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1. 发明专利

JPH1143434A MEDICINE FOR OPENING POTASSIUM CHANNEL 失效
公开(公告)号：JPH1143434A
公开(公告)日：1999-02-16
申请号：JP16290198
申请日：1998-05-27
申请人： POLA CHEM IND INC
发明人： NAMIKI TAKAYUKI , YUASA MASAYUKI , TAKAKUWA TAKAKO , ICHINOMIYA SATOSHI , TAMAI MASASHI , KAWAZU YUKIO , KISHII KENICHI , FUNAYAMA NORIO , HIYAMA NAOKI , TANEDA KYOKO , YAHIRO TOMOAKI , SUGIO MAYUMI
IPC分类号： C07D487/14 , A61K31/505 , A61P9/00 , A61P13/02 , A61P15/00 , A61P25/00 , A61P25/02 , A61P37/00
摘要： PROBLEM TO BE SOLVED: To obtain the subject medicine useful for treating immunological disease, central neural disease, muscular disease, circulatory system disease, and so on, by including a pyrrolopyrazolopyrimidine compound. SOLUTION: This medicine, which is a potassium channel-opening medicine, is obtained by including a pyrrolopyrazolopyrimidine compound shown by the formula [R is an alkyl; R is H, a halogen, a (substituted) alkyl, etc.; R is nitro, amino, a heterocyclic ring, etc.], (e.g. 8-tert-butyl-6,7-dihydro-5-methyl-3- nitro-8H-pyrrolo(3,2e)pyrazolo(1,5-a)pyrimidine) or a salt thereof. The medicine can be prepared for inhalation, injection, oral administration, transrectal administration, percutaneous absorption, and so on. The medicine can contain vehicle, binder, coating, lubricant, and so on. It is preferable to administer the medicine at a rate of 1-1000 mg, as the compound of the formula, per one adult per day in one to several portions.

2. 发明专利

JPH10218881A NEW PYRROLOPYRAZOLOPYRIMIDINE DERIVATIVE 失效
公开(公告)号：JPH10218881A
公开(公告)日：1998-08-18
申请号：JP2038797
申请日：1997-02-03
申请人： POLA CHEM IND INC
发明人： NAMIKI TAKAYUKI , YUASA MASAYUKI , TAKAKUWA TAKAKO , ICHINOMIYA SATOSHI , TAMAI MASASHI , HIYAMA NAOKI , KAWAZU YUKIO , YAHIRO TOMOAKI , SUGIO MAYUMI
IPC分类号： A61K31/505 , A61P11/00 , C07D487/04 , C07D487/14
摘要： PROBLEM TO BE SOLVED: To obtain the new subject compound that is useful as a synthetic intermediate for a preventive or therapeutic agent for respiratory diseases as asthma by using a pyrrolopyrazolopyrimidine resultant from the reaction of the specific pyrazolopyrimidine and an amine. SOLUTION: This novel compound is represented by formula I[R is a straight, branched or cyclic alkyl; R is (substituted) alkyl, alkoxycarbonyl, a halogen, H] or its salt, typically ethyl 8-cyclopentyl-6,7-dihydro-8H- pyrrolo[3.2-e]pyrazolo[1,5-a]pyrimidine-5-carboxylate and is useful as a synthetic intermediate for a medicine that prevents and treats pulmonary diseases. This new compound is prepared by reaction of a pyrazolopyrimidine of formula II [R is a (substituted) alkyl, an alkoxycarbonyl, a halogen; X is a halogen] with an amine of the formula: R1 -NH2 .

3. 发明专利

JP2003048874A New biphenylureide derivative and medicine containing the same as active ingredient 有权
标题翻译：新的联苯胺衍生物和含有它的药物作为活性成分
公开(公告)号：JP2003048874A
公开(公告)日：2003-02-21
申请号：JP2001236702
申请日：2001-08-03
申请人： Pola Chem Ind Inc , ポーラ化成工業株式会社
发明人： NAMIKI TAKAYUKI , MITANI MASAMIKI , TAMAI MASASHI , KISHII KENICHI , HIYAMA NAOKI , KIMURA MAKOTO , MASUDA TOMOKO , ICHINOMIYA SATOSHI
IPC分类号： C07D257/04 , A61K31/216 , A61K31/41 , A61P3/06 , A61P9/10 , A61P9/12 , A61P43/00 , C07C311/46 , C07C311/60
摘要： PROBLEM TO BE SOLVED: To provide a new compound useful for preventing and/or treating the complication of hypertension and hyperlipemia.
SOLUTION: A compound expressed by formula (1) [wherein, R
1 is a halogen or a phenyl (substituted with a 1-4C alkyl) or a 1-8C alkyl; R
2 is H or a 1-4C alkyl; R
3 is a 2-6C alkyl; and R
4 is a partial structural formula 1 or 2 (wherein, R
5 is H or a triphenylmethyl; and R
6 is H, a 3-5C alkyl or a (substituted) phenylaminocarbonyl)] or a pharmaceutically permissible salt of the compound, and a medicine containing the same are provided. A biphenylureide derivative (1) has both excellent angiotensin II receptor antagonism and acyl coenzyme-A cholesterol acyltransferase inhibiting activity at the same time, and it is useful as a medicine for preventing and/or treating the complication of hypertension and hyperlipemia, and a disease caused by the complication, or the like.
COPYRIGHT: (C)2003,JPO
摘要翻译：要解决的问题：提供可用于预防和/或治疗高血压和高脂血症并发症的新化合物。解决方案：由式（1）表示的化合物[其中，R 1是卤素或苯基（被1-4C烷基取代）或1-8C烷基; R2是H或1-4C烷基; R3是2-6C烷基; 和R4是部分结构式1或2（其中，R5是H或三苯基甲基，R6是H，3-5C烷基或（取代的）苯基氨基羰基）]或化合物的药学上允许的盐，以及药物包含相同的。联苯醚衍生物（1）同时具有优异的血管紧张素II受体拮抗作用和酰基辅酶A胆固醇酰基转移酶抑制活性，可用作预防和/或治疗高血压和高脂血症并发症的药物由并发症引起的等等。

4. 发明专利

JPH08217695A SKIN PREPARATION FOR EXTERNAL USE 失效
公开(公告)号：JPH08217695A
公开(公告)日：1996-08-27
申请号：JP4646595
申请日：1995-02-10
申请人： POLA CHEM IND INC
发明人： ENDO MASAYUKI , SAGIYA HIROMICHI , SATO MASAHIRO , ISO TOSHIAKI , FUNAYAMA NOBUO , HIYAMA NAOKI , UMEDA MINAKO
IPC分类号： C07D487/04 , A61K8/00 , A61K8/30 , A61K8/44 , A61K8/49 , A61K8/73 , A61K31/415 , A61K31/435 , A61K31/505 , A61K31/55 , A61K45/00 , A61P17/00 , A61P43/00 , A61Q19/00 , C07D401/06 , C07D403/06 , C07D471/08 , A61K7/00 , A61K7/48
摘要： PURPOSE: To obtain the subject skin preparation for external use effective for treating pruritus such as atopic dermatitis, containing a specific moisture- retaining component and an antagonist. CONSTITUTION: The skin preparation for external use contains (A) 5-40wt.% one or more moisture-retaining components of an amino acid (preferably lysine, threonine, serine, alanine or glycine) and/or its salt, a saccharide (preferably glucose, lactose or maltose), a polyhydric alcohol containing three or more OH groups (preferably glycerol), a polysaccharide (preferably chondroitinsulfuric acid, mucin or chitin) and/or its salt, a pyrrolidonecarboxylic acid and/or its salt and a phospholipid (preferably lecithin) and (B) 0.01-5wt.% antagonist of 5-hydroxytryptamine (preferably 1,2,3,4,10,14bhexahydro-2-methyldibenzo[c, f]pyrazino[1,2-a]azepine of formula.

5. 发明专利

JP2002201127A UREA DERIVATIVE 失效
公开(公告)号：JP2002201127A
公开(公告)日：2002-07-16
申请号：JP2000402702
申请日：2000-12-28
申请人： POLA CHEM IND INC
发明人： NAMIKI TAKAYUKI , KISHII KENICHI , MITANI MASAMIKI , TAMAI MASASHI , HIYAMA NAOKI , KIMURA MAKOTO , ICHINOMIYA SATOSHI
IPC分类号： C07D257/04 , A61K31/41 , A61P3/06 , A61P9/10 , A61P9/12
摘要： PROBLEM TO BE SOLVED: To obtain a medicine having antihypertensive actions and antihyperlipemic actions on complications of hypertension and hyperlipemia. SOLUTION: This compound represented by the formula (A) [R1 denotes a 5-7C alkyl group; R2 denotes an aromatic hydrocarbon group or a cycloalkyl group which may have a substituent group; R3 denotes tetrazolyl group or NHSO2CF3; and Z denotes a single bond or SO2NH] or its salt is found to have antagonistic actions on angiotensin II receptors and inhibitory actions on acylcoenzyme A cholesterol acyltransferases.

6. 发明专利

JPH08208518A ANTIPRURITIC AGENT 失效
公开(公告)号：JPH08208518A
公开(公告)日：1996-08-13
申请号：JP1824695
申请日：1995-02-06
申请人： POLA CHEM IND INC
发明人： FUNAYAMA NOBUO , SAGIYA HIROMICHI , SATO MASAHIRO , ISO TOSHIAKI , ENDO MASAYUKI , HIYAMA NAOKI , UMEDA MINAKO
IPC分类号： C07D487/04 , A61K9/00 , A61K31/415 , A61K31/435 , A61K31/505 , A61K31/55 , A61K45/00 , A61P17/00 , A61P43/00 , C07D401/06 , C07D403/06 , C07D451/00
摘要： PURPOSE: To obtain an antipruritic agent which contains a hydroxytryptamine antagonist as an active ingredient and is effective for treating itching, particularly efficacious for improving atopic dermatitis resistant to conventional anti- inflammatory analgesic agents. CONSTITUTION: This agent contains a 5-hydroxytryptamine antagonist, typically 1-methylindol-3-yl-carbonyl-4,5,6,7-tetrahydrobenzimidazole. The daily doses of the 5-hydroxytryptamine antagonist are 1-1,000mg orally., 0.1-500mg in injection and 0.1-500mg percutaneously per an adult. This agent is preferably used in the form of an external preparation for skin since it can be applied near a lesion with side-effect reduced, and the external preparation contains this agent in a concentration of 0.1-5wt.%.

7. 发明专利

JPH10120683A PYRROLOPYRAZOLOPYRIMIDINE AND MEDICINE CONTAINING THE SAME AS ACTIVE INGREDIENT 失效
公开(公告)号：JPH10120683A
公开(公告)日：1998-05-12
申请号：JP23086297
申请日：1997-08-27
申请人： POLA CHEM IND INC
发明人： NAMIKI TAKAYUKI , YUASA MASAYUKI , TAKAKUWA TAKAKO , ICHINOMIYA SATOSHI , KAWAZU YUKIO , KISHII KENICHI , FUNAYAMA NOBUO , HARADA MARIKO , TANEDA KYOKO , HIYAMA NAOKI , YAHIRO TOMOAKI , SUGIO MAYUMI
IPC分类号： C07D487/14 , A61K31/505 , A61P11/00 , A61P11/08
摘要： PROBLEM TO BE SOLVED: To obtain the subject new compound which comprises a specific pyrrolopyrazolopyrimidine, has excellent bronchodilation and airways contraction inhibitory action and is useful as a medicine for respiratory diseases with weak action on circulatory organs and reduced in side-effects. SOLUTION: This compound is a new 1 pyerrolopyrazolopyrimidine represented by formula I [R is an alkyl; R is H, a halogen, a (substituted) alkyl, a (substituted) amino, carboxyl, an alkoxycarbonyl, carbamoyl, an alkylcarbamoyl; R is nitro, amino, a heterocyclic group, a (halogen-substituted) alkylsulfonylamino, R CONH (R is an alkyl, carboxyl or the like), R CO (R is amino, OH, an alkyl, an alkoxy)] and is useful for prevention and treatment of respiratory diseases. The compound is prepared by reaction of a pyrazolopyrimidine of formula II (X is a halogen) with a compound represented by the formula: NH2 -R .

8. 发明专利

JPH08217694A ANTI-ITCHING SKIN PREPARATION FOR EXTERNAL USE 失效
公开(公告)号：JPH08217694A
公开(公告)日：1996-08-27
申请号：JP4490895
申请日：1995-02-09
申请人： POLA CHEM IND INC
发明人： ENDO MASAYUKI , SAGIYA HIROMICHI , SATO MASAHIRO , ISO TOSHIAKI , FUNAYAMA NOBUO , HIYAMA NAOKI , UMEDA MINAKO
IPC分类号： A61K47/10 , A61K31/415 , A61K31/435 , A61K31/505 , A61K31/55 , A61K45/00 , A61P17/00 , A61P37/08 , A61P43/00
摘要： PURPOSE: To obtain the subject skin preparation for external use useful for treating pruritus such as atopic dermatitis, containing a specific antagonist and an alcohol having short chain length. CONSTITUTION: The skin preparation for external use contains (A) preferably 0.01-1wt.% antagonist of 5-hydroxytryptamine and (B) preferably 1-90wt.% one or more of alcohols having short chain length (preferably ethanol, isopropanol or n-propanol). 1,2,3,4,10,14b-Hexahydro-2-methyldibenzo[c,f] pyrazino[1,2-a]azepine of formula I, 1-methylindol-3-yl-carbonyl-4,5,6,7- tetrahydrobenzimidazole of formula II or 1-methyl-N-(endo-9-methyl-9- azabicyclo[3,3,1]non-3-yl)-H-indole-carboxamide of formula III can be used as the component A.

9. 发明专利

JP2004267244A Evaluation method of wrinkle 审中-公开
标题翻译：皱纹的评价方法
公开(公告)号：JP2004267244A
公开(公告)日：2004-09-30
申请号：JP2003058110
申请日：2003-03-05
申请人： Pola Chem Ind Inc , ポーラ化成工業株式会社
发明人： GOMI TAKAMASA , NISHIMORI YASUTOMO , HIYAMA NAOKI , SHISHIDO MAYUMI
IPC分类号： G01B11/02 , A61B5/107 , A61B5/117 , G01N21/17
摘要： PROBLEM TO BE SOLVED: To provide a quantitative evaluation method of wrinkle by two-dimensionalizing the image of a part formed with the wrinkle, extracting the part of the wrinkle from the two-dimensional image, non-visualizing the image other than the wrinkle, converting the shape of the wrinkle part into a physical quantity and comparing physical quantities for every individual. SOLUTION: This evaluation method of the wrinkle formed on an animal two-dimensionalizes the image of the part formed with the wrinkle, extracts the part of the wrinkle from the two-dimensional image, non-visualizes the image of the part other than the wrinkle, converts the shape of the wrinkle into the physical quantity and compares the physical quantities for every individual. A favorably citable two-dimensionalizing means is photography or the like. A favorably citable means which extracts the wrinkle part, non-visualizes the image other than the part of the wrinkle and converts the shape of the wrinkle into the physical quantity is a method of putting a transparent and/or translucent sheet on a photography, copying the part of the wrinkle on the transparent and/or translucent sheet, and measuring the length of a taken line segment. COPYRIGHT: (C)2004,JPO&NCIPI
摘要翻译：要解决的问题：为了通过对形成有皱纹的部分的图像进行二维化来提供皱纹的定量评估方法，从二维图像中提取部分褶皱，不可视化图像以外的图像皱纹，将皱纹部分的形状转换成物理量，并比较每个人的物理量。解决方案：这种在动物上形成的皱纹的评估方法使形成皱纹的部分的图像二维化，从二维图像中提取部分皱纹，使其他部分的图像不可视化比皱纹，将皱纹的形状转换成物理量，并比较每个人的物理量。有利地可引用的二维化装置是摄影等。有利的可引用方式是提取皱纹部分，除皱部分以外的图像不可视化，并将皱纹的形状转换成物理量是将透明和/或半透明片材放置在摄影，复印透明片和/或半透明片上的部分褶皱，并测量所取线段的长度。版权所有（C）2004，JPO＆NCIPI

10. 发明专利

JP2004107256A New biphenylimidazopyridine derivative and medicine comprising the same as active ingredient 有权
公开(公告)号：JP2004107256A
公开(公告)日：2004-04-08
申请号：JP2002271897
申请日：2002-09-18
申请人： Pola Chem Ind Inc , ポーラ化成工業株式会社
发明人： NAMIKI TAKAYUKI , MITANI MASAMIKI , TAMAI MASASHI , KISHII KENICHI , HIYAMA NAOKI , KIMURA MAKOTO , MASUDA TOMOKO , ICHINOMIYA SATOSHI
IPC分类号： C07D471/04 , A61K31/437 , A61P3/06 , A61P9/10 , A61P9/12 , A61P43/00
摘要： PROBLEM TO BE SOLVED: To obtain a compound useful for preventing and treating complication of hypertension and hyperlipemia and diseases caused by the complication. SOLUTION: The biphenylimidazopyridine derivative represented by general formula (1) (R 1 and R 2 are each independently a 1-6C straight-chain, branched or cyclic alkyl group; R 3 is a phenyl group which may contain a 1-6C straight-chain, branched or cyclic alkyl group and/or a halogen atom as a substituent group or a 1-8C straight-chain, branched or cyclic alkyl; X is an aminosulfonyl bond (NHSO 2 ), a sulfonylaminosulfonyl bond (SO 2 NHSO 2 ), a sulfonylaminocarbonyl bond (SO 2 NHCO) or a sulfonylurea bond (SO 2 NHCONH)). The prophylactic and/or the therapeutic agent for the complication of hypertension and hyperlipemia comprises the derivative or its salt as an active ingredient. The biphenylimidazopyridine derivative and the medicine comprising it as the active ingredient have angiotensin II receptor antagonism and ACAT inhibiting activity and are useful for preventing and/or treating the complication of hypertension and hyperlipemia and diseases caused by the complication. COPYRIGHT: (C)2004,JPO

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