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1. 发明申请

WO9906046A9 COMBINATIONS OF HMG-COA REDUCTASE INHIBITORS AND NICOTINIC ACID AND METHODS FOR TREATING HYPERLIPIDEMIA 审中-公开
标题翻译： HMG-COA还原酶抑制剂与烟碱酸的组合以及治疗高脂血症的方法
公开(公告)号：WO9906046A9
公开(公告)日：1999-04-29
申请号：PCT/US9815989
申请日：1998-07-31
申请人： KOS PHARMA INC
发明人： BOVA DAVID J , DUNNE JOSEPHINE
IPC分类号： A61K9/22 , A61K9/24 , A61K31/44 , A61K31/455 , A61K31/465 , A61K31/60 , A61K9/20
CPC分类号： A61K31/465 , A61K9/209 , A61K31/44 , A61K31/455 , A61K31/60
摘要： The present invention relates to solid pharmaceutical combinations for oral administration comprising nicotinic acid or a nicotinic acid compound or mixtures thereof in an extended release form and an HMG-CoA reductase inhibitor, which are useful for altering lipid levels in subjects suffering from, for example, hyperlipidemia and atherosclerosis, without causing drug-induced hepatotoxicity, myopathy or rhabdomyolysis. The present invention also relates to methods of altering serum lipids in subjects to treat, for example, hyperlipidemia in hyperlipidemics, lipidemia in normolipidemics diagnosed with or predisposed to cardiovascular disease, and atherosclerosis, by administering such oral solid pharmaceutical combinations once per day as a single dose during the evening hours, without causing drug-induced hepatotoxicity, myopathy or rhabdomyolysis, or without causing in at least an appreciable number of individuals drug-induced hepatotoxicity, myopathy or rhabdomyolysis to such a level that discontinuation of such therapy would be required. More particularly, the present invention concerns oral solid pharmaceutical combinations comprised of, for example, (1) an HMG-CoA reductase inhibitor for immediate or extended release, (2) nicotinic acid, a nicotinic acid compound or mixtures thereof, and (3) a swelling agent to form a sustained release composition for extended release of the nicotinic acid or nicotinic acid compound or mixtures thereof for nocturnal or evening dosing for reducing serum lipids and increasing HDL-cholesterol. In accordance with the present invention, and by way of example, a composition for oral administration during the evening hours to alter serum lipids comprised of nicotinic acid and hydroxypropyl methylcellulose in the form of an extended or sustained release tablet or caplet coated with a coating comprising an HMG-CoA reductase inhibitor in immediate release form is disclosed. Also in accordance with the present invention, the pharmaceutical combinations may include a nonsteroidal anti-inflammatory agent for reducing the capacity of nicotinic acid or nicotinic acid compounds to provoke flushing reactions in individuals.
摘要翻译：本发明涉及用于口服给药的固体药物组合，其包含呈延长释放形式的烟酸或烟酸化合物或其混合物和HMG-CoA还原酶抑制剂，其可用于改变患有（例如）高脂血症和动脉粥样硬化，而不引起药物诱导的肝毒性，肌病或横纹肌溶解症。本发明还涉及改变受试者的血脂以治疗例如高脂血症中的高脂血症，诊断患有心血管疾病或易患心血管疾病或易患心血管疾病的血脂正常的血脂异常和动脉粥样硬化的方法，其通过每天一次给予这种口服固体药物组合在不引起药物引起的肝毒性，肌病或横纹肌溶解的情况下，或者至少在可察觉数量的个体中没有导致药物诱导的肝毒性，肌病或横纹肌溶解至需要停止这种治疗的水平。更特别地，本发明涉及口服固体药物组合，其包含例如（1）用于立即或延长释放的HMG-CoA还原酶抑制剂，（2）烟酸，烟酸化合物或其混合物，和（3）溶胀剂以形成延迟释放烟酸或烟酸化合物或其混合物的持续释放组合物用于夜间或夜间给药以减少血脂和增加HDL-胆固醇。根据本发明，并且举例来说，用于在傍晚时间口服给药的组合物，以改变包含烟酸和羟丙基甲基纤维素的血清脂质，所述血清脂质为延伸或缓释片剂或囊片，其形式为涂覆有包衣公开了立即释放形式的HMG-CoA还原酶抑制剂。还根据本发明，药物组合可以包括用于降低烟酸或烟酸化合物在个体中引起潮红反应的能力的非甾体抗炎剂。

2. 发明申请

WO9906052A9 METHODS OF PRETREATING HYPERLIPIDEMIC INDIVIDUALS WITH A FLUSH INHIBITING AGENT PRIOR TO THE START OF SINGLE DAILY DOSE NICOTINIC ACID THERAPY TO REDUCE FLUSHING PROVOKED BY NICOTINIC ACID 审中-公开
标题翻译：在单次日剂量开始使用消融抑制剂之前预防高血压个体的方法NICOTINIC ACID治疗以减少NICOTINIC所提供的扑食
公开(公告)号：WO9906052A9
公开(公告)日：1999-04-29
申请号：PCT/US9815987
申请日：1998-07-31
申请人： KOS PHARMA INC
发明人： CEFALI EUGENIO A
IPC分类号： A61K31/455 , A61K31/60 , A61K31/785 , A61K31/62
CPC分类号： A61K31/455 , A61K31/60 , A61K31/785 , A61K31/40 , A61K31/365 , A61K31/22 , A61K2300/00
摘要： The present invention relates to pretreating individuals with an effective amount of a flush inhibiting agent for a sufficient period of time prior to the start of single daily dose nicotinic acid therapy to reduce the capacity of nicotinic acid to induce flushing reactions in such individuals during nicotinic acid therapy. In accordance with the present invention, the flush inhibiting agents are administered orally one to four times a day, and preferably one to two times per day, for between about 7 to about 14 days prior to the start of the nicotinic acid therapy. Examples of flush inhibiting agents include nonsteroidal anti-inflammatory agents. Aspirin is a prefered flush inhibiting agent and may be orally administered in daily doses of between about 80 mg to about 1000 mg, and preferably between about 80 mg and about 650 mg, and more preferably between about 80 mg and about 325 mg, during the pretreatment period. Also consistent with the present invention, the pretreatment therapy may be continued during and administered concurrently with the nicotinic acid therapy, in which the nicotinic acid is preferably administered once per day as a single dose during the evening hours or before or at bedtime. The nicotinic acid may be administered alone or in combination with HMG-CoA reductase inhibitors as well as other lipid-altering agents, like cholestyramine and colestipol.
摘要翻译：本发明涉及在开始单一日剂量烟酸治疗之前，将有效量的冲洗抑制剂预处理足够的时间以减少在烟酸中这些个体烟酸诱导潮红反应的能力治疗。根据本发明，在开始烟碱酸治疗之前约7至约14天，每天口服一至四次，优选每天一至二次口服冲洗抑制剂。冲洗抑制剂的实例包括非甾体抗炎剂。阿司匹林是优选的冲洗抑制剂，并且可以在约80mg至约1000mg之间，优选约80mg至约650mg，更优选约80mg至约325mg的日剂量下口服施用预处理期。还与本发明一致，预处理治疗可以在烟碱酸治疗期间持续进行，并且其中烟酸优选在傍晚时间或睡前或在睡前时每天以单一剂量施用一次。烟酸可以单独施用或与HMG-CoA还原酶抑制剂以及其他脂质改变剂如考烯胺和考来泊泊组合施用。

3. 发明申请

WO02067852A2 A CONTROLLED RELEASE PHARMACEUTICAL COMPOSITION 审中-公开
标题翻译：受控释放的药物组合物
公开(公告)号：WO02067852A2
公开(公告)日：2002-09-06
申请号：PCT/US0201879
申请日：2002-01-22
申请人： KOS PHARMA INC
发明人： GUTIERREZ-ROCCA JOSE , DUNNE JOSEPHINE , RIOS SAUL A
IPC分类号： A61K9/22 , A61K9/48 , A61K9/52 , A61K9/54 , A61K9/56 , A61K9/58 , A61K9/62 , A61K9/64 , A61K36/31 , A61K
CPC分类号： A61K9/4866 , A61K9/4858
摘要： A sustained/prolonged release pharmaceutical dosage form is disclosed. The form comprises a hard shell capsule and a formulation comprising (a) a water insoluble medicament, (b) a high melting fatty ester, (c) a low viscosity oil, (d) a cellulosic polymer, and (e) a non-ionic surfactant.
摘要翻译：公开了持续/延长释放的药物剂型。该形式包括硬壳胶囊和制剂，其包含（a）水不溶性药物，（b）高熔点脂肪酯，（c）低粘度油，（d）纤维素聚合物，和（e）离子表面活性剂。

4. 发明申请

WO9906035A3 COMBINATIONS OF HMG-CoA REDUCTASE INHIBITORS AND NICOTINIC ACID COMPOUNDS AND METHODS FOR TREATING HYPERLIPIDEMIA ONCE A DAY AT NIGHT 审中-公开
标题翻译： HMG-CoA还原酶抑制剂与烟碱酸化合物的组合以及在晚上一天治疗高脂血症的方法
公开(公告)号：WO9906035A3
公开(公告)日：1999-04-22
申请号：PCT/US9815990
申请日：1998-07-31
申请人： KOS PHARMA INC
发明人： BOVA DAVID J , DUNNE JOSEPHINE
IPC分类号： A61K9/16 , A61K9/20 , A61K9/24 , A61K9/48 , A61K31/455 , A61K45/06 , A61P3/06 , A61P9/10 , A61K31/785
CPC分类号： A61K45/06 , A61K9/2054 , A61K9/209 , A61K31/455 , A61K31/44 , A61K31/40 , A61K31/365 , A61K31/22 , A61K2300/00
摘要： The present invention relates to solid pharmaceutical combinations for oral administration comprising nicotinic acid or a nicotinic acid compound or mixtures thereof in an extended release form and an HMG-CoA reductase inhibitor, which are useful for altering lipid levels in subjects suffering from, for example, hyperlipidemia and atherosclerosis, without causing drug-induced hepatotoxicity, myopathy or rhabdomyolysis. The present invention also relates to methods of altering serum lipids in subjects to treat, for example, hyperlipidemia in hyperlipidemics, lipidemia in normolipidemics diagnosed with or predisposed to cardiovascular disease, and atherosclerosis, by administering such oral solid pharmaceutical combinations once per day as a single dose during the evening hours, without causing drug-induced hepatotoxicity, myopathy or rhabdomyolysis, or without causing in at least an appreciable number of individuals drug-induced hepatotoxicity, myopathy or rhabdomyolysis to such a level that discontinuation of such therapy would be required. More particularly, the present invention concerns oral solid pharmaceutical combinations comprised of, for example, (1) an HMG-CoA reductase inhibitor for immediate or extended release, (2) nicotinic acid, a nicotinic acid compound or mixtures thereof, and (3) a swelling agent to form a sustained release composition for extended release of the nicotinic acid or nicotinic acid compound or mixtures thereof for nocturnal or evening dosing for reducing serum lipids and increasing HDL-cholesterol. In accordance with the present invention, and by way of example, a composition for oral administration during the evening hours to alter serum lipids comprised of nicotinic acid and hydroxypropyl methylcellulose in the form of an extended or sustained release tablet or caplet coated with a coating comprising an HMG-CoA reductase inhibitor in immediate release form is disclosed. Also in accordance with the present invention, the pharmaceutical combinations may include a nonsteroidal anti-inflammatory agent for reducing the capacity of nicotinic acid or nicotinic acid compounds to provoke flushing reactions in individuals.
摘要翻译：本发明涉及用于口服给药的固体药物组合，其包含呈延长释放形式的烟酸或烟酸化合物或其混合物和HMG-CoA还原酶抑制剂，其可用于改变患有（例如）高脂血症和动脉粥样硬化，而不引起药物诱导的肝毒性，肌病或横纹肌溶解症。本发明还涉及改变受试者的血脂以治疗例如高脂血症中的高脂血症，诊断患有心血管疾病或易患心血管疾病或易患心血管疾病的血脂正常的血脂异常和动脉粥样硬化的方法，其通过每天一次给予这种口服固体药物组合在不引起药物引起的肝毒性，肌病或横纹肌溶解的情况下，或者至少在可察觉数量的个体中没有导致药物诱导的肝毒性，肌病或横纹肌溶解至需要停止这种治疗的水平。更特别地，本发明涉及口服固体药物组合，其包含例如（1）用于立即或延长释放的HMG-CoA还原酶抑制剂，（2）烟酸，烟酸化合物或其混合物，和（3）溶胀剂以形成延迟释放烟酸或烟酸化合物或其混合物的持续释放组合物用于夜间或夜间给药以减少血脂和增加HDL-胆固醇。根据本发明，并且举例来说，用于在傍晚时间口服给药的组合物，以改变包含烟酸和羟丙基甲基纤维素的血清脂质，所述血清脂质为延伸或缓释片剂或囊片，其形式为涂覆有包衣公开了立即释放形式的HMG-CoA还原酶抑制剂。还根据本发明，药物组合可以包括用于降低烟酸或烟酸化合物在个体中引起潮红反应的能力的非甾体抗炎剂。

5. 发明申请

WO9521611A3 Compositions comprising a mast cell degranulation-blocking agent for treatment of endogenous, painful gastrointestinal conditions of non-inflammatory,nonulcerative origin 审中-公开
标题翻译：组合物，其包含用于治疗非炎性，非溃疡性起源的内源性，疼痛性胃肠道疾病的肥大细胞脱颗粒阻断剂
公开(公告)号：WO9521611A3
公开(公告)日：1995-10-05
申请号：PCT/US9501392
申请日：1995-02-09
申请人： KOS PHARMA INC
发明人： THEOHARIDES THEHARIS C
IPC分类号： A61K31/00 , A61K31/13 , A61K31/135 , A61K31/35 , A61K31/415 , A61K31/417 , A61K31/445 , A61K31/495 , A61K31/55 , A61K31/565 , A61K38/09 , A61P1/00 , A61P1/06 , A61K31/575
CPC分类号： A61K38/09 , A61K31/00 , A61K31/13 , A61K31/135 , A61K31/35 , A61K31/415 , A61K31/417 , A61K31/445 , A61K31/495 , A61K31/55 , A61K31/565 , Y10S514/01 , A61K2300/00
摘要： A method for treating endogenous, painful gastrointestinal conditions of non-inflammatory, non-ulcerative origin, such as abdominal migraine and irritable bowel syndrome, entails administering a pharmacologically effective amount of a mast cell degranulation-blocking agent, e.g. a naturally occurring polyamine, a heterocyclic histamine-1 receptor antagonist, a histamine-3 receptor agonist or an anti-female sex hormone.

6. 发明申请

WO2004022126A3 METHOD OF TREATING A SYSTEMIC DISEASE 审中-公开
标题翻译：治疗系统性疾病的方法
公开(公告)号：WO2004022126A3
公开(公告)日：2004-11-18
申请号：PCT/US0327246
申请日：2003-09-03
申请人： KOS PHARMA INC
发明人： ADJEI AKWETE , GENOVA PERRY , ZHU YAPING
IPC分类号： A61K9/00 , A61K9/12 , A61K9/14 , A61L9/04 , A61M20060101 , A61M11/00
CPC分类号： A61K9/008
摘要： A method of treating a systemic disease in a patient in need of such treatment is l disclosed. The method comprising maintaining the inspiratory flow rate and volume of the patient to a certain value and then administering a medicament aerosol formulation to the patient using a breath activated inhalation device.
摘要翻译：公开了一种治疗需要这种治疗的患者的全身性疾病的方法。该方法包括将患者的吸气流速和体积保持在一定值，然后使用呼吸激活吸入装置向患者施用药物气溶胶制剂。

7. 发明申请

WO9805354A3 TREATMENT OF STRESS-INDUCED SKIN DISEASE BY CORTICOTROPIN RELEASING HORMONE ANTAGONISTS AND SKIN MAST CELL DEGRANULATION INHIBITORS 审中-公开
标题翻译：通过CORTICOTROPIN释放激素拮抗剂和皮肤细胞降解抑制剂治疗应激诱导的皮肤病
公开(公告)号：WO9805354A3
公开(公告)日：1998-05-14
申请号：PCT/US9713776
申请日：1997-08-06
申请人： KOS PHARMA INC
发明人： THEOHARIDES THEOHARIS C
IPC分类号： A61K38/22 , A61K39/00 , A61K31/00 , A61K38/00 , A61K39/395
CPC分类号： A61K45/06 , A61K31/352 , A61K31/495 , A61K38/2228 , A61K2300/00
摘要： A method of reducing or blocking a stress-related atopic skin disease such as exzema or urticaria in a subject comprising administering to the patient an agent that antagonizes CRH-induced activation of skin mast cells, the agent being used alone or together with a second agent that inhibits activation of skin mast cells. Such agents include compositions that reduce the production or secretion of CRH, neurotensin or somatostatin or an agent that inhibits the physiological action of CRH, neurotensin or somostatin on skin mast cells. The effects of CRH on skin mast cells can also be inhibited by histamine-3 receptor antagonists and by inhibitors of the phosphorylation of skin mast cell moesin.

8. 发明公开

EP0866799A4 APOLIPOPROTEIN E2 AND TREATMENT OF ALZHEIMER'S DISEASE 失效
标题翻译：载脂蛋白E2与阿尔茨海默病众神之治疗
公开(公告)号：EP0866799A4
公开(公告)日：2000-08-23
申请号：EP96937887
申请日：1996-10-31
申请人： KOS PHARMA INC , UNIV BOSTON
发明人： ZANNIS VASSILIS I , ALESHKOV SERGIE B
IPC分类号： A01K67/027 , A61K38/00 , C07K14/775 , C12N5/00 , C12N5/10 , C12N15/09 , C12R1/91 , C07K1/00 , C12N15/00
CPC分类号： C07K14/775 , A61K38/00
摘要： Recombinant apolipoprotein E2 (apoE2) which binds to amyloid peptide A beta .
摘要翻译：重组载脂蛋白E2（APOE2），其结合至淀粉样肽的Aβ。

9. 发明公开

EP1274717A4 COMPOUNDS AND METHODS FOR LOWERING CHOLESTEROL LEVELS WITHOUT INDUCING HYPERTRIGLYCERIDEMIA 有权
标题翻译：化合物和方法降低胆固醇MIRROR时不感应高甘油三酯血症
公开(公告)号：EP1274717A4
公开(公告)日：2004-07-14
申请号：EP01926716
申请日：2001-04-06
申请人： KOS PHARMA INC , UNIV BOSTON
发明人： ZANNIS VASSILIS I , KYPREOS KYRIAKOS E
IPC分类号： C12N15/09 , A61K35/76 , A61K38/00 , A61K48/00 , A61P3/06 , A61P9/10 , C07K14/775 , C12N5/08 , C07H21/04
CPC分类号： C07K14/775 , A61K38/00 , A61K48/00 , C12N2799/021

10. 发明公开

EP1007119A4 BREATH COORDINATED INHALER 失效
标题翻译：气雾
公开(公告)号：EP1007119A4
公开(公告)日：2001-08-29
申请号：EP98914481
申请日：1998-04-03
申请人： KOS PHARMA INC
发明人： HAUSER STEPHEN G
IPC分类号： A61M15/00 , A61M11/00
CPC分类号： A61M15/0091 , A61M15/0023 , A61M15/008 , A61M15/0096
摘要： An improved breath coordinated inhaler (10) is provided for administering medication to a patient in aerosol form for respiratory inhalation therapy. The improved inhaler (10) comprises a compact housing (18) adapted to receive and support a medication canister (12), including a valve assembly (14) actuated to deliver a dosage of the medication in aerosol form. The housing (18) includes a plunger mounted at a first end thereof for displacing the canister against a spray nozzle (24) located at a second end of the housing to actuate the valve assembly (14), and deliver the medication through a mouthpiece (26) to the patient. The plunger (36) is associated with a seal arrangement for venting the housing (18) when the plunger is depressed to allow the patient to draw in air in timed relation to the medication delivery, and to substantially reseal the housing (18) against ingress of contaminants when the plunger (36) is released.
摘要翻译：提供改进的呼吸协调式吸入器（10），用于以气雾剂形式向患者施用用于呼吸吸入治疗的药物。改进的吸入器（10）包括适于接收和支撑药物罐（12）的紧凑壳体（18），包括阀组件（14），所述阀组件被致动以递送一定剂量的气雾剂形式的药物。壳体（18）包括安装在其第一端的柱塞，用于抵靠位于壳体的第二端处的喷嘴（24）移动罐以致动阀组件（14），并且将药物递送通过咬嘴 26）给患者。柱塞（36）与用于在柱塞被压下时使壳体（18）排气以允许患者相对于药物输送定时吸入空气并且基本上重新密封壳体（18）以防止进入当柱塞（36）被释放时污染物的量。

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