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11. 发明授权

US3976721A Method of producing polystyrene composition 失效
标题翻译：生产聚苯乙烯组合物的方法
公开(公告)号：US3976721A
公开(公告)日：1976-08-24
申请号：US583265
申请日：1975-06-03
申请人： Kunio Satake , Tsuyoshi Yamada , Kuniaki Sakamoto , Kiyoshi Hayakawa , Isaburo Fukawa
发明人： Kunio Satake , Tsuyoshi Yamada , Kuniaki Sakamoto , Kiyoshi Hayakawa , Isaburo Fukawa
IPC分类号： C08F279/00 , C08F279/02 , C08L9/06
CPC分类号： C08F279/02
摘要： A novel high-impact polystyrene composition superior to conventional high-impact polystyrene composition, in low temperature high-impact properties, tensile strength, processability, toughness, stiffness, etc. can be obtained by a radical polymerization of a mixture of (1) 2-20% by weight of a random copolymer having a composition of continuously and gradually reduced styrene content along the polymer chain of the copolymer which is obtained by the solution polymerization of butadiene and styrene in the presence of a lithium base catalyst and (2) 80-98% by weight of styrene, carried out in bulk polymerization manner or in a manner in which bulk and suspension polymerizations are used in series.
摘要翻译：通过（1）2（1）的混合物的自由基聚合，可获得优于常规高抗冲聚苯乙烯组合物，低温高冲击性能，拉伸强度，加工性，韧性，刚度等的新型高抗冲聚苯乙烯组合物 -20重量％的无规共聚物，其具有沿着共聚物的聚合物链连续且逐渐降低的苯乙烯含量的组合物，其通过在锂碱催化剂的存在下通过丁二烯和苯乙烯的溶液聚合获得，和（2）80 -98重量％的苯乙烯，以本体聚合的方式进行，或以串联使用本体和悬浮聚合的方式进行。

12. 发明授权

US5741797A Heteroatom substituted alkyl benzylaminoquinuclidines 失效
标题翻译：杂原子取代的烷基苄基氨基奎宁
公开(公告)号：US5741797A
公开(公告)日：1998-04-21
申请号：US556916
申请日：1995-11-20
申请人： Kunio Satake
发明人： Kunio Satake
IPC分类号： A61K31/435 , A61P1/00 , A61P11/00 , A61P25/00 , A61P25/04 , A61P25/06 , A61P29/00 , C07D453/02 , C07D403/02
CPC分类号： C07D453/02
摘要： Compounds useful in the treatment of inflammatory disorders, central nervous system disorders and other disorders of the formula I and the pharmaceutically-acceptable salts thereof; ##STR1## wherein R is C.sub.1 -C.sub.6 alkyl; X is C.sub.1 -C.sub.6 alkyl having one or more substituents which include at least one heteroatom; Ar.sup.1 and Ar.sup.2 are each, independently, aryl optionally substituted by one C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, halogen, cyano, nitro, phenoxy, mono C.sub.1 -C.sub.6 alkylamino, di C.sub.1 -C.sub.6 alkylamino, halosubstituted C.sub.1 -C.sub.6 alkyl, or halosubstituted C.sub.1 -C.sub.6 alkoxy; Y is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, Z--(CH.sub.2).sub.p --, or W--(CH.sub.2).sub.m --CHR.sup.2 --(CH.sub.2).sub.n --NR.sup.1 CO-- wherein Y is at the 4-, 5- or 6-position on the quinuclidine ring; R.sup.1 is hydrogen, C.sub.1 -C.sub.6 alkyl, benzyl or --(CH.sub.2).sub.r --W; R.sup.2 is hydrogen or C.sub.1 -C.sub.6 alkyl which may be substituted by one hydroxy, amino, methylthio, methylmercapto, benzyl, 4-hydroxybenzyl, 3-indolylmethyl or --(CH.sub.2).sub.r --W; R.sup.1 may form a ring with R.sup.2 ; Z is C.sub.1 -C.sub.6 alkoxy, --CONR.sup.4 R.sup.5, --CO.sub.2 R.sup.4, --CHR.sup.4 OR.sup.5, --CHR.sup.4 NR.sup.5 R.sup.6, --COR.sup.4, --CONR.sup.4 OR.sup.5 or optionally substituted aryl; each W is independently cyano, hydroxymethyl, C.sub.2 -C.sub.6 alkoxymethyl, aminomethyl, mono C.sub.1 -C.sub.6 alkylaminomethyl, di C.sub.1 -C.sub.6 alkylaminomethyl, carboxyl, carbamoyl or C.sub.1 -C.sub.6 alkoxycarbonyl; R.sup.4, R.sup.5 and R.sup.6 are independently hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.3 -C.sub.8 cycloalkyl or an optionally substituted aryl or heterocyclic group; p is 0 to 6; and m, n and r are each, independently, 0 to 3.
摘要翻译： PCT No.PCT / JP94 / 00781 Sec。 371日期：1995年11月20日 102（e）1995年11月20日日期PCT 1994年5月13日PCT PCT。第WO94 / 26740号公报日期1994年11月24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; （I）其中R是C1-C6烷基; X是具有一个或多个包含至少一个杂原子的取代基的C 1 -C 6烷基; Ar 1和Ar 2各自独立地为任选地被一个C 1 -C 6烷基，C 1 -C 6烷氧基，C 1 -C 6烷硫基，卤素，氰基，硝基，苯氧基，单C 1 -C 6烷基氨基，二C 1 -C 6烷基氨基，卤代C1 -C 1-6烷基或卤素取代的C 1 -C 6烷氧基; Y是氢，C 1 -C 6烷基，C 2 -C 6烯基，C 3 -C 8环烷基，Z-（CH 2）p - 或W-（CH 2）m -CHR 2 - （CH 2）n -NR 1 CO- - 在奎宁环上的5-或6-位; R1是氢，C1-C6烷基，苄基或 - （CH2）r-W; R2是氢或可被一个羟基，氨基，甲硫基，甲基巯基，苄基，4-羟基苄基，3-吲哚基甲基或 - （CH 2）r-W取代的C 1 -C 6烷基; R1可以与R2形成环; Z是C1-C6烷氧基，-CONR4R5，-CO2R4，-CHR4OR5，-CHR4NR5R6，-COR4，-CONR4OR5或任选取代的芳基; 每个W独立地是氰基，羟甲基，C2-C6烷氧基甲基，氨基甲基，单C1-C6烷基氨基甲基，二C1-C6烷基氨基甲基，羧基，氨基甲酰基或C1-C6烷氧基羰基; R 4，R 5和R 6独立地是氢，C 1 -C 6烷基，C 1 -C 6烷氧基，C 3 -C 8环烷基或任选取代的芳基或杂环基; p为0〜6; m，n和r各自独立地为0〜3。

13. 发明授权

US5716965A Substituted 3-aminoquinuclidines 失效
标题翻译：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。

14. 发明授权

US5604241A Substituted benzylaminoquinuclidines as substance P antagonists 失效
标题翻译：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。

15. 发明授权

US5569662A Quinuclidine derivatives as substance P antagonists 失效
标题翻译：奎宁环衍生物作为物质P拮抗剂
公开(公告)号：US5569662A
公开(公告)日：1996-10-29
申请号：US313289
申请日：1994-10-03
申请人： Kunio Satake , Hiroaki Wakabayashi , Masami Nakane
发明人： Kunio Satake , Hiroaki Wakabayashi , Masami Nakane
IPC分类号： C07D453/02 , A61K31/445
CPC分类号： C07D453/02
摘要： Compounds useful in the treatment of inflammatory disorders, central nervous system disorders and other disorders of formula (I) and the pharmaceutically-acceptable salts thereof, wherein X.sup.1 is alkoxy or halosubstituted alkoxy; X.sup.2 is hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, halosubstitued alkyl, halosubstituted alkoxy, alkylamino, dialkylamino, alkylsulfonylamino (which may be substituted), N-alkyl-N-alkylsulfonylamino (which may be substituted), alkanoylamino (which may be substituted) or N-alkyl-N-alkanoylamino (which may be substituted); Ar.sup.1 and Ar.sup.2 are each, independently, thienyl, phenyl, fluorophenyl, chlorophenyl or bromophenyl; A is Y--(CH.sub.2).sub.m --CH(R.sup.2)--(CH.sub.2).sub.n --NR.sup.1 --; R.sup.1 is hydrogen, alkyl, benzyl or --(CH.sub.2).sub.p --Y; R.sup.2 is hydrogen, alkyl (which may be substituted), benzyl, 4-hydroxybenzyl, 3-indolylmethyl or --(CH.sub.2).sub.p --Y; Y is --CN, --CH.sub.2 Z or --COZ; Z is hydroxy, amino, alkoxy, alkylamino or dialkylamino; m, n and p are each, independently, 0, 1, 2 or 3; and R.sup.1 and R.sup.2 may be connected to form a ring.
摘要翻译： PCT No.PCT / US93 / 01810 Sec。 371日期：1994年10月3日 102（e）日期1994年10月3日PCT 1993年3月5日PCT公布。 WO93 / 19064 PCT公开号日期1993年9月30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X1是烷氧基或卤代取代的烷氧基; X 2是氢，卤素，烷基，烯基，炔基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，卤素取代的烷基，卤代烷氧基，烷基氨基，二烷基氨基，烷基磺酰基氨基（其可被取代的），N-烷基-N-烷基磺酰基氨基），烷酰基氨基（其可以被取代）或N-烷基-N-烷酰基氨基（其可以被取代）; Ar1和Ar2各自独立地为噻吩基，苯基，氟苯基，氯苯基或溴苯基; A是Y-（CH 2）m -CH（R 2） - （CH 2）n -NR 1; R1是氢，烷基，苄基或 - （CH2）p-Y; R 2是氢，烷基（其可以被取代），苄基，4-羟基苄基，3-吲哚基甲基或 - （CH 2）p-Y; Y是-CN，-CH2Z或-COZ; Z是羟基，氨基，烷氧基，烷基氨基或二烷基氨基; m，n和p各自独立地为0,1,2或3; 并且R1和R2可以连接形成环。

16. 发明授权

US4423190A Block copolymer mixture of conjugated diene and vinyl aromatic hydrocarbon 失效
标题翻译：共轭二烯和乙烯基芳烃的嵌段共聚物混合物
公开(公告)号：US4423190A
公开(公告)日：1983-12-27
申请号：US333656
申请日：1981-12-23
申请人： Isaburo Fukawa , Kunio Satake , Tsuyoshi Yamada , Kiyoshi Hayakawa , Yasushi Sato
发明人： Isaburo Fukawa , Kunio Satake , Tsuyoshi Yamada , Kiyoshi Hayakawa , Yasushi Sato
IPC分类号： C08F297/04
CPC分类号： C08F297/044
摘要： A novel block copolymer mixture of conjugated diene (C.D.) and vinylaromatic hydrocarbon (V.H.) having a superior transparency and impact-resistance is produced by the following two step polymerizations using an organolithium compound as a catalyst and a solvent consisting mainly of an aliphatic hydrocarbon: a first step (A) of preparing a living (co)polymer of C.D. or C.D. and V.H., by polymerizing the monomer(s) in a ratio by weight of V. H. to C.D. of 0/100 to 60/40 and in an amount of 1 to 80% by weight of total monomers to be used, in the presence of said catalyst and solvent, and a second step (B) of preparing V.H. polymer or block copolymer of V.H. and C.D., by adding to said living (co)polymer, remaining monomer(s), in a ratio by weight of V.H. to C.D. of 100/0 to 65/35 and in an amount of 99 to 20% by weight of total monomers to be used, and said catalyst and solvent, and polymerizing the remaining monomer(s) to obtain a block copolymer mixture, this block copolymer mixture having a ratio of V.H. content of ultimate block copolymers to that of the (co)polymers obtained only in step (B), of at least 1/1.8, and a ratio of V.H. portion to C.D. portion of 60/40 to 95/5.
摘要翻译：通过使用有机锂化合物作为催化剂和主要由脂肪族烃组成的溶剂进行以下两步聚合，制备具有优异的透明性和耐冲击性的共轭二烯（CD）和乙烯基芳烃（VH）的新型嵌段共聚物混合物：制备CD的活性（共）聚合物的第一步骤（A）或C.D. 和V.H.通过以V H.与C.D.重量比的比例聚合单体。在所述催化剂和溶剂的存在下，使用的总单体重量为0/100至60/40且为1至80重量％，以及制备VH聚合物或嵌段共聚物的第二步骤（B） VH和CD，通过以VH与CD的重量比加入所述活性（共）聚合物，剩余单体为100/0至65/35，并且使用的总单体的重量为99至20重量％，所述催化剂和溶剂，并使剩余的单体聚合以获得嵌段共聚物混合物，该嵌段共聚物最终嵌段共聚物的VH含量与仅在步骤（B）中获得的（共）聚合物的VH含量的比率为至少1 / 1.8，VH部分与CD的比例部分为60/40至95/5。

17. 发明授权

US4208356A Process for producing mixture of block copolymers 失效
标题翻译：制备嵌段共聚物混合物的方法
公开(公告)号：US4208356A
公开(公告)日：1980-06-17
申请号：US609684
申请日：1975-09-02
申请人： Isaburo Fukawa , Kunio Satake , Tsuyoshi Yamada , Kiyoshi Hayakawa , Yasushi Sato
发明人： Isaburo Fukawa , Kunio Satake , Tsuyoshi Yamada , Kiyoshi Hayakawa , Yasushi Sato
IPC分类号： C08F297/04
CPC分类号： C08F297/044
摘要： A novel block copolymer mixture of conjugated diene (C.D.) and vinylaromatic hydrocarbon (V.H.) having a superior transparency and impact-resistance is produced by the following two step polymerizations using an organolithium compound as a catalyst and a solvent consisting mainly of an aliphatic hydrocarbon:a first step (A) of preparing a living (co)polymer of C.D. or C.D. and V.H., by polymerizing the monomer(s) in a ratio by weight of V.H. to C.D. of 0/100 to 60/40 and in an amount of 1 to 80% by weight of total monomers to be used, in the presence of said catalyst and solvent, anda second step (B) of preparing V.H. polymer or block copolymer of V.H. and C.D., by adding to said living (co)polymer, remaining monomer(s), in a ratio by weight of V.H. to C.D. of 100/0 to 65/35 and in an amount of 99 to 20% by weight of total monomers to be used, and said catalyst and solvent, and polymerizing the remaining monomer(s) to obtain a block copolymer mixture,this block copolymer mixture having a ratio of V.H. content of ultimate block copolymers to that of the (co)polymers obtained only in step (B), of at least 1/1.8, and a ratio of V.H. portion to C.D. portion of 60/40 to 95/5.
摘要翻译：通过使用有机锂化合物作为催化剂和主要由脂肪族烃组成的溶剂进行以下两步聚合，制备具有优异的透明性和耐冲击性的共轭二烯（CD）和乙烯基芳烃（VH）的新型嵌段共聚物混合物：制备CD的活性（共）聚合物的第一步（A）或C.D. 和V.H.通过以V.H.至C.D.的重量比将聚合单体进行聚合。在所述催化剂和溶剂的存在下，使用的总单体重量为0/100至60/40且为1至80重量％，以及制备VH聚合物或嵌段共聚物的第二步骤（B） VH和CD，通过以VH与CD的重量比加入所述活性（共）聚合物，剩余单体为100/0至65/35，并且使用的总单体的重量为99至20重量％，所述催化剂和溶剂，并使剩余的单体聚合以获得嵌段共聚物混合物，该嵌段共聚物最终嵌段共聚物的VH含量与仅在步骤（B）中获得的（共）聚合物的VH含量的比率为至少1 / 1.8，VH部分与CD的比例部分为60/40至95/5。

18. 发明授权

US06416979B1 5-substituted picolinic acid compounds production by Marasmiellus sp 失效
标题翻译：由马拉斯马司属（Malasmiellus sp。）生产的5-取代吡啶甲酸化合物
公开(公告)号：US06416979B1
公开(公告)日：2002-07-09
申请号：US09657730
申请日：2000-09-08
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： C12P1712
CPC分类号： A61K31/44
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。

19. 发明授权

US06329396B1 Substituted benzylaminopiperidine compounds 失效
标题翻译：取代的苄基氨基哌啶化合物
公开(公告)号：US06329396B1
公开(公告)日：2001-12-11
申请号：US09562144
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 substituted benzylaminopiperidine compounds that are useful in the treatment of gastrointestinal disorders; central nervous system (CNS) disorders; 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 in humans.
摘要翻译：本发明提供了可用于治疗胃肠道疾病的取代的苄基氨基哌啶化合物; 中枢神经系统（CNS）疾病; 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; 或血管生成，特别是在哺乳动物受试者，特别是人类中的CNS紊乱。

20. 发明授权

US6034107A 5-Substituted picolinic acid compounds and their production process 失效
标题翻译： 5-取代的吡啶甲酸化合物及其制备方法
公开(公告)号：US6034107A
公开(公告)日：2000-03-07
申请号：US178949
申请日：1998-10-26
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： C07D213/78 , A61K31/00 , A61K31/44 , A61K31/4427 , A61K31/4439 , A61P11/00 , A61P19/00 , A61P19/02 , A61P29/00 , A61P43/00 , C07D213/79 , C07D213/81 , C07D213/84 , C07D401/04 , C12N1/14 , C12P17/12 , C12P17/16 , C12R1/645
CPC分类号： C07D213/79 , C07D213/81 , C07D213/84 , C07D401/04 , C12P17/12
摘要： The present invention provides novel 5-substituted picolinic acid compounds of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sup.1 and R.sup.2 are independently H, C.sub.2 -C.sub.6 acyl or halo-substituted benzoyl; and R.sup.3 is --C(O)O--C.sub.1 -C.sub.6 alkyl, C(O)OH, CN, CONH.sub.2, CONHCH.sub.3, CON(CH.sub.3).sub.2, 1-methyltetrazole or 2-methyltetrazole, with the proviso that when R.sub.2 is acetyl and R.sup.3 is methoxycarbonyl, R.sup.1 is not H; and that when R.sup.3 is CN, CONH.sub.2, CONHCH.sub.3, CON(CH.sub.3).sub.2, 1-methyltetrazole or 2-methyltetrazole, R.sup.1 and R.sup.2 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R 3为CN时，CONH 2，CONHCH 3，CON（CH 3）2，1-甲基四唑或2-甲基四唑，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，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。

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