- NOVEL COMPOUNDS FOR USE IN COGNITION IMPROVEMENT
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Novel compounds for use in cognition improvement It relates to certain compounds having a polycyclic structure and a -(C=O)NRaRb moiety, wherein the polycyclic structure comprises at least three ring systems, wherein one ring system is a polycyclic ring system comprising from 2 to 4 rings; at least one ring is an aromatic ring; and wherein the structure comprises at least 3 nitrogen atoms and 1 oxygen atom. It also relates to pharmaceutical compositions containing them, and to their use in medicine, in particular in the treatment and/or prevention of neurological disorders coursing with a cognition deficit or impairment, or neurodegenerative diseases.
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Page/Page column 69; 70
(2016/04/19)
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- NOVEL COMPOUNDS AS DUAL INHIBITORS OF PHOSPHODIESTERASES AND HISTONE DEACETYLASES
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It relates to certain compounds having a polycyclic structure and a hydroxamic acid moiety, wherein the polycyclic structure comprises at least three ring systems, wherein one ring system is a polycyclic ring system comprising from 2 to 4 rings; at least one ring is an aromatic ring; and wherein the structure comprises at least 3 nitrogen atoms and 1 oxygen atom. It also relates to a process for their preparation, as well as to pharmaceutical compositions containing them, and to their use in medicine, in particular in the treatment and/or prevention of neurological disorders coursing with a cognition deficit or impairment, or neurodegenerative diseases. wherein B1 is a radical selected from the group consisting of formula (A"), formula (B"), formula (C"), and formula (D"):
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Page/Page column 138; 139
(2014/09/16)
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- N-BUTYRAMIDE, THE PREPARATION METHOD AND USE THEREOF
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Disclosed are N-{1-[3-(2-ethoxy-5-(4-ethylpiperazinyl)sulfonylphenyl)-4,5-dihydro-5-oxo-1,2,4-triazin-6-yl]ethyl}butyramide (which is represented by formula III), its preparation method, intermediates during preparation procedure, preparation method for such intermediates and a method for preparing vardenafil from the compound. In the method for preparing vardenafil, a chloro-sulfonation reaction carries out in the early stage of the preparation procedure.
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Page/Page column 6-7
(2011/08/08)
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- PROCESSES FOR THE PREPARATION OF VARDENAFIL
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The present invention provides processes for the preparation of vardenafil, its pharmaceutically acceptable salts, hydrates and intermediates.
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Page/Page column 15
(2011/02/24)
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- N-{1-Y3-(2-ETHOXY-5-(4-ETHYLPIPERAZINYL)BENZENESULFONYL)-4,5-DIHYDRO-5-OXO-1,2,4-TRIAZIN-6-YL¨ETHYL}BUTYRAMIDE, THE PREPARATION METHOD AND USE THEREOF
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Disclosed are N-{1-[3-(2-ethoxy-5-(4-ethylpiperazinyl)sulfonylphenyl)-4,5-dihydro-5-oxo-1,2,4-triazin-6-yl]ethyl}butyramide (which is represented by formula III), its preparation method, intermediates during preparation procedure, preparation method for such intermediates and a method for preparing vardenafil from the compound. In the method for preparing vardenafil, a chloro-sulfonation reaction carries out in the early stage of the preparation procedure.
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Page/Page column 8
(2010/10/01)
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- An improved synthetic route for preparative process of vardenafil
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A new, convergent synthetic route for the process optimization of vardenafil (Levitra), a potent and effective PDE5 inhibitor, is described. Key improved steps in the preparative process are that the chlorosulfonation reaction is at the beginning and the dehydration-cyclisation reaction is at a later stage so that the synthetic route has a better overall yield and simpler workup operations. The yield of vardenafil produced from this synthetic route is around 45% over seven steps with purity at 99.2% (HPLC).
- Mao, Yongjun,Tian, Guanghui,Liu, Zheng,Shen, Jingshan,Shen, Jingkang
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scheme or table
p. 1206 - 1208
(2010/04/22)
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- NEW AGENTS FOR THE TREATMENT OF THE LOW URINARY TRACT DYSFUNCTIONS
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The present invention relates to novel compounds that are derivatives of 5 -phosphodiesterase inhibitors that comprise in their formula a polysulfurated group and that are useful for treating dysfunctions of low urinary tract such as incontinence, benign prostatic hyperplasia and erectile dysfunction.
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Page/Page column 21
(2009/04/25)
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- Novel imidazotriazinones and the use thereof
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Novel imidazotrizinones of general formula (I), a method for the production and the pharmaceutical use thereof are disclosed.
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- 2-phenyl substituted imidazotriazinones as phosphodiesterase inhibitors
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The 2-phenyl-substituted imidazotriazinones having short, unbranched alkyl radicals in the 9-position are prepared from the corresponding 2-phenyl-imidazotriazinones by chlorosulphonation and subsequent reaction with the amines. The compounds inhibit cGMP-metabolizing phosphodiesterases and are suitable for use as active compounds in pharmaceuticals, for the treatment of cardiovascular and cerebrovascular disorders and/or disorders of the urogenital system, in particular for the treatment of erectile dysfunction.
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- Process for the preparation of sulphonamide-substituted imidazotriazinones
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The present invention relates to a process for the preparation of sulphonamide-substituted imidazotriazinones of the general formula (I) characterized in that compounds of the formula (II) are reacted with sulphuric acid and the products obtained are then reacted with thionyl chloride and converted in situ in an inert solvent using an amine into the compounds according to the invention and, if appropriate, reacted to give the corresponding salts, hydrates or N-oxides.
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- 2-Phenyl-substituited Imidazotriazinones as Phoshodiesterase Inhibitors
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2-(Sulfamoyl-substituted phenyl)-3H-imidazo (5,1-f) (1,2,4) triazin-4-ones (I) are new. Imidazotriazinones of formula (I) and their salts, N-oxides and isomeric forms are new: R1 = H or 1-4C alkyl; R2 = 1-4C straight chain alkyl; R3, R4 = H, 2-8C alkenyl, 1-8C alkoxy or 1-10C alkyl (optionally interrupted by O and/or substituted by a very wide range of specific groups); or R3 or R4 = NR20R21, adamantyl, 2,2-dimethyl-4-phenyl-1,3-dioxan-5-yl, sulfolanyl, hydroxy-sulfolanyl, 2-oxo-tetrahydrofuran-3-yl; or 3-8C cycloalkyl, 6-10C aryl or 5-7 membered heterocycle, all optionally substituted by specific groups; or NR3R4 = (a) optionally benzo-fused, saturated, partially unsaturated or unsaturated 5-7 membered heterocycle, optionally containing 1-3 of S, N, O and NR37 and optionally substituted by a very wide range of specific groups; or (b) a group of formula (i)-(iv); R20,R21 = H or 1-6C alkyl; R37 = H, OH, CHO, CF3, up to 4C acyl, up to 4C alkoxycarbonyl, 1-4C alkoxy, 1-6C alkyl (optionally substituted by specific groups) or -(CO)iE; i = 0 or 1; E = 3-7C cycloalkyl or benzyl; 6-10C aryl or 5- or 6-membered heteroaryl, both optionally substituted by specific groups ; or 5-methyl-1-oxo-2,1,3-oxadiazol-4-yl, N-methylpiperazino or morpholino; R5,R6 = H, 1-6C alkyl, OH or 1-6C alkoxy. The full definitions are given in the DEFINITIONS (Full Definitions) field. An Independent claim is included for the preparation of (I).
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- Imidazo[5,1-f][1,2,4]triazin-4(3H)-ones, a new class of potent PDE 5 inhibitors
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2-Aryl-substituted imidazo[5,1-f][1,2,4]triazin-4(3H)-ones represent a new class of potent cGMP-PDE 5 inhibitors that prove to be superior to other purine-isosteric inhibitors. Subnanomolar inhibitors of PDE 5 with activity in in vivo models for erectile dysfunction have been identified. BAY 38-9456 (Vardenafil-hydrochloride) has been selected for clinical studies in the indication of erectile dysfunction.
- Haning, Helmut,Niew?hner, Ulrich,Schenke, Thomas,Es-Sayed, Mazen,Schmidt, Gunter,Lampe, Thomas,Bischoff, Erwin
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p. 865 - 868
(2007/10/03)
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