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1. 发明申请

WO2004021969A2 NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS 审中-公开
标题翻译：非核苷酸逆转录酶抑制剂
公开(公告)号：WO2004021969A2
公开(公告)日：2004-03-18
申请号：PCT/EP2003/009872
申请日：2003-09-05
申请人： MEDIVIR AB , ANTONOV, Dmitry , SUND, Christian , LINDSTRÖM, Stefan , SAHLBERG, Christer
发明人： ANTONOV, Dmitry , SUND, Christian , LINDSTRÖM, Stefan , SAHLBERG, Christer
IPC分类号： A61K
CPC分类号： C07D213/73 , C07D213/65 , C07D307/93 , C07D311/94 , C07D333/78 , C07D335/06 , C07D405/12 , Y02P20/582
摘要： A compound of the formula (Y): where; R 1 is O, S; R 2 is a nitrogen-containing heterocycle; R 3 is H, C l -C 3 alkyl; X is -(CR 8 R 8 ') n -D-(CR 8 R 8 ') m -; D is a bond, -NR 9 -, -O-, -S-, -S(=O)- or -S(=O) 2 -; n and m are independently 0, 1 or 2, R 8 and R 8 ' are independently H, C 1 -C 3 alkyl, haloC 1 -C 3 alkyl, hydroxy, or R 8 and R 8 ' together with their adjacent C atom is -C(=O)-; R 9 is independently H, C 1 -C 3 alkyl; E is CH 2 -, -CHOH-, -C(=O)-, -NR 9 -, -O-, -S-, -S(=O) 2 -; n and m are independently 0, 1 or 2; p and q are independently 0, 1 or 2, where p+q ≤ 2; R 10 is an optionally substituted carbocycle or heterocycle; R 11 is independently H, C 1 -C 3 alkyl, halo substituted C l -C 3 alkyl, hydroxy; have utility as HIV antivirals.
摘要翻译：式（Y）的化合物：其中; R1为O，S; R2是含氮杂环; R3是H，C1-C3烷基; X是 - （CR8R8'）n-D-（CR8R8'）m-; D是键，-NR 9 - ， - O - ， - S - ， - S（= O） - 或-S（= O） n和m独立地为0,1或2，R 8和R 8'独立地为H，C 1 -C 3烷基，卤代C 1 -C 3烷基，羟基或R 8和R 8'与它们相邻的C原子一起为-C（= O） - ; R9独立地为H，C1-C3烷基; E是CH 2 - ， - CHOH - ， - C（= O） - ， - NR 9 - ， - O - ， - S - ， - S（= O） n和m独立地为0,1或2; p和q独立地为0,1或2，其中p + q <= 2; R 10是任选取代的碳环或杂环; R 11独立地为H，C 1 -C 3烷基，卤素取代的C 1 -C 3烷基，羟基; 具有艾滋病毒抗病毒药物的作用。

2. 发明申请

WO1989008263A1 A NOVEL SPECTROFLUOROMETRIC METHOD AND COMPOUNDS THAT ARE OF VALUE FOR THE METHOD 审中-公开
标题翻译：一种新的方法和方法的价值的方法和化合物
公开(公告)号：WO1989008263A1
公开(公告)日：1989-09-08
申请号：PCT/SE1989000073
申请日：1989-02-22
申请人： WALLAC OY , MUKKALA, Veli-Matti , SUND, Christian , KWIATKOWSKI, Marek
发明人： WALLAC OY
IPC分类号： G01N33/58
CPC分类号： C07D239/26 , C07D213/22 , C07D239/30 , C07F5/003 , C07F9/58 , G01N33/533
摘要： A spectrofluorometric method for the detection of target structures by the use of two or more fluorescent lanthanide chelate probes for specifically marking each of said structures. The probes used differ with respect to their excitation or emission wavelength maxima. Also disclosed are certain lanthanide chelates that can be used in the method, either for synthesizing the probes or to be used directly as probes. The chelating ligand of these novel probes comprises two heterocyclic rings (preferably pyridyl) linked together so that jointly they can coordinate (chelate) one metal ion. The bridge linking the two rings together permits electron delocalization between the rings. Attached to their 6-positions the two rings carry chelating groups having heteroatoms (N, O or S) that participate in the chelation of the metal ion. Preferably the chelating groups at the 6-positions are -CH2N(CH2COOH)2, -CH2N(CH2CH2COOH)2, (a) or (b).
摘要翻译：用于通过使用两种或多种荧光镧系元素螯合探针来检测靶结构的分光荧光法，用于特别标记每个所述结构。使用的探针在其激发或发射波长最大值方面不同。还公开了可用于该方法的某些镧系元素螯合物，用于合成探针或直接用作探针。这些新型探针的螯合配体包含两个连接在一起的杂环（优选吡啶基），因此它们可共同配合（螯合）一种金属离子。将两个环连接在一起的桥允许环之间的电子离域化。附着在它们的6位上，两个环带有具有参与金属离子螯合的杂原子（N，O或S）的螯合基团。优选6位上的螯合基团是-CH 2 N（CH 2 COOH）2，-CH 2 N（CH 2 CH 2 COOH）2，（a）或（b）。

3. 发明申请

WO2009053277A1 ASPARTYL PROTEASE INHIBITORS 审中-公开
标题翻译： ASPARTYL PROTEASE抑制剂
公开(公告)号：WO2009053277A1
公开(公告)日：2009-04-30
申请号：PCT/EP2008/063802
申请日：2008-10-14
申请人： MEDIVIR AB , SUND, Christian , SAHLBERG, Christer , BELDA, Oscar
发明人： SUND, Christian , SAHLBERG, Christer , BELDA, Oscar
IPC分类号： C07C237/00 , A61K31/16 , C07D213/74 , C07D265/30
CPC分类号： C07D213/74 , C07C237/06 , C07C237/08 , C07C237/10 , C07C243/28 , C07C271/16 , C07C311/08 , C07C311/18 , C07D265/30
摘要： The invention provides compounds of the formula (I) wherein A is selected from the partial structures A1, A2 and A3; Ry and Ry' are both hydrogen, or Ry and Ry' together with the nitrogen atom to which they are attached form a cyclic amine such as morpholine, piperidine, piperazine or pyrrolidine; L is NHNH, CH 2 NH, O or S; Y is NH, NHNH, NHC(=O), S(=O) 2 NH, NHS(=O) 2 , CH 2 , CH 2 NH, O, S or S(=0) p ; Q is aryl or heterocyclyl; Z is O, S, NRa or S(=0) p ; m is O, 1 or 2; n is O, 1, 2 or 3; p is independently 1 or 2; q is 0 or 1; Ra is H or C 1 -C 4 alkyl; R1 is hydrogen, C 1 -C 6 alkyl, C 3 -C 7 cycloalkylC 0 -C 3 alkyl, arylC 0 -C 3 alkyl or heterocyclylC 0 -C 3 alkyl, R 4'' is H or C 1 -C 6 alkyl; or R 4' and R 4'' together with the carbon atom to which they are attached define a C 3 -C 6 cycloalkyl; W is H, C 1 -C 6 alkyl, C 3 -C 7 ycycloalkyl, aryl or heterocyclyl; or a pharmaceutically acceptable salt, hydrate or N-oxide thereof. The compounds of the invention are inhibitors of aspartyl proteases such as renin and are among other things useful for the treatment of conditions associated with activities of the RAS, such as hypertension, heart failure and renal insufficiency.
摘要翻译：本发明提供式（I）化合物，其中A选自部分结构A1，A2和A3; Ry和Ry'都是氢，或者Ry和Ry'与它们所连接的氮原子一起形成环胺，如吗啉，哌啶，哌嗪或吡咯烷; L是NHNH，CH 2 NH，O或S; Y是NH，NHNH，NHC（= O），S（= O）2NH，NHS（= O）2，CH2，CH2NH，O，S或S（= O）p; Q是芳基或杂环基; Z是O，S，NR a或S（= O）p; m为O，1或2; n是0,1,2或3; p独立地为1或2; q为0或1; R a是H或C 1 -C 4烷基; R 1是氢，C 1 -C 6烷基，C 3 -C 7环烷基C 0 -C 3烷基，芳基C 0 -C 3烷基或杂环基C 0 -C 3烷基，R 4“是H或C 1 -C 6烷基; 或R 4'和R 4“与它们所连接的碳原子一起定义为C 3 -C 6环烷基; W是H，C 1 -C 6烷基，C 3 -C 7环烷基，芳基或杂环基; 或其药学上可接受的盐，水合物或N-氧化物。本发明的化合物是天冬氨酰蛋白酶如肾素的抑制剂，并且其它可用于治疗与RAS活性有关的病症，例如高血压，心力衰竭和肾功能不全。

4. 发明申请

WO2008119772A1 AMIDE DERIVATIVES AS INHIBITORS OF ASPARTYL PROTEASES 审中-公开
标题翻译：作为ASPARTYL蛋白抑制剂的酰胺衍生物
公开(公告)号：WO2008119772A1
公开(公告)日：2008-10-09
申请号：PCT/EP2008/053765
申请日：2008-03-28
申请人： MEDIVIR AB , KVARNSTRÖM, Ingemar , WÅNGSELL, Fredrik , ROSENQUIST, Åsa , SAMUELSSON, Bertil , SAHLBERG, Christer , SUND, Christian , BELDA, Oscar , IVANOV, Vladimir , ODEN, Lourdes , NORÉN, Rolf
发明人： KVARNSTRÖM, Ingemar , WÅNGSELL, Fredrik , ROSENQUIST, Åsa , SAMUELSSON, Bertil , SAHLBERG, Christer , SUND, Christian , BELDA, Oscar , IVANOV, Vladimir , ODEN, Lourdes , NORÉN, Rolf
IPC分类号： C07C311/08 , A61K31/18 , A61P9/12 , A61P9/04 , A61P27/06 , A61P13/12 , C07C309/66 , C07C311/07 , C07C255/57
CPC分类号： C07C311/08 , C07C255/57 , C07C309/66 , C07C311/07 , C07C2601/02 , C07C2601/08
摘要： The invention provides compounds of the formula (I). N-oxides, addition salts, quaternary amines, metal complexes, stereochemically isomeric forms and metabolites thereof, wherein W is H, C 1 -C 6 alkyl, C 3 -C 6 cycloalkyl, aryl or heterocyclyl; Q is aryl or heterocyclyl; A is a five or six membered saturated, partially unsaturated or aromatic ring; D is formula (II) or formula (III); and the other variables are as defined in the specification. The compounds of the invention are inhibitors of aspartyl proteases such as renin and BACE and are among other things useful for the treatment and/or prophylaxis of conditions associated with activities of the RAS, such as hypertension, heart failure and renal insufficiency and for the treatment and or prophylaxis of conditions associated with BACE activity such as of Alzheimer's disease.
摘要翻译：本发明提供式（I）化合物。 N-氧化物，加成盐，季胺，金属配合物，立体化学异构形式及其代谢物，其中W是H，C 1 -C 6烷基，C 1 -C 6烷基， 3个-C 6环烷基，芳基或杂环基; Q是芳基或杂环基; A是五或六元饱和，部分不饱和或芳环; D是式（II）或式（III）; 其他变量如规范中所定义。本发明的化合物是天冬氨酰蛋白酶如肾素和BACE的抑制剂，并且用于治疗和/或预防与RAS活性有关的病症，例如高血压，心力衰竭和肾功能不全以及治疗和/或预防与诸如阿尔茨海默氏病之类的BACE活性相关的病症。

5. 发明申请

WO1988002784A1 HYBRIDIZATION ASSAY AND MEANS TO BE USED IN THE ASSAY 审中-公开
标题翻译：杂交测定和在测定中使用的方法
公开(公告)号：WO1988002784A1
公开(公告)日：1988-04-21
申请号：PCT/SE1987000474
申请日：1987-10-16
申请人： WALLAC OY , PHARMACIA AB , YLIKOSKI, Jyrki , HURSKAINEN, Pertti , DAHLÉN, Patrik , SUND, Christian , LÖVGREN, Timo , KWIATKOWSKI, Marek
发明人： WALLAC OY , PHARMACIA AB
IPC分类号： C12Q01/68
CPC分类号： C07H21/00 , C12Q1/6816
摘要： A method for the detection of a nucleotide sequence of a nucleic acid in a sample. The method comprises the steps: (i) contacting under hybridization condition the single stranded form of the nucleotide sequence with a single stranded nucleic acid probe, in which a plurality of rare earth metal chelate groups is covalently linked via a water-soluble polymer of non-nucleic acid structure to a nucleotide sequence complementary to the sequence to be detected, for the formation of a double stranded nucleic acid that as one of its strand has the nucleotide sequence to be detected and as the other strand the nucleotide sequence of the probe, and (ii) detecting the formation of double stranded nucleic acid containig the probe by measuring the time-resolved fluorescence from the rare earth chelates incorporated in said double stranded nucleic acid. The plurality of rare earth metal chelate groups have at least one metal ion selected from the group consisting of Eu , Sm , Tb and Dy as the chelated rare earth metal. The probes as given above are also claimed.
摘要翻译：检测样品中核酸的核苷酸序列的方法。该方法包括以下步骤：（i）在杂交条件下使单链形式的核苷酸序列与单链核酸探针接触，其中多个稀土金属螯合基团通过非水溶性聚合物共价连接，核酸结构与待检测序列互补的核苷酸序列，为了形成作为其一条链中具有待检测的核苷酸序列的双链核酸，作为另一条链的探针的核苷酸序列，和（ii）通过测量掺入所述双链核酸中的稀土螯合物的时间分辨荧光来检测含有探针的双链核酸的形成。多个稀土金属螯合物基团具有选自Eu 3+，Sm 3+，Tb 3+和Dy 3+中的至少一种金属离子作为螯合稀土金属。上述的探针也被要求保护。

6. 发明申请

WO2010024772A1 ASPARTYL PROTEASE INHIBITORS 审中-公开
标题翻译： ASPARTYL PROTEASE抑制剂
公开(公告)号：WO2010024772A1
公开(公告)日：2010-03-04
申请号：PCT/SE2009/050976
申请日：2009-08-28
申请人： Medivir AB , SAHLBERG, Christer , SUND, Christian , WIKTELIUS, Daniel , BELDA, Oscar
发明人： SAHLBERG, Christer , SUND, Christian , WIKTELIUS, Daniel , BELDA, Oscar
IPC分类号： C07C237/22 , A61K38/05 , A61P27/06 , A61P9/04 , A61P9/12 , C07D213/04 , C07D275/02
CPC分类号： C07D213/30 , C07C237/22 , C07C255/60 , C07C2601/02 , C07D277/24
摘要： The invention provides compounds of the formula (I wherein Q is trifluoromethyl, C 3 -C 6 cycloalkyl, phenyl, p-fluorophenyl, pyridyl, thiazolyl, furyl, thienyl or C 3 -C 6 cycloalkylethynyl; R 3 is C 1 -C 6 alkyl; R 4 is C 1 -C 6 alkyl; W is cyano or fluoro; or a pharmaceutically acceptable salt, hydrate or N-oxide thereof. The compounds of the invention are inhibitors of aspartyl proteases such as renin and are among other things useful for the treatment of conditions associated with activities of the RAS, such as hypertension, heart failure and renal insufficiency.
摘要翻译：本发明提供式（I）化合物，其中Q为三氟甲基，C 3 -C 6环烷基，苯基，对氟苯基，吡啶基，噻唑基，呋喃基，噻吩基或C3-C6环烷基乙炔基; R3为C1-C6烷基; R4为C1-C6烷基; W为氰基或氟;或其药学上可接受的盐，水合物或N-氧化物。本发明的化合物是天冬氨酰蛋白酶如肾素的抑制剂，并且其它可用于治疗与RAS活性相关的病症，例如高血压，心力衰竭和肾功能不全。

7. 发明申请

WO2007048557A1 PROTEASE INHIBITORS 审中-公开
标题翻译： PROTEASE抑制剂
公开(公告)号：WO2007048557A1
公开(公告)日：2007-05-03
申请号：PCT/EP2006/010194
申请日：2006-10-23
申请人： MEDIVIR AB , SUND, Christian , LINDBORG, Björn , KALAYANOV, Genadiy , SAMUELSSON, Bertil , WALLBERG, Hans , HALLBERG, Anders
发明人： SUND, Christian , LINDBORG, Björn , KALAYANOV, Genadiy , SAMUELSSON, Bertil , WALLBERG, Hans , HALLBERG, Anders
IPC分类号： C07C271/22 , C07C311/06 , C07C275/24 , C07D213/42 , C07D241/12 , C07D333/58 , C07D317/58 , C07D261/08 , A61K31/18 , A61K31/17 , A61K31/325 , A61K31/38 , A61K31/42 , A61K31/44 , A61K31/495
CPC分类号： C07D213/42 , C07C271/22 , C07C275/24 , C07C2602/08 , C07D241/12 , C07D277/24 , C07D333/50
摘要： Compounds of the formula (I), wherein R 1 , R 2 , X and N are as defined in the specification; L is F, NH 2 , NHAlk or N(Alk) 2 n is 1 or 2; A' and A" are terminal groups as defined in the specification. The compounds have utility as HIV-1 protease inhibitors.
摘要翻译：式（I）的化合物，其中R 1，R 2，X和N如说明书中所定义; L是F，NH 2，NHAlk或N（Alk）2 n是1或2; A'和A“是说明书中定义的末端基团，该化合物可用作HIV-1蛋白酶抑制剂。

8. 发明申请

WO1990000622A1 OLIGONUCLEOTIDE HYBRIDIZATION PROBES AND MEANS FOR THE SYNTHESIS OF THE MOST PREFERRED PROBES 审中-公开
标题翻译：寡核苷酸杂交探针和合成最优选探针的手段
公开(公告)号：WO1990000622A1
公开(公告)日：1990-01-25
申请号：PCT/SE1989000377
申请日：1989-07-03
申请人： WALLAC OY , PHARMACIA AB , KWIATKOWSKI, Marek , SUND, Christian , HURSKAINEN, Pertti
发明人： WALLAC OY , PHARMACIA AB
IPC分类号： C12Q01/68
CPC分类号： C07H21/00 , Y02P20/55
摘要： Oligonucleotide probe labeled at one of its teminal positions with a non-linear branched polymer carrying a plurality of negatively charged groups, preferably phosphodiester groups, and optionally also analytically indicatable groups covalently linked to terminal ends of the branches of said polymer. The preferred indicatable groups are lanthanide chelates. A compound that can be used for the synthesis of the probe is also disclosed. The compound has formula (I), where R1 and R2 are lower alkyl; R3 is lower alkyl (C1-C7), or aryl each of which optionally being provided with electron-withdrawing substituents; and A1, A2 and A3 are hydrogen, A'-O-B, A''-O-B or A'''-O-B, at most one of A1-3 being hydrogen and A', A'' and A''' being a hydrocarbon chain providing a distance of 5-9 atoms between the phosphorous atom and the oxygen directly bound to B, and B being a protecting group. In the preferred compound at least two of A1-3 are identical while the other is hydrogen.
摘要翻译：寡核苷酸探针在其一个末端位置上带有携带多个带负电荷基团，优选磷酸二酯基团的非直链支化聚合物，以及任选地可分析地连接到所述聚合物分支末端的可分析指示基团。优选的指示性基团是镧系元素螯合物。还公开了可用于合成探针的化合物。化合物具有式（I），其中R 1和R 2是低级烷基; R3是低级烷基（C1-C7）或芳基，其各自任选具有吸电子取代基; 并且A1，A2和A3是氢，A'-OB，A'-OB或A''-OB，至多一个A1-3是氢，A'，A“和A” 烃链在磷原子和直接与B结合的氧之间提供5-9个原子的距离，B是保护基。在优选的化合物中，A1-3中的至少两个是相同的，而另一个是氢。

9. 发明申请

WO2008114054A1 PROTEASE INHIBITORS 审中-公开
标题翻译： PROTEASE抑制剂
公开(公告)号：WO2008114054A1
公开(公告)日：2008-09-25
申请号：PCT/GB2008/050193
申请日：2008-03-18
申请人： MEDIVIR AB , KANGASMETSA, Jussi , PARKES, Kevin , TOZER, Matt , JOHNSON, Tony , GRABOWSKA, Urszula , ODEN, Lourdes , SUND, Christian , NILSSON, Magnus , IVANOV, Vladimir , KAHNBERG, Pia
发明人： KANGASMETSA, Jussi , PARKES, Kevin , TOZER, Matt , JOHNSON, Tony , GRABOWSKA, Urszula , ODEN, Lourdes , SUND, Christian , NILSSON, Magnus , IVANOV, Vladimir , KAHNBERG, Pia
IPC分类号： C07D491/04 , A61K31/407 , A61P19/00
CPC分类号： C07D491/04
摘要： Compounds of the formula (II): wherein R 2 is the side chain of leucine, isoleucine, cyclohexylglycine, O-methyl threonine, 4-fluoroleucine or 3-methoxyvaline; R 3 is H, methyl or fluoro; R 4 is C 1 -C 6 alkyl; E is a bond or thiazolyl, optionally substituted with methyl or fluoro; n is 0 or 1; or a pharmaceutically acceptable salt, N-oxide or hydrate thereof; have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsinK, such as osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.
摘要翻译：式（II）的化合物：其中R 2是亮氨酸的侧链，异亮氨酸，环己基甘氨酸，O-甲基苏氨酸，4-氟代亮氨酸或3-甲氧基缬氨酸; R 3是H，甲基或氟; R 4是C 1 -C 6烷基; R 4是C 1 -C 6烷基; E是任选被甲基或氟取代的键或噻唑基; n为0或1; 或其药学上可接受的盐，N-氧化物或其水合物; 可用于治疗特征为组织蛋白酶K不适当表达或活化的疾病，例如骨质疏松症，骨关节炎，类风湿性关节炎或骨转移。

10. 发明申请

WO2008107365A1 NEW COMPOUNDS 审中-公开
标题翻译：新化合物
公开(公告)号：WO2008107365A1
公开(公告)日：2008-09-12
申请号：PCT/EP2008/052416
申请日：2008-02-28
申请人： MEDIVIR AB , BELDA, Oscar , SUND, Christian , IVANOV, Vladimir , WIKTELIUS, Daniel , SAHLBERG, Christer , SAMUELSSON, Bertil , ROSENQUIST, Åsa , WÅNGSELL, Fredrik , KVARNSTRÖM, Ingemar
发明人： BELDA, Oscar , SUND, Christian , IVANOV, Vladimir , WIKTELIUS, Daniel , SAHLBERG, Christer , SAMUELSSON, Bertil , ROSENQUIST, Åsa , WÅNGSELL, Fredrik , KVARNSTRÖM, Ingemar
IPC分类号： A61K31/44 , C07D213/40 , C07C237/12 , C07D213/38
CPC分类号： C07D307/33 , C07C237/22 , C07C255/60 , C07D213/38 , C07D213/40
摘要： The invention provides compounds of the formula I wherein Q is aryl or heterocyclyl any of which is optionally substituted; Z is O, S, NRa or S(=O) p ; Y is NH, NHNH, CH 2 NH, O, S or S(=O) p ; n is 0, 1, 2 or 3; m is 0, 1 or 2; p is 1 or 2; Ra is H or C 1 -C 4 alkyl; R 1 is hydrogen, C 1 -C 6 alkyl, C 0 -C 3 alkanediylC 3 -C 7 cycloalkyl, C 0 -C 3 alkanediylaryl or C 0 - C3alkanediylheterocyclyl; R 2 is hydrogen or C 1 -C 6 alkyl; X' is hydrogen, fluoro, hydroxy, amino or C 1 -C 6 alkoxy; X" is hydrogen, or when X' is fluoro, then X" may also be fluoro; R 3 is C 1 -C 6 alkyl; R 4' is C 1 -C 6 alkyl; R 4" is H or C 1 -C 6 alkyl; or R 4' and R 4" together with the carbon atom to which they are attached define a C 3 -C 6 cycloalkyl; W is C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl, aryl or heterocyclyl any of which is optionally substituted; or a pharmaceutically acceptable salt, hydrate or N-oxide thereof. The compounds of the invention are inhibitors of aspartyl proteases such as renin and are among other things useful for the treatment of conditions associated with activities of the RAS, such as hypertension, heart failure and renal insufficiency.
摘要翻译：本发明提供式I化合物，其中Q是任选被取代的芳基或杂环基; Z是O，S，NR a或S（= O）p。 Y是NH，NHNH，CH 2 NH，O，S或S（= O）p; n为0,1,2或3; m为0,1或2; p为1或2; R a是H或C 1 -C 4烷基; R 1是氢，C 1 -C 6烷基，C 0 -C 3 - 烷二基C 3 -C 7环烷基，C 0 -C 3烷二基芳基或C 0 < / C3-烷二基杂环基; R 2是氢或C 1 -C 6烷基; R 2是氢或C 1 -C 6烷基; X'是氢，氟，羟基，氨基或C 1 -C 6烷氧基; X“是氢，或者当X'是氟时，X”也可以是氟; R 3是C 1 -C 6烷基; R 3是C 1 -C 6烷基; R 4是C 1 -C 6烷基; R 4是C 1 -C 6烷基; R 4是H或C 1 -C 6烷基;或R 4'和R“ 4“与它们所连接的碳原子一起定义为C 3 -C 6环烷基; W是C 1 -C 6烷基，C 3 -C 7环烷基，芳基或杂环基，其中任何一个任选地被取代; 或其药学上可接受的盐，水合物或N-氧化物。本发明的化合物是天冬氨酰蛋白酶如肾素的抑制剂，并且其它可用于治疗与RAS活性有关的病症，例如高血压，心力衰竭和肾功能不全。

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