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    Morpholino-oxazinyl-terminated alkylamino ethynyl alanine amino diol compounds for treatment of hypertension
    41.
    发明授权
    Morpholino-oxazinyl-terminated alkylamino ethynyl alanine amino diol compounds for treatment of hypertension 失效
    用于治疗高血压的吗啉代恶嗪基封端的烷基氨基乙炔基丙氨酸氨基二醇化合物

    公开(公告)号：US5422349A

    公开(公告)日：1995-06-06

    申请号：US930069

    申请日：1992-08-14

    申请人： Gunnar J. Hanson ,  Robert E. Manning

    发明人： Gunnar J. Hanson ,  Robert E. Manning

    IPC分类号： C07D295/12 ,  A61K31/395 ,  A61K31/425 ,  A61K31/535 ,  A61K31/5375 ,  A61K31/54 ,  A61K31/55 ,  A61P9/00 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P27/02 ,  A61P27/06 ,  A61P43/00 ,  C07D265/06 ,  C07D265/30 ,  C07D265/32 ,  C07D267/10 ,  C07D277/04 ,  C07D285/00 ,  C07D295/13 ,  C07D498/08 ,  C07D295/00

    CPC分类号： C07D265/30 ,  C07D265/32 ,  C07D267/10 ,  C07D277/04 ,  C07D285/00 ,  C07D295/13

    摘要： Compounds characterized generally as morpholino/oxazinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 ; wherein X is selected from oxygen atom and methylene; wherein B is selected from morpholino, oxo-substituted-morpholino and 1,3-oxazinyl groups; wherein R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R.sub.2 is phenylmethyl; wherein each of R.sub.3 and R.sub.5 is hydrido; wherein R.sub.4 is selected from--(CH.sub.2).sub.q --C.tbd.C--Vwherein V is selected from hydrido and methyl; wherein R.sub.6 is cyclohexylmethyl; wherein R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.

    摘要翻译： 通常被视为吗啉代/恶嗪基封端的烷基氨基乙炔基丙氨酸氨基二醇衍生物的化合物可用作治疗高血压的肾素抑制剂。 特别感兴趣的化合物是式I的化合物.Ein X选自氧原子和亚甲基; 其中B选自吗啉代，氧代取代吗啉代和1,3-恶嗪基; 其中R1选自氢，甲基，乙基，异丙基和正丙基; 其中R2是苯基甲基; 其中R3和R5各自是氢的; 其中R 4选自 - （CH 2）q -C 3 CON C-V，其中V选自氢和甲基; 其中R6是环己基甲基; 其中R 7选自异丁基，环丙基和环丙基甲基; 其中q是选自0至3的数字（包括端值）; 并且其中n是选自0至3的数字，包括端值; 或其药学上可接受的盐。

    Benzo-fused oxazopinyl-terminated alkylamino ethynyl alanine amino diol compounds for treatment of hypertension
    43.
    发明授权
    Benzo-fused oxazopinyl-terminated alkylamino ethynyl alanine amino diol compounds for treatment of hypertension 失效
    用于治疗高血压的苯并稠合的恶唑啉基封端的烷基氨基乙炔基丙氨酸氨基二醇化合物

    公开(公告)号：US5411954A

    公开(公告)日：1995-05-02

    申请号：US199410

    申请日：1994-02-22

    申请人： Gunnar J. Hanson ,  Robert E. Manning

    发明人： Gunnar J. Hanson ,  Robert E. Manning

    IPC分类号： C07D295/12 ,  A61K31/395 ,  A61K31/425 ,  A61K31/535 ,  A61K31/5375 ,  A61K31/54 ,  A61K31/55 ,  A61P9/00 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P27/02 ,  A61P27/06 ,  A61P43/00 ,  C07D265/06 ,  C07D265/30 ,  C07D265/32 ,  C07D267/10 ,  C07D277/04 ,  C07D285/00 ,  C07D295/13 ,  C07D498/08 ,  C07D267/14

    CPC分类号： C07D265/30 ,  C07D265/32 ,  C07D267/10 ,  C07D277/04 ,  C07D285/00 ,  C07D295/13

    摘要： Compounds characterized generally as benzo-fused oxazopinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 ; wherein X is selected from oxygen atom and methylene; wherein B is a benzo-fused oxazopinyl group; wherein R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R.sub.2 is phenylmethyl; wherein each of R.sub.3 and R.sub.5 is hydrido; wherein R.sub.4 is selected from--(CH.sub.2).sbsb.q--C.ident.C-Vwherein V is selected from hydrido and methyl; wherein R.sub.6 is cyclohexylmethyl; wherein R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.

    摘要翻译： 通常以苯并稠合的恶唑啉基封端的烷基氨基乙炔基丙氨酸氨基二醇衍生物表征的化合物可用作治疗高血压的肾素抑制剂。 特别感兴趣的化合物是式I的化合物（I）其中A选自CO和SO 2; 其中X选自氧原子和亚甲基; 其中B是苯并稠合的恶唑啉基; 其中R1选自氢，甲基，乙基，异丙基和正丙基; 其中R2是苯基甲基; 其中R3和R5各自是氢的; 其中R 4选自 - （CH 2）q -C = C-V，其中V选自氢和甲基; 其中R6是环己基甲基; 其中R 7选自异丁基，环丙基和环丙基甲基; 其中q是选自0至3的数字（包括端值）; 并且其中n是选自0至3的数字，包括端值; 或其药学上可接受的盐。

    Renal-selective biphenylmethyl imidazole angiotensin II antagonists for treatment of hypertension
    45.
    发明授权
    Renal-selective biphenylmethyl imidazole angiotensin II antagonists for treatment of hypertension 失效
    肾选择性联苯甲基咪唑血管紧张素II拮抗剂治疗高血压

    公开(公告)号：US5302610A

    公开(公告)日：1994-04-12

    申请号：US810321

    申请日：1991-12-19

    申请人： Robert E. Manning ,  David B. Reitz

    发明人： Robert E. Manning ,  David B. Reitz

    IPC分类号： A61K47/48 ,  C07D233/68 ,  C07D403/10 ,  A61K31/415 ,  A61K31/495 ,  C07D233/54 ,  C07D241/04 ,  C07D257/04 ,  C07D265/30

    CPC分类号： C07D403/10 ,  A61K47/48023 ,  A61K47/48061 ,  C07D233/68

    摘要： Renal-selective compounds are described which, in one embodiment, are prodrugs preferentially converted in the kidney to compounds capable of blocking angiotensin II (AII) receptors. These prodrugs are conjugates formed from two components, namely, a first component provided by an AII antagonist compound and a second component which is capable of being cleaved from the first component when both components are chemically linked within the conjugate. The two components are chemically linked by a bond which is cleaved selectively in the kidney, for example, by an enzyme. The liberated AII antagonist compound is then available to block AII receptors within the kidney. Conjugates of particular interest are glutamyl derivatives of biphenylmethyl 1H-substituted imidazole compounds, of which N-acetyl-L-glutamic acid, 5-[[4'-[2-butyl-4-chloro-5-(hydroxymethyl)-1H-imidazol-1-ylmethyl][1,1'-biphenyl]-2-yl]carbonyl]hydrazide (shown below) is an example: ##STR1##

    摘要翻译： 描述了肾选择性化合物，其在一个实施方案中是优先在肾中转化为能够阻断血管紧张素II（AII）受体的化合物的前药。 这些前药是由两种组分形成的缀合物，即由AII拮抗剂化合物提供的第一组分和当两种组分在缀合物内化学连接时能够从第一组分切割的第二组分。 两种组分通过在肾脏中有选择性地切割的键化学连接，例如通过酶。 然后释放的AII拮抗剂化合物可用于阻断肾脏内的AII受体。 特别感兴趣的缀合物是联苯甲基1H-取代的咪唑化合物的谷氨酰基衍生物，其中N-乙酰基-L-谷氨酸5 - （（4' - （2-丁基-4-氯-5-（羟甲基） 咪唑-1-基甲基）（1,1'-联苯）-2-基）羰基）酰肼（如下所示）是一个实例：（*化学结构*）

    N-substituted N-(alpha-triazolyl-toluyl)pyrrole compounds and use for treatment of circulatory disorders
    46.
    发明授权
    N-substituted N-(alpha-triazolyl-toluyl)pyrrole compounds and use for treatment of circulatory disorders 失效
    N-取代的N-（ALPHA-TRIAZOLYL-TOLUYL）吡咯烷酮化合物和用于治疗循环障碍的用途

    公开(公告)号：US5175180A

    公开(公告)日：1992-12-29

    申请号：US630714

    申请日：1990-12-20

    申请人： Philippe R. Bovy ,  David B. Reitz ,  Robert E. Manning

    发明人： Philippe R. Bovy ,  David B. Reitz ,  Robert E. Manning

    IPC分类号： C07D403/10 ,  C07D403/14

    CPC分类号： C07D403/10 ,  C07D403/14

    摘要： A class of N-substituted N-(.alpha.-triazolyltoluyl)pyrrole compounds described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of the formula ##STR1## wherein m is one; wherein R.sup.1 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, n-pentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, cyclohexanoyl, 1-oxo-2-cyclohexylethyl, benzoyl, 1-oxo-2-phenethyl, 1-oxopropyl, 1-oxobutyl, 1-oxopentyl and 2-hydroxybutyl; wherein R.sup.2 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, isopentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, propylthio, butylthio, and hydroxyalkyl; wherein each of R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9 and R.sup.10 is independently selected from hydrido, halo, nitro, trifluoromethyl, hydroxy, alkoxy, cyano, carboxyl and methoxycarbonyl; with the proviso that at least one of R.sup.5 and R.sup.8 must be selected from COOH, SH, PO.sub.3 H.sub.2, SO.sub.3 H, CONHNH.sub.2, CONHNHSO.sub.2 CF.sub.3, OH, ##STR2## wherein each of R.sup.42 and R.sup.43 is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl; or a tautomer thereof or a pharmaceutically-acceptable salt thereof. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.

    摘要翻译： 描述用于治疗循环系统疾病的一类N-取代的N-（α-三唑基甲苯磺酰基）吡咯化合物。 特别感兴趣的化合物是式IMAMA的血管紧张素II拮抗剂，其中m是1; 其中R1选自甲基，乙基，正丙基，异丙基，正丁基，仲丁基，异丁基，叔丁基，4-甲基丁基，正戊基，新戊基，苯基，苄基，苯乙基，环己基，环己基甲基，环己基乙基 ，环己酰基，1-氧代-2-环己基乙基，苯甲酰基，1-氧代-2-苯乙基，1-氧代丙基，1-氧代丁基，1-氧代戊基和2-羟基丁基; 其中R2选自甲基，乙基，正丙基，异丙基，正丁基，仲丁基，异丁基，叔丁基，正戊基，异戊基，新戊基，苯基，苄基，苯乙基，环己基，环己基甲基，丙硫基，丁硫基 ，和羟烷基; 其中R 3，R 4，R 5，R 6，R 7，R 8，R 9和R 10各自独立地选自氢，卤素，硝基，三氟甲基，羟基，烷氧基，氰基，羧基和甲氧基羰基; 条件是R 5和R 8中的至少一个必须选自COOH，SH，PO3H2，SO3H，CONHNH2，CONHNHSO2CF3，OH，其中R42和R43各自独立地选自氯，氰基，硝基，三氟甲基， 甲氧基羰基和三氟甲基磺酰基; 或其互变异构体或其药学上可接受的盐。 这些化合物特别可用于治疗或控制高血压和充血性心力衰竭。

    N-substituted imidazol-2-one compounds for treatment of circulatory disorders
    47.
    发明授权
    N-substituted imidazol-2-one compounds for treatment of circulatory disorders 失效
    用于治疗循环系统疾病的N-取代咪唑-2-酮化合物

    公开(公告)号：US5087634A

    公开(公告)日：1992-02-11

    申请号：US606806

    申请日：1990-10-31

    申请人： David B. Reitz ,  Robert E. Manning

    发明人： David B. Reitz ,  Robert E. Manning

    IPC分类号： C07D233/70 ,  C07D403/10 ,  C07D409/14

    CPC分类号： C07D403/10 ,  C07D233/70 ,  C07D409/14

    摘要： A class of N-substituted imidazol-2-one compounds is described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of the formula ##STR1## wherein m is one; wherein R.sup.1 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, n-pentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, cyclohexanoyl, 1-oxo-2-cyclohexylethyl, benzoyl, 1-oxo-2-phenethyl, 1-oxopropyl, 1-oxobutyl, 1-oxopentyl and 2-hydroxybutyl; wherein R.sup.0 is selected from hydrido, methyl, fluoro, chloro, monofluoromethyl, difluoromethyl, trifluoromethyl, formyl, carboxyl and dimethoxymethyl; wherein R.sup.2 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, isopentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, propylthio, butylthio, and hydroxyalkyl; wherein each of R.sup.3, R.sup.4, R.sup.6, R.sub.7, R.sup.8, R.sup.10 and R.sup.11 is hydrido; with the proviso that at least one of R.sup.5 and R.sup.9 must be selected from COOH, SH, PO.sub.3 H.sub.2, SO.sub.3 H, CONHNH.sub.2, CONHNHSO.sub.2 CF.sub.3, OH, ##STR2## wherein each of R.sup.42 and R.sup.43 is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl; or a tautomer thereof or a pharmaceutically-acceptable salt thereof. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.

    摘要翻译： 描述了一类用于治疗循环障碍的N-取代咪唑-2-酮化合物。 特别感兴趣的化合物是式IMAMA的血管紧张素II拮抗剂，其中m是1; 其中R1选自甲基，乙基，正丙基，异丙基，正丁基，仲丁基，异丁基，叔丁基，4-甲基丁基，正戊基，新戊基，苯基，苄基，苯乙基，环己基，环己基甲基，环己基乙基 ，环己酰基，1-氧代-2-环己基乙基，苯甲酰基，1-氧代-2-苯乙基，1-氧代丙基，1-氧代丁基，1-氧代戊基和2-羟基丁基; 其中R 0选自氢，甲基，氟，氯，单氟甲基，二氟甲基，三氟甲基，甲酰基，羧基和二甲氧基甲基; 其中R2选自甲基，乙基，正丙基，异丙基，正丁基，仲丁基，异丁基，叔丁基，正戊基，异戊基，新戊基，苯基，苄基，苯乙基，环己基，环己基甲基，丙硫基，丁硫基 ，和羟烷基; 其中R3，R4，R6，R7，R8，R10和R11各自为氢; 条件是R 5和R 9中的至少一个必须选自COOH，SH，PO 3 H 2，SO 3 H，CONHNH 2，CONHNHSO 2 CF 3，OH，其中R 42和R 43各自独立地选自氯， 氰基，硝基，三氟甲基，甲氧基羰基和三氟甲基磺酰基; 或其互变异构体或其药学上可接受的盐。 这些化合物特别可用于治疗或控制高血压和充血性心力衰竭。

    Core spun filtration roving
    48.
    发明授权
    Core spun filtration roving 失效
    芯纺过滤粗纱

    公开(公告)号：US4225442A

    公开(公告)日：1980-09-30

    申请号：US935752

    申请日：1978-08-22

    申请人： Maurice H. Tremblay ,  Robert E. Manning ,  Gerard Lanoue ,  Frank Gaiteri, Jr.

    发明人： Maurice H. Tremblay ,  Robert E. Manning ,  Gerard Lanoue ,  Frank Gaiteri, Jr.

    IPC分类号： B01D29/11 ,  B01D39/16 ,  B01D39/20 ,  D02G3/36 ,  D02G3/44 ,  B01D27/02 ,  B01D29/08 ,  D02G3/38

    CPC分类号： D02G3/447 ,  B01D29/111 ,  B01D39/1607 ,  B01D39/2017 ,  B01D39/2041 ,  D02G3/36 ,  B01D2239/0464 ,  B01D2239/0636 ,  B01D2239/065 ,  B01D2239/0695 ,  B01D2239/10 ,  D10B2505/04

    摘要： A low twist, high bulk filtration roving is prepared by wrapping a sliver comprised of individual fibers, around a core in the conventional manner. Exemplary of the bulk fibers which may be employed are naturally occurring fibers such as jute, cotton, animal hair; synthetic polymer fibers, such as acrylic, nylon, polyester, olefin, aramid, teflon; man-made organic fibers deriving from natural sources such as rayon or cellulose acetate; and inorganic fibers such as metal, glass, graphite; or a blend of two or more of these fibers. Examples of the core, which can be continuous filaments, monofilaments or spun yarn, are one or more strands of the same composition as the fibers, or a combination thereof, twisted paper which can be plain, impregnated or metallized, and metal wire. Where the material is capable of being cast in film form, slit film may be employed as the strand(s). The composite roving is wound upon a rigid perforated tubular center to form a filter cartridge.

    摘要翻译： 通过以常规方式围绕芯部包裹由单独的纤维组成的纱条来制备低捻度，大批量过滤粗纱。 可以使用的本体纤维的示例是天然存在的纤维，例如黄麻，棉花，动物毛; 合成聚合物纤维，如丙烯酸，尼龙，聚酯，烯烃，芳族聚酰胺，特氟隆; 人造丝或乙酸纤维素等天然来源的人造有机纤维; 无机纤维如金属，玻璃，石墨; 或这些纤维中的两种或更多种的混合物。 可以是连续长丝，单丝或短纤纱的芯的实例是与纤维相同组成的一条或多条线，或其组合，可以是平坦的，浸渍的或金属化的扭曲纸和金属线。 当材料能够以薄膜形式铸造时，可以使用切割薄膜作为绞合线。 将复合粗纱卷绕在刚性穿孔的管状中心上以形成滤筒。

    N,N'-disubstituted-p-phenylenediamines
    49.
    发明授权
    N,N'-disubstituted-p-phenylenediamines 失效
    N，N {40-二取代对苯二胺

    公开(公告)号：US3963780A

    公开(公告)日：1976-06-15

    申请号：US442615

    申请日：1974-02-14

    申请人： Robert E. Manning

    发明人： Robert E. Manning

    IPC分类号： C07C87/29

    CPC分类号： Y10S514/909

    摘要： N,N'-disubstituted-p-phenylenediamines, e.g., N-(3-isopropoxypropyl)-N'-(2-octyl)-p-phenylenediamine or N-phenethyl-N'-(2-octyl)-p-phenylenediamine, are prepared by condensing phenylenediamines with an alkyl carbonyl in the presence of a reducing catalyst, and are useful as hypolipidemic and anti-obesity agents.

    摘要翻译： N，N'-二取代对苯二胺，例如N-（3-异丙氧基丙基）-N' - （2-辛基） - 对苯二胺或N-苯乙基-N' - （2-辛基） - 对苯二胺 通过在还原催化剂的存在下将亚苯基二胺与烷基羰基缩合制备，并且可用作降血脂和抗肥胖剂。