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1. 发明公开

EP1157997A4 NOVEL DIPEPTIDE COMPOUND AND MEDICINAL USE THEREOF 审中-公开
标题翻译：新的二肽连接及他们的医疗用途
公开(公告)号：EP1157997A4
公开(公告)日：2002-05-08
申请号：EP00987774
申请日：2000-12-28
申请人： JAPAN ENERGY CORP
发明人： MIMOTO TSUTOMU , TERASHIMA KEISUKE , TAKAKU HARUO , MATSUMOTO SHINJI , SHINTANI MAKOTO , NOJIMA SATOSHI
IPC分类号： A61P31/18 , C07D207/16 , C07D277/06 , C07K5/023 , A61K31/426 , C07D207/14 , C07D277/04
CPC分类号： C07D277/06 , C07D207/16
摘要： A novel dipeptide compound which inhibits the enzymatic activity of an HIV protease and is represented by formula (I); and an anti-AIDS agent containing the dipeptide compound as the active ingredient. [In the formula, R?1, R2, and R3¿ each represents C¿1-4? alkyl, alkoxy, hydrogen, etc. (provided that not all of R?1, R2, and R3¿ are hydrogen) and R?2 and R3¿ may be bonded to each other to form a ring; R4 represents C¿1-4? alkyl or hydrogen; X represents methylene or sulfur; Y represents, e.g., a five- or six-membered monocycle or aryloxyalkyl having up to 12 carbon atoms (provided that the aromatic ring may have been substituted by alkyl, etc.); and Z represents a C1-6 aliphatic hydrocarbon or an aromatic hydrocarbon having up to 12 carbon atoms (provided that this aromatic ring may have been substituted by alkyl, etc. or at least one carbon atom of the aromatic hydrocarbon may have been replaced with a heteroatom).]

2. 发明公开

EP0882727A4 NOVEL PURINE DERIVATIVES 失效
标题翻译：新的嘌呤衍生物
公开(公告)号：EP0882727A4
公开(公告)日：2000-01-26
申请号：EP97929512
申请日：1997-07-03
申请人： JAPAN ENERGY CORP
发明人： HIROTA KOHSAKU , ISOBE YOSHIAKI , CHIBA NOBUYOSHI , SATOH HARUMI , TAKAKU HARUO , MATSUI HIROYUKI , OGITA HARUHISA
IPC分类号： C07D473/00 , C07D473/30 , C07D473/34 , A61K31/52
CPC分类号： C07D473/00 , C07D473/30 , C07D473/34
摘要： Purine derivatives represented by general formula (I), their tautomers or pharmaceutically acceptable salts thereof, and interferon secretion inducers, antiviral agents and anticancer drugs containing the same. In said formula (I) R2 represents hydrogen or hydrocarbyl (wherein -CH¿2?- not directly bonded to the purine skeleton and CH2 in -CH3 not directly bonded to the purine skeleton may be replaced by carbonyl, sulfonyl, -O- or -S-; =CH2 may be replaced by =O or =S; and C-H in -CH2 not directly bonded to the purine skeleton, C-H in -CH3 not directly bonded to the purine skeleton, C-H in ⊃ CH not directly bonded to the purine skeleton, C-H in =CH- not directly bonded to the purine skeleton and C-H in =CH2 may be replaced by N, C-halogeno or C-CN); R?6¿ represents hydroxy or amino optionally substituted by one or two hydrocarbon groups; R8 represents hydroxy, mercaptor, acyloxy or oxycarbonyl substituted by hydrocarbyl; and R9 represents hydrocarbyl (wherein -CH¿2?- not directly bonded to the purine skeleton and CH2 in -CH3 not directly bonded to the purine skeleton may be replaced by carbonyl, sulfonyl, -O- or -S-; =CH2 may be replaced by =O or =S; and C-H in -CH2 not directly bonded to the purine skeleton, C-H in -CH3 not directly bonded to the purine skeleton, C-H in > CH not directly bonded to the purine skeleton, C-H in =CH- not directly bonded to the purine skeleton, C-H in =CH2 and C-H in CH may be replaced by N, C-halogeno or C-CN).

3. 发明公开

EP0900566A4 NOVEL TRIPEPTIDE COMPOUNDS AND ANTI-AIDS DRUGS 失效
标题翻译：新型TRIPEPTIDVEBINDUNGEN及药物防治艾滋病
公开(公告)号：EP0900566A4
公开(公告)日：2001-04-25
申请号：EP97949191
申请日：1997-12-22
申请人： JAPAN ENERGY CORP
发明人： TAKAKU HARUO , NOJIMA SATOSHI , MIMOTO TSUTOMU , TERASHIMA KEISUKE , KISO YOSHIAKI
IPC分类号： C07D263/04 , C07D277/06 , C07D417/12 , C07K5/02 , A61K31/40 , A61K31/42 , A61K31/425 , A61K31/47 , A61K31/495 , A61K38/05 , A61K38/07 , C07D207/16 , C07D241/04 , C07K5/078 , C07K5/117
CPC分类号： C07D263/04 , C07D277/06 , C07D417/12 , C07K5/0202
摘要： Novel tripeptide compounds having excellent HIV protease inhibitory activites and represented by general formula (I), pharmacologically acceptable salts thereof, and anti-AIDS drugs containing the same as the active ingredient. An example of the compounds is (R)-N-(2-methylbenzyl)-3-{(2S, 3S)-3-[N-(2-chromonecarbonyl)-L-asparaginyl]amino-2-hydroxy-4-phenylbutanoyl}-5, 5-dimethyl-1, 3-thiazolidine-4-carboxamide.

4. 发明专利

ZA9811778B Inhibitors of type 2 helper t cell-selective immune response 未知
公开(公告)号：ZA9811778B
公开(公告)日：1999-06-22
申请号：ZA9811778
申请日：1998-12-22
申请人： JAPAN ENERGY CORP
发明人： ISOBE YOSHIAKI , OGITA HARUHISA , TOBE MASANORI , TAKAKU HARUO , MATSUI HIROYUKI , TOMIZAWA HIDEYUKI
IPC分类号： A61K31/52 , C07D473/00 , C07D473/34 , A61K

5. 发明专利

NZ329798A PURINE DERIVATIVES THEIR TAUTOMERS AND SALTS THEREOF AND INTERFERON SECRETION INDUCERS, ANTIVIRAL AGENTS AND ANTICANCER DRUGS CONTAINING THE SAME 未知
公开(公告)号：NZ329798A
公开(公告)日：1999-04-29
申请号：NZ32979897
申请日：1997-07-03
申请人： JAPAN ENERGY CORP
发明人： HIROTA KOHSAKU , ISOBE YOSHIAKI , CHIBA NOBUYOSHI , TAKAKU HARUO , MATSUI HIROYUKI , OGITA HARUHISA
IPC分类号： C07D473/00 , C07D473/30 , C07D473/34 , A61K31/52
摘要： A purine derivative represented by the following general formula (I): wherein R is a hydrogen atom or a hydrocarbon group containing at most 14 carbon atoms; any -CH2- group in said hydrocarbon group may be replaced with a carbonyl group, a sulfonyl group, -O- or -S- when said -CH2- group is not directly attached to the purine ring or is in -CH3 group not directly attached to the purine ring; any =CH2 group may be replaced with =O or =S; C-H group in said hydrocarbon group may be replaced with N, a C-halogen group or a C-CN group when said C-H group is in -CH2-group not directly attached to the purine ring, in -CH3 group not directly attached to the purine ring, in >CH-group not directly attached to the purine ring, in =CH-group not directly attached to the purine ring or in =CH2 group; R is a hydroxyl group, an amino group or an amino group mono- or di-substituted with a hydrocarbon group containing at most 10 carbon atoms; R is a hydroxyl group, a mercapto group, an acyloxy group containing at most 18 carbon atoms or an oxycarbonyloxy group substituted with a hydrocarbon group containing at most 19 carbon atoms; R is a hydrocarbon group containing at most 14 carbon atoms; any -CH2- group in said R may be replaced with a carbonyl group, a sulfonyl group, -O- or -S- when said -CH2- group is not directly attached to the purine ring or is in -CH3 group not directly attached to the purine ring; any =CH2 group may be replaced with =O or =S; C-H group in said R may be replaced with N, a C-halogen group or a C-CN group when said C-H group is in -CH2-group not directly attached to the purine ring, in -CH3 group not directly attached to the purine ring, in >CH-group not directly attached to the purine ring, in =CH-group not directly attached to the purine ring, in =CH2 group or in IDENTICAL CH group; or its tautomer or pharmaceutically acceptable salts thereof, and an interferon inducer, an anti-virus agent or an anti-cancer agent which comprises said purine derivative or pharmaceutically acceptable salts thereof as an active ingredient.

6. 发明专利

NO984284D0 未知
公开(公告)号：NO984284D0
公开(公告)日：1998-09-16
申请号：NO984284
申请日：1998-09-16
申请人： JAPAN ENERGY CORP
发明人： TAKAKU HARUO , NOJIMA SATOSHI , MIMOTO TSUTOMU , TERASHIMA KEISUKE , KISO YOSHIAKI
IPC分类号： C07D263/04 , C07D277/06 , C07D417/12 , C07K5/02 , C07K
摘要： A novel tripeptide compound represented by the following general formula (I) exhibiting superior HIV protease inhibition activity, and an anti-AIDS medicine comprising this compound as an effective component and a pharmaceutically acceptable salt thereof. (R)-N-(2-methylbenzyl)-3-ä(2S,3S)-3-ÄN-(2-chromonecarbonyl)-L-asparagi nylÜamino-2-hydroxy-4-phenylbutanoylü-5,5-dimethyl-1,3-thiazol idine-4-carboxamide can be given as a typical example of this compound.

7. 发明专利

NO980908L 未知
公开(公告)号：NO980908L
公开(公告)日：1998-04-30
申请号：NO980908
申请日：1998-03-02
申请人： JAPAN ENERGY CORP
发明人： HIROTA KOHSAKU , ISOBE YOSHIAKI , CHIBA NOBUYOSHI , SATOH HARUMI , TAKAKU HARUO , MATSUI HIROYUKI , OGITA HARUHISA
IPC分类号： C07D473/00 , C07D473/30 , C07D473/34 , A61K31/52
摘要： A purine derivative represented by the following general formula (I): wherein R is a hydrogen atom or a hydrocarbon group containing at most 14 carbon atoms; any -CH2- group in said hydrocarbon group may be replaced with a carbonyl group, a sulfonyl group, -O- or -S- when said -CH2- group is not directly attached to the purine ring or is in -CH3 group not directly attached to the purine ring; any =CH2 group may be replaced with =O or =S; C-H group in said hydrocarbon group may be replaced with N, a C-halogen group or a C-CN group when said C-H group is in -CH2-group not directly attached to the purine ring, in -CH3 group not directly attached to the purine ring, in >CH-group not directly attached to the purine ring, in =CH-group not directly attached to the purine ring or in =CH2 group; R is a hydroxyl group, an amino group or an amino group mono- or di-substituted with a hydrocarbon group containing at most 10 carbon atoms; R is a hydroxyl group, a mercapto group, an acyloxy group containing at most 18 carbon atoms or an oxycarbonyloxy group substituted with a hydrocarbon group containing at most 19 carbon atoms; R is a hydrocarbon group containing at most 14 carbon atoms; any -CH2- group in said R may be replaced with a carbonyl group, a sulfonyl group, -O- or -S- when said -CH2- group is not directly attached to the purine ring or is in -CH3 group not directly attached to the purine ring; any =CH2 group may be replaced with =O or =S; C-H group in said R may be replaced with N, a C-halogen group or a C-CN group when said C-H group is in -CH2-group not directly attached to the purine ring, in -CH3 group not directly attached to the purine ring, in >CH-group not directly attached to the purine ring, in =CH-group not directly attached to the purine ring, in =CH2 group or in IDENTICAL CH group; or its tautomer or pharmaceutically acceptable salts thereof, and an interferon inducer, an anti-virus agent or an anti-cancer agent which comprises said purine derivative or pharmaceutically acceptable salts thereof as an active ingredient.

8. 发明专利

NZ514017A Novel dipeptide compound and medicinal use thereof 未知
公开(公告)号：NZ514017A
公开(公告)日：2003-10-31
申请号：NZ51401700
申请日：2000-12-28
申请人： JAPAN ENERGY CORP
发明人： MIMOTO TSUTOMU , TERASHIMA KEISUKE , TAKAKU HARUO , MATSUMOTO SHINJI , SHINTANI MAKOTO , NOJIMA SHUN
IPC分类号： A61P31/18 , C07D207/16 , C07D277/06 , C07K5/023 , A61K31/426 , C07D207/14 , C07D277/04
摘要： A dipeptide compound as shown by formula (I) wherein: R1, R2 and R3 independently represent a linear or branched, saturated or unsaturated lower alkyl group, alkoxyl group, alkyl amino group, or dialkyl amino group having 1-4 carbon atoms (with a carbon atom being either replaced by an oxygen atom or not), a halogeno group, or a hydrogen atom, provided that all of the R1, R2 and R3 are not a hydrogen atom at the same time, R2 and R3 may form a ring together; R4 represents a linear or branched lower alkyl group having 1-4 carbon atoms or a hydrogen atom; X is a methylene group or a sulfur atom; Y represents a five or six member monocyclic or polycyclic hydrocarbon group, a heterocyclic group having a structure in which one or more carbon atom in the monocyclic or polycyclic hydrocarbon group is replaced by a hetero atom, an aryloxyalkyl group having 12 or less carbon atoms, in which one or more carbon atoms in the monocyclic or polycyclic hydrocarbon group is replaced by a hetero atom, an aryloxyalkyl group having 12 or less carbon atoms, in which the monocyclic or polycyclic hydrocarbon group or the aryloxyalkyl aromatic ring may be substituted with an alkyl group, alkoxy group, ahlogeno group, amino group or hydroxyl group; and Z represents an aliphatic hydrocarbon group having 1-6 carbon atoms or an aromatic hydrocarbon group having 12 or less carbon atoms in which the aromatic ring may be substituted with an alkyl group, alkoxy group, or halogeno group, or one or more carbon atom in the aromatic hydrocarbon group may be replaced by a hetero atom. Also disclosed is the use of said compound in the preparation of an anti-AIDS medicine.

9. 发明专利

NZ505297A Type 2 helper t cell-selective immune response inhibitors 未知
公开(公告)号：NZ505297A
公开(公告)日：2001-07-27
申请号：NZ50529798
申请日：1998-12-21
申请人： JAPAN ENERGY CORP
发明人： ISOBE YOSHIAKI , OGITA HARUHISA , TOBE MASANORI , TAKAKU HARUO , MATSUI HIROYUKI , TOMIZAWA HIDEYUKI
IPC分类号： A61K31/52 , C07D473/00 , C07D473/34 , C07D473/16
摘要： A type 2 helper T cell-selective immune response inhibitor of formula (I), the tautomer or a salt of the purine derivative, wherein; R2 is hydrogen or a C1-14 hydrocarbon group in which -CH2- not directly bound to the purine skeleton and CH2 in -CH3 not directly bound to the purine skeleton may be substituted by carbonyl, sulfonyl, -O- or -S-; =CH2 may be substituted by =O or =S; C-H in -CH2- not directly bound to the purine skeleton, C-H in -CH3- not directly bound to the purine skeleton, C-H in >CH- not directly bound to the purine skeleton, C-H in =CH- not directly bound to the purine skeleton and C-H in =CH2 may be substituted by N, C-halogen or C-CN; R6 is hydroxyl, amino or amino which is mono- or di-substituted by a C1-10 hydrocarbon group(s); R8 is hydroxyl, mercapto, C1-18 acyloxy or C1-19 hydrocarbon group-substituting oxycarbonyloxy; and R9 is a C1-14 hydrocarbon group in which -CH2- not directly bound to the purine skeleton and CH2 in -CH3 not directly bound to the purine skeleton may be substituted by carbonyl, sulfonyl, -O- or -S-, =CH2 may be substituted by =O or =S; C-H in -CH2- not directly bound to the purine skeleton, C-H in -CH3- not directly bound to the purine skeleton, C-H in >CH- not directly bound to the purine skeleton, C-H in =CH- not directly bound to the purine skeleton and C-H in =CH2 and C-H in CH may be substituted by N, C-halogen or C-CN. The type 2 helper T cell selective immune response inhibitor enhances the immune response on the type 1 helper T cell side and simultaneously inhibits the immune response on the type 2 helper T cell side. The purine derivatives are used as the active ingredient of pharmaceutical compositions in the treatment of allergic or autoimmune diseases.

10. 发明专利

AU721578B2 Novel tripeptide compounds and anti-aids drugs 未知
公开(公告)号：AU721578B2
公开(公告)日：2000-07-06
申请号：AU7888598
申请日：1997-12-22
申请人： JAPAN ENERGY CORP
发明人： TAKAKU HARUO , NOJIMA SATOSHI , MIMOTO TSUTOMU , TERASHIMA KEISUKE , KISO YOSHIAKI
IPC分类号： C07D263/04 , C07D277/06 , C07D417/12 , C07K5/02 , A61K31/425 , A61K38/06 , C07D241/04
摘要： A novel tripeptide compound represented by the following general formula (I) exhibiting superior HIV protease inhibition activity, and an anti-AIDS medicine comprising this compound as an effective component and a pharmaceutically acceptable salt thereof. (R)-N-(2-methylbenzyl)-3-ä(2S,3S)-3-ÄN-(2-chromonecarbonyl)-L-asparagi nylÜamino-2-hydroxy-4-phenylbutanoylü-5,5-dimethyl-1,3-thiazol idine-4-carboxamide can be given as a typical example of this compound.

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