摘要:
The present invention relates to a compound of the formula: ##STR1## wherein Ar represents an optionally substituted aromatic group; Q represents a divalent aliphatic hydrocarbon group; R.sub.1 represents hydrogen, cyano, an optionally substituted hydrocarbon group, a group of the formula: ##STR2## wherein R.sup.3 and R.sub.4 independently represent hydrogen, acyl or an optionally substituted hydrocarbon group, or R.sup.3 and R.sup.4 jointly form a ring, or acyl; R.sup.2 represents acyl; ......... represents a single bond or a double bond; m represents 1 or 2 or a salt, a process of producing thereof and an anti-neurodegenerative composition.
摘要:
A compound represented by the formula: ##STR1## wherein Ar.sup.1 and Ar.sup.2 independently represent an optionally substituted aromatic group; Q represents an optionally substituted divalent aliphatic hydrocarbon group optionally containing O or S; R.sup.1 represents H, acyl group, etc.; and X represents an electron-withdrawing group, an optionally substituted aromatic group, a group of the formula: ##STR2## wherein R.sup.2 and R.sup.3 independently represent H, acyl group or an optionally substituted hydrocarbon group, etc., etc.; or salts thereof are useful as an excellent anti-neurodegenerative agent.
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 &bgr; 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 &bgr; protein can be obtained in high yield.
摘要:
A melanin-concentrating hormone antagonist which comprises a compound of the formula: 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; R1 and R2 are independently hydrogen atom or a hydrocarbon group which may have substituents; R1 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与相邻的氮原子一起可以形成可以具有取代基的含氮杂环; R 2可以与Ar一起形成螺环; 或R 2连同相邻的氮原子和Y可以形成可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等的药剂。
摘要:
A compound of the formula: 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—, —(CH2)p-X1-(CH2)q-, —(CH2)r-CO-X1-, —SO2—NR8— or —(CH2)r-SO2—NR8— 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 C1-6 aliphatic hydrocarbon group optionally containing O or S, which may be substituted; R1 and R2 each is H or a lower alkyl which may be substituted, or R1 and R2 form a 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-&bgr; protein production and/or secretion and is useful as a pharmaceutical composition for preventing and/or treating the neurodegenerative disease, etc.
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—, —SO2—, —NR8—, —CONR8—, SO2NR8 and —COO— (wherein R8 is H, a hydrocarbon group or acyl), or a bivalent C1-6 aliphatic hydrocarbon group which may contain one or two above bivalent groups; R1 and R2 are H or C1-6 alkyl, or R1 and R2 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-&bgr; 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 2 - , - NR 8 - , - CONR 8 - ,SO 2 NR 8和-COO-(其中R 8是H,烃基或酰基) ,或可以含有一个或两个上述二价基团的二价C 1-6脂族烃基; R1和R2是H或C1-6烷基,或R1和R2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。
摘要:
A compound of the formula: 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—, —(CH2)p-X1— (CH2)q-, —(CH2)r-CO—X1—, —SO2—NR8— or —(CH2)r-SO2—NR8— 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 C1-6 aliphatic hydrocarbon group optionally containing O or S, which may be substituted; R1 and R2 each is H or a lower alkyl which may be substituted, or R1 and R2 form a 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-&bgr; protein production and/or secretion and is useful as a pharmaceutical composition for preventing and/or treating the neurodegenerative disease, etc.
摘要:
A melanin-concentrating hormone antagonist which comprises a compound of the formula: 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; R1 and R2 are independently hydrogen atom or a hydrocarbon group which may have substituents; R1 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与相邻的氮原子一起可以形成可以具有取代基的含氮杂环; R 2可以与Ar一起形成螺环; 或R 2连同相邻的氮原子和Y可以形成可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等的药剂。
摘要:
A polyurethaneurea elastomer obtained by reacting a polyisocyanate component obtained by reacting 1,5-naphthalene diisocyanate with a polyol, with an amine component consisting essentially of an amine compound of the formula (1): ##STR1## wherein R is a bivalent polyalkylene polyether or polyalkylene polyester having an average molecular weight of at least 200, which may contain unsaturated bonds in the polyalkylene.
摘要:
The present invention relates to a compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom, carboxylic acid acyl or carbamoyl which may be substituted; R is an aliphatic hydrocarbon group which may be substituted or alicylic hydrocarbon group which may be substituted, or a salt thereof.The compound of the present invention has the effects to prevent and improve dysfunctions caused by oxygen free radicals, and can be used as preventive and therapeutic drugs against dysfunctions in the circulatory system.