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1. 发明申请

WO1995021814A1 NOVEL DERIVATIVES OF TETRAMETHYLCYCLOPROPANE 审中-公开
标题翻译：四氢呋喃的新衍生物
公开(公告)号：WO1995021814A1
公开(公告)日：1995-08-17
申请号：PCT/US1995001388
申请日：1995-02-08
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM , STERLING, Jeff , HERZIG, Yaacov , BIALER, Meir , HAJ-YEHIA, Abdullah , YAGEN, Boris
发明人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM
IPC分类号： C07C233/58
CPC分类号： C07C237/22 , C07C233/58
摘要： The present invention relates to derivatives of 2,2,3,3-tetramethylcyclopropane carboxylic acid (TMCA) of general formula (I), wherein R is a lower alkyl group (C1-C6), an aryl group, an aralkyl group or an amide of general formula (II), where R1 and R2 are the same or different and may be a hydrogen, a lower alkyl group (C1-C6), an aryl group or an aralkyl group, and n=0-3, to their racemic mixtures and the D and L enantiomers. The invention also relates to processes for the preparation of said compounds and for pharmaceutical preparations comprising same. The new compounds show improved activity against epilepsy.
摘要翻译：本发明涉及通式（I）的2,2,3,3-四甲基环丙烷羧酸（TMCA）的衍生物，其中R是低级烷基（C1-C6），芳基，芳烷基或酰胺，其中R 1和R 2相同或不同，并且可以是氢，低级烷基（C 1 -C 6），芳基或芳烷基，并且n = 0-3。外消旋混合物和D和L对映异构体。本发明还涉及制备所述化合物和包含其的药物制剂的方法。新化合物显示改善的针对癫痫的活性。

2. 发明申请

WO1995018617A1 1-AMINOINDAN DERIVATIVES AND COMPOSITIONS THEREOF 审中-公开
标题翻译： 1-氨基嘌呤衍生物及其组合物
公开(公告)号：WO1995018617A1
公开(公告)日：1995-07-13
申请号：PCT/US1995000245
申请日：1995-01-09
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TECHNION RESEARCH AND DEVELOPMENT FOUNDATION LTD. , COHEN, Sasson , HERZIG, Yaacov , LEVY, Ruth , SPEISER, Tzipora , SHIRVAN, Mitchell , STERLING, Jeff , VEINBERG, Alex , YOUDIM, Moussa, B., H. , FINBERG, John, P., M. , SKLARZ, Benjamin , SAYAG, Naim
发明人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TECHNION RESEARCH AND DEVELOPMENT FOUNDATION LTD.
IPC分类号： A61K31/495
CPC分类号： C07C237/04 , A61K31/135 , A61K31/137 , A61K31/165 , A61K31/166 , A61K31/167 , A61K31/18 , A61K31/195 , A61K31/215 , A61K31/216 , A61K31/24 , A61K31/27 , A61K31/275 , A61K31/277 , C07C209/88 , C07C211/42 , C07C213/10 , C07C215/44 , C07C217/74 , C07C233/06 , C07C233/23 , C07C233/74 , C07C2602/08 , C07C2602/10 , A61K2300/00
摘要： Novel derivatives of 1-aminoindan and their salts are described. Parkinson's disease, dementia, epilepsy, convulsions, seizures, acute neurological traumatic disorder or neurotrauma are treated by administering a compound of formula (I).
摘要翻译：描述了1-氨基茚满及其盐的新型衍生物。通过施用式（I）化合物治疗帕金森病，痴呆，癫痫，抽搐，癫痫发作，急性神经外伤性疾病或神经损伤。

3. 发明申请

WO1998002152A1 PHARMACEUTICAL COMPOSITIONS COMPRISING S-(-)-N-PROPARGYL-1-AMINO INDAN 审中-公开
标题翻译：包含S - （ - ） - N-PROPARGYL-1-AMINO INDAN的药物组合物
公开(公告)号：WO1998002152A1
公开(公告)日：1998-01-22
申请号：PCT/IL1997000205
申请日：1997-06-20
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TECHNION RESEARCH AND DEVELOPMENT FOUNDATION LTD. , LEVY, Ruth , YOUDIM, Moussa, B., H. , FINBERG, John, P., M. , COHEN, Sasson , STERLING, Jeff
发明人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TECHNION RESEARCH AND DEVELOPMENT FOUNDATION LTD.
IPC分类号： A61K31/135
CPC分类号： C07C211/42 , A61K31/135 , C07C2602/08 , Y10S514/878 , Y10S514/879 , Y10S514/903
摘要： Pharmaceutical compositions for the treatment of a neurological disorder or neurotrauma or for improving memory in a patient, comprising a therapeutically effective amount of S-(-)-N-propargyl-1-aminoindan or a pharmaceutically acceptable salt thereof as active ingredient, and a pharmaceutically active carrier. The pharmaceutical compositions are adapted, in particular for treating a neurological disorder or neurotrauma involving damage caused to the central or peripheral nervous system as a result of ischemic damage, stroke, hypoxia or anoxia, neurodegenerative diseases, Parkinson's Disease, Alzheimer's Disease, neurotoxic injury, head trauma injury, spinal trauma injury or any other form of nerve damage.
摘要翻译：用于治疗神经障碍或神经损伤或改善患者记忆力的药物组合物，其包含治疗有效量的S - （ - ） - N-炔丙基-1-氨基茚满或其药学上可接受的盐作为活性成分，和药学活性载体。该药物组合物特别用于治疗由于缺血性损伤，中风，缺氧或缺氧引起的对中枢或周围神经系统造成的损伤的神经障碍或神经损伤，神经变性疾病，帕金森病，阿尔茨海默病，神经毒性损伤，头部创伤，脊髓损伤或任何其他形式的神经损伤。

4. 发明申请

WO1997012583A2 STABLE COMPOSITIONS CONTAINING N-PROPARGYL-1-AMINOINDAN 审中-公开
标题翻译：含有N-丙基-1-氨基茚的稳定组合物
公开(公告)号：WO1997012583A2
公开(公告)日：1997-04-10
申请号：PCT/IL1996000115
申请日：1996-09-18
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , BERGER PESKIN, Tirtsah , CACIULARU, Fanny
发明人： TEVA PHARMACEUTICAL INDUSTRIES LTD.
IPC分类号： A61K00/00
CPC分类号： A61K9/2018 , A61K31/135
摘要： A pharmaceutical composition comprising as active ingredient a racemic, S(-), and R(+)-N-propargyl-1-aminoindan or a pharmaceutically acceptable salt thereof, and at least 60 % by weight of at least one pentahydric or hexahydric alcohol. Optionally the composition may contain citric acid and magnesium stearate.
摘要翻译：一种药物组合物，其包含作为活性成分的外消旋的S（ - ）和R（+） - N-炔丙基-1-氨基茚满或其药学上可接受的盐，和至少60重量％的至少一种五元或六元醇。任选地，组合物可以含有柠檬酸和硬脂酸镁。

5. 发明申请

WO1995011016A1 R-ENANTIOMER OF N-PROPARGYL-1-AMINOINDAN, SALTS, COMPOSITIONS AND USES THEREOF 审中-公开
标题翻译： N-丙基-1-氨基茚的R-增效剂，其盐，组合物及其用途
公开(公告)号：WO1995011016A1
公开(公告)日：1995-04-27
申请号：PCT/US1994011567
申请日：1994-10-12
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TECHNION RESEARCH AND DEVELOPMENT FOUNDATION, LTD. , YOUDIM, Moussa, B., H. , FINBERG, John, P., M. , LEVY, Ruth , STERLING, Jeffrey , LERNER, David , BERGER-PASKIN, Tirtsah , YELLIN, Haim , VEINBERG, Alex
发明人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TECHNION RESEARCH AND DEVELOPMENT FOUNDATION, LTD.
IPC分类号： A61K31/135
CPC分类号： C07C211/30 , A61K31/195 , A61K31/215 , A61K45/06 , C07C2602/08 , Y02A50/395 , A61K2300/00
摘要： The subject invention provides R(+)-N-propargyl-1-aminoindan and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions containing same. The subject invention also provides methods of treating a subject afflicted with Parkinson's disease, a memory disorder, dementia, depression, hyperactive syndrome, an affective illness, a neurodegenerative disease, a neurotoxic injury, brain ischemia, a head trauma injury, a spinal trauma injury, schizophrenia, an attention deficit disorder, multiple sclerosis, or withdrawal symptoms, using R(+)-N-propargyl-1-aminoindan or the pharmaceutically acceptable salt of the subject invention. The subject invention further provides a method of preventing nerve damage in a subject. Finally, the subject invention provides methods of preparing R(+)-N-propargyl-1-aminoindan, a salt thereof, and racemic N-propargyl-1-aminoindan.
摘要翻译：本发明提供了R（+） - N-炔丙基-1-氨基茚满及其药学上可接受的盐，以及含有它们的药物组合物。本发明还提供了治疗患有帕金森病，记忆障碍，痴呆，抑郁症，多动症综合征，情感疾病，神经变性疾病，神经毒性损伤，脑缺血，头部创伤损伤，脊髓损伤损伤，精神分裂症，注意力缺陷障碍，多发性硬化或戒断症状，使用本发明的R（+） - N-炔丙基-1-氨基茚满或其药学上可接受的盐。本发明进一步提供一种预防受试者的神经损伤的方法。最后，本发明提供了制备R（+） - N-炔丙基-1-氨基茚满其盐和外消旋的N-炔丙基-1-氨基茚满的方法。

6. 发明申请

WO2014058979A2 LAQUINIMOD FOR REDUCING THALAMIC DAMAGE IN MULTIPLE SCLEROSIS 审中-公开
标题翻译：用于减少多发性硬化性脑血管损伤的LAQUINIMOD
公开(公告)号：WO2014058979A2
公开(公告)日：2014-04-17
申请号：PCT/US2013/064061
申请日：2013-10-09
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , FILIPPI, Massimo , COMI, Giancarlo , ROCCA, Maria, Assunta
发明人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , FILIPPI, Massimo , COMI, Giancarlo , ROCCA, Maria, Assunta
IPC分类号： A61K31/4704
CPC分类号： A61K31/4704 , A61K9/0053
摘要： This invention provides methods for inhibiting or reducing thalamic damage in a subject comprising administering to the subject an amount of laquinimod, wherein the subject is a human patient afflicted with a form of multiple sclerosis or presenting a clinically isolated syndrome who has been determined to have thalamic damage at baseline, a subject afflicted with a disease or disorder other than a form of multiple sclerosis or a clinically isolated syndrome, or a subject not afflicted with a form of multiple sclerosis or a presenting clinically isolated syndrome, and laquinimod and laquinimod pharmaceutical compositions for use thereof. This invention also provides methods for inhibiting or reducing tremor or spasticity in a subject afflicted by tremor or spasticity, comprising administering to the subject an amount of laquinimod, and laquinimod and laquinimod pharmaceutical compositions for use thereof.
摘要翻译：本发明提供了抑制或减少受试者的丘脑损伤的方法，其包括向受试者施用一定量的拉喹莫德，其中受试者是患有多发性硬化症形式的人类患者或呈现临床分离的综合征，其被确定为具有丘脑患有基线时的损伤，患有多发性硬化症或临床分离综合征形式的疾病或障碍的受试者或未患有多发性硬化症或呈现临床分离综合征形式的受试者，以及拉喹莫德和拉喹莫德药物组合物使用它。本发明还提供了抑制或减轻由震颤或痉挛状态所引起的震颤或痉挛状态的方法，其包括给予受试者一定量的用于其的拉喹莫德和拉喹莫德和拉喹莫德药物组合物。

7. 发明申请

WO1998028255A1 PREPARATION OF GABAPENTIN 审中-公开
标题翻译：加巴酚的制备
公开(公告)号：WO1998028255A1
公开(公告)日：1998-07-02
申请号：PCT/US1997023164
申请日：1997-12-24
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , PESACHOVICH, Michael , SINGER, Claude , PILARSKI, Gideon
发明人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC.
IPC分类号： C07C61/06
CPC分类号： C07C227/42 , C07C229/28 , C07C2601/14
摘要： There is disclosed a method of converting gabapenting hydrochloride substantially free of inorganic salts to gabapenting form II. The method comprises the steps of: (1) obtaining gabapentin hydrochloride that is substantially free of inorganic salts; (2) mixing a solution of the gabapenting hydrochloride with an additional amine in a first solvent so as to obtain a precipitate comprising gabapenting; and then (3) recovering gabapentin form II from the precipitate. The precipitated gabapentin is a novel polymorphic form of gabapentin possessing a crystalline structure characterized by novel sets of peaks in the powder X-ray diffraction pattern and in the FTIR spectra. This newly disclosed polymorph of gabapentin is characterized herein as gabapentin form III. The recovery step may comprise, for example, one of two alternative methods, slurrying the gabapentin form II in methanol, and then filtering the suspension to obtain gabapentin form II, or solubilizing the gabapentin form III in methanol with heating by reflux, and then cooling the solution to obtain gabapentin form II by crystallization.
摘要翻译：公开了一种将基本上不含无机盐的盐酸氢化盐转化为耙状II的方法。该方法包括以下步骤：（1）获得基本上不含无机盐的盐酸加巴喷丁; （2）在第一溶剂中将加巴喷丁盐酸盐溶液与另外的胺混合，以获得包含加砂的沉淀物; 然后（3）从沉淀物中回收加巴喷丁II型。沉淀的加巴喷丁是一种具有特征在于粉末X射线衍射图和FTIR光谱中新颖的峰组的加巴喷丁的新型多晶型物。这种新公开的加巴喷丁多晶型物在本文中被表征为加巴喷丁形式III。回收步骤可以包括例如两种替代方法之一，将加巴喷丁II型在甲醇中制浆，然后过滤悬浮液以获得形式II的加巴喷丁，或者通过回流加热将加巴喷丁形式III溶解在甲醇中，然后冷却通过结晶获得形式II的加巴喷丁的溶液。

8. 发明申请

WO1996040632A1 10-THIO-SUBSTITUTED 1,8-DIHYDROXY-9(10H)-ANTHRACENONE DERIVATIVES FOR USE IN THE TREATMENT OF INFLAMMATORY CONDITIONS 审中-公开
标题翻译：用于治疗炎症条件的10 -ThIO-替代的1,8-二羟基-9（10H） - 亚硝基苯酮衍生物
公开(公告)号：WO1996040632A1
公开(公告)日：1996-12-19
申请号：PCT/IB1996000652
申请日：1996-06-03
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD.
发明人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , MUELLER, Klaus , HUANG, Hsu-Shan , WIEGREBE, Wolfgang
IPC分类号： C07C323/52
CPC分类号： C07C323/22 , C07C323/35 , C07C323/52 , Y10S514/863
摘要： 10-Thio-substituted 1,8-dihydroxy-9(10H)-anthracenones of formula (III), in which R represents a substituted alkyl group or a substituted phenyl group which is useful in the treatment of inflammatory conditions, especially psoriasis.
摘要翻译：式（III）的10-硫代取代的1,8-二羟基-9（10H） - 蒽基酮，其中R表示可用于治疗炎性疾病，特别是牛皮癣的取代的烷基或取代的苯基。

9. 发明申请

WO1996040623A1 2-SUBSTITUTED 1,8-DIHYDROXY-9(10H)-ANTRACENONE AS PROLIFERATION AND 5-LIPOXYGENASE INHIBITORS 审中-公开
标题翻译： 2-取代的1,8-二羟基-9（10H） - 丙酮酮作为增殖剂和5-LIPOXYGENASE抑制剂
公开(公告)号：WO1996040623A1
公开(公告)日：1996-12-19
申请号：PCT/IB1996000596
申请日：1996-06-03
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD.
发明人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , MUELLER, Klaus , PRINZ, Helge , WIEGREBE, Wolfgang
IPC分类号： C07C259/06
CPC分类号： C07C59/90 , C07C69/738 , C07C69/94 , C07C259/06 , C07C259/10 , C07C2603/24
摘要： 2-substituted 1,8-dihydroxy-9(10H)-antrhacenones of general formula (I), therapeutic compositions containing at least one 2-substituted 1,8-dihydroxy-9(10H)-anthracenone compound and methods of treating inflammatory conditions especially psoriasis are provided. In said formula, Y represents a linear or branched chain alkyl group having 1 to 10 carbon atoms, a phenylalkyl group having 7 to 10 carbon atoms, a phenylacyl group having 7 to 10 carbon atoms, an amino group, or an amino group substituted with a linear or branched chain alkyl group having 1 to 10 carbon atoms; and X represents a hydroxyl group, an ester group substituted with a straight or branched chain alkyl group having 1 to 10 carbon atoms, an amino group, amino group substituted with a straight or branched chain alkyl group having 1 to 10 carbon atoms, a hydroxilamine group, or an N-alkyl substituted hydroxylamine, said N-alkyl being straight or branched chain and having 1 to 10 carbon atoms, with the proviso that when X is hydroxyl, Y is not an alkyl group having 1 to 3 carbon atoms or CH2 Phenyl-4.
摘要翻译：具有通式（I）的2-取代的1,8-二羟基-9（10H） - 蒽醌，含有至少一种2-取代的1,8-二羟基-9（10H） - 蒽基蒽醌化合物的治疗组合物和治疗炎性病症的方法特别提供牛皮癣。在所述式中，Y表示碳原子数1〜10的直链或支链烷基，碳原子数7〜10的苯基烷基，碳原子数7〜10的苯基酰基，氨基或被具有1至10个碳原子的直链或支链烷基; X表示羟基，被碳原子数1〜10的直链或支链烷基取代的酯基，氨基，被碳原子数1〜10的直链或支链烷基取代的氨基，羟基胺基团或N-烷基取代的羟胺，所述N-烷基是直链或支链并且具有1-10个碳原子，条件是当X是羟基时，Y不是具有1至3个碳原子的烷基或CH2 苯基-4。

10. 发明申请

WO1995035073A1 OPHTHALMIC DELIVERY SYSTEM 审中-公开
标题翻译： OPHTHALMIC交付系统
公开(公告)号：WO1995035073A1
公开(公告)日：1995-12-28
申请号：PCT/US1995007789
申请日：1995-06-19
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , THE BEN GURION UNIVERSITY OF THE NEGEV , LEMON COMPANY
发明人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , THE BEN GURION UNIVERSITY OF THE NEGEV , LEMON COMPANY , COHEN, Smadar , LOBEL, Esther
IPC分类号： A61F02/14
CPC分类号： A61K9/0048 , A61K47/36 , Y10S514/912
摘要： The present invention relates to formulations particularly well suited for use as delivery systems in the delivery of an active agent to the eye. The formulations comprise an alginate having a particular proportion of guluronic acid.
摘要翻译：本发明涉及特别适合用作将活性剂递送至眼睛的递送系统的制剂。制剂包含具有特定比例的古罗糖醛酸的藻酸盐。

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