摘要:
A prophylactic and/or therapeutic agent for diseases accompanied by chronic musculoskeletal pain comprising as an active ingredient a compound having an adenosine A2A receptor antagonistic action, for example, represented by the following formula (I) (wherein R1, R2 and R3 are the same or different, each representing a hydrogen atom, lower alkyl, lower alkenyl or lower alkynyl; R4 represents cycloalkyl, —(CH2)n—R5 or the following formula (II); and X1 and X2 are the same or different, each representing an oxygen atom or a sulfur atom) or a pharmaceutically acceptable salt thereof.
摘要翻译:一种伴有慢性肌肉骨骼疼痛的疾病的预防和/或治疗剂,其包含作为活性成分的具有腺苷A 2A受体拮抗作用的化合物,例如由下式(I)表示的化合物(其中 R 1,R 2和R 3相同或不同,各自表示氢原子,低级烷基,低级烯基或低级炔基; R 4表示环烷基, - (CH 2)n - R 5 -R 5或下式(II); 和X 1和X 2相同或不同,各自表示氧原子或硫原子)或其药学上可接受的盐。
摘要:
Provided are: an agent for suppressing an undesirable effect of an opioid-type analgesic (opioid), which comprises a compound having adenosine A2A receptor antagonistic activity or a pharmaceutically acceptable salt thereof as an active ingredient; the agent for suppressing an undesirable effect of an opioid-type analgesic (opioid), wherein the undesirable effect of the opioid-type analgesic (opioid) is analgesic tolerance or constipation; the agent for suppressing an undesirable effect of an opioid-type analgesic (opioid), wherein the undesirable effect of the opioid-type analgesic (opioid) is analgesic tolerance; and the like.
摘要:
Provided are: an agent for suppressing an undesirable effect of an opioid-type analgesic (opioid), which comprises a compound having adenosine A2A receptor antagonistic activity or a pharmaceutically acceptable salt thereof as an active ingredient; the agent for suppressing an undesirable effect of an opioid-type analgesic (opioid), wherein the undesirable effect of the opioid-type analgesic (opioid) is analgesic tolerance or constipation; the agent for suppressing an undesirable effect of an opioid-type analgesic (opioid), wherein the undesirable effect of the opioid-type analgesic (opioid) is analgesic tolerance; and the like.
摘要:
For example, a piperidine derivative represented by following formula (I) (wherein, —C(═O)-Z- represents —C(═O)—CH2—, —C(═O)—C(CH3)2—, —C(═O)—NH—, —C(═O)—O—, —C(═O)—S—, —C(═O)—CH2CH2—, —C(═O)—CH═CH—, —C(═O)—CH2O—, —C(═O)—CH2S—, —C(═O)—CH2CH2CH2— or —C(═O)—NR8CH2—; R1 represents a hydrogen atom, substituted or unsubstituted lower alkyl, or the like; R2 represents a hydrogen atom or hydroxy; R3 represents a hydrogen atom, substituted or unsubstituted lower alkyl, or the like; R5 represents a hydrogen atom, hydroxy, or the like; R6 represents a hydrogen atom, hydroxy, substituted or unsubstituted lower alkyl, or the like, etc.; R7 represents a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, or the like; n and k each independently represents an integer of 0 to 2; and ---- represents a single bond, or a double bond together with R4, where in case ---- is a single bond, R4 represents a hydrogen atom, hydroxy, or the like) or a pharmaceutically acceptable salt thereof and the like having an antagonistic activity for a glutamic acid receptor (NR2B/NMDA receptor) of an N-methyl-D-aspartic acid (NMDA) type containing an NR2B subunit are provided.
摘要翻译:例如,由下式(I)表示的哌啶衍生物(其中,-C(-O)-Z-表示-C(-O)-CH 2 - , - C( - -C(= O)-NH-, - C(-O)-O - , - C(-O) - S - , - C(-O)-CH 2 CH 2 - , - C(-O)-CH-CH - , - C(-O)-CH O - , - C(-O)-CH 2 S - , - C(-O)-CH 2 CH 2 2-CH 2 - 或-C( - )-NR 8 CH 2 - ; R 1 - SUP>表示氢原子,取代或未取代的低级烷基等; R 2表示氢原子或羟基; R 3表示氢原子,取代或未取代的 低级烷基等; R 5表示氢原子,羟基等; R 6表示氢原子,羟基,取代或未取代的低级烷基,或 R 7表示氢原子,卤素,取代或未取代的低级烷基等; n和k各自独立地表示0〜2的整数;< U STYLE = “ SINGLE“> ----表示单键,或与R 4连接的双键,其中如果是单键,则R” 对于N-甲基-D-葡萄糖酸的谷氨酸受体(NR2B / NMDA受体)具有拮抗作用的氨基酸或其药学上可接受的盐等) 提供了含有NR2B亚基的天冬氨酸(NMDA)型。
摘要:
A method for treating migraine comprising administering, as an active ingredient, a xanthine derivative represented by the following formula or a pharmaceutically acceptable salt thereof.
摘要:
(wherein R1, R2 and R3 are the same or different, and represent a hydrogen atom, lower alkyl, lower alkenyl or lower alkynyl; R4 represents cycloalkyl, —(CH2)n—R5 or a group represented by the above formula (II); and X1 and X2 are the same or different, and represent an oxygen atom or a sulfur atom) The present invention provides, for example, agents for treating migraine comprising, as an active ingredient, a xanthine derivative represented by the above formula (I) or a pharmaceutically acceptable salt thereof.
摘要翻译:(其中R 1,R 2和R 3相同或不同,表示氢原子,低级烷基,低级烯基或低级 炔基; R 4表示环烷基, - (CH 2 CH 2)n -R 5或由下式表示的基团: 上述式(II); X 1和X 2相同或不同,表示氧原子或硫原子)本发明提供例如, 用于治疗偏头痛的药剂,其包含作为活性成分的由上式(I)表示的黄嘌呤衍生物或其药学上可接受的盐。
摘要:
The present invention provides an agent for the treatment of bladder irritative symptoms accompanied by benign prostatic hyperplasia, comprising, as an active ingredient, a compound having a slowly-inactivating A-type K+ channel opening activity or a pharmaceutically acceptable salt thereof, and a method for screening agents for the treatment of bladder irritative symptoms accompanied by benign prostatic hyperplasia, comprising measuring a slowly-inactivating A-type K+ channel opening activity as an index.
摘要:
The present invention provides a pharmaceutical composition which is useful in the treatment for overactive bladder and the like, and comprises 3,3,3-trifluoro-2-hydroxy-2-methyl-N-(5,5,10-trioxo-4,10-d ihydrothieno[3,2-c][1]benzothiepin-9-yl)propanamide or a pharmaceutically acceptable salt thereof, and an anticholinergic agent.
摘要:
The present invention provides a therapeutic agent for bladder irritative symptoms associated with benign prostatic hyperplasia comprising, as an active ingredient, a tricyclic compound represented by formula (I): [wherein R1 represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkoxy or halogen; X1-X2-X3 represents CR5═CR6—CR7═CR8, N(O)m═CR6—CR7═CR8, CR5═CR6—N(O)m═CR8, CR5═CR6—CR7═N(O)m, CR5═CR6—O, CR5═CR6—S, O—CR7═CR8, S—CR7═CR8 or O—CR7═N; Y represents 13 CH2S—, —CH2SO—, —CH2SO2—, —CH2O—, —CH═CH—, —(CH2)p—, —SCH2—, —SOCH2—, —SO2CH2— or —OCH2—; and R2 represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkenyl, substituted or unsubstituted lower alkoxy, amino, mono(substituted or unsubstituted lower alkyl)-substituted amino, di(substituted or unsubstituted lower alkyl)-substituted amino, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted aralkylamino, substituted or unsubstituted arylamino or a substituted or unsubstituted heteroalicyclic group] or a pharmaceutically acceptable salt thereof.
摘要:
Disclosed is a tricyclic compound represented by the formula (I): ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represents hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, amino, C1-6 alkylamino, halogenated C1-6 alkyl, halogenated C1-6 alkoxy, halogen, nitro, cyano, carboxy, C1-6 alkoxycarbonyl, hydroxymethyl, CR.sup.9 R.sup.10 CO.sub.2 R.sup.11 (wherein each of R.sup.9, R.sup.10 and R.sup.11 independently represents hydrogen or C1-6 alkyl) or CONR.sup.12 R.sup.13 (wherein each of R.sup.12 and R.sup.13 independently represents hydrogen or C1-6-alkyl); R.sup.5 represents hydrogen or C1-6 alkyl; each of R.sup.6, R.sup.7 and R.sup.8 independently represents hydrogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkanoyloxy, C1-6 alkylthio, thiocyanato or halogen; X represents CH or N; Y.sup.1 -Y.sup.2 represents CH.sub.2 -O, CH.sub.2 -S(O).sub.n, (wherein n represents 0, 1, or 2), CH.sub.2 CH.sub.2, CH.dbd.CH or CON(R.sup.14) (wherein R.sup.14 represents hydrogen or C1-6 alkyl) and Z represents oxygen or sulfur, or a pharmaceutically acceptable salt thereof. The compound possesses an acyl coenzyme A: cholesterol acyltransferase-inhibiting activity, and thus are expected to have preventive and therapeutic effects on hyperlipemia and arteriosclerosis.
摘要翻译:公开了由式(I)表示的三环化合物:其中R 1,R 2,R 3和R 4各自独立地表示氢,C 1-6烷基,C 1-6烷氧基,C 1-6烷硫基,氨基, C 1-6烷基氨基,卤代C 1-6烷基,卤代C 1-6烷氧基,卤素,硝基,氰基,羧基,C 1-6烷氧基羰基,羟甲基,CR 9 R 10 CO 2 R 11(其中R 9,R 10和R 11各自独立地表示氢或C 1-6烷基 )或CONR 12 R 13(其中R 12和R 13各自独立地表示氢或C 1-6 - 烷基); R5表示氢或C1-6烷基; R 6,R 7和R 8各自独立地表示氢,C 1-6烷基,羟基,C 1-6烷氧基,C 1-6烷酰氧基,C 1-6烷硫基,氰硫基或卤素; X表示CH或N; Y1-Y2表示CH2-O,CH2-S(O)n,(其中n表示0,1或2),CH2CH2,CH = CH或CON(R14)(其中R14表示氢或C1-6烷基) Z表示氧或硫,或其药学上可接受的盐。 该化合物具有酰基辅酶A:胆固醇酰基转移酶抑制活性,因此预期对高脂血症和动脉硬化具有预防和治疗作用。