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1. 发明专利

JP2000204078A TYPE I PROTEIN, GERANYLGERANYLTRANSFERASE INHIBITORY COMPOUND 失效
公开(公告)号：JP2000204078A
公开(公告)日：2000-07-25
申请号：JP524999
申请日：1999-01-12
申请人： BANYU PHARMA CO LTD
发明人： OKUBO MITSURU , ONO JUN , ASAHI SHUICHI , SAGARA TAKESHI , SATO TOSHIHIKO , MORISHIMA HAJIME
IPC分类号： C07D233/64 , A61K31/00 , A61K31/415 , A61K31/4164 , A61K38/55 , A61P31/00 , A61P31/04 , C07K5/06
摘要： PROBLEM TO BE SOLVED: To obtain a new compound having an excellent type I protein geranylgeranyltransferase inhibitory activity and useful as an antifungal agent having a new action mechanism. SOLUTION: This type I protein geranylgeranyltransferase inhibitory compound is a compound of formula I (X is O or NH; W is carbonyl or methylene; R is a non-aromatic heterocyclic ring, an aliphatic ring, a 7-12C aralkyl or the like; Y is an aryl substitutable with a halogen; B is H, carbamoyl or an amino 1-3C alkylcarbamoyl), e.g. a compound of formula II. The compound of the formula I is obtained by performing a condensation reaction of a compound of formula III (Tr is trityl) obtained from histamine wish a compound of formula IV [e.g.; N-(1-indanecarbonyl)-D-1-naphthylalanine] in an inert solvent such as dimethylformamide, in the presence of a base such as hydrazine- monohydrate preferably at 20-60 deg.C for 1-12 hr and then de-blocking.

2. 发明专利

JP2000119226A PRODUCTION OF NEW AROMATIC AMINE OR AROMATIC HETEROCYCLIC AMINE UTILIZING CURTIUS REARRANGEMENT REACTION IN SOLID PHASE SYNTHESIS 失效
公开(公告)号：JP2000119226A
公开(公告)日：2000-04-25
申请号：JP29086998
申请日：1998-10-13
申请人： BANYU PHARMA CO LTD
发明人： SUNAMI SATOSHI , OKUBO MITSURU , SAGARA TAKESHI
IPC分类号： C07D213/73 , C07C209/56 , C07C211/44 , C07C211/47 , C07C211/50 , C07C211/52 , C07D213/74
摘要： PROBLEM TO BE SOLVED: To effectively and rapidly synthesize the subject amine useful as an intermediate for medicaments by utilizing Curtius rearrangement reaction of an aromatic (heterocyclic) carboxylic acid is solid phase. SOLUTION: This aromatic amine or aromatic heterocyclic amine is obtained by the following process: on (A) solid particles (pref. of p-benzyloxybenzyl alcohol resin), (B) an aromatic carboxylic acid (pref. substituted benzoic acid) or aromatic heterocyclic carboxylic acid (pref. substituted pyridinecarboxylic acid) is reacted with (C) an azide compound (pref. disphenylphosphoryl azide) to effect immobilization of (D) an aromatic substituted carbamate or aromatic heterocyclic substituted carbamate on the component A followed by, as necessary in the presence of a base, reaction of the component D with one or more kinds of reactant selected from alkylating agent, alkenylating agent and aralkylating agent and then isolating and collecting the objective amine from the component A.

3. 发明专利

JP2000204087A INHIBITOR AGAINST GERANYLGERANYL TRANSFERASE, I-TYPE PROTEIN 失效
公开(公告)号：JP2000204087A
公开(公告)日：2000-07-25
申请号：JP493999
申请日：1999-01-12
申请人： BANYU PHARMA CO LTD
发明人： OKUBO MITSURU , ONO JUN , ASAHI SHUICHI , SAGARA TAKESHI , SATO TOSHIHIKO , MORISHIMA HAJIME
IPC分类号： C07D277/20 , A61K31/00 , A61K31/425 , A61K31/426 , A61P31/00 , A61P31/10 , C07D277/56
摘要： PROBLEM TO BE SOLVED: To obtain a new compound useful as an antifungal agent, excellent in inhibiting activity against geranylgeranyl transferase, a fungous I-type protein, and having a new mode of action. SOLUTION: A compound of formula I (B is a 1-3C alkylene optionally having a 6-12C aryl or a single bond; Z is O, S or a single bond; R1 is a non-aromatic heterocycle, an aliphatic ring, a 6-12C aryl or the like; Y is a carbonyl or methylene; A is O or NH; X1 is a 2-5C alkylene, a 3-7C cycloalkylene, a 2-5C alkenylene or the like), for example, a compound of formula II The compound of formula I is obtained by condensing, for example, a compound of formula III [e.g. 2-(1,4-benzodioxan)carboxylic acid] with a compound of the formula: HAX1STr (Tr is trityl) (e.g. the compound of formula IV) in an inert solvent such as dimethylformamide in the presence of a base such as dimethylaminopyridine preferably at 20-60 deg.C for 1-12 hr followed by deblocking.

4. 发明专利

JPH10287637A AMIDINE DERIVATIVE 失效
公开(公告)号：JPH10287637A
公开(公告)日：1998-10-27
申请号：JP11183797
申请日：1997-04-14
申请人： BANYU PHARMA CO LTD
发明人： ITO SATOSHI , SAGARA TAKESHI , KOITO SEITA , NISHIOKA AKIRA , OUCHI KENJI , FUKURODA NAOHIRO
IPC分类号： C07D295/14 , A61K31/16 , A61K31/165 , A61K31/40 , A61K31/47 , A61K31/472 , A61K31/535 , A61K31/5375 , A61K31/55 , A61P3/00 , A61P3/08 , A61P3/10 , A61P9/00 , A61P25/00 , A61P27/02 , A61P43/00 , C07C257/14 , C07D213/81 , C07D217/04 , C07D295/16
摘要： PROBLEM TO BE SOLVED: To provide a new amidine derivative having antagonistic action on neuropeptide Y receptor and useful as an agent for the treatment or prevention of hyperphagia, obesity and diabetes. SOLUTION: This compound is expressed by formula I (n) is 0-6; (p) is 0 or 1; R is a group of formula II [Ar is an aryl; (k) is 0 or 1; (m) is 0-2; A is single bond, NH, etc.]; R is H, an aryl, etc.; R is NH(CH2 )r R [(r) is 1-2; R is an aryl, etc., etc.; X is (CH2 )t [(t) is 3 or 4], etc.}, e.g. N-[DL-N-α-(p- biphenylacetyl)-p-[[3-(p-dimethylaminophenyl)-1-imino-2- propenyl]aminomethyl]phenylalanyltetrahydroisoquinone. A drug is produced by including the compound in an amount of 1.0-100 wt.% based on the total drug. The daily administration rate of the compound is generally 0.1-100 mg/kg for adult in 1 to several divided doses. The compound of the formula can be synthesized by using the reaction of a compound of formula III with a compound of formula R CO2 H as the starting process.

5. 发明专利

JPH10237036A PRODUCTION OF AMIDINE 失效
公开(公告)号：JPH10237036A
公开(公告)日：1998-09-08
申请号：JP5854097
申请日：1997-02-26
申请人： BANYU PHARMA CO LTD
发明人： SAGARA TAKESHI , ITO SATOSHI , KOITO SEITA , NISHIOKA AKIRA
IPC分类号： B01J31/02 , C07B61/00 , C07C257/14
摘要： PROBLEM TO BE SOLVED: To efficiently and simply synthesize an optically active amidine by reacting an imide eater with an amine immobilized on solid granules in the presence of a mixture solution comprising a halogenated hydrocarbon, a base and a lower alcohol. SOLUTION: This method for producing an amidine comprises (1) chemically binding a protected amine derivative or a compound having a functional group capable of being converted into an amino group to a solid reaction carrier, (2) removing the protecting group from the amino group or converting the functional group capable of being converted into an amino group into the amino group, (3) treating the amine, such as an amino acid, held no the solid carrier with an imide ester acid adduct (preferably an imide lower alkyl ester) in the pressure of a mixture comprising a halogenated hydrocarbon, a base and a lower alcohol (especially preferably a mixture solution of methylene chloride, triethylamine and methanol), and (4) if necessary, subjecting the amidine derivative held on the solid carrier to a protecting group-removing reaction and further to a derivation reaction and subsequently releasing the obtained amidine from the solid carrier.

6. 发明公开

EP1754706A4 SELECTIVE INHIBITORS AGAINST Cdk4 AND Cdk6 HAVING AMINOTHIAZOLE SKELETON 审中-公开
标题翻译：选择性抑制剂反对CDK4和CDK6与AMINOTHIAZOLSKELETT
公开(公告)号：EP1754706A4
公开(公告)日：2010-08-18
申请号：EP05743671
申请日：2005-05-19
申请人： BANYU PHARMA CO LTD
发明人： IWASAWA YOSHIKAZU , SHIBATA JUN , SHIMAMURA TADASHI , KURIHARA HIDEKI , MITA TAKASHI , KAWANISHI NOBUHIKO , HASHIHAYATA TAKASHI , KAWAMURA MIKAKO , SAGARA TAKESHI , ARAI SACHIE , HIRAI HIROSHI
IPC分类号： C07D417/12 , A61K31/506 , A61K31/513 , A61K31/5377 , A61P35/00 , A61P43/00 , C07D417/14 , C07D491/08
CPC分类号： C07D417/14 , C07D417/12 , C07D491/08

7. 发明公开

EP1914232A4 N-DIHYDROXYALKYL-SUBSTITUTED 2-OXOIMIDAZOLE DERIVATIVE 有权转让
标题翻译： N-二羟基烷基取代基2-氧代氨基甲酸酯
公开(公告)号：EP1914232A4
公开(公告)日：2009-10-28
申请号：EP06781147
申请日：2006-07-11
申请人： BANYU PHARMA CO LTD
发明人： HASHIMOTO MASAYA , IWASAWA YOSHIKAZU , KAWAMOTO HIROSHI , OHTA HISASHI , OZAKI SATOSHI , SAGARA TAKESHI , SAKOH HIROKI , SATOH ATSUSHI
IPC分类号： C07D401/04 , A61K31/454 , A61P3/04 , A61P9/00 , A61P9/02 , A61P9/10 , A61P13/02 , A61P19/02 , A61P19/06 , A61P25/06 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P29/00 , A61P43/00
CPC分类号： C07D401/04

8. 发明公开

EP1415986A4 SPIRO COMPOUNDS 有权
标题翻译：螺环化合物
公开(公告)号：EP1415986A4
公开(公告)日：2005-11-02
申请号：EP02755790
申请日：2002-08-02
申请人： BANYU PHARMA CO LTD
发明人： FUKAMI TAKEHIRO , NONOSHITA KATSUMASA , SAGARA TAKESHI , KISHINO HIROYUKI
IPC分类号： A61K31/4747 , A61P1/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/00 , A61P9/00 , A61P9/02 , A61P9/10 , A61P9/12 , A61P11/00 , A61P13/12 , A61P15/00 , A61P25/04 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P27/06 , A61P29/00 , A61P43/00 , C07D209/96 , C07D307/94 , C07D401/12 , C07D403/12 , C07D405/12 , C07D471/10 , C07D491/10 , C07D491/107 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/506 , A61P25/00 , C07D403/14
CPC分类号： C07D401/12 , A61K31/4747 , C07D209/96 , C07D307/94 , C07D403/12 , C07D405/12 , C07D471/10 , C07D491/10
摘要： The invention relates to compounds represented by the general formula (|) or the like: (|) [wherein A is a linear C1-6 hydrocarbon group which may be substituted or interrupted by oxygen or nitrogen; Ar1 is an aryl or heteroaryl group which may be substituted; n is 0 or 1; R0 is hydrogen or lower alkylene attached to an arbitrary binding site of A; T, U, V and W are each optionally substituted methine or nitrogen, with the proviso that at least two of them are each methine; X is -N(SO2R1)-, -N(COR2)-, or -CO-; Y is -C(R3)(R4)-, -O-, or -N(R5)-; and Z is methine or nitrogen]. The compounds exhibit NPY antagonism and are therefore useful as treating agents for various diseases in which NPY participates, e.g., circulatory diseases, central nervous system diseases such as hyperphagia, metabolic diseases such as obesity and diabetes, and so on.

9. 发明公开

EP2016080A4 DIHYDROPYRAZOLOPYRIMIDINONE DERIVATIVES 有权转让
标题翻译： DIHYDROPYRAZOLOPYRIMIDINONDERIVATE
公开(公告)号：EP2016080A4
公开(公告)日：2009-05-13
申请号：EP07742843
申请日：2007-04-25
申请人： BANYU PHARMA CO LTD
发明人： SAKAMOTO TOSHIHIRO , SUNAMI SATOSHI , YAMAMOTO FUYUKI , NIIYAMA KENJI , BAMBA MAKOTO , TAKAHASHI KEIJI , FURUYAMA HIDETOMO , SAGARA TAKESHI , OTSUKI SACHIE , NISHIBATA TOSHIHIDE , YOSHIZUMI TAKASHI , HIRAI HIROSHI
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00 , A61P43/00
CPC分类号： C07D487/04 , A61K31/4162 , A61K31/519

10. 发明公开

EP2017278A4 DIHYDROPYRAZOLOPYRIMIDINONE DERIVATIVE 有权转让
标题翻译： DIHYDROPYRAZOLOPYRIMIDINONDERIVAT
公开(公告)号：EP2017278A4
公开(公告)日：2009-04-22
申请号：EP07742851
申请日：2007-04-25
申请人： BANYU PHARMA CO LTD
发明人： SAKAMOTO TOSHIHIRO , SUNAMI SATOSHI , YAMAMOTO FUYUKI , NIIYAMA KENJI , BAMBA MAKOTO , TAKAHASHI KEIJI , FURUYAMA HIDETOMO , GOTO YASUHIRO , SAGARA TAKESHI , OTSUKI SACHIE , NISHIBATA TOSHIHIDE , YOSHIZUMI TAKASHI , HIRAI HIROSHI
IPC分类号： C07D471/04 , A61K31/519 , A61K31/5377 , A61K31/54 , A61K31/551 , A61P35/00 , A61P43/00 , C07D487/04
CPC分类号： C07D487/04 , A61K31/4162 , A61K31/519
摘要： Disclosed is a compound represented by the following general formula (I) or the like. (I) (In the formula, Ar1 represents an optionally substituted aryl group or heteroaromatic ring group; R1 represents an optionally substituted lower alkyl group, lower alkenyl group, lower alkynyl group or cyclo-lower alkyl group, or alternatively an optionally substituted aryl group, aralkyl group or heteroaromatic ring group; R2 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, or alternatively an optionally substituted aryl group, aralkyl group or heteroaromatic ring group; R3 represents a hydrogen atom or a lower alkyl group; R4 represents a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a group represented by -N(R1k)R1m; and T and U respectively represent a nitrogen atom or a methine group.) This compound has an excellent Wee1 kinase inhibitory activity, and thus is useful in the field of pharmaceutical products, particularly in the field of drugs for treating various cancers.
摘要翻译：公开了由以下通式（I）等表示的化合物。（I）（式中，Ar 1表示可以具有取代基的芳基或杂芳环基，R 1表示可以具有取代基的低级烷基，低级链烯基，低级炔基或环低级烷基，或者可以具有取代基的芳基，芳烷基或杂芳环基; R 2表示氢原子，低级烷基，低级链烯基或低级炔基，或者可选地取代的芳基，芳烷基或杂芳环基; R 3表示氢原子或低级烷基; R 4表示氢原子，卤素原子，羟基，低级烷基或由-N（R 1k）R 1 m表示的基团; T和U分别表示氮原子或次甲基。该化合物具有优异的Wee1激酶抑制活性，因此可用于药品领域，特别是用于治疗各种癌症的药物领域。

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