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1. 发明授权

US06495547B1 (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：US06495547B1
公开(公告)日：2002-12-17
申请号：US09641485
申请日：2000-08-18
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： C07D40514
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：式（I）化合物的本发明是其立体化学异构形式，其N-氧化物形式或其药学上可接受的酸加成盐，其中Alk1是任选被羟基，C 1-4烷氧基或C 1-4烷基羰基氧基取代的C 1-6烷二基; -Z1-Z2-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; R4是氢或C1-6烷基; A是式-NR6-Alk2-（b-1）或-N-哌啶基 - （CH2）m（b-2）的二价基团，其中m是0或1; R5是一种基团，其中n是1或2; p1为0，p2为1或2; 或p1为1或2，p2为0; X是氧。硫或= NR9; Y是氧或硫; R7是氢，C1-6烷基，C3-6环烷基，苯基或苯基甲基; R8是C1-6烷基，C3-6环烷基苯基或苯基甲基; R9是氰基，C1-6烷基，C3-6环烷基，C1-6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。

2. 发明授权

US6133277A (Benzodioxan, benzofuran or benzopyran) derivatives having fundic relaxation properties 有权
公开(公告)号：US6133277A
公开(公告)日：2000-10-17
申请号：US192686
申请日：1998-11-16
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 , A61K31/54 , A01N43/54 , A61K31/505 , C07D285/16 , C07D473/00
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 Alk.sup.1 is C.sub.1-6 alkanediyl optionally substituted with hydroxy, C.sub.1-4 alkyloxy or C.sub.1-4 alkylcarbonyloxy; --Z.sup.1 --Z.sup.2 -- is a bivalent radical; R.sup.1, R.sup.2 and R.sup.3 are each independently selected from hydrogen, C.sub.1-6 alkyl, hydroxy, halo and the like; or when R.sup.1 and R.sup.2 are on adjacent carbon atoms, R.sup.1 and R.sup.2 taken together may form a bivalent radical; R.sup.4 is hydrogen or C.sub.1-6 alkyl; A is a bivalent radical of formula --NR.sup.6 --Alk.sup.2 -- (b-1), or --Npiperidinyl--(CH.sub.2).sub.m (b-2) wherein m is 0 or 1; R.sup.5 is a radical of formula ##STR1## wherein n is 1 or 2; p.sup.1 is 0, and p.sup.2 is 1 or 2; or p.sup.1 is 1 or 2, and p.sup.2 is 0; X is oxygen, sulfur or .dbd.NR.sup.9 ; Y is oxygen or sulfur; R.sup.7 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, phenyl or phenylmethyl; R.sup.8 is C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl phenyl or phenylmethyl; R.sup.9 is cyano, C.sub.1-6 alkyl, C.sub.3-6 cyclo-alkyl, C.sub.1-6 alkyloxycarbonyl or aminocarbonyl; R.sup.10 is hydrogen or C.sub.1-6 alkyl; 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.

3. 发明授权

US6100268A Vasoconstrictive dihydrobenzopyran derivatives 失效
标题翻译：血管收缩性二氢苯并吡喃衍生物
公开(公告)号：US6100268A
公开(公告)日：2000-08-08
申请号：US123893
申请日：1998-07-28
申请人： Guy Rosalia Eugene Van Lommen , Piet Tom Bert Paul Wigerinck , Marcel Frans Leopold De Bruyn , Wim Gaston Verschueren , Marc Francis Josephine Schroven
发明人： Guy Rosalia Eugene Van Lommen , Piet Tom Bert Paul Wigerinck , Marcel Frans Leopold De Bruyn , Wim Gaston Verschueren , Marc Francis Josephine Schroven
IPC分类号： C07D491/052 , A61K31/35 , A61K31/352 , A61K31/40 , A61K31/4025 , A61K31/415 , A61K31/425 , A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/50 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/53 , A61P9/00 , A61P9/08 , C07D311/58 , C07D311/78 , C07D311/92 , C07D311/94 , C07D405/12 , C07D405/14 , C07D409/14 , C07D417/12 , C07D493/04
CPC分类号： C07D405/12 , C07D311/58 , C07D405/14 , C07D409/14 , C07D417/12 , C07D493/04
摘要： The present invention is concerned with compounds of formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen or C.sub.1-6 alkyl; R.sup.3 is hydrogen or C.sub.1-6 -alkyl; R.sup.4 is hydrogen, halo, C.sub.1-6 alkyl, hydroxy, C.sub.1-6 alkyloxy, aryloxy or arylmethoxy; R.sup.5 and R.sup.6 designate R.sup.5a and R.sup.6a wherein R.sup.5a and R.sup.6a taken together form a bivalent radical; or R.sup.5 and R.sup.6 can designate R.sup.5b and R.sup.6b wherein R.sup.5b is hydrogen and R.sup.6b is a heterocycle or an optionally substituted alkenyl or alkynyl group; or R.sup.5 and R.sup.6 designate R.sup.5c and R.sup.6c, wherein R.sup.5c and R.sup.6c are hydrogen, halo, C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-6 alkynyl, hydroxy, C.sub.1-6 alkyloxy, cyano, aminoC.sub.1-6 alkyl, carboxyl, C.sub.1-6 alkyloxycarbonyl, nitro, amino, aminocarbonyl, C.sub.1-6 alkylcarbonylamino, or mono-di(C.sub.1-6 alkyl)amino; Q is a heterocyclic ring containing at least one nitrogen atom or a radical of formula ##STR2## pharmaceutical compositions, preparations and use as a medicine are also described.
摘要翻译：本发明涉及式的化合物及其药学上可接受的酸加成盐及其立体化学异构形式，其中R 1是氢或C 1-6烷基; R2是氢或C1-6烷基; R3是氢或C1-6烷基; R4是氢，卤素，C1-6烷基，羟基，C1-6烷氧基，芳氧基或芳基甲氧基; R5和R6表示R5a和R6a，其中R5a和R6a一起形成二价基团; 或R5和R6可以表示R5b和R6b，其中R5b是氢，R6b是杂环或任选取代的烯基或炔基; 或者R5和R6表示R5c和R6c，其中R5c和R6c是氢，卤素，C1-6烷基，C3-6烯基，C3-6炔基，羟基，C1-6烷氧基，氰基，氨基C1-6烷基，羧基，C1-6烷氧基羰基，硝基，氨基，氨基羰基，C 1-6烷基羰基氨基或单 - 二（C 1-6烷基）氨基; Q是含有至少一个氮原子的杂环或式的药物组合物的基团，作为药物的制剂和用途也被描述。

4. 发明授权

US5824682A Vasoconstrictive dihydrobenzopyran derivatives 失效
标题翻译：血管收缩性二氢苯并吡喃衍生物
公开(公告)号：US5824682A
公开(公告)日：1998-10-20
申请号：US586760
申请日：1996-01-30
申请人： Guy Rosalia Eugene Van Lommen , Piet Tom Bert Paul Wigerinck , Marcel Frans Leopold De Bruyn , Wim Gaston Verschueren , Marc Francis Josephine Schroven
发明人： Guy Rosalia Eugene Van Lommen , Piet Tom Bert Paul Wigerinck , Marcel Frans Leopold De Bruyn , Wim Gaston Verschueren , Marc Francis Josephine Schroven
IPC分类号： C07D491/052 , A61K31/35 , A61K31/352 , A61K31/40 , A61K31/4025 , A61K31/415 , A61K31/425 , A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/50 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/53 , A61P9/00 , A61P9/08 , C07D311/58 , C07D311/78 , C07D311/92 , C07D311/94 , C07D405/12 , C07D405/14 , C07D409/14 , C07D417/12 , C07D493/04
CPC分类号： C07D405/12 , C07D311/58 , C07D405/14 , C07D409/14 , C07D417/12 , C07D493/04
摘要： The present invention is concerned with compounds of formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen or C.sub.1-6 alkyl; R.sup.3 is hydrogen or C.sub.1-6 alkyl; R.sup.4 is hydrogen, halo, C.sub.1-6 alkyl, hydroxy, C.sub.1-6 alkyloxy, aryloxy or arylmethoxy; R.sup.5 and R.sup.6 designate R.sup.5a and R.sup.6a wherein R.sup.5a and R.sup.6a taken together form a bivalent radical; or R.sup.5 and R.sup.6 can designate R.sup.5b and R.sup.6b wherein R.sup.5b is hydrogen and R.sup.6b is a heterocycle or an optionally substituted alkenyl or alkynyl group; or R.sup.5 and R.sup.6 designate R.sup.5c and R.sup.6c, wherein R.sup.5c and R.sup.6c are hydrogen, halo, C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-6 alkynyl, hydroxy, C.sub.1-6 alkyloxy, cyano, aminoC.sub.1-6 alkyl, carboxyl, C.sub.1-6 alkyloxycarbonyl, nitro, amino, aminocarbonyl, C.sub.1-6 alkylcarbonylamino, or mono-di(C.sub.1-6 alkyl)amino; Q is a heterocyclic ring containing at least one nitrogen atom or a radical of formula ##STR2## pharmaceutical compositions, preparations and use as a medicine are also described.
摘要翻译： PCT No.PCT / EP94 / 02703 Sec。 371日期1996年1月30日 102（e）日期1996年1月30日PCT 1994年8月12日PCT PCT。公开号WO95 / 05383 日期：1995年2月23日本发明涉及式（I）化合物及其药学上可接受的酸加成盐及其立体化学异构形式，其中R 1为氢或C 1-6烷基; R2是氢或C1-6烷基; R3是氢或C1-6烷基; R4是氢，卤素，C1-6烷基，羟基，C1-6烷氧基，芳氧基或芳基甲氧基; R5和R6表示R5a和R6a，其中R5a和R6a一起形成二价基团; 或R5和R6可以表示R5b和R6b，其中R5b是氢，R6b是杂环或任选取代的烯基或炔基; 或者R5和R6表示R5c和R6c，其中R5c和R6c是氢，卤素，C1-6烷基，C3-6烯基，C3-6炔基，羟基，C1-6烷氧基，氰基，氨基C1-6烷基，羧基，C1-6烷氧基羰基，硝基，氨基，氨基羰基，C 1-6烷基羰基氨基或单 - 二（C 1-6烷基）氨基; Q是含有至少一个氮原子的杂环或式（ⅩⅧ）基团的药物组合物，制剂和作为药物的用途。

5. 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。

6. 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。

7. 发明授权

US06900222B1 Pyrrolidinyl, piperdinyl or homopiperidinyl substituted (benzodioxan, benzofuran or benzopyran) derivatives 有权
公开(公告)号：US06900222B1
公开(公告)日：2005-05-31
申请号：US09980451
申请日：2000-05-23
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： A61K31/505 , A61K31/513 , A61P1/06 , A61P1/14 , A61P9/00 , C07D405/12 , C07D405/14
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 thereon 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

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.

9. 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。

10. 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。

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