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    Substituted benzylaminoquinuclidines as substance P antagonists
    2.
    发明授权
    Substituted benzylaminoquinuclidines as substance P antagonists 失效
    取代的苄基氨基奎宁啶作为物质P拮抗剂

    公开(公告)号：US5604241A

    公开(公告)日：1997-02-18

    申请号：US416913

    申请日：1995-04-20

    申请人： Fumitaka Ito ,  Kunio Satake ,  Kaoru Shimada

    发明人： Fumitaka Ito ,  Kunio Satake ,  Kaoru Shimada

    IPC分类号： C07D453/02 ,  C07F9/6561 ,  A61K31/445

    CPC分类号： C07F9/6561 ,  C07D453/02

    摘要： Compounds useful in the treatment of inflammatory disorders, central nervous system disorders and other disorders of the formula I ##STR1## and the pharmaceutically-acceptable salts thereof, wherein Ar.sup.1 and Ar.sup.2 are each independently aryl or substituted aryl; R.sup.1 is alkyl having from 1 to 6 carbon atoms;R.sup.2 is hydrogen or alkyl having from 1 to 6 carbon atoms;and either X and Y are taken separately and they are each, independently, hydrogen, dialkylphosphoryl having 2 to carbon atoms, alkyl having from 1 to 6 carbon atoms, alkenyl having from 2 to 6 carbon atoms or alkynyl having from 2 to 6 carbon atoms; or X and Y are taken together and they represent a hydrocarbon chain having 3, 4, or 5 carbon atoms, optionally containing up to 2 double bonds and optionally having 1 or 2 substituents selected from oxo, hydroxy and alkyl having from 1 to 6 carbon atoms; or Y is methoxy when X is ethyl; provided that when X and Y are taken together they are attached to adjacent carbon atoms; and provided that if either X or Y is hydrogen, then the other one must be alkenyl or alkynyl; and provided that when Y is methoxy and X is ethyl, then Y is at the 4-position and X is at the 5-position, Ar.sup.1 or Ar.sup.2 must each be phenyl, R.sup.1 is methyl and R.sup.2 is hydrogen.

    摘要翻译： PCT No.PCT / US93 / 09168 Sec。 371日期1995年04月20日 102（e）1995年4月20日PCT PCT 1993年9月30日PCT公布。 公开号WO94 / 08997 日期1994年4月28日可用于治疗炎症性疾病，中枢神经系统疾病和式I的其它病症及其药学上可接受的盐的化合物，其中Ar1和Ar2各自独立地为芳基或取代的芳基; R1是具有1至6个碳原子的烷基; R2是氢或具有1至6个碳原子的烷基; X和Y分开取代，它们各自独立地为氢，具有2-碳原子的二烷基磷酰基，具有1-6个碳原子的烷基，具有2-6个碳原子的链烯基或具有2-6个碳原子的炔基 ; 或X和Y一起并且它们表示具有3,4或5个碳原子的烃链，任选地含有至多2个双键并且任选地具有1或2个选自氧代，羟基和具有1至6个碳原子的烷基的取代基 原子 或当X为乙基时，Y为甲氧基; 条件是当X和Y一起取代时，它们连接到相邻的碳原子上; 并且条件是如果X或Y是氢，则另一个必须是烯基或炔基; 并且条件是当Y为甲氧基且X为乙基时，则Y为4-位，X为5-位，Ar1或Ar2各自为苯基，R1为甲基，R2为氢。

    Substituted 3-aminoquinuclidines
    4.
    发明授权
    Substituted 3-aminoquinuclidines 失效
    取代的3-氨基亚奎宁

    公开(公告)号：US5716965A

    公开(公告)日：1998-02-10

    申请号：US175353

    申请日：1993-12-20

    申请人： Fumitaka Ito ,  Toshihide Kokura ,  Masami Nakane ,  Kunio Satake ,  Hiroaki Wakabayashi

    发明人： Fumitaka Ito ,  Toshihide Kokura ,  Masami Nakane ,  Kunio Satake ,  Hiroaki Wakabayashi

    IPC分类号： C07D453/02 ,  A61K31/445

    CPC分类号： C07D453/02

    摘要： Compounds of the formula ##STR1## wherein W, Ar.sup.1, Ar.sup.2 and Ar.sup.3 are defined as below; and the pharmaceutically acceptable salts of such compounds. These compounds are substance P antagonists and useful in the treatment of gastrointestinal disorders, inflammatory disorders, central nervous system disorders and pain.

    摘要翻译： PCT No.PCT / US92 / 04002 Sec。 371日期：1993年12月20日 102（e）1993年12月20日日期PCT提交1992年5月19日PCT公布。 出版物WO92 / 20676 日期：1992年11月26日其中W，Ar 1，Ar 2和Ar 3如下定义的式（Ⅰ）化合物： 和这些化合物的药学上可接受的盐。 这些化合物是物质P拮抗剂，可用于治疗胃肠道疾病，炎性疾病，中枢神经系统疾病和疼痛。

    Substituted quinuclidines as substance P antagonists
    6.
    发明授权
    Substituted quinuclidines as substance P antagonists 失效
    取代的奎宁化合物作为P物质拮抗剂

    公开(公告)号：US5837711A

    公开(公告)日：1998-11-17

    申请号：US428240

    申请日：1995-04-28

    申请人： Fumitaka Ito ,  Toshihide Kokura ,  Masami Nakane ,  Kunio Satake ,  Hiroaki Wakabayashi

    发明人： Fumitaka Ito ,  Toshihide Kokura ,  Masami Nakane ,  Kunio Satake ,  Hiroaki Wakabayashi

    IPC分类号： C07D453/02 ,  A61K31/44

    CPC分类号： C07D453/02

    摘要： Certain novel substituted quinuclidine compounds having the ability to antagonize substance P and having the following formula: ##STR1## wherein Ar.sup.1 and Ar.sup.2 are each, independently, thienyl, phenyl, fluorophenyl, chlorophenyl or bromophenyl; X is --CONR.sup.3 R.sup.4, --CO.sub.2 R.sup.3, --CH.sub.2 OR.sup.3, --CH.sub.2 NR.sup.3 R.sup.4 or --CONR.sup.3 OR.sup.4 ; R.sup.1, R.sup.3 and R.sup.4 are each, independently, hydrogen or alkyl having 1 to 4 carbon atoms; R.sup.2 is alkyl having 1 to 4 carbon atoms; Y is alkylsulfonyl having 1 to 4 carbon atoms, N-alkyl-N-alkanoylamino (which may be substituted by halogen in the alkanoyl moiety) having 1 to 4 carbon atoms in the alkyl and the alkanoyl moieties, N-alkyl-N-alkylsulfonylamino (which may be substituted by halogen in the alkylsulfonyl moiety) having 1 to 4 carbon atoms in the alkyl and the alkyl sulfonyl moieties, alkenyl having 2 to 4 carbon atoms, alkynyl having 2 to 4 carbon atoms, halosubstituted alkyl having 1 to 4 carbon atoms, alkylamino having 1 to 4 carbon atoms, alkanoylamino (which may be substituted by halogen) having 1 to 4 carbon atoms or alkylsulfonylamino (which may be substituted by halogen) having 1 to 4 carbon atoms. These compounds are useful in the treatment gastrointestinal or central nervous system disorders and the alleviation of inflammatory diseases, asthma, pain and migraine in mammals and as the active ingredient in pharmaceutical compositions for treating such conditions.

    摘要翻译： PCT No.PCT / US93 / 09169 Sec。 371日期：1995年4月28日 102（e）日期1995年4月28日PCT 1993年9月30日PCT公布。 出版物WO94 / 10170 日期：1994年5月11日具有拮抗物质P并具有下式的新颖取代的奎宁环化合物：其中Ar 1和Ar 2各自独立地为噻吩基，苯基，氟苯基，氯苯基或溴苯基; X是-CONR 3 R 4，-CO 2 R 3，-CH 2 OR 3，-CH 2 NR 3 R 4或-CONR 3 OR 4; R 1，R 3和R 4各自独立地为氢或具有1至4个碳原子的烷基; R2是具有1至4个碳原子的烷基; Y是具有1至4个碳原子的烷基磺酰基，在烷基和烷酰基部分中具有1至4个碳原子的N-烷基-N-烷酰基氨基（其可被烷酰基部分中被卤素取代）为N-烷基-N-烷基磺酰基氨基 （其可以被烷基磺酰基部分中的卤素取代）在烷基和烷基磺酰基部分中具有1至4个碳原子，具有2至4个碳原子的烯基，具有2至4个碳原子的炔基，具有1至4个碳原子的卤代烷基 原子，具有1至4个碳原子的烷基氨基，具有1至4个碳原子的烷酰基氨基（其可以被卤素取代）或具有1至4个碳原子的烷基磺酰基氨基（可被卤素取代）。 这些化合物可用于治疗哺乳动物的胃肠道或中枢神经系统疾病和减轻炎性疾病，哮喘，疼痛和偏头痛，并用作用于治疗这些病症的药物组合物中的活性成分。

    Process for preparing 1,4-dihydropyridine compounds
    7.
    发明授权
    Process for preparing 1,4-dihydropyridine compounds 失效
    制备1,4-二氢吡啶化合物的方法

    公开(公告)号：US06649767B2

    公开(公告)日：2003-11-18

    申请号：US10224928

    申请日：2002-08-20

    申请人： Kunio Satake ,  Noriaki Murase

    发明人： Kunio Satake ,  Noriaki Murase

    IPC分类号： C07D21302

    CPC分类号： C07D417/06

    摘要： A process for preparing a 1,4-dihydropyridine compound comprising contacting an enamine compound and a compound having a structure of in the presence of a base; and treating the reaction mixture thus obtained in the presence of an acid or a combination of acids under mild reaction conditions. A resulting 1,4-dihydropyridine compound is useful as an anti-inflammatory agent or the like.

    摘要翻译： 一种制备1,4-二氢吡啶化合物的方法，包括使烯胺化合物和具有在碱存在下的结构的化合物接触; 并在温和的反应条件下，在酸或酸的组合存在下处理由此得到的反应混合物。 得到的1,4-二氢吡啶化合物可用作抗炎剂等。

    Substituted benzylaminopiperidine compounds
    8.
    发明授权
    Substituted benzylaminopiperidine compounds 失效
    取代的苄基氨基哌啶化合物

    公开(公告)号：US06506775B1

    公开(公告)日：2003-01-14

    申请号：US09564398

    申请日：2000-05-01

    申请人： Kunio Satake ,  Yuji Shishido ,  Hiroaki Wakabayashi

    发明人： Kunio Satake ,  Yuji Shishido ,  Hiroaki Wakabayashi

    IPC分类号： C07D21156

    CPC分类号： C07D211/56

    摘要： The invention provides a compound of formula (I): and its pharmaceutically acceptable salts, wherein R is halo C2-C8 alkenyl or halo C2-C8 alkynyl; R1 is hydrogen, halo or C1-C6 alkoxy; or R and R1, together with the two carbon atoms to which they are attached, form a C4-C6 cycloalkyl or a C4-C6 oxacycloalkyl ring wherein said ring may be optionally substituted by one or more substituents selected from the group consisting of halo, C1-C6 alkyl and halo C1-C6 alkyl; X is C1-C6 alkoxy, halo C1-C6 alkoxy, phenoxy or halo; and Ar is phenyl optionally substituted by halo. These compounds are useful in the treatment of a gastrointestinal disorder; a central nervous system (CNS) disorder; an inflammatory disease; emesis; urinary incontinence; pain; migraine; sunburn; diseases, disorders and adverse conditions caused by Heliobacter pylori; or angiogenesis especially CNS disorders in a mammalian subject, especially humans.

    摘要翻译： 本发明提供式（I）化合物及其药学上可接受的盐，其中R为卤代C 2 -C 8烯基或卤代C 2 -C 8炔基; R 1为氢，卤素或C 1 -C 6烷氧基;或R和R 1与 它们连接的两个碳原子形成C 4 -C 6环烷基或C 4 -C 6氧杂环烷基环，其中所述环可任选地被一个或多个选自卤素，C 1 -C 6烷基和卤代C 1 -C 6烷基的取代基取代， C6烷基; X是C1-C6烷氧基，卤代C1-C6烷氧基，苯氧基或卤代; 并且Ar是任选被卤素取代的苯基。这些化合物可用于治疗胃肠道疾病; 中枢神经系统（CNS）障碍; 炎性疾病; 呕吐 尿失禁 疼痛; 偏头痛 晒斑; 由幽门螺杆菌引起的疾病，病症和不良状况; 或血管发生，尤其是哺乳动物受试者尤其是人类的CNS疾病。

    5-substituted picolinic acid compounds and their method of use
    9.
    发明授权
    5-substituted picolinic acid compounds and their method of use 失效
    5-取代吡啶甲酸化合物及其使用方法

    公开(公告)号：US06194442B1

    公开(公告)日：2001-02-27

    申请号：US09460483

    申请日：1999-12-14

    申请人： Hideo Hirai ,  Katsuomi Ichikawa ,  Nakao Kojima ,  Hiroyuki Nishida ,  Kunio Satake ,  Nobuji Yoshikawa

    发明人： Hideo Hirai ,  Katsuomi Ichikawa ,  Nakao Kojima ,  Hiroyuki Nishida ,  Kunio Satake ,  Nobuji Yoshikawa

    IPC分类号： A61K3144

    CPC分类号： A61K31/44 ,  Y02A50/411

    摘要： The present invention provides novel 5-substituted picolinic acid compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 and R2 are independently H, C2-C6 acyl or halo-substituted benzoyl; and R3 is —C(O)O—C1-C6 alkyl, C(O)OH, CN, CONH2, CONHCH3, CON(CH3)2, 1-methyltetrazole or 2-methyltetrazole, with the proviso that when R2 is acetyl and R3 is methoxycarbonyl, R1 is not H; and that when R3 is CN, CONH2, CONHCH3, CON(CH3)2, 1-methyltetrazole or 2-methyltetrazole, R1 and R2 are H. The present invention also relates to a pharmaceutical composition comprising compound of the present invention, which is useful in the treatment of IL-1 and TNF mediated diseases or the like. The present invention further relates to a process for producing the compounds of the formula (I).

    摘要翻译： 本发明提供式（I）的新的5-取代的吡啶甲酸化合物或其药学上可接受的盐：其中R 1和R 2独立地为H，C 2 -C 6酰基或卤素取代的苯甲酰基; 并且R 3是-C（O）O-C 1 -C 6烷基，C（O）OH，CN，CONH 2，CONHCH 3，CON（CH 3）2,1-甲基四唑或2-甲基四唑，条件是当R 2是乙酰基和 R3是甲氧基羰基，R1不是H; 当R3为CN，CONH2，CONHCH3，CON（CH3）2,1-甲基四唑或2-甲基四唑时，R 1和R 2为H.本发明还涉及含有本发明化合物的药物组合物，其有用 在治疗IL-1和TNF介导的疾病等中。本发明还涉及制备式（I）化合物的方法。