Nitrogen Containing Hetero Ring Patents (Class 514/176)
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Patent number: 8969328Abstract: 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: GrantFiled: February 8, 2011Date of Patent: March 3, 2015Assignee: Bayer Intellectual Property GmbHInventors: Wolfgang Schwede, Ulrich Klar, Carsten Möller, Andrea Rotgeri, Wilhelm Bone, Christoph Huwe
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Publication number: 20150057257Abstract: 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: ApplicationFiled: November 10, 2014Publication date: February 26, 2015Applicant: CHIESI FARMACEUTICI S.p.A.Inventors: Eleonora GHIDINI, Andrea RIZZI
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Publication number: 20150056267Abstract: 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: ApplicationFiled: October 31, 2014Publication date: February 26, 2015Inventors: Jun Liu, Curtis Chong, David J. Sullivan
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Publication number: 20150051179Abstract: 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: ApplicationFiled: June 24, 2014Publication date: February 19, 2015Inventor: David Casebier
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Patent number: 8957055Abstract: 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: GrantFiled: August 28, 2013Date of Patent: February 17, 2015Assignee: Institut National de la Sante et de la Recherche Medicale (INSERM)Inventors: Marc Poirot, Philippe De Medina, Sandrine Poirot
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Publication number: 20150037407Abstract: 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: ApplicationFiled: August 22, 2014Publication date: February 5, 2015Inventors: Rebanta Bandyopadhyay, Susen Werle
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Patent number: 8940719Abstract: 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: GrantFiled: July 3, 2006Date of Patent: January 27, 2015Assignee: Academia SinicaInventors: Wen-Shan Li, Yi-Ching Wang, Hsueh-Fen Juan
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Publication number: 20150018322Abstract: 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: ApplicationFiled: July 11, 2014Publication date: January 15, 2015Inventors: Klaus Nickisch, Bindu Santhamma, Gulzar Ahmed, Frederick Meece, Walter Elger, Ralf Wyrwa, Hareesh Nair
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Publication number: 20150018323Abstract: 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: ApplicationFiled: July 14, 2014Publication date: January 15, 2015Inventors: Nima Sharifi, Kai-Hsiung Chang
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Patent number: 8932614Abstract: 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: GrantFiled: August 24, 2012Date of Patent: January 13, 2015Inventors: Paul B. Savage, Carl Genberg
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Publication number: 20150011517Abstract: 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: ApplicationFiled: January 30, 2013Publication date: January 8, 2015Inventor: Feng Lu
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Publication number: 20140371181Abstract: 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: ApplicationFiled: July 10, 2014Publication date: December 18, 2014Inventor: David S. Casebier
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Patent number: 8906889Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-3 cycloalkenyl triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II, III and IV: wherein X can be a C4-8 cycloalkyl, C4-8 cycloalkenyl, C4-9 spirocycloalkyl, C4-9 spirocycloalkenyl, C4-8 oxacycloalkyl, C4-8 dioxacycloalkyl, C6-8 oxacycloalkenyl, C6-8 dioxacycloalkenyl, C6-9 oxaspirocycloalkyl, or C6-9 oxaspirocycloalkenyl ring. These compounds are useful for the treatment of HIV and AIDS.Type: GrantFiled: February 6, 2013Date of Patent: December 9, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Jacob Swidorski, Nicholas A. Meanwell, Alicia Regueiro-Ren, Sing-Yuen Sit, Jie Chen, Yan Chen
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Publication number: 20140356417Abstract: Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.Type: ApplicationFiled: June 12, 2014Publication date: December 4, 2014Inventors: Peter Cullis, Marcel Bally, Marco Ciufolini, Norbert Maurer, Igor Jigaltsev
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Publication number: 20140343024Abstract: Described herein are compounds, methods of making such compounds, pharmaceutical compositions, and medicaments comprising such compounds, and methods of using such compounds to treat androgen receptor mediated diseases or conditions. The present invention provides therapies and therapeutic regimens for the treatment of prostate cancer.Type: ApplicationFiled: June 24, 2014Publication date: November 20, 2014Inventors: Jodie Pope Morrison, Cy Aaron Stein, David Scott Casebier
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Patent number: 8884022Abstract: Disclosure is provided for carbamate compounds that prevent, remove and/or inhibit the formation of biofilms, compositions including these compounds, devices including these compounds, and methods of using the same.Type: GrantFiled: January 4, 2013Date of Patent: November 11, 2014Assignee: North Carolina State UniversityInventors: Christian Melander, Steven A. Rogers
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Publication number: 20140329787Abstract: The present invention relates to a novel Phytophthora phospholipase C and uses thereof, methods of identifying modulators and inhibitors of a biological function of the phospholipase C, and methods of inhibiting Phytophthora growth comprising inhibiting a biological function of a novel Phytophthora phospholipase C.Type: ApplicationFiled: October 17, 2012Publication date: November 6, 2014Inventors: Dean Ian Phillips, Peter Luke Beech
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Patent number: 8877715Abstract: There is provided a series of novel neuropeptide Y-cytotoxic conjugates, compositions comprising the same, and methods relating to their therapeutic use for the treatment of disease or condition states associated with aberrant or undesirable proliferation of cells that express NPY-Y1 receptors.Type: GrantFiled: August 18, 2011Date of Patent: November 4, 2014Assignee: Ipsen Pharma S.A.S.Inventors: Zheng Xin Dong, Kevin Zhou, Daniel B. Deoliveira
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Publication number: 20140309181Abstract: Small compounds that modulate the expression of and/or function of sodium channel, voltage-gated, alpha subunit (SCNxA) are presented. Pharmaceutical compositions containing such small molecules and their use in treating diseases and disorders associated with the expression of SCNxA are also presented.Type: ApplicationFiled: August 28, 2012Publication date: October 16, 2014Applicant: CuRNA, Inc.Inventors: Joseph Collard, Olga Khorkova Sherman, Jane H. Hsiao
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Publication number: 20140294737Abstract: The invention provides a method of treating rhinitis. The method comprises administering an effective amount of a danazol compound or a pharmaceutically acceptable salt thereof. The invention also provides a pharmaceutical product formulated for nasal administration. The product comprises a danazol compound or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 5, 2012Publication date: October 2, 2014Inventor: David Bar-Or
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Patent number: 8846647Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-17 and C-3 modified triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II and III: These compounds are useful for the treatment of HIV and AIDS.Type: GrantFiled: January 27, 2012Date of Patent: September 30, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Alicia Regueiro-Ren, Zheng Liu, Jacob Swidorski, Ny Sin, Brian Lee Venables, Sing-Yuen Sit, Yan Chen, Jie Chen, Nicholas A. Meanwell
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Publication number: 20140288037Abstract: Described herein are compounds, methods of making such compounds, pharmaceutical compositions, and medicaments comprising such compounds, and methods of using such compounds to treat androgen receptor mediated diseases or conditions. In some embodiments, the solid matrix comprises a polymer. In some embodiments, the polymer is soluble in an aqueous solution. In particular embodiments, the aqueous solution is water. In other embodiments, the aqueous solution has a pH of 5.0 or greater.Type: ApplicationFiled: July 18, 2012Publication date: September 25, 2014Applicant: Tokai Pharmaceuticals, Inc.Inventors: David Scott Casebier, Abdellah Sentissi, Richard Christian Moreton, Mark Turnbull
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Publication number: 20140287039Abstract: Pharmaceutical compositions, including unit dosage forms, comprising fine particle abiraterone acetate with or without an antioxidant and or a sequestering agent as well as methods for producing and using such compositions are described.Type: ApplicationFiled: March 17, 2014Publication date: September 25, 2014Applicant: ICEUTICA INC.Inventors: H. William Bosch, Marck Norret, Paul Nemeth, Matt Callahan
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Publication number: 20140288036Abstract: 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: ApplicationFiled: November 15, 2013Publication date: September 25, 2014Applicant: the University of Maryland, BaltimoreInventors: Angela Brodie, Vincent Njar
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Publication number: 20140271761Abstract: A method and kit for manufacturing 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: ApplicationFiled: May 27, 2014Publication date: September 18, 2014Applicant: BRIGHAM YOUNG UNIVERSITYInventors: PAUL B. SAVAGE, Carl Genberg
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Publication number: 20140274984Abstract: The present invention relates to acid addition salts of 5?-hydroxy-6?-[2-(1H-imidazol-4-yl)ethylamino]cholestan-3?-ol, to their preparation and to applications thereof.Type: ApplicationFiled: October 17, 2012Publication date: September 18, 2014Applicants: AFFICHEM, INSERM (Institute National de la Sante et de la Recherche MedicaleInventors: Marc Poirot, Sandrine Poirot, Philippe de Medina, Michael Paillasse
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Publication number: 20140274983Abstract: 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: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: University of Maryland, BaltimoreInventors: Vincent Njar, Angela Brodie, Lalji K. Gediya
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Patent number: 8835411Abstract: The disclosure generally relates to the novel compounds of formula I, including their salts, which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.Type: GrantFiled: December 6, 2011Date of Patent: September 16, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Yasutsuga Ueda, Timothy P. Connolly, Barry L. Johnson, Chen Li, B. Narasimhulu Naidu, Manoj Patel, Kevin Peese, Margaret E. Sorenson, Michael A. Walker, Michael S. Bowsher, Rongti Li
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Patent number: 8835412Abstract: Anti-inflammatory and antiallergic compounds of the glucocorticosteroid series according to formula (I) defined herein are useful for treating diseases of the respiratory tract characterized by airway obstruction.Type: GrantFiled: March 15, 2012Date of Patent: September 16, 2014Assignee: Chiesi Farmaceutici S.p.A.Inventors: Eleonora Ghidini, Anna Maria Capelli
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Publication number: 20140256694Abstract: The present invention describes steroid antibiotic conjugates. These single drug entities are formed connecting a steroid moiety and two same antibiotics moieties, or a steroid moiety and two different antibiotics moieties. Upon topical application to the eye, the conjugate hybrid would undergo enzymatic and/or hydrolytic cleavage to release the individual drugs.Type: ApplicationFiled: March 6, 2014Publication date: September 11, 2014Applicant: Allergan, Inc.Inventors: Santosh C. Sinha, Ken Chow, LIMING WANG, MICHAEL E. GARST, MAYSSA ATTAR, BRANDON D. SWIFT
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Publication number: 20140256612Abstract: The present invention describes novel single drug entities, formed by direct linkage of an antibiotic to a steroidal drug. Upon topical application to the eye, the conjugate would undergo enzymatic and/or hydrolytic cleavage to release the individual drugs. The antibiotic is coupled directly to the steroid drug.Type: ApplicationFiled: March 6, 2014Publication date: September 11, 2014Applicant: Allergan, Inc.Inventors: Santosh C. Sinha, Ken Chow, LIMING WANG, MICHAEL E. GARST, MAYSSA ATTAR, BRANDON D. SWIFT
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Publication number: 20140256660Abstract: The present invention describes novel single drug entities, formed by the linkage of an antibiotic with a steroidal drug via a linker. Upon topical application to the eye, the conjugate would undergo enzymatic and/or hydrolytic cleavage to release the individual drugs.Type: ApplicationFiled: March 6, 2014Publication date: September 11, 2014Applicant: Allergan, Inc.Inventors: Santosh C. Sinha, Smita S. Bhat, Ken Chow, LIMING WANG, MICHAEL E. GARST, MAYSSA ATTAR, BRANDON D. SWIFT
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Publication number: 20140249122Abstract: The present invention relates to novel aminosteroid derivatives substituted in position 3 andor 6, and to the use thereof in the context of the treatment of type 2 diabetes and of insulin resistance.Type: ApplicationFiled: October 16, 2012Publication date: September 4, 2014Applicants: UNIVERSITE NICE SOPHIA ANTIPOLIS, UNIVERSITE D'AIX-MARSEILLE, INSERM (Institut National de la Sante Et de la Recherche Medicate), CENTRE NATIONAL DE LA RECHERCHE SCIENTIFQUEInventors: Roland Marinus Theodorus Govers, Jean-Michel Brunel
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Publication number: 20140243298Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, alkyl and alkenyl C-3 modified betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II, III and IV: a compound of Formula I a compound of Formula II a compound of Formula III and a compound of Formula IV These compounds are useful for the treatment of HIV and AIDS.Type: ApplicationFiled: February 21, 2014Publication date: August 28, 2014Inventors: Jacob Swidorski, Yan Chen, Sing-Yuen Sit, Nicholas A. Meanwell, Alicia Regueiro-Ren, Jie Chen
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Publication number: 20140243278Abstract: Disclosed is an acid addition salt of donepezil, wherein acid counterion is selected from the group consisting of pamoic acid, cypionic acid, camphor sulfonic acid, enanthic acid, fusidic acid, gluceptic acid, gluconic acid, lactobionic acid, lauric acid, valeric acid, Dibenzoyl-D-Tartaric acid and terephthalic acid. Disclosed is a process for the preparation and pharmaceutical composition comprising the same. More specifically, disclosed is concerned with the pamoate acid addition salts of donepezil. Disclosed also is long acting formulation comprising the acid addition salt of donepezil and process for the preparation thereof.Type: ApplicationFiled: July 3, 2012Publication date: August 28, 2014Inventors: Sunil Sadanand Nadkarni, Arunkumar Gupta, Jaya Abraham, Manish Parikh, Mahesh Suthar, Bipin Manavadariya, Vivek Mishra
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Publication number: 20140228333Abstract: In one aspect, the invention relates to methods for treating muscle atrophy by providing to an animal in need thereof an effective amount of a compound. The compound can modulate the expression levels of multiple mRNA of a muscle atrophy signature. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: June 6, 2012Publication date: August 14, 2014Applicants: UNIVERSITY OF IOWA RESEARCH FOUNDATION, The United States of America as Represented by the Department of Veterans AffairsInventors: Christopher M. Adams, Steven D. Kunkel, Michael Welsh
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Publication number: 20140228334Abstract: Process for producing composite materials by reactive spray-drying, where a liquid phase A, which comprises inorganic cations, and a liquid phase B, which comprises anions which, with the inorganic cations, form a salt that is insoluble in the mixture of the liquid phases are sprayed together using at least one multi-substance nozzle, and where at least one hydrophobic active ingredient is present in dissolved form in at least one liquid spraying phase, and where the salt formed from the cations of phase A and the anions of phase B has a solubility of less than 0.02 mol/l in the neutral aqueous medium.Type: ApplicationFiled: February 7, 2014Publication date: August 14, 2014Applicant: BASF SEInventors: Andreas Kempter, Max Siebert, Heidrun Debus
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Publication number: 20140227347Abstract: 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: ApplicationFiled: December 19, 2013Publication date: August 14, 2014Applicant: AMPIO PHARMACEUTICALS, INC.Inventor: David Bar-Or
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Patent number: 8802661Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, modified C-3 and C-28 betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors. These compounds are useful for the treatment of HIV and AIDS.Type: GrantFiled: June 2, 2011Date of Patent: August 12, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Alicia Regueiro-Ren, Zheng Liu, Jacob Swidorski, Nicholas A. Meanwell, Sing-Yuen Sit, Jie Chen, Yan Chen, Ny Sin
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Patent number: 8802128Abstract: Biocompatible intraocular implant systems are formulated for discontinuous or intermittent release of therapeutic levels of a therapeutic agent (such as a steroid) to minimize development of side effects associated with continuous or long term use of such agent. The implant system may comprise one or more implant, and preferably, although not necessarily, also contains an auxiliary agent having an activity effective to lessen at least one side effect associated with said therapeutic agent compared to the use of an otherwise identical implant system lacking said auxiliary agent. The implants containing the therapeutic agent and auxiliary agent may be placed in an eye to treat one or more ocular conditions while reducing the ocular side effects otherwise accompanying the use of such therapeutic agent.Type: GrantFiled: July 21, 2006Date of Patent: August 12, 2014Assignee: Allergan, Inc.Inventors: Michael R. Robinson, Scott M. Whitcup
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Publication number: 20140221328Abstract: The present invention relates to certain novel salts of Betulinic acid derivatives, to process for preparing such compounds, to use the compounds in treating diseases or disorders mediated by HIV infection, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: September 22, 2011Publication date: August 7, 2014Inventors: Bandi Parthasaradhi Reddy, Vedula Manohar Sharma, Kura Rathnakar Reddy, Musku Madhanmohan Reddy
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Publication number: 20140213563Abstract: This invention provides methods of diagnosing and treating syndromes of reversion to fetal consciousness in a neonate.Type: ApplicationFiled: January 24, 2014Publication date: July 31, 2014Applicant: The Regents of the University of CaliforniaInventors: John E. MADIGAN, Monica R. ALEMAN
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Patent number: 8791094Abstract: Described herein are compounds, methods of making such compounds, pharmaceutical compositions, and medicaments comprising such compounds, and methods of using such compounds to treat androgen receptor mediated diseases or conditions. Such compounds include inhibitors of cytochrome C17?-hydroxylase/C17,20-lyase such as 3-?-Hydroxy-17-(1H-benzimidazol-1-yl)androsta-5,16-diene.Type: GrantFiled: August 5, 2010Date of Patent: July 29, 2014Assignee: Tokai Pharmaceuticals, Inc.Inventors: Jodie Pope Morrison, Cy Aaron Stein, David Scott Casebier
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Patent number: 8790691Abstract: Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.Type: GrantFiled: May 26, 2009Date of Patent: July 29, 2014Assignee: The University of British ColumbiaInventors: Pieter Cullis, Marcel Bally, Marco Ciufolini, Norbert Maurer, Igor Jigaltsev
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Patent number: 8791095Abstract: 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: GrantFiled: February 5, 2010Date of Patent: July 29, 2014Assignee: Tokai Pharmaceuticals, Inc.Inventor: David Casebier
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Patent number: 8785424Abstract: The present invention relates to a compound of following formula (I): or to a pharmaceutically acceptable salt thereof, as well as to pharmaceutical compositions including same and to the use thereof as a drug, in particular for treating a proliferative disease such as cancer.Type: GrantFiled: May 20, 2010Date of Patent: July 22, 2014Assignees: Pierre Fabre Medicament, Centre National de la Recherche Scientifique (CNRS)Inventors: Christophe Long, Yves Guminski, Fadila Derguini, Joséphine Beck, Frédéric Cantagrel
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Patent number: 8785423Abstract: The present invention provides methods of inducing cell cycle arrest and/or cell growth inhibition, with the methods comprising administering to the cells an effective dose of the compounds of the present invention.Type: GrantFiled: April 14, 2009Date of Patent: July 22, 2014Assignee: University of Maryland, BaltimoreInventors: Vincent Njar, Angela Brodie, Robert Bruno
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Patent number: 8754069Abstract: Compounds of Formula I: that possess unique antiviral activity are provided as HIV maturation inhibitors. These compounds are useful for the treatment of HIV and AIDS.Type: GrantFiled: September 20, 2012Date of Patent: June 17, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Zheng Liu, Nicholas A. Meanwell, Alicia Regueiro-Ren
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Patent number: 8754068Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, modified C-3 betulinic acid and other structurally related natural products derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors. These compounds are useful for the treatment of HIV and AIDS.Type: GrantFiled: June 2, 2011Date of Patent: June 17, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Alicia Regueiro-Ren, Jacob Swidorski, Zheng Liu, Nicholas A. Meanwell, Sing-Yuen Sit, Jie Chen, Ny Sin
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Patent number: 8748415Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-28 amines of C-3 modified betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors. These compounds are useful for the treatment of HIV and AIDS.Type: GrantFiled: January 27, 2012Date of Patent: June 10, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Alicia Regueiro-Ren, Jacob Swidorski, Sing-Yuen Sit, Yan Chen, Jie Chen, Nicholas A. Meanwell, Zheng Liu