Albany Molecular Research, Inc.

Merck Sharp + Dohme Corp.

Alcon Research, Ltd.

Knopp Biosciences, LLC

Novartis Ag

Mark Hadden

Alan John Henderson

Peter Guzzo

Matthew Surman

May Xiaowu Jiang

James Grabowski

Alexander Usyatinsky

Cheng Guo

Mark R Hellberg

Ravi P Nargund

Steven Armen Boyd

Shuwen He

Jian Liu

Iyassu Sebhat

George T Topalov

Scott S Harried

David A Mareska

Linus S Lin

Hwang-Hsing Chen

James S Hale

Charles A Flentge

Lynn Resnick

Bruce Sargent

Justin K Belardi

Christopher L Franklin

Tianying Jian

Andrew Rusinko

Allan James Goodman

Bryon Severns

Kai Zhang

Emily Freeman

Larry Yet

Peter H Dobbelaar

Charles Raymond Heap

Wenge Cui

Hélène Decornez

Megan Ruenz

Shuang Liu

Charles R Heap

Chuang Liu

Alan J Henderson

Hélène Y Decornez

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

Compounds represented by formula 1 can be potent and/or partially selective for the Kv7.2/7.3 heteromultimer. They may be useful in treating disorders related to seizures, pain, neurotransmitter release, etc.

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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

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

Mark Hadden