67191-53-1Relevant academic research and scientific papers
NOVEL DIHYDROPYRIDOISOQUINOLINONES AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS
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Paragraph 0312, (2016/11/14)
A compound according to Formula (I): wherein R1, LA, CyA, RA, R2, R3, and R4 are as described herein. The present invention relates to novel compounds according to Formula I that antagonize GPR84, a G-protein-coupled receptor that is involved in inflammatory conditions, and methods for the production of these novel compounds, pharmaceutical compositions comprising these compounds, and methods for the prevention and/or treatment of inflammatory conditions, pain, neuroinflammatory conditions, neurodegenerative conditions, infectious diseases, autoimmune diseases, endocrine and/or metabolic diseases, cardiovascular diseases, leukemia, and/or diseases involving impairment of immune cell functions by administering a compound of the invention.
NOVEL DIHYDROPYRIDOISOQUINOLINONES AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS
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Paragraph 00271, (2016/01/12)
A compound according to Formula I: wherein R1, LA, GA, R2a, R2b, R3, R4, R5, and R6 are as described herein. The present invention relates to novel compound
FSH RECEPTOR ANTAGONISTS
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Page/Page column 26-27, (2013/04/10)
The invention relates to FSH receptor antagonist according to general formula (I) or a pharmaceutically acceptable salt thereof and to a pharmaceutical composition containing the same. The compounds can be used for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, and for the treatment of uterine fibroids and other menstrual-related disorders
HETEROCYLIC COMPOUNDS AS ANTAGONISTS OF THE OREXIN RECEPTORS
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Page/Page column 20, (2011/06/19)
The present invention relates to a heterocyclic derivative according to formula (I) wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders or diseases influenced by modulation of orexins, such as sleep disorders.
N1,N3-Diacyl-3,4-dihydropyrimidin-2(1H)-ones: neutral acyl group transfer reagents
Singh, Kamaljit,Singh, Kawaljit
experimental part, p. 10395 - 10399 (2010/02/28)
Readily available N1,N3-diacyl-3,4-dihydropyrimidin-2(1H)-ones efficiently acylate ammonia, primary and secondary amines to furnish primary, secondary and tertiary amides in good to excellent yields. The wide applicability of the procedure is demonstrated
Potential cancer chemopreventive activity of simple isoquinolines, 1-benzylisoquinolines, and protoberberines
Cui, Wenhua,Iwasa, Kinuko,Tokuda, Harukuni,Kashihara, Akiko,Mitani, Yosuke,Hasegawa, Tomoko,Nishiyama, Yumi,Moriyasu, Masataka,Nishino, Hoyoku,Hanaoka, Miyoji,Mukai, Chisato,Takeda, Kazuyoshi
, p. 70 - 79 (2008/02/04)
Seventeen simple isoquinolines, 15 1-benzylisoquinolines, and 19 protoberberines were tested for their inhibitory activities against Epstein-Barr virus early antigen (EBV-EA) activation induced by 12-O-tetradecanoylphorbol- 13-acetate (TPA) in Raji cells. Among the tested alkaloids, the inhibitory activity of all 1-benzylisoquinolines and 11 protoberberines was higher than that of β-carotene. The 1-benzylisoquinolines 19, 21, 22, 29, and 34 and protoberberines 41, 47-49, 51, 52, and 55 showed potent inhibitory effects on EBV-EA induction (96-100% inhibition at 1 × 103 mol ratio/TPA). These alkaloids were more active than the naturally occurring alkaloids, 23, 25, 33, 53, and 54. In addition, fifteen simple isoquinolines, eighteen 1-benzylisoquinolines and eight protoberberines were evaluated with respect to their ability to scavenge 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radicals. Nine simple isoquinolines, ten 1-benzylisoquinolines, and four protoberberines were more potent than α-tocopherol, and four 1-benzylisoquinolines, 20 and 28-30, exhibited potent activities (SC50 4.5-5.8 μM). Their activities were higher than the naturally occurring alkaloids, 23, 25, and 33. Therefore, some of the isoquinoline alkaloids indicating the high activity on both assays may be potentially valuable cancer chemopreventive agents. Structure-activity relationships are discussed for both tests.
First Carbamates Conversion to Amides by Simple Alkyl Group Transfer from Trialkylalanes
El Kaim, Laurent,Grimaud, Laurence,Lee, Anabelle,Perroux, Yannick,Tirla, Cornelia
, p. 381 - 383 (2007/10/03)
(Equation presented) N-Monosubstituted carbamates are cleanly converted to amides under treatment with trialkylaluminum. This reaction involves an aluminum-assisted internal delivery of alkyl groups. It can be applied to new and mild protecting group strategies for alcohols.
Mapping the Melatonin Receptor. 4. Comparison of the Binding Affinities of a Series of Substituted Phenylalkyl Amides
Garratt, Peter J.,Travard, Sylvie,Vonhoff, Stefan,Tsotinis, Andrew,Sugden, David
, p. 1796 - 1805 (2007/10/03)
A series of 2-, 3-, and 4-substituted phenylalkyl amides were prepared as potential melatonin analogs in order to investigate the nature of the binding site of the melatonin receptor in chicken brain.The length of the alkyl chain was systematically varied
THE REACTION OF 1-ALKYLDIHYDROISOQUINOLINES WITH BENZYNE. AN UNEXPECTED ENTRY TO DIBENZINDOLIZINES.
Atanes, Nieves,Guitian, Enrique,Saa, Carlos,Castedo, Luis,Saa, Jose M.
, p. 817 - 820 (2007/10/02)
The reaction of 1-ethylidene-2-formyl-1,2,3,4-tetrahydroisoquinolines 4a and 4b, or 1-ethyl-3,4-dihydroisoquinolines 3a and 3b, with benzyne led, by a formal 3+2 cycloaddition, to dibenzindolizines 5a and 5b, respectively.Compound 5b was also synthesized
