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    Piperidinyl-terminated alkylamino ethynl alanine amino diol compounds for treatment of hypertension
    91.
    发明授权
    Piperidinyl-terminated alkylamino ethynl alanine amino diol compounds for treatment of hypertension 失效
    哌啶基封端的烷基氨基乙炔丙氨酸二氨基二醇化合物治疗高血压

    公开(公告)号：US5780494A

    公开(公告)日：1998-07-14

    申请号：US841536

    申请日：1997-04-23

    Applicant: Gunnar J. Hanson

    Inventor： Gunnar J. Hanson

    IPC: C07D205/04 ,  C07D209/44 ,  C07D209/52 ,  C07D211/14 ,  C07D211/26 ,  C07D211/38 ,  C07D211/70 ,  C07D211/78 ,  C07D217/04 ,  C07D221/22 ,  C07D223/14 ,  C07D295/13 ,  C07D451/02 ,  C07D453/06 ,  A61K31/405 ,  A61K31/40 ,  C07D207/06 ,  C07D209/08

    CPC classification number: C07D221/22 ,  C07D205/04 ,  C07D209/44 ,  C07D209/52 ,  C07D211/14 ,  C07D211/26 ,  C07D211/38 ,  C07D211/70 ,  C07D211/78 ,  C07D217/04 ,  C07D223/14 ,  C07D295/13 ,  C07D451/02 ,  C07D453/06

    Abstract: Compounds characterized generally as piperidinyl-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 a piperidinyl group, an isoindolyl group and an azabicyclononyl 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 ##STR2## wherein 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.

    Abstract translation: 通常被称为哌啶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（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选自哌啶基，异吲哚基和氮杂双环壬基; 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。

    Tricyclic 2,3,4,5-tetrahydro-1H-3-benzapines
    94.
    发明授权
    Tricyclic 2,3,4,5-tetrahydro-1H-3-benzapines 失效
    三环2,3,4,5-四氢-1H-3-苯偶氮

    公开(公告)号：US5512562A

    公开(公告)日：1996-04-30

    申请号：US202401

    申请日：1994-02-24

    Applicant: Rolf Hohlweg ,  Erik B. Nielsen

    Inventor： Rolf Hohlweg ,  Erik B. Nielsen

    IPC: A61K31/55 ,  A61P25/00 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P43/00 ,  C07D223/14 ,  C07D223/32 ,  C07D405/04 ,  C07D491/04 ,  C07D491/048 ,  C07D491/056 ,  C07D495/04 ,  C07D498/04

    CPC classification number: C07D405/04 ,  C07D223/14 ,  C07D223/32 ,  C07D491/04 ,  C07D495/04

    Abstract: Tricyclic benzazepines having the general formula ##STR1## wherein A together with the .alpha.- and .beta.-marked carbon atoms is a cyclopentene, cyclohexene, furan, dihydrofuran, pyran, dihydropyran, thiophene, oxazole, pyrrole, pyrroline, tetrahydropyridine or dioxole ring, R.sup.1 is H or alkyl, R.sup.2 and R.sup.3 independently are H, alkoxy, halogen, nitro, cyano or hydroxy, or R.sup.2 and R.sup.3 together may form a furan, dihydrofuran, cyclopentene or dioxole ring and R.sup.4 is H, alkoxy, nitro, cyano, hydroxy or halogen, or a pharmaceutically acceptable salt thereof, are useful in treatment of certain disorders in the central nervous system, e.g., psychosis, pain, depression, sleep disturbances, dyskinesia, Parkinson's disease, stroke.

    Abstract translation: 具有通式的三环苯并吖庚因其中A与α和β标记的碳原子一起是环戊烯，环己烯，呋喃，二氢呋喃，吡喃，二氢吡喃，噻吩，恶唑，吡咯，吡咯啉，四氢吡啶或二氧杂环戊烯环，R1 R 2和R 3独立地是H，烷氧基，卤素，硝基，氰基或羟基，或者R 2和R 3一起可以形成呋喃，二氢呋喃，环戊烯或二氧杂环戊烯，R4是H，烷氧基，硝基，氰基，羟基 或卤素或其药学上可接受的盐可用于治疗中枢神经系统中的某些疾病，例如精神病，疼痛，抑郁症，睡眠障碍，运动障碍，帕金森病，中风。

    14-O-p-chlorobenzoylaconine and analgesic/anti-inflammatory agent containing the same
    96.
    发明授权
    14-O-p-chlorobenzoylaconine and analgesic/anti-inflammatory agent containing the same 失效
    14-O-对氯苯甲酰乌头碱和含有其的镇痛/抗炎剂

    公开(公告)号：US5330983A

    公开(公告)日：1994-07-19

    申请号：US989018

    申请日：1993-03-05

    Applicant: Mitsuo Murayama

    Inventor： Mitsuo Murayama

    IPC: A61K31/435 ,  A61K36/18 ,  A61P25/04 ,  A61P29/00 ,  C07D221/18 ,  C07D221/22 ,  C07D223/14

    CPC classification number: C07D221/22

    Abstract: Analgesic/anti-inflammatory agent containing as active ingredient 14-O-p-chlorobenzoylaconine or a salt thereof. 14-O-p-chlorobenzoylaconine is a novel substance and a compound with high safety which shows an analgesic action on both inflammatory and non-inflammatory pains as well as an anti-inflammatory action. This compound can be used in the treatment of pain-causing diseases, both inflammatory and non-inflammatory, as well as in the treatment of inflammation.

    Abstract translation: PCT No.PCT / JP91 / 01298 Sec。 371日期1993年3月5日 102（e）1993年3月5日PCT 1991年9月27日PCT。含有作为有效成分的14-O-对氯苯甲酰乌头碱或其盐的镇痛/抗炎剂。 14-O-对氯苯甲酰乌头碱是一种新型物质和具有高度安全性的化合物，其对炎性和非炎症性疼痛以及抗炎作用均显示镇痛作用。 该化合物可用于治疗炎性和非炎症性疼痛的疾病以及治疗炎症。

    Azabicyclo compounds, useful as intermediates
    99.
    发明授权
    Azabicyclo compounds, useful as intermediates 失效
    氮杂双环化合物，可用作中间体

    公开(公告)号：US4697019A

    公开(公告)日：1987-09-29

    申请号：US824205

    申请日：1986-03-21

    Applicant: Francis D. King

    Inventor： Francis D. King

    IPC: A61K31/435 ,  A61K31/445 ,  A61P1/00 ,  A61P43/00 ,  C07D221/00 ,  C07D223/04 ,  C07D227/00 ,  C07D471/08 ,  C07D487/08 ,  C07D221/04 ,  C07D223/14

    CPC classification number: C07D471/08 ,  C07D223/04

    Abstract: A compound of formula (XXII): ##STR1## or a compound of formula (XXIII): ##STR2## wherein in formula (XXIII), j.sup.1 -1 is 1 to 4; and Q.sub.6 and Q.sub.7 are on the same carbon atom; and wherein, in formulae (XXII) and (XXIII), Q.sub.6 is NH.sub.2 and Q.sub.7 is H, and either p is 0 to 2 and q is 1; or p is 1 and q is 0 to 3; and one of R.sub.5 and R.sub.6 is hydrogen, C.sub.1-6 alkyl, phenyl or phenyl --C.sub.1-3 alkyl, which phenyl moieties may be substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, CF.sub.3 or halogen; and the other of R.sub.5 and R.sub.6 is hydrogen or C.sub.1-6 alkyl.

    Abstract translation: （XXII）化合物：ⅩⅩⅫ或式（ⅩⅩⅢ）化合物：其中在式（ⅩⅩⅢ）中，j1-1为1至4; Q6和Q7位于相同的碳原子上; 并且其中，在式（XXII）和（XXIII）中，Q 6为NH 2且Q 7为H，p为0〜2，q为1。 或p为1，q为0至3; R 5和R 6中的一个是氢，C 1-6烷基，苯基或苯基-C 1-3烷基，该苯基部分可被C 1-6烷基，C 1-6烷氧基，CF 3或卤素取代; R 5和R 6中的另一个是氢或C 1-6烷基。

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