- INHINITORS OF GLI1 AS THERAPEUTIC AGENTS
-
This disclosure relates to compounds, pharmaceutical compositions comprising them, and methods of using the compounds and compositions for treating diseases related to glioma- associated oncogene (Gli) expression. More particularly, this disclosure relate
- -
-
-
- 5-HT2C RECEPTOR AGONISTS AND COMPOSITIONS AND METHODS OF USE
-
Provided in some embodiments are compounds of Formula A, as defined herein, that modulate the activity of 5-HT2C receptor. Also provided in some embodiments are methods, such as, for weight management, inducing satiety, and decreasing food intake, and for
- -
-
-
- NAPTHOQUINONES, PRO-DRUGS, AND METHODS OF USE THEREOF
-
Provided herein are naphthoquinones compounds such as those with a hydrogen bond donating group of the formula (I): wherein: R1, R2, R3, R4, R5, and n are as defined herein. Also provided herein are pharmaceutical composition of the present compounds and methods of treatment using the compounds including their use in the treatment of cancer.
- -
-
-
- CARBAMATE DERIVATIVE COMPOUNDS, PROCESSES FOR PREPARING THEM AND THEIR USES
-
The present invention relates to a pharmaceutical composition for treating or preventing CNS disorders containing a carbamate derivative compound and/or pharmaceutically acceptable salt thereof as an active ingredient. Furthermore, the present invention relates to a method for treatment or prevention CNS disorders comprising administering a carbamate derivative compound in a pharmaceutically effective amount to a subject in need of treatment or prevention of CNS disorders.
- -
-
-
- Development of a new family of chiral auxiliaries
-
A new family of chiral auxiliaries designed on a conformationally restricted version of (-)-8-phenylmenthol has been developed. Both enantiomers are available from an inexpensive synthesis conducted on multigram scale. A first application has showed compa
- Gelat, Fabien,Richard, Vincent,Berger, Olivier,Montchamp, Jean-Luc
-
p. 1819 - 1821
(2015/04/27)
-
- Photoassisted synthesis of enantiopure alkaloid mimics possessing unprecedented polyheterocyclic cores
-
Enantiopure alkaloid mimics are synthesized via high yielding intramolecular cycloadditions of photogenerated azaxylylenes tethered to pyrroles, with further growth of molecular complexity via post-photochemical transformations of primary photoproducts. This expeditious access to structurally unprecedented polyheterocyclic cores is being developed in the context of diversity-oriented synthesis, as the modular design allows for rapid "pre-assembly" of diverse photoprecursors from simple building blocks/diversity inputs.
- Kumar, N.N. Bhuvan,Mukhina, Olga A.,Kutateladze, Andrei G.
-
p. 9608 - 9611
(2013/07/26)
-
- Rapid photoassisted access to N,O,S-polyheterocycles with benzoazocine and hydroquinoline cores: Intramolecular cycloadditions of photogenerated azaxylylenes
-
Ring the changes: A new photoassisted approach to give conformationally constrained N,O,S-polyheterocyclic scaffolds of unprecedented topologies was achieved by intramolecular [4+4] and [4+2] cycloadditions of photogenerated o-azaxylylenes (23 examples; see scheme). The precursors can be readily assembled by simple and high-yielding reactions, thus making this a powerful synthetic method amenable to high-throughput diversity-oriented synthesis.
- Mukhina, Olga A.,Bhuvan Kumar,Arisco, Teresa M.,Valiulin, Roman A.,Metzel, Greg A.,Kutateladze, Andrei G.
-
p. 9423 - 9428
(2011/11/06)
-
- Substituted Nitrogen Heterocycles and Synthesis and Uses Thereof
-
The invention relates to a nitrogen heterocycle compound of formula 1: Also disclosed are a method of synthesizing the compound and use of the compound for treating various diseases and conditions.
- -
-
Page/Page column 30-31
(2009/10/06)
-
- Synthesis and structure-activity relationships of N-substituted spiropiperidines as nociceptin receptor ligands
-
A series of N-substituted analogs based upon the spiropiperidine core of 1 was synthesized and exhibited high binding affinity to the nociceptin (NOP) receptor. The selectivities against other known opioid receptors were determined.
- Caldwell, John P.,Matasi, Julius J.,Zhang, Hongtao,Fawzi, Ahmad,Tulshian, Deen B.
-
p. 2281 - 2284
(2007/10/03)
-
- N-PHENYL-1,1,1-TRIFLUOROMETHANESULFONAMIDE HYDRAZONE DERIVATIVE COMPOUNDS AND THEIR USAGE IN CONTROLLING PARASITES
-
Novel N-phenyl-1,1,1-trifluoromethanesulfonamide compounds useful for controlling endo and/or ectoparasites in the environment are provided, together with methods of making the same, and methods of using the inventive compounds to treat parasite infestations in vivo and ex vivo.
- -
-
Page/Page column 41
(2008/06/13)
-
- Synthesis of indoles via 6π-electrocyclic ring closures of trienecarbamates
-
A new method for the preparation of indoles from readily available α-haloenones and α-(trialkylstannyl)enecarbamates is described. Following a Stille coupling, trienecarbamate 2 is electronically activated to undergo a facile 6π-electrocyclic ring closure
- Greshock, Thomas J.,Funk, Raymond L.
-
p. 4946 - 4947
(2007/10/03)
-
- 4-(2-Methyl-5,6,7,8-tetrahydro-quinolin-7-ylmethyl)-1,3-dihydro-imidazole-2-thione as specific alpha2B agonist and methods of using the same
-
The compound of the formula wherein the * indicates an asymmetric carbon, is specific to alpha2B adrenergic receptors in preference over alpha2A and alpha2C adrenergic receptors, and as such has no or only minimal cardivascular and/or sedatory activity. The compound is useful as medicament in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors.
- -
-
-
- 4-(substituted cycloalkylmethyl) imidazole-2-thiones, 4-(substituted cycloalkenylmethyl) imidazole-2-thiones, 4-(substituted cycloalkylmethyl) imidazol-2-ones and 4-(substituted cycloalkenylmethyl) imidazol-2-ones and related compounds
-
Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardivascular and/or sedatory activity. These compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors. Compounds of Formula 1 where X is O also have the advantageous property that they have no or only minimal cardivascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardivascular and/or sedatory activity.
- -
-
-
- A Convenient Synthesis of 7-Halo-1-indanones and 8-Halo-1-tetralones
-
A regioselective oxidation of N-indan-4-yl-acetamide or N-(5,6,7,8-tetrahydronaphthalen-1-yl)acetamide with potassium permanganate followed by acidic hydrolysis gave 7-aminoindan-1-one or 8-aminotetral-1-one in good yield. The amino ketones were converted to the corresponding 7-haloindanone or the 8-halotetralone. Another method to prepare 7-haloindan-1-ones was completed by a cyclization of 3-chloro-1-(2-halophenyl)propan-1-one under Friedel-Crafts conditions to produce the product in gram quantity.
- Nguyen, Phong,Corpuz, Evelyn,Heidelbaugh, Todd M.,Chow, Ken,Garst, Michael E.
-
p. 10195 - 10198
(2007/10/03)
-
- 4-SUBSTITUTED IMIDAZOLE-2-THIONES AND IMIDAZOL- 2-ONES AS AGONISTS OF THE ALPHA- 2B AND ALPHA-2C ADRENERGIC RECEPTORS
-
Compounds of Formula (I): where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardivascular and/or sedatory activity. These compounds of Formula (I) are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors. Compounds of Formula (I) where X is O also have the advantageous property that they have no or only minimal cardivascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardivascular and/or sedatory activity.
- -
-
-
