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1. 发明授权

US08580981B2 Process for the preparation of (3R,3aS,6aR)-hexahydrofuro [2,3-b] furan-3-yl (1S,2R)-3-[[(4-aminophenyl) sulfonyl] (isobutyl) amino]-1-benzyl-2-hydroxypropylcarbamate 有权
标题翻译：制备（3R，3aS，6aR）六氢呋喃并[2,3-b]呋喃-3-基（1S，2R）-3 - [[（4-氨基苯基）磺酰基]（异丁基）氨基] -1 苄基-2-羟丙基氨基甲酸酯
公开(公告)号：US08580981B2
公开(公告)日：2013-11-12
申请号：US13060942
申请日：2009-09-01
申请人： Piet Tom Bert Paul Wigerinck , Dominique Louis Nestor Ghislain Surleraux , Wim Gaston Verschueren , Herman Augustinus De Kock , Wim Albert Alex Aelterman
发明人： Piet Tom Bert Paul Wigerinck , Dominique Louis Nestor Ghislain Surleraux , Wim Gaston Verschueren , Herman Augustinus De Kock , Wim Albert Alex Aelterman
IPC分类号： C07D493/04
CPC分类号： C07D493/04
摘要： The present invention relates to a process for the preparation of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate as well as novel intermediates for use in said process. (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate is particularly useful as an HIV protease inhibitor.
摘要翻译：本发明涉及制备（3R，3aS，6aR） - 六氢呋喃并[2,3-b]呋喃-3-基（1S，2R）-3 - [[（4-氨基苯基）磺酰基] 异丁基）氨基] -1-苄基-2-羟基丙基氨基甲酸酯以及用于所述方法的新型中间体。（3R，3aS，6aR） - 六氢呋喃并[2,3-b]呋喃-3-基（1S，2R）-3 - [[（4-氨基苯基）磺酰基]（异丁基）氨基] -1-苄基-2- 羟丙基氨基甲酸酯特别可用作HIV蛋白酶抑制剂。

2. 发明申请

US20100280268A1 HOMOGENEOUS TIME RESOLVED FLUORESCENCE BASED TEST SYSTEM 审中-公开
标题翻译：均匀时间分辨率基于荧光的测试系统
公开(公告)号：US20100280268A1
公开(公告)日：2010-11-04
申请号：US12293589
申请日：2007-04-06
申请人： Géry Karel Julia Dams , Inge Vereycken , Koenraad Lodewijk August Van Acker , Emmanuel Marie Paul Ernest Gustin , Wim Gaston Verschueren , Asa Catrine Ohagen
发明人： Géry Karel Julia Dams , Inge Vereycken , Koenraad Lodewijk August Van Acker , Emmanuel Marie Paul Ernest Gustin , Wim Gaston Verschueren , Asa Catrine Ohagen
IPC分类号： C07C69/76 , G01N21/64 , C07C63/00 , C07C229/54
CPC分类号： G01N33/56988 , G01N33/542
摘要： The present invention concerns a fluorescence resonance energy transfer based high throughput test system to measure the formation of the HIV gp41 six-helix bundle. In a first embodiment the current invention relates to a homogeneous time resolved fluorescence-based test system comprising a first helical polypeptide consisting essentially of the sequence of IQN36 (SEQ ID NO:1); a second helical polypeptide consisting essentially of the sequence of C34 (SEQ ID NO: 2) wherein said IQN36 is labeled with a light emitting fluorophore and said C34 is labeled with an ultra-violet excitable fluorophore.
摘要翻译：本发明涉及基于荧光共振能量转移的高通量测试系统来测量HIV gp41六螺旋束的形成。在第一个实施方案中，本发明涉及基于均匀时间分辨荧光的测试系统，其包含基本上由IQN36（SEQ ID NO：1）序列组成的第一螺旋多肽; 基本上由C34（SEQ ID NO：2）的序列组成的第二螺旋多肽，其中所述IQN36用发光荧光团标记，所述C34用紫外线可激发荧光团标记。

3. 发明授权

US07763641B2 Broadspectrum heterocyclic substituted phenyl containing sulfonamide HIV protease inhibitors 失效
标题翻译：支链杂环取代苯基含磺酰胺HIV蛋白酶抑制剂
公开(公告)号：US07763641B2
公开(公告)日：2010-07-27
申请号：US10499221
申请日：2002-12-20
申请人： Sandrine Marie Helene Vendeville , Wim Gaston Verschueren , Abdellah Tahri , Samuel Leo Christiaan Moors , Montserrat Erra Sola
发明人： Sandrine Marie Helene Vendeville , Wim Gaston Verschueren , Abdellah Tahri , Samuel Leo Christiaan Moors , Montserrat Erra Sola
IPC分类号： A61K31/42 , A61K31/44 , A61K31/425 , C07D277/54
CPC分类号： C07D231/12 , C07C311/18 , C07C2603/18 , C07D233/64 , C07D233/88 , C07D263/32 , C07D277/40 , C07D277/42 , C07D277/46 , C07D417/04 , C07D417/12 , C07D417/14 , C07D493/04 , C07D513/04
摘要： The present invention concerns the compounds having the formula (I), N-oxides, salt, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein Haryl is an aromatic monocyclic, bicyclic or tricyclic heterocycle having 3 to 14 ring members which contains one or more heteroatom ring members selected from nitrogen, oxygen and sulfur and which may optionally be substituted on (i) one or more carbon atoms by C1-6alkyl, halogen, hydroxy, optionally mono- or disubstituted amino, nitro, cyano, haloC1-6alkyl, carboxyl, C3-7cycloalkyl, optionally mono- or disubstituted aminocarbonyl, methylthio, methylsulfonyl, aryl, —(R7a)n—M—R7b, Het1 and Het2; whereby the optional substituents on any amino function are independently selected from R5 and —A—R6; and on (ii) a nitrogen atom if present by hydroxy or —A—R6. It further relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with another anti-retroviral agent, and to their use in assays as reference compounds or as reagents.
摘要翻译：本发明涉及具有式（I）的化合物，N-氧化物，盐，立体异构形式，外消旋混合物，前药，酯和代谢物，其中Haryl是具有3至14个环成员的芳族单环，双环或三环杂环，含有一个或多个选自氮，氧和硫的杂原子环成员，并且其可任选地在（i）一个或多个碳原子上被C 1-6烷基，卤素，羟基，任选单或二取代的氨基，硝基，氰基，卤代烷基，羧基，C 3-7环烷基，任选的单或二取代的氨基羰基，甲硫基，甲基磺酰基，芳基， - （R 7a）n-M-R 7b，Het 1和Het 2; 其中任何氨基官能团上的任选取代基独立地选自R5和-A-R6; 和（ii）如果存在羟基或-A-R 6的氮原子。它还涉及它们作为广谱的HIV蛋白酶抑制剂，其制备方法以及药物组合物和包含它们的诊断试剂盒的用途。它还涉及与另一种抗逆转录病毒剂的组合，以及它们在测定中用作参考化合物或作为试剂。

4. 发明授权

US07595334B2 Broadspectrum 2-(substituted-amino)-benzoxazole sulfonamide HIV protease inhibitors 失效
公开(公告)号：US07595334B2
公开(公告)日：2009-09-29
申请号：US11626183
申请日：2007-01-23
申请人： Dominique Louis Nestor Ghislain Surleraux , Sandrine Marie Helene Vendeville , Wim Gaston Verschueren , Marie-Pierre T. M. M. G. De Bethune , Herman Augustinus De Kock , Abdellah Tahri , Montserrat Erra Solà
发明人： Dominique Louis Nestor Ghislain Surleraux , Sandrine Marie Helene Vendeville , Wim Gaston Verschueren , Marie-Pierre T. M. M. G. De Bethune , Herman Augustinus De Kock , Abdellah Tahri , Montserrat Erra Solà
IPC分类号： A61K31/421 , A61K31/426 , C07D263/54 , C07D277/02 , C07D413/02
CPC分类号： C07D413/04 , C07D263/58 , C07D417/12 , C07D417/14 , C07D493/04
摘要： The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9—; t is 0, 1 or 2; R2 is H or C1-6alkyl; L is —C(═O)—, —O—C(═O)—, —NR8—C(═O)—, —O—C1-6alkanediyl-C(═O)—, —NR8—C1-6alkanediyl-C(═O)—, —S(═O)2—, —O—S(═O)2—, —NR8—S(═O)2; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC(═O), carboxyl, aminoC(═O), mono- or di(C1-4alkyl)aminoC(═O), C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; A is C1-6alkanediyl, —C(═O)—, —C(═S)—, —S(═O)2—, C1-6alkanediyl-C(═O)—, C1-6alkanediyl-C(═S)— or C1-6alkanediyl-S(═O)2—; R5 is H, OH, C1-6alkyl, Het1C1-6alkyl, Het2C1-6alkyl, optionally substituted aminoC1-6alkyl; R6 is C1-6alkylO, Het1, Het1O, Het2, Het2O, aryl, arylO, C1-6alkyloxycarbonylamino or amino; and in case -A- is other than C1-6alkanediyl then R6 may also be C1-6alkyl, Het1C1-4alkyl, Het1OC1-4alkyl, Het2C1-4alkyl, Het2OC1-4alkyl, arylC1-4alkyl, arylOC1-4alkyl or aminoC1-4alkyl; whereby each of the amino groups in the definition of R6 may optionally be substituted; -A-R6 is hydroxyC1-6alkyl; R5 and -A-R6 taken together with the nitrogen atom to which they are attached may also form Het1 or Het2. It further relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with another anti-retroviral agent, and to their use in assays as reference compounds or as reagents.

5. 发明授权

US07244752B2 Broadspectrum 2-(substituted-amino)-benzoxazole sulfonamide HIV protease inhibitors 有权
公开(公告)号：US07244752B2
公开(公告)日：2007-07-17
申请号：US10474162
申请日：2002-04-09
申请人： Dominique Louis Nestor Ghislain Surleraux , Sandrine Marie Helene Vendeville , Wim Gaston Verschueren , Marie-Pierre T. M. M. G. De Bethune , Herman Augustinus De Kock , Abdellah Tahri , Montserrat Erra Solà
发明人： Dominique Louis Nestor Ghislain Surleraux , Sandrine Marie Helene Vendeville , Wim Gaston Verschueren , Marie-Pierre T. M. M. G. De Bethune , Herman Augustinus De Kock , Abdellah Tahri , Montserrat Erra Solà
IPC分类号： A61K31/421 , A61K31/426 , C07D263/54 , C07D277/02 , C07D413/02 , C07D417/02
CPC分类号： C07D413/04 , C07D263/58 , C07D417/12 , C07D417/14 , C07D493/04
摘要： The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9—; t is 0, 1 or 2; R2 is H or C1-6alkyl; L is —C(═O)—, —O—C(═O)—, —NR8—C(═O)—, —O—C1-6alkanediyl-C(═O)—, —NR8—C1-6alkanediyl-C(═O)—, —S(═O)2—, —O—S(═O)2—, —NR8—S(═O)2; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC(═O), carboxyl, aminoC(═O), mono- or di(C1-4alkyl)aminoC(═O), C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; A is C1-6alkanediyl, —C(═O)—, —C(═S)—, —S(═O)2—, C1-6alkanediyl-C(═O)—, C1-6alkanediyl-C(═S)— or C1-6alkanediyl-S(═O)2—; R5 is H, OH, C1-6alkyl, Het1C1-6alkyl, Het2C1-6alkyl, optionally substituted aminoC1-6alkyl; R6 is C1-6alkylO, Het1, Het1O, Het2, Het2O, aryl, arylO, C1-6alkyloxycarbonylamino or amino; and in case -A- is other than C1-6alkanediyl then R6 may also be C1-6alkyl, Het1C1-4alkyl, Het1OC1-4alkyl, Het2C1-4alkyl, Het2OC1-4alkyl, arylC1-4alkyl, arylOC1-4alkyl or aminoC1-4alkyl; whereby each of the amino groups in the definition of R6 may optionally be substituted; -A-R6 is hydroxyC1-6alkyl; R5 and -A-R6 taken together with the nitrogen atom to which they are attached may also form Het1 or Het2. It further relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with another anti-retroviral agent, and to their use in assays as reference compounds or as reagents.

6. 发明申请

US20110160468A1 PROCESS FOR THE PREPARATION OF (3R,3AS,6AR)-HEXAHYDROFURO [2,3-B] FURAN-3-YL (1S,2R)-3-[[(4-AMINOPHENYL) SULFONYL] (ISOBUTYL) AMINO]-1-BENZYL-2-HYDROXYPROPYLCARBAMATE 有权
标题翻译：（3R，3AS，6AR） - 六氢呋喃并[2,3-b]呋喃-3-基（1S，2R）-3 - [[（4-氨基戊基）磺酰基]（异丁基）氨基] -1 苯基-2-羟基丙酸酯
公开(公告)号：US20110160468A1
公开(公告)日：2011-06-30
申请号：US13060942
申请日：2009-09-01
申请人： Piet Tom Bert Paul Wigerinck , Dominique Louis Nestor Ghislain Surleraux , Wim Gaston Verschueren , Herman Augustinus De Kock , Wim Albert Alex Aelterman
发明人： Piet Tom Bert Paul Wigerinck , Dominique Louis Nestor Ghislain Surleraux , Wim Gaston Verschueren , Herman Augustinus De Kock , Wim Albert Alex Aelterman
IPC分类号： C07D493/04 , C07C213/08 , C07C271/20 , C07C215/28
CPC分类号： C07D493/04
摘要： The present invention relates to a process for the preparation of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate as well as novel intermediates for use in said process. (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate is particularly useful as an HIV protease inhibitor.
摘要翻译：本发明涉及制备（3R，3aS，6aR） - 六氢呋喃并[2,3-b]呋喃-3-基（1S，2R）-3 - [[（4-氨基苯基）磺酰基] 异丁基）氨基] -1-苄基-2-羟基丙基氨基甲酸酯以及用于所述方法的新型中间体。（3R，3aS，6aR） - 六氢呋喃并[2,3-b]呋喃-3-基（1S，2R）-3 - [[（4-氨基苯基）磺酰基]（异丁基）氨基] -1-苄基-2- 羟丙基氨基甲酸酯特别可用作HIV蛋白酶抑制剂。

7. 发明授权

US07358239B2 Pyrrolidinyl, piperidinyl or homopiperidinyl substituted (benzodioxan, benzofuran or benzopyran) derivatives 有权
公开(公告)号：US07358239B2
公开(公告)日：2008-04-15
申请号：US11079606
申请日：2005-03-14
申请人： Marcel Frans Leopold De Bruyn , Kristof Van Emelen , Piet Tom Bert Paul Wigerinck , Wim Gaston Verschueren
发明人： Marcel Frans Leopold De Bruyn , Kristof Van Emelen , Piet Tom Bert Paul Wigerinck , Wim Gaston Verschueren
IPC分类号： A61P1/00 , A61K31/00 , A61K31/55 , A61K31/54 , A61K31/497 , A61K31/4965 , A61K31/517 , A61K31/505 , A61K31/41 , A61K31/415 , A61K31/40 , C07D245/00 , C07D487/00 , C07D243/00 , C07D273/00 , C07D285/00 , C07D239/00 , C07D241/00 , C07D403/00 , C07D417/00 , C07D513/00 , C07D233/00
CPC分类号： C07D405/12 , C07D405/14
摘要： The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ═NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a bivalent radical. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impaired fundic relaxation.

8. 发明授权

US06852714B2 (Benzodioxan, benzofuran or benzopyran) derivatives having fundic relaxation properties 有权
标题翻译：（苯并二恶烷，苯并呋喃或苯并吡喃）衍生物
公开(公告)号：US06852714B2
公开(公告)日：2005-02-08
申请号：US10235623
申请日：2002-09-05
申请人： Piet Tom Bert Paul Wigerinck , Wim Gaston Verschueren , Marc Francis Josephine Schroven , Marcel Frans Leopold De Bruyn
发明人： Piet Tom Bert Paul Wigerinck , Wim Gaston Verschueren , Marc Francis Josephine Schroven , Marcel Frans Leopold De Bruyn
IPC分类号： A61K31/4166 , A61K31/443 , A61K31/454 , A61K31/495 , A61K31/496 , A61K31/506 , A61P1/00 , A61P1/14 , A61P43/00 , C07D405/12 , C07D405/14 , C07D417/12 , A61K31/551 , A61K31/554 , C07D401/12 , C07D417/14
CPC分类号： C07D405/12 , C07D405/14
摘要： The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein Alk1 is C1-6alkanediyl optionally substituted with hydroxy, C1-4alkyloxy or C1-4alkylcarbonyloxy; -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical; R4 is hydrogen or C1-6alkyl; A is a bivalent radical of formula —NR6-Alk2-(b-1), or -Npiperidinyl-(CH2)m (b-2) wherein m is 0 or 1; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ═NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a bivalent radical. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impaired fundic relaxation.
摘要翻译：本发明的式（I）化合物是其立体化学异构体形式，其N-氧化物形式或其药学上可接受的酸加成盐，其中Alk是任选被羟基，C 1-4烷氧基或C 1 -C 18烷氧基取代的C 1-6烷二基 -4-烷基羰基氧基; -Z 1 -Z 2 - 是二价基团; R 1，R 2和R 3各自独立地选自氢，C 1-6烷基，羟基，卤素等; 或当R 1和R 2在相邻碳原子上时，R 1和R 2一起可以形成二价基团; R 4是氢或C 1-6烷基; A是式-NR 6 -Alk 2 - （b-1）或者N-哌啶基 - （CH 2）m（b-2）的二价基团，其中m是0或1; R 5是脯氨酸的基团，n是1或2; p <1>为0，p <2为1或2; 或p <1>为1或2，p <2为0; X是氧，硫或= NR 9; Y是氧或硫; R 7是氢，C 1-6烷基，C 3-6环烷基，苯基或苯基甲基; R 8是C 1-6烷基，C 3-6环烷基苯基或苯基甲基; R 9是氰基，C 1-6烷基，C 3-6环烷基，C 1-6烷氧基羰基或氨基羰基; R 10是氢或C 1-6烷基; 而Q是二价基团。公开了用于制备所述产品的方法，包含所述产品的制剂及其作为药物的用途，特别是用于治疗与减退的放松有关的病症。

9. 发明授权

US06747045B2 (Benzodioxan, benzofuran or benzopyran) derivatives having fundic relaxation properties 有权
标题翻译：（苯并二恶烷，苯并呋喃或苯并吡喃）衍生物
公开(公告)号：US06747045B2
公开(公告)日：2004-06-08
申请号：US10116590
申请日：2002-04-03
申请人： Piet Tom Bert Paul Wigerinck , Wim Gaston Verschueren , Marc Francis Josephine Schroven , Marcel Frans Leopold De Bruyn
发明人： Piet Tom Bert Paul Wigerinck , Wim Gaston Verschueren , Marc Francis Josephine Schroven , Marcel Frans Leopold De Bruyn
IPC分类号： C07D40312
CPC分类号： C07D405/12 , C07D405/14
摘要： The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein Alk1 is C1-6alkanediyl optionally substituted with hydroxy, C1-4alkyloxy or C1-4alkylcarbonyloxy; —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical; R4 is hydrogen or C1-6alkyl; A is a bivalent radical of formula —NR6—Alk2— (b-1), or -Npiperidinyl-(CH2)m (b-2) wherein m is 0 or 1; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ═NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a bivalent radical. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impaired fundic relaxation.
摘要翻译：本发明的式（I）化合物是其立体化学异构体形式，其N-氧化物形式或其药学上可接受的酸加成盐，其中Alk是任选被羟基，C 1-4烷氧基或C 1 -C 18烷氧基取代的C 1-6烷二基 -4-烷基羰基氧基; -Z 1 -Z 2 - 是二价基团; R 1，R 2和R 3各自独立地选自氢，C 1-6烷基，羟基，卤素等; 或当R 1和R 2在相邻碳原子上时，R 1和R 2一起可以形成二价基团; R 4是氢或C 1-6烷基; A是式-NR 6 -Alk 2 - （b-1）或者N-哌啶基 - （CH 2）m（b-2）的二价基团，其中m是0或1; R 5是脯氨酸的基团，n是1或2; p <1>为0，p <2为1或2; 或p <1>为1或2，p <2为0; X是氧，硫或= NR 9; Y是氧或硫; R 7是氢，C 1-6烷基，C 3-6环烷基，苯基或苯基甲基; R 8是C 1-6烷基，C 3-6环烷基苯基或苯基甲基; R 9是氰基，C 1-6烷基，C 3-6环烷基，C 1-6烷氧基羰基或氨基羰基; R 10是氢或C 1-6烷基; 而Q是二价基团。公开了用于制备所述产品的方法，包含所述产品的制剂及其作为药物的用途，特别是用于治疗与减退的放松有关的病症。

10. 发明申请

US20100029632A1 BROADSPECTRUM 2-AMINO-BENZOXAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS 有权
标题翻译： BROADSPECTRUM 2-氨基苯并噻唑磺酰胺艾滋病毒蛋白酶抑制剂
公开(公告)号：US20100029632A1
公开(公告)日：2010-02-04
申请号：US12575216
申请日：2009-10-07
申请人： Dominique Louis Nestor Ghislain SURLERAUX , Sandrine Marie Helene Vendeville , Wim Gaston Verschueren , Marie-Pierre T.M.M.G. De Bethune , Herman Augustinus De Kock , Abdellah Tahri
发明人： Dominique Louis Nestor Ghislain SURLERAUX , Sandrine Marie Helene Vendeville , Wim Gaston Verschueren , Marie-Pierre T.M.M.G. De Bethune , Herman Augustinus De Kock , Abdellah Tahri
IPC分类号： A61K31/5383 , A61K31/421 , C12N7/04 , A61K31/426 , A61K31/436 , A61K31/4439 , A61K31/505 , A61P31/12
CPC分类号： C07D263/58 , C07D413/12 , C07D417/12 , C07D491/04 , C07D493/04 , C07D513/04
摘要： The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9—; t is 0, 1 or 2; R2 is H or C1-6alkyl; L is —C(═O)—, —O—C(═O)—, —NR8—C(═O)—, —O—C1-6alkanediyl-C(═O)—, —NR8—C1-6alkanediyl-C(═O)—, —S(═O)2—, —O—S(═O)2—, —NR8—S(═O)2; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC(═O), carboxyl, aminoC(═O), mono- or di(C1-4alkyl)aminoC(═O), C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; R5 and R6 are H or C1-6alkyl. It further relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with another anti-retroviral agent, and to their use in assays as reference compounds or as reagents.
摘要翻译：本发明涉及具有式N-氧化物，盐，立体异构形式，外消旋混合物，前药，酯和代谢物的化合物，其中R 1和R 8各自为H，任选取代的C 1-6烷基，C 2-6烯基，C 3-7环烷基，芳基，Het1，Het2; R1也可以是式（R11aR11b）NC（R10aR10b）CR9-的基团; t为0,1或2; R2是H或C1-6烷基; L是-C（-O） - ， - OC（-O） - ， - NR8-C（-O） - ， - O-C1-6烷二基-C（ - ） - ，-NR8-C1-6烷二基-C （-O） - ， - S（-O）2 - ， - O（O）2 - ， - NR 8 -S（-O）2; R 3是C 1-6烷基，芳基，C 3-7环烷基，C 3-7环烷基C 1-4烷基或芳基C 1-4烷基; R4是H，C1-4烷基OC（-O），羧基，氨基C（-O），单或二（C1-4烷基）氨基C（-O），C3-7环烷基，C2-6烯基，C2-6炔基或任选取代的C1 -6-烷基; R5和R6是H或C1-6烷基。它还涉及它们作为广谱的HIV蛋白酶抑制剂，其制备方法以及药物组合物和包含它们的诊断试剂盒的用途。它还涉及与另一种抗逆转录病毒剂的组合，以及它们在测定中用作参考化合物或作为试剂。

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