Astraea Therapeutics, LLC

Sri International

Nurulain Zaveri

Faming Jiang

Wan-Ru Chao

Dennis Mitsugu Yasuda

Lawrence Robert Toll

Ahlem Bensari

Michael Meyer

Nahid S Waleh

Cris M Olsen

Taline Khroyan

V Blair Journigan

Willma E Polgar

The present invention provides novel piperidinyl-containing nociceptin receptor ligand compounds and pharmaceutical compositions useful in the treatment of neurological diseases and conditions where such ligands mediate the negative effects of the condition. Such neurological diseases and conditions include acute and chronic pain, substance abuse/dependence, alcohol addiction, anxiety, depression, sleep disorders, gastrointestinal disorders, renal disorders, cardiovascular disorders and Parkinson's disease.

Piperidinyl nociceptin receptor compounds

Piperdinyl nociceptin receptor compounds

Provided herein are novel and selective high affinity &#x3b1;3&#x3b2;4 nicotinic acetycholine receptor ligands and pharmaceutical compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, drug addiction or pain using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of selectively antagonizing receptors such as, for example, the &#x3b1;3&#x3b2;4 nicotinic acetycholine receptor using the compounds and compositions disclosed herein.

Selective high affinity &#x3b1;3&#x3b2;4 nicotinic acetylcholine receptor antagonists

Nicotinic acetylcholine receptor modulators

Provided herein are novel and selective high affinity &#x3b1;3&#x3b2;4 nicotinic acetylcholine receptor ligands and pharmaceutical compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, drug addiction or pain using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods for modulating a nicotinic acetylcholine receptor (nAChR). In still other embodiments, provided herein are methods of selectively antagonizing receptors such as, for example, the &#x3b1;3&#x3b2;4 nicotinic acetylcholine receptor using the compounds and compositions disclosed herein.

The disclosure provides compounds capable of selectively or non-selectively modulating nicotinic acetylcholine receptors. The compounds, compositions, and methods described herein are useful, for example, in treating patients suffering from various medical conditions including pain, chemical addictions, Parkinson's disease, Alzheimer's disease, and neurodegenerative disorders. In one embodiment, the compounds comprise a 7- to 11-membered azabicyclo ring.

Compounds useful as chemotherapeutic, chemopreventive, and antiangiogenic agents are provided. The compounds are flavanoids, including flavanones, flavanols, and chalcones. The compounds have the structure of formula (I) wherein Rthrough Rand Rthrough Rare defined herein, and &#x3b1;, &#x3b2; and &#x3b3; are optional bonds, providing that when &#x3b1; is absent, &#x3b2; is present, and when &#x3b2; is absent, &#x3b1; is present. When &#x3b1; is present, preferred Rmoieties are selected from O, S, NH and CH, and when &#x3b1; is absent, preferred Rgroups are selected from OH, SH, NHand CH. When &#x3b3; is present, the preferred Rsubstituent is O, while when &#x3b3; is absent, the preferred Rsubstituent is OH. Pharmaceutical compositions are provided as well, as are methods of synthesis and use.

Flavanoids as chemotherapeutic, chemopreventive, and antiangiogenic agents

Compounds useful as chemotherapeutic, chemopreventive, and antiangiogenic agents are provided. The compounds are flavanoids, including flavanones, flavanols, and chalcones. The compounds have the structure of formula (I) wherein Rthrough Rand Rthrough Rare defined herein, and &#x3b1;, &#x3b2;, and &#x3b3; are optional bonds, providing that when &#x3b1; is absent, &#x3b2; is present, and when &#x3b2; is absent, &#x3b1; is present. When &#x3b1; is present, preferred Rmoieties are selected from O, S, NH and CH, and when &#x3b1; is absent, preferred Rgroups are selected from OH, SH, NHand CH. When &#x3b3; is present, the preferred Rsubstituent is O, while when &#x3b3; is absent, the preferred Rsubstituent is OH. Pharmaceutical compositions are provided as well, as are methods of synthesis and use.

Flavanoid compounds as chemotherapeutic, chemopreventive, and antiangiogenic agents

Novel compounds useful as chemotherapeutic and chemopreventive agents are provided. The compounds are analogs of polyphenol catechins that occur in green tea, such as epigallocatichin-3-gallate (EGCG), and have the structure of formula (I) wherein Rthrough Rare defined herein. Preferred Rmoieties are selected from O, S, NH and CH, and in exemplary compounds, Ris O and Ris a tri-substituted aroyloxy substituent, such as a 3,4,5-substituted benzoyloxy group. Pharmaceutical compositions are provided as well, as are methods of chemotherapy and chemoprevention.

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Saratoga, CA, United States of America

Nurulain Zaveri