公开(公告)号：US20080214495A1

公开(公告)日：2008-09-04

申请号：US11994846

申请日：2006-07-05

申请人： Christer Alstermark ,  Kosrat Amin ,  Kjell Andersson ,  Yantao Chen ,  Ulf Fahlander ,  Kevin Michael Foote ,  Kenneth Granberg ,  Daniel Hovdal

发明人： Christer Alstermark ,  Kosrat Amin ,  Kjell Andersson ,  Yantao Chen ,  Ulf Fahlander ,  Kevin Michael Foote ,  Kenneth Granberg ,  Daniel Hovdal

IPC分类号： A61K31/501 ,  C07D401/14 ,  A61K31/497 ,  A61K31/496 ,  A61K31/397 ,  A61P9/00

CPC分类号： C07D409/14 ,  C07D401/04 ,  C07D401/14

摘要： The invention relates to compounds of formula (I), wherein R1 and R3 are independently selected from carbon and nitrogen; R2 is oxo or thioxo; n is 0, 1 or 2; each R10 is independently selected from hydrogen and C1-3alkyl; R4 and R5 are each selected from carbon and nitrogen, wherein at least one of R4 and R5 is nitrogen; R6 is hydrogen or oxo; R7 is an aliphatic, partially saturated or aromatic carbocyclic ring, said carbocyclic ring having 0, 1 or 2 hetero nitrogen; m is 0, 1 or 2; each R11 is independently selected from hydrogen, hydroxy, oxo, C1-5alkyl, carboxy, hydroxyC1-5alkyl, carboxyC1-5alkyl, C1-5alkoxy-oxoC1-5alkyl, carbamoyl, C1-5alkylcarbamoyl, di (C1-5 alkyl)carbamoyl, carbamoylC1-4alkyl,C1-5alkylcarbamoylC1-4alkyl, di(C1-5alkyl)carbamoylC1-4alkyl, hydroxyC1-5alkylcarbamoyl, C1-5 alkoxyC1-5alkylcarbamoyl, hydroxyC1-5alkylcarbamoylC1-4alkyl, C1-5alkoxyC1-5 alkylcarbamoylC1-4 alkyl, CONR80(CH2)xS(O)pR90, CONH(CH2)qNR100R100, —C1-5 alkyl-Y1, —COOCHR170R180 and —CON R170R180; R8 is a bond, C1-4alkylene or C2-6alkenylene; R9 is an aromatic ring system having 0, 1 or 2 hetero atoms; wherein R9 is substituted by 0 or 1 halogen; or a pharmaceutically acceptable salt thereof, said compounds possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The invention also relates to processes for the preparation of the compounds, to their use, to pharmaceutical compositions comprising them, to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect, and to combinations comprising them.

公开(公告)号：US20080200431A1

公开(公告)日：2008-08-21

申请号：US11994844

申请日：2006-07-05

申请人： Christer Alstermark ,  Kosrat Amin ,  Kjell Andersson ,  Ulf Fahlander ,  Kenneth Granberg ,  Daniel Hovdal

发明人： Christer Alstermark ,  Kosrat Amin ,  Kjell Andersson ,  Ulf Fahlander ,  Kenneth Granberg ,  Daniel Hovdal

IPC分类号： A61K31/727 ,  C07D401/14 ,  A61K31/501 ,  A61P7/00 ,  C07D487/04 ,  A61K31/496

CPC分类号： C07D401/14

摘要： The invention relates to compounds of formula (I), Chemical formula should be inserted here. Please see paper copy wherein R1, R2, R3 and R4 are independently selected from carbon and nitrogen, and where is nitrogen; A1 is a single bond or a double bond; n is 0, 1, 2 or 3; each R5 is independently selected from hydrogen, halogen, C1-3 alkyl, oxo, oxy, oxido and thioxo; R6 is hydrogen or oxo; m is 0, 1, 2 or 3; A2 is a single bond or a double bond; each R7 is independently selected from hydrogen, hydroxy, oxo, C1-5alkyl, carboxy, cyano, tetrazolyl, N—C1-5alkyltetrazolyl, oxazolyl, C1-5oxazolyl, isoxazolyl, C1-5 isoxazolyl, hydroxyC1-5alkyl, carboxy C1-5alkyl, C1-5alkoxyoxo C1-5alkyl, carbamoyl, C1-5alkylcarbamoyl, di(C1-5alkyl)carbamoyl, carbamoyl C1-4alkyl, C1-5alkylcarbamoyl C1-4alkyl, di(C1-5alkyl)carbamoyl C1-4alkyl, hydroxy C1-5alkylcarbamoyl, C1-5alkoxy C1-5alkylcarbamoyl, hydroxy C1-5alkylcarbamoyl C1-4alkyl, C1-5alkoxy C1-5alkylcarbamoyl C1-4alkyl, —CONR8(CH2)xS(O)pR9, —CONH(CH2)qNR10R11, —C1-5alkyl-Y1, —COOCHR17R18 and —CONR17R18; and R30 is hydrogen, amino, methyl or halogen; or a pharmaceutically acceptable salt thereof, said compounds possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The invention also relates to processes for the preparation of the compounds, to their use, to pharmaceutical compositions comprising them, to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect, and to combinations comprising them.

公开(公告)号：US20080221063A1

公开(公告)日：2008-09-11

申请号：US11994847

申请日：2006-07-05

申请人： Christer Alstermark ,  Kjell Andersson ,  Ulf Fahlander ,  Kenneth Granberg

发明人： Christer Alstermark ,  Kjell Andersson ,  Ulf Fahlander ,  Kenneth Granberg

IPC分类号： A61K31/715 ,  C07D403/14 ,  A61K31/501

CPC分类号： C07D401/14

摘要： The invention relates to heterocyclic derivatives of formula (I), Chemical formula should be inserted here. Please see paper copy wherein R1 is hydrogen or C1-3alkyl; R2 is selected from hydroxy, C1-5alkyl, carboxy, cyano, tetrazolyl, N—C1-5alkyltetrazolyl, oxazolyl, C1-5oxazolyl, isoxazolyl, C1-5 isoxazolyl, hydroxyC1-5alkyl, carboxy C1-5alkyl, C1-5alkoxyoxo C1-5alkyl, carbamoyl, C1-5alkylcarbamoyl, di(C1-5alkyl)carbamoyl, C1-5alkylcarbamoyl C1-4alkyl, hydroxy C1-5alkylcarbamoyl, C1-5alkoxy C1-5alkylcarbamoyl; —C1-5alkyl-Y1, —COOCHR17R18 and —CONR17R18; and R3 is hydrogen or halogen; or a pharmaceutically acceptable salt thereof, said compounds possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The invention also relates to processes for the preparation of the compounds, to their use, to pharmaceutical compositions comprising them, to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect, and to combinations comprising them.

摘要翻译： 本发明涉及式（I）的杂环衍生物，其中应插入化学式。 请参见其中R 1是氢或C 1-3烷基的纸副本; R 2选自羟基，C 1-5烷基，羧基，氰基，四唑基，NC 1-5烷基四唑基，恶唑基， 1〜5个恶唑基，异恶唑基，C 1〜5个异恶唑基，羟基C 1-5烷基，羧基C 1-5 烷基，C 1-5烷氧基氧基C 1-5烷基，氨基甲酰基，C 1-5烷基氨基甲酰基，二（C 1） -5个烷基）氨基甲酰基，C 1-5烷基氨基甲酰基C 1-4烷基，羟基C 1-5烷基氨基甲酰基，C 1-5烷氧基C 1-5烷基氨基甲酰基; -C 1-5烷基-Y 1，-COOCHR 17 R 18和-CONR 17 R＆lt; 18＆gt;; R 3是氢或卤素; 或其药学上可接受的盐，所述化合物具有抗血栓形成和抗凝血性质，因此可用于治疗人或动物的方法。 本发明还涉及制备化合物，其用途，包含它们的药物组合物在制备用于产生抗血栓形成或抗凝血作用的药物中的用途，以及包含它们的组合的方法。