公开(公告)号：WO9804278A3

公开(公告)日：2003-04-17

申请号：PCT/EP9703898

申请日：1997-07-21

Applicant: BASF AG ,  BARLOZZARI TERESA ,  HAUPT ANDREAS ,  JANSSEN BERND ,  GRIESINGER CHRISTIAN ,  BELIK DANIEL ,  BORETZKY MICHAEL

Inventor： BARLOZZARI TERESA ,  HAUPT ANDREAS ,  JANSSEN BERND ,  GRIESINGER CHRISTIAN ,  BELIK DANIEL ,  BORETZKY MICHAEL

IPC: A61K38/00 ,  A61P35/00 ,  C07K4/00 ,  C07K5/02 ,  C07K5/027 ,  A61K38/04

CPC classification number: C07K5/0205 ,  A61K38/00

Abstract: The present invention provides antitumor peptides of formula (I): A-B-NR -CHD-CH(OCH3)-CH2CO-E-K and the acid salts thereof. A is an amino acid residue selected from the group consisting of N-methyl-D-prolyl, N-methyl-D-homoprolyl and N, N-dimethyl-2 -ethylphenylglycyl, or an amino acid residue of the formula R R N-CHX-CO, wherein R is a methyl group or an ethyl group, R is a hydrogen atom, a methyl group or an ethyl group, and X is an alkyl group. B is an amino acid residue selected from the group consisting of valyl, isoleucyl, leucyl, and 2-t-butylglycyl. R is a hydrogen atom or a methyl group. D is a normal or branched C2-C5-alkyl group. E is an amino acid residue selected from the group consisting of prolyl, homoprolyl, 5-methylprolyl, and phenylalanyl, or E is a residue derived from an amino acid comprising a pyrrolidine group. K is an alkoxy group or an amino group. An additional embodiment of the present invention is a method for treating a malignancy in a mammal, such as a human, comprising administering to the mammal an effective amount of a compound or compounds of the formula (I) in a pharmaceutically acceptable composition.

Abstract translation: 本发明提供式（I）的抗肿瘤肽：A-B-NR 3 -CHD-CH（OCH 3）-CH 2 CO-E-K及其酸式盐。 A是选自N-甲基-D-脯氨酰基，N-甲基-D-正戊基和N，N-二甲基-2-乙基苯基甘氨酰或式R 1的氨基酸残基的氨基酸残基。 R 2为N-CHX-CO，其中R 1为甲基或乙基，R 2为氢原子，甲基或乙基，X为烷基。 B是选自缬氨酰基，异亮氨酰基，亮氨酰基和2-叔丁基甘氨酰基的氨基酸残基。 R 3是氢原子或甲基。 D是正链或支链C 2 -C 5 - 烷基。 E是选自脯氨酰基，同环戊基，5-甲基脯氨酰基和苯丙氨酰基的氨基酸残基，或E是衍生自包含吡咯烷基的氨基酸的残基。 K是烷氧基或氨基。 本发明的另一个实施方案是用于治疗哺乳动物（例如人）的恶性肿瘤的方法，其包括向所述哺乳动物施用有效量的药学上可接受的组合物中的式（I）化合物或化合物。

公开(公告)号：WO9722621A3

公开(公告)日：1998-02-26

申请号：PCT/EP9605518

申请日：1996-12-11

Applicant: BASF AG ,  AMBERG WILHELM ,  BARLOZZARI TERESA ,  BERNARD HARALD ,  BUSCHMANN ERNST ,  HAUPT ANDREAS ,  HEGE HANS GUENTHER ,  JANSSEN BERND ,  KLING ANDREAS ,  LIETZ HELMUT ,  RITTER KURT ,  ULLRICH MARTINA ,  WEYMANN JUERGEN ,  ZIERKE THOMAS

Inventor： AMBERG WILHELM ,  BARLOZZARI TERESA ,  BERNARD HARALD ,  BUSCHMANN ERNST ,  HAUPT ANDREAS ,  HEGE HANS-GUENTHER ,  JANSSEN BERND ,  KLING ANDREAS ,  LIETZ HELMUT ,  RITTER KURT ,  ULLRICH MARTINA ,  WEYMANN JUERGEN ,  ZIERKE THOMAS

IPC: A61K38/00 ,  A61K31/00 ,  A61K38/08 ,  A61P35/00 ,  A61P35/02 ,  C07K1/00 ,  C07K7/06

CPC classification number: A61K38/08

Abstract: Novel peptides of the following formula (I): R1R2N-CHX-CO-A-B-D-E-(G)¿s?-K in which R?1, R2¿, A, B, D, E, G, K, X, and s have the meanings stated in the description, and the preparation thereof are described. The novel peptides have an antineoplastic effect.

公开(公告)号：WO0127077A3

公开(公告)日：2002-05-23

申请号：PCT/US0027361

申请日：2000-10-04

Applicant: BASF AG ,  TAYLOR NEIL R ,  BORHANI DAVID ,  EPSTEIN DAVID ,  RUDOLPH JOHANNES ,  RITTER KURT ,  FUJIMORI TARO ,  ROBINSON SIMON ,  ECKSTEIN JENS ,  HAUPT ANDREAS ,  WALKER NIGEL ,  DIXON RICHARD W ,  CHOQUETTE DEBORAH ,  BLANCHARD JILL ,  KLUGE ARTHUR ,  PAL KOLLOL ,  BOCKOVICH NICHOLAS ,  COME JON ,  HEDIGER MARK

Inventor： TAYLOR NEIL R ,  BORHANI DAVID ,  EPSTEIN DAVID ,  RUDOLPH JOHANNES ,  RITTER KURT ,  FUJIMORI TARO ,  ROBINSON SIMON ,  ECKSTEIN JENS ,  HAUPT ANDREAS ,  WALKER NIGEL ,  DIXON RICHARD W ,  CHOQUETTE DEBORAH ,  BLANCHARD JILL ,  KLUGE ARTHUR ,  PAL KOLLOL ,  BOCKOVICH NICHOLAS ,  COME JON ,  HEDIGER MARK

IPC: A61K38/00 ,  C07C309/24 ,  C07D307/85 ,  C07F9/38 ,  C07K5/02 ,  C07K5/113 ,  C12N9/16 ,  A61K31/185 ,  A61K31/343 ,  A61K31/662

CPC classification number: C12N9/16 ,  A61K38/00 ,  C07C309/24 ,  C07D307/85 ,  C07F9/3882 ,  C07K5/0205 ,  C07K5/0207 ,  C07K5/021 ,  C07K5/1021 ,  C07K2299/00

Abstract: The present application relates to compounds of the fornula (VII), wherein the substituents R -R , X and Y are as defined in the description and to compounds of formula (VIII) or formula (IX) and when R is in the ortho position to X, R and R are taken together with the atoms to which are each attached to form an aromatic heterocyclic ring. The application further relates to polypeptides which comprise the ligand binding domain of Cdc25, crystalline forms of these polypeptides and the use of these crystalline forms to determine the three dimensional structure of the catalytic domain of Cdc25. The invention also relates to the use of the three dimensional structure of the Cdc25 catalytic domain in methods of designing and/or identifying potential inhibitors of Cdc25 activity, for example, compounds which inhibit the binding of a native substrate to the Cdc25 catalytic domain.

Abstract translation: 本申请涉及式（VII）的化合物，其中取代基R 1 -R 5，X和Y如说明书和式（VIII）或式（IX）的化合物所定义，并且当 R 3位于X的邻位，R 3和R 4与各自连接的原子一起形成芳族杂环。 本申请还涉及包含Cdc25的配体结合结构域，这些多肽的结晶形式以及这些结晶形式用于确定Cdc25催化结构域的三维结构的多肽。 本发明还涉及Cdc25催化结构域的三维结构在设计和/或鉴定Cdc25活性的潜在抑制剂的方法中的用途，例如抑制天然底物与Cdc25催化结构域结合的化合物。

公开(公告)号：WO0116300A3

公开(公告)日：2002-05-30

申请号：PCT/US0023473

申请日：2000-08-25

Applicant: BASF AG ,  GPC BIOTECH INC ,  TAYLOR NEIL R ,  BORHANI DAVID ,  EPSTEIN DAVID ,  RUDOLPH JOHANNES ,  RITTER KURT ,  FUJIMORI TARO ,  ROBINSON SIMON ,  ECKSTEIN JENS ,  HAUPT ANDREAS ,  WALKER NIGEL ,  DIXON RICHARD W ,  CHOQUETTE DEBORAH ,  BLANCHARD JILL ,  KLUGE ARTHUR ,  PAL KOLLOL ,  BOCKOVICH NICHOLAS ,  COME JON ,  HEDIGER MARK

Inventor： TAYLOR NEIL R ,  BORHANI DAVID ,  EPSTEIN DAVID ,  RUDOLPH JOHANNES ,  RITTER KURT ,  FUJIMORI TARO ,  ROBINSON SIMON ,  ECKSTEIN JENS ,  HAUPT ANDREAS ,  WALKER NIGEL ,  DIXON RICHARD W ,  CHOQUETTE DEBORAH ,  BLANCHARD JILL ,  KLUGE ARTHUR ,  PAL KOLLOL ,  BOCKOVICH NICHOLAS ,  COME JON ,  HEDIGER MARK

IPC: C12N15/09 ,  A61K38/00 ,  A61K45/00 ,  A61P9/08 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07K5/10 ,  C07K5/107 ,  C12N9/16 ,  C12N9/99 ,  C12N15/55 ,  C07K7/06 ,  C30B29/58 ,  G06F17/50

CPC classification number: C07K5/1016 ,  A61K38/00 ,  C07K5/1027 ,  C12N9/16

Abstract: The present invention relates to polypeptides which comprise the ligand binding domain of Cdc25, crystalline forms of these polypeptides and the use of these crystalline forms to determine the three dimensional structure of the catalytic domain of Cdc25. The invention also relates to the use of the three dimensional structure of the Cdc25 catalytic domain in methods of designing and/or identifying potential inhibitors of Cdc25 activity, for example, compounds which inhibit the binding of a native substrate to the Cdc25 catalytic domain.

Abstract translation: 本发明涉及包含Cdc25的配体结合结构域，这些多肽的结晶形式以及这些结晶形式用于确定Cdc25催化结构域的三维结构的多肽。 本发明还涉及Cdc25催化结构域的三维结构在设计和/或鉴定Cdc25活性的潜在抑制剂的方法中的用途，例如抑制天然底物与Cdc25催化结构域结合的化合物。

公开(公告)号：WO0118032A2

公开(公告)日：2001-03-15

申请号：PCT/US0024658

申请日：2000-09-08

Applicant: BASF AG ,  UNIV ARIZONA ,  PETIT GEORGE R ,  SRIRANGAM JAYARAM K ,  WILLIAMS MICHAEL D ,  DURKIN KIERAN P M ,  BARLOZZARI TERESA ,  KLING ANDREAS ,  JANSSEN BERND ,  HAUPT ANDREAS

Inventor： PETIT GEORGE R ,  SRIRANGAM JAYARAM K ,  WILLIAMS MICHAEL D ,  DURKIN KIERAN P M ,  BARLOZZARI TERESA ,  KLING ANDREAS ,  JANSSEN BERND ,  HAUPT ANDREAS

IPC: C07K5/02 ,  C07K7/02 ,  C07K5/00

CPC classification number: C07K5/0202 ,  C07K5/0205 ,  C07K7/02

Abstract: The present invention provides compounds of formula (I) where R1-R5 are each, independently, a hydrogen atom or a normal or branched C1-C6-alkyl group; A is a methionyl, phenylalanyl or phenylglycyl residue; n is 0 or 1; R6 is a hydrogen atom; and R7 is a carbocyclic group, an aromatic group, a C1-C4-alkyl group, a pyridylalkyl group or a heterocyclic group. In another embodiment, R6 is benzyl or -C(O)OR8, where R8 is a C1-C6-alkyl group, and R7 is a heteroaromatic group, such as a 2-thiazolyl group.

Abstract translation: 本发明提供式（I）化合物，其中R 1 -R 5各自独立地为氢原子或正
或支链C 1 -C 6烷基; A是甲硫氨酰基，苯丙氨酰或苯基甘氨酰残基; n为0或1; R6是氢原子; 并且R 7是碳环基，芳基，C 1 -C 4 - 烷基，吡啶基烷基或杂环基。 在另一个实施方案中，R 6为苄基或-C（O）OR 8，其中R 8为C 1 -C 6烷基，R 7为杂芳族基团，例如2-噻唑基。

公开(公告)号：WO0061608A3

公开(公告)日：2001-01-11

申请号：PCT/EP0002710

申请日：2000-03-28

Applicant: BASF AG

Inventor： HILLEN HEINZ ,  SCHMIDT MARTIN ,  MACK HELMUT ,  SEITZ WERNER ,  HAUPT ANDREAS ,  ZECHEL JOHANN-CHRISTIAN ,  KLING ANDREAS

IPC: C12N9/99 ,  A61K38/00 ,  A61P1/04 ,  A61P1/18 ,  A61P5/14 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P13/12 ,  A61P15/00 ,  A61P17/02 ,  A61P19/02 ,  A61P21/04 ,  A61P25/00 ,  A61P25/28 ,  A61P29/00 ,  A61P37/02 ,  C07B43/00 ,  C07D401/12 ,  C07K5/06 ,  C07K5/065 ,  C07K5/062 ,  A61K38/05 ,  C07D409/12 ,  C07K5/068 ,  C07K5/072 ,  C07K5/078

CPC classification number: C07D401/12 ,  A61K38/00 ,  C07B43/00 ,  C07K5/06078

Abstract: The invention relates to peptidic substances, to the production of said substances and to their use as complement inhibitors. In particular, the invention relates to substances with a guanidine or amidine radical as the terminal group, especially inhibitors of the complement proteases C1s and C1r.

Abstract translation: 本发明涉及肽的物质，它们的制备和它们作为补体抑制剂的用途。 具体而言，存在与一个胍或脒基作为末端基团的物质。 特别地，本发明涉及的C1s和C1R Komplementproteasen的抑制剂。

公开(公告)号：WO9006943A3

公开(公告)日：1990-08-09

申请号：PCT/EP8901470

申请日：1989-12-02

Applicant: BASF AG

Inventor： BOEHM HANS-JOACHIM ,  DAUM LOTHAR ,  HAUPT ANDREAS ,  SCHMIED BERNHARD ,  WALKER NIGEL ,  ZECHEL JOHANN-CHRISTIAN

IPC: A61K38/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/06 ,  C07K1/04 ,  C07K7/06 ,  C07K7/08 ,  C07K7/64 ,  C07K14/52 ,  C07K14/525 ,  A61K37/02 ,  C07K7/56

CPC classification number: C07K14/525 ,  A61K38/00

Abstract: Peptides derived from TNF, of formula (I): X-A-Gly-Asp-Y, in which A X and Y have the meanings given in the description. Process for producing them. The novel peptides are useful therapeutic agents.

公开(公告)号：EP0920325A2

公开(公告)日：1999-06-09

申请号：EP97918936

申请日：1997-07-21

Applicant: BASF AG

Inventor： BARLOZZARI TERESA ,  HAUPT ANDREAS ,  JANSSEN BERND ,  GRIESINGER CHRISTIAN ,  BELIK DANIEL ,  BORETZKY MICHAEL

IPC: A61K38/00 ,  A61P35/00 ,  C07K4/00 ,  C07K5/02 ,  A61K38/07

CPC classification number: C07K5/0205 ,  A61K38/00

Abstract: The present invention provides antitumor peptides of formula (I): A-B-NR3-CHD-CH(OCH¿3?)-CH2CO-E-K and the acid salts thereof. A is an amino acid residue selected from the group consisting of N-methyl-D-prolyl, N-methyl-D-homoprolyl and N, N-dimethyl-2 -ethylphenylglycyl, or an amino acid residue of the formula R?1R2¿N-CHX-CO, wherein R1 is a methyl group or an ethyl group, R2 is a hydrogen atom, a methyl group or an ethyl group, and X is an alkyl group. B is an amino acid residue selected from the group consisting of valyl, isoleucyl, leucyl, and 2-t-butylglycyl. R3 is a hydrogen atom or a methyl group. D is a normal or branched C¿2?-C5-alkyl group. E is an amino acid residue selected from the group consisting of prolyl, homoprolyl, 5-methylprolyl, and phenylalanyl, or E is a residue derived from an amino acid comprising a pyrrolidine group. K is an alkoxy group or an amino group. An additional embodiment of the present invention is a method for treating a malignancy in a mammal, such as a human, comprising administering to the mammal an effective amount of a compound or compounds of the formula (I) in a pharmaceutically acceptable composition.

公开(公告)号：CA2223911C

公开(公告)日：2009-03-24

申请号：CA2223911

申请日：1996-07-12

Applicant: BASF AG

Inventor： HAUPT ANDREAS ,  JANSSEN BERND ,  KARL ULRICH ,  KLING ANDREAS ,  ZIERKE THOMAS ,  MULLER STEFAN ,  RITTER KURT ,  BUSCHMANN ERNST ,  AMBERG WILHELM ,  BERNARD HARALD

IPC: C07K1/02 ,  C07K11/00 ,  C07K1/12 ,  C07K5/06 ,  C07K5/078 ,  C07K5/08 ,  C07K5/083 ,  C07K5/10 ,  C07K5/103 ,  C07K7/06 ,  C12P21/02

Abstract: The description relates to a process for producing pentapeptides of the formula (I) in which A and R1-R3 have the meanings given, in which the pentapeptide is constructed in steps from a prolinamide of the formula (II) in which R1 and R2 have the meanings given above, and the group -NR1R2 may be hydrolytically separated from the peptide thus obtained.

公开(公告)号：BG65212B1

公开(公告)日：2007-07-31

申请号：BG10408900

申请日：2000-01-17

Applicant: BASF AG

Inventor： JANSSEN BERND ,  BARLOZZARI TERESA ,  HAUPT ANDREAS ,  ZIERKE THOMAS ,  KLING ANDREAS

IPC: A61K38/00 ,  C07K7/06 ,  A61K38/08 ,  A61P35/00 ,  C12P19/34

Abstract: The invention relates to inhibitors of the cellular growth and to their adjunctive to acid salts which are peptides with the formula A - B - D - E - F - (G)r - (K)s - L (I) where A, B, D, E, F, G. and K are -aminoacid residues and s and r are, individually, 0 or 1. L is univalent radical, such as aminogroup, N-substituted aminogroup, beta-hydroxyaminogroup, beta-hydroxyaminogroup, hydrasidogroup, alkoxygroup, thioalkoxygroup, aminooxygroup or oximatogroup. The invention also relates to a method for the treatment of cancer in mammals, including humans which includes the administration of an effective quantity of the above compound in a pharmaceutically acceptable composition.