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公开(公告)号:US06432957B1
公开(公告)日:2002-08-13
申请号:US09893681
申请日:2001-06-29
申请人: Tatsuhiko Kodoma , Masahiro Tamura , Toshiaki Oda , Yukiyoshi Yamazaki , Masahiro Nishikawa , Takeshi Doi , Yoshinori Kyotani
发明人: Tatsuhiko Kodoma , Masahiro Tamura , Toshiaki Oda , Yukiyoshi Yamazaki , Masahiro Nishikawa , Takeshi Doi , Yoshinori Kyotani
IPC分类号: A61K31496
CPC分类号: C07D401/14 , A61K31/496 , C07D213/74
摘要: A piperazine compound represented by formula (1): wherein X is —CH2—, —C(O)— or —CH(CH3)—; R1 is a hydrogen atom or alkyl group; and R2 is a hydrogen atom, alkyl group, hydroxyalkyl group, arylalkyl group, heteroarylalkyl group, carboxyalkyl group, carboxamidoalkyl group, aminoalkyl group or guanidinoalkyl group; an acid-addition salt thereof, or a hydrate thereof. The compound has excellent inhibitory effects on both cell adhesion and cell infiltration and is useful for prevention or treatment of diseases such as allergy, asthma, rheumatism, arteriosclerosis and inflammation.
摘要翻译: 由式(1)表示的哌嗪化合物:其中X是-CH 2 - , - C(O) - 或-CH(CH 3) - ; R1是氢原子或烷基; R2是氢原子,烷基,羟基烷基,芳基烷基,杂芳基烷基,羧基烷基,甲酰胺基烷基,氨基烷基或胍基烷基; 其酸加成盐或其水合物。 该化合物对细胞粘附和细胞浸润具有优异的抑制作用,可用于预防或治疗过敏,哮喘,风湿病,动脉硬化和炎症等疾病。
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公开(公告)号:US06509329B1
公开(公告)日:2003-01-21
申请号:US09893697
申请日:2001-06-29
申请人: Tatsuhiko Kodama , Masahiro Tamura , Toshiaki Oda , Yukiyoshi Yamazaki , Masahiro Nishikawa , Takeshi Doi , Yoshinori Kyotani
发明人: Tatsuhiko Kodama , Masahiro Tamura , Toshiaki Oda , Yukiyoshi Yamazaki , Masahiro Nishikawa , Takeshi Doi , Yoshinori Kyotani
IPC分类号: C07D25112
CPC分类号: C07D295/096 , A61K31/495 , A61K31/496 , A61K31/506 , A61K31/551 , C07D213/38
摘要: A cyclic diamine compound of formula (1): wherein A is a single bond or C≡C; X and Y are individually CH or a nitrogen atom; m is 1 or 2; and n is a number of 1 to 5; an acid-addition salt thereof, or a hydrate thereof. The compound has excellent inhibitory effects on both cell adhesion and cell infiltration and is useful as a medicine for prevention or treatment of diseases such as allergy, asthma, rheumatism, arteriosclerosis and inflammation.
摘要翻译: 式(1)的环状二胺化合物:其中A是单键或C = C; X和Y分别是CH或氮原子; m为1或2; n为1〜5的数; 其酸加成盐或其水合物。 该化合物对细胞粘附和细胞浸润具有优异的抑制作用,可用作预防或治疗诸如过敏,哮喘,风湿病,动脉硬化和炎症等疾病的药物。
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公开(公告)号:US06552188B2
公开(公告)日:2003-04-22
申请号:US09893699
申请日:2001-06-29
申请人: Tatsuhiko Kodama , Masahiro Tamura , Toshiaki Oda , Yukiyoshi Yamazaki , Masahiro Nishikawa , Shunji Takemura , Takeshi Doi , Yoshinori Kyotani
发明人: Tatsuhiko Kodama , Masahiro Tamura , Toshiaki Oda , Yukiyoshi Yamazaki , Masahiro Nishikawa , Shunji Takemura , Takeshi Doi , Yoshinori Kyotani
IPC分类号: A61K31496
CPC分类号: C07D213/81 , C07D213/36 , C07D213/82 , C07D401/12
摘要: Cyclic diamine compounds of formula (1) are disclosed: wherein A is (CH2)n, (CH2)n—CH═CH, CO—(CH2)n or CO—(CH2)n—CH═CH, in which n is a number of 0 to 3; Z represents a formula (2) or (3): in which R1, R2, R4, R5 and R6 are individually a hydrogen atom, alkyl group, alkoxy group, halogen atom or nitro group; R3is a hydrogen atom, alkyl group, alkoxy group, halogen atom, nitro group, naphthyl group, or phenyl group which may be substituted by 1 to 3 substituents selected from the group consisting of alkyl groups, alkoxy groups, halogen atoms, a nitro group and a phenyl group; and X and Y are individually CH or a nitrogen atom; and m is 1 or 2; an acid-addition salt thereof, or a hydrate thereof, and a medicine containing such a compound.
摘要翻译: 公开了式(1)的环二胺化合物:其中A是(CH 2)n,(CH 2)n -CH = CH,CO-(CH 2)n或CO-(CH 2)n -CH = CH,其中n是 数字0到3; Z表示式(2)或(3):其中R1,R2,R4,R5和R6分别为氢原子,烷基,烷氧基,卤素原子或硝基; R3是氢原子,烷基,烷氧基,卤素原子,硝基,萘基或可以被1〜3个选自烷基,烷氧基,卤原子,硝基的取代基取代的苯基 和苯基; X和Y分别是CH或氮原子; m为1或2;其酸加成盐或其水合物,以及含有这种化合物的药物。
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4.
公开(公告)号:US06498169B1
公开(公告)日:2002-12-24
申请号:US09983928
申请日:2001-10-26
申请人: Tatsuhiko Kodama , Masahiro Tamura , Toshiaki Oda , Yukiyoshi Yamazaki , Masahiro Nishikawa , Shunji Takemura , Takeshi Doi , Yoshinori Kyotani , Masao Ohkuchi
发明人: Tatsuhiko Kodama , Masahiro Tamura , Toshiaki Oda , Yukiyoshi Yamazaki , Masahiro Nishikawa , Shunji Takemura , Takeshi Doi , Yoshinori Kyotani , Masao Ohkuchi
IPC分类号: A61K314545
CPC分类号: C07D401/06 , A61K31/4545 , C07D211/58 , C07D401/12 , C07D401/14 , C07D403/14
摘要: A cyclic amine compound represented by the following general formula (1): wherein, R1, R2 and R3 each independently represent a hydrogen atom or an alkoxy group; W1 an W2 each independently represent N or CH; X represents O, NR4, CONR4 or NR4CO; R4 each independently represents a hydrogen atom, or an alkyl, aryl, heteroaryl, aralkyl, or heteroalkyl group; and l, m and n each represents a number of 0 to 1, a salt thereof and a hydrate thereof are provided. These compounds have inhibitory effects on both cell adhesion and cell infiltration and are useful as anti-asthmatic agents, anti-allergic agents, anti-rheumatic agents, anti-arteriosclerotic agents, anti-inflammatory agents, anti-Sjogren's syndrome agents or the like.
摘要翻译: 由以下通式(1)表示的环胺化合物:其中,R 1,R 2和R 3各自独立地表示氢原子或烷氧基; W 1,W 2各自独立地表示N或CH; X表示O,NR 4,CONR 4或 NR4CO; R4各自独立地表示氢原子,或烷基,芳基,杂芳基,芳烷基或杂烷基; 和l,m和n各自表示0至1的数,其盐和其水合物。这些化合物对细胞粘附和细胞浸润均具有抑制作用,可用作抗哮喘剂,抗过敏剂, 抗风湿剂,抗动脉硬化剂,抗炎剂,抗干燥素综合征剂等。
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5.
公开(公告)号:US06605620B1
公开(公告)日:2003-08-12
申请号:US10107180
申请日:2002-03-28
申请人: Tatsuhiko Kodama , Masahiro Tamura , Toshiaki Oda , Yukiyoshi Yamazaki , Masahiro Nishikawa , Shunji Takemura , Takeshi Doi , Yoshinori Kyotani , Masao Ohkuchi
发明人: Tatsuhiko Kodama , Masahiro Tamura , Toshiaki Oda , Yukiyoshi Yamazaki , Masahiro Nishikawa , Shunji Takemura , Takeshi Doi , Yoshinori Kyotani , Masao Ohkuchi
IPC分类号: A61K314545
CPC分类号: C07D401/06 , C07D211/58 , C07D213/38 , C07D401/12 , C07D401/14
摘要: A cyclic amine compound by the following general formula (1): wherein, R1, R2 and R3 each independently represent a hydrogen atom or an alkoxy group W1 and W2 each independently represent N or CH; X represents O, NR4, CONR4 or NR4CO; R4 represents a hydrogen atom, or an alkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl group; and l, m and n each represents a number of 0 or 1, a salt thereof and a hydrate thereof are provided. These compounds have inhibitory effects on both cell adhesion and cell infiltration and are useful as anti-asthmatic agents, anti-allergic agents, anti-rheumatic agents, anti-arteriosclerotic agents, anti-inflammatory agents, anti-Sjogren's syndrome agents or the like.
摘要翻译: 通式(1)表示的环状胺化合物:其中,R 1,R 2和R 3各自独立地表示氢原子或烷氧基,W 1和W 2各自独立地表示N或CH; X表示O,NR 4,CONR 4或NR 4 CO; R 4 表示氢原子,或烷基,芳基,杂芳基,芳烷基或杂芳烷基; 和l,m和n各自表示0或1的数,其盐和其水合物。 这些化合物对细胞粘附和细胞浸润具有抑制作用,并且可用作抗哮喘药,抗过敏剂,抗风湿剂,抗动脉硬化剂,抗炎剂,抗干燥素综合征剂等。
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公开(公告)号:US06472386B1
公开(公告)日:2002-10-29
申请号:US09893682
申请日:2001-06-29
申请人: Tatsuhiko Kodama , Masahiro Tamura , Toshiaki Oda , Yukiyoshi Yamazaki , Masahiro Nishikawa , Takeshi Doi , Yoshinori Kyotani
发明人: Tatsuhiko Kodama , Masahiro Tamura , Toshiaki Oda , Yukiyoshi Yamazaki , Masahiro Nishikawa , Takeshi Doi , Yoshinori Kyotani
IPC分类号: A61K31551
CPC分类号: C07D231/12 , C07D233/64 , C07D261/08 , C07D263/32 , C07D277/28 , C07D277/46 , C07D333/20 , C07D401/14 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要: A compound of formula (1): wherein A is a single bond, C≡C, CONH or NHCO; W is a carbon atom or a nitrogen atom; X is CH, a nitrogen atom, an oxygen atom or a sulfur atom; Y is CH, CHR1, in which R1 is a hydrogen atom, or a lower alkyl, hydroxy lower alkyl, lower alkoxy-lower-alkyl, aryl, aryl-lower-alkyl or heteroaryl-lower-alkyl group, a nitrogen atom, an oxygen atom, a sulfur atom or NR2, in which R2 is a hydrogen atom, or a lower alkyl, hydroxy lower alkyl, lower alkoxy-lower-alkyl, aryl, aryl-lower-alkyl or heteroaryl-lower-alkyl group; Z is a nitrogen atom, an oxygen atom, a sulfur atom, CH or NR3, in which R3 is a hydrogen atom, or a lower alkyl, hydroxy lower alkyl, lower alkoxy-lower-alkyl, aryl, aryl-lower-alkyl or heteroaryl-lower-alkyl group; m is 1 or 2; and n is a number of 1 to 5, with the proviso that one or two of W, X, Y and Z are heteroatoms; an acid-addition salt thereof, or a hydrate thereof. The compounds have inhibitory effects on cell adhesion and are useful for prevention or treatment of diseases such as allergy, asthma, rheumatism, arteriosclerosis and inflammation.
摘要翻译: 式(1)的化合物:其中A是单键,C = C,CONH或NHCO; W是碳原子或氮原子; X是CH,氮原子,氧原子或硫原子; Y是CH,CHR1,其中R1是氢原子,或低级烷基,羟基低级烷基,低级烷氧基 - 低级 - 烷基,芳基,芳基 - 低级 - 烷基或杂芳基 - 低级 - 烷基,氮原子, 氧原子,硫原子或NR 2,其中R2是氢原子,或低级烷基,羟基低级烷基,低级烷氧基 - 低级 - 烷基,芳基,芳基 - 低级 - 烷基或杂芳基 - 低级 - 烷基; Z是氮原子,氧原子,硫原子,CH或NR 3,其中R3是氢原子,或低级烷基,羟基低级烷基,低级烷氧基 - 低级 - 烷基,芳基,芳基 - 低级 - 烷基或 杂芳基 - 低级烷基; m为1或2; 并且n是1至5的数,条件是W,X,Y和Z中的一个或两个是杂原子; 其酸加成盐或其水合物。 这些化合物对细胞粘附具有抑制作用,可用于预防或治疗诸如过敏,哮喘,风湿病,动脉硬化和炎症等疾病。
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7.
公开(公告)号:US06395753B1
公开(公告)日:2002-05-28
申请号:US09941684
申请日:2001-08-30
申请人: Tatsuhiko Kodama , Masahiro Tamura , Toshiaki Oda , Yukiyoshi Yamazaki , Masahiro Nishikawa , Shunji Takemura , Takeshi Doi , Yoshinori Kyotani , Masao Ohkuchi
发明人: Tatsuhiko Kodama , Masahiro Tamura , Toshiaki Oda , Yukiyoshi Yamazaki , Masahiro Nishikawa , Shunji Takemura , Takeshi Doi , Yoshinori Kyotani , Masao Ohkuchi
IPC分类号: A61K314545
CPC分类号: C07D401/06 , A61K31/4545 , C07D211/58 , C07D401/12 , C07D401/14 , C07D403/14
摘要: A cyclic amine compound represented by the following general formula (1): wherein, R1, R2 and R3 each independently represent a hydrogen atom or an alkoxy group; W1 and W2 each independently represent N or CH; X represents O, NR4, CONR4 or NR4CO; R4 each independently represents a hydrogen atom, or an alkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl group; and l, m and n each represents a number of 0 or 1, a salt thereof and a hydrate thereof are provided. These compounds have inhibitory effects on both cell adhesion and cell infiltration and are useful as anti-asthmatic agents, anti-allergic agents, anti-rheumatic agents, anti-arteriosclerotic agents, anti-inflammatory agents, anti-Sjogren's syndrome agents or the like.
摘要翻译: 由以下通式(1)表示的环胺化合物:其中,R1,R2和R3各自独立地表示氢原子或烷氧基; W1和W2各自独立地表示N或CH; X表示O,NR4,CONR4或 NR4CO; R4各自独立地表示氢原子,或烷基,芳基,杂芳基,芳烷基或杂芳烷基; 和l,m和n各自表示0或1的数,其盐和其水合物。这些化合物对细胞粘附和细胞浸润都具有抑制作用,并且可用作抗哮喘剂,抗过敏剂, 抗风湿剂,抗动脉硬化剂,抗炎剂,抗干燥素综合征剂等。
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公开(公告)号:US07135473B2
公开(公告)日:2006-11-14
申请号:US10639457
申请日:2003-08-13
申请人: Tatsuhiko Kodama , Masahiro Tamura , Toshiaki Oda , Yukiyoshi Yamazaki , Masahiro Nishikawa , Takeshi Doi , Yoshinori Kyotani
发明人: Tatsuhiko Kodama , Masahiro Tamura , Toshiaki Oda , Yukiyoshi Yamazaki , Masahiro Nishikawa , Takeshi Doi , Yoshinori Kyotani
IPC分类号: A61K31/497 , A61P37/00 , C07D239/00 , C07D401/00 , C07D403/00
CPC分类号: C07D263/56 , A61K31/4184 , A61K31/423 , A61K31/496 , A61K31/517 , A61K31/551 , C07D209/14 , C07D215/12 , C07D235/14 , C07D239/74 , C07D243/06 , C07D277/64 , C07D295/096 , C07D307/81 , C07D333/58 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要: A cyclic diamine compound of formula (1): wherein R1 and R2 are individually a hydrogen atom or a methoxy group, provided R1 is a methoxy group when R2 is a hydrogen atom, or a hydrogen atom when R2 is a methoxy group; A is an oxygen atom, a sulfur atom, CH═CH, CH═N or NR3, in which R3 is a hydrogen atom, or a lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl, aryl or aryl lower alkyl group; B is a nitrogen atom, CH or CR4, in which R4 is a hydrogen atom, or a lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl, aryl or aryl lower alkyl group; m is 1 or 2; and n is a number of 1 to 5, an acid-addition salt thereof, or a hydrate thereof. The compound has inhibitory effects on cell adhesion and is useful for treatment of allergy, asthma, rheumatism, arteriosclerosis, and inflammation.
摘要翻译: 式(1)的环状二胺化合物:其中R 1和R 2各自独立地为氢原子或甲氧基,条件是R 1, 当R 2为氢原子时为甲氧基,或当R 2为甲氧基时为氢原子; A是氧原子,硫原子,CH-CH,CH-N或NR 3,其中R 3是氢原子,或低级烷基羟基 低级烷基,低级烷氧基低级烷基,芳基或芳基低级烷基; B是氮原子,CH或CR 4,其中R 4是氢原子,或低级烷基,羟基低级烷基,低级烷氧基低级烷基,芳基或 芳基低级烷基; m为1或2; n为1〜5的数,其酸加成盐或其水合物。 该化合物对细胞粘附具有抑制作用,可用于治疗过敏,哮喘,风湿病,动脉硬化和炎症。
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9.
公开(公告)号:US06867221B2
公开(公告)日:2005-03-15
申请号:US10191534
申请日:2002-07-10
申请人: Tatsuhiko Kodama , Masahiro Tamura , Toshiaki Oda , Yukiyoshi Yamazaki , Masahiro Nishikawa , Shunji Takemura , Takeshi Doi , Yoshinori Kyotani , Masao Ohkuchi
发明人: Tatsuhiko Kodama , Masahiro Tamura , Toshiaki Oda , Yukiyoshi Yamazaki , Masahiro Nishikawa , Shunji Takemura , Takeshi Doi , Yoshinori Kyotani , Masao Ohkuchi
IPC分类号: A61K31/4545 , A61P9/10 , A61P11/06 , A61P29/00 , A61P37/08 , A61P43/00 , C07D211/58 , C07D211/62 , C07D213/38 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/14
CPC分类号: C07D401/06 , A61K31/4545 , C07D211/58 , C07D211/62 , C07D213/38 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/14
摘要: A cyclic amine compound represented by the following general formula (1): wherein, R1, R2 and R3 each independently represent a hydrogen atom or an alkoxy group; W1 and W2 each independently represent N or CH; X represents O, NR4, CONR4 or NR4CO; R4 represents a hydrogen atom, or an alkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl group; and l, m and n each represents a number of 0 or 1, a salt thereof and a hydrate thereof are provided. These compounds have inhibitory effects on both cell adhesion and cell infiltration and are useful as anti-asthmatic agents, anti-allergic agents, anti-rheumatic agents, anti-arteriosclerotic agents, anti-inflammatory agents, anti-Sjogren's syndrome agents or the like.
摘要翻译: 由以下通式(1)表示的环胺化合物:其中,R 1,R 2和R 3各自独立地表示氢原子或烷氧基; W 1和W 2均为氢原子, 各自独立地表示N或CH; X表示O,NR 4,CONR 4或NR 4 CO; R 4表示氢原子或烷基,芳基,杂芳基,芳烷基或杂芳烷基; 和l,m和n各自表示0或1的数,其盐和其水合物。这些化合物对细胞粘附和细胞浸润都具有抑制作用,并且可用作抗哮喘剂,抗过敏剂, 抗风湿剂,抗动脉硬化剂,抗炎剂,抗干燥素综合征剂等。
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公开(公告)号:US06632810B2
公开(公告)日:2003-10-14
申请号:US09893696
申请日:2001-06-29
申请人: Tatsuhiko Kodama , Masahiro Tamura , Toshiaki Oda , Yukiyoshi Yamazaki , Masahiro Nishikawa , Takeshi Doi , Yoshinori Kyotani
发明人: Tatsuhiko Kodama , Masahiro Tamura , Toshiaki Oda , Yukiyoshi Yamazaki , Masahiro Nishikawa , Takeshi Doi , Yoshinori Kyotani
IPC分类号: A61K3155
CPC分类号: C07D263/56 , A61K31/4184 , A61K31/423 , A61K31/496 , A61K31/517 , A61K31/551 , C07D209/14 , C07D215/12 , C07D235/14 , C07D239/74 , C07D243/06 , C07D277/64 , C07D295/096 , C07D307/81 , C07D333/58 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要: A cyclic diamine compound of formula (1): wherein R1 and R2 are individually a hydrogen atom or a methoxy group, provided R1 is a methoxy group when R2 is a hydrogen atom, or a hydrogen atom when R2 is a methoxy group; A is an oxygen atom, a sulfur atom, CH═CH, CH═N or NR3, in which R3 is a hydrogen atom, or a lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl, aryl or aryl lower alkyl group; B is a nitrogen atom, CH or CR4, in which R4 is a hydrogen atom, or a lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl, aryl or aryl lower alkyl group; m is 1 or 2; and n is a number of 1 to 5, an acid-addition salt thereof, or a hydrate thereof. The compound has inhibitory effects on cell adhesion and is useful for treatment of allergy, asthma, rheumatism, arteriosclerosis, and inflammation.
摘要翻译: 式(1)的环状二胺化合物:其中R
PDAT>和R 2 SP> PDAT>分别为氢原子或甲氧基,条件是R 当R <2 SP> 是氢原子时,当R <2 SP>时, <1 SP> 是甲氧基 是甲氧基; A是氧原子,硫原子,CH = CH,CH = N或NR <3 SP> ,其中R <3 SP> 原子或低级烷基,羟基低级烷基,低级烷氧基低级烷基,芳基或芳基低级烷基; B是氮原子,CH或CR <4 SP> ,其中R <4 SP> 是氢原子或低级烷基羟基低级烷基 ,低级烷氧基低级烷基,芳基或芳基低级烷基; m为1或2; n为1〜5的数,或其酸加成盐或其水合物。 该化合物对细胞粘附具有抑制作用,可用于治疗过敏,哮喘,风湿病,动脉硬化和炎症。 PTEXT>
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