- Efforts towards a Noyori reduction of a 3-fluorpiperidin-4-one with dynamic kinetic resolution
-
A Noyori reduction of racemic 1-Boc-3-fluoropiperidin-4-one has been achieved under dynamic kinetic resolution conditions that results in a single cis enantiomer being obtained with both diastereo- and enantioselectivity > 90%. This medicinal chemistry building block can be generated on multi-gram scale using the developed conditions to a single enantiomer in a 60% yield after employing a crystallisation procedure.
- LePaih, Jacques,Goff, Dane A.,Singh, Rajinder,Shaw, Simon J.
-
-
- 6,7-DIHYDRO-5H-PYRROLO[3,4-B]PYRIDIN-5-ONE ALLOSTERIC MODULATORS OF THE M4 MUSCARINIC ACETYLCHOLINE RECEPTOR
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The present invention is directed to 6,7-dihydro-5H-pyrrolo[3,4-b]pyridine-5-one compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.
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Paragraph 0206
(2017/07/14)
-
- 1 -OXO-1,2-DIHYDROISOQUINOLIN-7-YL-(5-SUBSTITUTED-THIOPHEN-2-YL)-SULFONAMIDE COMPOUNDS, FORMULATIONS CONTAINING THOSE COMPOUNDS, AND THEIR USE AS AICARFT INHIBITORS IN THE TREATMENT OF CANCERS
-
1-Oxo-1,2-dihydroisoquinolin-7-yl-(5-substituted-thiophen-2-yl)-sulfonamide compounds, formulations containing those compounds, and their use as AICARFT inhibitors.
- -
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Page/Page column 36
(2016/06/28)
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- INHIBITORS OF RENAL OUTER MEDULLARY POTASSIUM CHANNEL
-
Disclosed are compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.
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Page/Page column 48; 49
(2016/09/22)
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- SPIRO[CYCLOBUTANE-1,3'-INDOLIN]-2'-ONE DERIVATIVES AS BROMODOMAIN INHIBITORS
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The present invention provides novel spiro[cyclobutane-1,3'-indolin]-2'- derivatives of formula (I) in which Cy R1, R2, R4, L and 'm' are have the meaning given in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula (I) are useful as bromodomain inhibitors in the treatment or prevention of diseases or disorders where bromodomain inhibition is desired.
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-
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- PYRAZOLO[1,5-A][1,3,5]TRIAZINE AND PYRAZOLO[1,5-A]PYRIMIDINE DERIVATIVES AS CDK INHIBITORS
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The present invention provides substituted pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives of formula (I), which are therapeutically useful, particularly as selective transcriptional CDK inhibitors including CDK7, CDK9, CDK12, CDK13 and CDK18, more particularly transcriptional CDK7 inhibitors wherein X, ring A, ring B, L1, L2, R1,R2, R3, R4, R6, m, n and p have the meanings given in the specification and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorder associated with selective transcriptional CDKs in a mammal. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives of formula (I) or a pharmaceutically acceptable salt thereof or a stereoisomer thereof.
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Page/Page column 50-51
(2016/09/26)
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- COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF MEK
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The present invention relates to compounds of formula I: in which n, R1, R2, R3a, R4 and R5 are defined in the Summary of the Invention; capable of inhibiting the activity of MEK. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of hyperproliferative diseases like cancer.
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-
-
- COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF MEK
-
The present invention relates to compounds of formula I in which n, R1, R2, R3a, R4 and R5 are defined in the Summary of the Invention; capable of inhibiting the activity of MEK. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of hyperproliferative diseases like cancer.
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- BIARYL COMPOUNDS USEFUL FOR THE TREATMENT OF HUMAN DISEASES IN ONCOLOGY, NEUROLOGY AND IMMUNOLOGY
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The present invention provides compounds and compositions thereof which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable characteristics for the same.
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Paragraph 0600
(2015/06/25)
-
- Tetraaza-cyclopenta[a]indenyl derivatives
-
The present invention provides compounds of Formula (I) as M1 receptor positive allosteric modulators for the treatment of diseases mediated by the muscarinic M1 mediator.
- -
-
Paragraph 0122-0124
(2015/01/18)
-
- Discovery of a novel class of imidazo[1,2-a ]pyridines with potent PDGFR activity and oral bioavailability
-
The in silico construction of a PDGFRβ kinase homology model and ensuing medicinal chemistry guided by molecular modeling, led to the identification of potent, small molecule inhibitors of PDGFR. Subsequent exploration of structure-activity relationships
- Hicken, Erik J.,Marmsater, Fred P.,Munson, Mark C.,Schlachter, Stephen T.,Robinson, John E.,Allen, Shelley,Burgess, Laurence E.,Delisle, Robert Kirk,Rizzi, James P.,Topalov, George T.,Zhao, Qian,Hicks, Julie M.,Kallan, Nicholas C.,Tarlton, Eugene,Allen, Andrew,Callejo, Michele,Cox, April,Rana, Sumeet,Klopfenstein, Nathalie,Woessner, Richard,Lyssikatos, Joseph P.
-
supporting information
p. 78 - 83
(2014/02/14)
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- PYRIMIDINE PYRAZOLYL DERIVATIVES
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The present invention provides compounds of Formula (I) for the treatment of cancer, rheumatoid arthritis and other diseases (I).
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Page/Page column 117
(2014/02/15)
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- TETRAAZA-CYCLOPENTA[A]INDENYL DERIVATIVES
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The present invention provides compounds of Formula (I) as M1 receptor positive allosteric modulators for the treatment of diseases mediated by the muscarinic M1 mediator.
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Page/Page column 106
(2015/01/09)
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- GPR 119 MODULATORS
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Compounds that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein- coupled receptor GPR119 in animals are described herein.
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-
-
- Enantioselective synthesis of cis -3-fluoropiperidin-4-ol, a Building block for medicinal chemistry
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The first enantioselective route to both enantiomers of cis-1-Boc-3-fluoropiperidin-4-ol, a highly prized building block for medicinal chemistry, is reported. An enantioselective fluorination is employed, taking advantage of the methodology reported by MacMillan, which uses a modified cinchona alkaloid catalyst. In studying the fluorination reaction, we have shown that the catalyst can be replaced by commercially available primary amines, including α-methylbenzylamine, with similar levels of enantioselectivity. The piperidinols are readily crystallized to obtain enantiopure material.
- Shaw, Simon J.,Goff, Dane A.,Boralsky, Luke A.,Irving, Mark,Singh, Rajinder
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p. 8892 - 8897
(2013/09/24)
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- 5-HT2B RECEPTOR ANTAGONISTS
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The present invention relates to novel fluorinated piperidine derivatives having antagonistic activity at the 5-HT2B receptor, pharmaceutical compositions comprising these compounds and their use as a medicine.
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-
Paragraph 0044; 0045
(2013/07/19)
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- HEPATITIS B ANTIVIRAL AGENTS
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The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.
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- BICYCLIC GPR119 MODULATORS
-
The present invention relates to compounds of Formula (I) that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions associated with the modulation of GPR119 receptor activity. The invention also relates to the process for preparation of the compounds, pharmaceutical compositions thereof. The invention further relates to methods o f treating, preventing and/or managing diseases, disorders syndromes or conditions associated with the modulation of GPR119 receptor by using either alone or in combinations of Formula (I)
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-
-
- 4- (5-CYANO-PYRAZOL-1-YL) -PIPERIDINE DERIVATIVES AS GPR 119 MODULATORS
-
Compounds that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein- coupled receptor GPR119 in animals are described herein.
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-
-
- 5-HT2B RECEPTOR ANTAGONISTS
-
The present invention relates to novel fluorinated piperidine derivatives having antagonistic activity at the 5-HT2B receptor, pharmaceutical compositions comprising these compounds and their use as a medicine in the treatment or prevention of pulmonary arterial hypertension, pulmonary fibrosis or irritable bowel syndrome.
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Page/Page column 10
(2012/03/26)
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- HETEROCYCLIC-SUBSTITUTED PYRROLOPYRIDINES AND PYRROLOPYRIMIDINES AS JAK INHIBITORS
-
The present invention provides heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines of Formula I: wherein X, Y, Z, L, A, R5, n, m, and r are defined above, as well as their compositions and methods of use, that modulate the activity
- -
-
-
- NOVEL HETEROCYCLYL COMPOUNDS
-
The invention is concerned with novel bicyclic compounds of formula (I), wherein n, m, p, A, L, R1, R2, R3, R4, R5, R6, R7, R7, R8, R9, and R10 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR2 receptor, CCR5 receptor and/or CCR3 receptor may be used, for example, in the prevention and/or treatment of inflammatory diseases, particularly peripheral arterial occlusive diseases or atherothrombosis.
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Page/Page column 26-27
(2011/05/03)
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- IMIDAZO-PYRAZOLES AS GPR119 INHIBITORS
-
Compounds of formula (I) wherein: X is (A) or (B); Y is O or a bond; R1 is -C(O)-O-R3 or R2 is hydrogen, cyano, C1-C6 alkyl, or C3-C6 cycloalkyl; R5 is hydrogen, cyano
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-
- DIAZEPAM DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTORS
-
The invention is concerned with novel bicyclic compounds of Formula (I), wherein n, m, p, A, L, R1, R2, R3, R4, R5, R6, R7, R7, R8, R9 and R10 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR2 receptor, CCR5 receptor and/or CCR3 receptor and can be used as medicaments.
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Page/Page column 61
(2011/05/06)
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- GPR 119 MODULATORS
-
Compounds of formula (I) that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.
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Page/Page column 39
(2011/04/24)
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- GPR 119 MODULATORS
-
Compounds of Formula (I) that modulate the activity of the G -protein-coupled receptor GPFM 19 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.
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Page/Page column 66
(2010/11/18)
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- THERAPEUTIC COMPOUNDS
-
The present invention relates to pyrazine substituted pyrrolopyridines which are inhibitors of JAK kinases (JAKl, JAK2, JAK3 and/or TYK2) and/or PDKl and are thus useful for the treatment of myeloproliferative disorders or cancer.
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Page/Page column 55
(2009/05/30)
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- N-LINKED HETEROCYCLIC RECEPTOR AGONISTS FOR THE TREATMENT OF DIABETES AND METABOLIC DISORDERS
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Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control.
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Page/Page column 73-74
(2009/03/07)
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- IMIDAZO[1,2-A]PYRIDINE COMPOUNDS AS RECEPTOR TYROSINE KINASE INHIBITORS
-
Compounds of Formula I: in which A, B, R1, R1a, R2, R3, R4, R5 R6, R7 and R8 have the meanings given in the specification, are receptor tyrosine inhibitors useful in the treatment of diseases mediated by class 3 and class 5 receptor tyrosine kinases. Particular compounds of this invention have also been found to be inhibitors of Pim-1.
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