公开(公告)号：EP3369732A1

公开(公告)日：2018-09-05

申请号：EP18163765.3

申请日：2010-10-27

申请人： ORION CORPORATION

发明人： WOHLFAHRT, Gerd ,  TÖRMÄKANGAS, Olli ,  KARJALAINEN, Arja ,  KNUUTTILA, Pia ,  HOLM, Patrik ,  RASKU, Sirpa ,  VESALAINEN, Anniina ,  SALO, Harri ,  HÖGLUND, Lisa

IPC分类号： C07D403/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D401/12 ,  C07D231/12 ,  C07D471/12 ,  C07D487/04 ,  C07D513/04

CPC分类号： C07D513/04 ,  C07D231/12 ,  C07D231/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

摘要： Compounds of formula (I) wherein R 1 to R 16 , A. B and E are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula ( I ) possess utility as tissue-selective androgen receptor modulators (SARM) and are particularly useful as medicaments in the treatment of prostate cancer and other AR dependent conditions and diseases where AR antagonism is desired.

公开(公告)号：EP2493858B1

公开(公告)日：2014-07-02

申请号：EP10781918.7

申请日：2010-10-27

申请人： Orion Corporation

发明人： WOHLFAHRT, Gerd ,  TÖRMÄKANGAS, Olli ,  SALO, Harri ,  HÖGLUND, Iisa ,  KARJALAINEN, Arja ,  KNUUTTILA, Pia ,  HOLM, Patrik ,  RASKU, Sirpa ,  VESALAINEN, Anniina

IPC分类号： C07D231/14 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  A61P35/00 ,  A61K31/42 ,  A61K31/438 ,  A61K31/497 ,  A61K31/4523 ,  A61K31/5377 ,  A61K31/416 ,  A61K31/44

CPC分类号： C07D513/04 ,  C07D231/12 ,  C07D231/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

公开(公告)号：EP1412343A1

公开(公告)日：2004-04-28

申请号：EP02755036.7

申请日：2002-07-10

申请人： ORION CORPORATION

发明人： KOSKELAINEN, Tuula ,  OTSOMAA, Leena ,  KARJALAINEN, Arto ,  KOTOVUORI, Pekka ,  TENHUNEN, Jukka ,  RASKU, Sirpa ,  NORE, Pentti ,  TIAINEN, Eija ,  TÖRMÄKANGAS, Olli

IPC分类号： C07D311/04 ,  C07D311/32 ,  C07D319/16 ,  C07D327/06 ,  C07D405/12 ,  C07D411/12 ,  C07C217/14 ,  C07C217/54 ,  C07C217/90 ,  A61K31/135 ,  A61K31/353 ,  A61K31/357 ,  A61K31/39 ,  A61K31/4178 ,  A61K31/4433 ,  A61P9/06 ,  A61P9/10

CPC分类号： C07D405/12 ,  C07C217/14 ,  C07C217/54 ,  C07C217/90 ,  C07C2602/08 ,  C07D213/64 ,  C07D311/28 ,  C07D311/58 ,  C07D311/60 ,  C07D411/12

摘要： Therapeutically active compounds of formula (I): wherein X is -O-, -CH2- or -C(O)-; Z is -CHR9- or valence bond; Y is -CH2-, -C(O)-, CH(OR10)-, -CH(NR11R12 )-, -O-, -S-, -S(O)- or -S(O2)-, provided that in case Z is a valence bond, Y is not C(O); the dashed line represents an optional double bond in which case Z is -CR9- and Y is -CH-, C(OR10)- or -C(NR11R12 )-; R1 is -(CH2)nNR4R7 or one of the following groups:n is 1 - 4; R2 and R3 are independently H, lower alkyl, lower alkoxy, -NO2, halogen, -CF3, -OH, -NHR8 or -COOH; R4 and R7 are independently H, lower alkyl or lower hydroxyalkyl; R5 is H, lower alkoxy, -CF3, -NH2 or -CN; R6 is -NO2 , -NR14R19, -CF3 or R8 and R16 are independently H or acyl; R9 is H or lower alkyl; R10 is H, alkylsulfonyl or acyl; R11 and R12 are independently H, lower alkyl or acyl; R13 and R18 are independently H or -OR20; R14 and R19 are independently H, acyl, alkylsulfonyl, C(S)NHR17 or C(O)NHR17; R15 is H or NH2; R17 is H or lower alkyl; R20 is H or acyl; and pharmaceutically acceptable salts and esters thereof are disclosed. The compounds are potent inhibitors of Na+/Ca2+ exchange mechanism.

公开(公告)号：EP3056485A1

公开(公告)日：2016-08-17

申请号：EP16157716.8

申请日：2010-10-27

申请人： Orion Corporation

发明人： WOHLFAHRT, Gerd ,  TÖRMÄKANGAS, Olli ,  KARJALAINEN, Arja ,  KNUUTTILA, Pia ,  HOLM, Patrik ,  RASKU, Sirpa ,  VESALAINEN, Anniina ,  SALO, Harri ,  HÖGLUND, Iisa

IPC分类号： C07D231/12

CPC分类号： C07D513/04 ,  C07D231/12 ,  C07D231/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

摘要： A compound of formula

摘要翻译： 式的化合物

公开(公告)号：EP1412343B1

公开(公告)日：2006-08-30

申请号：EP02755036.7

申请日：2002-07-10

申请人： Orion Corporation

发明人： KOSKELAINEN, Tuula ,  OTSOMAA, Leena ,  KARJALAINEN, Arto ,  KOTOVUORI, Pekka ,  TENHUNEN, Jukka ,  RASKU, Sirpa ,  NORE, Pentti ,  TIAINEN, Eija ,  TÖRMÄKANGAS, Olli

IPC分类号： C07D311/04 ,  C07D311/32 ,  C07D319/16 ,  C07D327/06 ,  C07D405/12 ,  C07D411/12 ,  C07C217/14 ,  C07C217/54 ,  C07C217/90 ,  A61K31/135 ,  A61K31/353 ,  A61K31/357 ,  A61K31/39 ,  A61K31/4178 ,  A61K31/4433 ,  A61P9/06 ,  A61P9/10

CPC分类号： C07D405/12 ,  C07C217/14 ,  C07C217/54 ,  C07C217/90 ,  C07C2602/08 ,  C07D213/64 ,  C07D311/28 ,  C07D311/58 ,  C07D311/60 ,  C07D411/12

摘要： Therapeutically active compounds of formula (I): wherein X is -O-, -CH2- or -C(O)-; Z is -CHR9- or valence bond; Y is -CH2-, -C(O)-, CH(OR10)-, -CH(NR11R12 )-, -O-, -S-, -S(O)- or -S(O2)-, provided that in case Z is a valence bond, Y is not C(O); the dashed line represents an optional double bond in which case Z is -CR9- and Y is -CH-, C(OR10)- or -C(NR11R12 )-; R1 is -(CH2)nNR4R7 or one of the following groups:n is 1 - 4; R2 and R3 are independently H, lower alkyl, lower alkoxy, -NO2, halogen, -CF3, -OH, -NHR8 or -COOH; R4 and R7 are independently H, lower alkyl or lower hydroxyalkyl; R5 is H, lower alkoxy, -CF3, -NH2 or -CN; R6 is -NO2 , -NR14R19, -CF3 or R8 and R16 are independently H or acyl; R9 is H or lower alkyl; R10 is H, alkylsulfonyl or acyl; R11 and R12 are independently H, lower alkyl or acyl; R13 and R18 are independently H or -OR20; R14 and R19 are independently H, acyl, alkylsulfonyl, C(S)NHR17 or C(O)NHR17; R15 is H or NH2; R17 is H or lower alkyl; R20 is H or acyl; and pharmaceutically acceptable salts and esters thereof are disclosed. The compounds are potent inhibitors of Na+/Ca2+ exchange mechanism.

摘要翻译： 式（I）的治疗活性化合物：worin在式（I）中所示在本发明中定义的变量; 和药学上可接受的盐和酯。 该化合物中的Na ^{+ /钙 2 + 交换机制的有效抑制剂。}

公开(公告)号：EP3885340A1

公开(公告)日：2021-09-29

申请号：EP21169615.8

申请日：2010-10-27

申请人： ORION CORPORATION

发明人： WOHLFAHRT, Gerd ,  TÖRMÄKANGAS, Olli ,  KARJALAINEN, Arja ,  KNUUTTILA, Pia ,  HOLM, Patrik ,  RASKU, Sirpa ,  VESALAINEN, Anniina ,  SALO, Harri ,  HÖGLUND, Lisa

IPC分类号： C07D231/14 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  A61P35/00 ,  A61K31/42 ,  A61K31/438 ,  A61K31/497 ,  A61K31/4523 ,  A61K31/416 ,  A61K31/44

摘要： Compounds of formula ( I ) wherein R 1 to R 16 , A. B and E are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula ( I ) possess utility as tissue-selective androgen receptor modulators (SARM) and are particularly useful as medicaments in the treatment of prostate cancer and other AR dependent conditions and diseases where AR antagonism is desired.

公开(公告)号：EP3056485B1

公开(公告)日：2018-05-09

申请号：EP16157716.8

申请日：2010-10-27

申请人： Orion Corporation

发明人： WOHLFAHRT, Gerd ,  TÖRMÄKANGAS, Olli ,  KARJALAINEN, Arja ,  KNUUTTILA, Pia ,  HOLM, Patrik ,  RASKU, Sirpa ,  VESALAINEN, Anniina ,  SALO, Harri ,  HÖGLUND, Iisa

IPC分类号： C07D231/12

CPC分类号： C07D513/04 ,  C07D231/12 ,  C07D231/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

摘要： Compounds of formula (I) wherein R 1 to R 16 , A. B and E are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as tissue-selective androgen receptor modulators (SARM) and are particularly useful as medicaments in the treatment of prostate cancer and other AR dependent conditions and diseases where AR antagonism is desired.

公开(公告)号：EP2493858A1

公开(公告)日：2012-09-05

申请号：EP10781918.7

申请日：2010-10-27

申请人： Orion Corporation

发明人： WOHLFAHRT, Gerd ,  TÖRMÄKANGAS, Olli ,  SALO, Harri ,  HÖGLUND, Iisa ,  KARJALAINEN, Arja ,  KNUUTTILA, Pia ,  HOLM, Patrik ,  RASKU, Sirpa ,  VESALAINEN, Anniina

IPC分类号： C07D231/14 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  A61P35/00 ,  A61K31/42 ,  A61K31/438 ,  A61K31/497 ,  A61K31/4523 ,  A61K31/5377 ,  A61K31/416 ,  A61K31/44

CPC分类号： C07D513/04 ,  C07D231/12 ,  C07D231/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

摘要： Compounds of formula (I) wherein R
1 to R
16 , A. B and E are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as tissue-selective androgen receptor modulators (SARM) and are particularly useful as medicaments in the treatment of prostate cancer and other AR dependent conditions and diseases where AR antagonism is desired.

公开(公告)号：EP1583759A1

公开(公告)日：2005-10-12

申请号：EP04701023.6

申请日：2004-01-09

申请人： Orion Corporation

发明人： OTSOMAA, Leena ,  KOSKELAINEN, Tuula ,  KARJALAINEN, Arto ,  RASKU, Sirpa ,  POLLESELLO, Piero ,  LEVIJOKI, Jouko

IPC分类号： C07D405/14 ,  C07D405/12 ,  C07D411/12 ,  C07D213/75 ,  A61K31/4433 ,  A61P9/00

CPC分类号： C07D213/75 ,  C07D405/12 ,  C07D405/14 ,  C07D411/12

摘要： Therapeutically active compounds of formula (I) or (II) wherein X is -O-, -CH2- or -C(O)-; Z is -CHR12- or a valence bond; Y is -CH2-, -C(O)-, CH(OR13)-, -O-, -S-; provided that in case Z is a valence bond, Y is not C(O); the dashed line representing an optional double bond in which case Z is -CR12- ­and Y is -CH2-, -C(O)- or -CH(OR10)- (in formula II) or -CH- (in formula I); R2 and R3 are independently H, lower alkyl, lower alkoxy, -NO2, halogen, -CF3, -OH, benzyloxy or a group of formula (IIIa). R1 is H, CN, halogen, -CONH2, -COOR15, CH2NR15R18, NHC(O)R5, NHCH2R5, NHR20, NR21R22, NHC(NH)NHCH3 or, in case the compound is of formula (II) wherein the optional double bond exists or in case R2 or R3 is benzyloxy or a group of formula (IIIa) or in case the pyridine ring of formula (I) or (II) is attached to the oxygen atom in 3-, 4- or 5-position, R1 can also be -NO2 or NR16R17; R4 is H, -NO2, CN, halogen, -CONH2, -COOR15, -CH2NR15R18, -NR16R17, NHC(O)R5 or -NHC(NH)NHCH3; R5 is alkyl substituted with 1-3 substituents selected from the group consisting of halogen, amino and hydroxy, or carboxyalkyl, in which the alkyl portion is optionally substituted with 1-3 substituents selected from the group consisting of halogen, amino and hydroxyl, -CHR6NR,R8 or one of the following groups: formula (IVa), (IVb), (IVc), (IVd), (IVe), and pharmaceutically acceptable salts and esters thereof. The compounds are potent inhibitors of Na+/Ca2+ exchange mechanism.