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1. 发明申请

WO2011107283A3 FORMULATIONS OF TAUROLIDINE AND METHOD FOR THE PRODUCTION THEREOF 审中-公开
标题翻译： FOR牛磺罗定和方法及其制剂
公开(公告)号：WO2011107283A3
公开(公告)日：2012-07-26
申请号：PCT/EP2011001064
申请日：2011-03-03
申请人： GAMPTEC GMBH , HEBER DIETER , MUELLER BERND
发明人： HEBER DIETER , MUELLER BERND
IPC分类号： A61K47/34 , A61K9/00 , A61K31/549 , A61P31/04 , C07D209/48 , C07D237/32 , C07D285/24 , C07D417/06
CPC分类号： C07D417/06 , A61K9/0024 , A61K9/0056 , A61K9/0095 , A61K31/549 , A61K47/34 , A61L27/54 , C07D209/48 , C07D237/32 , C07D285/24 , A61K2300/00
摘要： The invention relates to a composition comprising taurolidine and/or the hydrolysis products thereof and also a biodegradable (co)polymer or inorganic matrix for use as an implant for treating local infections of the skeleton and soft tissue. A lozenge and a spray solution or gargling solution likewise comprises taurolidine and/or the hydrolysis products thereof and is used in the treatment of throat inflammations, sore throats with difficulty in swallowing, inflammations of the mouth and throat area and laryngitis. A method for producing taurolidine is also disclosed.
摘要翻译：包含牛磺罗定和/或其水解产物和（e）中的可生物降解的（S）（共）聚合物或无机基质用作骨骼和软组织的局部感染的治疗的植入物的组合物。的锭剂和喷雾剂或漱口还包括牛磺罗定和/或其水解产物和在喉感染，咽喉炎的治疗使用时，吞咽困难，口咽和喉炎的炎症。一种用于牛磺罗定的制备方法也被公开。

2. 发明申请

WO2008144500A2 1-METHYL-BENZO[1,2,4]THIADIAZINE, 1-OXIDE DERIVATIVES 审中-公开
标题翻译： 1-甲基苯并[1,2,4]噻二嗪，1-氧化物衍生物
公开(公告)号：WO2008144500A2
公开(公告)日：2008-11-27
申请号：PCT/US2008063884
申请日：2008-05-16
申请人： ANADYS PHARMACEUTICALS INC , ZHOU YUEFEN , BERTOLINI THOMAS , LI LIANSBENG
发明人： ZHOU YUEFEN , BERTOLINI THOMAS , LI LIANSBENG
IPC分类号： C07D285/24 , A61K31/549 , A61K38/21 , A61P31/14
CPC分类号： C07D498/18 , A61K38/212 , A61K38/215 , C07D285/30 , C07D417/04 , C07D417/14 , A61K2300/00
摘要： The invention is directed to l-methyl-benzo[l,2,4]thiadiazine 1 -oxide derivatives and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.
摘要翻译：本发明涉及1-甲基 - 苯并[1,2,4]噻二嗪-1-氧化物衍生物和含有可用于治疗丙型肝炎病毒感染的化合物的药物组合物。

3. 发明申请

WO2008059025A1 NOVEL 2-(2-HYDROXYPHENYL) BENZOTHIADIAZINES USEFUL FOR TREATING OBESITY AND DIABETES 审中-公开
标题翻译：新的2-（2-羟基苯基）苯并二氮杂用于治疗糖尿病和糖尿病
公开(公告)号：WO2008059025A1
公开(公告)日：2008-05-22
申请号：PCT/EP2007/062408
申请日：2007-11-15
申请人： NOVO NORDISK A/S , OLESEN, Preben Houlberg , PETERSEN, Anders Klarskov , NIELSEN, Flemming Elmelund , CHRISTIANSEN, Lise Brown , HANSEN, Holger Claus
发明人： OLESEN, Preben Houlberg , PETERSEN, Anders Klarskov , NIELSEN, Flemming Elmelund , CHRISTIANSEN, Lise Brown , HANSEN, Holger Claus
IPC分类号： C07D285/24 , A61K31/549 , A61P3/04
CPC分类号： C07D285/24
摘要： The present invention relates to novel compounds that act as chemical uncouplers. Compounds of the invention are useful, inter alia, in the treatment, including prevention, of obesity, diabetes and a number of diseases or conditions associated therewith.
摘要翻译：本发明涉及用作化学解偶联剂的新型化合物。本发明的化合物尤其可用于治疗，包括预防肥胖症，糖尿病和与其相关的许多疾病或病症。

4. 发明申请

WO0001376A2 PHARMACEUTICAL COMPOSITIONS AND THEIR USES 审中-公开
标题翻译：药物组合物及其用途
公开(公告)号：WO0001376A2
公开(公告)日：2000-01-13
申请号：PCT/GB9902112
申请日：1999-07-02
申请人： EISAI CO LTD , TURSKI LECHOSLAW , SMITH TERENCE
发明人： TURSKI LECHOSLAW , SMITH TERENCE
IPC分类号： C07D243/02 , A61K31/00 , A61K31/225 , A61K31/35 , A61K31/40 , A61K31/4245 , A61K31/437 , A61K31/47 , A61K31/4725 , A61K31/473 , A61K31/4745 , A61K31/498 , A61K31/4985 , A61K31/5025 , A61K31/513 , A61K31/517 , A61K31/549 , A61K31/551 , A61K31/662 , A61K31/675 , A61K38/00 , A61K38/17 , A61K45/06 , A61P25/00 , A61P25/02 , A61P25/28 , C07D207/44 , C07D215/22 , C07D217/26 , C07D239/91 , C07D239/92 , C07D241/38 , C07D241/44 , C07D285/24 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D471/04 , C07D487/04 , C07D487/12 , C07D491/056 , C07D498/04 , C07D513/04 , C07D517/04
CPC分类号： A61K31/7048 , A61K31/00 , A61K31/225 , A61K31/35 , A61K31/4245 , A61K31/4725 , A61K31/4745 , A61K31/498 , A61K31/4985 , A61K31/513 , A61K31/517 , A61K31/551 , A61K31/675 , A61K38/17 , A61K45/06
摘要： New therapies can be devised based upon a demonstration of the role of glutamate in the pathogenesis of demyelinating disorders. Inhibitors of the interaction of glutamate with the AMPA and/or kainate receptor complex are likely to be useful in treating demyelinating disorders and can be formulated as pharmaceutical compositions.
摘要翻译：可以基于谷氨酸在脱髓鞘病变的发病机制中的作用的证明来设计新的疗法。谷氨酸与AMPA和/或红藻氨酸盐受体复合物的相互作用的抑制剂可能用于治疗脱髓鞘疾病并且可以配制成药物组合物。

5. 发明申请

WO9942456A3 NOVEL COMPOUNDS AND THEIR USE AS POSITIVE AMPA RECEPTOR MODULATORS 审中-公开
标题翻译：新型化合物及其作为阳性AMPA受体调节剂的应用
公开(公告)号：WO9942456A3
公开(公告)日：1999-10-07
申请号：PCT/DK9900070
申请日：1999-02-18
申请人： NEUROSEARCH AS , GOULIAEV ALEX HAAHR , LARSEN MOGENS , VARMING THOMAS , MATHIESEN CLAUS , JOHANSEN TINA HOLM , SCHEEL KRUEGER JOERGEN , OLSEN GUNNAR M , NIELSEN ELSEBET OESTERGAARD
发明人： GOULIAEV ALEX HAAHR , LARSEN MOGENS , VARMING THOMAS , MATHIESEN CLAUS , JOHANSEN TINA HOLM , SCHEEL-KRUEGER JOERGEN , OLSEN GUNNAR M , NIELSEN ELSEBET OESTERGAARD
IPC分类号： C07D239/74 , A61K31/18 , A61K31/517 , A61K31/535 , A61K31/536 , A61K31/5415 , A61K31/549 , A61K31/554 , A61P9/10 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/18 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P25/36 , A61P43/00 , C07C311/37 , C07C311/39 , C07D239/88 , C07D239/90 , C07D239/91 , C07D265/22 , C07D285/24 , C07D285/28 , C07D285/32 , C07D285/36 , C07D417/04 , C07D417/10 , C07D417/12 , C07D513/04 , A61K31/505 , A61K31/54 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04
CPC分类号： C07D417/04 , C07D239/90 , C07D285/24 , C07D285/28 , C07D513/04
摘要： The invention provides novel compounds represented by general formula (I) wherein the bond represented by the broken line may be a single, double bond or absent; and if the bond is absent, then the nitrogen is substituted with a hydrogen and R ; X represents SO2 or C=O of CH2; Y represents -CH(R )-, -N(R )- or -N(R )-CH2-, O; and the meaning of R , R , R , R , R , R , and R are as defined in the application. The compounds are useful as positive modulators of the AMPA-receptor.
摘要翻译：本发明提供了由通式（I）表示的新化合物，其中由虚线表示的键可以是单键，双键或不存在; 如果该键不存在，则该氮被氢和R 2取代; X代表CH 2的SO 2或C = O; Y代表-CH（R 4） - ， - N（R 4） - 或-N（R 4）-CH 2 - ，O; 并且R 2，R 3，R 4，R 5，R 6，R 7和R 8的含义如本申请中所定义。该化合物可用作AMPA受体的正调节剂。

6. 发明申请

WO1997049692A1 1,2,4-BENZOTHIADIAZINE DERIVATIVES, THEIR PREPARATION AND USE 审中-公开
标题翻译： 1,2,4-苯并噻嗪衍生物及其制备与应用
公开(公告)号：WO1997049692A1
公开(公告)日：1997-12-31
申请号：PCT/DK1997000266
申请日：1997-06-19
申请人： NOVO NORDISK A/S
发明人： NOVO NORDISK A/S , PIROTTE, Bernard , LEBRUN, Philippe , De TULLIO, Pascal , SOMERS, Fabian , DELARGE, Jacques , HANSEN, John, Bondo , NIELSEN, Flemming, Elmelund , HANSEN, Holger, Claus , MOGENSEN, John, Patrick , TAGMOSE, Tina, Moller
IPC分类号： C07D285/24
CPC分类号： A61K31/541 , A61K31/5415 , C07D285/24 , C07D453/02 , C07D453/06
摘要： 1,2,4-Benzothiadiazine derivatives represented by formula (I) wherein D, R , R , R , R , R , R , R , R , R are defined in the description, compositions thereof and methods for preparing the compounds are described. The compounds are useful in the treatment of diseases of the central nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system.
摘要翻译：由式（I）表示的1,2,4-苯并噻二嗪衍生物，其中D，R 1，R 2，R 3，R 4，R 5，R 12，R 13 >，R 14，R 15定义在说明书中，其组合物和制备化合物的方法被描述。该化合物可用于治疗中枢神经系统疾病，心血管系统，肺系统，胃肠系统和内分泌系统。

7. 发明申请

WO1992020666A1 BENZOTHIADIAZINE DERIVATIVE 审中-公开
标题翻译：苯并噻嗪衍生物
公开(公告)号：WO1992020666A1
公开(公告)日：1992-11-26
申请号：PCT/JP1992000672
申请日：1992-05-22
申请人： TAIHO PHARMACEUTICAL COMPANY, LIMITED , OHNO, Tomoyasu , YANO, Shingo , FUJIWARA, Kosuke , AJIOKA, Hirofusa , YAMAMOTO, Noriyuki , YAMADA, Shozo , KAJITANI, Makoto
发明人： TAIHO PHARMACEUTICAL COMPANY, LIMITED
IPC分类号： C07D285/24
CPC分类号： C07D417/12 , C07D285/24
摘要： A benzothiadiazine derivative represented by general formula (I), a hydrate and acid addition salt thereof, and a remedy for peptic ulcer containing said derivative, said hydrate or said salt as an active ingredient. In formula (I) X represents methylene or a lower alkyl-substituted nitrogen atom; Y and Z represent each methylene or carbonyl; A represents phenylene which may be substituted by methoxycarbonyl; B represents lower alkylene or lower alkenylene; R1 represents hydrogen, acetoxyacetyl, cyclohexylmethyl, or benzyl wherein the benzene ring may be substituted by lower alkoxy, halogen, nitro, lower alkyl, methylenedioxy or hydroxyl; R2 represents lower alkyl or phenyl; and R3 represents hydrogen, halogen or lower alkoxy, provided that the case where X, Y and Z represent each methylene, A represents unsubstituted phenylene, B represents lower alkylene, and R1 represents hydrogen is excluded.
摘要翻译：由通式（I）表示的苯并噻二嗪衍生物，其水合物和酸加成盐，以及含有所述衍生物，所述水合物或所述盐作为活性成分的消化性溃疡的药物。在式（I）中，X表示亚甲基或低级烷基取代的氮原子; Y和Z代表每个亚甲基或羰基; A表示可被甲氧基羰基取代的亚苯基; B表示低级亚烷基或低级亚烯基; 卤素，硝基，低级烷基，亚甲基二氧基或羟基取代的苯环，其中R 1表示氢，乙酰氧基乙酰基，环己基甲基或苄基，其中苯环可被低级烷氧基， R2代表低级烷基或苯基; 并且R 3表示氢，卤素或低级烷氧基，条件是X，Y和Z表示各亚甲基的情况，A表示未取代的亚苯基，B表示低级亚烷基，R 1表示氢。

8. 发明申请

WO2013167997A3 COMPOSITIONS AND METHODS FOR THE TREATMENT OF METABOLIC SYNDROME 审中-公开
标题翻译：用于治疗代谢综合征的组合物和方法
公开(公告)号：WO2013167997A3
公开(公告)日：2016-09-01
申请号：PCT/IB2013050907
申请日：2013-02-03
申请人： CELLIXBIO PRIVATE LTD
发明人： KANDULA MAHESH
IPC分类号： C07D285/24 , A61K31/549 , A61P3/00 , A61P9/00 , A61P13/12 , A61P25/00
CPC分类号： C07D285/24 , A61K31/549 , A61K47/48038 , A61K47/48061 , A61K47/542 , A61K47/545
摘要： The invention relates to the compounds of formula (I) or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof The pharmaceutical compositions comprising an effective amount of compounds of formula (I), and methods for the treatment of metabolic syndrome may be formulated for oral, buccal., rectal, topical, transdermal, transmueosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of acute hypertension or malignant hypertension, hypoglycemia in disease states such as insulinoma (a tumor producing insulin) or congenital hyperinsulinism, hyperuricemia, gout, dyslipidemia, obesity, urea cycle disorders, hyperglycemia, insulin resistance, diabetes mellitus, diabetes insipidus, type 1 diabetes, type 2 diabetes, microvascular complications, macrovascular complications, lipid disorders, prediabetes, obesity, arrhythmia, myocardial infarction, stroke, neuropathy, renal complications, hypertriglyceridemia and cardiovascular complications.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，以及多晶型物，溶剂合物，对映异构体，立体异构体和水合物。包含有效量的式（I）化合物的药物组合物和治疗方法代谢综合征可以配制用于口服，口腔，直肠，局部，透皮，透膜，静脉内，肠胃外给药，糖浆或注射。这样的组合物可用于治疗急性高血压或恶性高血压，疾病状态如胰岛素瘤（产生胰岛素）或先天性高胰岛素血症，高尿酸血症，痛风，血脂异常，肥胖，尿素循环障碍，高血糖症，胰岛素抵抗，糖尿病等疾病状态的低血糖，尿崩症，1型糖尿病，2型糖尿病，微血管并发症，大血管并发症，脂质障碍，糖尿病前期，肥胖，心律失常，心肌梗塞，中风，神经病，肾并发症，高甘油三酯血症和心血管并发症。

9. 发明申请

WO2012162323A1 HYPERTENSION AND HYPERURICEMIA 审中-公开
标题翻译：高血压和高血压
公开(公告)号：WO2012162323A1
公开(公告)日：2012-11-29
申请号：PCT/US2012/039011
申请日：2012-05-22
申请人： ARDEA BIOSCIENCES, INC. , MINER, Jeffrey
发明人： MINER, Jeffrey
IPC分类号： C07D285/24 , C07D249/12 , A01N37/44
CPC分类号： A61K31/4196 , A61K31/549 , C07D249/12 , C07D285/24
摘要： A method for treating hypertension in a subject in need thereof (e.g., wherein said treatment does not result in an increase in serum uric acid levels, abnormally elevated serum uric acid levels, hyperuricemia, serum uric acid levels of above 6 mg/dL, or in the development of gout in the subject), the method comprising administering to the subject: a. a thiazide diuretic; and b. an organic anion transporter 4 (OAT4) inhibitor. The thiazide diuretic is selected from hydrochlorothiazide, bendroflumethiazide, benzothiadiazine, hydroflumethiazide, clorothiazide, methyclothiazide, polythiazide, chlorthalidone, metolazone, indapamide, bumetanide, ethacrynic acid, furosemide or torsemide. The OAT4 inhibitor is 2-(5-bromo-4-(4-cyclopropylnaphthalen-1-yl)- 4H-1,2,4-triazol-3-ylthio)acetic acid or a pharmaceutically acceptable salt thereof.
摘要翻译：一种在有需要的受试者中治疗高血压的方法（例如，其中所述治疗不导致血清尿酸水平升高，血尿酸水平异常升高，高尿酸血症，血清尿酸水平高于6mg / dL，或在该主题的痛风的发展中），所述方法包括对所述受试者施用：a。噻嗪类利尿剂和b。有机阴离子转运蛋白4（OAT4）抑制剂。噻嗪类利尿剂选自氢氯噻嗪，弯甲氟噻嗪，苯并噻二嗪，氢氟噻嗪，氯噻嗪，甲基噻嗪，聚噻嗪，氯噻酮，美托拉宗，吲达帕胺，布美他尼，依他尼酸，呋塞米或托塞米。 OAT4抑制剂是2-（5-溴-4-（4-环丙基萘-1-基）-4H-1,2,4-三唑-3-基硫基）乙酸或其药学上可接受的盐。

10. 发明申请

WO2005019191A3 1, 1-DIOXIDO-4H-1,2,4-BENZOTHIADIAZINE DERIVATE UND VERWANDTE VERBINDUNGEN ALS INHIBITOREN DER HCV POLYMERASE ZUR BEHANDLUNG VON HEPATITIS C 审中-公开
标题翻译： 1，1-DIOXIDO-4H-1,2,4-BENZOTHIADIAZINE DERIVATE UND VERWANDTE VERBINDUNGEN ALS INHIBITOREN DER HCV Polymmerase ZUR BEHANDLUNG VON HEPATITIS C
公开(公告)号：WO2005019191A3
公开(公告)日：2005-05-19
申请号：PCT/US2004027000
申请日：2004-08-19
申请人： ABBOTT LAB , HUTCHINSON DOUGLAS K , BELLETTINI JOHN R
发明人： HUTCHINSON DOUGLAS K , BELLETTINI JOHN R
IPC分类号： A61K31/549 , C07D285/24 , A61P31/14
CPC分类号： C07D417/12 , C07D285/24 , C07D285/30 , C07D513/04
摘要： Compounds having the formula (I), wherein B is (a), (b), (c), or (d); A is a monocyclic or bicyclic ring selected from the group consisting of aryl, cycloalkyl, cycloalkenyl, heteroaryl and heterocycle (the other substituents are defined in the claims), are hepatitis C (HCV) polymerase inhibitors. Also disclosed are a composition processes for making the compounds, and synthetic intermediates employed in the processes.
摘要翻译：具有式（I）的化合物，其中B为（a），（b），（c）或（d）; A是选自芳基，环烷基，环烯基，杂芳基和杂环（其它取代基在权利要求中定义）的单环或双环，是丙型肝炎（HCV）聚合酶抑制剂。还公开了用于制备化合物的组合物方法和在该方法中使用的合成中间体。

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