Abstract: An object of the present invention is to provide a crystal of (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)-1-pyrrolidinyl)-2-propen-1-one, which is useful as an antitumor agent, the crystal being stable, excellent in oral absorbability, highly chemically pure, and suitable for mass production. The present invention provides a crystal of (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)-1-pyrrolidinyl)-2-propen-1-one that exhibits an X-ray powder diffraction spectrum containing at least three characteristic peaks at diffraction angles (2?±0.2°) selected from 9.5°, 14.3°, 16.7°, 19.1°, 20.8°, 21.9°, and 25.2°. The present invention also provides a crystal of (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)-1-pyrrolidinyl)-2-propen-1-one that exhibits an X-ray powder diffraction spectrum containing at least seven characteristic peaks at diffraction angles (2?±0.2°) selected from 13.5°, 17.9°, 19.5°, 20.
Abstract: Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (I) and (III): where R1, R2, R3, R3?, R4, R6a, R6a, R11a, and R11b are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, insomnia, anxiety, depression, traumatic brain injury (TBI), stress, and epilepsy.
Type:
Grant
Filed:
August 21, 2017
Date of Patent:
October 8, 2019
Assignee:
Sage Therapeutics, Inc.
Inventors:
Ravindra B. Upasani, Benny C. Askew, Boyd L. Harrison, Francesco G. Salituro, Albert J. Robichaud
Abstract: Bile acids and related compositions and methods of synthesis and use. More specifically, deoxycholic acid and related compositions, said compositions being free of all moieties of animal origin and free of pyrogenic moieties.
Type:
Grant
Filed:
May 23, 2018
Date of Patent:
October 8, 2019
Assignee:
ALLERGAN SALES, LLC
Inventors:
Robert M. Moriarty, Nathaniel E. David, Nadir Ahmeduddin Mahmood
Abstract: Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein , A, R1, R2, and R3 are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use, e.g., for treating a subject suffering from a disease or disorder described herein.
Type:
Grant
Filed:
July 26, 2017
Date of Patent:
October 1, 2019
Assignee:
Sage Therapeutics, Inc.
Inventors:
Albert J. Robichaud, Gabriel Martinez Botella, Francesco G. Salituro, Boyd L. Harrison
Abstract: The invention relates to compounds of formula (I): wherein R is ethyl, propyl or allyl, and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof. The compounds of formula (I) are useful as FXR agonists.
Abstract: Certain embodiments are directed to methods and compositions for preventing or treating bacterial infections. In certain embodiments the compositions comprise thioredoxin inhibitors, and/or thioredoxin-like inhibitors.
Type:
Grant
Filed:
July 15, 2014
Date of Patent:
September 3, 2019
Assignee:
THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM
Inventors:
Patrick Ketter, Bernard Arulanandam, M. Neal Guentzel
Abstract: The present invention discloses an application of an antidepressant compound in preparation of antidepressant drugs and antidepressant health-care foods, where the antidepressant compound has a structure represented by formula I. The antidepressant compound serves as the only active ingredient or one of active ingredients of antidepressant health-care foods. The antidepressant drug is a liquid preparation, a solid preparation, a spray, an aerosol, or the like. The antidepressant compound according to the present invention is applied in preparation of antidepressant drugs and antidepressant health-care foods, and has a chemical structure different from those of existing antidepressant drugs. The anti-depressant compound has significant antidepressant activities without obvious toxic and side effects, contributes to large-scale promotion and use on the market, and has broad application prospects.
Abstract: A method of obtaining conjugated estrogens from pregnant mare's urine by supercritical fluid extraction and the product thus obtained is disclosed.
Abstract: An anthraquinone compound of formula I (such as the compounds of formulae II to X) and processes for making the same are provided. Pharmaceutical compositions for use in the treatment of cancer, optionally in combination with an agent capable of reducing the level of oxygenation of a tumor, are also provided. Additionally, an option for combination with chemotherapeutic and radiotherapeutic modalities to enhance overall tumor cell kill is provided. Methods for the detection of cellular hypoxia, both in vivo and in vitro, are additionally provided.
Type:
Grant
Filed:
August 7, 2013
Date of Patent:
August 20, 2019
Assignee:
BIOSTATUS LIMITED
Inventors:
Stefan Ogrodzinski, Paul Smith, Stephanie McKeown, Laurence Patterson, Rachel Jane Errington
Abstract: Compounds useful for molecular imaging of cells expressing estrogen receptors are provided. Also provided are intermediates for making the compounds and methods of making the compounds using a modular convergent strategy. Further, methods of making the intermediates are described, as well as methods of diagnosing disease in a subject by using the compounds as imaging agents.
Abstract: The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof wherein R1 to R6 are as defined in the claims. The invention further relates to their use as inhibitors of 17?-HSD and in treatment or prevention of steroid hormone de-pendent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of the 17?-HSD1 enzyme and/or requiring the lowering of the endogenous estradiol concentration. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds or pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
June 25, 2014
Date of Patent:
August 13, 2019
Assignee:
FORENDO PHARMA LTD.
Inventors:
Maire Eloranta, Leena Hirvelä, Lauri Kangas, Pasi Koskimies, Risto Lammintausta, Mikko Unkila
Abstract: Provided are compositions comprising unequal mixtures of (R)-amisulpride and (S)-amisulpride, or pharmaceutically acceptable salts thereof, where the amount of (R)-amisulpride is greater than the amount of (S)-amisulpride, compositions and medicaments comprising the same used for the treatment of various diseases and disorders, and methods of using same for the treatment of various diseases and disorders, including, but not limited to, dosage regimens. In addition, provided are various formulations thereof, including, but not limited to, formulations employing polymorphs of enantiomeric amisulpride.
Type:
Grant
Filed:
December 4, 2018
Date of Patent:
August 6, 2019
Assignee:
Sunovion Pharmaceuticals Inc.
Inventors:
Seth Cabot Hopkins, Kenneth Stephen Koblan, John R. Snoonian, Harold Scott Wilkinson
Abstract: The present invention provides compounds of Formula (I) or Formula (II): pharmaceutical compositions comprising these compounds and methods of using these compounds to treat or prevent a disease or disorder mediated by FXR and/or TGR5.
Type:
Grant
Filed:
February 22, 2017
Date of Patent:
July 30, 2019
Assignee:
Enanta Pharmaceuticals, Inc.
Inventors:
Guoqiang Wang, Yat Sun Or, Jiang Long, Guoyou Xu, Peng Dai, Ruichao Shen, Xuechao Xing, Jing He
Abstract: Use of 5?-androstane-3?,5,6?-triol and analogs thereof in the preparation of a drug for the prophylaxis or treatment of an altitude sickness caused by hypobaric hypoxia is provided, so as to provide a new drug for the prophylaxis or treatment of an altitude sickness. Researches revealed that 5?-androstane-3?,5,6?-triol treatment can effectively reduce vasogenic edema of brain tissue of Macaca fascicularis caused by hypobaric hypoxia, reduce the increased cerebral water content, and protect from neuronal vacuolar degeneration caused by hypobaric hypoxia, therefore it can improve neurological dysfunctions caused by hypobaric hypoxia and is useful in prophylaxis or treatment of an altitude sickness.
Abstract: Methods of using 7?,11?-dimethyl-17?-hydroxy-4-estren-3-one bucyclate (I) and 7?,11?-dimethyl-17?-hydroxyestr-4-en-3-one 17-undecanoate (II) for various hormonal therapies, dosage forms comprising 7?,11?-dimethyl-17?-hydroxy-4-estren-3-one bucyclate and 7?,11?-dimethyl-17?-hydroxyestr-4-en-3-one 17-undecanoate, and processes for their preparation.
Type:
Grant
Filed:
February 7, 2011
Date of Patent:
July 16, 2019
Assignee:
The United States of America, as represented by the Secretary, Department of Health and Human Services
Abstract: The present invention provides compounds of Formula I: pharmaceutical compositions comprising these compounds and methods of using these compounds to treat or prevent a disease or disorder mediated by FXR and/or TGR5.
Type:
Grant
Filed:
February 22, 2017
Date of Patent:
June 18, 2019
Assignee:
ENANTA PHARMACEUTICALS, INC.
Inventors:
Yat Sun Or, Xuechao Xing, Guoqiang Wang, Ruichao Shen, Jing He
Abstract: The present invention provides compounds of Formula I, pharmaceutical compositions comprising these compounds and methods of using these compounds to treat or prevent a disease or disorder mediated by FXR and/or TGR5.
Type:
Grant
Filed:
February 22, 2017
Date of Patent:
June 18, 2019
Assignee:
ENANTA PHARMACEUTICALS, INC.
Inventors:
Yat Sun Or, Jing He, Guoqiang Wang, Xuechao Xing
Abstract: There is provided a method of treatment of hypersomnolence comprising administering the steroidal compound 3?-ethynyl-3?-hydroxy-5?-androstan-17-one oxime, or a pharmaceutically acceptable salt thereof, to a subject in need of such treatment.
Type:
Grant
Filed:
June 5, 2017
Date of Patent:
May 7, 2019
Assignee:
Umecrine Cognition AB
Inventors:
Torbjörn Bäckström, Magnus Doverskog, Maja Johansson, Pontus Wasling
Abstract: Anti-inflammatory and antiallergic compounds of the glucocorticosteroid series, according to formula (I) according to formula (I) defined herein are useful for treating diseases of the respiratory tract characterized by airway obstruction.
Abstract: The present invention provides tromethamine salt of (Z)-7-[3,5-Dihydroxy-2-((E)-3-hydroxy-5-phenyl-pent-1-enyl)-cyclopentyl]-hept-5-enoic acid in crystalline Form 1 and amorphous form. This compound is may also be referred to as “tromethamine salt of bimatoprost acid.” The invention crystalline form is useful for solid ocular implant or topical formulations, utilized in the treatment of various ocular conditions, such as, for example, ocular hypertension.
Type:
Grant
Filed:
June 27, 2014
Date of Patent:
April 30, 2019
Assignee:
ALLERGAN, INC.
Inventors:
Thomas K. Karami, Scott W. Smith, Fiona Dubas-Fisher, Adrian St. Clair Brown