- ANTI-FIBROTIC PYRIDINONES
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This application relates to polycyclic compounds with a pyridinone or pyridinone derivative core including, substituted pyridinones, 5,6- and 6,6- bicyclic heterocycles and substituted pyridine-thiones. This application also discloses methods of preparing these polycyclic compounds, pharmaceutical compositions and medicaments comprising said compounds and methods to treat, prevent or diagnose diseases, disorders or conditions associated with fibrosis.
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Paragraph 0536
(2015/11/02)
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- COMBINATIONS OF MEDICAMENTS, CONTAINING PDE4-INHIBITORS AND EP4-RECEPTOR-ANTAGONISTS
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The present invention relates to new medicament combinations which contain in addition to one or more PDE4-inhibitors (1) at least one EP4 receptor antagonist (2), as well as the use thereof for the treatment of preferably respiratory complaints such as particularly COPD, chronic sinusitis and asthma. The invention relates in particular to those medicament combinations which contain, in addition to one or more, preferably one, PDE4 inhibitor of general formula 1 wherein X is SO or SO2, but preferably SO, and wherein R1, R2, R3 and R4 have the meanings given in claim 1, at least one EP4 receptor antagonist (2), the preparation thereof and the use thereof for the treatment of respiratory complaints.
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Paragraph 0406; 0407
(2013/09/12)
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- DRUG COMBINATIONS CONTAINING PDE4 INHIBITORS AND NSAIDS
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The present invention relates to new drug combinations which contain in addition to one or more PDE4-inhibitors at least one NSAID (=non-steroidal anti-inflammatory drug) (2), processes for preparing them and their use in treating in particular respiratory complaints such as for example COPD, chronic sinusitis and asthma. The invention particularly relates to those drug combinations which contain, in addition to one or more, preferably one PDE4 inhibitor of general formula 1 wherein X is SO or SO2, but preferably SO, and wherein R1, R2, R3 and R4 have the meanings given in claim 1, at least one NSAID (2), the preparation thereof and the use thereof for the treatment of respiratory complaints.
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- METHODS OF USING DIHYDROPYRIDOPHTHALAZINONE INHIBITORS OF POLY (ADP-RIBOSE)POLYMERASE (PARP)
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Provided herein are methods of treating cancer comprising administering a topoisomerase inhibitor, temozolomide, or a platin in combination with a Compound of Formula (I) or Formula (II), where the substituents Y, Z, A, B, R1, R2, R3, R4 and R5 are as defined herein.
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Page/Page column 173
(2011/11/01)
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- SUBSTITUTED PIPERAZINO-DIHYDROTHIENOPYRIMIDINES
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The invention relates to new piperidino-dihydrothienopyrimidines of formula 1, as well as pharmacologically acceptable salts thereof, wherein X is SO or SO2, but preferably SO, and wherein R1, R2, R3 and R4 may have the meanings given in claim 1, as well as pharmaceutical compositions which contain these compounds. These new piperidino-dihydrothienopyrimidines are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system or cancers.
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Page/Page column 92
(2011/02/18)
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- DIHYDROPYRIDOPHTHALAZINONE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP)
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A compound having the structure set forth in Formula (I) and Formula (II): wherein the substituents Y, Z, A, B, R1, R2, R3, R4 and R5 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.
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Page/Page column 89
(2010/03/02)
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- AZABENZIMIDAZOLYL COMPOUNDS
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Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I), as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
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Page/Page column 55
(2008/06/13)
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- Structure-guided design of substituted aza-benzimidazoles as potent hypoxia inducible factor-1α prolyl hydroxylase-2 inhibitors
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We report the structure-based design and synthesis of a novel series of aza-benzimidazoles as PHD2 inhibitors. These efforts resulted in compound 22, which displayed highly potent inhibition of PHD2 function in vitro.
- Frohn, Mike,Viswanadhan, Vellarkad,Pickrell, Alexander J.,Golden, Jennifer E.,Muller, Kristine M.,Buerli, Roland W.,Biddlecome, Gloria,Yoder, Sean C.,Rogers, Norma,Dao, Jennifer H.,Hungate, Randall,Allen, Jennifer R.
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scheme or table
p. 5023 - 5026
(2009/05/26)
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- 3-(Imidazolyl methyl)-3-aza-bicyclo[3.1.0]hexan-6-yl)methyl ethers: A novel series of mGluR2 positive allosteric modulators
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The synthesis and structure-activity relationship (SAR) of a novel series of 3-(imidazolyl methyl)-3-aza-bicyclo[3.1.0]hexan-6-yl)methyl ethers, derived from a high throughput screening (HTS), are described. Subsequent optimization led to identification of potent, metabolically stable and orally available mGluR2 positive allosteric modulators (PAMs).
- Zhang, Lei,Rogers, Bruce N.,Duplantier, Allen J.,McHardy, Stanley F.,Efremov, Ivan,Berke, Helen,Qian, Weimin,Zhang, Andy Q.,Maklad, Noha,Candler, John,Doran, Angela C.,Lazzaro Jr., John T.,Ganong, Alan H.
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scheme or table
p. 5493 - 5496
(2009/06/18)
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- PHARMACOLOGICALLY ACTIVE IMIDAZO[4,5-C]PYRIDINES
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The invention relates to 6-substituted imidazo[4,5-c]pyridines of formula 1, in which X is O (oxygen) or NH and Y has either the meaning -CH2-AR or Y denotes the group gp (gp) wherein Z has the meaning -CHR8- or -CHR8-CHR9-. The compounds have gastric secretion inhibiting and excellent gastric and intestinal protective action properties.
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Page/Page column 42
(2010/02/11)
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- 1,3-DIHYDROIMIDAZOLE FUSED-RING COMPOUND
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The objective of this invention is to provide novel compounds that show excellent DPPIV-inhibiting activity. The present invention provides compounds represented by the general formula (I), salts thereof, or hydrates thereof, [wherein,T1 stands for a monocyclic or bicyclic 4 to 12-membered heterocycle having 1 or 2 nitrogen atoms in the ring, which may have substituents; in formula (I), the following formula represents a double bond or a single bond; X3 denotes an oxygen atom or a sulfur atom; X1 denotes a C2-6 alkynyl group which may have substituents; Z1 denotes a nitrogen atom or the formula -CR3=; Z2 and Z3 each independently denote a nitrogen atom, the formula -CR1=, a carbonyl group, or the formula -NR2-; R1, R2, R3, and X2 each independently denote a C1-6 alkyl group which may have substituents, and such].
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Page/Page column 82
(2008/06/13)
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- (1H-Imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: A novel class of potent MSK-1-inhibitors
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A novel series of imidazo[4,5-c]pyridines bearing a 1,2,5-oxadiazol-3- ylamine functionality has been developed. These are potent inhibitors of mitogen and stress-activated protein kinase-1.
- Bamford, Mark J.,Alberti, Michael J.,Bailey, Nicholas,Davies, Susannah,Dean, David K.,Gaiba, Alessandra,Garland, Stephen,Harling, John D.,Jung, David K.,Panchal, Terence A.,Parr, Christopher A.,Steadman, Jon G.,Takle, Andrew K.,Townsend, James T.,Wilson, David M.,Witherington, Jason
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p. 3402 - 3406
(2007/10/03)
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- Structure and properties of N-methyl-N-(4-pyridyl)-nitramine and 1,4-dihydro- 1-methyl-4-nitriminopyridine
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The molecular structure and spectral properties of N-methyl-N-(4-pyridyl)-nitramine (1) and 1,4-dihydro-l-methyl-4nitriminopyridine (3) were investigated by the X-ray diffraction, FTIR, nuclear magnetic resonance (NMR) methods and DFT theoretical calculat
- Kyzio?,Broda,Zaleski,Daszkiewicz
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p. 157 - 169
(2007/10/03)
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- IMIDAZOPYRIDINES AS MUSCARINIC AGENTS
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The compound of the formula: STR1 where R 1 is H, alkyl, perhaloalkyl, arylalkyl, alkenyl or alkynyl; R 2 is H when R. sub.4 is other than H, and, when R 4 is H, R 2 is STR2 in which R 5 is hydrogen or alkyl; R 3 is hydrogen or halogen; R. sub.4 is H or STR3 X, Y and Z are, independently, nitrogen or carbon, at least one of X, Y or Z being nitrogen; n is 1 or 2; n 1 is 0, 1, 2, 3, 4, or 5; or a pharmaceutically acceptable salt thereof are centrally active muscarinic agents.
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- Aminopyridine compounds
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An aminopyridine compound represented by the formula: STR1 wherein n represents 0 or 1; Z represents =S, =NCN or =CHNO2 ; R1 represents --NR3 R4, --NHNR3 R4, --NHCONHR3 or --NHSO2 R3 ; R2 represents H, or substituted or unsubstituted alkyl; R3 and R4, which may be the same or different, represent H, substituted or unsubstituted alkyl, aryl, substituted or unsubstituted acyl or alkoxycarbonyl group; and R3 and R4 may form a heterocyclic ring together with a nitrogen atom to which R3 and R4 are bound, through another heteroatom or without it; an optical isomer thereof or art acid salt thereof, which is excellent in pharmacological effect and repressed in side effects as a drug for circulatory diseases.
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- Aminopyridine compounds
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An aminopyridine compound represented by the formula: STR1 wherein n represents 0 or 1; Z represents =S, =O, =NCN or =CHNO2 ; R1 represents --CN, --NR3 R4, --CONR3 R4, --NHNR3 R4, --NHCONHR3, --NHSO2 R3 or --SR3 ; R2 represents H, or substituted or unsubstituted alkyl; R3 and R4, which may be the same or different, represent H, substituted or unsubstituted alkyl, aryl, substituted or unsubstituted acyl or alkoxycarbonyl group; and R3 and R4 may form a heterocyclic ring together with a nitrogen atom to which R3 and R4 are bound, through another heteroatom or without it; or an acid salt thereof, which is excellent in pharmacological effect and repressed in side effects as a drug for circulatory diseases.
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- SYNTHESES WITH AROMATIC NITRAMINES, V. PHOTOCHEMICAL REARRANGEMENT OF NITRAMINOPYRIDINES
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All three isomeric nitraminopyridines were photolysed in methanol with low-pressure mercury lamp (253.7 nm). 2-Nitraminopyridine yielded both 2-amino-3-nitro- and 2-amino-5-nitropyridines (isomer ratio 6.26 : 1). 3-Nitropyridine rearranged into both 4-nitro- and 2-nitro-3-aminopyridines (isomer ratio 1.28 : 1), whereas 4-nitraminopyridine gave 3-nitro-4-aminopyridine as the sole product. 1-Methyl-2-nitriminopyridine did not rearrange under the conditions applied, but 1-methyl-4-nitriminopyridine gave 3-nitro-4-methylaminopyridine.The latest product was also obtained when the same starting material was rearranged in conc. sulfuric acid.
- Sepiol, J.,Tomasik, P.
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p. 159 - 164
(2007/10/02)
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