-
公开(公告)号：EP1219294A1
公开(公告)日：2002-07-03
申请号：EP00961076.7
申请日：2000-09-19
发明人： KATO, Kaneyoshi , MORI, Masaaki , SUZUKI, Nobuhiro , SHIMOMURA, Yukio Takeda Yakuhin Matsushiro Res.410 , TAKEKAWA, Shiro , CHOH, Nobuo
IPC分类号： A61K31/137 , A61K31/27 , A61K31/4035 , A61K31/44 , A61K31/445 , A61K31/4453 , A61K31/472 , A61P43/00 , A61P31/04 , C07D211/14 , C07D211/18 , C07D211/46 , C07D211/58 , C07D211/70 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12
CPC分类号： C07D401/12 , A61K31/137 , A61K31/27 , A61K31/4035 , A61K31/44 , A61K31/445 , A61K31/4453 , A61K31/451 , C07C271/22 , C07D209/44 , C07D211/14 , C07D211/18 , C07D211/22 , C07D211/34 , C07D211/46 , C07D211/58 , C07D211/70 , C07D217/04 , C07D405/12 , C07D409/12 , C07D417/12
摘要： A compound represented by the formula
wherein Ar 1 and Ar 2 are each an aromatic group optionally having substituents, P and Q are each a divalent aliphatic hydrocarbon group which optionally contains ether oxygen or ether sulfur in a carbon chain and which optionally has substituents, R 1 and R 3 are each (i) a hydrogen atom, (ii) an acyl group or (iii) an hydrocarbon group optionally having substituents, R 2 and R 4 are each (i) a hydrogen atom, (ii) an alkyl group optionally having substituents or (iii) an alkylcarbonyl optionally having substituents, R 1 and R 2 or R 3 and R 4 each optionally forms, together with the adjacent nitrogen atom, a monocyclic or fused nitrogen-containing heterocyclic group optionally having substituents, j is 0 or 1, a salt thereof or a prodrug thereof are useful as melanin-concentrating hormone antagonists.摘要翻译： 由式
表示的化合物，其中Ar 1和Ar 2各自为任选具有取代基的芳族基团，P和Q各自为碳链中任选含有醚氧或醚硫的二价脂族烃基 R 1和R 3各自为（i）氢原子，（ii）酰基或（iii）任选具有取代基的烃基，R 2和R 4独立地为氢， 各自为（i）氢原子，（ii）任选具有取代基的烷基或（iii）任选具有取代基的烷基羰基，R 1和R 2或R 3和R 4各自任选地形成 与相邻的氮原子一起，任选具有取代基的单环或稠合含氮杂环基团，j为0或1，其盐或其前药可用作黑色素浓缩激素拮抗剂。 -
2.发明公开AMINE COMPOUNDS, THEIR PRODUCTION AND THEIR USE AS SOMATOSTATIN RECEPTOR ANTAGONISTS OR AGONISTS 审中-公开阿明化合物，它们的生产及其作为生长抑素受体拮抗剂或激动剂
公开(公告)号：EP1070054A1
公开(公告)日：2001-01-24
申请号：EP99945683.3
申请日：1999-04-08
IPC分类号： C07D215/12 , A61K31/47 , C07D215/14 , C07D215/18 , C07D215/20 , C07D215/42 , C07D215/58 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/06 , C07D405/06 , C07D409/10 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/14 , C07D471/10
CPC分类号： C07D401/06 , C07D215/12 , C07D215/18 , C07D215/20 , C07D215/38 , C07D215/58 , C07D241/42 , C07D401/10 , C07D401/14 , C07D403/06 , C07D405/06 , C07D409/10 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/14 , C07D471/10
摘要： The present invention provides a compound of formula (I) wherein Ar represents an aromatic group which may be substituted; X represents methylene, S, SO, SO2 or CO; Y represents a spacer having a main chain of 2 to 5 atoms; n represents an integer of 1 to 5; i) R?1 and R2¿ each represents a hydrogen atom or a lower alkyl which may be substituted, ii) R?1 and R2¿ form, taken together with the adjacent nitrogen atom, a nitrogen-containing heterocyclic ring which may be substituted, or iii) R1 or R2 together with -(CH¿2?)n-N= form, bonded to a component atom of Ring B, a spiro-ring which may be substituted; Ring A represents an aromatic Ring which may be substituted; Ring B represents a 4- to 7-membered nitrogen-containing non-aromatic ring which may be further substituted by alkyl or acyl, with a proviso that X represents S, SO, SO2 or CO when Ring A has as a substituent a group represented by the formula: -NHCOR?11¿ where R11 represents alkyl, alkoxyalkyl, alkylthioalkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl or a group represented by the formula: -NHR12 where R12 represents alkyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl, or a salt thereof; which has an excellent somatostatin receptor binding inhibition action.
-
公开(公告)号：EP1283055A1
公开(公告)日：2003-02-12
申请号：EP01919795.3
申请日：2001-04-05
IPC分类号： A61K45/00 , A61K31/4706 , A61K31/4709 , C07D215/42 , C07D215/44 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , A61P43/00 , A61P25/00 , A61P25/28 , A61P25/16
CPC分类号： C07D215/233 , A61K31/4706 , A61K31/4709 , A61K31/498 , C07D215/38 , C07D215/44 , C07D241/42 , C07D401/06 , C07D401/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D413/06
摘要： According to the present invention, there are provided compounds represented by formula (I):
[wherein R 1 and R 2 represent hydrogen atom, a lower alkyl group, etc.; ring A is an optionally substituted benzene ring, X is oxygen atom, etc.; and Y represents CH or N] or salts thereof, or prodrugs thereof, and use thereof as well as processes of manufacturing these compounds. The compounds of the present invention and the like possess a potent soluble beta amyloid precursor protein secretion promoting activity and suppress the functional disorders or apoptosis of cells, in particular neurons, mediated by the secreted soluble beta amyloid precursor proteins having a neurotrophic factor like property.摘要翻译： 根据本发明，提供了由式（I）表示的化合物：[其中R 1和R 2表示氢原子，低级烷基等; 环A是任选取代的苯环，X是氧原子等; Y代表CH或N]或其盐或其前药，以及它们的用途以及制备这些化合物的方法。 本发明的化合物等具有有效的可溶性β淀粉样蛋白前体蛋白分泌促进活性并抑制由具有神经营养因子样性质的分泌性可溶性β淀粉样蛋白前体蛋白介导的细胞，特别是神经元的功能性障碍或细胞凋亡。
-
4.发明公开AMINE COMPOUNDS, THEIR PRODUCTION AND USE AS AMYLOID-BETA PRODUCTION INHIBITORS 失效阿明衍生物，生产与应用，生产β淀粉样蛋白的抑制剂
公开(公告)号：EP0971878A1
公开(公告)日：2000-01-19
申请号：EP98905656.9
申请日：1998-02-26
IPC分类号： C07C217/74 , A61K31/135 , C07C255/54 , C07D295/08 , C07C233/43 , C07D211/26 , C07C311/21 , C07C211/60 , C07C323/19 , C07D333/16 , C07D213/30 , C07D211/44 , C07C217/76 , C07C233/25 , C07D317/54
CPC分类号： C07D213/30 , C07B2200/07 , C07C217/74 , C07C255/54 , C07C2602/10 , C07D215/14 , C07D215/20 , C07D215/58 , C07D271/06 , C07D277/64 , C07D295/096 , C07D307/80 , C07D317/54 , C07D333/16
摘要： A compound of formula (I) wherein Ar is an aromatic ring assembly group which may be substituted or a fused aromatic group which may be substituted; X is (i) a bond, (ii) -S-, -SO- or -SO2-, (iii) C1-6 alkylene, C2-6 alkenylene or C2-6 alkynylene, etc., (iv) -CO-O- or (v) -(CH2)p-x1-, -(CH¿2?)p-X?1-(CH¿2)q-, -(CH2)r-CO-X1-, -SO¿2-NR?8- or -(CH¿2?)r-SO2-NR?8¿- wherein X1 is O or NR8, R8 is H, a hydrocarbon group which may be substituted or an acyl, p is 0 to 5, q is 1 to 5, p+q is 1 to 5, and r is 1 to 4; Y is a divalent C¿1-6? aliphatic hydrocarbon group optionally containing O or S, which may be substituted; R?1 and R2¿ each is H or a lower alkyl which may be substituted, or R?1 and R2¿ form an N-containing heterocyclic ring which may be substituted; Ring A is a benzene ring which may be further substituted; and Ring B is a 4- to 8-membered ring which may be further substituted, or a salt thereof has the effect of inhibiting amyloid-β protein production and/or secretion and is useful as a pharmaceutical composition for preventing and/or treating the neurodegenerative disease, etc.
-
公开(公告)号：EP1218336A2
公开(公告)日：2002-07-03
申请号：EP00961075.9
申请日：2000-09-19
发明人： KATO, Kaneyoshi , TERAUCHI, Jun , MORI, Masaaki , SUZUKI, Nobuhiro , SHIMOMURA, Yukio , TAKEKAWA, Shiro , ISHIHARA, Yuji
IPC分类号： C07C235/00
CPC分类号： C07D207/277 , C07C217/74 , C07C219/28 , C07C233/29 , C07C233/44 , C07C233/80 , C07C235/42 , C07C235/50 , C07C235/56 , C07C235/64 , C07C235/84 , C07C237/40 , C07C271/28 , C07C275/42 , C07C311/21 , C07C2602/10 , C07C2602/12 , C07D209/18 , C07D209/22 , C07D209/42 , C07D211/16 , C07D211/18 , C07D211/22 , C07D211/26 , C07D211/32 , C07D211/52 , C07D211/62 , C07D211/70 , C07D213/56 , C07D213/81 , C07D213/82 , C07D215/14 , C07D215/38 , C07D233/24 , C07D239/28 , C07D239/30 , C07D261/18 , C07D263/14 , C07D263/34 , C07D265/28 , C07D271/06 , C07D295/096 , C07D295/13 , C07D295/185 , C07D307/68 , C07D307/81 , C07D311/58 , C07D317/60 , C07D319/20 , C07D333/24 , C07D333/28 , C07D333/38 , C07D335/16 , C07D405/04 , C07D405/12 , C07D413/04 , C07D413/12 , C07D493/04
摘要： A melanin-concentrating hormone antagonist which comprises a compound of formula (I) wherein Ar1 is a cyclic group which may have substituents; X is a spacer having a main chain of 1 to 6 atoms; Y is a bond or a spacer having a main chain of 1 to 6 atoms; Ar is a monocyclic aromatic ring which may be condensed with a 4 to 8 membered non-aromatic ring, and may have further substituents; R?1 and R2¿ are independently hydrogen atom or a hydrocarbon group which may have substituents; R?1 and R2¿, together with the adjacent nitrogen atom, may form a nitrogen-containing hetero ring which may have substituents; R2 may form a spiro ring together with Ar; or R2, together with the adjacent nitrogen atom and Y, may form a nitrogen-containing hetero ring which may have substituents; or a salt thereof; which is useful as an agent for preventing or treating obesity, etc.
摘要翻译： 一种黑色素浓缩激素拮抗剂，其包含下式化合物：其中Ar 1是可以具有取代基的环状基团; X是具有1至6个原子的主链的间隔物; Y是具有1至6个原子的主链的键或间隔基; Ar是可以与4至8元非芳族环稠合的单环芳族环，并且可以具有其它取代基; R 1和R 2独立地是氢原子或可以具有取代基的烃基; R 1和R 2以及相邻的氮原子可以形成可以具有取代基的含氮杂环; R 2可与Ar一起形成螺环; 或R 2与相邻的氮原子和Y一起形成可以具有取代基的含氮杂环; 或其盐; 其可用作预防或治疗肥胖症的药剂等。
-
公开(公告)号：EP1132376A1
公开(公告)日：2001-09-12
申请号：EP99972620.1
申请日：1999-11-18
IPC分类号： C07C235/10 , C07C237/22 , C07C237/42 , C07C235/50 , C07C233/87 , C07D295/12 , A61K31/165 , A61K31/166 , A61K31/216 , A61K31/18 , A61K31/40 , A61K31/4453 , A61P25/28 , A61P25/16
CPC分类号： C07D213/82 , C07C217/60 , C07C235/34 , C07C235/50 , C07C237/22 , C07C237/42 , C07C237/44 , C07C311/21 , C07D295/088 , C07D295/13
摘要： A compound of the formula:
wherein Ar is an aromatic group; X and Y are a bivalent group selected from -O-, -S-, -CO-, -SO-, -SO 2 -, -NR 8 -,-CONR 8 -, SO 2 NR 8 and -COO- (wherein R 8 is H, a hydrocarbon group or acyl), or a bivalent C 1-6 aliphatic hydrocarbon group which may contain one or two above bivalent groups; R 1 and R 2 are H or C 1-6 alkyl, or R 1 and R 2 may form, together with the adjacent nitrogen atom, a nitrogen-containing heterocyclic ring; and ring A is a monocyclic aromatic ring, or a salt thereof or a prodrug thereof exhibits an excellent inhibitory activity of the production and/or the secretion of amyloid-β protein.摘要翻译： 下式的化合物：其中Ar是芳族基团; X和Y是选自-O - ， - S-，-CO - ， - SO - ， - SO 2 - ，-NR 8 - ， - CONR 8 - ，SO 2 NR 8和-COO 2 - （其中R 8为H，烃基或酰基）或可含有一个或两个以上二价基团的二价C 1-6脂族烃基; R 1和R 2是H或C 1-6烷基，或者R 1和R 2可以与相邻的氮原子一起形成含氮杂环; 环A是单环芳环，或其盐或其前药对淀粉样蛋白-β蛋白的产生和/或分泌具有优异的抑制活性。
-
公开(公告)号：EP1382598A1
公开(公告)日：2004-01-21
申请号：EP02722787.5
申请日：2002-04-25
IPC分类号： C07D215/44 , C07D401/04 , C07D471/10 , C07D413/04 , C07D401/14 , C07D417/04 , C07D417/14 , C07D409/14 , C07D405/14 , A61K31/4709 , A61K31/538 , A61K31/5415 , A61K31/498 , A61K31/55 , A61K31/473 , A61K31/4725 , A61K31/496 , A61P25/00 , A61P25/16 , A61P25/28 , A61P43/00
CPC分类号： C07D215/233 , A61K31/4709 , A61K31/4725 , A61K31/473 , A61K31/496 , A61K31/498 , A61K31/538 , A61K31/5415 , A61K31/55 , C07D215/42 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D417/04 , C07D471/10
摘要： The object of the present invention is to provide soluble β-amyloid precursor protein secretory stimulators, which are effective in treating neurodegenerative diseases as well as cerebrovascular disorder-induced neuronopathy. More specifically, the present invention provides a novel compound of the following Formula (I) or a salt or prodrug thereof:
[wherein R 1 and R 2 each represent a hydrogen atom or a lower alkyl group, etc., Ar 1 and the ring B each represent an optionally substituted aromatic group, the ring A represents an optionally substituted benzene ring, the ring C represents an optionally substituted 4- to 8-membered ring which may further be condensed with an optionally substituted ring, X represents CH or N, and Y represents CH or N].摘要翻译： 本发明的目的是提供可溶性β-淀粉样蛋白前体蛋白质分泌刺激剂，其有效治疗神经变性疾病以及脑血管障碍诱发的神经元病变。 更具体地，本发明提供了下述式（I）的新化合物或其盐或前药：其中R 1和R 2各自表示氢原子或低级烷基等。 Ar 1和环B各自表示任选取代的芳族基团，环A表示任选取代的苯环，环C表示任选取代的4-至8-元环，其可以进一步与任选取代的 环，X表示CH或N，Y表示CH或N。
-
公开(公告)号：EP1270545A1
公开(公告)日：2003-01-02
申请号：EP01917774.0
申请日：2001-04-02
IPC分类号： C07C217/60 , C07C213/02 , C07C235/34 , C07C231/12 , A61K31/137 , A61P25/28
CPC分类号： C07C235/34 , C07B2200/07 , C07C217/74 , C07C2602/10
摘要： This invention provides a convenient and industrially advantageous process producing amine derivatives having the action of inhibiting the secretion and accumulation of amyloid β protein.
In Compound (I), the ether linkage is selectively cleaved without cleaving the amide linkage present in the same molecule and tertiary amines are not converted into quaternary salts, and thus Amine Derivative (V) with good qualities having the action of inhibiting the secretion and accumulation of amyloid β protein can be obtained in high yield.-
公开(公告)号：EP0968164A1
公开(公告)日：2000-01-05
申请号：EP98901088.9
申请日：1998-02-02
IPC分类号： C07C50/32 , C07C69/74 , C07D295/18 , A61K31/12
CPC分类号： C07D209/48 , C07C45/513 , C07C47/277 , C07C47/575 , C07C49/755 , C07C50/32 , C07C62/38 , C07C65/40 , C07C66/00 , C07C69/007 , C07C69/738 , C07C69/757 , C07C69/92 , C07C217/58 , C07C225/14 , C07C233/25 , C07C233/31 , C07C235/46 , C07C235/82 , C07C255/56 , C07C271/12 , C07C2602/24 , C07C2602/32 , C07D211/32 , C07D211/58 , C07D213/63 , C07D213/64 , C07D213/65 , C07D213/74 , C07D215/227 , C07D235/06 , C07D249/18 , C07D295/116 , C07D295/185 , C07D295/192
摘要： A compound of formula (I), wherein R?1 and R2¿ each represents a lower alkyl, or R?1 and R2¿ may be bonded together to form a ring; X represents a spacer of which the number of atoms constituting the principal chain is 1 to 15; Y represents an acyl, or a hydroxy, an amino or an aromatic group, each of which may be substituted; and ring A represents a 5- to 8-membered ring which may be further substituted apart from -X-Y, or a salt thereof is useful as a pharmaceutical composition for preventing or treating disease related to mitochondrial dysfunction.
摘要翻译： 下式的化合物：其中R 1和R 2各自表示低级烷基，或者R 1和R 2可以键合在一起形成环; X表示构成主链的原子数为1〜15的间隔基; Y表示可以被取代的酰基或羟基，氨基或芳基; 环A表示除-X-Y之外可以进一步取代的5-至8-元环，或其盐可用作预防或治疗与线粒体功能障碍有关的疾病的药物组合物。
-
10.发明公开USE OF VINYL CARBOXYLIC ACID COMPOUNDS FOR THE TREATMENT OR PREVENTION OF TRANSIENT ISCHAEMIC ATTACKS 失效VINYL二氧化碳衍生物用于治疗或预防短暂性脑缺血状态的使用
公开(公告)号：EP0810862A2
公开(公告)日：1997-12-10
申请号：EP96903205.0
申请日：1996-02-21
IPC分类号： A61K31
CPC分类号： A61K31/444 , A61K31/4406 , A61K31/443 , A61K31/4436 , A61K31/47
摘要： A pharmaceutical composition for treating a transient ischemic attack which comprises a compound of formula (I), wherein R1 is a pyridyl group, R2 is a phenyl, thienyl, furyl, naphthyl, benzothienyl or pyridyl group, which may be substituted with a lower alkoxy group, a lower alkyl group, a halogen atom, trifluoromethyl group, a lower alkenyl group or/and methylenedioxy group, R3 is hydrogen atom or a lower alkyl group, and l is an integer of 0 to 6, Y is sulfur atom, methylene group or a group of formula (a), wherein R4 is hydrogen atom or acetyl group, and m is 0 or 1, or a pharmaceutically acceptable salt.
-
-
-
-
-
-
-
-
-
搜索结果
10 条记录 (耗时 0.019 秒)
