- Inhibitors of nedd8-activating enzyme
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The invention relates to an administration unit comprising crystalline form I of {(1 S,2S,4R)-4-[(6-{[(1R,2S)-5-chloro-2methoxy-2,3-dihydro-1H-inden-1-yl]amino}pyrimidin-4-yl)oxy]-2-hydroxycyclopentyl}methyl sulfamate (I-216) hydrochloride salt and to a packaging comprising the administration unit according to the invention.
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Paragraph 0102
(2014/08/20)
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- INTERMEDIATE AND PROCESS FOR THE PREPARATION OF A SULFONAMIDE DERIVATIVE
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The invention relates to a crystalline form of 2-chloro-N-{2-[3-(2-{[(4'-hydroxybiphenyl-3- yl)methyl]amino}-2-oxoethyl)phenyl]-1,1-dimethylethyl}acetamide, a process for preparing the same and its use in the preparation of the ?2 agonist N-[(4'-hydroxybiphenyl-3- yl)methyl]-2-(3-{2-[((2R)-2-hydroxy-2-{4-hydroxy-3- [(methylsulfonyl)amino]phenyl}ethyl)amino]-2-methylpropyl} phenyl)acetamide which is useful in the treatment of respiratory diseases.
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Page/Page column 19; 20
(2013/03/26)
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- HETEROCYCLIC INHIBITORS OF GLUTAMINASE
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The invention relates to the heterocyclic compounds of Formula (I) as defined further herein, and pharmaceutical preparations thereof. The invention further relates to methods of treating cancer, immunological or neurological diseases using the heterocyclic compounds of the invention.
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Page/Page column 114
(2013/06/06)
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- COMPOUNDS FOR THE TREATMENT OF CNS DISORDERS
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The invention relates to novel cycloalkyl- or cycloalkenyl-substituted pyrazolopyrimidinones of formula (I), wherein ā is selected from the group A1 consisting of a C3-C8-cycloalkyl group or a C4-C8-cycloalkenyl group, whereby the members of C3-C8-cycloalkyl group being selected from the group of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptanyl and cyclooctanyl; and the members of the C4-C8-cycloalkenyl group, being selected from cyclobutenyl, cyclopentenyl, cyclohexenyl, cycloheptenyl, cyclooctenyl, cyclopentadienyl, cyclohexadienyl, cycloheptadienyl, cyclooctadienyl, cycloheptatrienyl, cyclooctathenyl, cyclooctatetraenyl. The new compounds shall be used for the manufacture of medicaments, in particular medicaments for improving perception, concentration, learning and/or memory in patients in need thereof. Chemically, the compounds are characterised as pyrazolopyrimidinones with a cycloalkyl-moiety directly bound to the 1 position of the pyrazolopyrimidinone and a second substituent in the 6 position which is bound via an optionally substituted methylene-bridge. Further aspects of the present invention refer to a process for the manufacture of the compounds and their use for producing medicaments.
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Page/Page column 41
(2012/05/20)
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- Enzymatic desymmetrization route to ethyl [3-(2-amino-2-methylpropyl) phenyl]acetate
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An efficient process to ethyl [3-(2-amino-2-methylpropyl)phenyl]acetate 6 has been developed. Key steps include a novel enzymatic desymmetrization of diester 2 and a Ritter reaction between alcohol 4 and chloroacetonitrile, followed by chemoselective deprotection with thiourea.
- De Koning, Pieter D.,Gladwell, Iain R.,Morrison, Natalie A.,Moses, Ian B.,Panesar, Maninder S.,Pettman, Alan J.,Thomson, Nicholas M.,Yazbeck, Daniel R.
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p. 871 - 875
(2012/06/18)
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- SUBSTITUTED-QUINOXALINE-TYPE BRIDGED-PIPERIDINE COMPOUNDS AND THE USES THEREOF
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The invention relates to Substituted-Quinoxaline-Type Bridged-Piperidine Compounds, compositions comprising an effective amount of a Substituted-Quinoxaline- Type Bridged-Piperidine Compound and methods to treat or prevent a condition, such as pain, compr
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Page/Page column 51; 88
(2010/04/03)
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- Inhalation by design: Novel ultra-long-acting β2- adrenoreceptor agonists for inhaled once-daily treatment of asthma and chronic obstructive pulmonary disease that utilize a sulfonamide agonist headgroup
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A novel series of potent and selective sulfonamide derived β2-adrenoreceptor agonists are described that exhibit potential as inhaled ultra-long-acting bronchodilators for the treatment of asthma and chronic obstructive pulmonary disease. Analogues from this series mediate very long-lasting smooth muscle relaxation in guinea pig tracheal strips. The sulfonamide agonist headgroup confers high levels of intrinsic crystallinity that could relate to the acidic sulfonamide motif supporting a zwitterionic form in the solid state. Optimization of pharmacokinetic properties was achieved through targeted introduction of a phenolic moiety to support rapid phase II clearance, thereby minimizing systemic exposure following inhalation and reducing systemically mediated adverse events. Compound 38 (PF-610355) is identified as a clinical candidate from this series, with in vivo duration of action studies confirming its potential for once-daily use in humans. Compound 38 is currently in advanced phase II clinical studies.
- Glossop, Paul A.,Lane, Charlotte A. L.,Price, David A.,Bunnage, Mark E.,Lewthwaite, Russell A.,James, Kim,Brown, Alan D.,Yeadon, Michael,Perros-Huguet, Christelle,Trevethick, Michael A.,Clarke, Nicholas P.,Webster, Robert,Jones, Rhys M.,Burrows, Jane L.,Feeder, Neil,Taylor, Stefan C. J.,Spence, Fiona J.
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experimental part
p. 6640 - 6652
(2010/11/19)
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- PROCESS FOR THE PREPARATION OF SULFONAMIDE DERIVATIVES
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The invention relates to a process for the preparation of compounds of formula (I) wherein Q1 is a group selected from formulae (II and (III) and a group *-NR6 -Q2-A or, if appropriate, their pharmaceutically acceptable sa
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Page/Page column 22
(2010/11/25)
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- FORMAMIDE DERIVATIVES USEFUL AS ADRENOCEPTOR
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The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
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Page/Page column 47-48; 81-82
(2008/06/13)
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- Sulfonamide derivatives for the treatment of diseases
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The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in
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Page/Page column 16
(2008/06/13)
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- Quinolinone derivatives, pharmaceutical compositions containing them and their use
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The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in
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Page/Page column 26
(2008/06/13)
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- Compounds for the treatment of diseases
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The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
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Page/Page column 21; 22
(2008/06/13)
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- Sulfonamide derivatives for the treatment of diseases
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The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
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Page/Page column 21
(2010/02/13)
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- COMPOUNDS HAVING BETA-AGONIST ACTIVITY
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The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
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Page/Page column 68
(2010/02/14)
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- COMPOUNDS FOR THE TREATMENT OF DISEASES
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The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in
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Page/Page column 48
(2010/02/14)
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