1014645-75-0Relevant articles and documents
SUBSTITUTED OXADIAZOLES FOR COMBATING PHYTOPATHOGENIC FUNGI
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Page/Page column 75-76, (2017/06/12)
The present invention relates the compounds of the formula I, or the N-oxides, or the agriculturally acceptable salts thereof and to their use for combating phytopathogenic harmful fungi, wherein the variables are defined as given in the description and c
BENZYLAMINE DERIVATIVES
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Page/Page column 36; 45, (2014/07/23)
The present invention provides compounds of formula (I): compositions comprising such compounds; the use of such compounds in therapy (for example in the treatment or prevention of a disease or condition in which plasma kallikrein activity is implicated); and methods of treating patients with such compounds; wherein R1 to R3, R5 to R9, A, P, V, W, X, Y and Z are as defined herein.
PYRIDINE AMIDE DERIVATIVES AS EP4 RECEPTOR ANTAGONISTS
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Paragraph 0297-0298, (2013/10/08)
The invention relates pyridine amide derivative of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are independently hydrogen, linear o branched (C1-C3)alkyl or joined together they form a cyclopropyl ring; R is independently selected from the group consisting of halogens and trifluoromethyl and p is 1, 2 or 3; A is C or N; E is a group of formula (B) or (C), wherein B is C(O)OH, C(O)O(C1-C3)alkyl, and C is selected from the group consisting of formula (I) m is 1,2 or 3, n is 0 or 1, W is —O—, —O(C1-C3 alkyl)-; —(C1-C3 alkyl)O—; —C(O)—; —C(═N—O(C1-C3 alkyl))-; —NH— or —NH(C1-C3alkyl)-; Ar is phenyl, optionally substituted with one or more substituents selected from the group consisting of halogen, trifluoromethyl, trifluoromethoxy, methyl, —NH(C1-C3alkyl)-; —N(C1-C3alkyl)(C1-C3alkyl)-, a from 5 to 7 membered heterocyclic ring containing one nitrogen atom which is covalently bonded to Ar and optionally containing one or two heteroatoms selected from N, O and S; and a 5- or 6-membered heteroaromatic ring containing 1 to 3 heteroatoms selected from S, O e N, such heteroaromatic ring being substituted with one or two substituents selected from the group consisting of (C1-C3)alkyl, (C3-C5)cycloalkyloxy, (C1-C3)alkylcarbonyl. The compounds of the invention could be used for manufacturing a medicament for the treatment of pathologies which require the use of an antagonist of the EP4 receptor, such as the treatment of acute and chronic pain, inflammatory pain, osteoarthritis, inflammation-associated disorder as arthritis, rheumatoid arthritis, cancer, endometriosis and migraine.
PYRIDINE AMIDE DERIVATIVES AS EP4 RECEPTOR ANTAGONISTS
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Page/Page column 42, (2012/06/30)
The invention relates pyridine amide derivative of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are independently hydrogen, linear o branched (C1-C3)alkyl or joined together they form a cyclopropyl ring; R is independently selected from the group consisting of halogens and trifluoromethyl and p is 1, 2 or 3; A is C or N; E is a group of formula (B) or (C), wherein B is C(O)OH, C(O)O(C1-C3)alkyl, and C is selected from the group consisting of formula (I) m is 1,2 or 3, n is 0 or 1, W is -O-, -O(C1-C3 alkyl)-; -(C1-C3 alkyl)O-; -C(O)-; -C(=N-O(C1-C3 alkyl))-; -NH- or -NH(C1-C3alkyl)-; Ar is phenyl, optionally substituted with one or more substituents selected from the group consisting of halogen, trifluoromethyl, trifluoromethoxy, methyl, -NH(C1-C3alkyl)-; -N(C1-C3alkyl)(C1-C3alkyl)-, a from 5 to 7 membered heterocyclic ring containing one nitrogen atom which is convalently bonded to Ar and optionally containing one or two heteroatoms selected from N, O and S; and a 5- or 6-membered heteroaromatic ring containing 1 to 3 heteroatoms selected from S, O e N, such heteroaromatic ring being substituted with one or two substituents selected from the group consisting of (C1-C3)alkyl, (C3-C5)cycloalkyloxy, (C1-C3)alkylcarbonyl. The compounds of the invention could be used for manufacturing a medicament for the treatment of pathologies which require the use of an antagonist of the EP4 receptor, such as the treatment of acute and chronic pain, inflammatory pain, osteoarthritis, inflammation-associated disorder as arthritis, rheumatoid artrhritis, cancer, endometriosis and migraine.
Discovery of 4-{1-[({1-[4-(trifluoromethyl)benzyl]-1H-indol-7-yl}carbonyl) amino]cyclopropyl}benzoic acid (MF-766), a highly potent and selective EP 4 antagonist for treating inflammatory pain
Colucci, John,Boyd, Michael,Berthelette, Carl,Chiasson, Jean-Francois,Wang, Zhaoyin,Ducharme, Yves,Friesen, Rick,Wrona, Mark,Levesque, Jean-Francois,Denis, Danielle,Mathieu, Marie-Claude,Stocco, Rino,Therien, Alex G.,Clarke, Patsy,Rowland, Steve,Xu, Daigen,Han, Yongxin
scheme or table, p. 3760 - 3763 (2010/09/03)
The discovery of a highly potent and selective EP4 antagonist MF-766 is discussed. This N-benzyl indole derivative exhibits good pharmacokinetic profile and unprecedented in vivo potency in the rat AIA model.
The discovery of 4-{l-[({2,5-dimethyl-4-[4-(trifluoromethyl)benzyl]- 3thienyl}carbonyl)amino]cyclopropyl}benzoic acid (MK-2894), a potent and selective prostaglandin e2 subtype 4 receptor antagonist
Blouin, Marc,Han, Yongxin,Burch, Jason,Farand, Julie,Mellon, Christophe,Gaudreault, Mireille,Wrona, Mark,Lévesque, Jean-Fran?ois,Denis, Danielle,Mathieu, Marie-Claude,Stocco, Rino,Vigneault, Erika,Therien, Alex,Clark, Patsy,Rowland, Steve,Xu, Daigen,o'Neill, Gary,Ducharme, Yves,Friesen, Rick
experimental part, p. 2227 - 2238 (2010/08/21)
The discovery of highly potent and selective second generation EP4 antagonist MK-2894 (34d) is discussed. This compound exhibits favorable pharmacokinetic profile in a number of preclinical species and potent anti-inflammatory activity in several animal models of pain/inflammation. It also shows favorable GI tolerability profile in rats when compared to traditional NSAID indomethacin.
INDOLE AND INDOLINE CYCLOPROPYL AMIDE DERIVATIVES AS EP4 RECEPTOR ANTAGONISTS
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Page/Page column 25-26, (2008/12/08)
The invention is directed to indole and indoline cyclopropyl amide derivatives as EP4 receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer. Ph
THIOPHENECARBOXAMIDE DERIVATIVES AS EP4 RECEPTOR LIGANDS
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Page/Page column 56-57, (2008/06/13)
The invention is directed to thiophenecarboxamide derivatives of formulae I and II as EP4 receptor ligands, antagonists or agonists, useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoi