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1. 发明申请

WO2008018639A2 GLYCINE TRANSPORTER INHIBITOR 审中-公开
标题翻译：甘氨酸运输商抑制剂
公开(公告)号：WO2008018639A2
公开(公告)日：2008-02-14
申请号：PCT/JP2007065988
申请日：2007-08-10
申请人： TAISHO PHARMA CO LTD , SEKIGUCHI YOSHINORI , OKUBO TAKETOSHI , SHIBATA TSUYOSHI , ABE KUMI , YAMAMOTO SHUJI , KASHIWA SHUHEI
发明人： SEKIGUCHI YOSHINORI , OKUBO TAKETOSHI , SHIBATA TSUYOSHI , ABE KUMI , YAMAMOTO SHUJI , KASHIWA SHUHEI
IPC分类号： C07D401/10 , C07D401/14 , C07D403/10 , C07D403/14 , C07D405/10 , C07D409/14 , C07D413/10 , C07D417/14
CPC分类号： A47J27/002 , A47J36/02 , C07D401/10 , C07D401/14 , C07D403/10 , C07D403/14 , C07D405/10 , C07D409/14 , C07D413/10 , C07D417/14
摘要： The present invention provides a compound represented by the following formula or a pharmaceutically acceptable salt of the compound or a hydrate of the compound or the salt, which is useful for the prevention or treatment of diseases such as schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, anxiety disorders (generalized anxiety disorder, panic disorder, obsessive compulsive disorder, social anxiety disorder, post-traumatic stress disorder, particular phobias, acute stress disorder, etc.), depression, drug abuse, convulsion, tremor, and sleep disorders, based on glycine uptake inhibitory effect.
摘要翻译：本发明提供下式所示的化合物或化合物的药学上可接受的盐或化合物或其盐的水合物，其可用于预防或治疗诸如精神分裂症，阿尔茨海默病，认知功能障碍，痴呆等疾病，焦虑症（广泛性焦虑症，恐慌症，强迫症，社交焦虑症，创伤后应激障碍，特定恐怖症，急性应激障碍等），抑郁症，药物滥用，惊厥，震颤和睡眠障碍对甘氨酸摄取抑制作用。

2. 发明申请

WO2004080389A2 HYDROXYEICOSADIENAMIDE COMPOUNDS 审中-公开
标题翻译：羟基二十碳烯酰胺化合物
公开(公告)号：WO2004080389A2
公开(公告)日：2004-09-23
申请号：PCT/US2004005222
申请日：2004-03-05
申请人： TAISHO PHARMA CO LTD , UNIV TEXAS , FALCK JOHN R , TANAMI TOHRU , ONO NAOYA , CHONAN TOMOMICHI , HIRANO HITOMI , MIYATA NORIYUKI , TODA YOSHIHISA , OKUYAMA SHIGERU
发明人： FALCK JOHN R , TANAMI TOHRU , ONO NAOYA , CHONAN TOMOMICHI , HIRANO HITOMI , MIYATA NORIYUKI , TODA YOSHIHISA , OKUYAMA SHIGERU
IPC分类号： A61K20060101 , C07C231/00 , C07C307/04 , C07C311/51 , A61K
CPC分类号： C07C311/51 , C07C307/04 , C07C2603/18
摘要： The present invention provides a hydroxyeicosadienamide compound an excellent inhibitory effect on elastase release, which is represented by Formula (I): (I), wherein n represents an integer of 0 to 5, and R represents an optionally substituted C1-20 alkyl group, an optionally substituted aryl group, -NR R , an optionally substituted unsaturated heterocyclic ring, or -(C1-4 alkylene)-Q or Q, wherein Q is an optionally substituted C4-10 bridged hydrocarbon or an optionally substituted aryl group, or a pharmaceutically acceptable salt or hydrate thereof.
摘要翻译：本发明提供一种羟基二十碳二烯酰胺化合物，其对弹性蛋白酶释放具有优异的抑制效果，其由式（I）表示：其中n表示0至5的整数，并且R表示任选取代的C 1-20烷基，任选取代的芳基，-NRXRY，任选取代的不饱和杂环或 - （C1-4亚烷基）-Q或Q，其中Q为任选取代的C 4-10桥碳氢化合物或任选取代的取代的芳基，或其药学上可接受的盐或水合物。

3. 发明申请

WO02051404A8 COMPOSITIONS FOR ORAL USE 审中-公开
标题翻译：口服使用的组合物
公开(公告)号：WO02051404A8
公开(公告)日：2003-11-13
申请号：PCT/JP0111457
申请日：2001-12-26
申请人： KYUSHU TLO CO LTD , TAISHO PHARMA CO LTD , NAKANO YOSHIO , YOSHIMURA MAMIKO , KOGA KEIKO HF
发明人： NAKANO YOSHIO , YOSHIMURA MAMIKO , KOGA TOSHIHIKO DI
IPC分类号： A61K8/69 , A61K8/70 , A61P1/02 , A61P31/04 , A61Q11/00 , A61K31/198
CPC分类号： A61Q11/00 , A61K8/70
摘要： Compositions for oral use which contain trifluoromethionine as the active ingredient. Thus, compositions for oral use which can be safely used in daily life for efficaciously preventing and/or treating diseases in the oral cavity such as bad breath, peridontal diseases and pyorrhea alveolaris are provided.
摘要翻译：用于口服的组合物，其含有三氟甲硫氨酸作为活性成分。因此，提供了可以安全地用于日常生活中用于有效预防和/或治疗口腔疾病如口臭，牙周病和脓包肺泡的口服用组合物。

4. 发明申请

WO2010095768A8 4 -ISOPROPYLPHENYL GLUCITOL COMPOUNDS AS SGLT1 INHIBITORS 审中-公开
标题翻译：作为SGLT1抑制剂的4-取代苯基葡萄糖醇化合物
公开(公告)号：WO2010095768A8
公开(公告)日：2011-08-04
申请号：PCT/JP2010053187
申请日：2010-02-23
申请人： TAISHO PHARMA CO LTD , KAKINUMA HIROYUKI , KOBASHI YOHEI , CHONAN TOMOMICHI , OI TAKAHIRO , SHIOZAWA FUMIYASU , IWATA YUKI , KAWABE KENICHI
发明人： KAKINUMA HIROYUKI , KOBASHI YOHEI , CHONAN TOMOMICHI , OI TAKAHIRO , SHIOZAWA FUMIYASU , IWATA YUKI , KAWABE KENICHI
IPC分类号： C07D309/10 , A61K31/351 , A61P3/10
CPC分类号： C07D309/10
摘要： The present invention provides 4-isopropylphenyl glucitol compounds which have no tendency to accumulate in the body and which inhibit SGLT1 activity to suppress postprandial hyperglycemia (or impaired glucose tolerance) through suppression of glucose absorption in the small intestine, whereby the compounds, for example, can suppress the onset of diabetes and metabolic syndrome or can treat these diseases. A 4-isopropylphenyl glucitol compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: [Chem. 1] wherein R1 represents a hydrogen atom, etc., R2 represents a methyl group, etc., R3 represents a C1-4 alkyl group substituted with an amino group(s), etc., and R4 represents a hydrogen atom, etc.
摘要翻译：本发明提供了通过抑制小肠中的葡萄糖吸收而不具有积累在体内的倾向并抑制SGLT1活性以抑制餐后高血糖（或葡萄糖耐量降低）的4-异丙基苯基葡糖醇化合物，其中化合物例如，可以抑制糖尿病和代谢综合征的发病，或可以治疗这些疾病。由下式（I）表示的4-异丙基苯基葡萄糖醇化合物或其药学上可接受的盐：[Chem。 1]其中R1表示氢原子等，R2表示甲基等，R3表示被氨基取代的C1-4烷基等，R4表示氢原子等。

5. 发明申请

WO2007043653A9 BENZIMIDAZOLE-5-CARBOXAMIDE DERIVATIVE 审中-公开
标题翻译：苯并咪唑-5-羧酰胺衍生物
公开(公告)号：WO2007043653A9
公开(公告)日：2007-06-07
申请号：PCT/JP2006320470
申请日：2006-10-13
申请人： TAISHO PHARMA CO LTD , OTA TOMOMI , TAKAHASHI HITOMI , KAKINUMA HIROYUKI , BUSUJIMA TSUYOSHI
发明人： OTA TOMOMI , TAKAHASHI HITOMI , KAKINUMA HIROYUKI , BUSUJIMA TSUYOSHI
IPC分类号： C07D235/06 , A61K31/4184 , A61K31/427 , A61K31/439 , A61K31/454 , A61K31/4709 , A61K31/497 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K31/551 , A61P9/10 , A61P9/12 , A61P13/12 , A61P43/00 , C07D235/18 , C07D401/12 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D453/02
CPC分类号： C07D235/12 , C07D235/06 , C07D235/08 , C07D235/10 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/06
摘要： Disclosed is a benzimidazole-5-carboxamide derivative represented by the formula below or a pharmaceutically acceptable salt or hydrate thereof. [Chemical formula] The benzimidazole-5-carboxamide derivative can inhibit the sEH activity to increase EETs and is expected to be useful as a therapeutic agent for hypertension, kidney diseases, cardiovascular diseases including cerebral infarction, inflammatory diseases associated with NF?B/I?B kinase activation, autoimmune diseases, endocrine/metabolic diseases including hyperlipemia and diabetes and adult respiratory distress syndrome because of its vasodilating activity.
摘要翻译：公开了由下式表示的苯并咪唑-5-甲酰胺衍生物或其药学上可接受的盐或水合物。 [化学式]苯并咪唑-5-甲酰胺衍生物可抑制sEH活性，增加EETs，预计可用作高血压，肾脏疾病，包括脑梗塞在内的心血管疾病，与NFκB/ I相关的炎性疾病的治疗剂 B激酶活化，自身免疫性疾病，内分泌/代谢性疾病，包括高脂血症和糖尿病以及由于其血管舒张活性而引起的成人呼吸窘迫综合征。

6. 发明申请

WO2006080412A2 CYANOPYRROLIDINE DERIVATIVE-CONTAINING COMPOSITION FOR SOLID PHARMACEUTICAL PREPARATIONS, SOLID PHARMACEUTICAL PREPARATION CONTAINING THE COMPOSITION, AND PROCESS FOR PRODUCING THE SOLID PHARMACEUTICAL PREPARATION 审中-公开
标题翻译：用于固体药物制剂的含氰基吡咯烷衍生物的组合物，含有该组合物的固体药物制剂以及制备固体药物制剂的方法
公开(公告)号：WO2006080412A2
公开(公告)日：2006-08-03
申请号：PCT/JP2006301258
申请日：2006-01-20
申请人： TAISHO PHARMA CO LTD , YAZAKI HIROAKI , IKUTA HIROSHI
发明人： YAZAKI HIROAKI , IKUTA HIROSHI
CPC分类号： A61K31/40 , A61K9/2018 , A61K9/2054
摘要： A composition for solid pharmaceutical preparations, essentially consisting of a cyanopyrrolidine derivative represented by the following general formula (1) or a pharmaceutically acceptable salt thereof, and at least one stabilizing ingredient selected from the group consisting of sugars and sugar alcohols, [Formula 1] [wherein R1 represents, for example, a halogen atom or a hydroxyl group, R 3 and R 4 may be the same or different, each represents, for example, a hydrogen atom or a halogen atom, X represents an oxygen atom or a sulfur atom, Y represents, for example, a group represented by -CR 5 R 6 - (wherein R 5 and R 6 may be the same or different, each represents, for example, a hydrogen atom or a halogen atom), W represents, for example, a hydrogen atom or an acyl group derived from naturally occurring amino acids, and Z represents, for example, a hydrogen atom or an alkyl group of 1 to 10 carbon atoms which may be substituted with one or more substituents selected from the group consisting of a halogen atom, a hydroxyl group, a hydroxylalkyl group of 1 to 5 carbon atoms, a carboxyl group, a mercapto group and the like].
摘要翻译：一种固体药物制剂用组合物，其基本上由下述通式（1）表示的氰基吡咯烷衍生物或其药学上可接受的盐和至少一种选自糖和糖醇的稳定成分组成，[式1] [其中R 1代表例如卤素原子或羟基，R 3和R 4可以相同或不同，各自代表氢，例如氢原子或卤素原子，X表示氧原子或硫原子，Y表示例如由-CR 5 R 6 - 表示的基团， R 5和R 6可以相同或不同，各自代表例如氢原子或卤素原子），W代表例如氢原子或由天然存在的氨基酸衍生的酰基，Z表示例如氢原子或可以被取代的1至10个碳原子的烷基与选自由卤素原子，羟基，1至5个碳原子的羟基烷基，羧基，巯基等组成的组中的一个或多个取代基组合]。

7. 发明申请

WO2004110585A9 RADIAL SPHERICAL CRYSTALLIZATION PRODUCT, PROCESS FOR PRODUCING THE SAME AND DRY POWDER PREPARATION CONTAINING THE CRYSTALLIZATION PRODUCT 审中-公开
标题翻译：径向球形结晶产品，其生产方法和含有结晶产品的干粉制备
公开(公告)号：WO2004110585A9
公开(公告)日：2006-03-23
申请号：PCT/JP2004007171
申请日：2004-05-26
申请人： TAISHO PHARMA CO LTD , DANJO KAZUMI , OKAMOTO HIROKAZU , FURUDATE TAKEAKI
发明人： DANJO KAZUMI , OKAMOTO HIROKAZU , FURUDATE TAKEAKI
IPC分类号： A61K9/00 , A61K47/10 , A61K47/26 , B01D11/02 , B01D9/02
CPC分类号： A61K9/0075 , A61K47/10 , A61K47/26 , B01D11/0411 , B01J2/02
摘要： A radial spherical crystallization product having multiple needle-shaped portions radially extending outward from the core portion. The radial spherical crystallization product is produced by, for example, bringing a supercritical fluid mixed with a modifier according to necessity and a solution containing a sample component, which have been introduced through different flow channels, into contact with each other at the time of injection from the flow channels into a crystallization vessel. This radial spherical crystallization product can be used as a drug delivery medium or medicine for transmucous or transpulmonary administration or as a fine carrier or fine stock drug such as dry powder inhale (DPI).
摘要翻译：一种径向球形结晶产物，其具有从芯部向外径向延伸的多个针状部分。径向球形结晶产物通过例如根据需要使与混合有改性剂的超临界流体和含有通过不同流动通道引入的样品组分的溶液在注射时彼此接触而制备从流动通道进入结晶容器。该径向球形结晶产物可用作药物递送介质或用于经皮或经肺给药的药物或作为细小载体或精细储存药物如干粉吸入（DPI）。

8. 发明申请

WO03086293A2 PHARMACEUTICAL PREPARATION FOR TASTE MASKING 审中-公开
标题翻译：药物掩蔽的药物制剂
公开(公告)号：WO03086293A2
公开(公告)日：2003-10-23
申请号：PCT/US0310829
申请日：2003-04-09
申请人： TAISHO PHARMA CO LTD , ANDO SHINJI , STELLA VALENTINO J
发明人： ANDO SHINJI , STELLA VALENTINO J
IPC分类号： A61K47/42 , A61K9/08 , A61K9/10 , A61K9/14 , A61K9/20 , A61K9/48 , A61K31/121 , A61K31/192 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/407 , A61K31/4152 , A61K31/421 , A61K31/5415 , A61K47/48 , A61P29/00 , A61K
CPC分类号： A61K31/421 , A61K9/2045 , A61K9/2054 , A61K31/192 , A61K31/40 , A61K31/404 , A61K31/407 , A61K31/4152 , A61K31/5415 , A61K47/645
摘要： The present invention relates to taste-masked pharmaceutical oral dosage formulations comprising complexes of a drug and polylysine or polyarginine for taste-masking, to convenient taste-masked oral dosage forms comprising the complexes and to methods of masking the taste of a drug, and preventing sublimation of the drug while providing good bioavailability.
摘要翻译：本发明涉及包含药物和聚赖氨酸或聚精氨酸复合物以用于掩味的掩味药物口服剂量制剂，以及包含复合物的方便的掩味口服剂型和掩蔽药物味道的方法，以及防止药物升华，同时提供良好的生物利用度。

9. 发明申请

WO2007136116A3 C-PHENYL GLYCITOL COMPOUND FOR THE TREATMENT OF DIABETES 审中-公开
标题翻译：用于治疗糖尿病的C-PHENYL GLYCITOL化合物
公开(公告)号：WO2007136116A3
公开(公告)日：2008-03-13
申请号：PCT/JP2007060653
申请日：2007-05-18
申请人： TAISHO PHARMA CO LTD , KAKINUMA HIROYUKI , KOBASHI YOHEI , HASHIMOTO YUKO , OI TAKAHIRO , TAKAHASHI HITOMI , AMADA HIDEAKI , IWATA YUKI
发明人： KAKINUMA HIROYUKI , KOBASHI YOHEI , HASHIMOTO YUKO , OI TAKAHIRO , TAKAHASHI HITOMI , AMADA HIDEAKI , IWATA YUKI
IPC分类号： C07D309/12 , A61K31/351 , A61P3/10 , C07D405/10
CPC分类号： C07D405/10 , C07D309/12
摘要： Provided is a novel C-phenyl glycitol compound that may serve as a prophylactic or therapeutic agent for diabetes by inhibiting both SGLT1 activity and SGLT2 activity, thereby exhibiting a glucose absorption suppression action and a urine glucose excretion action. A C-phenyl glycitol compound represented by Formula (I) below or a pharmaceutically acceptable salt thereof or a hydrate thereof wherein R 1 and R 2 are the same or different and represent a hydrogen atom, a hydroxyl group, a C 1-6 alkyl group, a C 1-6 alkoxy group or a halogen atom, R 3 is a hydrogen atom, a C 1-6 alkyl group, a C 1-6 alkoxy group or a halogen atom, Y is a C 1-6 alkylene group, -O-(CH 2 )n- (n is an integer of 1 to 4) or a C 2-6 alkenylene group, provided that when Z is NHC(= NH)NH 2 or -NHCON(R B )R C , n is not 1, Z is -CONHR A , -NHC(=NH)NH2 or -NHCON(R B )R C , Formula (A) or Formula (B).
摘要翻译：提供了可以通过抑制SGLT1活性和SGLT2活性而作为糖尿病的预防或治疗剂的新颖的C-苯基糖醇化合物，从而表现出葡萄糖吸收抑制作用和尿葡萄糖排泄作用。由下式（I）表示的C-苯基糖醇化合物或其药学上可接受的盐或其水合物，其中R 1和R 2相同或不同，表示氢原子，羟基，C 1-6烷基，C 1-6烷氧基或卤素原子，R 3 >是氢原子，C 1-6烷基，C 1-6烷氧基或卤素原子，Y是C 1-6 亚烷基，-O-（CH 2 CH 2）n - （n为1〜4的整数）或C 2-6亚烯基，提供当Z是NHC（= NH）NH 2或-NHCON（R B）R C）时，n不是1，Z是 - CONHR A，NHC（= NH）NH 2或-NHCON（R B）R C，式（A）或式（B）。

10. 发明申请

WO2006001511A8 PYRROLOPYRIMIDINE AND PYRROLOPYRIDINE DERIVATIVES SUBSTITUTED WITH A CYCLIC AMINO GROUP AS CRF ANTAGONISTS 审中-公开
标题翻译：以循环氨基作为CRF拮抗剂取代吡咯并嘧啶衍生物和吡咯啉衍生物
公开(公告)号：WO2006001511A8
公开(公告)日：2006-02-23
申请号：PCT/JP2005012152
申请日：2005-06-24
申请人： TAISHO PHARMA CO LTD , NAKAZATO ATSURO , OKUBO TAKETOSHI , NOZAWA DAI , TAMITA TOMOKO , KENNIS LUDO E J
发明人： NAKAZATO ATSURO , OKUBO TAKETOSHI , NOZAWA DAI , TAMITA TOMOKO , KENNIS LUDO E J
IPC分类号： C07D471/04 , C07D487/04 , C07D519/00 , C07F9/00 , A61K31/437 , A61K31/519 , A61P25/00 , C07D209 , C07D221 , C07D239 , C07D451 , C07D471 , C07F9/38 , C07F9/40
CPC分类号： C07D471/04 , C07D487/04
摘要： [PROBLEM TO BE SOLVED] An object of the present invention is to provide an antagonist against CRF receptors and/or an agonist for receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal diseases, drug dependence, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alopecia, irritable bowel syndrome, sleep disorders, epilepsy, dermatitides, schizophrenia, pain, etc. [SOLUTION] A pyrrolopyrimidine or pyrrolopyridine derivative substituted with a cyclic amino group represented by the following formula [I] has a high affinity for CRF receptors and/or d receptors, and is effective against diseases in which CRF is considered to be involved.
摘要翻译： [待解决的问题]本发明的目的是提供一种CRF受体拮抗剂和/或受体激动剂，其有效作为涉及CRF的疾病的治疗或预防剂，例如抑郁症焦虑症，阿尔茨海默病，帕金森病，亨廷顿氏舞蹈病，进食障碍，高血压，胃肠道疾病，药物依赖，脑梗塞，脑缺血，脑水肿，头部外伤，炎症，免疫相关疾病，脱发，肠易激综合征，睡眠疾病，癫痫，皮肤病，精神分裂症，疼痛等。解决方案由下式[I]表示的环状氨基取代的吡咯并嘧啶或吡咯并吡啶衍生物对CRF受体和/或d受体具有高亲和力，并且是有效的针对CRF被认为涉及的疾病。

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