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    • 3. 发明申请
    • NOVEL BENZIMIDAZOLE DERIVATIVES
    • 新型苯并咪唑衍生物
    • WO2004002986A2
    • 2004-01-08
    • PCT/JP2003/008161
    • 2003-06-26
    • BANYU PHARMACEUTICAL CO., LTD.OTAKE, NorikazuMORIYA, MinoruOGINO, YoshioMATSUDA, KenjiNAGAE, YoshikazuKANATANI, AkioFUKAMI, Takehiro
    • OTAKE, NorikazuMORIYA, MinoruOGINO, YoshioMATSUDA, KenjiNAGAE, YoshikazuKANATANI, AkioFUKAMI, Takehiro
    • C07D471/04
    • C07D473/30C07D405/04C07D471/04C07D471/10C07D473/00C07D491/04
    • A compound of the formula (I): (wherein A, B, C and D are independently nitrogen or optionally substituted methine; E is nitrogen, methine or hydroxy substituted methine; n is 0 or 1; T, U, V and W are independently nitrogen or optionally substituted methine; X is - N(S0 2 R 4 )-, - N (COR 5 ) - or - CO-; Y is -C (R 6 ) (R 7 )_, -0- or -N (R 8 )_, provided that the compound (I) when E is nitrogen, n is 0, X is -CO-, and Y is - 0- is excluded) is useful as an agent for the treatment of various diseases related to NPY, for example cardiovascular disorders such as angina, acute or congestive heart failure, myocardial infarction, hypertension, nephropathy, electrolyte abnormality, vasospasm, arteriosclerosis, etc., central nervous system disorders such as bulimia, depression, anxiety, seizure, epilepsy, dementia, pain, alcoholism, drug withdrawal, circadian rhythm disorders, schizophrenia, memory impairment, sleep disorders, cognitive impairment, etc., metabolic diseases such as obesity, diabetes, hormone abnormality, hypercholesterolemia, hyperlipidemia, gout, fatty liver, etc., genital or reproductive disorders such as infertility, preterm labor, sexual dysfunction, etc., gastro-intestinal disorders, respiratory disorder, inflammatory diseases or glaucoma, and the like, also for example, atherosclerosis, hypogonadism, hyperandrogenism, polycystic ovary syndrome, hirsutism, gastro-intestinal motility disorder, obesity-related gastro-esophageal reflux, obesity hypoventilation (Pickwickian syndrome), sleep apnea, inflammation, systemic inflammation of the vasculature, osteoarthritis, insulin resistance, bronchoconstriction, alcohol preference, metabolic syndrome, Alzheimer's disease, cardiac hypertrophy, left ventricular hypertrophy, hypertriglyceridemia, low HDL cholesterol, cardiovascular disorders such as coronary heart disease (CHD), cerebrovascular disease, stroke, peripheral vascular disease, sudden death, gallbladder diseases, cancer (breast, endometrial, colon), breathlessness, hyperuricemia, impaired fertility, low back pain, and increased anesthetic risk.
    • 式(I)的化合物:其中A,B,C和D独立地为氮或任选取代的次甲基; E为氮,次甲基或羟基取代的次甲基; n为0或1; T,U,V和W为 独立的氮或任选取代的次甲基; X是-N(SO 2 R 4) - , - N(COR 5) - 或 - CO-; Y是-C(R 6) 其中当E为氮时,化合物(I)为n,n为0,X为-CO-,Y为0〜 - 被排除)可用作治疗与NPY相关的各种疾病的药剂,例如心血管疾病如心绞痛,急性或充血性心力衰竭,心肌梗塞,高血压,肾病,电解质异常,血管痉挛,动脉硬化等, 中枢神经系统疾病如贪食症,抑郁症,焦虑症,癫痫发作,癫痫症,痴呆症,酗酒,戒酒,药物戒断,昼夜节律紊乱,精神分裂症,记忆障碍,睡眠障碍,认知障碍等,代谢疾病如肥胖 ,糖尿病,激素异常,高胆固醇血症,高脂血症,痛风,脂肪肝等,生殖器官或生殖障碍如不育症,早产,性功能障碍等,胃肠疾病,呼吸系统疾病,炎性疾病或青光眼,以及 例如动脉粥样硬化,性腺机能减退,雄激素过多症,多囊卵巢综合征,多毛症,胃肠动力障碍,肥胖相关的胃食管反流,肥胖低通气(皮克维克综合征),睡眠呼吸暂停,炎症,脉管系统的全身炎症, 骨关节炎,胰岛素抵抗,支气管收缩,酒精偏爱,代谢综合征,阿尔茨海默病,心脏肥大,左心室肥大,高甘油三酯血症,低HDL胆固醇,心血管疾病如冠心病(CHD),脑血管疾病,中风,外周血管疾病,突发 死亡,胆囊疾病,癌症(乳腺癌,子宫内膜癌,结肠癌) ),呼吸困难,高尿酸血症,生育能力受损,腰痛,麻醉风险增加。
    • 4. 发明申请
    • 1,2,3,4-TETRAHYDROISOQUINOLINE DERIVATIVES
    • 1,2,3,4-四氢喹啉衍生物
    • WO1990002119A1
    • 1990-03-08
    • PCT/JP1989000825
    • 1989-08-15
    • BANYU PHARMACEUTICAL CO., LTD.ISHIKAWA, KiyofumiHAYAMA, TakashiFUKAMI, TakehiroTAKAHASHI, IkukoMIURA, KeikoOKUYAMA, Akira
    • BANYU PHARMACEUTICAL CO., LTD.
    • C07D217/14
    • C07D217/04C07D217/16C07D217/20
    • The invention relates to 1,2,3,4-tetrahydroisoquinoline derivatives represented by following general formula (I) and antitumor effect potentiators containing said compounds as active ingredients. In the said formula, R represents a lower alkyl group or, when combined with R or R , represents a methylene group, one of R and R represents a lower alkyl group or, when combined with R , represents a methylene group, and the other represents a lower alkenyl group, a substituted or unsubstituted aryl-lower alkenyl group, a substituted or unsubstituted aryl-lower alkyl group (provided that an unsubstituted phenyl group is omitted), a substituted or unsubstituted aryl group (provided that an unsubstituted phenyl group is omitted) or a group represented by -(CH2)m-A (wherein A represents a halogen atom, a lower alkylthio group, a lower alkylsulfinyl group, a lower alkylsulfonyl group, a substituted or unsubstituted aryl-lower alkylthio group, a substituted or unsubstituted aryl-lower alkylsulfinyl group, a substituted or unsubstituted aryl-lower alkylsulfonyl group, a substituted or unsubstituted arylthio group, a substituted or unsubstituted arylsulfinyl group, a substituted or unsubstituted arylsulfonyl group, a substituted or unsubstituted alkyloxy group or a substituted or unsubstituted aryloxy group, an N-benzyl-N-(lower alkyl)amino group, an N-phenyl-N-(lower alkyl)amino group, an N,N-di(lower alkyl)amino group, a di(lower alkyloxy)phosphinoyl group or a dibenzyloxyphosphinoyl group, and m represents 2 to 4), R represents a lower alkyl group, Ar represents a phenyl group optionally substituted by 1 to 3 lower alkyloxy groups, and n represents 0 to 2.
    • 本发明涉及由以下通式(I)表示的1,2,3,4-四氢异喹啉衍生物和含有所述化合物作为活性成分的抗肿瘤作用增强剂。 在所述式中,R 2表示低级烷基,或者当与R 1或R 3结合时,表示亚甲基,R 1和R 3之一表示低级烷基 或者当与R 2结合时,表示亚甲基,另一个表示低级烯基,取代或未取代的芳基 - 低级烯基,取代或未取代的芳基 - 低级烷基(条件是未取代的苯基 (其中A表示卤素原子,低级烷硫基,低级烷基亚磺酰基,低级烷基亚磺酰基)表示的基团, 烷基磺酰基,取代或未取代的芳基 - 低级烷硫基,取代或未取代的芳基 - 低级烷基亚磺酰基,取代或未取代的芳基 - 低级烷基磺酰基,取代或未取代的芳硫基,取代或未取代的芳基亚磺酰基,取代基 取代或未取代的烷氧基或取代或未取代的芳氧基,N-苄基-N-(低级烷基)氨基,N-苯基-N-(低级烷基)氨基,N ,N-二(低级烷基)氨基,二(低级烷氧基)膦酰基或二苄氧基膦酰基,m表示2〜4),R 4表示低级烷基,Ar表示任选被 1〜3个低级烷氧基,n表示0〜2。
    • 5. 发明申请
    • NOVEL AMINOPYRAZOLE DERIVATIVES
    • 新型氨基吡唑衍生物
    • WO1998025908A1
    • 1998-06-18
    • PCT/JP1997004571
    • 1997-12-12
    • BANYU PHARMACEUTICAL CO., LTD.FUKAMI, TakehiroFUKURODA, TakahiroKANATANI, AkioIHARA, Masaki
    • BANYU PHARMACEUTICAL CO., LTD.
    • C07D231/40
    • C07D401/12C07D231/40
    • Compounds represented by general formula (I), (wherein Ar represents an aryl group which may be substituted with a group selected among halogen atoms and lower alkyl and halogenated lower alkyl groups; Ar represents an aryl group or a heteroaromatic group which may be substituted with a group selected among halogen atoms and lower alkyl, lower alkenyl, halogenated lower alkyl, lower alkoxy, lower alkylthio, lower alkylamino, di(lower alkyl)amino, and aryl groups; R and R , which may be the same or different, represent each a hydrogen atom or a lower alkyl group; R and R , which may be the same or different, represent each a hydrogen atom or a lower alkyl group, or R and R combine with each other to form an alkylene group bearing 2 to 4 carbon atoms and optionally having a lower alkyl group; and R represents a hydrogen atom or a lower alkyl or lower alkoxy group) or salts thereof; a process for preparing the same; and a therapeutic agent for bulimia, obesity, or diabetes, comprising the compound or salt thereof as the active ingredient.
    • 由通式(I)表示的化合物(其中Ar 1表示可以被选自卤素原子和低级烷基和卤代低级烷基的基团取代的芳基; Ar 2表示芳基或杂芳族 可以被选自卤素原子和低级烷基,低级烯基,卤代低级烷基,低级烷氧基,低级烷硫基,低级烷基氨基,二(低级烷基)氨基和芳基的基团取代的基团; R 1和R 2' 2'可以相同或不同,表示氢原子或低级烷基; R 3和R 4可以相同或不同,表示氢原子或低级烷基 或R 3和R 4彼此结合形成具有2至4个碳原子并且任选具有低级烷基的亚烷基; R 5表示氢原子或低级烷基或低级烷氧基 基团)或其盐; 其制备方法; 以及包含其化合物或其盐作为活性成分的贪食症,肥胖症或糖尿病的治疗剂。
    • 9. 发明申请
    • PYRAZOLE DERIVATIVES
    • 吡唑衍生物
    • WO1998025907A1
    • 1998-06-18
    • PCT/JP1997004567
    • 1997-12-12
    • BANYU PHARMACEUTICAL CO., LTD.FUKAMI, TakehiroFUKURODA, TakahiroKANATANI, AkioIHARA, Masaki
    • BANYU PHARMACEUTICAL CO., LTD.
    • C07D231/40
    • C07D401/04C07D231/40C07D401/12C07D403/04C07D403/12C07D405/04C07D405/12C07D409/12C07D487/04
    • Compounds represented by general formula (I), (wherein ring A and ring B are in a state of ortho fusion, the ring A representing an aromatic carbocyclic or heterocyclic ring, and the ring B representing a four- to seven-membered aliphatic carbocyclic or nitrogen-containing heterocyclic ring wherein the nitrogen atom can be present in only the site of fusion with the ring A; Ar represents an aromatic carbocyclic or heterocyclic group optionally substituted with a group selected among halogen atoms and lower alkyl, lower alkenyl, halogenated lower alkyl, lower alkoxy, lower alkylthio, lower alkylamino, di(lower alkyl)amino, and aromatic carbocyclic groups; and R represents a substituent selected among halogen atoms, nitro, lower alkyl, lower alkoxy, aromatic carbocyclic groups, and a carbonyl group having an aromatic carbocyclic group, or a hydrogen atom, provided that when the group represented by formula (a), is the group represented by formula (b), Ar represents neither phenyl nor 4-chlorophenyl) or salts thereof; a process for preparing the same; and a therapeutic agent for bulimia, obesity, or diabetes, comprising the compound or salt thereof as the active ingredient.
    • 由通式(I)表示的化合物(其中环A和环B处于邻位融合的状态,环A表示芳族碳环或杂环,环B代表四至七元脂族碳环或 含氮杂环,其中氮原子可以仅存在于与环A的融合位点; Ar表示任选被选自卤素原子的基团取代的芳族碳环或杂环基,低级烷基,低级烯基,卤代低级烷基 ,低级烷氧基,低级烷硫基,低级烷基氨基,二(低级烷基)氨基和芳族碳环基; R表示选自卤素原子,硝基,低级烷基,低级烷氧基,芳族碳环基团和具有 芳香族碳环基或氢原子,条件是当由式(a)表示的基团是由式(b)表示的基团时,Ar不表示苯基或者4-c 氯苯基)或其盐; 其制备方法; 以及包含其化合物或其盐作为活性成分的贪食症,肥胖症或糖尿病的治疗剂。
    • 10. 发明申请
    • NOVEL UREA DERIVATIVES
    • 新尿素衍生物
    • WO1998024768A1
    • 1998-06-11
    • PCT/JP1997004399
    • 1997-12-02
    • BANYU PHARMACEUTICAL CO., LTD.FUKAMI, TakehiroFUKURODA, TakahiroKANATANI, AkioIHARA, Masaki
    • BANYU PHARMACEUTICAL CO., LTD.
    • C07D231/40
    • C07D401/04C07D231/40C07D401/12C07D403/12C07D405/04
    • Compounds represented by general formula (I) or salts thereof, a process for producing the same, and a remedy for hyperphagia, adiposis, or diabetes which comprises the same as the active ingredient: wherein A represents nitrogen or a group represented by C-R ; Ar represents aryl optionally having substituent(s) selected from the group consisting of halogeno, lower alkyl, and lower haloalkyl; Ar represents aryl or heteroaryl optionally having substituent(s) selected from the group consisting of halogeno, lower alkyl, lower alkenyl, lower haloalkyl, lower alkoxy, lower alkylthio, lower alkylamino, lower dialkylamino, and aryl; R represents hydrogen or lower alkyl or is bonded to R to represent a bond; R represents hydrogen or lower alkyl; R and R are the same or different and each represents hydrogen or lower alkyl, or R and R are bonded to each other to represent C2-4 alkylene optionally having lower alkyl; and R represents hydrogen, hydroxy, lower alkyl, or lower alkoxy or is bonded to R to represent a bond.
    • 由通式(I)表示的化合物或其盐,其制备方法,以及包含与活性成分相同的食欲过盛,脂肪酸或糖尿病的药物:其中A表示氮或CR 5表示的基团 >; Ar 1表示任选具有选自卤代,低级烷基和低级卤代烷基的取代基的芳基; Ar 2表示任选具有选自卤代,低级烷基,低级烯基,低级卤代烷基,低级烷氧基,低级烷硫基,低级烷基氨基,低级二烷基氨基和芳基的取代基的芳基或杂芳基。 R 1表示氢或低级烷基或与R 5键合以表示键; R 2表示氢或低级烷基; R 3和R 4相同或不同,各自表示氢或低级烷基,或R 3和R 4彼此键合,表示任选具有低级烷基的C 2-4亚烷基; 并且R 5表示氢,羟基,低级烷基或低级烷氧基,或与R 1键合以表示键。