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1. 发明专利

JP2007326814A Treatment for cancer having resistance to radiotherapy 审中-公开
标题翻译：治疗耐受放射治疗的癌症
公开(公告)号：JP2007326814A
公开(公告)日：2007-12-20
申请号：JP2006159253
申请日：2006-06-08
申请人： Pola Chem Ind Inc , ポーラ化成工業株式会社
发明人： KUBOTA NOBUO , YAHIRO TOMOAKI , TOMIYAMA SUSUMU , FUJIWARA HIROMITSU , SHIRAISHI KOZUE
IPC分类号： A61K31/4168 , A61N5/10 , A61P35/00 , A61P43/00 , C07D233/88
摘要： PROBLEM TO BE SOLVED: To provide a means suppressing relapse and metastasis and further increasing the effect in radiotherapy of radiation resistant cancer except hypoxic state, by irradiating radiation in the presence of 1-(1-hydroxymethyl-2,3-dihydroxypropyl)oxymethyl-2-nitroimidazole.
SOLUTION: In radiotherapy of cancer having radiation resistance, a radiation sensitizer of chemical formula 1 is used to sensitize and treat. The compound of chemical formula 1 of 10-400 mg is administered based on 1 kg body weight of animal or human and radiation is irradiated. The radiation resistant cancer is preferably lung adenocarcinoma. Fractionated irradiation therapy comprising administering 10-400 mg compound of formula 1 per 1 kg body weight to the animal or the human and then repeating 5-40 times irradiation of 1-10 Gy is preferable.
COPYRIGHT: (C)2008,JPO&INPIT
摘要翻译：待解决的问题：为了提供抑制复发和转移的手段，并且进一步增加除了缺氧状态之外的耐辐射癌的放射治疗的效果，通过在1-（1-羟甲基-2,3-二羟基丙基基）氧甲基-2-硝基咪唑。解决方案：在具有耐辐射性的癌症的放射治疗中，化学式1的辐射敏化剂用于敏化和治疗。基于1kg体重的动物或人施用10-400mg的化学式1化合物，并照射辐射。耐辐射癌优选为肺腺癌。分级照射疗法包括给动物或人体每1kg体重10-400mg式1化合物，然后重复5-40次1-10Gy的照射。版权所有（C）2008，JPO＆INPIT

2. 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 .

3. 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.

4. 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 .

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