代的Het或(低级烷基)-Het; 羧基; 羧基(低级烷基); C6或C10芳基,C7-14芳烷基或Het,所述芳基,芳烷基或Het任选被取代; 且R1为H; C 1-6烷基,C 3-7环烷基,C 2-6烯基或C 2-6炔基,全部被卤素取代; 或其药学上可接受的盐或酯。

    Dab9 derivatives of lipopeptide antibiotics and methods of making and using the same
    2.
    发明授权
    Dab9 derivatives of lipopeptide antibiotics and methods of making and using the same 失效
    Dab9衍生物的脂肽抗生素及其制备及使用方法

    公开(公告)号:US07655623B2

    公开(公告)日:2010-02-02

    申请号:US11539139

    申请日:2006-10-05

    CPC classification number: C07K7/56 A61K38/00

    Abstract: The present invention provides Dab9 derivatives of amphomycin-type lipopepetide antibiotics that display antimicrobial activity against Gram-positive bacteria, methods and intermediates for synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of infections.

    Abstract translation: 本发明提供了表现出抗革兰氏阳性菌的抗微生物活性的两性霉素型脂蛋白抗生素的Dab9衍生物,用于合成化合物的方法和中间体以及在多种情况下使用化合物的方法,包括治疗和预防感染。

    Hepatitis C inhibitor tri-peptides
    3.
    发明授权
    Hepatitis C inhibitor tri-peptides 有权
    丙型肝炎抑制剂三肽

    公开(公告)号:US06410531B1

    公开(公告)日:2002-06-25

    申请号:US09849057

    申请日:2001-05-04

    Abstract: Racemates, diastereoisomers and optical isomers of a compound of formula (I): wherein B is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of which optionally substituted with C1-6 alkyl; C1-6 alkoxy; C1-6 alkanoyl; hydroxy; hydroxyalkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with C1-6 alkyl; amido; or (lower alkyl)amide; or B is an acyl derivative of formula R4—C(O)—; a carboxyl of formula R4—O—C(O)—; an amide of formula R4—N(R5)—C(O)—; a thioamide of formula R4—N(R5)—C(S)—; or a sulfonyl of formula R4—SO2; R5 is H or C1-6 alkyl; and Y is H or C1-6 alkyl; R3 is C1-8 alkyl, C3-7 cycloalkyl, or C4-10 alkylcycloalkyl, all optionally substituted with hydroxy, C1-6 alkoxy, C1-6 thioalkyl, amido, (lower alkyl)amido, C6 or C10 aryl, or C7-16 aralkyl; R2 is CH2—R20, NH—R20, O—R20 or S—R20, wherein R20 is a saturated or unsaturated C3-7 cycloalkyl or C4-10 (alkylcycloalkyl), all of which being optionally mono-, di- or tri-substituted with R21, or R20 is a C6 or C10 aryl or C7-14 aralkyl optionally substituted, or R20 is Het or (lower alkyl)-Het, both optionally substituted, Het or (lower alkyl)-Het; carboxyl; carboxy(lower alkyl); C6 or C10 aryl, C7-14 aralkyl or Het, said aryl, aralkyl or Het being optionally substituted; and R1 is H; C1-6 alkyl, C3-7 cycloalkyl, C2-6 alkenyl, or C26 alkynyl, all optionally substituted with halogen; or a pharmaceutically acceptable salt or ester thereof.

    Abstract translation: 式(I)化合物的外消旋物,非对映异构体和光学异构体:其中B是H,C6或C10芳基,C7-16芳烷基; Het或(低级烷基)-Het,其全部任选被C 1-6烷基取代; C 1-6烷氧基 C 1-6烷酰基; 羟基; 羟烷基 光环; 卤代烷基 硝基 氰基; 氰基烷基 任选被C 1-6烷基取代的氨基; 氨基酸 或(低级烷基)酰胺; 或B是式R4-C(O) - 的酰基衍生物; 式R4-O-C(O) - 的羧基; 式R 4 -N(R 5)-C(O) - 的酰胺; 式R 4 -N(R 5)-C(S) - 的硫代酰胺; 或式R4-SO2的磺酰基; R5是H或C1-6烷基; 并且Y是H或C 1-6烷基; R 3是C 1-8烷基,C 3-7环烷基或C 4-10烷基环烷基,全部被羟基,C 1-6烷氧基,C 1-6硫烷基,酰氨基,(低级烷基) ,C6或C10芳基或C7-16芳烷基; R2是CH2-R20,NH-R20,O-R20或S-R20,其中R20是饱和或不饱和的C3-7环烷基或C4-10(烷基环烷基),全部 其任选被R 21单取代,二取代或三取代,或R 20为任选取代的C 6或C 10芳基或C 7-14芳烷基,或R 20为Het或(低级烷基)-Het,均为任选取代的Het或 (低级烷基)-Het; 羧基; 羧基(低级烷基); C6或C10芳基,C7-14芳烷基或Het,所述芳基,芳烷基或Het任选被取代; 且R1为H; C 1-6烷基,C 3-7环烷基,C 2-6烯基或C 26炔基,全部被卤素取代; 或其药学上可接受的盐或酯。

    Hepatitis C inhibitor tri-peptides
    4.
    再颁专利
    Hepatitis C inhibitor tri-peptides 有权
    丙型肝炎抑制剂三肽

    公开(公告)号:USRE41894E1

    公开(公告)日:2010-10-26

    申请号:US12042627

    申请日:2008-03-05

    Abstract: Racemates, diastereoisomers and optical isomers of a compound of formula (I): wherein B is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of which optionally substituted with C1-6 alkyl; C1-6 alkoxy; C1-6 alkanoyl; hydroxy; hydroxy-alkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with C1-6 alkyl; amido; or (lower alkyl)amide; or B is an acyl derivative of formula R4—C(O)—; a carboxyl of formula R4—O—C(O)—; an amide of formula R4—N(R5)—C(O)—; a thioamide of formula R4—N(R5)—C(S)—; or a sulfonyl of formula R4—SO2; R5 is H or C1-6 alkyl; and Y is H or C1-6 alkyl; R3 is C3-7 cycloalkyl, or C4-10 alkylcycloalkyl, all optionally substituted with hydroxy, C1-6 alkoxy, C1-6 thioalkyl, amido, (lower alkyl)amido, C6 or C10 aryl, or C7-16 aralkyl; R2 is CH2—R20, NH—R20, O—R20 or S—R20, wherein R20 is a saturated or unsaturated C3-7 cycloalkyl or C4-10 (alkylcycloalkyl), all of which being optionally mono-, di- or tri-substituted with R21, or R20 is a C6 or C10 aryl or C7-14 aralkyl optionally substituted, or R20 is Het or (lower alkyl)-Het, both optionally substituted, Het or (lower alkyl)-Het; carboxyl; carboxy(lower alkyl); C6 or C10 aryl, C7-14 aralkyl or Het, said aryl, aralkyl or Het being optionally substituted; and R1 is H; C1-6 alkyl, C3-7 cycloalkyl, C2-6 alkenyl, or C2-6 alkynyl, all optionally substituted with halogen; or a pharmaceutically acceptable salt or ester thereof.

    Abstract translation: 式(I)化合物的外消旋体,非对映异构体和光学异构体:其中B是H,C6或C10芳基,C7-16芳烷基; Het或(低级烷基)-Het,其全部任选被C 1-6烷基取代; C 1-6烷氧基 C 1-6烷酰基; 羟基; 羟基 - 烷基; 光环; 卤代烷基 硝基 氰基; 氰基烷基 任选被C 1-6烷基取代的氨基; 氨基酸 或(低级烷基)酰胺; 或B是式R4-C(O) - 的酰基衍生物; 式R4-O-C(O) - 的羧基; 式R 4 -N(R 5)-C(O) - 的酰胺; 式R 4 -N(R 5)-C(S) - 的硫代酰胺; 或式R4-SO2的磺酰基; R5是H或C1-6烷基; Y为H或C 1-6烷基; R 3为C 3-7环烷基或C 4-10烷基环烷基,全部任选被羟基取代,C 1-6烷氧基,C 1-6硫烷基,酰氨基,(低级烷基)酰氨基,C 6或C 10芳基或C 7-16芳烷基; R2是CH2-R20,NH-R20,O-R20或S-R20,其中R20是饱和或不饱和的C3-7环烷基或C4-10(烷基环烷基),它们都是任选的单 - ,二 - 或三 - 或R 20为任选取代的C 6或C 10芳基或C 7-14芳烷基,或R 20为Het或(低级烷基)-Het,均为任选取代的Het或(低级烷基)-Het; 羧基; 羧基(低级烷基); C6或C10芳基,C7-14芳烷基或Het,所述芳基,芳烷基或Het任选被取代; 且R1为H; C 1-6烷基,C 3-7环烷基,C 2-6烯基或C 2-6炔基,全部被卤素取代; 或其药学上可接受的盐或酯。

    Hepatitis C inhibitor tri-peptides
    5.
    再颁专利
    Hepatitis C inhibitor tri-peptides 有权
    丙型肝炎抑制剂三肽

    公开(公告)号:USRE41356E1

    公开(公告)日:2010-05-25

    申请号:US12118926

    申请日:2008-05-12

    Abstract: Racemates, diastereolsomers and optical isomers of a compound of formula (I): wherein B is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of which optionally substituted with C1-6 alkyl; C1-6 alkoxy; C1-6 alkanoyl; hydroxy; hydroxyalkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with C1-6 alkyl; amido; or (lower alkyl)amide; or B is an acyl derivative of formula R4—C(O)—; a carboxyl of formula R4—O—C(O)—; an amide of formula R4—N(R5)—C(O)—; a thioamide of formula R4—N(R5)—C(S)—; or a sulfonyl of formula R4—SO2; R5 is H or C1-6 alkyl; and Y is H or C1-6 alkyl; R3 is C1-8 alkyl, C3-7 cycloalkyl, or C4-10 alkylcycloalkyl, all optionally substituted with hydroxy, C1-6 alkoxy, C1-6 thioalkyl, amido, (lower alkyl)amido, C6 or C10 aryl, or C7-16 aralkyl; R2 is CH2—R20, NH—R20, O—R20 or S—R20, wherein R20 is a saturated or unsaturated C3-7 cycloalkyl or C4-10 (alkylcycloalkyl), all of which being optionally mono-, di- or tri-substituted with R21, or R20 is a C6 or C10 aryl or C7-14 aralkyl optionally substituted, or R20 is Het or (lower alkyl)-Het, both optionally substituted, Het or (lower alkyl)-Het; carboyl; carboxy(lower alkyl); C6 or C10 aryl, C7-14 aralkyl or Het, said aryl, aralkyl or Het being optionally substituted; and R1 is H; C1-6 alkyl, C3-7 cycloalkyl, C2-6 alkenyl, or C2-6 alkynyl, all optionally substituted with halogen; or a pharmaceutically acceptable salt or ester thereof.

    Abstract translation: 式(I)化合物的外消旋物,非对映异构体和光学异构体:其中B是H,C6或C10芳基,C7-16芳烷基; Het或(低级烷基)-Het,其全部任选被C 1-6烷基取代; C 1-6烷氧基; C 1-6烷酰基; 羟基; 羟烷基 光环; 卤代烷基 硝基 氰基; 氰基烷基 任选被C 1-6烷基取代的氨基; 氨基酸 或(低级烷基)酰胺; 或B是式R4-C(O) - 的酰基衍生物; 式R4-O-C(O) - 的羧基; 式R 4 -N(R 5)-C(O) - 的酰胺; 式R 4 -N(R 5)-C(S) - 的硫代酰胺; 或式R4-SO2的磺酰基; R5是H或C1-6烷基; Y为H或C 1-6烷基; R 3是C 1-8烷基,C 3-7环烷基或C 4-10烷基环烷基,全部任选被羟基,C 1-6烷氧基,C 1-6硫烷基,酰氨基,(低级烷基)酰氨基,C 6或C 10芳基或C 7〜 16芳烷基; R2是CH2-R20,NH-R20,O-R20或S-R20,其中R20是饱和或不饱和的C3-7环烷基或C4-10(烷基环烷基),它们都是任选的单 - ,二 - 或三 - 或R 20为任选取代的C 6或C 10芳基或C 7-14芳烷基,或R 20为Het或(低级烷基)-Het,均为任选取代的Het或(低级烷基)-Het; 羰基 羧基(低级烷基); C6或C10芳基,C7-14芳烷基或Het,所述芳基,芳烷基或Het任选被取代; 且R1为H; C 1-6烷基,C 3-7环烷基,C 2-6烯基或C 2-6炔基,全部被卤素取代; 或其药学上可接受的盐或酯。

    Method of identifying potential inhibitors of human papillomavirus protein E2 using x-ray atomic coordinates
    6.
    发明授权
    Method of identifying potential inhibitors of human papillomavirus protein E2 using x-ray atomic coordinates 有权
    使用x射线原子坐标识别人乳头瘤病毒蛋白E2的潜在抑制剂的方法

    公开(公告)号:US07167801B2

    公开(公告)日:2007-01-23

    申请号:US10193460

    申请日:2002-07-11

    Abstract: A crystallizable composition, comprising an human papillomavirus (HPV-11) E2 transactivation domain (TAD)-like polypeptide of SEQ ID NO. 2 complexed with an inhibitor L (sodium (2R,3R,4S,5R)-5-(3,4-dichlorophenyl)-5′-methyl-1′,3′-dioxo-4-({[4-(1,2,3-thiadiazol-4-yl)phenyl]amino}carbonyl)-1′,3′,4,5-tetrahydro-3H-spiro[furan-2,2′-indene]-3-carboxylate). The invention also provides a method for producing the crystallized HPV E2 TAD-inhibitor complex (HPV E2 TAD-L) comprising: a) mixing purified HPV E2 TAD, contained in a purification buffer, with solublized inhibitor L to generate a complex solution containing the HPV E2 TAD-L complex; and b) crystallizing the complex from a) in a crystallization buffer. The invention also provides a method for producing crystallized apo HPV E2 TAD, comprising: a) mixing apo HPV E2 TAD, contained in a purification buffer, with a crystallization buffer.X-ray crystal structure coordinates the HPV E2 TAD-L complex, are also provided, which define an inhibitor binding pocket. The inhibitor binding pocket is useful for screening potential small molecule inhibitors that bind to the pocket that may be inhibitors of papillomavirus infection.

    Abstract translation: 一种可结晶组合物,其包含SEQ ID NO.1的人乳头状瘤病毒(HPV-11)E2反式激活结构域(TAD)样多肽。 2与抑制剂L((2R,3R,4S,5R)-5-(3,4-二氯苯基)-5'-甲基-1',3'-二氧代-4 - ({[4-(1 ,2,3-噻二唑-4-基)苯基]氨基}羰基)-1',3',4,5-四氢-3H-螺[呋喃-2,2'-茚] -3-羧酸乙酯)。 本发明还提供了一种生产结晶的HPV E2 TAD抑制剂复合物(HPV E2 TAD-L)的方法,包括:a)将纯化缓冲液中纯化的HPV E2 TAD与溶出的抑制剂L混合以产生含有 HPV E2 TAD-L复合物; 和b)从结晶缓冲液中的a)结晶复合物。 本发明还提供了一种用于生产结晶apo HPV E2 TAD的方法,其包括:a)将包含在纯化缓冲液中的apo HPV E2 TAD与结晶缓冲液混合。 还提供X射线晶体结构协调HPV E2 TAD-L复合物,其定义了抑制剂结合口袋。 抑制剂结合口袋可用于筛选结合口袋的可能是乳头瘤病毒感染抑制剂的潜在小分子抑制剂。

    Dab9 derivatives of lipopeptide antibiotics and methods of making and using the same
    7.
    发明授权
    Dab9 derivatives of lipopeptide antibiotics and methods of making and using the same 失效
    Dab9衍生物的脂肽抗生素及其制备及使用方法

    公开(公告)号:US07125844B2

    公开(公告)日:2006-10-24

    申请号:US10336641

    申请日:2003-01-02

    CPC classification number: C07K7/56 A61K38/00

    Abstract: The present invention provides Dab9 derivatives of amphomycin-type lipopeptide antibiotics that display antimicrobial activity against Gram-positive bacteria, methods and intermediates for synthesizing such compounds, and methods of using the compounds in a variety of contexts, including in the treatment and prevention of infections.

    Abstract translation: 本发明提供了显示抗革兰氏阳性菌的抗微生物活性的两性霉素型脂肽抗生素的Dab 9+衍生物,用于合成这些化合物的方法和中间体,以及在各种情况下使用该化合物的方法, 包括治疗和预防感染。

    Non-nucleoside reverse transcriptase inhibitors
    8.
    发明授权
    Non-nucleoside reverse transcriptase inhibitors 有权
    非核苷逆转录酶抑制剂

    公开(公告)号:US06716836B2

    公开(公告)日:2004-04-06

    申请号:US10096779

    申请日:2002-03-13

    CPC classification number: C07D471/14

    Abstract: A compound of formula I: wherein A is a connecting chain of (C1-3) alkyl; B is O or S; R1 is H, (C1-6) alkyl, halo, CF3, or OR1a wherein R1a is H or (C1-6)alkyl; R2 is H or Me; R3 is H or Me; R4 is H, (C1-4) alkyl, (C3-4) cycloalkyl and (C1-4)alkyl(C3-7)cycloalkyl; W is selected from  wherein, a) one of Y is SO2 and the other Y is NR5, provided that both are not the same, wherein R5 is H, (C1-6)alkyl,(C3-6) cycloalkyl, the alkyl being substituted, COR5o, COOR5p or CONR5pPR5q; and each R8 is H, (C1-4) alkyl, (C3-6) cycloalkyl, or (C1-4) alkyl-(C3-6) cycloalkyl; or b) E is CR8aR8b wherein R8a and R8b is H, or alkyl and J is CH2; or J is CR8aR8b and E is CH2, and the dotted line represents a single bond; or c) E is C(O) and J is CR8aR8b or J is C(O) and E is CR8aR8b and the dotted line represents a single bond; or d) E and J are CR8aR8b and the dotted line represents a double bond. Compounds of formula I have activity against HIV WT and double mutant strains.

    Abstract translation: 式I的化合物:其中A是(C 1-3)烷基的连接链; B是O或S; R 1是H,(C 1-6)烷基,卤素,CF 3或OR 1a,其中R 1a是H或(C 1-6)烷基; R 2是H或Me; R 3是H或Me; R 4是H,(C 1-4)烷基,(C 3-4)环烷基和(C 1-4)烷基(C 3-7)环烷基; W选自其中,a)Y中的一个是SO 2,另一个Y 条件是两者不相同,其中R 5是H,(C 1-6)烷基,(C 3-6)环烷基,取代的烷基,COR 50,COOR 5p, 或CONR <5p> PR <5q>; 并且每个R 8是H,(C 1-4)烷基,(C 3-6)环烷基或(C 1-4)烷基 - (C 3-6)环烷基; 或b)E是CR 8a R 8b,其中R 8a和R 8b是H,或烷基,J是CH 2; 或J为CR 8a R 8b且E为CH 2,虚线表示单键; 或c)E是C(O),J是CR 8a R 8b或J是C(O),E是CR 8a R 8b,虚线代表单键; 或d)E和J是CR 8a R 8b,虚线表示双键。 式I化合物具有抗HIV WT和双突变株的活性。

    Hepatitis C inhibitor tri-peptides
    9.
    发明授权
    Hepatitis C inhibitor tri-peptides 有权
    丙型肝炎抑制剂三肽

    公开(公告)号:US06534523B1

    公开(公告)日:2003-03-18

    申请号:US10091293

    申请日:2002-03-05

    Abstract: Racemates, diastereoisomers and optical isomers of a compound of formula (I): wherein B is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of which optionally substituted with C1-6 alkyl; C1-6 alkoxy; C1-6 alkanoyl; hydroxy; hydroxyalkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with C1-6 alkyl; amido; or (lower alkyl)amide; or B is an acyl derivative of formula R4—C(O)—; a carboxyl of formula R4—O—C(O)—; an amide of formula R4—N(R5)—C(O)—; a thioamide of formula R4—N(R5)—C(S)—; or a sulfonyl of formula R4—SO2; R5 is H or C1-6 alkyl; and Y is H or C1-6 alkyl; R3 is C1-8 alkyl, C3-7 cycloalkyl, or C4-10 alkylcycloalkyl, all optionally substituted with hydroxy, C1-6 alkoxy, C1-6 thioalkyl, amido, (lower alkyl)amido, C6 or C10 aryl, or C7-16 aralkyl; R2 is CH2—R20, NH—R20, O—R20 or S—R20, wherein R20 is a saturated or unsaturated C3-7 cycloalkyl or C4-10 (alkylcycloalkyl), all of which being optionally mono-, di- or tri-substituted with R21, or R20 is a C6 or C10 aryl or C7-14 aralkyl optionally substituted, or R20 is Het or (lower alkyl)-Het, both optionally substituted, Het or (lower alkyl)-Het; carboxyl; carboxy(lower alkyl); C6 or C10 aryl, C7-14 aralkyl or Het, said aryl, aralkyl or Het being optionally substituted; and R1 is H; C1-6 alkyl, C3-7 cycloalkyl, C2-6 alkenyl, or C2-6 alkynyl, all optionally substituted with halogen; or a pharmaceutically acceptable salt or ester thereof.

    Abstract translation: 式(I)化合物的外消旋物,非对映异构体和光学异构体:其中B是H,C6或C10芳基,C7-16芳烷基; Het或(低级烷基)-Het,其全部任选被C 1-6烷基取代; C 1-6烷氧基 C 1-6烷酰基; 羟基; 羟烷基 光环; 卤代烷基 硝基 氰基; 氰基烷基 任选被C 1-6烷基取代的氨基; 氨基酸 或(低级烷基)酰胺; 或B是式R4-C(O) - 的酰基衍生物; 式R4-O-C(O) - 的羧基; 式R 4 -N(R 5)-C(O) - 的酰胺; 式R 4 -N(R 5)-C(S) - 的硫代酰胺; 或式R4-SO2的磺酰基; R5是H或C1-6烷基; 并且Y是H或C 1-6烷基; R 3是C 1-8烷基,C 3-7环烷基或C 4-10烷基环烷基,全部被羟基,C 1-6烷氧基,C 1-6硫烷基,酰氨基,(低级烷基) ,C6或C10芳基或C7-16芳烷基; R2是CH2-R20,NH-R20,O-R20或S-R20,其中R20是饱和或不饱和的C3-7环烷基或C4-10(烷基环烷基),全部 其任选被R 21单取代,二取代或三取代,或R 20为任选取代的C 6或C 10芳基或C 7-14芳烷基,或R 20为Het或(低级烷基)-Het,均为任选取代的Het或 (低级烷基)-Het; 羧基; 羧基(低级烷基); C6或C10芳基,C7-14芳烷基或Het,所述芳基,芳烷基或Het任选被取代; 且R1为H; C 1-6烷基,C 3-7环烷基,C 2-6烯基或C 2-6炔基,全部被卤素取代; 或其药学上可接受的盐或酯。

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