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公开(公告)号：JP2001031637A
公开(公告)日：2001-02-06
申请号：JP2000144771
申请日：2000-05-17
发明人： FUJISAWA TETSUNORI , KOTAKE SHINJIRO , ITO HAJIME , YASUDA JUNKO , OTANI YOSHIKAZU , MORIKAWA TADANORI
IPC分类号： A61K31/198 , A61K31/223 , A61K31/27 , A61P1/00 , A61P1/02 , A61P11/06 , A61P17/06 , A61P19/02 , A61P25/00 , A61P27/02 , A61P27/16 , A61P37/00 , A61P43/00 , C07C239/14 , C07C239/20 , C07C251/06 , C07C257/14 , C07C317/04
摘要： PROBLEM TO BE SOLVED: To obtain a new compound comprising a hydroxamic acid derivative, capable of inhibiting metalloproteinases and excellent in physiological activities such as percutaneous absorbability or oral absorbability. SOLUTION: This compound is represented by formula I [R1 is H, a (substituted) aralkyl or the like; R2 is H, a (substituted) aralkyloxycarbonyl or the like; R3, R7 and R8 are each H, OH, a (substituted) alkyl or the like; R4 is a (substituted) alkyl or the like; R5 is H, a (substituted) alkyl or the like; R6 is H, OH or the like, X is O, a (substituted) 1-6C alkylene or the like; Y is A-B or the like; A is a (substituted) 1-6C alkylene or the like; B is H, amino or the like], e.g. Na-[4-(N-hydroxyamino)-2(R)-isobutyl-3(S)-(3-phenylpropyl) succinyl]-L-4'-aminomethylphenylalamine. The compound represented by formula I is obtained by respectively converting R9 and R11 to R13 of a compound represented by formula II into the objective groups R3 to R6 and then converting the CO2R10 site of the compound into an amide bond-containing site.
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公开(公告)号：JP2000270874A
公开(公告)日：2000-10-03
申请号：JP8251699
申请日：1999-03-25
发明人： CARLOS LOPEZ-OTIN , CUADRA ELENA LLANO , ALBERTO M PENDAS , JOSE P FUREIHE , AOKI TAKANORI , SHINAGAWA AKIRA , IWATA KAZUSHI
IPC分类号： C12N15/09 , A61K31/00 , A61K31/70 , A61K31/7088 , A61K31/711 , A61K38/46 , A61K39/395 , A61K45/00 , A61K48/00 , A61P9/00 , A61P9/10 , A61P11/00 , A61P19/00 , A61P19/02 , A61P19/10 , A61P21/00 , A61P21/04 , A61P25/00 , A61P25/28 , A61P35/00 , A61P35/04 , A61P43/00 , C07K16/40 , C12N1/19 , C12N1/21 , C12N5/10 , C12N9/50 , C12P21/08 , C12Q1/68 , G01N33/53 , G01N33/573
摘要： PROBLEM TO BE SOLVED: To obtain a new kind of human membrane-bound metalloprotease which can activate progelatinase A and is useful for elucidation of the mechanism of development and treatment of and development of a medicine for various diseases including cancer and so on. SOLUTION: This is a naturally-occurring human membrane-bound metalloprotease which can activate progelatinase A, is a progelatinase-activating factor other than MT1-MMP, MT2-MMP, MT3-MMP, and MT4-MMP, or a new human membrane-bound protein (or salt thereof) which has a homology at 64% or more to the amino acid sequence of the naturally-occurring human membrane-bound protein, a matrix metalloprotease activity, and an ability of activating progelatinase A, or comparable antigenicity, and is useful for elucidation of the mechanism of development and treatment of and development of a medicine for various diseases including cancer and so on. This protein is obtained by cloning from a cDNA library derived from human.
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公开(公告)号：JP2000256384A
公开(公告)日：2000-09-19
申请号：JP5469299
申请日：1999-03-02
摘要： PROBLEM TO BE SOLVED: To obtain the subject new compound capable of exhibiting excellent performances such as chemical selectivity, enantiomer selectivity, catalytic efficiency, or the like, as a catalyst for a catalytic asymmetric synthesis reaction such as an asymmetric hydrogenation reaction, an asymmetric hydrosilylation reaction, or the like. SOLUTION: A 1,1'-bis(dialkylphosphino)ferrocene compound represented by formula I (R1 is a 1-6C alkyl; R2 is a 1-6C alkyl) such as 1,1'-bis(t- butylmethylsulfino)ferrocene. The compound of formula I is obtained by subjecting a borane complex of a 1,1'-bis(dialkylphosphino)ferrocene compound of formula II to deboronation and complexing treatment. The compound of formula I is useful as a ligand, forms a complex with a transition metal selected from the group consisting of rhodium, iridium, ruthenium, palladium and nickel and is useful as a catalyst for asymmetric synthesis.
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4.发明专利
公开(公告)号：JP2000093173A
公开(公告)日：2000-04-04
申请号：JP25110599
申请日：1999-09-06
发明人： HAYAKAWA TARO , OKADA YASUNORI , IWATA KAZUSHI , FUJIMOTO NOBORU , MORI NOBUKO , CHO KEN , KOBAYASHI MASAYOSHI , YONEZAWA KAYOKO , SAKAI CHIE , SHINTANI TAKASHI
IPC分类号： C12N15/09 , C12N5/10 , C12N9/64 , C12N15/02 , C12P21/08 , G01N33/573 , G01N33/574 , G01N33/577
摘要： PROBLEM TO BE SOLVED: To obtain a new monoclonal antibody which is immunoreactive only with an antigen determinant which exists in human stromal collagenase or an antigen determinant which exists in human 92 kDa gelatinase, and is useful for immunohistological analysis of these enzymes and so on. SOLUTION: This is a new monoclonal antibody which is immunoreactive only with an antigen determinant which exists in human stromal collagenase or an antigen determinant which exists in human 92 kDa gelatinase, reacts specifically with potential or active human stromal collagenase or human 92 kDa gelatinase, and is useful for immunohistochemically detecting these enzymes in tissues and cells, and for diagnosing rheumatoid arthritis, cancer, and so on. The monoclonal antibody is obtained by culturing a hybridoma obtained by fusing a mouse spleen cell immunized with these enzymes with a myeloma cell.
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公开(公告)号：JP2000086533A
公开(公告)日：2000-03-28
申请号：JP28044698
申请日：1998-09-17
发明人： KANZAKI TAMOTSU , MIYOSHI ITSUO , SAIKI IKUO , SHINTANI TAKASHI , AOKI TAKANORI , OKU TORU , IWATA KAZUSHI
IPC分类号： C12N15/09 , A61K31/00 , A61K38/55 , A61P17/00 , A61P17/10 , A61P37/00 , A61P37/08 , C12P21/00
摘要： PROBLEM TO BE SOLVED: To obtain am antiallergic medicine useful for treating and preventing allergy, particularly allergic diseases I and II by incorporating, as an active ingredient, a tissue inhibitor selected from tissue inhibitors against metalloprotease(TIMPs). SOLUTION: This medicine contains, as an active ingredient, a tissue inhibitor [inhibitor which specifically inhibits the activity of matrix metalloproteases(MMPs)] selected from tissue inhibitors against metalloprotease(TIMPs). It is preferable to administer the medicine to an adult (60 kg) orally at a dose of 0.01 mg-1 g per day, or parenterally, for example, by injection at a dose of 0.001 mg-30 mg per day, or as ointment at a dose of 0.01-100 mg per each application. This medicine is useful particularly for allergy I (e.g. atopic dermatitis, bronchial asthma, and pollen disease) and allergy IV (e.g. allergic contact dermatitis).
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公开(公告)号：JP2001330598A
公开(公告)日：2001-11-30
申请号：JP2000150309
申请日：2000-05-22
发明人： SAKATA KAZUTO , TADA MASAHITO , OKAMOTO KOSEI , FUJIMOTO NOBORU , ABE SHINKICHI
摘要： PROBLEM TO BE SOLVED: To provide an easily-portable and inexpensive multi-layer filler packed column capable of preventing movement and mixing of layers of a filler. SOLUTION: This multi-layer filler packed column 10 is a column having a laminate 5 having plural layers 20-70 of the filler, and is equipped with filters 1-3 for filler movement prevention arranged on the upper face and the bottom face of the laminate and interlayers of the filler of the laminate. The filters have a similar shape to the outer cylinder section of the column, and are fixed in the column by the frictional force between edges of the filters and the outer cylinder inner wall of the column. Hereby, movement and mixing of the layers of the filler can be prevented, and the easily-portable and inexpensive multi-layer filler packed column can be provided.
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公开(公告)号：JP2001192364A
公开(公告)日：2001-07-17
申请号：JP2000352603
申请日：2000-11-20
发明人： FUJISAWA TETSUNORI , KOTAKE SHINJIRO , MORITA YASUO , HONGO TOMOKO , ITO HAJIME , YASUDA JUNKO , SUDA EIKO , IGETA KATSUHIRO , MORIKAWA TADANORI
IPC分类号： C07D333/34 , C07C257/14 , C07C257/18 , C07C259/06 , C07C279/14 , C07C279/18 , C07C305/24 , C07C309/61 , C07C323/60 , C07F9/12
摘要： PROBLEM TO BE SOLVED: To provide a novel synthetic intermediate for hydroxamic acid derivative that has high inhibitory activity against MMPs and increased solubility in water. SOLUTION: This novel compound is represented by general formula (1). In an embodiment, this novel compound is represented by general formula (2), wherein R1 and R2 are each H, OH or an arylalkylene group and the like; R3 and R4 are each an alkyl; R5 is an amidino group, sulfonic acid group or the like; R6 is H, benzyl or the like.
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公开(公告)号：JP2001131085A
公开(公告)日：2001-05-15
申请号：JP2000253522
申请日：2000-08-24
IPC分类号： A61K47/06 , A61K38/00 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/18 , A61K47/20 , A61K47/22 , A61K47/26 , A61K47/28 , A61K47/40 , A61P29/00
摘要： PROBLEM TO BE SOLVED: To prepare a medicinal composition for transdermal and transmucosal absorption. SOLUTION: This medicinal composition for transdermal and transmucosal absorption contains one or more kinds selected from (1) a peptide compound of a compound represented by general formula (I): Y-L-Tyr-Q-N(R1)-CH(R2)-CO-X [R1 is a hydrogen atom or a 1-6C alkyl group; R2 is a benzyl group (having a substituent); Q is D-Arg or L-Arg; Y is two hydrogen atoms of the N-terminal amino group of L-Tyr, of a 1-6C alkyl group, a 1-6C alkylcarbonyl group or the like substituting the hydrogen atom (s); and X is OR5 (R5 is a hydrogen atom or a 1-6C alkyl group)] or a salt thereof, and (2) alcohols, higher alkanes, higher fatty acids, higher fatty acid esters, terpenes and the like.
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公开(公告)号：JP2001055327A
公开(公告)日：2001-02-27
申请号：JP2000173115
申请日：2000-06-09
发明人： FUJISAWA TETSUNORI , KOTAKE SHINJIRO , HONGO KAZUYA , ITO HAJIME , OTANI YOSHIKAZU , YASUDA JUNKO , MORIKAWA TADANORI
IPC分类号： C07D295/16 , A61K31/18 , A61K31/19 , A61K31/216 , A61K31/22 , A61K31/27 , A61K31/277 , A61K31/403 , A61K31/4035 , A61K31/4166 , A61K31/4409 , A61K31/4418 , A61K31/4453 , A61K31/5375 , A61K31/663 , A61K31/7028 , A61P1/04 , A61P3/10 , A61P17/06 , A61P19/02 , A61P35/00 , A61P37/00 , A61P43/00 , C07D209/48 , C07D213/53 , C07D233/74 , C07H15/04
摘要： PROBLEM TO BE SOLVED: To obtain the subject new medicine which can exhibit a high metalloproteinase-inhibiting activity, can improve the utility and biological activity of the medicine in living bodies, and is useful as a medicine for preventing and/or treating ulcerative colitis, autoimmune diseases, and so on, by including a hydroxamic acid derivative as an active ingredient. SOLUTION: This medicine contains a compound of formula I [R1 is H, an aralykl or the like; R2 is H, an aralkyloxycarbonyl or the like; R3 is H, hydroxy or the like; R4 is an alkyl or the like; R5 is OR9 (R9 is H, an alkyl or the like) or the like; R6 is H, hydroxy, amino or the like; R7 is H, hydroxy, an alkyl or the like; R8 is H, hydroxy, an alkyl or the like], for example, Na-[4-(hydroxyamino)-2(R)-isobutyl-3(RS)-methylsuccinyl]-Ne-acetimidoy l-L-lysine N-methylamide.monohydrochloride, as an active ingredient. The compound of formula I can be obtained from a compound of formula II [R13 is the same as R3 or the like; R14 is the same as R4 or the like; R15 is the same as R6 or the like; R16 is OR17 (O17 is the same as R9) or the like] which is an intermediate.
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公开(公告)号：JP2000157263A
公开(公告)日：2000-06-13
申请号：JP35211098
申请日：1998-11-26
发明人： CARLOS LOPEZ-OTIN , INIGO SANTAMARIA , GLORIA VELASCO , ALBERTO M PENDAS , AOKI TAKANORI , IWATA KAZUSHI
IPC分类号： C12N15/09 , A61K31/00 , A61K38/55 , A61K39/395 , A61K45/00 , A61K48/00 , C07K16/40 , C12N1/19 , C12N1/21 , C12N5/00 , C12N5/10 , C12N9/50 , C12P21/08 , C12Q1/68 , C12R1/91 , G01N33/53 , G01N33/573
摘要： PROBLEM TO BE SOLVED: To provide a novel protein that is a human-originating cathepsin Y protein or a protein that has an amino acid sequence homology with cysteine protease activity and antigenicity, thus is useful in the elucidation and therapy for Alzheimer's disease, neurodegenerative diseases, cancers and the like. SOLUTION: This novel protein is a human-originating cathepsin Y protein or a novel protein that has at least 49% homology with the human-originating cathepsin protein, and has cysteine protease activity or has the same level of antigenicity or their salt. This protein participates to the intracellular protein metabolism, antigen presentation, activation of hormone precursors, and bone modification and participates in Alzheimer's disease, pulmonary emphysema, rheumatoid arthritis, muscular dystrophy, osteoporosis, infiltration and metastasis of cancers and is useful in the elucidation of pathogenic mechanism and for their treatment. This protein is obtained by incorporating the gene that is cloned from a human-originating cDNA library into the vector and expressing the gene in the host cells of a microorganism, for example, Escherichia coil.
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