公开(公告)号：CA1315781C

公开(公告)日：1993-04-06

申请号：CA604676

申请日：1989-07-04

Applicant: HARTOG JACOBUS A J

Inventor： DEN HARTOG JACOBUS A J ,  VAN STUIVENBERG HERMAN H ,  VAN WIJNGAARDEN INEKE

IPC: A61K31/55 ,  A61P1/04 ,  C07D471/04 ,  C07D491/04 ,  C07D491/048 ,  C07D491/147 ,  C07D495/04 ,  C07D495/14 ,  C07D491/00 ,  C07D495/00

Abstract: DIR 0422 The invention relates to a group of new 1,4-diazepine derivatives of the formula wherein A represents a group of the formulae 2-10 (2) (3) (4) (5) (6) (7) (8) (9) (10) These compounds have a strong anti-ulcer activity after oral administration.

公开(公告)号：AU2003250232A1

公开(公告)日：2003-12-19

申请号：AU2003250232

申请日：2003-05-28

Applicant: SOLVAY PHARM BV ,  HARTOG JACOBUS A J ,  REINDERS JAN H ,  SCHARRENBURG GUUSTAAF J M VAN ,  PRAS RAVES MARIA L ,  GUSTAFSON GARY R

Inventor： HARTOG JACOBUS A J DEN ,  REINDERS JAN H ,  SCHARRENBURG GUUSTAAF J M VAN ,  PRAS-RAVES MARIA L ,  GUSTAFSON GARY R

IPC: C07D251/42 ,  A61K31/53 ,  A61K31/5377 ,  A61P1/00 ,  A61P1/04 ,  A61P3/10 ,  A61P7/02 ,  A61P7/06 ,  A61P9/06 ,  A61P9/10 ,  A61P9/12 ,  A61P11/00 ,  A61P11/02 ,  A61P11/06 ,  A61P17/00 ,  A61P17/04 ,  A61P17/06 ,  A61P19/02 ,  A61P19/10 ,  A61P25/00 ,  A61P25/04 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28 ,  A61P27/06 ,  A61P29/00 ,  A61P31/04 ,  A61P31/12 ,  A61P35/00 ,  A61P35/02 ,  A61P37/00 ,  A61P37/08 ,  A61P43/00 ,  C07D251/50 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14

公开(公告)号：WO2005032547A1

公开(公告)日：2005-04-14

申请号：PCT/EP2004/052392

申请日：2004-10-01

Applicant: SOLVAY PHARMACEUTICALS B.V. ,  DEN HARTOG, Jacobus, A., J. ,  DAVID, Samuel ,  JASSERAND, Daniel ,  VAN SCHARRENBURG, Gustaaf, J., M. ,  VAN STUIVENBERG, Herman, H. ,  TUINSTRA, Tinka

Inventor： DEN HARTOG, Jacobus, A., J. ,  DAVID, Samuel ,  JASSERAND, Daniel ,  VAN SCHARRENBURG, Gustaaf, J., M. ,  VAN STUIVENBERG, Herman, H. ,  TUINSTRA, Tinka

IPC: A61K31/4025

CPC classification number: A61K31/397 ,  A61K31/4025 ,  A61K31/4184 ,  A61K31/4523 ,  A61K31/517 ,  C07D401/04 ,  C07D403/04

Abstract: The invention relates to a group of hydronopol substituted benzimidazolone and quinazolinone derivatives which are agonists on human ORL1 (nociceptin) receptors. The invention also relates to the preparation of these compounds, to pharmaceutical compositions containing a pharmacologically active amount of at least one of these novel benzimidazolone and quinazolinone derivatives as an active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of disorders in which ORL1 receptors are involved. The invention relates to compounds of the general formula (1) wherein the symbols have the meanings as given in the description.

Abstract translation: 本发明涉及作为人类ORL1（伤害感受素）受体的激动剂的一组水诺酮取代的苯并咪唑酮和喹唑啉酮衍生物。 本发明还涉及这些化合物的制备，含有药理活性量的这些新的苯并咪唑酮和喹唑啉酮衍生物中的至少一种作为活性成分的药物组合物，以及这些药物组合物用于治疗疾病的用途 其中涉及ORL1受体。 本发明涉及通式（1）的化合物，其中符号具有说明书中给出的含义。

公开(公告)号：WO2005028466A1

公开(公告)日：2005-03-31

申请号：PCT/EP2004/052275

申请日：2004-09-23

Applicant: SOLVAY PHARMACEUTICALS B.V. ,  DEN HARTOG, Jacobus, A., J. ,  VAN SCHARRENBURG, Gustaaf, J., M. ,  STUIVENBERG, Herman, H. ,  TUINSTRA, Tinka ,  TERPSTRA, Jan-Willem

Inventor： DEN HARTOG, Jacobus, A., J. ,  VAN SCHARRENBURG, Gustaaf, J., M. ,  STUIVENBERG, Herman, H. ,  TUINSTRA, Tinka ,  TERPSTRA, Jan-Willem

IPC: C07D401/04

CPC classification number: C07C251/20 ,  C07C2603/28 ,  C07D401/04 ,  C07D451/04

Abstract: The invention relates to a group of novel benzimidazolone and quinazolinone derivatives which are agonists on human ORL1 (nociceptin) receptors. The invention also relates to the preparation of these compounds, to pharmaceutical compositions containing a pharmacologically active amount of at least one of these imidazolone and quinazolinone derivatives as an active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of disorders in which ORL1 receptors are involved. The invention relates to compounds of the general formula (1): wherein the symbols have the meanings as given in the description.

Abstract translation: 本发明涉及一组新的苯并咪唑酮和喹唑啉酮衍生物，它们是人类ORL1（伤害感受素）受体的激动剂。 本发明还涉及这些化合物的制备，含有药理活性量的这些咪唑啉酮和喹唑啉酮衍生物中的至少一种作为活性成分的药物组合物，以及这些药物组合物在治疗疾病中的用途 哪个ORL1受体参与。 本发明涉及通式（1）的化合物：其中符号具有说明书中给出的含义。

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。

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。