公开(公告)号：EP1470121B1

公开(公告)日：2012-07-11

申请号：EP03705858.3

申请日：2003-01-23

申请人： Bayer HealthCare LLC

发明人： NAGARATHNAM, Dhanapalan ,  DUMAS, Jacques ,  HATOUM-MOKDAD, Holia ,  BOYER, Stephen ,  WANG, Chunguang ,  PLUEMPE, Hans ,  FEURER, Achim ,  BENNABI, Samir

IPC分类号： C07D401/12 ,  C07D239/48 ,  C07D413/12 ,  C07D403/12 ,  C07D413/14 ,  C07D409/14 ,  C07D471/04 ,  A61K31/506

CPC分类号： C07D239/48 ,  A61K31/506 ,  C07D401/12 ,  C07D403/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04

摘要： Disclosed are compounds and derivatives thereof, their synthesis, and their use as Rho-kinase inhibitors. These compounds are useful for inhibiting tumor growth, treating erectile dysfunction, and treating other indications mediated by Rho-kinase, e.g., coronary heart disease.

公开(公告)号：EP2090571B1

公开(公告)日：2012-05-16

申请号：EP08163784.5

申请日：2002-10-14

申请人： Boehringer Ingelheim Pharma GmbH & Co. KG ,  Boehringer Ingelheim Pharmaceuticals, Inc. ,  BOEHRINGER INGELHEIM INTERNATIONAL GMBH

发明人： Dahmann, Georg ,  Himmelsbach, Frank ,  Wittneben, Helmut ,  Pautsch, Alexander ,  Prokopowicz, Anthony S. ,  Krist, Bernd ,  Schnapp, Gisela ,  Steegmaier, Martin ,  Lenter, Martin ,  Schoop, Andreas ,  Steurer, Steffen ,  Spevak, Walter

IPC分类号： C07D239/48 ,  C07D403/12 ,  C07D471/04 ,  C07D401/12 ,  C07D413/12 ,  A61K31/505 ,  A61K31/506 ,  A61P35/00 ,  C07D235/00 ,  C07D221/00

CPC分类号： C07D239/48 ,  C07D231/12 ,  C07D233/56 ,  C07D239/50 ,  C07D239/80 ,  C07D249/08 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D451/04 ,  C07D451/06 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10

公开(公告)号：EP2443095A1

公开(公告)日：2012-04-25

申请号：EP10725720.6

申请日：2010-06-17

申请人： Cellzome Limited

发明人： MAJOR, Jeremy ,  PITON, Nelly

IPC分类号： C07D239/48 ,  C07D403/12 ,  C07D403/14 ,  A61K31/506 ,  A61P37/00

CPC分类号： C07D403/12 ,  C07D239/48 ,  C07D403/14

摘要： The invention relates to compounds of formula (I), wherein R
1 to R
6 and T
0 have the meaning as cited in the description and the claims. Said compounds are useful as inhibitors of ZAP-70 for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.

公开(公告)号：EP2440534A2

公开(公告)日：2012-04-18

申请号：EP10725114.2

申请日：2010-06-10

申请人： Cellzome Limited

发明人： RAMSDEN, Nigel ,  MAJOR, Jeremy ,  MOREL, Adeline ,  SUNOSE, Mihiro ,  PITON, Nelly

IPC分类号： C07D239/48 ,  A61K31/505 ,  C07D401/12 ,  C07D405/12

CPC分类号： C07D239/48

摘要： The invention relates to compounds of formula (I), wherein R
1 to R
5 , X and X
1 to X
3 have the meaning as cited in the description and the claims. Said compounds are useful as inhibitors of ZAP-70 for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.

公开(公告)号：EP2440533A1

公开(公告)日：2012-04-18

申请号：EP10785625.4

申请日：2010-06-14

申请人： Socpra-Sciences Et Génie S.E.C.

发明人： MULHBACHER, Jérôme ,  LAFONTAINE , Daniel ,  MALOUIN , François ,  ALLARD , Marianne ,  MARSAULT , Eric

IPC分类号： C07D239/46 ,  A61K31/513 ,  A61K31/519 ,  A61L2/16 ,  A61P31/04 ,  C07D239/48 ,  C07D239/50 ,  C07D239/56 ,  C07D498/04 ,  C07D513/04 ,  G01N33/569

CPC分类号： A61K31/675 ,  A61K31/4412 ,  A61K31/505 ,  A61K31/513 ,  A61K31/519 ,  A61K31/535 ,  A61K31/5383 ,  A61K31/54 ,  A61K31/542 ,  C07D239/46 ,  C07D239/48 ,  C07D239/50 ,  C07D498/04 ,  C07D513/04 ,  Y10T436/141111 ,  Y10T436/143333

摘要： The present invention includes novel compounds and pharmaceutically acceptable formulations of said compounds which exhibit antibiotic activity against microorganisms bearing a guanine riboswitch that controls the expression of the guaA gene, including organisms which are resistant to certain antibiotic families, and which are useful as antibacterial agents for treatment or prophylaxis of bacterial infections in animals or in humans, in particular but not limited to infections of the mammary gland, or their use as antiseptics, agents for sterilization or disinfection.

公开(公告)号：EP2194985A4

公开(公告)日：2012-01-25

申请号：EP08837766

申请日：2008-10-08

申请人： MEDICINES MALARIA VENTURE MMV

发明人： TARNCHOMPOO BONGKOCH ,  YUTHAVONG YONGYUTH ,  VILAIVAN TIRAYUT ,  CHITNUMSUB PENCHIT ,  THONGPANCHANG CHAWANEE ,  KAMCHONWONGPAISAN SUMALEE ,  MATTHEWS DAVID ,  VIVAS LIVIA ,  YUVANIYAMA JIRUNDON ,  CHARMAN SUSAN ,  CHARMAN WILLIAM ,  KATIYAR SANJAY BABU

IPC分类号： C07D239/48 ,  A61K31/495 ,  A61K31/496 ,  C07D401/04 ,  C07D401/12

CPC分类号： C07D401/04 ,  C07D239/48 ,  C07D401/12

摘要： The present invention relates to novel compounds that are inhibitors of wild type and mutant dihydrofolate reductase (DHFR) of Plasmodium falciparum, which are useful for the treatment of malaria. It also relates to processes of making and using such compounds. The antimalarial compounds of the present invention have low toxicity to a host infected with the malarial parasite, and are potent when administered in pharmaceutical compositions.

公开(公告)号：EP2197853B1

公开(公告)日：2011-11-09

申请号：EP08836924.4

申请日：2008-09-26

申请人： Dow AgroSciences LLC

发明人： GUENTHENSPBERGER, Katherine ,  JOHNSON, Timothy ,  NIYAZ, Noormohamed ,  HUNTER, Ricky ,  BROWN, Annette ,  TRULLINGER, Tony

IPC分类号： C07D239/48 ,  C07D401/12 ,  A01N43/54

CPC分类号： C07D239/48 ,  A01N43/54 ,  A01N43/84 ,  C07D401/12

摘要： Pyrimidinyl aryl hydrazones are effective at controlling insects.

公开(公告)号：EP1853568B1

公开(公告)日：2011-09-07

申请号：EP06707872.5

申请日：2006-01-27

申请人： Tibotec Pharmaceuticals

发明人： HEERES, Jan ,  LEWI, Paulus Joannes ,  LEEMANS, Rudolf ,  MOENS, Luc Jozef Raphael ,  JANSSEN, Paul Adriaan Jan

IPC分类号： C07D239/50 ,  C07D239/48 ,  A61K31/505 ,  A61P31/18

CPC分类号： C07D239/50 ,  C07D239/48

摘要： HIV replication inhibitors of formula (I) pharmaceut ically acceptable addition salts or stereochemically isomeric forms thereof, wherein X is NR4, S, SO or SO2; the preparation of these compounds as well as pharmaceutical compositions comprising these compounds; the use of these compounds for the prevention or the treatment of HIV infection.

公开(公告)号：EP1797048B1

公开(公告)日：2011-08-17

申请号：EP05803358.0

申请日：2005-09-29

申请人： Tibotec Pharmaceuticals

发明人： GUILLEMONT, Jerôme, Emile, Georges ,  HEERES, Jan ,  LEWI, Paulus Joannes

IPC分类号： C07D239/48 ,  C07D401/12 ,  C07D417/12 ,  C07D405/12 ,  C07D409/12 ,  C07D403/12 ,  C07D413/14 ,  A61K31/505

CPC分类号： C07D403/12 ,  C07D239/48 ,  C07D239/50 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/14 ,  C07D417/12

摘要： HIV replication inhibitors of formula (I) N-oxides, a pharmaceutically acceptable addition salts, a quaternary amines or a stereoisomeric forms thereof, wherein -a1=a2-a3=a4 - is -CH=CH-CH=CH-, -N=CH-CH=CH-, -N=CH-N=CH-, -N=CH- CH=N-, -N=N-CH=CH-; -b1=b2-b3=b4- is -CH=CH-CH=CH-, -N=CH-CH=CH-, -N=CH-N=CH-, -N=CH-CH=N-, -N=N-CH=CH-; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally subst ituted C1-6alkyl; C1-6alkyloxycarbonyl; R2 is OH; halo; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; substituted amino; polyhalomethyl; polyhalo methylt hio; -S(=O)rR6; C(=NH)R6; R2a is CN; amino; substituted amino; optionally subst ituted C1-6alkyl; halo; optionally substituted C1-6alkyloxy; substituted carbonyl; -CH=N-NH-C(=O)-R16; optionally substituted C1-6alkyloxy C1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; -C(=N-O-R8)-C1-4alkyl; R7 or -X3-R7; X1 is -NR1-, -O-, -C(=O)-, CH2 , -CHOH-, -S-, -S(=O)r-; R3 is CN; amino; C1-6alkyl; halo; optionally substituted C1-6alkyloxy; substituted carbonyl; -CH=N-NH-C(=O)-R16; substituted C1-6alkyl; optionally substituted C1-6alkyloxy C1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; -C(=N-O-R8)-C1-4alkyl; R7; -X3-R7; R4 is halo; OH; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; CN; nitro; polyhalo C1-6alkyl; polyhalo C1-6alkyloxy; substituted carbonyl; formyl; amino; mono- or di(C1-4alkyl)amino or R7; R5 is-Y-CqH2q-L or -CqH2q-Y-CrH2r-L; L is aryl or Het; processes for the preparation of these compounds, pharmaceut ical compositions comprising these compounds as active ingredient and the use of these compounds for the prevention or the treatment of HIV infection.

公开(公告)号：EP2132185B1

公开(公告)日：2011-08-03

申请号：EP08737283.5

申请日：2008-04-10

申请人： Richter Gedeon Nyrt.

发明人： BARTÁNÉ SZALAI, Gizella ,  ÁGAINÉ CSONGOR, Éva ,  DOMÁNY, György ,  GYERTYÁN, István ,  KISS, Béla ,  LASZY, Judit ,  SÁGHY, Katalin ,  SCHMIDT, Éva ,  FARKAS, Sándor ,  KOMLÓDI, Zsolt

IPC分类号： C07D239/48 ,  A61K31/506 ,  A61P25/00

CPC分类号： C07D239/48

摘要： The present invention relates to new dopamine D3 and D2 ligands of formula (I): wherein Rl, R2 and Q are as described herein, and/or geometric isomers and/or stereoisomers and/or diastereomers and/or salts and/or hydrates and/or solvates and/or polymorphs thereof. The invention also relates to processes for preparing the same, to compositions containing the same and to their use in the treatment and/or prevention of conditions which requires modulation of dopamine receptors.