公开(公告)号：EP2252611A1

公开(公告)日：2010-11-24

申请号：EP09708584.9

申请日：2009-02-06

申请人： N.V. Organon

发明人： VAN RIJN, Rachel Deborah ,  LOOZEN, Hubert, Jan, Jozef ,  TIMMERS, Cornelis, Marius ,  VAN DER VEEN, Lars, Anders ,  KARSTENS, Willem, Frederik, Johan

IPC分类号： C07D471/04 ,  C07D471/18 ,  A61K31/551 ,  A61P15/08

CPC分类号： C07D471/04 ,  C07D471/18

摘要： The invention relates to 5,6 - dihydropyrrolo [2,1-a] isoquinoline and pyrrolo[2,1-a] isoquinoline derivatives according to general formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.

公开(公告)号：EP2197445A2

公开(公告)日：2010-06-23

申请号：EP08787554.8

申请日：2008-08-28

申请人： N.V. Organon

发明人： KARSTENS, Willem, Frederik, Johan ,  CONTI, Paolo, Giovanni, Martino ,  TIMMERS, Cornelis, Marius ,  PLATE, Ralf ,  VAN KOPPEN, Christianus, Johannes

IPC分类号： A61K31/47 ,  A61P5/08 ,  C07D215/38

CPC分类号： C07D215/38 ,  A61K31/47 ,  A61K31/4709 ,  C07D401/10 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12

摘要： The present invention relates the use of a compound, a pharmaceutical composition, compounds and a kit for treating or preventing disorders in a mammal responsive to TSH receptor mediated pathways, including disorders such as hyperthyroidism, Graves' disease, Graves Ophthalmopathy, Graves' associated pretibial dermopathy, nodular goitre and thyroid cancer comprising administering to said mammal an effective amount of a tetrahydroquinoline compound of Formula (I) or an pharmaceutically acceptable salt thereof.

摘要翻译： 本发明涉及化合物，药物组合物，化合物和用于治疗或预防针对TSH受体介导的途径的哺乳动物疾病的试剂盒的应用，包括诸如甲状腺机能亢进，格雷夫斯病，格雷夫斯眼病，格雷夫斯相关的前囟素 皮肤病，结节性甲状腺肿和甲状腺癌，包括向所述哺乳动物施用有效量的式（I）的四氢喹啉化合物或其药学上可接受的盐。

公开(公告)号：EP2435433A1

公开(公告)日：2012-04-04

申请号：EP10723991.5

申请日：2010-05-25

申请人： N.V. Organon

发明人： LOOZEN, Hubert, Jan, Jozef ,  TIMMERS, Cornelis, Marius

IPC分类号： C07D471/04 ,  C07D519/00 ,  A61K31/4745 ,  A61P15/08

CPC分类号： C07D471/04 ,  C07D519/00

摘要： The invention relates to imidazoiso[5,1-
a ]quinoline and 5,6-dihydro-imidazoiso[5,1-
a ]quinoline derivatives according to general Formula (1) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.

公开(公告)号：EP1879581A1

公开(公告)日：2008-01-23

申请号：EP06754954.3

申请日：2006-05-02

申请人： N.V. Organon

发明人： KARSTENS, Willem, Frederik, Johan ,  TIMMERS, Cornelis, Marius

IPC分类号： A61K31/47 ,  C07D215/20 ,  C07D401/12 ,  A61K31/4709 ,  A61P5/24

CPC分类号： C07D215/20 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12

摘要： The present invention- relates to 2-methyl-4-phenyl-5-oxo-1 ,4,5,6,7,8-hexahydroquinoline derivatives having the general Formula (I) wherein the substituents are defined as in the description, or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, as well as to the use of these 2-methyl-4-phenyl-5-oxo-1 ,4,5,6,7,8-hexahydroquinoline derivatives in therapy, more specifically for the treatment of fertility disorders.

摘要翻译： 本发明涉及具有通式（I）的2-甲基-4-苯基-5-氧代-1,4,5,6,7,8-六氢喹啉衍生物，其中取代基如说明书中所定义，或 其药学上可接受的盐。 本发明还涉及包含所述衍生物的药物组合物，以及这些2-甲基-4-苯基-5-氧代-1,4,5,6,7,8-六氢喹啉衍生物在治疗中的用途，更具体地 用于治疗生育障碍。

公开(公告)号：EP1879580A1

公开(公告)日：2008-01-23

申请号：EP06754952.7

申请日：2006-05-02

申请人： N.V. Organon

发明人： TIMMERS, Cornelis, Marius ,  KARSTENS, Willem, Frederik, Johan ,  GRIMA POVEDA, Pedro, Manuel

IPC分类号： A61K31/47 ,  C07D215/20 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12 ,  A61K31/4709 ,  A61P5/24

CPC分类号： C07D401/12 ,  C07D215/20 ,  C07D405/12 ,  C07D417/12

摘要： The invention relates to a 4-phenyl-5-oxo-l,4,5,6,7,8-hexahydroquinoline derivative according to Formula (I), wherein the substituents are defined as in the description, or a pharmaceutically salt thereof. The compounds of this invention are potent FSH receptor activators and may be used for treating fertility disorders in e.g. controlled ovarian hyperstimulation and IVF procedures.

公开(公告)号：EP2252611B1

公开(公告)日：2011-10-05

申请号：EP09708584.9

申请日：2009-02-06

申请人： N.V. Organon

发明人： VAN RIJN, Rachel Deborah ,  LOOZEN, Hubert, Jan, Jozef ,  TIMMERS, Cornelis, Marius ,  VAN DER VEEN, Lars, Anders ,  KARSTENS, Willem, Frederik, Johan

IPC分类号： C07D471/04 ,  C07D471/18 ,  A61K31/551 ,  A61P15/08

CPC分类号： C07D471/04 ,  C07D471/18

摘要： The invention relates to 5,6 - dihydropyrrolo [2,1-a] isoquinoline and pyrrolo[2,1-a] isoquinoline derivatives according to general formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.

公开(公告)号：EP1879580B1

公开(公告)日：2009-03-11

申请号：EP06754952.7

申请日：2006-05-02

申请人： N.V. Organon

发明人： TIMMERS, Cornelis, Marius ,  KARSTENS, Willem, Frederik, Johan ,  GRIMA POVEDA, Pedro, Manuel

IPC分类号： A61K31/47 ,  C07D215/20 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12 ,  A61K31/4709 ,  A61P5/24

CPC分类号： C07D401/12 ,  C07D215/20 ,  C07D405/12 ,  C07D417/12

摘要： The invention relates to a 4-phenyl-5-oxo-l,4,5,6,7,8-hexahydroquinoline derivative according to Formula (I), wherein the substituents are defined as in the description, or a pharmaceutically salt thereof. The compounds of this invention are potent FSH receptor activators and may be used for treating fertility disorders in e.g. controlled ovarian hyperstimulation and IVF procedures.

公开(公告)号：EP1879581B1

公开(公告)日：2008-09-03

申请号：EP06754954.3

申请日：2006-05-02

申请人： N.V. Organon

发明人： KARSTENS, Willem, Frederik, Johan ,  TIMMERS, Cornelis, Marius

IPC分类号： A61K31/47 ,  C07D215/20 ,  C07D401/12 ,  A61K31/4709 ,  A61P5/24

CPC分类号： C07D215/20 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12

摘要： The present invention- relates to 2-methyl-4-phenyl-5-oxo-1 ,4,5,6,7,8-hexahydroquinoline derivatives having the general Formula (I) wherein the substituents are defined as in the description, or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, as well as to the use of these 2-methyl-4-phenyl-5-oxo-1 ,4,5,6,7,8-hexahydroquinoline derivatives in therapy, more specifically for the treatment of fertility disorders.

公开(公告)号：EP1322651B1

公开(公告)日：2008-01-23

申请号：EP01982306.1

申请日：2001-09-17

申请人： N.V. Organon

发明人： TIMMERS, Cornelis, Marius ,  KARSTENS, Willem, Frederik, Johan

IPC分类号： C07D495/04 ,  C07D239/78 ,  A61K31/519 ,  A61P5/24 ,  C07D487/04 ,  C07D471/04 ,  C07D491/04 ,  C07D215/48

CPC分类号： C07D471/04 ,  C07D239/78 ,  C07D495/04

摘要： A bicyclic heteroaromatic compound according to general formula (I), or a pharmaceutically acceptable salt thereof, wherein R1 is (3-8C)cycloalkyl, (2-7C)heterocycloalkyl, (6-14C)aryl or (4-13C)heteroaryl; all optionally substituted with one or more substituents; R2 is (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkynyl, (6-14C)aryl or (4-13C)heteroaryl; R3 is (1-8C)alkyl, (3-8C)cycloalkyl, (2-7C)heterocycloalkyl, (6-14C)aryl or (4-13C)heteroaryl; Y is CH or N; Z is NH¿2? or OH; A is S, N(H), N(R), O or a bond and B is N(H), O or a bond; X1-X2 is C=C, C(O)-NH, NH-C(O), C(O)-O, O-C(O), C=N, N=C or S or O. The compounds of the invention can be used in fertility regulation therapies.