Nitrogen Containing Hetero Ring Patents (Class 514/176)
  • Patent number: 10377790
    Abstract: Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (I): and pharmaceutical compositions thereof. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, tinnitus, and status epilepticus.
    Type: Grant
    Filed: April 29, 2016
    Date of Patent: August 13, 2019
    Assignee: Sage Therapeutics, Inc.
    Inventors: Gabriel Martinez Botella, Boyd L. Harrison, Albert Jean Robichaud, Francesco G. Salituro, Richard Thomas Beresis
  • Patent number: 10323061
    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
  • Patent number: 10098896
    Abstract: Described are steroidal C-17 benzoazoles, pyrimidinoazoles (azabenzoazoles) and diazines. Methods for their synthesis are also described, which include methods having a step of nucleophilic vinylic “addition-elimination” substitution reaction of 3?-acetoxy-17-chloro-16-formylandrosta-5,16-diene or analogs thereof and benzoazole or pyrimidinoazole nucleophiles and methods having a palladium catalyzed cross-coupling reaction of 17-iodoandrosta-5,16-dien-3?-ol or analogs thereof with tributylstannyl diazines. The compounds are potent inhibitors of human CYP17 enzyme as well as potent antagonists of both wild type and mutant androgen receptors (AR). The compounds are useful for the treatment of human prostate cancer.
    Type: Grant
    Filed: May 19, 2016
    Date of Patent: October 16, 2018
    Assignee: UNIVERSITY OF MARYLAND BALTIMORE
    Inventors: Angela Brodie, Vincent C. O. Njar
  • Patent number: 10092577
    Abstract: The invention relates to a composition for preventing bearing loss in subject or for at least partially restoring bearing in a subject having a reduced auditory function. The composition comprises at least one sterol compound inducing neuron differentiation. Said composition is placed in contact with at least part of the cochlea.
    Type: Grant
    Filed: July 28, 2015
    Date of Patent: October 9, 2018
    Assignee: Affichem
    Inventors: Philippe De Medina, Michaël Paillasse, Mats Ulfendahl
  • Patent number: 10045999
    Abstract: The invention relates to the use of an anabolic amino acid derivative stimulus acting in combination with vitamin D for the manufacture of a medicament or nutritional composition for the prevention and/or treatment of a loss of any one of muscle mass, muscle strength, muscle function, and physical function, or any combination thereof, in a mammal.
    Type: Grant
    Filed: June 25, 2015
    Date of Patent: August 14, 2018
    Assignee: N. V. Nutricia
    Inventors: Marion-Eve Adeline Jourdan, Yvette Charlotte Luiking, George Verlaan, Sovianne Ter Borg
  • Patent number: 10045998
    Abstract: Combinations of (3?)-17-(pyridin-3-yl)androsta-5,16-dien-3-yl acetate (Abiraterone acetate) with acidic substances such as citric acid, ascorbic acid, methyl-4-hydroxy benzoate, saccharin, vanillic acid, adipic acid, maleic acid, malic acid, tartaric acid are useful as pharmaceutical preparations and show improved properties such as aqueous solubility and dissolution kinetics, especially in the form of cocrystals or their combination with a suitable acid.
    Type: Grant
    Filed: December 9, 2014
    Date of Patent: August 14, 2018
    Assignee: BASF SE
    Inventors: Tiziana Chiodo, Beate Salvador, Marcus Vossen, Andreas Hafner, Tobias Hintermann, Martin Szelagiewicz, Fritz Blatter, Martin Viertelhaus, Walter Weishaar
  • Patent number: 10023606
    Abstract: Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (I): and pharmaceutical compositions thereof. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, tinnitus, status epilepticus.
    Type: Grant
    Filed: September 22, 2016
    Date of Patent: July 17, 2018
    Assignee: Sage Therapeutics, Inc.
    Inventors: Gabriel Martinez Botella, Boyd L. Harrison, Albert Jean Robichaud, Francesco G. Salituro, Richard Thomas Beresis
  • Patent number: 10000527
    Abstract: The present invention discloses a novel bile acid derivatives having substituted nitrogen functionality at C-11 and process for synthesis thereof. These C-11 substituted bile acid derivatives shows anticancer and antimycobacterial activity.
    Type: Grant
    Filed: November 24, 2014
    Date of Patent: June 19, 2018
    Assignee: Council of Scientific and Industrial Research
    Inventors: Pore Vandana Sudhir, Jaisingh Manohar Divse, Chaitanya Rajendra Charolkar
  • Patent number: 9987292
    Abstract: The invention provides a method of inhibiting vascular hyperpermeability in an animal in need thereof. The method comprises administering a vascular-hyperpermeability-inhibiting amount of a danazol compound to the animal. The invention also provides a method of modulating the cytoskeleton of an endothelial cell in an animal. The method comprises administering an effective amount of a danazol compound to the animal.
    Type: Grant
    Filed: December 2, 2015
    Date of Patent: June 5, 2018
    Assignee: Ampio Pharmaceuticals, Inc.
    Inventor: David Bar-Or
  • Patent number: 9884067
    Abstract: The present disclosure provides the design and synthesis of novel steroidal compounds that cause down-regulation of the androgen receptor (AR), both full length and splice variant. The compounds are potential agents for the treatment of all forms of prostate cancer and other diseases that depend on functional AR.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: February 6, 2018
    Assignees: University of Maryland, Baltimore, University of Maryland Eastern Shore, Thomas Jefferson University
    Inventors: Vincent C. O. Njar, Lalji K. Gediya, Puranik Purushottamachar, Abhijit Godbole, Andrew Kwegyir-Afful, Tadas Vasaitis
  • Patent number: 9850272
    Abstract: The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof wherein R2, R3, R4, R7 and R8 are as defined in the claims. The invention further relates to their use as inhibitors of 17?-HSD1 and in treatment or prevention of steroid hormone dependent 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: December 26, 2017
    Assignee: FORENDO PHARMA LTD.
    Inventors: Leena Hirvelä, Lauri Kangas, Pasi Koskimies, Risto Lammintausta, Mikko Unkila
  • Patent number: 9845337
    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.
    Type: Grant
    Filed: November 10, 2014
    Date of Patent: December 19, 2017
    Assignee: CHIESI FARMACEUTICI S.P.A.
    Inventors: Eleonora Ghidini, Andrea Rizzi
  • Patent number: 9809597
    Abstract: Compositions and methods for modulating innate and adaptive immunity and for use in immunotherapy are disclosed. In particular, the invention relates to novel ganciclovir derivatives and methods of using them for the treatment of immune-related disorders, including inflammation, autoimmunity, and infections, and neurological disorders, and cancer.
    Type: Grant
    Filed: August 19, 2016
    Date of Patent: November 7, 2017
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Ritwik Burai, Hilal Lashuel, Vidhu Mathur, Anton Wyss-Coray
  • Patent number: 9714266
    Abstract: The invention relates to AKR1C3 inhibitors of formula (I) and to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of bleeding disorders and endometriosis.
    Type: Grant
    Filed: February 18, 2014
    Date of Patent: July 25, 2017
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Ulrich Bothe, Matthias Busemann, Naomi Barak, Andrea Rotgeri, Oliver Martin Fischer, Tobias Marquardt
  • Patent number: 9663551
    Abstract: Novel solanidine-derived compounds, the synthesis method thereof and the uses of same in the fields of phytosanitary protection and health. In particular, the novel compounds have toxic and/or repellent properties in relation to aphids, as well as other properties.
    Type: Grant
    Filed: July 21, 2014
    Date of Patent: May 30, 2017
    Assignees: UNIVERSITÉ DE PICARDIE JULES VERNE, SEMENCES INNOVATION PROTECTION RECHERCHE ET ENVIRONMENT
    Inventors: Rémi Beaulieu, Jacques Attoumbre, Virginie Gobert-Deveaux, Eric Grand, Imane Stasik, José Kovensky, Philippe Giordanengo
  • Patent number: 9663549
    Abstract: The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof wherein R2 to R7 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 afore-mentioned compounds or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: June 25, 2014
    Date of Patent: May 30, 2017
    Assignee: FORENDO PHARMA LTD.
    Inventors: Maire Eloranta, Leena Hirvelä, Lauri Kangas, Pasi Koskimies, Risto Lammintausta, Mikko Unkila
  • Patent number: 9623034
    Abstract: The present disclosure relates to pharmaceutically acceptable complex formulae comprising complexes of Abiraterone acetate and pharmaceutically acceptable excipients, process for the preparation thereof and pharmaceutical compositions containing them. The complex formulae of the present disclosure have improved physicochemical properties which results in reduced food effect which allows significant dose reduction and the abandoning of the requirement of taking the drug on an empty stomach.
    Type: Grant
    Filed: February 9, 2016
    Date of Patent: April 18, 2017
    Assignee: Druggability Technologies IP Holdco Limited
    Inventors: Réka Angi, Tamás Jordán, Orsolya Basa-Dénes, Tamás Solymosi, Zsolt Ötvös, Hristos Glavinas, Genovéva Filipcsei
  • Patent number: 9610294
    Abstract: The present invention provides methods and compositions for the treatment of fluid accumulation in and/or under the retina.
    Type: Grant
    Filed: January 2, 2015
    Date of Patent: April 4, 2017
    Assignees: INSERM (INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE), UNIVERSITE PARIS DESCARTES, ASSISTANCE PUBLIQUE HOPITAUX DE PARIS
    Inventors: Francine Behar-Cohen, Nicolette Farman, Frederic Jaisser
  • Patent number: 9433627
    Abstract: Disclosed herein are compositions comprising an amide related to a prostaglandin and a biogenic amine. Other aspects relate to certain chemical compounds, pharmaceutical compositions, and methods of treating glaucoma.
    Type: Grant
    Filed: December 20, 2013
    Date of Patent: September 6, 2016
    Assignee: Allergan, Inc.
    Inventors: David F. Woodward, Robert M. Burk
  • Patent number: 9387216
    Abstract: Described herein are methods and compositions for the treatment of prostate cancer in a subject in need thereof. The prostate cancer may be a castration resistant and an androgen receptor antagonist-resistant prostate cancer. The methods may comprise administering to the subject a CYP17-lyase inhibitor of Formula II.
    Type: Grant
    Filed: July 6, 2015
    Date of Patent: July 12, 2016
    Assignees: Tokai Pharmaceuticals, Inc., University of Washington, University of Maryland, Baltimore
    Inventors: Vincent C. O. Njar, Amina Zoubeidi, Karen Ferrante, Eva Corey, Douglas B. Jacoby
  • Patent number: 9365611
    Abstract: Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (I): and pharmaceutical compositions thereof. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, tinnitus, and status epilepticus.
    Type: Grant
    Filed: April 17, 2014
    Date of Patent: June 14, 2016
    Assignee: SAGE THERAPEUTICS, INC.
    Inventors: Gabriel Martinez Botella, Boyd L. Harrison, Albert Jean Robichaud, Francesco G. Salituro, Richard Thomas Beresis
  • Patent number: 9351979
    Abstract: The invention provides a method of inhibiting vascular hyperpermeability in an animal in need thereof. The method comprises administering a vascular-hyperpermeability-inhibiting amount of a danazol compound to the animal. The method comprises administering an effective amount of a danazol compound to the animal accounting for the body fat content of the animal. The invention also provides a method of modulating the cytoskeleton of an endothelial cell in an animal.
    Type: Grant
    Filed: December 19, 2013
    Date of Patent: May 31, 2016
    Assignee: Ampio Pharmaceuticals, Inc.
    Inventor: David Bar-Or
  • Patent number: 9353144
    Abstract: The present disclosure relates to a novel vascular leakage inhibitor. The novel vascular leakage inhibitor of the present invention inhibits the apoptosis of vascular endothelial cells, inhibits the formation of actin stress fibers induced by VEGF, and enhances the cortical actin ring structure, thereby inhibiting vascular leakage. Accordingly, the vascular leakage inhibitor of the present invention can prevent or treat various diseases caused by vascular leakage. Since the vascular leakage inhibitor of the present invention is synthesized from commercially available or easily synthesizable pregnenolones, it has remarkably superior feasibility of commercial synthesis.
    Type: Grant
    Filed: December 28, 2012
    Date of Patent: May 31, 2016
    Assignee: INDUSTRY-ACADEMIC COOPERATION FOUNDATION, YONSEI UNIVERSITY
    Inventors: Young-Gune Kwon, Young-Ger Suh
  • Patent number: 9295731
    Abstract: Base-labile crosslinkers, base-labile conjugates comprising such crosslinkers, methods of their synthesis and use are disclosed.
    Type: Grant
    Filed: April 1, 2013
    Date of Patent: March 29, 2016
    Inventor: Mark Quang Nguyen
  • Patent number: 9295679
    Abstract: Prodrugs of steroidal C-17 benzoazoles, pyrimidinoazoles (az-abenzoazoles) and diazines. Methods of synthesis are also described, whereby a prodrug group is substituted for a functional group at A ring portion of the ABC ring structure of the steroid. Suitable pro-drug groups include amino acid groups, succinate groups, phosphate groups, or sulfamate groups. The prodrugs of the disclosed compounds allow for improved oral bioavailability of the compounds that are inhibitors of human CYP 17 enzyme as well as potent antagonists of both wild type and mutant androgen receptors (AR). The compounds and the corresponding prodrugs are useful for the treatment of conditions such as human prostate cancer, breast cancer, and prostate hyperplasia.
    Type: Grant
    Filed: March 2, 2015
    Date of Patent: March 29, 2016
    Assignee: University of Maryland, Baltimore
    Inventors: Vincent Njar, Angela Brodie, Lalji K. Gediya
  • Patent number: 9260473
    Abstract: Bivalent multifunctional A? oligomerization inhibitors (BMAOIs) that target multiple risk factors involved in Alzheimer's disease are provided. The BMAOIs are useful for the treatment and/or prevention of Alzheimer's disease, as well as for diagnostic imaging of A? plaques in brain tissue. The BMAOIs comprise i) an A? oligomer (ApO)-inhibitor moiety which may have antioxidant activity (e.g. curcumin, curcumin derivatives, curcumin hybrids, resveratrol, etc.); ii) a cell membrane/lipid raft (CM/LR) anchoring moiety (e.g. cholesterol, cholesterylamine, a steroid, etc.); and iii) a spacer or linker moiety that stably links i) and ii) together.
    Type: Grant
    Filed: July 14, 2011
    Date of Patent: February 16, 2016
    Assignee: Virginia Commonwealth University
    Inventors: Shujin Zhang, Tai Liang Guo
  • Patent number: 9255118
    Abstract: Photosensitive compounds for use in a method of treating a disease or condition are described. The photosensitive compounds have the formula R—Y, wherein R is a ruthenium complex and Y is at least one sulphur-containing photoreleasable group, and the compounds comprise at least one ruthenium-sulphur bond; or a pharmaceutically acceptable salt, solvate, ester or amide, such that upon influence of visible or near infra-red light (400-1400 nm) in vivo, said at least one ruthenium-sulphur bond is broken, thereby generating a pharmacologically active compound.
    Type: Grant
    Filed: October 18, 2011
    Date of Patent: February 9, 2016
    Assignee: UNIVERSITEIT LEIDEN
    Inventor: Sylvestre Bonnet
  • Patent number: 9096639
    Abstract: The invention relates to 17-hydroxy-13-methyl-17-pentafluoroethyl-11-acyloxyalkylenephenyldodecahydrocyclopenta[a]phenanthren-3-one derivatives of the formula I with progesterone-antagonizing action and to processes for preparation thereof, to use thereof for treatment and/or prophylaxis of disorders and to the use thereof for production of medicaments for treatment and/or prophylaxis of disorders, especially of fibroids of the uterus (myomas, uterine leiomyomas), endometriosis, heavy menstrual bleeds, meningiomas, hormone-dependent breast cancers and complaints associated with the menopause, or for fertility control and emergency contraception.
    Type: Grant
    Filed: July 7, 2010
    Date of Patent: August 4, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Ulrich Klar, Wolfgang Schwede, Carsten Moller, Andrea Rotgeri, Ursula Krenz
  • Publication number: 20150139905
    Abstract: The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.
    Type: Application
    Filed: October 9, 2014
    Publication date: May 21, 2015
    Inventors: Dinesh Chimmanamada, Weiwen Ying
  • Patent number: 9034857
    Abstract: Provided are methods and compositions for reducing superoxide anions such that a prophylactic or therapeutic effect against conditions associated with excess oxidative stress achieved. The compositions and methods provide for reducing inflammation and for enhancing lifespan of eukaryotic organisms. A screen for identifying compounds that can be used in these methods is also provided.
    Type: Grant
    Filed: March 24, 2011
    Date of Patent: May 19, 2015
    Assignees: Health Research, Inc., STC.UNM
    Inventors: William C. Burhans, Catherine E. Prudom Gineste, Christopher P. Allen, Oleg Ursu, Anna Waller, Larry A. Sklar
  • Publication number: 20150132295
    Abstract: This document provides methods and materials related to genetic variations associated with endometriosis. For example, this document provides methods for using such genetic variations to assess risk of, or susceptibility of developing or diagnosing endometriosis.
    Type: Application
    Filed: November 11, 2014
    Publication date: May 14, 2015
    Inventors: ELI HATCHWELL, PEGGY S. EIS
  • Publication number: 20150133415
    Abstract: Compositions, and methods of using such compositions, useful for placement, for example injection, into the interior of human or animal eyes are provided. Such compositions include a therapeutic component, such as one or more corticosteroids, a biocompatible polymeric component, and a solvent component. The composition is in a fluid form before placement in the interior of an eye, and becomes less fluid after the composition is placed in the eye to form an extended or delayed release drug delivery element or system. The drug delivery element is formed by the dissipation of the solvent from the composition when the composition is placed in the interior of an eye. One example of a composition includes triamcinolone acetonide as a therapeutic agent. A method of treating an ophthalmic condition, or otherwise improving or enhancing vision of a patient, comprises placing the fluid composition in the interior of the eye. The method may be practiced by injecting the fluid composition into the interior of the eye.
    Type: Application
    Filed: January 16, 2015
    Publication date: May 14, 2015
    Inventor: Scott M. Whitcup
  • Publication number: 20150133416
    Abstract: Pharmaceutical composition comprising abiraterone acetate, which exhibits a reduced food effect and improved bioavailability.
    Type: Application
    Filed: May 3, 2013
    Publication date: May 14, 2015
    Inventors: Pascal Grenier, Guy Vergnault
  • Patent number: 9029355
    Abstract: In certain embodiments, the invention is directed to composition comprising stable particles comprising ganaxolone, wherein the volume weighted median diameter (D50) of the particles is from about 50 nm to about 500 nm.
    Type: Grant
    Filed: November 22, 2013
    Date of Patent: May 12, 2015
    Assignee: Marinus Pharmaceuticals
    Inventors: Kenneth Shaw, Mingbao Zhang
  • Publication number: 20150119373
    Abstract: The invention relates to novel betulinic acid derivatives and related compounds, and pharmaceutical compositions useful for therapeutic treatment of viral diseases and particularly HIV mediated diseases.
    Type: Application
    Filed: April 19, 2013
    Publication date: April 30, 2015
    Inventors: Bandi Parthasaradhi Reddy, Vedula Manohar Sharma, Kura Rathnakar Reddy, Mamnoor Prem Kumar, Kasireddy Bhaskar Reddy, Mogili Narsingam, Mukkera Venkati, Lanka VL Subrahmanyam, Ravi Mallikarjun Reddy
  • Patent number: 9018198
    Abstract: Prodrugs of steroidal C-17 benzoazoles, pyrimidinoazoles (az-abenzoazoles) and diazines. Methods of synthesis are also described, whereby a prodrug group is substituted for a functional group at A ring portion of the ABC ring structure of the steroid. Suitable pro-drug groups include amino acid groups, succinate groups, phosphate groups, or sulfamate groups. The prodrugs of the disclosed compounds allow for improved oral bioavailability of the compounds that are inhibitors of human CYP 17 enzyme as well as potent antagonists of both wild type and mutant androgen receptors (AR). The compounds and the corresponding prodrugs are useful for the treatment of conditions such as human prostate cancer, breast cancer, and prostate hyperplasia.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: April 28, 2015
    Assignee: University of Maryland
    Inventors: Vincent Njar, Angela Brodie, Lalji K. Gediya
  • Publication number: 20150099727
    Abstract: This application is directed to the use of aminosteroid compounds for the selective inhibition of the enzyme PTP1B in a mammal for the treatment of diabetes.
    Type: Application
    Filed: April 19, 2013
    Publication date: April 9, 2015
    Applicant: Ohr Pharmaceutical Inc.
    Inventors: Michael McLane, Inez Ruiz-White, W. Lee Maloy, Henry R. Wolfe
  • Patent number: 8975244
    Abstract: The present invention relates to a process for the synthesis of (3beta)17-(3-pyridinyl)androsta-5,16-dien-3-yl acetate (Abiraterone acetate) represented by the structure of formula (1), and salts thereof, especially salts with pharmaceutically acceptable acids. The present invention further relates to certain intermediates in such processes.
    Type: Grant
    Filed: February 10, 2014
    Date of Patent: March 10, 2015
    Assignee: Mapi Pharma Ltd.
    Inventors: Ehud Marom, Shai Rubnov, Michael Mizhiritskii
  • Patent number: 8969328
    Abstract: The invention relates to 17-hydroxy-17-pentafluoroethyl-estra-4,9(10)-dien-11-aryl derivatives of formula I with progesterone-antagonizing action and methods of production thereof, use thereof for the treatment and/or prevention of diseases and use thereof for producing medicinal products for the treatment and/or prevention of diseases, in particular uterine fibroids (myomata, uterine leiomyomata), endometriosis, heavy menstrual bleeding, meningiomata, hormone-dependent breast cancers and menopause-associated complaints or for fertility control and emergency contraception.
    Type: Grant
    Filed: February 8, 2011
    Date of Patent: March 3, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Wolfgang Schwede, Ulrich Klar, Carsten Möller, Andrea Rotgeri, Wilhelm Bone, Christoph Huwe
  • Publication number: 20150056267
    Abstract: Described herein are methods of inhibiting angiogenesis, and treating or preventing a disease or disorder (or symptoms thereof) associated with angiogenesis, wherein an anti-angiogenesis compound is administered to a subject.
    Type: Application
    Filed: October 31, 2014
    Publication date: February 26, 2015
    Inventors: Jun Liu, Curtis Chong, David J. Sullivan
  • Publication number: 20150057257
    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.
    Type: Application
    Filed: November 10, 2014
    Publication date: February 26, 2015
    Applicant: CHIESI FARMACEUTICI S.p.A.
    Inventors: Eleonora GHIDINI, Andrea RIZZI
  • Publication number: 20150051179
    Abstract: Steroidal C-17 nitrogen-containing heterocycles of Formula I: wherein: the ABCD ring structure is the nucleus of a steroid, or an analog thereof; X is a group capable of coordinating a heme group of CYP17, and Y is an hydroxyl functionality, a suitable ester, or a prodrug group, for the treatment of urogenital and/or androgen-related cancers, such as castration-resistant prostate cancer. The invention provides methods of synthesizing new chemical entities and methods of using the same in treating urogenital and/or androgen-related cancers.
    Type: Application
    Filed: June 24, 2014
    Publication date: February 19, 2015
    Inventor: David Casebier
  • Patent number: 8957055
    Abstract: Sterol derivatives of formula (I) and a method for the production of the compounds, a medicament using one of the compounds and a pharmaceutical composition comprising the medicament.
    Type: Grant
    Filed: August 28, 2013
    Date of Patent: February 17, 2015
    Assignee: Institut National de la Sante et de la Recherche Medicale (INSERM)
    Inventors: Marc Poirot, Philippe De Medina, Sandrine Poirot
  • Publication number: 20150037407
    Abstract: A method to improve the safety of handling of drug substances that are dispensed as solid oral dosage forms is described that does not alter the drug-release profile and the therapeutic efficacy of the pharmaceutical product.
    Type: Application
    Filed: August 22, 2014
    Publication date: February 5, 2015
    Inventors: Rebanta Bandyopadhyay, Susen Werle
  • Patent number: 8940719
    Abstract: Certain chemical entities chosen from compounds of Formula I: and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, and mixtures thereof are described. Pharmaceutical compositions comprising at least one chemical entity chosen from compounds of Formula I and a pharmaceutically acceptable vehicle are described. Also described are methods for inhibiting ?-2,3-sialyltransferase activity in cells, and methods for treating a patient having a disease responsive to inhibition of ?-2,3-sialyltransferase activity.
    Type: Grant
    Filed: July 3, 2006
    Date of Patent: January 27, 2015
    Assignee: Academia Sinica
    Inventors: Wen-Shan Li, Yi-Ching Wang, Hsueh-Fen Juan
  • Publication number: 20150018323
    Abstract: Methods and kits for characterizing a subject having a steroid-dependent disease such as prostate cancer are described. A method of treating a steroid-dependent disease in a subject by obtaining a biological sample from the subject, determining if the HSD3B1(1245C) gene or 3?HSD1(367T) protein is expressed in the biological sample, and providing treatment other than or in addition to steroid ablation to the subject if the HSD3B1(1245C) gene or 3?HSD1(367T) protein is expressed is also described.
    Type: Application
    Filed: July 14, 2014
    Publication date: January 15, 2015
    Inventors: Nima Sharifi, Kai-Hsiung Chang
  • Publication number: 20150018322
    Abstract: Various prodrug compounds having the general structure: Active agent-(acid)-(linker)-SO2NR1R2 are described herein. Compounds having this general structure were shown to be more orally active than the unmodified parent molecule.
    Type: Application
    Filed: July 11, 2014
    Publication date: January 15, 2015
    Inventors: Klaus Nickisch, Bindu Santhamma, Gulzar Ahmed, Frederick Meece, Walter Elger, Ralf Wyrwa, Hareesh Nair
  • Patent number: 8932614
    Abstract: A composite that includes a polymeric material having a void structure and particulate ceragenin material (i.e., ceragenin particles) associated with the void structure. The average particle size of the ceragenin particles in the composite is in a range from 5 nm to 20 ?m, 50 nm to 10 ?m, 100 nm to 5 ?m, or 1 ?m to 10 ?m. The composite has a high loading of ceragenin particles (e.g., about 10% to about 25%, by weight). The composite has good polymer stability, the ability to release ceragenins from the ceragenin particles disposed in the composite over a sustained period of time at a characteristic elution rate, and the ability to kill large numbers of bacteria and other susceptible microbes over the sustained period of time.
    Type: Grant
    Filed: August 24, 2012
    Date of Patent: January 13, 2015
    Inventors: Paul B. Savage, Carl Genberg
  • Publication number: 20150011517
    Abstract: The present invention relates to a lupane triterpenoid derivatives and pharmaceutical use thereof, specifically relates to a lupane triterpenoid derivatives of formula (I)˜(III), a pharmaceutical composition and a combination preparation comprising a lupane triterpenoid derivatives or a pharmaceutically acceptable salt thereof in a therapeutically-effective dose, particularly relates to the use in preparation of a medicament for the treatment of HIV-1/AIDS.
    Type: Application
    Filed: January 30, 2013
    Publication date: January 8, 2015
    Inventor: Feng Lu
  • Publication number: 20140371181
    Abstract: Prodrugs of C-17-heterocyclic-steroidal drugs providing improved oral bioavailability and phamacokinetics are described. The drugs are inhibitors of human CYP 17 enzyme, as well as potent antagonists of both wild type and mutant androgen receptors (AR), and are useful for the treatment of urogenital and/or androgen-related cancers, diseases and/or conditions, such as human prostate cancer, breast cancer, and prostate hyperplasia. The disclosure describes methods of synthesizing and using the prodrugs in cancer therapy.
    Type: Application
    Filed: July 10, 2014
    Publication date: December 18, 2014
    Inventor: David S. Casebier