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    BENZISOXAZOLE DERIVATIVES HAVING D4-ANTAGONISTIC ACTIVITY
    1.
    发明申请
    BENZISOXAZOLE DERIVATIVES HAVING D4-ANTAGONISTIC ACTIVITY 审中-公开
    具有D4-拮抗活性的苯并恶唑衍生物

    公开(公告)号：WO9940067A2

    公开(公告)日：1999-08-12

    申请号：PCT/EP9900852

    申请日：1999-02-05

    Applicant: DUPHAR INT RES ,  HARTOG JACOBUS A J ,  VISSER GERBEN M ,  STEEN BARTHOLOMEUS J VAN ,  TULP MARTINUS T M ,  RONKEN ERIC ,  KRUSE CORNELIS G ,  LANGE JOSEPHUS H M

    Inventor： DEN HARTOG JACOBUS A J ,  VISSER GERBEN M ,  VAN STEEN BARTHOLOMEUS J ,  TULP MARTINUS T M ,  RONKEN ERIC ,  KRUSE CORNELIS G ,  LANGE JOSEPHUS H M

    IPC: A61K31/445 ,  A61K31/454 ,  A61K31/55 ,  A61P25/00 ,  A61P25/16 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07D413/14 ,  C07D

    CPC classification number: C07D413/14

    Abstract: The present invention relates to a group of novel benzisoxazole derivatives which are potent and selective antagonists of the dopamine D4-receptor. The compounds have general formula (I) wherein (R1)n represents 0, 1, or 2 substituents, which can be the same or different, from the group C1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino mono- or dialkyl (C1-2)-amino, sulfonyl-(C1-3)alkyl or -alkoxy, sulfonyl trifluoromethyl, sulfonyl amino, and sulfonyl mono- or dialkyl (C1-2)-amino, X is O, S, NH or NCH3, Y represents CH2 or (CH2)2, (R2)m represents 0, 1, or 2 substituents, which can be the same or different, from the group methyl and ethyl, or (R2)m is a methylene bridge or ethylene bridge, A is a group -CH2-(CRH)p- wherein R is hydrogen or methyl and p is 0 or 1, and B represents 2- or 3-indolyl or 2-benzimidazolyl, which groups may be substituted at carbon with 1 or 2 substituents from the group C-1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino, mono- or dialkyl (C1-2)amino, sulfonyl-(C1-3)alkyl or -alkoxy, sulfonyl trifluoromethyl, sulfonyl amino, and sulfonyl mono- or dialkyl (C1-2)-amino.

    Abstract translation: 本发明涉及一组新颖的苯并异恶唑衍生物，它们是多巴胺D4-受体的有效和选择性拮抗剂。 所述化合物具有通式（I）：其中（R 1）n表示0,1或2个取代基，所述取代基可以相同或不同，选自C 1-3烷基或烷氧基，卤素，三氟甲基，硝基， （C1-2） - 氨基，磺酰基 - （C1-3）烷基或 - 烷氧基，磺酰基三氟甲基，磺酰基氨基和磺酰基单或二烷基（C1-2） - 氨基，X是O，S，NH或 NCH 3，Y代表CH 2或（CH 2）2，（R 2）m代表0,1或2个可与甲基和乙基相同或不同的取代基，或（R 2）m是亚甲基桥或亚乙基 桥基，A是基团-CH 2 - （CRH）p - ，其中R是氢或甲基，p是0或1，B代表2-或3-吲哚基或2-苯并咪唑基，这些基团可以在碳上被1 或C1-C3-烷基或烷氧基，卤素，三氟甲基，硝基，氨基，单或二烷基（C1-2）氨基，磺酰基 - （C1-3）烷基或 - 烷氧基，磺酰基三氟甲基， 磺酰基氨基和磺酰基单或二烷基（C1-2） - 氨基。

    2-AMINOQUINOLINE DERIVATIVES HAVING D4-AGONISTIC ACTIVITY
    2.
    发明申请
    2-AMINOQUINOLINE DERIVATIVES HAVING D4-AGONISTIC ACTIVITY 审中-公开
    具有D4-激活活性的2-氨基喹啉衍生物

    公开(公告)号：WO9940068A2

    公开(公告)日：1999-08-12

    申请号：PCT/EP9900855

    申请日：1999-02-05

    Applicant: DUPHAR INT RES ,  HARTOG JACOBUS A J ,  VISSER GERBEN M ,  STEEN BARTHOLOMEUS J VAN ,  TULP MARTINUS T M ,  RONKEN ERIC ,  KRUSE CORNELIS G

    Inventor： DEN HARTOG JACOBUS A J ,  VISSER GERBEN M ,  VAN STEEN BARTHOLOMEUS J ,  TULP MARTINUS T M ,  RONKEN ERIC ,  KRUSE CORNELIS G

    IPC: A61K31/4709 ,  A61K31/496 ,  A61P25/00 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07D201/00 ,  C07D215/38 ,  C07D401/12 ,  C07D405/12 ,  C07D

    CPC classification number: C07D215/38 ,  C07D401/12 ,  C07D405/12

    Abstract: The present invention relates to a group of novel 2-aminoquinoline derivatives which are potent and selective agonists of the dopamine D4-receptor. The compounds have general formula (I) wherein (R1)n represents 1 or 2 substituents, which can be the same or different, from the group C1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino, and mono- or dialkyl (C1-2)-amino, or two groups R1 at adjacent carbon atoms together with the benzene ring may form the benzdioxane group or benzofuran group, X represents nitrogen or carbon, and the dotted line may represent a double bond, (R2)p represents 0, 1 or 2 substituents, which can be the same or different, from the group methyl and ethyl, or (R2)p is a methylene bridge or ethylene bridge, R3 is hydrogen or methyl, and (R)m represents 0, 1, or 2 substituents, which can be the same or different and can be located at all available positions of the quinolyl group, from the group C1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino, and mono- or dialkyl (C1-2)-amino, on the understanding that R1 cannot represent o-OCH3 when X is nitrogen, (R2)p and R3 are hydrogen, m is 0 and n is 1.

    Abstract translation: 本发明涉及一组新的2-氨基喹啉衍生物，其是多巴胺D4-受体的有效和选择性激动剂。 化合物具有通式（I），其中（R1）n表示1或2个可以相同或不同的取代基，可以是C1-3 - 烷基或烷氧基，卤素，三氟甲基，硝基，氨基和单 - 或 二烷基（C1-2） - 氨基或两个相邻碳原子的R1与苯环一起形成苯并二恶烷基或苯并呋喃基，X表示氮或碳，虚线表示双键，（R2） p表示0,1或2个与甲基和乙基基团相同或不同的取代基，或（R2）p是亚甲基桥或乙烯桥，R3是氢或甲基，（R）m表示0 ，1或2个取代基，其可以相同或不同，并且可以位于喹啉基的所有可用位置，C 1-3 - 烷基或烷氧基，卤素，三氟甲基，硝基，氨基和单 - 或 二烷基（C 1-2） - 氨基，但应理解，当X为氮时，R 1不能表示o-OCH 3，（R 2）p和R 3为氢，m为0，n为 是1。

    5.
    发明专利
    未知

    公开(公告)号：ES2196785T3

    公开(公告)日：2003-12-16

    申请号：ES99910210

    申请日：1999-02-05

    Applicant: DUPHAR INT RES

    Inventor： DEN HARTOG JACOBUS A J ,  VISSER GERBEN M ,  VAN STEEN BARTHOLOMEUS J ,  TULP MARTINUS T M ,  RONKEN ERIC ,  KRUSE CORNELIS G

    IPC: A61K31/4709 ,  A61K31/496 ,  A61P25/00 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07D201/00 ,  C07D215/38 ,  C07D401/12 ,  C07D405/12

    Abstract: The present invention relates to a group of novel 2-aminoquinoline derivatives which are potent and selective agonists of the dopamine D4-receptor. The compounds have general formula (I) wherein (R1)n represents 1 or 2 substituents, which can be the same or different, from the group C1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino, and mono- or dialkyl (C1-2)amino, or two groups R1 at adjacent carbon atoms together with the benzene ring may form the benzdioxane group or benzofuran group, X represents nitrogen or carbon, and the dotted line may represent a double bond, (R2)p represents 0, 1 or 2 substituents, which can be the same or different, from the group methyl and ethyl, or (R2)p is a methylene bridge or ethylene bridge, R3 is hydrogen or methyl, and (R)m represents 0, 1, or 2 substituents, which can be the same or different and can be located at all available positions of the quinolyl group, from the group C1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino, and mono- or dialkyl (C1-2)amino, on the understanding that R1 cannot represent o-OCH3 when X is nitrogen, (R2)p and R3 are hydrogen, m is 0 and n is 1

    BENZISOXAZOLE DERIVATIVES HAVING D4-ANTAGONISTIC ACTIVITY
    7.
    发明专利
    BENZISOXAZOLE DERIVATIVES HAVING D4-ANTAGONISTIC ACTIVITY 未知

    公开(公告)号：CA2320120A1

    公开(公告)日：1999-08-12

    申请号：CA2320120

    申请日：1999-02-05

    Applicant: DUPHAR INT RES

    Inventor： VISSER GERBEN M ,  TULP MARTINUS T M ,  DEN HARTOG JACOBUS A J ,  VAN STEEN BARTHOLOMEUS J ,  KRUSE CORNELIS G ,  LANGE JOSEPHUS H M ,  RONKEN ERIC

    IPC: A61K31/445 ,  A61K31/454 ,  A61K31/55 ,  A61P25/00 ,  A61P25/16 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07D413/14

    Abstract: The present invention relates to a group of novel benzisoxazole derivatives which are potent and selective antagonists of the dopamine D4-receptor. The compounds have general formula (I) wherein (R1)n represents 0, 1, or 2 substituents, which can be the same or different, from the group C1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino mono- or dialkyl (C1-2)-amino, sulfonyl-(C1-3)alkyl or -alkoxy, sulfonyl trifluoromethyl, sulfonyl amino, and sulfonyl mono- or dialkyl (C1-2)-amino, X is O, S, NH or NCH3, Y represents CH2 or (CH2)2, (R2)m represents 0, 1, or 2 substituents, which can be the same or different, from the group methyl and ethyl, or (R2)m is a methylene bridge or ethylene bridge, A is a group -CH2-(CRH)p- wherein R is hydrogen or methyl and p is 0 or 1, and B represents 2- or 3-indolyl or 2-benzimidazolyl, which groups may be substituted at carbon with 1 or 2 substituents from the group C1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino, mono- or dialkyl (C1-2)amino, sulfonyl-(C1-3)alkyl or -alkoxy, sulfonyl trifluoromethyl, sulfonyl amino, and sulfonyl mono- or dialkyl (C1-2)-amino.

    ALKYLENEDIOXYPHENYL ETHER DERIVATIVES HAVING ANTI-ISCHAEMIC, MEMORY ENHANCING AND ANTI-CONVULSIVE ACTIVITY
    9.
    发明专利
    ALKYLENEDIOXYPHENYL ETHER DERIVATIVES HAVING ANTI-ISCHAEMIC, MEMORY ENHANCING AND ANTI-CONVULSIVE ACTIVITY 未知

    公开(公告)号：CA2063314A1

    公开(公告)日：1992-09-21

    申请号：CA2063314

    申请日：1992-03-18

    Applicant: DUPHAR INT RES

    Inventor： LANGE JOSEPHUS H M ,  TOOROP GERRIT P ,  VAN WIJNGAARDEN INEKE ,  DEN HARTOG JACOBUS A J

    IPC: C07D317/64 ,  C07D319/18 ,  C07D405/06 ,  A61K31/36 ,  A61K31/445 ,  A61K31/495

    Abstract: DIR 0482 The invention relates to compounds having anti-ischaemic activity, memory enhancing activity and anti-convulsive activity of the formulae 1A and 1B (1A) (1B) wherein -R1 + R2 together form an alkylene group having 1-3 C-atoms which may be substituted with one or more alkyl group(s) having 13 C-atoms; -Z is methylene optionally substituted with one alkyl group having 1-3 C-atoms, or with one phenylalkyl group with 1-3 C-atoms in the alkyl group, which phenyl group may be substituted with a group (R5)p wherein. R6 is halogen, hydroxy, alkyl or hydroxyalkyl having 1-5 C-atoms, alkoxy having 1-3 C-atoms, S-alkyl, S(O)-alkyl or S(O)2-alkyl having 1-3 Catoms, amino, mono- or dialkylamino having 1-3 C-atoms per alkyl group, trifluoromethyl, trifluoromethoxy, a sulphonylamido group SO2NHR or a carbalkoxy group COOR wherein R is alkyl having 1-4 C-atoms, the group COOH, SO3H,CONH2, the amidino group or cyano group, and p has the value 0-3; -R3 and R4 independent of each other represent hydrogen, alkyl having 1-10 C-atoms, alkenyl or alkynyl having 3-10 Catoms, cycloalkyi having 3-8 C-atoms, cycloalkyl-alkyl having 3-8 ring atoms and 1-5 C-atoms in the alkyl group, phenylalkyl or heteroaryl-alkyl having 1-5 C-atoms in the alkyl group, phenylalkenyl, heteroaryl-alkenyl, phenylalkynyl or heteroaryl-alkynyl group having 3-5 C-atoms in the alkenyl group or alkynyl group, which groups R3 and R4 may be substituted with a group (R8)p wherein R6 and p have the above mentioned meanings, or wherein R3+R4 together with DIR 0482 the nitrogen atom form a saturated or unsaturated heterocyclic group of 5-7 ring atoms, which may contain a second hetero-atom from the group consisting of oxygen, sulphur and nitrogen, which ring may be substituted with a group (R5)p wherein R6 and p have the above mentioned meanings, or with phenylalkyl, heteroarylalkyl, phenylalkenyl, heteroaryl-alkenyl, phenylalkynyl or heteroaryl-alkynyl having at most 3 C-atoms in the alkyl, alkenyl or alkynyl part, which groups may be substituted with a group (R6)p wherein R6 and p have the above-mentioned meanings, or which ring may be annelated with a phenyl group; -R5 is alkyl having 1-12 C-atoms, alkenyl or alkynyl having 3-12 C-atoms, cycloalkyl having 3-8 C-atoms, cycloalkyl-alkyl having 3-8 ring atoms and 1-5 C-atoms in the alkyl group, phenylalkyl or heteroaryl-alkyl having 1-5 C-atoms in the alkyl sub-group, phenylalkenyl, heteroaryl-alkenyl, phenylalkynyl or heteroaryl-alkynyl having 3-5 C-atoms in the alkenyl subgroup or alkynyl sub-group, which groups may be substituted with a group (R6)p, wherein R6 and p have the abovementioned meanings, and which alkyl sub-groups, alkenyl sub-groups and alkynyl sub-groups may contain a group -O-, S- or CO, or a pharmacologically acceptable salt thereof

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