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    • 1. 发明申请
    • SULPIRIDE DERIVATIVES PHARMACEUTICAL COMPOSITIONS
    • SULPIRIDE衍生物药物组合物
    • WO2006028500A1
    • 2006-03-16
    • PCT/US2005/006088
    • 2005-02-24
    • BARBEAU PHARMA, INC.BARBEAU, Donald L.
    • BARBEAU, Donald L.
    • A61K31/40
    • C07D207/09
    • The present invention relates to pharmaceutical compositions containing sulpiride compounds having the general formula (I): where R 1 is branched or straight chain alkyl having from 1 to about 7 carbon atoms, a substituted or unsubstituted aryl, a substituted or unsubstituted cycloalkyl, a substituted or unsubstituted aralkyl, a substituted or unsubstituted alkylcycloakyl, or a group having the formula (CH 2 ) n R 2 where R 2 is a substituted or unsubstituted aryl or a substituted or unsubstituted cycloalkyl, and n is an alkyl group having from 0 to about 6 carbon atoms and pharmaceutically acceptable salts or diluents.
    • 本发明涉及包含具有通式(I)的舒必利化合物的药物组合物:其中R 1是具有1至约7个碳原子的支链或直链烷基,取代或未取代的芳基, 取代或未取代的环烷基,取代或未取代的芳烷基,取代或未取代的烷基环烷基或具有式(CH 2)n R 2 R 2的基团 其中R 2是取代或未取代的芳基或取代或未取代的环烷基,n是具有0至约6个碳原子的烷基和其药学上可接受的盐或稀释剂。
    • 2. 发明申请
    • STABLE PHARMACEUTICAL COMPOSITIONS
    • 稳定的药物组合物
    • WO2003075928A2
    • 2003-09-18
    • PCT/US2003/006521
    • 2003-03-04
    • BARBEAU, Donald, L.
    • BARBEAU, Donald, L.
    • A61K31/502
    • C07D237/34
    • Pharmaceutical compounds having the general formula: (I) or compounds having the formula: (II) Where R 1 and R 2 are independently H, branched or straight chain alkyl having from 1 to about 7 carbon atoms, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aralkyl, substituted or unsubstituted alkylcycloalkyl, lower alkenyl or R 1 and R 2 together form part of a substituted or unsubstituted cycloalkyl having from about 4 of about 7 carbon atoms; where R 3 is a branched or straight chain alkyl having from 1 to about 7 carbon atoms, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, substituted or unsubstituted cycloalkyl, aralkyl, substituted or unsubstituted alkylcycloalkyl or a group having the formula (CH 2 ) n COOH where n is from 1 to about 7.
    • 具有通式(I)的药物化合物或具有式(II)的化合物:其中R 1和R 2独立地为H 具有1至约7个碳原子的支链或直链烷基,取代或未取代的环烷基,取代或未取代的芳烷基,取代或未取代的烷基环烷基,低级链烯基或R 1和R 2, 一起形成具有约4个约7个碳原子的取代或未取代的环烷基的一部分; 其中R 3是具有1至约7个碳原子的支链或直链烷基,取代或未取代的芳基,取代或未取代的芳烷基,取代或未取代的环烷基,芳烷基,取代或未取代的烷基环烷基或基团 具有式(CH 2)n -COOH,其中n为1至约7。
    • 3. 发明申请
    • NONCARDIOTOXIC PHARMACEUTICAL COMPOUNDS
    • 非药用药物化合物
    • WO2006020573A2
    • 2006-02-23
    • PCT/US2005/028137
    • 2005-08-09
    • BARBEAU, Donald, L.
    • BARBEAU, Donald, L.
    • A61K31/675C07F9/59
    • C07F9/2458C07F9/2462C07F9/2466C07F9/247C07F9/2475C07F9/5532C07F9/5535C07F9/5728C07F9/588C07F9/591C07F9/65061C07F9/650958C07F9/6533C07F9/6547C07F9/65517C07F9/65527C07F9/655345C07F9/65583C07F9/65586C07F9/6561
    • The present invention relates to novel noncardiotoxic compounds and pharmaceutical compositions useful in the treatment of a variety of disorders including the treatment of depression, allergies, psychoses, cancer and gastrointestinal disorders. In particular, the present invention describes pharmaceutical compositions that mitigate life-threatening arrhythmias such as torsade de pointes. Torsade de pointes is a particular cardiac problem associated with many therapeutic agents and has been implicated as a possible cause of sudden death, particularly in those individuals with a past history of disturbances of cardiac rhythm, myocardial infarction, congenital repolarization abnormalities and cardiac risk factors such as hyperlipidemia and age. This arrhythmia is a variant of paroxysmal ventricular tachycardia associated with a prolonged QTc interval or prominent U waves on the ECG. Torsade de pointes is potentially lethal because it can progress to ventricular fibrillation, life-threatening arrhythmias or precipitate sudden death.
    • 本发明涉及用于治疗各种障碍的新型非心脏毒性化合物和药物组合物,包括治疗抑郁症,过敏反应,精神病,癌症和胃肠道疾病。 特别地,本发明描述了减轻危及生命的心律失常的药物组合物,例如尖端扭转型室性心律失常。 特征是与许多治疗剂相关的特定的心脏问题,并且已经被认为是猝死的可能原因,特别是在具有过去心律失调史,心肌梗死,先天性复极化异常和心脏危险因素的个体中 作为高脂血症和年龄。 这种心律失常是与心电图延长的QTc间期或突出的U波相关的阵发性室性心动过速的变体。 由于可能会导致心室纤维性颤动,危及生命的心律失常或突然猝死,可能导致脚部扭转。
    • 5. 发明申请
    • BIOADHESIVE PHARMACEUTICAL COMPOSITIONS
    • 生物药物组合物
    • WO2004064754A2
    • 2004-08-05
    • PCT/US2004001536
    • 2004-01-21
    • BARBEAU DONALD L
    • C07H5/04A61K
    • C07H5/04
    • Disclosed are compounds having the formula (I) wherein R2 is hydrogen, a monomeric glycoside or an oligomeric glycoside, R3 is hydrogen, a monomeric glycoside, an oligomeric glycoside, or a group having the formula (II), R is a lower alkylene, R' is selected from the group consisting of moieties having the formula (III), (IV) and (V) where X = 0 or 1, Y = 0 or 1, R1 is hydrogen or a pharmacologically active drug residue, R8 a pharmacologically active drug residue, R4, R5, and R6 are independently hydrogen, alkyl, aryl, aralkyl, and cycloalkyl or together form a nitrogen-containing ring, and R7 is hydroxyl or hydroxyalkyl.
    • 公开了具有式(I)的化合物,其中R2是氢,单体糖苷或低聚糖苷,R3是氢,单体糖苷,低聚糖苷或具有式(II)的基团,R是低级亚烷基, R'选自具有式(III),(IV)和(V)的部分,其中X = 0或1,Y = 0或1,R1为氢或药理活性药物残基,R8为药理学上 活性药物残基,R4,R5和R6独立地是氢,烷基,芳基,芳烷基和环烷基,或一起形成含氮环,并且R 7是羟基或羟烷基。
    • 6. 发明申请
    • NONCARDIOTOXIC PHARMACEUTICAL COMPOUNDS
    • 非药用药物化合物
    • WO2006020573A3
    • 2009-04-16
    • PCT/US2005028137
    • 2005-08-09
    • BARBEAU DONALD L
    • BARBEAU DONALD L
    • C07F9/06A61K31/41A61K31/435C07F9/02C07F9/08C07F9/28
    • C07F9/2458C07F9/2462C07F9/2466C07F9/247C07F9/2475C07F9/5532C07F9/5535C07F9/5728C07F9/588C07F9/591C07F9/65061C07F9/650958C07F9/6533C07F9/6547C07F9/65517C07F9/65527C07F9/655345C07F9/65583C07F9/65586C07F9/6561
    • The present invention relates to novel noncardiotoxic compounds and pharmaceutical compositions useful in the treatment of a variety of disorders including the treatment of depression, allergies, psychoses, cancer and gastrointestinal disorders. In particular, the present invention describes pharmaceutical compositions that mitigate life-threatening arrhythmias such as torsade de pointes. Torsade de pointes is a particular cardiac problem associated with many therapeutic agents and has been implicated as a possible cause of sudden death, particularly in those individuals with a past history of disturbances of cardiac rhythm, myocardial infarction, congenital repolarization abnormalities and cardiac risk factors such as hyperlipidemia and age. This arrhythmia is a variant of paroxysmal ventricular tachycardia associated with a prolonged QTc interval or prominent U waves on the ECG. Torsade de pointes is potentially lethal because it can progress to ventricular fibrillation, life-threatening arrhythmias or precipitate sudden death.
    • 本发明涉及用于治疗各种疾病的新型非心脏毒性化合物和药物组合物,包括治疗抑郁症,过敏反应,精神病,癌症和胃肠道疾病。 特别地,本发明描述了减轻危及生命的心律失常的药物组合物,例如尖端扭转型室性心律失常。 特征是与许多治疗剂相关的特定的心脏问题,并且已经被认为是猝死的可能原因,特别是在具有过去心律失调史,心肌梗死,先天性复极化异常和心脏危险因素的个体中 作为高脂血症和年龄。 这种心律失常是与心电图延长的QTc间期或突出的U波相关的阵发性室性心动过速的变体。 由于可能会导致心室纤维性颤动,危及生命的心律失常或突然猝死,可能导致脚部扭转。
    • 7. 发明申请
    • BIOADHESIVE PHARMACEUTICAL COMPOSITIONS
    • 生物药物组合物
    • WO2004064754A8
    • 2006-07-20
    • PCT/US2004001536
    • 2004-01-21
    • BARBEAU DONALD L
    • BARBEAU DONALD L
    • C07H5/04
    • C07H5/04
    • Disclosed are compounds having the formula (I) wherein R 2 is hydrogen, a monomeric glycoside or an oligomeric glycoside, R 3 is hydrogen, a monomeric glycoside, an oligomeric glycoside, or a group having the formula (II), R is a lower alkylene, R' is selected from the group consisting of moieties having the formula (III), (IV) and (V) where X = 0 or 1, Y = 0 or 1, R 1 is hydrogen or a pharmacologically active drug residue, R 8 a pharmacologically active drug residue, R 4 , R 5 , and R 6 are independently hydrogen, alkyl, aryl, aralkyl, and cycloalkyl or together form a nitrogen-containing ring, and R 7 is hydroxyl or hydroxyalkyl.
    • 公开了具有式(I)的化合物,其中R 2 2是氢,单体糖苷或低聚糖苷,R 3是氢,单糖苷,低聚糖苷, 或具有式(II)的基团,R是低级亚烷基,R'选自具有式(III),(IV)和(V)的部分,其中X = 0或1,Y = 0 或1,R 1是氢或药理活性药物残基,R 8是药理学活性药物残基,R 4,R 3, R 5和R 6独立地是氢,烷基,芳基,芳烷基和环烷基,或一起形成含氮环,并且R 7是羟基或 羟。