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1. 发明申请

WO2006057912A2 RASAGILINE ORALLY DISINTEGRATING COMPOSITIONS 审中-公开
公开(公告)号：WO2006057912A2
公开(公告)日：2006-06-01
申请号：PCT/US2005/041882
申请日：2005-11-17
申请人： TEVA PHARMACEUTICAL INDUSTRIES, LTD. , TEVA PHARMACEUTICALS USA, INC , PATASHNIK, Shulamit , LICHT, Daniella , GILBERT, Adrian
发明人： PATASHNIK, Shulamit , LICHT, Daniella , GILBERT, Adrian
IPC分类号： A61K31/4166
CPC分类号： A61K9/0056 , A61K9/2018 , A61K9/2054 , A61K9/2059 , A61K31/135 , A61K31/4166
摘要： This invention provides a solid pharmaceutical composition comprising rasagiline or a pharmaceutically acceptable salt of rasagiline, and particles having a non-filamentous microstructure of at least two sugar alcohols. This invention also provides a solid pharmaceutical composition comprising rasagiline or a pharmaceutically acceptable salt of rasagiline, a mixture of a disintegrant, a flow agent and particles having a non-filamentous microstructure of at least two sugar alcohols, a supplemental sugar alcohol, a supplemental flow agent, and a supplemental disintegrant. This invention further provides a method of treating a subject afflicted with Parkinson’s disease comprising administering to the subject a therapeutically effective amount of the solid pharmaceutical composition, thereby treating the subject. Finally, this invention provides a process of making such solid pharmaceutical compositions.
摘要翻译：本发明提供了一种固体药物组合物，其包含雷沙吉兰或雷沙吉兰的药学上可接受的盐，以及具有至少两种糖醇的非丝状微结构的颗粒。本发明还提供固体药物组合物，其包含雷沙吉兰或雷沙吉兰的药学上可接受的盐，崩解剂，流动剂和具有至少两种糖醇的非丝状微结构的颗粒的混合物，补充糖醇，补充流代理和补充崩解剂。本发明还提供了治疗患有帕金森病的受试者的方法，其包括向受试者施用治疗有效量的固体药物组合物，从而治疗受试者。最后，本发明提供制备这种固体药物组合物的方法。

2. 发明申请

WO2004071421A3 SUSTAINED RELEASE FORMULATION OF N-(2-PROPYLPENTANOYL) GLYCINAMIDE AND RELATED COMPOUNDS 审中-公开
标题翻译： N-（2-丙酰氨基）甘氨酰胺及相关化合物的持续释放配方
公开(公告)号：WO2004071421A3
公开(公告)日：2004-11-18
申请号：PCT/US2004003281
申请日：2004-02-05
申请人： TEVA PHARMA , TEVA PHARMACEUTICAL USA INC , LICHT DANIELLA , LOVINGER IOANA , ABD-ELHAI SUHER , DAGAN-LION MAZZI , GILBERT ADRIAN , LEIBOVITCH NOA , COHEN SASSON , LEVY RUTH
发明人： LICHT DANIELLA , LOVINGER IOANA , ABD-ELHAI SUHER , DAGAN-LION MAZZI , GILBERT ADRIAN , LEIBOVITCH NOA , COHEN SASSON , LEVY RUTH
IPC分类号： A61K9/20 , A61K9/22 , A61K31/16 , A61K31/19
CPC分类号： A61K31/16 , A61K9/2009 , A61K9/2013 , A61K9/2018 , A61K9/2054 , A61K31/19
摘要： The subject provides a sustained release tablet comprising the following components: a) a uniform admixture of an active ingredient selected from the group consisting of valproic sodium acid, a pharmaceutically acceptable salt or ester of valproic acid, divalproex sodium, valpromide and a compound having the structure of formula (I) or formula (II), wherein R1, R2, and R3 are independently the same or different and are hydrogen, a C1-C6 alkyl group, an aralkyl group, or an aryl group, and n is an integer which is greater than or equal to 0 and less than or equal to 3; and a binder, and b) a hydroxypropylmethyl cellulose, a process for manufacturing the tablet and a method of treating neuropathic pain, epilepsy, mania in bipolar disorder, a headache disorder, pain or of effecting pain prophylaxis in a subject.
摘要翻译：受试者提供了包含以下组分的持续释放片剂：a）选自丙戊酸钠，丙戊酸的药学上可接受的盐或酯，二价丙磺酸钠，valpromide和具有下列成分的化合物的活性成分的均匀混合物：式（I）或式（II）的结构，其中R 1，R 2和R 3独立地相同或不同，为氢，C 1 -C 6烷基，芳烷基或芳基，n为整数大于或等于0且小于或等于3; 和粘合剂，以及b）羟丙基甲基纤维素，制备片剂的方法以及治疗神经性疼痛，癫痫，双相情感障碍中的躁狂症，头痛障碍，疼痛或对受试者进行疼痛预防的方法。

3. 发明申请

WO2004071421A2 SUSTAINED RELEASE FORMULATION OF N-(2-PROPYLPENTANOYL) GLYCINAMIDE AND RELATED COMPOUNDS 审中-公开
标题翻译： N-（2-丙酰氨基）甘氨酰胺及相关化合物的持续释放配方
公开(公告)号：WO2004071421A2
公开(公告)日：2004-08-26
申请号：PCT/US2004/003281
申请日：2004-02-05
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICAL USA, INC. , LICHT, Daniella , LOVINGER, Ioana , ABD-ELHAI, Suher , DAGAN-LION, Mazzi , GILBERT, Adrian , LEIBOVITCH, Noa , COHEN, Sasson , LEVY, Ruth
发明人： LICHT, Daniella , LOVINGER, Ioana , ABD-ELHAI, Suher , DAGAN-LION, Mazzi , GILBERT, Adrian , LEIBOVITCH, Noa , COHEN, Sasson , LEVY, Ruth
IPC分类号： A61K
CPC分类号： A61K31/16 , A61K9/2009 , A61K9/2013 , A61K9/2018 , A61K9/2054 , A61K31/19
摘要： The subject provides a sustained release tablet comprising the following components: a) a uniform admixture of an active ingredient selected from the group consisting of valproic sodium acid, a pharmaceutically acceptable salt or ester of valproic acid, divalproex sodium, valpromide and a compound having the structure: (I) wherein R 1 , R 2 , and R 3 are independently the same or different and are hydrogen, a C 1 -C 6 alkyl group, an aralkyl group, or an aryl group, and n is an integer which is greater than or equal to 0 and less than or equal to 3; and a binder, and b) a hydroxypropylmethyl cellulose, a process for manufacturing the tablet and a method of treating neuropathic pain, epilepsy, mania in bipolar disorder, a headache disorder, pain or of effecting pain prophylaxis in a subject.
摘要翻译：受试者提供了包含以下组分的持续释放片剂：a）选自丙戊酸钠，丙戊酸的药学上可接受的盐或酯，二价丙磺酸钠，valpromide和具有下列成分的化合物的活性成分的均匀混合物：结构式（I）其中R1，R2和R3独立地相同或不同，为氢，C1-C6烷基，芳烷基或芳基，n为大于或等于 0和小于等于3; 和粘合剂，以及b）羟丙基甲基纤维素，制备片剂的方法以及治疗神经性疼痛，癫痫，双相情感障碍中的躁狂症，头痛障碍，疼痛或对受试者进行疼痛预防的方法。

4. 发明申请

WO2006057912A3 RASAGILINE ORALLY DISINTEGRATING COMPOSITIONS 审中-公开
标题翻译： RASAGILINE ORAZY DISINTEGRATING组合物
公开(公告)号：WO2006057912A3
公开(公告)日：2006-08-17
申请号：PCT/US2005041882
申请日：2005-11-17
申请人： TEVA PHARMA , TEVA PHARMA , PATASHNIK SHULAMIT , LICHT DANIELLA , GILBERT ADRIAN
发明人： PATASHNIK SHULAMIT , LICHT DANIELLA , GILBERT ADRIAN
IPC分类号： A61K31/135
CPC分类号： A61K9/0056 , A61K9/2018 , A61K9/2054 , A61K9/2059 , A61K31/135 , A61K31/4166
摘要： This invention provides a solid pharmaceutical composition comprising rasagiline or a pharmaceutically acceptable salt of rasagiline, and particles having a non-filamentous microstructure of at least two sugar alcohols. This invention also provides a solid pharmaceutical composition comprising rasagiline or a pharmaceutically acceptable salt of rasagiline, a mixture of a disintegrant, a flow agent and particles having a non-filamentous microstructure of at least two sugar alcohols, a supplemental sugar alcohol, a supplemental flow agent, and a supplemental disintegrant. This invention further provides a method of treating a subject afflicted with Parkinson's disease comprising administering to the subject a therapeutically effective amount of the solid pharmaceutical composition, thereby treating the subject. Finally, this invention provides a process of making such solid pharmaceutical compositions.
摘要翻译：本发明提供了包含雷沙吉兰或雷沙吉兰药学上可接受的盐的固体药物组合物，以及具有至少两种糖醇的非丝状微观结构的颗粒。本发明还提供了一种固体药物组合物，其包含雷沙吉兰或雷沙吉兰药学上可接受的盐，崩解剂，流动剂和具有至少两种糖醇的非丝状微结构的颗粒，补充糖醇，辅助流药剂和补充崩解剂。本发明进一步提供了治疗患有帕金森氏病的受试者的方法，包括给予受试者治疗有效量的固体药物组合物，从而治疗受试者。最后，本发明提供了制备这种固体药物组合物的方法。

5. 发明申请

WO2015112601A1 MODIFIED RELEASE FORMULATIONS OF PRIDOPIDINE 审中-公开
标题翻译： PRIDOPIDINE的改良释放配方
公开(公告)号：WO2015112601A1
公开(公告)日：2015-07-30
申请号：PCT/US2015/012248
申请日：2015-01-21
申请人： IVAX INTERNATIONAL GMBH , TEVA PHARMACEUTICALS USA, INC. , LICHT, Daniella , LOVINGER, Ioana , GUILATT, Laura Yehudit , BASSAN, Merav
发明人： LICHT, Daniella , LOVINGER, Ioana , GUILATT, Laura Yehudit , BASSAN, Merav
IPC分类号： A61K31/451 , C07D211/20 , C07D211/24
CPC分类号： A61K31/451 , A61K9/1617 , A61K9/1652 , A61K9/2009 , A61K9/2054 , A61K9/2059 , A61K9/2068
摘要： The subject invention provides a modified release solid oral dosage form comprising a therapeutically effective amount of Pridopidine or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable rate controlling excipient, wherein the solid oral dosage form provides an in vivo plasma pridopidine concentration profile having a Mean C max of about 1,400 ng/ml or less. The subject invention also provides a method of treating an individual afflicted with a neurodegenerative disease or disease related to dopamine, comprising once daily administration of a modified release solid oral dosage form.
摘要翻译：本发明提供了一种包含治疗有效量的施多替啶或其药学上可接受的盐和至少一种药学上可接受的速率控制赋形剂的改良释放固体口服剂型，其中所述固体口服剂型提供了体内血浆丙泊德定浓度分布，其具有平均Cmax约为1400ng / ml或更低。本发明还提供了治疗患有与多巴胺相关的神经变性疾病或疾病的个体的方法，其包括每日一次施用改良释放固体口服剂型。

6. 发明申请

WO2010085354A1 DELAYED RELEASE RASAGILINE FORMULATION 审中-公开
标题翻译：延迟释放RASAGILINE配方
公开(公告)号：WO2010085354A1
公开(公告)日：2010-07-29
申请号：PCT/US2010/000174
申请日：2010-01-21
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , SAFADI, Muhammad , LICHT, Daniella , COHEN, Rachel , FRENKEL, Anton , KOLTAI, Tamas , ZHOLKOVSKY, Marina
发明人： SAFADI, Muhammad , LICHT, Daniella , COHEN, Rachel , FRENKEL, Anton , KOLTAI, Tamas , ZHOLKOVSKY, Marina
IPC分类号： A01N3/02 , A61K31/135
CPC分类号： A61K9/2893 , A61K9/2013 , A61K9/2018 , A61K9/2054 , A61K9/2059 , A61K9/2846 , A61K9/2886 , A61K31/135 , C07C59/265 , C07C211/42 , C07C2602/08
摘要： Disclosed are formulations of rasagiline base which are designed to delay release of rasagiline while maintaining specific pharmacokinetic properties. Also, disclosed are rasagiline citrate salt and the use and process of manufacture thereof.
摘要翻译：公开了雷沙吉兰碱的制剂，其被设计为延迟雷沙吉兰的释放，同时保持特定的药代动力学性质。还公开了雷沙吉兰柠檬酸盐及其制备方法和用途。

7. 发明申请

WO2004071424A3 IMMEDIATE RELEASE FORMULATION OF N<->(2<->PROPYLPENTANOYL)GLYCINAMIDE 审中-公开
标题翻译：立即释放N - （2 - 丙酰胺）甘氨酰胺的配方
公开(公告)号：WO2004071424A3
公开(公告)日：2005-02-24
申请号：PCT/US2004003346
申请日：2004-02-05
申请人： TEVA PHARMA , TEVA PHARMA , LICHT DANIELLA , ABD-ELHAI SUHER , COHEN RACHEL , DAGAN-LION MAZZI , GILBERT ADRIAN , LEIBOVITCH NOA , COHEN SASSON , LEVY RUTH
发明人： LICHT DANIELLA , ABD-ELHAI SUHER , COHEN RACHEL , DAGAN-LION MAZZI , GILBERT ADRIAN , LEIBOVITCH NOA , COHEN SASSON , LEVY RUTH
IPC分类号： A61K20060101 , A61K9/20 , A61K31/16 , A61K31/19
CPC分类号： A61K31/16 , A61K9/2018 , A61K9/2054 , A61K9/2059 , A61K31/19
摘要： The subject invention provides an immediate release tablet comprising the following components: a) a uniform admixture of an active ingredient selected from the group consisting of valproic sodium acid, a pharmaceutically acceptable salt or ester of valproic acid, divalproex sodium, valpromide and a compound having the structure: wherein R1, R2, and R3 are independently the same or different and are hydrogen, a C1-C6 alkyl group, an aralkyl group, or an aryl group, and n is an integer which is greater than or equal to 0 and less than or equal to 3; and a hydroxypropyl cellulose, and b) a disintegrant, a process for manufacturing the tablet and a method of treating neuropathic pain, epilepsy, mania in bipolar disorder, a headache disorder, pain or of effecting pain prophylaxis in a subject.
摘要翻译：本发明提供了包含以下组分的速释片剂：a）选自丙戊酸钠，丙戊酸的药学上可接受的盐或酯，二价丙磺酸钠，valpromide和具有下列成分的化合物的活性成分的均匀混合物：结构式：其中R1，R2和R3独立地相同或不同，为氢，C1-C6烷基，芳烷基或芳基，n为大于或等于0的整数，小于或等于3; 和羟丙基纤维素，以及b）崩解剂，制造片剂的方法以及治疗受试者中的神经性疼痛，癫痫，躁狂症，双相情感障碍，头痛症，疼痛或疼痛预防的方法。

8. 发明申请

WO2004071424A2 IMMEDIATE RELEASE FORMULATION OF N-(2-PROPYLPENTANOYL)GLYCINAMIDE 审中-公开
标题翻译：立即释放N - （2 - 丙酰胺）甘氨酰胺的配方
公开(公告)号：WO2004071424A2
公开(公告)日：2004-08-26
申请号：PCT/US2004/003346
申请日：2004-02-05
申请人： TEVA PHARMACEUTICAL INDUSTRIES, LTD. , TEVA PHARMACEUTICALS USA, INC. , LICHT, Daniella , ABD-ELHAI, Suher , COHEN, Rachel , DAGAN-LION, Mazzi , GILBERT, Adrian , LEIBOVITCH, Noa , COHEN, Sasson , LEVY, Ruth
发明人： LICHT, Daniella , ABD-ELHAI, Suher , COHEN, Rachel , DAGAN-LION, Mazzi , GILBERT, Adrian , LEIBOVITCH, Noa , COHEN, Sasson , LEVY, Ruth
IPC分类号： A61K
CPC分类号： A61K31/16 , A61K9/2018 , A61K9/2054 , A61K9/2059 , A61K31/19
摘要： The subject invention provides an immediate release tablet comprising the following components: a) a uniform admixture of an active ingredient selected from the group consisting of valproic sodium acid, a pharmaceutically acceptable salt or ester of valproic acid, divalproex sodium, valpromide and a compound having the structure:(F)I or (F) II wherein R 1 , R 2 , and R 3 are independently the same or different and are hydrogen, a C 1 -C 6 alkyl group, an aralkyl group, or an aryl group, and n is an integer which is greater than or equal to 0 and less than or equal to 3; and a hydroxypropyl cellulose, and b) a disintegrant, a process for manufacturing the tablet and a method of treating neuropathic pain, epilepsy, mania in bipolar disorder, a headache disorder, pain or of effecting pain prophylaxis in a subject.
摘要翻译：本发明提供了包含以下组分的速释片剂：a）选自丙戊酸钠，丙戊酸的药学上可接受的盐或酯，二价丙磺酸钠，valpromide和具有下列成分的化合物的活性成分的均匀混合物：结构：（F）I或（F）II其中R1，R2和R3独立地相同或不同，为氢，C1-C6烷基，芳烷基或芳基，n为整数大于或等于0且小于或等于3; 和羟丙基纤维素，以及b）崩解剂，制造片剂的方法以及治疗受试者中的神经性疼痛，癫痫，躁狂症，双相情感障碍，头痛症，疼痛或疼痛预防的方法。

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