- S1P1 AGONIST AND APPLICATION THEREOF
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The present invention relates to a class of tricyclic compounds and an application thereof as a sphingosine 1-phosphate type 1 (S1P1) receptor agonist. The invention specifically relates to a compound represented by formula (II), and a tautomer and pharmaceutically acceptable salt of same.
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Paragraph 0500-0503
(2021/10/02)
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- THIADIAZOLE MODULATORS OF S1P AND METHODS OF MAKING AND USING
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The invention is directed to compounds of the formula: wherein each of the variables are defined herein, as well as methods of making and using the compounds as agonists of S1P1 and/or S1P5 for instance treating an autoimmune disease.
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Paragraph 0168
(2017/01/26)
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- NITROGEN-CONTAINING HETEROCYCLIC COMPOUND
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The present invention provides a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity and useful as a medicament such as a prophylactic or therapeutic drug for Alzheimer's disease, schizophrenia, pain, sleep disorder, Parkinson's disease dementia, dementia with Lewy bodies and the like, and the like. The present invention relates to a compound represented by the formula (I) or a salt thereof. wherein each symbol is as described in the attached DESCRIPTION.
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Paragraph 0330
(2017/08/01)
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- Practical Synthesis of a S1P Receptor 1 Agonist via a Guareschi-Thorpe Reaction
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A practical synthesis of S1P receptor 1 agonist ACT-334441 (1) through late-stage convergent coupling of two key intermediates is described. The first intermediate is 2-cyclopentyl-6-methoxyisonicotinic acid whose skeleton was built from 1-cyclopentylethanone, ethyl oxalate, and cyanoacetate in a Guareschi-Thorpe reaction in 42% yield over five steps. The second, chiral intermediate, is a phenol ether derived from enantiomerically pure (R)-isopropylidene glycerol ((R)-solketal) and 3-ethyl-4-hydroxy-5-methylbenzonitrile in 71% yield in a one-pot reaction. The overall sequence entails 18 chemical steps with 10 isolated intermediates. All raw materials are cheap and readily available in bulk quantities, the reaction conditions match with standard pilot plant equipment, and the route reproducibly afforded 3-20 kg of 1 in excellent purity and yield for clinical studies.
- Schmidt, Gunther,Bolli, Martin H.,Lescop, Cyrille,Abele, Stefan
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p. 1637 - 1646
(2016/09/23)
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- Design and structural analysis of aromatic inhibitors of type II dehydroquinase from mycobacterium tuberculosis
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3-Dehydroquinase, the third enzyme in the shikimate pathway, is a potential target for drugs against tuberculosis. Whilst a number of potent inhibitors of the Mycobacterium tuberculosis enzyme based on a 3-dehydroquinate core have been identified, they generally show little or no in vivo activity, and were synthetically complex to prepare. This report describes studies to develop tractable and drug-like aromatic analogues of the most potent inhibitors. A range of carbon-carbon linked biaryl analogues were prepared to investigate the effect of hydrogen bond acceptor and donor patterns on inhibition. These exhibited inhibitory activity in the high-micromolar range. The addition of flexible linkers in the compounds led to the identification of more potent 3-nitrobenzylgallate- and 5-aminoiso-phthalate-based analogues.
- Howard, Nigel I.,Dias, Marcio V.B.,Peyrot, Fabienne,Chen, Liuhong,Schmidt, Marco F.,Blundell, Tom L.,Abell, Chris
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p. 116 - 133
(2015/04/14)
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- 2-METHOXY-PYRIDIN-4-YL-DERIVATIVES
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The invention relates to pyridine derivatives of Formula (I) wherein A, R1, R2, R3, and R4 are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
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- PYRIDIN-4-YL DERIVATIVES
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The invention relates to pyridine derivatives of Formula (I), wherein A, R1, R2, R3, and R4 are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
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- 2-METHOXY-PYRIDIN-4-YL DERIVATIVES
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The invention relates to pyridine derivatives of Formula (I) wherein A, R1, R2, R3, and R4 are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
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- PYRROLIDINE-FUSED THIADIAZINE DIOXIDE COMPOUNDS AS BACE 1NHIBITORS, COMPOSITIONS, AND THEIR USE
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In its many embodiments, the present invention provides provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, where in each of W, Z, R1H, R2, R3, R4, ring A, ring B, m, n, p, and- L1 - is as defined herein. The novel compounds of the invention have surprisingly been found to exhibit properties which are expected to render them advantageous as BACE inhibitors and/or for the treatment and prevention of various pathologies related there to. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including Alzheimer?s disease, are also disclosed
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Page/Page column 72
(2012/10/18)
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- PYRIDIN-4-YL DERIVATIVES
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The invention relates to pyridine derivatives of Formula (I), wherein A, R1, R2, R3, and R4 are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
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- PYRIDINE DERIVATIVES AS S1P1/EDG1 RECEPTOR MODULATORS
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The invention relates to novel pyridine derivatives of formula (D, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents. Formula (I) wherein A represents and the other substituents are as defined in the claims.
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Page/Page column 17
(2011/09/20)
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- AZAINDAZOLE COMPOUNDS AS CCR1 RECEPTOR ANTAGONISTS
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Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are methods of making and methods of using same.
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Page/Page column 176; 177
(2010/04/27)
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- Pyridin-4-yl derivatives as immunomodulating agents
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The invention relates to pyridine derivatives of Formula (I) wherein A, R1, R2, R3, R4, R5, and R6 are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
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Page/Page column 19
(2010/04/23)
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- PYRIDINE DERIVATIVES AS S1P1/EDG1 RECEPTOR MODULATORS
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The invention relates to novel pyridine derivatives of formula (D, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents. Formula (I) wherein A represents and the other substituants are as defined in the claims.
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Page/Page column 47-48
(2009/04/25)
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- PYRIDIN-4-YL DERIVATIVES AS IMMUNOMODULATING AGENTS
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The invention relates to pyridine derivatives of Formula (I) wherein A, R1, R2, R3, R4, R5, and R6 are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
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Page/Page column 47
(2008/06/13)
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- MGLUR5 MODULATORS II
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The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.
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Page/Page column 19
(2008/06/13)
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- mGluR5 modulators III
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The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.
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Page/Page column 13
(2008/06/13)
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- MGluR5 modulators IV
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The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.
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Page/Page column 11
(2008/06/13)
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- Substituted pyridyl compounds, herbicidal compositions and method of use
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Substituted pyridyl compounds, e.g. 2,6-dichloro-4(2-(2,2,2-trichloroethyl)oxiranyl) pyridine; herbicidal compositions containing such compounds and method for the control of undesired vegetation using these compositions.
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