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    Cyclopropanated macrocyclic ketones and lactones
    21.
    发明授权
    Cyclopropanated macrocyclic ketones and lactones 有权
    环丙基化大环酮和内酯

    公开(公告)号：US07189881B2

    公开(公告)日：2007-03-13

    申请号：US11105626

    申请日：2005-04-14

    申请人： Anubhav P. S. Narula ,  Edward Mark Arruda ,  Franc T. Schiet

    发明人： Anubhav P. S. Narula ,  Edward Mark Arruda ,  Franc T. Schiet

    IPC分类号： C07D49/00

    CPC分类号： C11D3/50 ,  C07C45/69 ,  C07C49/427 ,  C07D225/04 ,  C07D313/00 ,  C07D337/00

    摘要： The present invention is directed to novel cyclopropanated macrocyclic ketone and lactone compounds of the general formula wherein X is an atom or a functional group selected from the group consisting of O, N, S, CH, or CH2; wherein Y is a straight or branched hydrocarbon moiety consisting of 1 to 20 carbon atoms; wherein W is a straight or branched hydrocarbon moiety of consisting of 1 to 20 carbon atoms; and wherein O is an oxygen atom; and the use of these novel compounds in creating fragrances, and scents in items such as perfumes, colognes and personal care products.

    摘要翻译： 本发明涉及新的环丙烷化大环酮和通式的内酯化合物，其中X是选自O，N，S，CH或CH 2的原子或官能团。 ; 其中Y是由1至20个碳原子组成的直链或支链烃部分; 其中W是由1至20个碳原子组成的直链或支链烃部分; 并且其中O是氧原子; 以及这些新型化合物在制造香料中的用途，以及香水，古龙水和个人护理产品中的香料。

    CARBOCYCLIC OXIME HEPATITIS C VIRUS SERINE PROTEASE INHIBITORS
    24.
    发明申请
    CARBOCYCLIC OXIME HEPATITIS C VIRUS SERINE PROTEASE INHIBITORS 有权
    CARBOCYCLIC OXIME HEPATITIS C病毒丝氨酸蛋白酶抑制剂

    公开(公告)号：US20090149491A1

    公开(公告)日：2009-06-11

    申请号：US12269941

    申请日：2008-11-13

    申请人： Dong Liu ,  Yat Sun Or ,  Zhe Wang

    发明人： Dong Liu ,  Yat Sun Or ,  Zhe Wang

    IPC分类号： A61K31/4709 ,  C07D245/02 ,  C07D215/00 ,  C07D471/12 ,  A61K31/4375

    CPC分类号： C07D471/04 ,  C07D225/04 ,  C07D245/04 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12

    摘要： The present invention discloses compounds of formula I, II, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. More specifically, the invention relates to oxime compounds containing a carbocyclic P2 unit. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

    摘要翻译： 本发明公开了式I，II的化合物或其药学上可接受的盐，酯或前药：其抑制丝氨酸蛋白酶活性，特别是丙型肝炎病毒（HCV）NS3-NS4A蛋白酶的活性。 因此，本发明的化合物干扰丙型肝炎病毒的生命周期，也可用作抗病毒剂。 更具体地，本发明涉及含有碳环P2单元的肟化合物。 本发明还涉及药物组合物，其包含用于给患有HCV感染的受试者施用的上述化合物。 本发明还涉及通过施用包含本发明化合物的药物组合物来治疗受试者的HCV感染的方法。

    Macrocylic Inhibitors of Hepatitis C Virus
    25.
    发明申请
    Macrocylic Inhibitors of Hepatitis C Virus 有权
    丙型肝炎病毒的大胆抑制剂

    公开(公告)号：US20090105302A1

    公开(公告)日：2009-04-23

    申请号：US11995827

    申请日：2006-07-28

    申请人： Kenneth Alan Simmen ,  Herman Augustinus De Kock ,  Pierre Jean-Marie Bernard Raboisson ,  Carl Erik Daniel Jonsson ,  Karl Magnus Nilsson ,  Bengt Bertil Samuelsson ,  Asa Annica Kristina Rosenquist ,  Dmitry Antonov ,  Lourdes Salvador Oden ,  Susana Ayesa Alvarez ,  Bjorn Olof Classon

    发明人： Kenneth Alan Simmen ,  Herman Augustinus De Kock ,  Pierre Jean-Marie Bernard Raboisson ,  Carl Erik Daniel Jonsson ,  Karl Magnus Nilsson ,  Bengt Bertil Samuelsson ,  Asa Annica Kristina Rosenquist ,  Dmitry Antonov ,  Lourdes Salvador Oden ,  Susana Ayesa Alvarez ,  Bjorn Olof Classon

    IPC分类号： A61K31/427 ,  A61P31/14 ,  C07D401/12 ,  A61K31/4523 ,  A61K31/407 ,  C07D417/12 ,  A61K31/4155 ,  A61K31/395

    CPC分类号： C07D401/12 ,  C07D225/04 ,  C07D245/04 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D487/04

    摘要： Inhibitors of HCV replication of formula (I) and the N-oxides, salts, or stereoisomers thereof, wherein each dashed line (represented by - - - - -) represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR6, —NH—SO2R7; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, or C3-7cycloalkyl; n is 3, 4, 5, or 6; R4 and R5 independently from one another are hydrogen, halo, hydroxy, nitro, cyano, carboxyl, C1-6alkyl, C1-6alkoxy, C1-6alkoxyC1-6alkyl, C1-6alkylcarbonyl, C1-6alkoxy-carbonyl, amino, azido, mercapto, C1-6alkylthio, polyhaloC1-6alkyl, aryl or Het; W is aryl or Het; R6 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R7 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl or naphthyl, each optionally substituted with 1-3 substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1-4 heteroatoms each independently selected from N, O or S, and optionally substituted with 1-3 substituents; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I). Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.

    摘要翻译： 式（I）的HCV复制抑制剂及其N-氧化物，盐或立体异构体，其中每个虚线（由 - - - - 表示）表示任选的双键; X为N，CH，X为双键，C为C; R1是-OR6，-NH-SO2R7; R2是氢，并且其中X是C或CH，R2也可以是C1-6烷基; R 3是氢，C 1-6烷基，C 1-6烷氧基C 1-6烷基或C 3-7环烷基; n为3,4,5或6; R 4和R 5彼此独立地是氢，卤素，羟基，硝基，氰基，羧基，C 1-6烷基，C 1-6烷氧基，C 1-6烷氧基C 1-6烷基，C 1-6烷基羰基，C 1-6烷氧基羰基，氨基，叠氮基，巯基， C 1-6烷硫基，多卤代C 1-6烷基，芳基或Het; W是芳基或Het; R6是氢; 芳基; Het; 任选被C 1-6烷基取代的C 3-7环烷基; 或任选被C 3-7环烷基，芳基或与Het取代的C 1-6烷基; R7是芳基; Het; 任选被C 1-6烷基取代的C 3-7环烷基; 或任选被C 3-7环烷基，芳基或与Het取代的C 1-6烷基; 芳基是苯基或萘基，各自任选被1-3个取代基取代; Het是含有1-4个杂原子的5或6元饱和的，部分不饱和的或完全不饱和的杂环，各自独立地选自N，O或S，并且任选被1-3个取代基取代; 含有化合物（I）的药物组合物和制备化合物（I）的方法。 还提供了式（I）的HCV抑制剂与利托那韦的生物可利用组合。

    Analogs of duocarmycin and cc-1065
    26.
    发明授权
    Analogs of duocarmycin and cc-1065 失效
    杜卡霉素和cc-1065的类似物

    公开(公告)号：US06281354B1

    公开(公告)日：2001-08-28

    申请号：US09423576

    申请日：1999-11-09

    申请人： Dale L. Boger

    发明人： Dale L. Boger

    IPC分类号： C07D22332

    CPC分类号： C07D487/04 ,  C07D223/14 ,  C07D223/32 ,  C07D225/04 ,  C07D487/10

    摘要： The field of this invention is antitumor antibiotics. More particularly, the present invention relates to analogs of duocarmycin and CC-1065, which analogs have antitumor antibiotics activity.

    摘要翻译： 本发明的领域是抗肿瘤抗生素。 更具体地说，本发明涉及杜卡霉素和CC-1065的类似物，其类似物具有抗肿瘤抗生素活性。

    Substituted 1,11-diaminoundecanes, processes for producing them, and their use
    29.
    发明授权
    Substituted 1,11-diaminoundecanes, processes for producing them, and their use 失效
    取代的1,11-二氨基十一烷，其制备方法及其用途

    公开(公告)号：US4487947A

    公开(公告)日：1984-12-11

    申请号：US421208

    申请日：1982-09-22

    申请人： Dieter Reinehr ,  Josef Pfeifer

    发明人： Dieter Reinehr ,  Josef Pfeifer

    IPC分类号： C07D225/00 ,  C07D225/02 ,  C07D225/04 ,  C07D307/52 ,  C07D333/20 ,  C08G59/50 ,  C08G69/26 ,  C07D307/06 ,  C07D307/04

    CPC分类号： C07C251/72 ,  C07D225/00 ,  C07D225/02 ,  C07D225/04 ,  C07D307/52 ,  C07D333/20 ,  C08G59/50 ,  C08G69/26

    摘要： There are described novel substituted 1,11-diaminoundecanes, particularly those of the formula ##STR1## [R.sub.1 is alkyl having 1-12 C atoms, R.sub.2 is hydrogen or alkyl having 1-12 C atoms, R.sub.3 is alkyl having 1-12 C atoms, cycloalkyl having 4-12 C atoms, aralkyl having 7 or 8 C atoms, unsubstituted or substituted aryl, pyridyl, furyl or thienyl, R.sub.4 is hydrogen, alkyl having 1-12 C atoms, cycloalkyl having 4-12 C atoms, or unsubstituted or substituted aryl, or R.sub.1 and R.sub.2 and/or R.sub.3 and R.sub.4 together are alkylene having 3-11 C atoms], and processes for producing them. The compound of the formula I can be used for example for producing polycondensation products, particularly polyamides. They can be used also as curing agents for epoxide resins.

    摘要翻译： 描述了新的取代的1,11-二氨基十一烷，特别是式（I）的那些：[R1是具有1-12个碳原子的烷基，R2是氢或具有1-12个C原子的烷基，R3是具有1个 -12个C原子，具有4-12个碳原子的环烷基，7或8个C原子的芳烷基，未取代或取代的芳基，吡啶基，呋喃基或噻吩基，R4是氢，具有1-12个碳原子的烷基，具有4-12个碳原子的环烷基 原子或未取代或取代的芳基，或R 1和R 2和/或R 3和R 4一起是具有3-11个碳原子的亚烷基）和其制备方法。 式I化合物可用于制备缩聚产物，特别是聚酰胺。 它们也可以用作环氧树脂的固化剂。

    Substituted 1,11-diaminoundecanes, processes for producing them and their use
    30.
    发明授权
    Substituted 1,11-diaminoundecanes, processes for producing them and their use 失效
    取代的1,11-二氨基十一烷，其制备方法及其用途

    公开(公告)号：US4484004A

    公开(公告)日：1984-11-20

    申请号：US421209

    申请日：1982-09-22

    申请人： Dieter Reinehr ,  Josef Pfeifer

    发明人： Dieter Reinehr ,  Josef Pfeifer

    IPC分类号： C07D225/00 ,  C07D225/02 ,  C07D225/04 ,  C07D307/52 ,  C07D333/20 ,  C08G59/50 ,  C08G69/26 ,  C07C87/02 ,  C07C87/00

    CPC分类号： C07C251/72 ,  C07D225/00 ,  C07D225/02 ,  C07D225/04 ,  C07D307/52 ,  C07D333/20 ,  C08G59/50 ,  C08G69/26

    摘要： There are described novel substituted 1,11-diaminoundecanes, particularly those of the formula ##STR1## [R.sub.1 is alkyl having 1-12 C atoms, R.sub.2 is hydrogen or alkyl having 1-12 C atoms, R.sub.3 is alkyl having 1-12 C atoms, cycloalkyl having 4-12 C atoms, aralkyl having 7 or 8 C atoms, unsubstituted or substituted aryl, pyridyl, furyl or thienyl, R.sub.4 is hydrogen, alkyl having 1-12 C atoms, cycloalkyl having 4-12 C atoms, or unsubstituted or substituted aryl, or R.sub.1 and R.sub.2 and/or R.sub.3 and R.sub.4 together are alkylene having 3-11 C atoms], and processes for producing them. The compound of the formula I can be used for example for producing polycondensation products, particularly polyamides. They can be used also as curing agents for epoxide resins.

    摘要翻译： 描述了新的取代的1,11-二氨基十一烷，特别是式（I）的那些：[R1是具有1-12个碳原子的烷基，R2是氢或具有1-12个C原子的烷基，R3是具有1个 -12个C原子，具有4-12个C原子的环烷基，7或8个C原子的芳烷基，未取代或取代的芳基，吡啶基，呋喃基或噻吩基，R4是氢，具有1-12个碳原子的烷基，具有4-12个碳原子的环烷基 原子或未取代或取代的芳基，或R 1和R 2和/或R 3和R 4一起是具有3-11个碳原子的亚烷基）和其制备方法。 式I化合物可用于制备缩聚产物，特别是聚酰胺。 它们也可以用作环氧树脂的固化剂。