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    • 1. 发明申请
    • FLUORINATED 1,4-DISUBSTITUTED PIPERIDINE DERIVATIVES
    • 氟化1,4-取代的哌啶衍生物
    • WO1998005641A1
    • 1998-02-12
    • PCT/JP1997002600
    • 1997-07-28
    • BANYU PHARMACEUTICAL CO., LTD.TSUCHIYA, YoshimiNOMOTO, TakashiOHSAWA, HirokazuKAWAKAMI, KumikoOHWAKI, KenjiNISHIKIBE, Masaru
    • BANYU PHARMACEUTICAL CO., LTD.
    • C07D211/46
    • C07D401/06C07D211/58C07D405/06C07D409/06
    • Novel fluorinated 1,4-disubstituted piperidine derivatives represented by general formula (I) or pharmaceutically acceptable salts thereof, wherein Ar represents aryl or heteroaryl having 1 or 2 heteroatoms selected from the group consisting of nitrogen, oxygen and sulphur in which one to three hydrogen atoms on the aryl or heteroaryl ring may be substituted by lower alkyl, etc.; R represents C1-3 cycloalkyl in which one to four arbitrary hydrogen atoms may be substituted by fluorine; R represents saturated or unsaturated, aliphatic C5-15 hydrocarbon in which one to six arbitrary hydrogen atoms may be substituted by fluorine, aralkyl, arylalkenyl, or heteroarylalkyl or heteroarylalkenyl having one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, in which one to three hydrogen atoms on the aralkyl, arylalkenyl, heteroarylalkyl or heteroarylalkenyl ring may be substituted by lower alkyl, trifluoromethyl, cyano, hydroxy, nitro, lower alkoxycarbonyl, halogeno, lower alkoxy, amino, etc.; and X represents O or NH, provided that at least one of R and R has one or more fluorine atoms. Because of having selective muscarinic receptor antagonism and being excellent in oral activity, persistence of the action and dynamic in vivo, these compounds are useful as efficacious and safe remedies or preventives with little side effects for respiratory, urologic and digestive diseases.
    • 由通式(I)表示的新型氟化1,4-二取代哌啶衍生物或其药学上可接受的盐,其中Ar表示具有1或2个选自氮,氧和硫的杂原子的芳基或杂芳基,其中一至三个氢 芳基或杂芳基环上的原子可以被低级烷基等取代; R 1表示其中一至四个任意氢原子可被氟取代的C 1-3环烷基; R 2表示饱和或不饱和的脂族C 5-15烃,其中一至六个任意氢原子可被氟,芳烷基,芳基烯基或具有一个或两个选自氮,氧的杂芳基烷基或杂芳基烯基取代 和其中芳烷基,芳基烯基,杂芳基烷基或杂芳基烯基环上的一至三个氢原子可被低级烷基,三氟甲基,氰基,羟基,硝基,低级烷氧基羰基,卤代,低级烷氧基,氨基等取代的硫。 并且X表示O或NH,条件是R 1和R 2中的至少一个具有一个或多个氟原子。 由于具有选择性的毒蕈碱受体拮抗作用,口服活性优异,作用持久,体内动态,因此这些化合物作为呼吸系统,泌尿系统和消化系统疾病副作用少的有效和安全的补救措施或预防措施是有用的。
    • 2. 发明申请
    • 1,4-DISUBSTITUTED PIPERIDINE DERIVATIVES
    • 1,4-取代的哌啶衍生物
    • WO1997045414A1
    • 1997-12-04
    • PCT/JP1997001770
    • 1997-05-27
    • BANYU PHARMACEUTICAL CO., LTD.TSUCHIYA, YoshimiNOMOTO, TakashiOHSAWA, HirokazuKAWAKAMI, KumikoOHWAKI, KenjiNISHIKIBE, Masaru
    • BANYU PHARMACEUTICAL CO., LTD.
    • C07D211/58
    • C07D211/58
    • 1,4-Disubstituted piperidine derivatives represented by general formula (I) and pharmaceutically acceptable salts thereof, wherein Ar represents heteroaryl having one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur and optionally fused to aryl or benzene (wherein each hydrogen on the aryl and heteroaryl rings may be substituted by lower alkyl, halogeno, lower alkoxy, amino or hydroxymethyl); R represents C3-6 cycloalkyl having one or two hydroxyl groups on the ring; R represents heteroarylalkyl having one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur and optionally fused to saturated or unsaturated aliphatic C5-15 hydrocarbon, aralkyl, arylalkenyl or benzene (wherein each hydrogen on the aralkyl, arylalkenyl and heteroarylalkyl rings may be substituted by lower alkyl, halogeno, lower alkoxy, amino or hydroxymethyl); and X represents O or NH. Because of having a selective muscarine M3 receptor antagonism, these compounds are useful as safe remedies or preventives with little side effects for respiratory diseases such as asthma, chronic respiratory obstruction and pulmonary fibrosis; urologic diseases in association with urination disorders such as frequent urination, urgency of micturition and urinary incontinence; and digestive diseases such as irritable bowel syndrome and convulsion or motor hyperenergia of digestive tracts.
    • 由通式(I)表示的1,4-二取代哌啶衍生物及其药学上可接受的盐,其中Ar表示具有一个或两个选自氮,氧和硫并且任选地与芳基或苯稠合的杂原子的杂芳基(其中每个 芳基和杂芳基环上的氢可以被低级烷基,卤代,低级烷氧基,氨基或羟甲基取代); R 1表示在环上具有一个或两个羟基的C 3-6环烷基; R 2表示具有一个或两个选自氮,氧和硫的杂原子的杂芳基烷基,并且任选地与饱和或不饱和的脂族C 5-15烃,芳烷基,芳基烯基或苯稠合(其中芳烷基上的每个氢,芳烯基烯基和 杂芳基烷基环可以被低级烷基,卤代,低级烷氧基,氨基或羟甲基取代); X表示O或NH。 由于具有选择性的毒蕈碱M3受体拮抗作用,这些化合物可用作对哮喘,慢性呼吸阻塞和肺纤维化等呼吸系统疾病具有副作用的安全补救措施或预防药物; 泌尿系统疾病与排尿障碍如排尿紧急,排尿紧急和尿失禁有关; 消化道疾病如肠易激综合征,消化道惊厥或运动过敏等。
    • 4. 发明申请
    • AMINOPYRIDINE DERIVATIVES
    • 氨基吡啶衍生物
    • WO1997034873A1
    • 1997-09-25
    • PCT/JP1997000890
    • 1997-03-19
    • BANYU PHARMACEUTICAL CO., LTD.FUKAMI, TakehiroMASE, ToshiakiTSUCHIYA, YoshimiKANATANI, AkioFUKURODA, Takahiro
    • BANYU PHARMACEUTICAL CO., LTD.
    • C07D213/74
    • C07D417/06C07D213/74C07D401/12C07D405/12C07D409/12C07D413/06C07D413/12C07D417/12C07D417/14
    • Compounds of general formula [I] or pharmaceutically acceptable salts thereof; and agents for the treatment of hyperphagia, obesity or diabetes, comprising the same as the active ingredient wherein Ar is aryl or hetero-aryl which may be substituted with a radical selected from the group consisting of lower alkyl, lower hydroxyalkyl, lower alkylene and -NR R ; R is hydrogen or lower alkyl; R and R are each independently lower alkyl, or alternatively R and R are united to form alkylene which may be interrupted by oxygen or sulfur and may be substituted with one or two lower alkyl radicals; R is hydrogen or lower alkyl which may be substituted with a radical selected from the group consisting of hydroxyl, amino, carbamoyl and lower alkoxycarbonyl; Ar is aryl or hetero-aryl which may be substituted with a radical selected from the group consisting of halogeno, hydroxyl, lower alkyl, lower haloalkyl, lower alkoxy, lower alkylthio, lower hydroxyalkyl, lower alkoxy lower alkyl, -NR Rc and -NR -CO-NR R ; and W is oxygen, sulfur, -CHR - or -NR -.
    • 通式[I]的化合物或其药学上可接受的盐; 以及用于治疗肥胖,肥胖或糖尿病的药物,其包含与活性成分相同的活性成分,其中Ar 1是可以被选自下列的基团取代的芳基或杂芳基:低级烷基,低级羟烷基,低级 亚烷基和-NR a R b; R 1是氢或低级烷基; R 2和R 3各自独立地为低级烷基,或者R 2和R 3相互结合形成可被氧或硫中断的亚烷基并且可以被一个或两个低级烷基取代 ; R 4是氢或可以被选自羟基,氨基,氨基甲酰基和低级烷氧基羰基的基团取代的低级烷基; Ar 2是可以被选自卤代,羟基,低级烷基,低级卤代烷基,低级烷氧基,低级烷硫基,低级羟烷基,低级烷氧基低级烷基,-NR' c> R c和-NR e -CO-NR f R g; W是氧,硫,-CHR j - 或-NR k - 。
    • 5. 发明申请
    • 1,4-DISUBSTITUTED PIPERIDINE DERIVATIVES
    • 1,4-取代的哌啶衍生物
    • WO1996033973A1
    • 1996-10-31
    • PCT/JP1996001128
    • 1996-04-25
    • BANYU PHARMACEUTICAL CO., LTD.TSUCHIYA, YoshimiNOMOTO, TakashiOHSAWA, HirokazuKAWAKAMI, KumikoOHWAKI, KenjiNISHIKIBE, Masaru
    • BANYU PHARMACEUTICAL CO., LTD.
    • C07D211/46
    • C07D401/12C07D211/46C07D211/58C07D405/12C07D409/12C07D417/12
    • Novel 1,4-disubstituted piperidine derivatives represented by general formula (I) and pharmaceutically acceptable salts thereof, wherein Ar represents phenyl wherein one or two arbitrary hydrogen atoms on its ring may be substituted by substituent(s) selected from the group consisting of halogeno and lower alkyl or an aromatic 5- or 6-membered heterocycle having one or two heteroatoms selected from the group consisting of oxygen, nitrogen and sulfur; R represents C3-6 cycloalkyl or C3-6 cycloalkenyl; R represents saturated or unsaturated aliphatic C5-15 hydrocarbon group; and X represents O or NH. The compounds have a selective antagonism against the muscarine M3 receptor and a high safety with little side effect. Thus they are useful in the treatment or prevention of respiratory diseases such as asthma, chronic respiratory obstruction and pulmonary fibrosis, urological diseases accompanied with urination disorders such as frequent urination, urgency of micturition and urinary incontinence and digestive diseases such as convulsion or motion hyperenergia of the digestive tracts and irritable large intestine.
    • 由通式(I)表示的新的1,4-二取代哌啶衍生物及其药学上可接受的盐,其中Ar表示苯基,其中其一个或两个任意的氢原子可以被选自以下的取代基取代:卤代 和具有一个或两个选自氧,氮和硫的杂原子的低级烷基或芳族5-或6-元杂环; R 1表示C 3-6环烷基或C 3-6环烯基; R 2表示饱和或不饱和的脂族C 5-15烃基; X表示O或NH。 这些化合物对毒蕈碱M3受体具有选择性拮抗作用,安全性高,副作用小。 因此,它们可用于治疗或预防呼吸系统疾病如哮喘,慢性呼吸阻塞和肺纤维化,泌尿系统疾病伴随排尿障碍,例如尿频,排尿紧急和尿失禁以及消化系统疾病如惊厥或运动过敏 消化道和易怒大肠。
    • 6. 发明申请
    • SUBSTITUTED HETEROCYCLIC DERIVATIVE HAVING SQUALENE EPOXIDASE INHIBITORY EFFECT AND USE THEREOF
    • 具有平均环氧化酶抑制作用的取代的杂环衍生物及其用途
    • WO1993024478A1
    • 1993-12-09
    • PCT/JP1993000723
    • 1993-05-28
    • BANYU PHARMACEUTICAL CO., LTD.TSUCHIYA, YoshimiNOMOTO, TakashiMITSUYA, MorihiroNONOSHITA, KatsumasaHAYASHI, MasahiroSATO, ToshihikoSAWASAKI, YoshioKAMEI, Toshio
    • BANYU PHARMACEUTICAL CO., LTD.
    • C07D333/16
    • C07D333/08C07D333/16C07D333/18C07D333/24
    • A substituted heterocyclic derivative represented by general formula (I), wherein R represents a 5- or 6-membered heterocyclic group containing one or two heteroatoms selected from among nitrogen and other atoms; Q represents (II), (III), -CH=CH-CH2-, etc., -CH2-O-CH2-, or thrimethylene; X and Y may be the same or different from each other and each represents methylene, oxygen, etc., or alternatively X and Y may be combined together to represent vinylene, etc.; Q represents either (a) a 5- or 6-membered aromatic group represented by (IV) wherein A &cir& _, B &cir& _, D &cir& _ and E &cir& _ represent each nitrogen, etc., or =CH-; and p represents an integer of 0 or 1, or (b) a group represented by -F &cir& _-G &cir& _-I &cir& _- wherein F &cir& _, G &cir& _ and I &cir& _ may be the same or different from each other and each represents oxygen, etc., or =CH-; R represents lowr alkyl, etc.; Q represents ethylene, etc.; Q represents vinylene, etc.; R and R may be the same or different from each other and each represents lower alkyl, or alternatively R and R are combined together with the adjacent carbon atom to represent cycloalkyl; and R represents hydrogen, lower alkyl, etc.
    • 由通式(I)表示的取代的杂环衍生物,其中R表示含有一个或两个选自氮原子和其它原子的杂原子的5-或6-元杂环基; Q 1表示(II),(III),-CH = CH-CH 2 - 等,-CH 2 -O-CH 2 - 或三亚甲基; X和Y可以相同或不同,各自表示亚甲基,氧等,或者X和Y可以组合在一起代表亚乙烯基等; Q 2表示(a)由(IV)表示的5或6元芳族基团,其中A 1和R 3各自表示每个氮等,或= CH- ; 并且p表示0或1的整数,或(b)由-F 1和R 3表示的基团,其中F 1和R 3可以相同或不同 彼此各自表示氧等,或= CH-; R 1表示低级烷基等; Q 3表示乙烯等。 Q 4表示亚乙烯基等; R 2和R 3可以彼此相同或不同,并且各自表示低级烷基,或者R 2和R 3与相邻的碳原子一起代表环烷基; R 4表示氢,低级烷基等。