公开(公告)号：WO2003002543A1

公开(公告)日：2003-01-09

申请号：PCT/EP2002/007183

申请日：2002-06-28

Applicant: ABBOTT LABORATORIES ,  STARCK, Dorothea ,  BLUMBACH, Kai ,  BUSCHMANN, Ernst

Inventor： STARCK, Dorothea ,  BLUMBACH, Kai ,  BUSCHMANN, Ernst

IPC: C07D239/34

CPC classification number: C07D239/34

Abstract: Pyrimidinoxyalkylpiperazines of the formula (I) in which n represents an integer from 2 to 6, R 1 represents H, C 1 -C 6 -alkyl or phenyl ( C 1 -C 6 )-alkyl in which the phenyl radical can be substituted by one or more substituents selected from C 1 -C 6 -alkyl and C 1 -C 6 -alkoxy, R 2 represents H, C 1 -C 4 -alkyl, OH, C 1 -C 6 -alkoxy, NH 2 or C 1 -C 6 -halogenoalkyl, R 3 and R 4 , independently of each other, represent H, C 1 -C 6 -alkyl, C 1 -C 6 -hydroxyalkyl, C 1 -C 6 -halogenoalkyl, pyrrolyl or phenyl, which latter can be substituted by one or more substituents selected from C 1 -C 6 -alkyl, C 1 -C 6 -hydroxyalkyl, C 1 -C 6 -alkoxy, OH, halogen or C 1 -C 6 -halogenoalkyl, phenyl, cyano or nitro. The compounds can be used for treating diseases which respond to modulation of the dopamine D 3 receptor and are characterized by a high degree of bioavailability.

Abstract translation: 式（I）的嘧啶基亚烷基哌嗪，其中n表示2至6的整数，R 1表示H，C 1 -C 6 - 烷基或苯基（C 1 -C 6） - 烷基，其中苯基可以被一个或多个选自以下的取代基取代 C 1 -C 6烷基和C 1 -C 6烷氧基，R 2表示H，C 1 -C 4 - 烷基，OH，C 1 -C 6 - 烷氧基，NH 2或C 1 -C 6 - 卤代烷基，R 3和R 4彼此独立地表示H ，C 1 -C 6 - 烷基，C 1 -C 6 - 羟基烷基，C 1 -C 6 - 卤代烷基，吡咯基或苯基，后者可以被一个或多个选自C 1 -C 6烷基，C 1 -C 6羟基烷基，C 1 -C 6 - 烷氧基，OH，卤素或C 1 -C 6 - 卤代烷基，苯基，氰基或硝基。 该化合物可用于治疗对多巴胺D3受体的调节作出反应的疾病，其特征在于高度的生物利用度。

公开(公告)号：WO1997022621A2

公开(公告)日：1997-06-26

申请号：PCT/EP1996005518

申请日：1996-12-11

Applicant: BASF AKTIENGESELLSCHAFT ,  AMBERG, Wilhelm ,  BARLOZZARI, Teresa ,  BERNARD, Harald ,  BUSCHMANN, Ernst ,  HAUPT, Andreas ,  HEGE, Hans-Guenther ,  JANSSEN, Bernd ,  KLING, Andreas ,  LIETZ, Helmut ,  RITTER, Kurt ,  ULLRICH, Martina ,  WEYMANN, Jürgen ,  ZIERKE, Thomas

Inventor： BASF AKTIENGESELLSCHAFT

IPC: C07K07/06

CPC classification number: A61K38/08

Abstract: Novel peptides of the following formula (I): R R N-CHX-CO-A-B-D-E-(G)s-K in which R , R , 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.

Abstract translation: 下式（I）的新肽：R 1 R 2 N-CHX-CO-ABDE-（G）sK，其中R 1，R 2，A，B，D，E， G，K，X和S具有说明书中所述的含义，并描述其制备。 新型肽具有抗肿瘤作用。

公开(公告)号：WO1995030691A1

公开(公告)日：1995-11-16

申请号：PCT/EP1995001577

申请日：1995-04-26

Applicant: BASF AKTIENGESELLSCHAFT ,  AMBERG, Wilhelm ,  BERNARD, Harald ,  BUSCHMANN, Ernst ,  HAUPT, Andreas ,  JANITSCHKE, Lothar ,  JANSSEN, Bernd ,  KARL, Ulrich ,  KLING, Andreas ,  MÜLLER, Stefan ,  DE POTZOLLI, Bernd ,  RITTER, Kurt ,  THYES, Marco ,  ZIERKE, Thomas

Inventor： BASF AKTIENGESELLSCHAFT

IPC: C07K07/06

CPC classification number: C07K7/06 ,  A61K38/00 ,  C07K5/101 ,  Y02P20/55

Abstract: Disclosed is the compound Me2Val-Val-MeVal-Pro-Pro-NHBzl. HCl. The compound is produced from Z-Val-Val-MeVal-Pro-OR , wherein Z and R have the meanings indicated in the description. The compound disclosed has anti-neoplastic properties.

Abstract translation: 它是连接Me2Val-VAL -Meval-PRO-PRO-NHBz1。 HC1描述。 它是由Z-VAL-缬氨酸-Meval-PRO-OR <1>，其中Z和R <1>具有说明书中给出的含义的。 所述化合物具有抗肿瘤活性。

公开(公告)号：WO1993008148A1

公开(公告)日：1993-04-29

申请号：PCT/EP1992002213

申请日：1992-09-24

Applicant: BASF AKTIENGESELLSCHAFT ,  KLEIN, Ulrich ,  NEUMANN, Ulrich ,  MACKENROTH, Wolfgang ,  RENZ, Guenter ,  KRIEG, Wolfgang ,  MACKENROTH, Christiane ,  BUSCHMANN, Ernst ,  DE KRAMER, Jacobus, Jan ,  MILLI, Roland

Inventor： BASF AKTIENGESELLSCHAFT

IPC: C07C33/02

CPC classification number: C07C33/02 ,  C07C43/313 ,  C07C43/315 ,  Y02P20/55

Abstract: A process is disclosed for preparing a mixture of 8E,10E-dodecadienol (Ia), 8E,10Z-dodecadienol (Ib), 8Z,10E-dodecadienol (Ic) and 8Z,10Z-dodecadienol (Id), H3C-CH=CH-CH=CH-(CH2)6-CH2-OH, (8E,10E = Ia), (8E,10Z = Ib), (8Z,10E = Ic), (8Z,10Z = Id) from 1,8-octandiol (II) which is transformed by a halogenating agent into (III): Hal-CH2-(CH2)6-CH2-OH, (III) is then reacted with (IV): H2C=CH-O-R, producing (V): Hal-CH2-(CH2)6-CH2-O-CH(CH3)-OR, which is transformed in the presence of magnesium with crotonaldehyde into (VI): H3C-CH=CH-CH(OH)-(CH2)8-O-CH(CH3)-OR. The alcohol protective group is split off from (VI) in the presence of an acid, at the same time as the hydroxyl function is eliminated. Also disclosed are intermediates for this process, and a process for fighting the fruit surface eating tortrix moth Cydia pomonella with this mixture according to the mating interruption method.

公开(公告)号：WO1993005053A1

公开(公告)日：1993-03-18

申请号：PCT/EP1992002007

申请日：1992-09-01

Applicant: BASF AKTIENGESELLSCHAFT ,  SCHAEFER, Bernd ,  BUSCHMANN, Ernst ,  REISSENWEBER, Gernot

Inventor： BASF AKTIENGESELLSCHAFT

IPC: C07F09/535

CPC classification number: C07F9/5352

Abstract: A process is disclosed for producing α-chlor-methylen-triorganylphosphorane carboxylic acid derivatives having the formula (I), in which R stands for C organic substituents; A stands for CN or CO-B; B stands for C or O organic residues that remain inert in chlorinating conditions, by chlorinating phosphoranes having the formula (II) with chlorine. Chlorination is carried out in the presence of a mineral base as hydrogen chloride acceptor, whereas chlorine and the base are synchronously but separately introduced into the reaction mixture according to their consumption. The products (I) obtained by this process represent important intermediates for plant protective substances.

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：WO1997017364A1

公开(公告)日：1997-05-15

申请号：PCT/EP1996004709

申请日：1996-10-30

Applicant: BASF AKTIENGESELLSCHAFT ,  KLING, Andreas ,  JANSSEN, Bernd ,  AMBERG, Wilhelm ,  HAUPT, Andreas ,  RITTER, Kurt ,  BUSCHMANN, Ernst ,  BERNARD, Harald ,  MÜLLER, Stefan ,  ZIERKE, Thomas ,  BARLOZZARI, Teresa ,  DE ARRUDA, Monika ,  ROBINSON, Simon

Inventor： BASF AKTIENGESELLSCHAFT

IPC: C07K07/06

CPC classification number: C07K7/06 ,  A61K38/00

Abstract: Novel peptides of the formula A-B-D-E-F-L, wherein A, B, D, E, F, and L have the meanings stated in the specification, and their preparation are disclosed. The novel compounds are suitable for controlling diseases.

Abstract translation: 式A-B-D-E-F-L的新肽，其中A，B，D，E，F和L具有说明书中所述的含义，并且公开了它们的制备。 新型化合物适用于控制疾病。

公开(公告)号：WO1997005096A1

公开(公告)日：1997-02-13

申请号：PCT/EP1996003075

申请日：1996-07-12

Applicant: BASF AKTIENGESELLSCHAFT ,  BUSCHMANN, Ernst ,  ZIERKE, Thomas

Inventor： BASF AKTIENGESELLSCHAFT

IPC: C07C231/02

CPC classification number: C07K7/06 ,  C07C231/02 ,  C07K1/082 ,  Y02P20/55

Abstract: The description relates to a process for producing alpha -(N,N dialkyl)-amino carboxylic acid amides of formula (I) in which the constituents have the meanings given, in which the corresponding free acids are reacted with primary or secondary amines in the presence of anhydrides of an alkane phosphonic acid.

Abstract translation: 提供了一种方法用于α-制备 - （N，N-二烷基）的式-aminocarbonsäureamiden（I），其中取代基如所定义，描述，其在于，相应的游离酸与伯胺或仲胺 在烷烃膦酸的酸酐的存在。

公开(公告)号：WO1997005162A1

公开(公告)日：1997-02-13

申请号：PCT/EP1996003073

申请日：1996-07-12

Applicant: BASF AKTIENGESELLSCHAFT ,  AMBERG, Wilhelm ,  BERNARD, Harald ,  BUSCHMANN, Ernst ,  HAUPT, Andreas ,  JANSSEN, Bernd ,  ULRICH, Karl ,  KLING, Andreas ,  MÜLLER, Stefan ,  RITTER, Kurt ,  ZIERKE, Thomas

Inventor： BASF AKTIENGESELLSCHAFT

IPC: C07K07/06

CPC classification number: C07K7/06 ,  C07K5/06165 ,  C07K5/0808 ,  C07K5/101

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

Abstract translation: 本发明提供了一种制备其中A和R <1> -R <3>所定义，所述的式（I），其中包括在一个由下式的脯氨酸酰胺逐渐开始（五肽的五肽 II），<2>具有上面给出的含义，其中R <1>和R，积聚并且因此获得的肽，如果合适的话，基团-NR <1> [R <2>通过水解分裂。

公开(公告)号：WO1995030690A1

公开(公告)日：1995-11-16

申请号：PCT/EP1995001576

申请日：1995-04-26

Applicant: BASF AKTIENGESELLSCHAFT ,  AMBERG, Wilhelm ,  BERNARD, Harald ,  BUSCHMANN, Ernst ,  HAUPT, Andreas ,  JANITSCHKE, Lothar ,  JANSSEN, Bernd ,  KARL, Ulrich ,  KLING, Andreas ,  MÜLLER, Stefan ,  DE POTZOLLI, Bernd ,  RITTER, Kurt ,  THYES, Marco ,  ZIERKE, Thomas

Inventor： BASF AKTIENGESELLSCHAFT

IPC: C07K05/10

CPC classification number: C07K7/06 ,  C07K5/101

Abstract: Compounds of formula (I) are disclosed, wherein R , R , R , and R have the meanings indicated in the description, as well as a process for the production of these compounds. The compounds are suitable for use as starting material for the synthesis of substances which have anti-tumour properties.

Abstract translation: 可用于制备式I的化合物所描述（I）其中，R <1>，R <2>，R <3>和R <4>具有说明书中所示的含义，和一种方法。 所述化合物可用作强效抗肿瘤物质的合成原料是有用的。