92 patents
Utility
SUBSTITUTED PYRIDO[2,1-a]ISOQUINOLINES AS VMAT2 INHIBITORS
11 Jan 24
Nicole Harriott, Nicholas Pagano, Byron A. Boon
Filed: 9 Jun 23
Utility
Synthetic Methods for Preparation of 4-(2-CHLORO-4-METHOXY-5-METHYLPHENYL)-N-[(1S)-2-CYCLOPROPYL-1-(3-FLUORO-4-METHYLPHENYL)ETHYL]-5-METHYL-N-PROP-2-YNYL-1,3-THIAZOL-2-AMINE
14 Sep 23
The present disclosure relates to the fields of chemistry and medicine, more particularly to processes for making 4-(2-chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]-5-methyl-N-prop-2-ynyl-1,3-thiazol-2-amine (Compound 1), pharmaceutically acceptable salts, and crystalline forms thereof, for the treatment of congenital adrenal hyperplasia (CAH).
Andrew PALMER, Scott STIRN, Joel RADISSON, Christina Marie COSTA
Filed: 10 Jun 20
Utility
Treatment of congenital adrenal hyperplasia
22 Aug 23
CRF1 receptor antagonists have the potential to directly inhibit ACTH release in patients with CAH and thereby allow normalization of androgen production while using lower, more physiologic doses of hydrocortisone, and thus reducing treatment-associated side effects.
Dimitri E. Grigoriadis
Filed: 20 Oct 20
Utility
CRF1 Receptor Antagonist for the Treatment of Congenital Adrenal Hyperplasia
17 Aug 23
Provided are methods related to treating congenital adrenal hyperplasia in a subject in need thereof comprising administering to the subject a compound of Formula (I): [INSERT FORMULA] (I), or a pharmaceutically acceptable salt thereof.
Robert H. Farber, Jean L. Chan, Eiry Roberts, Gordon B. Cutler, JR., Arline Nakanishi, Anne Charlier, Gordon Raphael Loewen, Xiaoping Zhang, Nagdeep Giri, Scott Stirn, Brian Sayers, Graeme Taylor, Christina Marie Costa, Stacy Parks, Anthony D. Vickery, Kristie M. Downing, Kingsley Iyoha, Ayanda Ngwenya-Jones, Gurvinder Mehton
Filed: 9 Jun 21
Utility
Pharmaceutical Formulations for Treating Endometriosis, Uterine Fibroids, Polycystic Ovary Syndrome or Adenomyosis
17 Aug 23
The present disclosure relates to pharmaceutical compositions comprising a gonadotropin-releasing hormone (GnRH) antagonist and methods of preparing and using such compositions.
Jayanthy Jayanth, Kevin C. Spence, Gregory A. McClelland, Anna V. Stepanenko, Kristof Chwalisz, Charlotte D. Owens, James W. Thomas, Jane Castelli-Haley, Keith Gordon, Michael C. Snabes, Ahmed M. Soliman, Geoff Zhang, David Metzger, Yanxia Li, Tzuchi R. Ju, Xi Shao, Oscar Antunez Flores, Rita Jain, Juki Wing-Keung Ng, Janine D. North, Hannah Palac, Paul M. Peloso
Filed: 13 Feb 23
Utility
Substituted pyrido[2,1-a]isoquinolines as VMAT2 inhibitors
8 Aug 23
Nicole Harriott, Nicholas Pagano, Byron A. Boon
Filed: 12 Jan 23
Utility
Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
1 Aug 23
Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Willy Moree, Martin Rowbottom, Warren Wade, Liren Zhao, Richard Lowe, Nicole Smith, Neil Ashweek, Yun-Fei Zhu
Filed: 18 Dec 20
Utility
Synthetic Methods for Preparation of 4-(2-CHLORO-4-METHOXY-5-METHYLPHENYL)-N-[(1S)-2-CYCLOPROPYL-1-(3-FLUORO-4-METHYLPHENYL)ETHYL]-5-METHYL-N-PROP-2-YNYL-1,3-THIAZOL-2-AMINE
27 Jul 23
The present disclosure relates to the fields of chemistry and medicine, more particularly to processes for making 4-(2-chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]-5-methyl-N-prop-2-ynyl-1,3-thi-azol-2-amine (Compound 1), pharmaceutically acceptable salts, and crystalline forms thereof, for the treatment of congenital adrenal hyperplasia (CAH).
Andrew Palmer, Scott Stirn, Joel Radisson, Christina Marie Costa
Filed: 9 Jun 21
Utility
GPR52 Modulators and Methods of Use
27 Jul 23
Juan Pablo Cueva-Garcia, Neil J. Ashweek, Collin Regan
Filed: 21 Apr 21
Utility
VMAT2 Inhibitors and Methods of Use
25 May 23
This disclosure relates generally to VMAT2 inhibitor compounds, compositions, and methods related thereto.
Nicole Harriott, Nicholas Pagano, Byron A. Boon
Filed: 12 Jan 23
Utility
Methods for the administration of certain VMAT2 inhibitors
23 May 23
Provided are methods of administering a vesicular monoamine transport 2 (VMAT2) inhibitor chosen from valbenazine and (+)-α-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,1 1b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-ol, or a pharmaceutically acceptable salt and/or isotopic variant thereof, to a patient in need thereof wherein the patient is also being administered digoxin.
Christopher F. O'Brien, Haig P. Bozigian
Filed: 20 Oct 20
Utility
Muscarinic Receptor 4 Antagonists and Methods of Use
27 Apr 23
Nicole Harriott, Nicholas Pagano, Corinne Rose Ley
Filed: 3 Feb 21
Utility
Testosterone Containing Pharmaceutical Composition
2 Mar 23
We disclose a pharmaceutical composition adapted for oral delivery comprising native testosterone; a treatment regimen comprising administration of the composition(s); and methods and uses for the treatment of hormone related conditions such as hypogonadism in human male, female and transgender subjects.
Martin Whitaker, John Porter, Richard Ross, Stewart Jones, Elizabeth Cocks
Filed: 18 Jan 21
Utility
CRF Receptor Antagonists and Methods of Use
2 Mar 23
Neil J. ASHWEEK, John P. WILLIAMS, Lev Alexander ZEGELMAN, Christina Marie COSTA, Scott STIRN, Shawn BRANUM, Jackie LE, John Lloyd TUCKER, Brian M. COCHRAN, David KUCERA, Donald HETTINGER, Max A. MELLMER
Filed: 1 Dec 20
Utility
Muscarinic Receptor 4 Antagonists and Methods of Use
16 Feb 23
Nicholas Pagano, Nicole Harriott, Brian M. Cochran, Scott Stirn, Christina Marie Costa
Filed: 3 Dec 20
Utility
CRF Receptor Antagonists and Methods of Use
29 Dec 22
Compounds are provided herein, as well as related preparations, compositions and methods for treating diseases and/or disorders that would benefit from the same such as congenital adrenal hyperplasia (CAH).
Evan SMITH, Sha LUO, Gordon Raphael LOEWEN, Neil J. ASHWEEK, John P. WILLIAMS
Filed: 25 Sep 20
Utility
Processes for the Synthesis of Valbenazine
17 Nov 22
The present application relates to processes for making (2R,3R,11bR)-3-isobutyl-9,10-dimethoxy-2,3,4,6,7,11b -hexahydro-1H-pyrido[2,1-a]isoquinolin-2-yl (S)-2-amino-3-methylbutanoate di(4-methylbenzenesulfonate), which is an inhibitor of vesicular monoamine transporter 2 (VMAT2) useful in the treatment of hyperkinetic movement disorders such as tardive dyskinesia (TD).
John TUCKER, David KUCERA, Donald HETTINGER, Brian M. COCHRAN, Shawn BRANUM, Jackie LE, Kevin MCGEE
Filed: 11 Sep 20
Utility
Processes for the preparation of uracil derivatives
4 Oct 22
The present invention relates to processes and intermediates for preparing Gonadotropin-Releasing Hormone (GnRH) receptor antagonists of structure (VI); and stereoisomers and pharmaceutically acceptable salts thereof.
Donald J. Gallagher, Laszlo R. Treiber, Robert Michael Hughes, Onorato Campopiano, Peng Wang, Yuxin Zhao, Shine K. Chou, Michael Allen Ouellette, Donald Nicholas Hettinger
Filed: 10 Jan 20
Utility
Methods for the administration of certain VMAT2 inhibitors
13 Sep 22
Provided are methods of administering a vesicular monoamine transport 2 (VMAT2) inhibitor chosen from valbenazine and (+)-α-3-isobutyl-9,10-dimethoxy-1, 3,4, 6,7,11 b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-ol, or a pharmaceutically acceptable salt and/or isotopic variant thereof, to a patient in need thereof wherein the patient is a CYP2D6 poor metabolizer.
Christopher F. O'Brien, Haig P. Bozigian
Filed: 26 Oct 20
Utility
High dosage valbenazine formulation and compositions, methods, and kits related thereto
26 Apr 22
Solid pharmaceutical compositions with high drug loading are provided.
Richard Alexander Moore, Jr., Gregory A. McClelland, Christopher F. O'Brien
Filed: 19 Oct 20