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1. 发明申请

WO1993010809A1 FIBRONECTIN-CONTAINING OPHTHALMIC SOLUTION, METHOD OF MANUFACTURE OF AN OPHTHALMIC SOLUTION, METHOD OF PRESERVING AN OPHTHALMIC SOLUTION, AND METHODS OF TREATMENT OF OPHTHALMIC WOUNDS 审中-公开
标题翻译：含有FIBRONECTIN的眼科解决方案，制造光学溶液的方法，保留眼用溶液的方法和治疗眼底损伤的方法
公开(公告)号：WO1993010809A1
公开(公告)日：1993-06-10
申请号：PCT/US1992010243
申请日：1992-11-19
申请人： NEW YORK BLOOD CENTER, INC. , JCR PHARMACEUTICALS CO., LTD. , SANTEN PHARMACEUTICAL CO., LTD.
发明人： NEW YORK BLOOD CENTER, INC. , JCR PHARMACEUTICALS CO., LTD. , SANTEN PHARMACEUTICAL CO., LTD. , HOROWITZ, Bernard , SHULMAN, Richard, W. , SETTON, Adrianne, J. , NISHIMURA, Toyohiko , KAWASHIMA, Yoichi
IPC分类号： A61K37/04
CPC分类号： A61K38/39 , A61K9/0048 , Y10S514/912
摘要： A stable and soluble multi-dose ophthalmic solution is disclosed. The solution contains fibronectin, an amino acid, a sugar, and a lower alkyl p-hydroxybenzoate. A method of treatment of ophthalmic wounds employing the ophthalmic solution, a process for preparing fibronectin for ophthalmic use, a method of lyophilizing an aqueous solution of fibronectin free of albumin, a method for inhibiting bacterial growth in an ophthalmic solution while preserving the cellular adhesion and wound healing activities of fibronectin, and a method of treatment of ophthalmic wounds administering a wound-healing accelerator solution are also disclosed.
摘要翻译：公开了一种稳定且可溶的多剂量眼用溶液。该溶液含有纤连蛋白，氨基酸，糖和对羟基苯甲酸的低级烷基酯。一种使用眼用溶液治疗眼部伤口的方法，制备用于眼科用途的纤维连接蛋白的方法，冻干不含白蛋白的纤连蛋白水溶液的方法，在保留细胞粘附的同时抑制眼用溶液中的细菌生长的方法，还公开了纤连蛋白的伤口愈合活性，以及施用伤口愈合促进剂溶液的眼科伤口治疗方法。

2. 发明申请

WO1997049419A1 OPHTHALMIC DRUG COMPOSITIONS 审中-公开
标题翻译： OPHTHALMIC药物组合物
公开(公告)号：WO1997049419A1
公开(公告)日：1997-12-31
申请号：PCT/JP1997002015
申请日：1997-06-11
申请人： SANTEN PHARMACEUTICAL CO., LTD. , NISHIDA, Teruo , NAKAMURA, Masatsugu , NAKATA, Katsuhiko
发明人： SANTEN PHARMACEUTICAL CO., LTD.
IPC分类号： A61K38/07
CPC分类号： C07K5/1016 , A61K9/0048 , A61K38/046 , A61K38/07 , C07K7/22 , Y10S514/912
摘要： The minimum activity-exhibiting site of substance P has now been found and the action of a compound consisting of the units constituting the minimum site on the ophthalmic region has been elucidated, on the basis of which the following ophthalmic drug compositions containing the above compound as the active ingredient are provided: an ophthalmic drug composition (particularly corneal disease remedy) containing as the active ingredient Phe-Gly-Leu-Met-NH2 or a pharmaceutically acceptable salt thereof; and a corneal disease remedy (particularly elongation accelerator for corneal epithelium) containing as the active ingredients Phe-Gly-Leu-Met-NH2 or a pharmaceutically acceptable salt thereof and insulin-like growth factor-I. These preparations preferably take the dosage form of eye drops.
摘要翻译：已经发现物质P的最低活性表现位点，并且已经阐明了由构成眼部区域的最小部位的单元组成的化合物的作用，基于此，含有上述化合物的下列眼用药物组合物提供活性成分：含有作为活性成分Phe-Gly-Leu-Met-NH 2或其药学上可接受的盐的眼用药物组合物（特别是角膜疾病治疗剂）以及作为活性成分Phe-Gly-Leu-Met-NH 2或其药学上可接受的盐和胰岛素样生长因子-I的角膜疾病治疗（特别是角膜上皮的延伸促进剂）。这些制剂优选采用滴眼剂的剂型。

3. 发明申请

WO1996014293A1 NOVEL 1,3-DIALKYLUREA DERIVATIVE HAVING HYDROXYL GROUP 审中-公开
标题翻译：具有羟基的新型1,3-二氨基脲衍生物
公开(公告)号：WO1996014293A1
公开(公告)日：1996-05-17
申请号：PCT/JP1995002236
申请日：1995-11-01
申请人： SANTEN PHARMACEUTICAL CO., LTD. , KAWASHIMA, Yoichi , FUJIMURA, Ken-ichi , SUHARA, Hiroshi , MIYAWAKI, Nobuaki , FUJITA, Yuko
发明人： SANTEN PHARMACEUTICAL CO., LTD.
IPC分类号： C07C275/10
CPC分类号： C07C275/24 , C07C2601/14
摘要： A compound represented by general formula (I) and salts thereof, wherein R and R represent carboxyl optionally converted into an ester, amide or hydroxamate group; R represents lower alkyl or phenyl lower alkyl; and R represents hydrogen, lower alkyl, amino lower alkyl, lower alkylamino lower alkyl, hydroxy lower alkyl, mercapto lower alkyl, carboxy lower alkyl, lower alkoxycarbonyl lower alkyl, imidazolyl lower alkyl, indolyl lower alkyl, optionally substituted phenyl, optionally substituted phenyl lower alkyl, optionally substituted naphthyl or optionally substituted naphthyl lower alkyl. The compound has an inhibitory effect on endopeptidase 24.11 and being useful as a remedy for cardiovascular diseases such as cardiac insufficiency and hypertension, kidney diseases such as renal insufficiency, gastrointestinal disorders such as diarrhea and gastric hyperacidity, endocrine/metabolic diseases such as obesity, and autoimmune diseases such as rheumatism, and as an analgesic agent for muscular pain, hemicrania, etc.
摘要翻译：由通式（I）表示的化合物及其盐，其中R 1和R 4表示任选转化为酯，酰胺或异羟肟基的羧基; R 2表示低级烷基或苯基低级烷基; R 3表示氢，低级烷基，氨基低级烷基，低级烷基氨基低级烷基，羟基低级烷基，巯基低级烷基，羧基低级烷基，低级烷氧基羰基低级烷基，咪唑基低级烷基，吲哚基低级烷基，任意取代的苯基，取代的苯基低级烷基，任选取代的萘基或任选取代的萘基低级烷基。该化合物对内肽酶24.11具有抑制作用，可用作心血管疾病如心功能不全和高血压，肾脏疾病如肾功能不全，胃肠疾病如腹泻和胃酸过多，内分泌/代谢疾病如肥胖症的补救措施，以及自身免疫性疾病如风湿病，以及作为肌肉疼痛，血红素等的镇痛剂。

4. 发明申请

WO1995013269A1 1,4-BENZOTHIAZINE DERIVATIVE 审中-公开
公开(公告)号：WO1995013269A1
公开(公告)日：1995-05-18
申请号：PCT/JP1994001907
申请日：1994-11-10
申请人： SANTEN PHARMACEUTICAL CO., LTD. , KAWASHIMA, Yoichi , OTA, Atsutoshi , MIBU, Hiroyuki , MATSUBAYASHI, Kenichiro
发明人： SANTEN PHARMACEUTICAL CO., LTD.
IPC分类号： C07D279/12
CPC分类号： C07D279/16
摘要： A compound represented by general formula (I) or a salt thereof and an intermediate for synthesizing the same wherein R represents optionally protected hydroxy; R represents lower alkyl; R represents hydrogen, lower alkyl, optionally protected hydroxy or lower alkoxy, wherein the lower alkyl group may be substituted by optionally protected hydroxy, amino or lower alkylamino; R represents carboxyl which may be in the form of an ester or amide; A represents alkylene; and B represents -CH2- or >C=S. This compound has the activities of stabilizing proteins and inhibiting lipid peroxide formation, and is promising as an excellent cataract remedy.
摘要翻译：由通式（I）表示的化合物或其盐和用于合成其的中间体，其中R 1表示任选保护的羟基; R 2表示低级烷基; R 3表示氢，低级烷基，任选保护的羟基或低级烷氧基，其中低级烷基可被任选被保护的羟基，氨基或低级烷基氨基取代; R 4表示可以是酯或酰胺形式的羧基; A表示亚烷基; B表示-CH 2 - 或> C = S。该化合物具有稳定蛋白质和抑制脂质过氧化物形成的活性，并且作为优异的白内障治疗是有希望的。

5. 发明申请

WO1989000044A1 ARTIFICIAL LACRIMA 审中-公开
标题翻译：人造LACRIMA
公开(公告)号：WO1989000044A1
公开(公告)日：1989-01-12
申请号：PCT/JP1988000674
申请日：1988-07-06
申请人： SANTEN PHARMACEUTICAL CO., LTD. , IWAO, Jun-ichi , ISO, Tadashi , UEMURA, Osamu , KAWASHIMA, Yo-ichi
发明人： SANTEN PHARMACEUTICAL CO., LTD.
IPC分类号： A61K09/08
CPC分类号： A61K31/715 , A61K9/0048
摘要： An artificial lacrima containing sodium hyaluronate and having a pH of 5.5 to 8.0 and an osmotic pressure ratio (to physiological saline) of 0.85 to 1.55, and a drug for treating corneal xerosis which contains sodium hyaluronate as a major component are disclosed.

6. 发明申请

WO1983000865A1 BENZOTHIAZOLINE COMPOUNDS 审中-公开
标题翻译：苯并噻唑化合物
公开(公告)号：WO1983000865A1
公开(公告)日：1983-03-17
申请号：PCT/JP1982000363
申请日：1982-09-10
申请人： SANTEN PHARMACEUTICAL CO., LTD. , IWAO, Jun-ichi , OYA, Masayuki , ISO, Tadashi
发明人： SANTEN PHARMACEUTICAL CO., LTD.
IPC分类号： C07D277/66
CPC分类号： C07D277/66
摘要： Benzothiazoline derivatives represented by the general formula (I): wherein R represents a lower alkanoyl group, R represents one or more groups selected from among a hydrogen atom, a lower alkyl group, a lower alkoxy group, a hydroxy group, a halogen atom, a nitro group, a halogen-substituted lower alkyl group, and a sulfamoyl group, R represents or -COR , R and R each represents a hydrogen atom, a lower alkyl group, a cyclohexyl group or a substituted lower alkyl group, R represents a hydrogen atom, an alkyl group, a substituted alkyl group, an alkanoyl group, a substituted alkanoyl group, an alkenoyl group, a substituted alkenoyl group or a furylcarbonyl group, R represents a hydrogen atom, a hydroxy group, a phenyl-lower alkyl group or a benzoyl group, R represents a hydroxy group, a lower alkoxy group, represents a straight or branched alkylene group containing 1 to 6 carbon atoms, m represents 0 or 1, n represents 0 or 1, and p represents 4 or 5, and salts thereof, useful for treating cardiovascular diseases, and a process for their preparation.
摘要翻译：由通式（I）表示的苯并噻唑啉衍生物：其中R 1表示低级烷酰基，R 2表示选自氢原子，低级烷基，低级烷氧基中的一个或多个基团，羟基，卤素原子，硝基，卤素取代的低级烷基和氨磺酰基，R 3表示“或”或“-COR”，R 4和R 5均为H. 各自表示氢原子，低级烷基，环己基或取代的低级烷基，R 6表示氢原子，烷基，取代的烷基，烷酰基，取代的烷酰基，烯酰基基团，取代的烯酰基或呋喃基羰基，R 7表示氢原子，羟基，苯基 - 低级烷基或苯甲酰基，R 8表示羟基，低级烷氧基， IMAGE>表示含有1至6个碳原子的直链或支链亚烷基，m表示0或1，n表示0或1，p 呈现4或5及其盐，可用于治疗心血管疾病，及其制备方法。

7. 发明申请

WO1998025602A1 GLAUCOMA REMEDY 审中-公开
标题翻译： GLAUCOMA补救
公开(公告)号：WO1998025602A1
公开(公告)日：1998-06-18
申请号：PCT/JP1997004539
申请日：1997-12-10
申请人： SANTEN PHARMACEUTICAL CO., LTD. , SHIRASAWA, Eiichi , KAGEYAMA, Masaaki
发明人： SANTEN PHARMACEUTICAL CO., LTD.
IPC分类号： A61K31/195
CPC分类号： A61K31/195
摘要： To find out a new pharmacological activity of 1,3-dialkylurea derivatives in the ophthalmic field. A glaucoma remedy which comprises as the active ingredient a compound represented by general formula (I) or a salt thereof: wherein R represents carboxy or ester thereof; R represents hydrogen, lower alkyl, or hydroxy; R represents lower alkyl; R represents carboxy or ester thereof; R represents an aromatic group; and A represents lower alkylene. The compound is especially preferably one represented by formula (I) in which R , R , R , R and R represent carboxy, hydroxy, isobutyl, carboxy, and naphthyl, respectively, and A represents methylene.
摘要翻译：找出眼科领域中1,3-二烷基脲衍生物的新药理活性。作为活性成分含有通式（I）表示的化合物或其盐的青光眼药物，其中R 1表示羧基或其酯; R 2表示氢，低级烷基或羟基; R 3表示低级烷基; R 4表示羧基或其酯; R 5表示芳基; A代表低级亚烷基。该化合物特别优选由式（I）表示的化合物，其中R 1，R 2，R 3，R 4和R 5表示羧基，羟基，异丁基，羧基和萘基， A表示亚甲基。

8. 发明申请

WO1998009943A1 NOVEL SULFUR-CONTAINING AMINO ACID DERIVATIVES 审中-公开
标题翻译：新型含硫氨基酸衍生物
公开(公告)号：WO1998009943A1
公开(公告)日：1998-03-12
申请号：PCT/JP1997003124
申请日：1997-09-05
申请人： SANTEN PHARMACEUTICAL CO., LTD. , HORIUCHI, Masato , FUJIMURA, Kenichi , SUHARA, Hiroshi
发明人： SANTEN PHARMACEUTICAL CO., LTD.
IPC分类号： C07C323/60
CPC分类号： C07C323/65 , C07C323/60 , C07C329/06 , C07C2601/14
摘要： Novel sulfur-containing amino acid derivatives of general formula (I) and exhibiting a high inhibitory activity against LTA4 hydrases. In said formula (I), R is H, alkyl, (substituted) phenylalkyl, alkanoyl or (substituted) benzoyl; R is ester, amide or carboxyl; R is hydroxyl, alkyl, halogenoalkyl, alkoxy, halogenoalkoxy, alkylthio, (substituted) phenyl, (substituted) phenoxy, (substituted) phenylthio, halogeno, alkylsulfonyl, halogenoalkylsulfonyl, nitro or cyano; R is alkyl; and A and A are each alkylene.
摘要翻译：新型含有通式（I）的含硫氨基酸衍生物，对LTA4水解酶具有较高的抑制活性。在所述式（I）中，R 1是H，烷基，（取代的）苯基烷基，烷酰基或（取代的）苯甲酰基; R 2是酯，酰胺或羧基; R 3是羟基，烷基，卤代烷基，烷氧基，卤代烷氧基，烷硫基，（取代）苯基，（取代的）苯氧基，（取代的）苯硫基，卤代，烷基磺酰基，卤代烷基磺酰基，硝基或氰基; R 4是烷基; A 1和A 2均为亚烷基。

9. 发明申请

WO1994005647A1 3-OXO-1,4-BENZOTHIAZINE DERIVATIVE 审中-公开
公开(公告)号：WO1994005647A1
公开(公告)日：1994-03-17
申请号：PCT/JP1993001190
申请日：1993-08-25
申请人： SANTEN PHARMACEUTICAL CO., LTD. , KAWASHIMA, Yoichi , OTA, Atsutoshi , MIBU, Hiroyuki
发明人： SANTEN PHARMACEUTICAL CO., LTD.
IPC分类号： C07D279/16
CPC分类号： C07D279/16 , Y02P20/55
摘要： A compound represented by general formula (I), which is useful as a cataract remedy, wherein R represents optionally protected hydroxy; R represents lower alkyl; R represents hydrogen, lower alkyl, optionally protected hydroxy or lower alkoxy, provided that the lower alkyl may be substituted by optionally protected hydroxy, amino or lower alkylamino; R represents carboxyl which may be in the form of ester or carboxamide; and A represents alkylene.
摘要翻译：由通式（I）表示的化合物，其可用作白内障治疗，其中R 1表示任选保护的羟基; R 2表示低级烷基; R 3表示氢，低级烷基，任选保护的羟基或低级烷氧基，条件是低级烷基可以被任选保护的羟基，氨基或低级烷基氨基取代; R 4表示可以是酯或甲酰胺形式的羧基; A表示亚烷基。

10. 发明申请

WO1991001718A1 METHOD OF PHOTOSTABILIZING EYEWASH AND PHOTOSTABILIZED EYEWASH 审中-公开
标题翻译：光敏化学和光致发光眼睛的方法
公开(公告)号：WO1991001718A1
公开(公告)日：1991-02-21
申请号：PCT/JP1990000950
申请日：1990-07-26
申请人： EISAI CO., LTD. , SANTEN PHARMACEUTICAL CO., LTD. , MORITA, Takakazu , MITA, Shiro , KAWASHIMA, Yoichi
发明人： EISAI CO., LTD. , SANTEN PHARMACEUTICAL CO., LTD.
IPC分类号： A61K09/08
CPC分类号： A61K33/22 , A61K9/0048 , A61K31/047 , A61K2300/00
摘要： A method of photostabilizing an eyewash containing a photo-unstable medicine as an ingredient, which comprises adding thereto boric acid and/or borax and a polyhydric alcohol.

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