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公开(公告)号:JP2004043502A
公开(公告)日:2004-02-12
申请号:JP2003358317
申请日:2003-10-17
Applicant: Basf Ag , ビーエーエスエフ アクチェンゲゼルシャフト
Inventor: LEMAIRE HANS-GEORG , HILLEN HEINZ , MOELLER ACHIM , DAUM LOTHAR , DOERPER THOMAS , SUBKOWSKI THOMAS
IPC: A61K35/22 , A61K38/00 , A61P7/02 , A61P7/04 , A61P11/00 , A61P19/00 , A61P19/02 , A61P25/00 , A61P29/00 , A61P31/04 , A61P37/02 , A61P37/08 , A61P43/00 , C07K1/18 , C07K1/22 , C07K7/08 , C07K14/00 , C07K14/435 , C07K14/47 , C07K14/715 , C07K16/18
CPC classification number: C07K16/18 , A61K38/00 , C07K14/7151
Abstract: PROBLEM TO BE SOLVED: To obtain a protein which can neutralize the action of TNFα (tumor necrusis factor α).
SOLUTION: This protein has molecular weight of about 42,000 daltons measured by SDS gel electrophoresis and has at the N-terminus an amino acid sequence; Xaa Thr Pro Tyr Ala Pro Glu Pro Gly Ser Thr Cys Arg Leu Arg Glu (Xaa is H, phenylalanine residue (Phe) or an amino acid sequence; Ala Phe, Val Ala Phe, Gln Val Ala Phe, Ala Gln Val Ala Phe, Pro Ala Gln Val Ala Phe or Leu Pro Ala Gln Val Ala Phe), and a mutein is obtained by subjecting the protein having the TNFα suppressing action to a proper substitution, deletion or addition of an amino acid or peptide or the change of a glycoside group without strongly lowering the TNFα suppressing action.
COPYRIGHT: (C)2004,JPO-
公开(公告)号:JP2002302500A
公开(公告)日:2002-10-18
申请号:JP2002013319
申请日:2002-01-22
Applicant: BASF AG
Inventor: LEMAIRE HANS-GEORG , HILLEN HEINZ , MOELLER ACHIM , DAUM LOTHAR , DOERPER THOMAS , SUBKOWSKI THOMAS
IPC: A61K35/22 , A61K38/00 , A61K38/17 , A61K38/19 , A61P7/00 , A61P7/02 , A61P7/04 , A61P11/00 , A61P19/00 , A61P19/02 , A61P19/08 , A61P25/00 , A61P29/00 , A61P31/04 , A61P37/00 , A61P37/02 , A61P37/08 , A61P43/00 , C07K1/18 , C07K1/22 , C07K7/08 , C07K14/00 , C07K14/435 , C07K14/47 , C07K14/525 , C07K14/715 , C07K16/18
Abstract: PROBLEM TO BE SOLVED: To obtain a protein which can neutralize the action of TNFα. SOLUTION: The protein has a molecular weight of about 42,000 daltons in the first glycosylated form and has at the N-terminus an amino acid sequence; Xaa Thr Pro Tyr Ala Pro Glu Pro Gly Ser Thr Cys Arg Leu Arg Glu (Xaa is H, phenylalanine residue (Phe) or an amino acid sequence; Ala Phe, Val Ala Phe, Gln Val Ala Phe, Ala Gln Val Ala Phe, Pro Ala Gln Val Ala Phe or Leu Pro Ala Gln Val Ala Phe), and the protein and a mutein obtained by the proper substitution, deletion or addition of an amino acid or peptide for/ from/or to/the protein or the change of a glycoside group without strongly lowering the action of the protein are used for suppressing the abnormal increase in the TNF-α.
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公开(公告)号:WO0078933A2
公开(公告)日:2000-12-28
申请号:PCT/EP0005261
申请日:2000-06-07
Applicant: BASF AG , DEAR NEIL T , BOEHM THOMAS , MOELLER ACHIM
Inventor: DEAR NEIL T , BOEHM THOMAS , MOELLER ACHIM
IPC: G01N33/50 , A61K38/57 , A61K45/00 , A61P15/00 , A61P15/08 , C12N9/64 , C12N15/09 , C12Q1/37 , G01N33/15 , C12N9/00
CPC classification number: C12N9/6472 , A61K38/57
Abstract: The invention relates to a novel mammalian calpain CAPN11, to the synthesis and to the use thereof.
Abstract translation: 新的蛋白酶和它们的用途。
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公开(公告)号:WO9954310A3
公开(公告)日:2000-02-17
申请号:PCT/EP9902633
申请日:1999-04-20
Applicant: BASF AG , LUBISCH WILFRIED , MOELLER ACHIM , TREIBER HANS JOERG , KNOPP MONIKA
Inventor: LUBISCH WILFRIED , MOELLER ACHIM , TREIBER HANS-JOERG , KNOPP MONIKA
IPC: C07D295/08 , A61K31/166 , A61K31/27 , A61K31/40 , A61K31/455 , A61K31/495 , A61K31/535 , A61K31/5375 , A61P9/00 , A61P13/12 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/28 , A61P27/12 , A61P29/00 , A61P35/00 , A61P35/04 , A61P37/02 , A61P43/00 , C07C229/38 , C07C237/20 , C07C237/22 , C07C237/32 , C07C237/36 , C07D213/82 , C07D295/14 , C07D295/155 , A61K31/16 , A61K31/395 , C07D209/14 , C07D233/64
CPC classification number: C07D213/82 , A61K31/195 , A61K31/5375 , C07C229/38 , C07C237/22 , C07C237/32 , C07C2601/14 , C07D295/155
Abstract: The invention relates to cysteine protease inhibitors of the general formula (I), in which A is -(CH2)p-R , where R can be pyrrolidine, morpholine, piperidine, -NR R and formula (a) and p can be 1 or 2; B can be possibly substituted phenyl, pyridyl, pyrimidyl and pyridazyl; D is a bond, -(CH2)m-, -CH=CH-, -CC-; R is chlorine, bromine, fluorine, alkyl, NHCO alkyl, NHSO2 alkyl, NO2, -O-alkyl and NH2; R is an alkyl which can carry a possibly substituted phenyl ring, indolyl ring and cyclohexyl ring; and Y is phenyl, pyridine, pyrimidine and pyrazine; R is hydrogen, COOR and CO-Z, where Z is NR R and and formulae (b), (c), (d); n is 0, 1 or 2 and m is 0, 1, 2, 3 or 4.
Abstract translation: 通式(I)其中A是半胱氨酸蛋白酶抑制剂: - (CH 2)p <1>,其中R <1>吡咯烷,吗啉,哌啶,-NR <5> R可以是<6>和式(a) 且p是数字1和2; B:任选取代的苯基,吡啶基,嘧啶基和哒嗪基可表示; D:键, - (CH 2)间 - ,-CH = CH-,可以是-CC-; [R <2>:表示氯,溴,氟,烷基,NHCO烷基,NHSO 2烷基,NO 2,-O-烷基和NH 2; [R <3>: - 烷基可以带有任选取代的苯基环,吲哚基环和环己基环; Y:苯基,吡啶,嘧啶和吡嗪; [R <4>:,COOR <9>和CO-Z是氢,其中Z是NR <10> - [R <11>,和式(B),(C),(D)的装置; n是数字0,1或2,并且m是数字0,1,2,3或4。
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公开(公告)号:BG106186A
公开(公告)日:2002-12-29
申请号:BG10618601
申请日:2001-12-06
Applicant: BASF AG
Inventor: DEAR NEIL T , BOEHM THOMAS , MOELLER ACHIM
IPC: G01N33/50 , A61K38/57 , A61K45/00 , A61P15/00 , A61P15/08 , C12N9/64 , C12N15/09 , C12Q1/37 , G01N33/15 , C12N9/00
Abstract: The invention relates to novel calpains and their use. 6 claims, 3 figures
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公开(公告)号:HU0201800A2
公开(公告)日:2002-09-28
申请号:HU0201800
申请日:2000-06-07
Applicant: BASF AG
Inventor: BOEHM THOMAS , DEAR NEIL T , MOELLER ACHIM
IPC: G01N33/50 , A61K38/57 , A61K45/00 , A61P15/00 , A61P15/08 , C12N9/64 , C12N15/09 , C12Q1/37 , G01N33/15 , C12N15/57
Abstract: The invention relates to a novel mammalian calpain CAPN11, to the synthesis and to the use thereof.
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公开(公告)号:NO20015922L
公开(公告)日:2002-02-12
申请号:NO20015922
申请日:2001-12-04
Applicant: BASF AG
Inventor: DEAR NEIL T , BOEHM THOMAS , MOELLER ACHIM
IPC: G01N33/50 , A61K38/57 , A61K45/00 , A61P15/00 , A61P15/08 , C12N9/64 , C12N15/09 , C12Q1/37 , G01N33/15 , C12N9/50
Abstract: The invention relates to a novel mammalian calpain CAPN11, to the synthesis and to the use thereof.
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公开(公告)号:BG63388B1
公开(公告)日:2001-12-31
申请号:BG10339999
申请日:1999-05-12
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , MOELLER ACHIM , TREIBER HANS-JOERG
IPC: A61K31/403 , A61K31/4035 , A61K31/405 , A61K31/4439 , A61K31/496 , A61K31/517 , A61K31/519 , A61K31/5377 , A61P9/00 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/28 , A61P35/00 , A61P35/04 , A61P43/00 , C07D209/48 , C07D209/66 , C07D239/70 , C07D239/96 , C07D401/12 , C07D471/04 , C07D475/02 , A61K31/505 , A61K31/40
Abstract: The compounds are used in medicine. The heterocycle benzamides have the formula where R1, R2, R3, R4, R5, X, m & n have the meanings listed in the description. 17 claims
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公开(公告)号:HU0102732A2
公开(公告)日:2001-12-28
申请号:HU0102732
申请日:1999-04-20
Applicant: BASF AG
Inventor: KNOPP MONIKA , LUBISCH WILFRIED , MOELLER ACHIM , TREIBER HANS-JOERG
IPC: C07D295/08 , A61K31/16 , A61K31/166 , A61K31/27 , A61K31/395 , A61K31/40 , A61K31/455 , A61K31/495 , A61K31/535 , A61K31/5375 , A61P9/00 , A61P13/12 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/28 , A61P27/12 , A61P29/00 , A61P35/00 , A61P35/04 , A61P37/02 , A61P43/00 , C07C229/38 , C07C237/20 , C07C237/22 , C07C237/32 , C07C237/36 , C07D209/14 , C07D213/82 , C07D233/64 , C07D237/32 , C07D237/36 , C07D295/14 , C07D295/155
Abstract: An amide of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: A —(CH2)p—R1, where R1 can be pyrrolidine, morpholine, piperidine, —NR5R6 and and R5, R6 and R7 can, independently of one another, be hydrogen, C1-C4-alkyl, CH2Ph, Ph, CH2CH2Ph, it also being possible for the phenyl rings to be substituted by R6, and p can be 1 and 2, and B can be phenyl, pyridyl, pyrimidyl and pyridazyl, it also being possible for the rings to be substituted by up to 2 R8 radicals, and D can be a bond, —(CH2)m—, —CH═CH—, —C═C—, and R2 is chlorine, bromine, fluorine, C1-C6-alkyl, NHCO—C1-C4-alkyl, NHSO2—C1-C4-alkyl, NO2, —O—C1-C4-alkyl and NH2, and R3 is —C1-C6-alkyl, branched or unbranched, and which may also carry a phenyl ring, indolyl ring or cyclohexyl ring which is in turn substituted by a maximum of two R8 radicals, where R8 is hydrogen, C1-C4-alkyl, branched or unbranched, —O—C1-C4-alkyl, OH, Cl, F, Br, I, CF3, NO2, NH2, CN, COOH, COO—C1-C4-alkyl, NHCO—C1-C4-alkyl, —NHSO2—C1-C4-alkyl and —SO2—C1-C4-alkyl; and Y is phenyl, pyridine, pyrimidine and pyrazine and R4 is hydrogen, COOR9 and CO—Z in which Z is NR10R11 and R9 is hydrogen, C1-C6-alkyl, linear or branched, and which may [lacuna] substituted by a phenyl ring which may itself also be substituted by one or two R12 radicals, and R10 is hydrogen, C1-C6-alkyl, linear or branched, and which may [lacuna] substituted by a phenyl ring which itself may also be substituted by one or two R12 radicals, and R11 is hydrogen, C1-C6-alkyl, branched or unbranched, which may also be and substituted by a phenyl ring which may also carry an R9 radical, and R12 can be hydrogen, C1-C4-alkyl, branched or unbranched, —O—C1-C4-alkyl, OH, Cl, F, Br, J, CF3, NO2, NH2, CN, COOH, COO—C1-C4-alkyl, —NHCO—C1-C4-alkyl, —NHCO-phenyl, —NHSO2—C1-C4-alkyl, NHSO2-phenyl, —SO2—C1-C4-alkyl and —SO2-phenyl, R13 is hydrogen, C1-C6-alkyl, linear or branched, and which may [lacuna] substituted by a phenyl ring which may itself also be substituted by one or two R12 radicals, and R14 is hydrogen, C1-C6-alkyl, linear or branched, and which may [lacuna] substituted by a phenyl ring which may itself also be substituted by one or two R12 radicals, and n is a number 0, 1 or 2, and m,q are, independently of one another, a number 0, 1, 2, 3 or 4.
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公开(公告)号:NO20015922D0
公开(公告)日:2001-12-04
申请号:NO20015922
申请日:2001-12-04
Applicant: BASF AG
Inventor: DEAR NEIL T , BOEHM THOMAS , MOELLER ACHIM
IPC: G01N33/50 , A61K38/57 , A61K45/00 , A61P15/00 , A61P15/08 , C12N9/64 , C12N15/09 , C12Q1/37 , G01N33/15 , C12N
Abstract: The invention relates to a novel mammalian calpain CAPN11, to the synthesis and to the use thereof.
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