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1. 发明授权

US08426421B2 Protease inhibitors 有权
标题翻译：蛋白酶抑制剂
公开(公告)号：US08426421B2
公开(公告)日：2013-04-23
申请号：US13541519
申请日：2012-07-03
申请人： Lourdes Salvador Odén , Magnus Nilsson , Pia Kahnberg , Bertil Samuelsson , Urszula Grabowska
发明人： Lourdes Salvador Odén , Magnus Nilsson , Pia Kahnberg , Bertil Samuelsson , Urszula Grabowska
IPC分类号： A61K31/496
CPC分类号： C07D277/40 , C07D491/048 , C07D495/04
摘要： Compounds of the formula II: wherein R1 and R2 are independently H, F or CH3; or R1 forms an ethynyl bond and R2 is H or optionally substituted C3-C6 cycloalkyl; R3 is (optionally substituted) C1-C3 alkyl or C3-C6 cycloalkyl; R4 is methyl or fluoro; m is 0-2; E is optionally substituted thiazolyl; A1 and A2 together define an optionally substituted piperazine or piperidine ring have utility in the treatment of osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.
摘要翻译：式II化合物：其中R 1和R 2独立地为H，F或CH 3; 或R 1形成乙炔基，R 2为H或任选取代的C 3 -C 6环烷基; R 3是（任选取代的）C 1 -C 3烷基或C 3 -C 6环烷基; R4是甲基或氟; m为0-2; E是任选取代的噻唑基; A1和A2一起限定任选取代的哌嗪或哌啶环可用于治疗骨质疏松症，骨关节炎，类风湿性关节炎或骨转移。

2. 发明授权

US08242119B2 Protease inhibitors 有权
标题翻译：蛋白酶抑制剂
公开(公告)号：US08242119B2
公开(公告)日：2012-08-14
申请号：US12739489
申请日：2009-09-24
申请人： Lourdes Salvador Odén , Magnus Nilsson , Pia Kahnberg , Bertil Samuelsson , Urszula Grabowska
发明人： Lourdes Salvador Odén , Magnus Nilsson , Pia Kahnberg , Bertil Samuelsson , Urszula Grabowska
IPC分类号： A61K31/496 , C07D491/04
CPC分类号： C07D277/40 , C07D491/048 , C07D495/04
摘要： Compounds of the formula II: wherein R1 and R2 are independently H, F or CH3; or R1 forms an ethynyl bond and R2 is H or C3-C6 cycloalkyl which is optionally substituted with one or two substituents independently selected from methyl, CF3, OMe or halo; R3 is C1-C3 alkyl or C3-C6 cycloalkyl, either of which is optionally substituted with one or two methyl and/or a fluoro, trifluoromethyl or methoxy, when R3 is C3-C6 cycloalkyl it may alternatively be gem substituted with fluoro; R4 is methyl or fluoro; m is 0, 1 or 2; E is a bond, or thiazolyl, optionally substituted with methyl or fluoro; A1 is CH or N, A2 is CR6R7 or NR6, provided at least one of A1 and A2 comprises N; R6 is H, C1-C4 alkyl, C1-C4 haloalkyl, C1-C3 alkyl-O—C1-C3 alkyl, or when A2 is C, R6 can also be C1-C4alkoxy or F; R7 is H, C1-C4 alkyl or F or a pharmaceutically acceptable salt, N-oxide or hydrate thereof, have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.
摘要翻译：式II化合物：其中R 1和R 2独立地为H，F或CH 3; 或R1形成乙炔基，R2是H或C3-C6环烷基，其任选地被一个或两个独立地选自甲基，CF 3，OMe或卤素的取代基取代; R 3是C 1 -C 3烷基或C 3 -C 6环烷基，当R 3是C 3 -C 6环烷基时，它们任选被一个或两个甲基和/或氟，三氟甲基或甲氧基取代，也可以被氟取代; R4是甲基或氟; m为0,1或2; E是任选被甲基或氟取代的键或噻唑基; A1是CH或N，A2是CR6R7或NR6，条件是A1和A2中的至少一个包括N; R6是H，C1-C4烷基，C1-C4卤代烷基，C1-C3烷基-O-C1-C3烷基，或当A2是C时，R6也可以是C1-C4烷氧基或F; R7是H，C1-C4烷基或F或其药学上可接受的盐，N-氧化物或其水合物，可用于治疗组织蛋白酶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骼转移。

3. 发明授权

US08466158B2 Cysteine protease inhibitors 有权
标题翻译：半胱氨酸蛋白酶抑制剂
公开(公告)号：US08466158B2
公开(公告)日：2013-06-18
申请号：US13468787
申请日：2012-05-10
申请人： Magnus Nilsson , Lourdes Salvador Odén , Pia Kahnberg , Urszula Grabowska
发明人： Magnus Nilsson , Lourdes Salvador Odén , Pia Kahnberg , Urszula Grabowska
IPC分类号： A61K31/496
CPC分类号： C07D491/048
摘要： Compounds of the formula II: wherein R2 is the side chain of leucine, isoleucine, cyclohexylglycine, O-methyl threonine, 4-fluoroleucine or 3-methoxyvaline; R3 is H, methyl or F; Rq is trifluoromethyl and Rq′ is H or Rq and Rq′ define keto; Q is a p-(C1-C6alkylsulphonyl)phenyl- or an optionally substituted 4-(C1-C6alkyl)piperazin-1-yl-thiazol-4-yl-moiety have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.
摘要翻译：式II化合物：其中R2是亮氨酸的侧链，异亮氨酸，环己基甘氨酸，O-甲基苏氨酸，4-氟亮氨酸或3-甲氧基缬氨酸; R3是H，甲基或F; Rq是三氟甲基，Rq'是H或Rq，Rq'定义酮基; Q是对 - （C 1 -C 6烷基磺酰基）苯基 - 或任选取代的4-（C 1 -C 6烷基）哌嗪-1-基 - 噻唑-4-基 - 部分可用于治疗以不适当表达或活化为特征的疾病组织蛋白酶K，例如骨质疏松症，骨关节炎，类风湿性关节炎或骨转移。

4. 发明授权

US07666834B2 Macrocyclic inhibitors of hepatitis C virus 有权
标题翻译：丙型肝炎病毒的大环抑制剂
公开(公告)号：US07666834B2
公开(公告)日：2010-02-23
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 Jönsson , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Åsa Annica Kristina Rosenquist , Dmitry Antonov , Lourdes Salvador Odén , Susana Ayesa Alvarez , Björn Olof Classon
发明人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Carl Erik Daniel Jönsson , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Åsa Annica Kristina Rosenquist , Dmitry Antonov , Lourdes Salvador Odén , Susana Ayesa Alvarez , Björn Olof Classon
IPC分类号： A61K38/00
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为氢; 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。

5. 发明授权

US08227407B2 Macrocyclic inhibitors of hepatitis C virus 有权
标题翻译：丙型肝炎病毒的大环抑制剂
公开(公告)号：US08227407B2
公开(公告)日：2012-07-24
申请号：US11995835
申请日：2008-01-16
申请人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Lili Hu , Dominique Louis Nestor Ghislain Surleraux , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Åsa Annica Kristina Rosenquist , Lourdes Salvador Odén
发明人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Lili Hu , Dominique Louis Nestor Ghislain Surleraux , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Åsa Annica Kristina Rosenquist , Lourdes Salvador Odén
IPC分类号： A61K38/55 , A61K38/00
CPC分类号： C07D487/04 , C07D245/04 , C07K5/06139
摘要： Macrocylic compounds having inhibitory activity on the replication of the hepatitis C virus (HCV) of the general formula (I) X is N, CH and where X bears a double bond it is C; R1a and R1b are hydrogen, C3-7cycloalkyl, aryl, Het, C1-6alkoxy, C1-6alkyl optionally substituted with halo, C1-6alkoxy, cyano, polyhaloC1-6alkoxy, C3-7cycloalkyl, aryl, or with Het; or R1a and R1b together with the nitrogen to which they are attached form a 4 to 6 membered heterocyclic ring which may be optionally substituted; Het being a heterocyclic ring; L is a direct bond, —O—, —O—C1-4alkanediyl-, —O—CO—, —O—C(═O)—NR5a— or —O—C(═O)—NR5a—C1-4alkanediyl-; n is 3, 4, 5, or 6; p is 1, or 2; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, C3-7cycloalkyl, amino, mono- or diC1-6alkylamino; R4 is aryl or a saturated, a partially unsaturated or completely unsaturated 5 or 6 membered monocyclic or 9 to 12 membered bicyclic heterocyclic ring system wherein said ring system contains one nitrogen, and optionally one to three additional heteroatoms selected from O, S and N, and wherein the remaining ring members are carbon atoms; wherein said ring system may be optionally substituted; and pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I).
摘要翻译：对通式（I）X的丙型肝炎病毒（HCV）的复制具有抑制活性的大环化合物是N，CH，其中X具有双键，其为C; R 1a和R 1b是氢，C 3-7环烷基，芳基，Het，C 1-6烷氧基，任选被卤素，C 1-6烷氧基，氰基，多卤代C 1-6烷氧基，C 3-7环烷基，芳基或与Het取代的C 1-6烷基; 或R 1a和R 1b与它们所连接的氮一起形成可任选被取代的4至6元杂环; Het是一个杂环; L是直接键，-O - ， - O-C 1-4烷二基 - ， - O-CO - ， - O-C（= O）-NR 5a - 或-O-C（= O）-NR 5a -C 1-4烷二基 - ; n为3,4,5或6; p为1或2; 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，C 3-7环烷基，氨基，单或二C 1-6烷基氨基; R4是芳基或饱和的，部分不饱和的或完全不饱和的5或6元单环或9至12元双环杂环体系，其中所述环体系含有一个氮，以及任选地一至三个选自O，S和N的杂原子，并且其中剩余的环成员是碳原子; 其中所述环系可以任选地被取代; 和含有化合物（I）的药物组合物和制备化合物（I）的方法。

6. 发明授权

US06894177B2 Intermediate compounds of non-nucleoside reverse transcriptase inhibitors 失效
标题翻译：非核苷逆转录酶抑制剂的中间体化合物
公开(公告)号：US06894177B2
公开(公告)日：2005-05-17
申请号：US10377057
申请日：2003-02-28
申请人： Stefan Lindström , Christer Sahlberg , Hans Wallberg , Genaidy Kalyanov , Lourdes Salvador Odén , Lotta Naeslund
发明人： Stefan Lindström , Christer Sahlberg , Hans Wallberg , Genaidy Kalyanov , Lourdes Salvador Odén , Lotta Naeslund
IPC分类号： C07D335/06 , A61K31/4155 , A61K31/422 , A61K31/427 , A61K31/428 , A61K31/44 , A61K31/4433 , A61K31/4436 , A61K31/4709 , A61K31/497 , A61K31/506 , A61P31/18 , A61P37/04 , A61P43/00 , C07C43/23 , C07C245/18 , C07D307/93 , C07D311/78 , C07D311/94 , C07D401/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D311/02
CPC分类号： C07D417/12 , A61K31/4433 , A61K31/4436 , C07C43/23 , C07C245/18 , C07D307/93 , C07D405/12 , C07D409/12 , C07D413/12
摘要： Compounds of the formula I: where; R1 is O, S; R2 is an optionally substituted nitrogen-containing heterocycle, wherein the nitrogen is located at the 2 position relative to the (thio)urea bond; R3 is H, C1-C3 alkyl, R4-R7 are independently selected from H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, haloC1-C6 alkyl, C1-C6 alkanoyl, haloC1-C6 alkanoyl, C1-C6 alkoxy, haloC1-C6 alkoxy, C1-C6 alkyloxy-C1-C6 alkyl, haloC1-C6 alkyloxy-C1-C6 alkyl hydroxy-C1-C6 alkyl, amino-C1-C6 alkyl, carboxy-C1-C6 alkyl, cyano-C1-C6 alkyl, amino, carboxy, carbamoyl, cyano, halo, hydroxy, keto; X is —(CH2)n−—D—(CH2)m—; D is —O—, —S—; n and m are independently 0 or 1; and prodrugs and pharmaceutically acceptable salts thereof, have utility as inhibitors of HIV-1 reverse transcriptase, particularly drug escape mutants.
摘要翻译：式I化合物：其中; R 1是O，S; R 2是任选取代的含氮杂环，其中氮位于相对于（硫）脲键的2位; R 3是H，C 1 -C 3烷基，R 4 -R 7，独立地选自H，C 1 -C 6烷基，C 2 -C 6亚烷基，C 2 -C 6亚烷基， C 2 -C 6炔基，卤代C 1 -C 6烷基，C 1 -C 12烷基，C 1 -C 6烷基，C 1〜 C 6 -C 6烷酰基，C 1 -C 6烷酰基，C 1 -C 6烷酰基，烷氧基，卤代C 1 -C 6烷氧基，C 1 -C 6烷氧基-C

7. 发明申请

US20120289519A1 PROTEASE INHIBITORS 有权
标题翻译： PROTEASE抑制剂
公开(公告)号：US20120289519A1
公开(公告)日：2012-11-15
申请号：US13541519
申请日：2012-07-03
申请人： Lourdes Salvador ODÉN , Magnus Nilsson , Pia Kahnberg , Bertil Samuelsson , Urszula Grabowska
发明人： Lourdes Salvador ODÉN , Magnus Nilsson , Pia Kahnberg , Bertil Samuelsson , Urszula Grabowska
IPC分类号： A61K31/496 , A61P19/02
CPC分类号： C07D277/40 , C07D491/048 , C07D495/04
摘要： Compounds of the formula II: wherein R1 and R2 are independently H, F or CH3; or R1 forms an ethynyl bond and R2 is H or optionally substituted C3-C6 cycloalkyl; R3 is (optionally substituted) C1-C3 alkyl or C3-C6 cycloalkyl; R4 is methyl or fluoro; m is 0-2; E is optionally substituted thiazolyl; A1 and A2 together define an optionally substituted piperazine or piperidine ring have utility in the treatment of osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.
摘要翻译：式II化合物：其中R 1和R 2独立地是H，F或CH 3; 或R 1形成乙炔基，R 2为H或任选取代的C 3 -C 6环烷基; R3是（任选取代的）C 1 -C 3烷基或C 3 -C 6环烷基; R4是甲基或氟; m为0-2; E是任选取代的噻唑基; A1和A2一起限定任选取代的哌嗪或哌啶环可用于治疗骨质疏松症，骨关节炎，类风湿性关节炎或骨转移。

8. 发明授权

US06716850B2 Non-nucleoside reverse transcriptase inhibitors 失效
标题翻译：非核苷逆转录酶抑制剂
公开(公告)号：US06716850B2
公开(公告)日：2004-04-06
申请号：US10092752
申请日：2002-03-05
申请人： Stefan Lindström , Christer Sahlberg , Hans Wallberg , Genaidy Kalyanov , Lourdes Salvador Odén , Lotta Naeslund
发明人： Stefan Lindström , Christer Sahlberg , Hans Wallberg , Genaidy Kalyanov , Lourdes Salvador Odén , Lotta Naeslund
IPC分类号： C07D40512
CPC分类号： C07D417/12 , A61K31/4433 , A61K31/4436 , C07C43/23 , C07C245/18 , C07D307/93 , C07D405/12 , C07D409/12 , C07D413/12
摘要： Compounds of the formula I: where; R1 is O, S; R2 is an optionally substituted nitrogen-containing heterocycle, wherein the nitrogen is located at the 2 position relative to the (thio)urea bond; R3 is H, C1-C3 alkyl, R4-R7 are independently selected from H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, haloC1-C6 alkyl, C1-C6 alkanoyl, haloC1-C6 alkanoyl, C1-C6 alkoxy, haloC1-C6 alkoxy, C1-C6 alkyloxy-C1-C6 alkyl, haloC1-C6 alkyloxy-C1-C6 alkyl hydroxy-C1-C6 alkyl, amino-C1-C6 alkyl, carboxy-C1-C6 alkyl, cyano-C1-C6 alkyl, amino, carboxy, carbamoyl, cyano, halo, hydroxy, keto; X is —(CHR8)n-—D—(CHR8)m—; D is —NR9—, —O—, —S—, —S(═O)— or —S(═O)2—; R8 is independently H, C1-C3 alkyl, halo substitutedC1-C3alkyl; R9 is H, C1-C3 alkyl; n and m are independently 0, 1 or 2; and prodrugs and pharmaceutically acceptable salts thereof, have utility as inhibitors of HIV-1 reverse transcriptase, particularly drug escape mutants.
摘要翻译：式I化合物：其中R 1为O，S; R 2为任选取代的含氮杂环，其中氮位于相对于（硫）脲键的2位; R 3为H，C 1 -C 3烷基，R 4 -R 7独立地选自H，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷基，C 1 -C 6烷酰基，卤代C 1 -C 6烷酰基，C 1 -C 6烷氧基，卤代C 1 -C 6烷氧基， C 1 -C 6烷氧基-C 1 -C 6烷基，卤代C 1 -C 6烷氧基-C 1 -C 6烷基羟基-C 1 -C 6烷基，氨基-C 1 -C 6烷基，羧基-C 1 -C 6烷基，氰基-C 1 -C 6烷基，氨基，羧基，氨基甲酰基，氰基，卤素，羟基，酮基; X是 - （CHR 8）n -D-（CHR 8）m - ; D是-NR 9 - ， - O - ， - S - ， - S（= O） - 或 -S（= O）2 - ; R 8独立地是H，C 1 -C 3烷基，卤素取代的C 1 -C 3烷基; R 9是H，C 1 -C 3烷基; n和m独立地是0,1或2;以及前药和药学上可接受的盐具有用作HIV-1逆转录酶的抑制剂，特别是药物逃逸突变体。

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