公开(公告)号：EP4136081A1

公开(公告)日：2023-02-22

申请号：EP21717118.0

申请日：2021-04-14

申请人： F. Hoffmann-La Roche AG

发明人： BERCHTOLD, Stefan ,  GALLEY, Guido ,  GROEBKE ZBINDEN, Katrin ,  GUBA, Wolfgang ,  KRUMM, Danny

IPC分类号： C07D285/16 ,  C07D417/06 ,  A61P29/00 ,  A61K31/549

公开(公告)号：EP1828155A4

公开(公告)日：2011-04-20

申请号：EP05851657

申请日：2005-11-15

申请人： NICOX SA

IPC分类号： C07D285/16 ,  A61K31/41 ,  A61K31/4245 ,  A61K31/5375 ,  A61K31/54 ,  C07D269/00 ,  C07D295/00 ,  C07D411/12

CPC分类号： C07D411/12 ,  A61K31/4245 ,  A61K31/63 ,  A61K45/06 ,  A61K2300/00

公开(公告)号：EP1812412B1

公开(公告)日：2008-04-23

申请号：EP05806565.7

申请日：2005-10-29

申请人： Sanofi-Aventis Deutschland GmbH

发明人： KLEEMAN, Heinz-Werner

IPC分类号： C07D277/20 ,  C07D279/02 ,  C07D285/00 ,  C07D285/16 ,  A61K31/00 ,  A61P9/00

CPC分类号： C07D277/20 ,  C07D277/22 ,  C07D279/02 ,  C07D285/01 ,  C07D285/16

摘要： The invention relates to substituted benzoylguanidines of formula (I), where R1 to R8, X and Y have the meanings given in the claims and the pharmaceutically-acceptable salts thereof which are substituted acylguanidines and inhibit cellular Sodium/Proton antiporter (Na+/H+-Exchanger, NHE). Compounds of formula (I) and the pharmaceutically-acceptable salts thereof are suitable for the prevention and treatment of disease caused by activation of or by an activated NHE as a result of the NHE-inhibitory properties thereof and also of secondary diseases caused by damage brought about by the NHE.

公开(公告)号：EP1708713B1

公开(公告)日：2008-03-12

申请号：EP05700747.8

申请日：2005-01-07

申请人： F. Hoffmann-la Roche AG

发明人： SUI, Meng ,  ZHAO, Shu-Hai

IPC分类号： A61K31/517 ,  A61K31/5415 ,  A61K31/536 ,  C07D239/80 ,  C07D285/16 ,  C07D265/18 ,  C07D405/06 ,  A61P25/18

CPC分类号： C07D403/04 ,  C07D239/80 ,  C07D265/18 ,  C07D285/16 ,  C07D413/04 ,  C07D417/04

摘要： The invention relates to substituted quinazolinone compunds of formula (I) or a pharmaceutically acceptable salt thereof, wherein Y is C or S; m is 1 when Y is C and m is 2 when Y is S; n is 1 or 2; p is from 0 to 3; q is from 1 to 3; Z is -(CRaRb)r- or -SO2-, wherein r is from 0 to 2 and each of Ra and Rb is independently hydrogen or alkyl; X is CH or N; R2 is optionally substituted aryl or optionally substituted heteroaryl; preferably R2 is aryl, and more preferably phenyl optionally substituted by one or more trifluoromethyl, halo, cyano, C1-C6 alkyl or C1-C6 alkoxy; A is -NR3- or -O- wherein R3 is: hydrogen; alkyl, acyl, amidoalkyl, hydroxyalkyl or alkoxyalkyl; the other substituents are defined in the claims. The compounds are modulators of the 5-hydroxytryptamine receptor and are useful for the treatment of diseases of the central nervous system such as psychoses, schizophrenia, manic depressions, neurological disorders, memory disorders, attention deficit disorder, Parkinson’s disease, amyotrophic lateral sclerosis, Alzheimer’s disease, food uptake disorders, and Huntington’s disease.

公开(公告)号：EP1708713A1

公开(公告)日：2006-10-11

申请号：EP05700747.8

申请日：2005-01-07

申请人： F. Hoffmann-la Roche AG

发明人： SUI, Meng ,  ZHAO, Shu-Hai

IPC分类号： A61K31/517 ,  A61K31/5415 ,  A61K31/536 ,  C07D239/80 ,  C07D285/16 ,  C07D265/18 ,  C07D405/06 ,  A61P25/18

CPC分类号： C07D403/04 ,  C07D239/80 ,  C07D265/18 ,  C07D285/16 ,  C07D413/04 ,  C07D417/04

摘要： The invention relates to substituted quinazolinone compunds of formula (I) or a pharmaceutically acceptable salt thereof, wherein Y is C or S; m is 1 when Y is C and m is 2 when Y is S; n is 1 or 2; p is from 0 to 3; q is from 1 to 3; Z is -(CRaRb)r- or -SO2-, wherein r is from 0 to 2 and each of Ra and Rb is independently hydrogen or alkyl; X is CH or N; R2 is optionally substituted aryl or optionally substituted heteroaryl; preferably R2 is aryl, and more preferably phenyl optionally substituted by one or more trifluoromethyl, halo, cyano, C1-C6 alkyl or C1-C6 alkoxy; A is -NR3- or -O- wherein R3 is: hydrogen; alkyl, acyl, amidoalkyl, hydroxyalkyl or alkoxyalkyl; the other substituents are defined in the claims. The compounds are modulators of the 5-hydroxytryptamine receptor and are useful for the treatment of diseases of the central nervous system such as psychoses, schizophrenia, manic depressions, neurological disorders, memory disorders, attention deficit disorder, Parkinson’s disease, amyotrophic lateral sclerosis, Alzheimer’s disease, food uptake disorders, and Huntington’s disease.

公开(公告)号：EP1498411A4

公开(公告)日：2005-11-30

申请号：EP03723188

申请日：2003-04-24

申请人： ONO PHARMACEUTICAL CO

发明人： HATAYAMA AKIRA ,  TSURUTA HIROSHI ,  OCHI YASUO ,  IMAWAKA HARUO ,  OHMOTO KAZUYUKI

IPC分类号： C07C243/24 ,  A61K31/16 ,  A61K31/165 ,  A61K31/341 ,  A61K31/351 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/4035 ,  A61K31/4152 ,  A61K31/4166 ,  A61K31/4168 ,  A61K31/421 ,  A61K31/423 ,  A61K31/425 ,  A61K31/426 ,  A61K31/427 ,  A61K31/428 ,  A61K31/429 ,  C07C243/34 ,  C07C251/76 ,  C07C251/84 ,  C07C251/86 ,  C07D207/22 ,  C07D207/50 ,  C07D209/46 ,  C07D209/48 ,  C07D211/28 ,  C07D211/72 ,  C07D211/86 ,  C07D211/98 ,  C07D213/70 ,  C07D213/76 ,  C07D213/77 ,  C07D213/78 ,  C07D233/38 ,  C07D233/52 ,  C07D233/80 ,  C07D239/10 ,  C07D239/18 ,  C07D239/36 ,  C07D241/08 ,  C07D241/18 ,  C07D263/26 ,  C07D263/28 ,  C07D265/08 ,  C07D265/10 ,  C07D265/32 ,  C07D265/33 ,  C07D275/02 ,  C07D275/03 ,  C07D275/06 ,  C07D277/18 ,  C07D277/36 ,  C07D277/50 ,  C07D277/54 ,  C07D277/60 ,  C07D277/82 ,  C07D279/02 ,  C07D279/06 ,  C07D279/12 ,  C07D285/10 ,  C07D285/16 ,  C07D309/04 ,  C07D309/28 ,  C07D335/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D513/10 ,  C07F9/59 ,  C07F9/6558 ,  C07D207/408 ,  C07D211/26 ,  C07D213/53 ,  C07D231/08 ,  C07D233/32 ,  C07D307/52 ,  C07D309/06 ,  C07D413/12 ,  C07D487/04

CPC分类号： C07D209/48 ,  A61K31/16 ,  A61K31/165 ,  A61K31/341 ,  A61K31/351 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/4035 ,  A61K31/4152 ,  A61K31/4166 ,  A61K31/4168 ,  A61K31/421 ,  A61K31/423 ,  A61K31/425 ,  A61K31/426 ,  A61K31/427 ,  A61K31/428 ,  A61K31/429 ,  C07C243/34 ,  C07C251/76 ,  C07C251/84 ,  C07C251/86 ,  C07C2601/08 ,  C07C2601/14 ,  C07D207/22 ,  C07D207/50 ,  C07D209/46 ,  C07D211/28 ,  C07D211/72 ,  C07D211/86 ,  C07D211/98 ,  C07D213/70 ,  C07D213/76 ,  C07D213/77 ,  C07D213/78 ,  C07D233/38 ,  C07D233/52 ,  C07D233/80 ,  C07D239/10 ,  C07D239/18 ,  C07D239/36 ,  C07D241/08 ,  C07D241/18 ,  C07D263/26 ,  C07D263/28 ,  C07D265/08 ,  C07D265/10 ,  C07D265/33 ,  C07D275/02 ,  C07D275/03 ,  C07D275/06 ,  C07D277/18 ,  C07D277/36 ,  C07D277/50 ,  C07D277/54 ,  C07D277/60 ,  C07D277/82 ,  C07D279/02 ,  C07D279/06 ,  C07D279/12 ,  C07D285/10 ,  C07D285/16 ,  C07D309/04 ,  C07D309/28 ,  C07D335/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D513/10 ,  C07F9/591 ,  C07F9/65583

摘要： The present invention relates to a diketohydrazine derivative of formula (I) and a pharmaceutically acceptable salt thereof (the symbols in the formula have the same meaning as described in the specification). The compound of formula (I) has an inhibitory activity against cysteine protease, and it is useful for the treatment of inflammatory diseases, immune diseases, ischemic diseases, respiratory diseases, circulatory diseases, blood diseases, neuronal diseases, hepatic or biliary diseases, osseous or articular diseases, metabolic diseases, etc. And the compound has inhibitory activity against elastase and it is also useful for the treatment of COPD (chronic obstacle pulmonary diseases).

摘要翻译： 本发明涉及式（I）的二酮肼衍生物及其药学上可接受的盐（式中的符号具有与说明书中所述相同的含义）。 式（I）化合物对半胱氨酸蛋白酶具有抑制活性，可用于治疗炎性疾病，免疫疾病，缺血性疾病，呼吸系统疾病，循环系统疾病，血液病，神经元疾病 ，肝或胆道疾病，骨关节疾病，代谢疾病等。该化合物对弹性蛋白酶具有抑制活性，也可用于治疗慢性阻塞性肺疾病（慢性阻塞性肺疾病）。

公开(公告)号：EP1531815A1

公开(公告)日：2005-05-25

申请号：EP03761446.8

申请日：2003-06-27

申请人： NOVO NORDISK A/S

发明人： POLISETTI, Dharma, Rao ,  KODRA, János, Tibor ,  LAU, Jesper ,  BLOCH, Paw ,  VALCARCE-LOPEZ,Maria,Carmen, ,  BLUME, Niels ,  GUZEL, Mustafa ,  SANTHOSH, Kalpathy, Chidambareswaran ,  MJALLI, Adnan, M., M. ,  ANDREWS, Robert, Carl ,  SUBRAMANIAN, Govindan ,  ANKERSEN, Michael ,  VEDSOE, Per ,  MURRAY, Anthony ,  JEPPESEN, Lone ,  LAU, Jesper

IPC分类号： A61K31/433 ,  A61P3/10 ,  A61P3/06 ,  A61P3/04 ,  C07D277/48 ,  C07D277/52 ,  C07D213/75 ,  C07D417/12 ,  C07D277/56 ,  C07D417/06 ,  C07D417/14 ,  C07D285/16 ,  C07D487/04 ,  C07D277/54

CPC分类号： C07D277/38 ,  A61K31/426 ,  A61K31/427 ,  A61K31/454 ,  A61K31/55 ,  A61K45/06 ,  C07D213/75 ,  C07D277/46 ,  C07D277/48 ,  C07D277/52 ,  C07D277/54 ,  C07D277/56 ,  C07D285/135 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D473/38

摘要： This invention relates to aryl carbonyl derivatives of the general formula (I), which are activators of glucokinase which may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.(Formul 1).

公开(公告)号：EP0973513A4

公开(公告)日：2003-03-19

申请号：EP97912787

申请日：1997-10-23

申请人： ZYMOGENETICS INC ,  OSTEOSCREEN INC ,  UNIV TEXAS

发明人： ORME MARK W ,  BAINDUR NAND ,  ROBBINS KIRK G ,  HARRIS SCOTT M ,  KONTOYIANNI MARIA ,  HURLEY LAURENCE H ,  KERWIN SEAN M ,  MUNDY GREGORY R ,  PETRIE CHARLES

IPC分类号： C07D239/74 ,  A61K31/00 ,  A61K31/136 ,  A61K31/192 ,  A61K31/196 ,  A61K31/215 ,  A61K31/4184 ,  A61K31/426 ,  A61K31/428 ,  A61K31/437 ,  A61K31/44 ,  A61K31/444 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/498 ,  A61K31/502 ,  A61K31/517 ,  A61K31/53 ,  A61K31/535 ,  A61K31/5415 ,  A61K31/549 ,  A61K31/655 ,  A61P19/08 ,  A61P19/10 ,  C07C49/84 ,  C07C69/92 ,  C07C225/32 ,  C07C233/55 ,  C07C233/59 ,  C07C233/80 ,  C07C235/38 ,  C07C237/20 ,  C07C243/22 ,  C07C243/32 ,  C07C243/34 ,  C07C243/38 ,  C07C245/08 ,  C07C251/20 ,  C07C251/28 ,  C07C251/48 ,  C07C251/66 ,  C07C251/86 ,  C07C259/10 ,  C07C311/39 ,  C07C323/62 ,  C07C337/06 ,  C07D213/53 ,  C07D213/76 ,  C07D213/78 ,  C07D213/85 ,  C07D215/12 ,  C07D215/38 ,  C07D235/08 ,  C07D235/22 ,  C07D241/42 ,  C07D265/16 ,  C07D277/20 ,  C07D277/56 ,  C07D277/64 ,  C07D277/82 ,  C07D279/16 ,  C07D285/16 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D471/04 ,  C07D521/00 ,  A61K31/165 ,  A61K31/33 ,  A61K31/405 ,  A61K31/415 ,  A61K31/42 ,  A61K31/425 ,  A61K31/505

CPC分类号： A61K31/655 ,  A61K31/196 ,  A61K31/4184 ,  A61K31/428 ,  A61K31/444 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/498 ,  A61K31/517 ,  A61K31/53

摘要： Compounds containing two aromatic systems covalently linked through a linker containing one or more atoms, or "linker" defined as including a covalent bond per se so as to space the aromatic systems at a distance 1.5-15 ANGSTROM , are effective in treating conditions associated with bone deficits. The compounds can be administered to vertebrate subjects alone or in combination with additional agents that promote bone growth or that inhibit bone resorption. They can be screened for activity prior to administration by assessing their ability to effect the transcription of a reporter gene coupled to a promoter associated with a bone morphogenetic protein and/or their ability to stimulate calvarial growth in model animal systems.

公开(公告)号：EP0533268B1

公开(公告)日：2001-08-16

申请号：EP92202806.3

申请日：1992-09-14

申请人： GLAXO GROUP LIMITED

发明人： Oxford, Alexander William ,  Mitchell, William Leonard ,  Bradshaw, John ,  Clitherow, John Watson ,  Carter, Malcolm

IPC分类号： C07D271/06 ,  A61K31/41 ,  C07D271/10 ,  C07D249/06 ,  C07D285/16 ,  C07D249/08 ,  C07D285/18 ,  C07D285/12 ,  A61P25/24

CPC分类号： C07D249/08 ,  C07D249/06 ,  C07D271/06 ,  C07D271/07 ,  C07D271/107 ,  C07D285/06 ,  C07D285/08 ,  C07D285/12

公开(公告)号：EP0675885B1

公开(公告)日：2000-09-06

申请号：EP94903690.9

申请日：1993-12-21

申请人： COMMONWEALTH SCIENTIFIC AND INDUSTRIAL RESEARCH ORGANISATION

发明人： RIZZARDO, Ezio ,  EVANS, Richard, Alexander ,  MOAD, Graeme ,  THANG, San Hoa

IPC分类号： C07D327/02 ,  C07D327/10 ,  C08G75/06 ,  C08G75/14 ,  C08G75/20 ,  C07D335/02 ,  C07D339/08 ,  C07D279/02 ,  C07D279/06 ,  C07D285/18 ,  C07D285/16

CPC分类号： C07D327/10 ,  C07D327/02

摘要： Compounds of formula (1), wherein: R?1 and R2¿ are independently selected from the group comprising hydrogen, C¿1? to C6 alkyl, C1 to C6 haloalkyl, phenyl, and substituted phenyl; X is selected from the group comprising sulfur, sulphone, disulfide; Y is selected from oxygen, carbon, N-H, N-alkyl, N-aryl, or sulfur; and Z is any linking functionality. The compounds represent a new class of ring opening monomers.