81228-87-7Relevant academic research and scientific papers
Substituted Pyrrolidines and Methods of Use
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Paragraph 1645, (2018/04/20)
The invention discloses compounds of Formula (I) wherein R1, R2, R2A, R3, R3A, R4, and R5 are as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treating cystic fibrosis by administering a compound of the invention.
PYRROLOPYRIDINEAMINO DERIVATIVES AS MPS1 INHIBITORS
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Paragraph 0739, (2014/02/15)
The present invention relates to the use of certain pyrrolopyridineamino derivatives (hereinafter referred to as “PPA derivatives”), particularly 1H-pyrrolo[3,2-c]pyridine-6-amino derivatives, to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps kinase itself. In particular, the present invention relates to PPA derivatives for use as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of the PPA derivatives, and pharmaceutical compositions comprising them. Formula (I)
3-SUBSTITUTED-6-(PYRIDINYLMETHOXY)-PYRROLOPYRIDINE COMPOUNDS
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Page/Page column 27-28, (2012/06/16)
The invention provides certain 3-substituted-6-(pyridinylmethoxy)-pyrrolopyridine compounds, particularly compounds of formula I and pharmaceutical compositions thereof. The invention further provides methods of using a compound of formula I to treat Parkinsons disease Formula (I).
PYRROLOPYRIDINEAMINO DERIVATIVES AS MPS1 INHIBITORS
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Page/Page column 103, (2012/10/07)
The present invention relates to the use of certain pyrrolopyridineamino derivatives (hereinafter referred to as "PPA derivatives"), particularly 1H-pyrrolo[3,2-c]pyridine-6- amino derivatives, to inhibit the spindle checkpoint function of Monospindle 1 (Mps1 – also known as TTK) kinases either directly or indirectly via interaction with the Mps kinase itself. In particular, the present invention relates to PPA derivatives for use as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of the PPA derivatives, and pharmaceutical compositions comprising them. Formula (I)
NOVEL VINBLASTINE DERIVATIVES, THEIR PREPARATION, USE AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAID DERIVATIVES
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Page/Page column 42, (2009/12/05)
The invention provides vinblastine derivatives represented by the following formula 1 or their physiologically acceptable salts, their preparation, use and pharmaceutical compositions comprising the said derivatives. The said vinblastine derivatives show inhibiting activities against tumor cell lines and can be used as medicaments for treating malignant tumors.
C(10) ETHYL ESTER AND C(10) CYCLOPROPYL ESTER SUBSTITUTED TAXANES
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Page/Page column 47, (2009/12/27)
Taxanes having an ethyl ester or cyclopropyl ester substituent at C(10), a keto substituent at C(9), a hydroxy substituent at C(7), a thienyl substituent at C(3') and a cyclobutyloxycarbamate or cyclopentyloxycarbamate substituent at C(3'), pharmaceutical compositions comprising such taxanes, methods of treatment and administration, and methods of preparation of medicaments comprising the taxanes.
ARYLALKOXYL HEPATITIS C VIRUS PROTEASE INHIBITORS
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Page/Page column 53, (2008/06/13)
The present invention discloses compounds of Formula I or II, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering to the subject a pharmaceutical composition comprising a compound of the present invention.
Rationally designed 'dipeptoid' analogues of cholecystokinin (CCK): N-terminal structure-affinity relationships of α-methyl-tryptophan derivatives
Eden,Higginbottom,Hill,Horwell,Hunter,Martin,Pritchard,Rahman,Richardson,Roberts
, p. 37 - 45 (2007/10/02)
The structure-affinity relationships (SAR) between the N-terminii of a series of α-methyl-tryptophanylphenethylamide derivatives and the cholecystokinin (CCK) B receptor are discussed. A series of compounds with the general formula R-X-α-methyl-tryptophanylphenethylamide was prepared, where R is a cycloalkyl, a bicycloalkyl or a tricycloalkyl group and X is a urethane, thiourethane, amide, urea or a sulphinamide linking group. The CCK-B receptor binding affinities of these are discussed. The SAR form part of a systematic program for the rational design of 'dipeptoid' analogues of the neuropeptide CCK. Beginning with 1,1-dimethylpropyl (±)-[1-(1H-indol-3-ylmethyl)-1-methyl-2-oxo-2- [(2-phenylethyl)amino carbamate (IC50 = 4720 nM on CCK-B binding affinity) the N-terminal moiety was systematically changed for groups of varying size, shape and lipophilicity until the optimal N-terminal group was obtained and the favoured linking group chosen, resulting in the compound tricyclo[3.3.1.13,7)]dec-2-yl(R)-[(1H-indol-3-ylmethyl)-1-methyl- 2-oxo-2[(2-phenylethyl)amino]ethyl]carbamate with and IC50 = 32 nM on CCK-B receptor binding affinity.
Carbamate dihydropyridazinones, their preparation and therapeutic agents containing these compounds
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, (2008/06/13)
Novel 6-phenyl-4,5-dihydro-3(2H)-pyridazinones which are substituted in the p-position of the phenyl ring by a carbamate or thiocarbamate group, processes for their preparation, pharmaceutical formulations containing these compounds, and their use as drug
