Albany Molecular Research, Inc.

Merck Sharp + Dohme Corp.

Alcon Research, Ltd.

Harmony Biosciences, Inc.

Curia Global, Inc.

Alan John Henderson

Peter Guzzo

Mark Hadden

Matthew Surman

May Xiaowu Jiang

James Grabowski

Alexander Usyatinsky

Matthew L Isherwood

Cheng Guo

Animesh Ghosh

Mark R Hellberg

Ravi P Nargund

Shuwen He

He Zhao

Jian Liu

Iyassu Sebhat

Emily Elizabeth Freeman

Linus S Lin

Hwang-Hsing Chen

Bruce Sargent

Christopher L Franklin

Tianying Jian

Kassoum Nacro

Andrew Rusinko

Allan James Goodman

Bryon Severns

Larry Yet

Peter H Dobbelaar

Chong Yew Lee

Kai Xiang

Megan Ruenz

Matthew David Surman

Substituted pyridoindoles for incorporation in pharmaceutical compositions employed in the treatment of various diseases correspond to formula (I) wherein Ris H or optionally substituted alkyl; R, R, Rare each independently selected from H, &#x2014;O-alkyl, &#x2014;S-alkyl, alkyl, halo, &#x2014;CF, and &#x2014;CN; G is &#x2014;CRR&#x2014;NR&#x2014; or &#x2014;NR&#x2014;CRR; Ris H, optionally substituted alkyl, optionally substituted heterocycle, &#x2014;C(&#x2550;O)&#x2014;R, &#x2014;C(&#x2550;O)&#x2014;O&#x2014;R, or &#x2014;C(&#x2550;O)&#x2014;NRR; Rand Rare each optionally substituted alkyl or optionally substituted heterocycle; R, R, R, R, R, R, Rand Rare each independently selected from H or optionally substituted alkyl; Rand Rare each independently H or halogen; L is &#x2014;CH&#x2014;O&#x2014;, &#x2014;CHCH&#x2014;, &#x2014;CH&#x2550;CH&#x2014; or a bond; and B is aryl or heteroaryl or cycloalkyl; with the proviso that, when L is a direct bond, B cannot be unsubstituted heteroaryl or heteroaryl monosubstituted with fluorine.

(1-azinone)-substituted pyridoindoles

The present invention relates to benzofuro[3,2-c]pyridine and azepine analogs as serotonin sub-type 6 (5-HT) modulators, pharmaceutical compositions including these compounds, methods of preparation, and use thereof. These compounds are useful in the treatment of central nervous system disorders including obesity, metabolic syndrome, cognition, schizophrenia, attention deficit hyperactivity disorder, bipolar disorder, rare and orphan diseases, and sleep disorders. The subject compounds have the structure of formula (I) with the substituents being described herein.

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Substituted pyridoindoles for incorporation in pharmaceutical compositions employed in the treatment of various diseases correspond to formula (I) wherein Ris H or optionally substituted alkyl; R, R, Rare each independently selected from H, &#x2014;O-alkyl, &#x2014;S-alkyl, alkyl, halo, &#x2014;CF, and &#x2014;CN; G is &#x2014;CRR&#x2014;NR&#x2014; or &#x2014;NR&#x2014;CRR; R; is H, optionally substituted alkyl, optionally substituted heterocycle, &#x2014;C(&#x2550;O)&#x2014;R, &#x2014;C(&#x2550;O)&#x2014;O&#x2014;R, or &#x2014;C(&#x2550;O)&#x2014;NRR; Rand Rare each optionally substituted alkyl or optionally substituted heterocycle; R, R, R, R, R, R, Rand Rare each independently selected from H or optionally substituted alkyl; Rand Rare each independently H or halogen; L is &#x2014;CH&#x2014;O&#x2014;, &#x2014;CHCH&#x2014;, &#x2014;CH&#x2550;CH&#x2014; or a bond; and B is aryl or heteroaryl or cycloalkyl; with the proviso that, when L is a direct bond, B cannot be unsubstituted heteroaryl or heteroaryl monosubstituted with fluorine.

Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.

Azabicycloalkane-indole and azabicycloalkane-pyrrolo-pyridine MCH-1 antagonists, methods of making, and use thereof

MCH-1 receptor antagonists are disclosed having the general formula  These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.

Azinone-substituted azapolycycle MCH-1 antagonists, methods of making, and use thereof

The present invention relates to epiminocycloalkyl[b]indole derivatives as serotonin sub-type 6 (5-HT) modulators, pharmaceutical compositions including these compounds, and methods of preparation and use thereof. These compounds are useful in the treatment of central nervous system disorders including obesity, metabolic syndrome, cognition, and schizophrenia. The subject compounds have the structure of formula (I) with the substituents being described herein.

5-pyridinone substituted indazoles of the formula and methods of their use are presented.

5-pyridinone substituted indazoles

Various 5-substituted 1-substituted indazoles are described, as are pharmaceutical compositions containing these compounds and methods of treatment of diseases using these compounds. Other embodiments are also described.

Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.

Substituted imidazoles as bombesin receptor subtype-3 modulators

Methods for using 6-aminoimidazo[1,2-b]pyridazine analogs are disclosed herein to treat rho kinase-mediated diseases or rho kinase-mediated conditions, including controlling intraocular pressure and treating glaucoma, are disclosed. Ophthalmic pharmaceutical compositions useful in the treatment of eye diseases such as glaucoma, and additionally useful for controlling intraocular pressure, the compositions comprising an effective amount of 6-aminoimidazo[1,2-b]pyridazine analogs, are disclosed herein.

6-aminoimidazo[1,2-b]pyridazine analogs as rho kinase inhibitors for the treatment of rho kinase-mediated diseases and conditions

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Albany, NY, United States of America

Alan John Henderson