Nitrogen Containing Hetero Ring Patents (Class 514/176)
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Patent number: 7517870Abstract: The present invention concerns the use of compounds that interfere with the hedgehog signaling pathway for the manufacture of a medicament for preventing, inhibiting, and/or reversing ocular diseases related with ocular neovascularization. Particularly, the above-mentioned diseases are (wet) age-related macular degeneration, (proliferative) diabetic retinopathy, neovascular glaucoma, retinal vein occlusion, or retinopathy of prematurity (ROP).Type: GrantFiled: December 3, 2004Date of Patent: April 14, 2009Assignee: Fondazione TelethonInventors: Alberto Auricchio, Markus Hildinger, Enrico Maria Surace
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Publication number: 20090082320Abstract: Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and/or muscle tissue while antagonizing the AR in the prostate of a male patient or in the uterus of a female patient. These compounds are therefore useful in the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, cancer cachexia, muscular dystrophies, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.Type: ApplicationFiled: November 18, 2008Publication date: March 26, 2009Inventors: Robert S. Meissner, James J. Perkins
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Publication number: 20090069277Abstract: Compounds from 14 Kenyan plants, including from the root of Dovyalis abyssinica and Clutia robusta have been characterized and isolated, and their uses are disclosed.Type: ApplicationFiled: September 6, 2007Publication date: March 12, 2009Inventors: Paul Kiprono Chepkwony, Maria Medina, Mitchell Medina
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Publication number: 20090042846Abstract: This invention relates to certain sugar esters of phytosterols of formula (I).Type: ApplicationFiled: September 15, 2008Publication date: February 12, 2009Applicant: BIODERM RESEARCHInventor: SHYAM K. GUPTA
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Publication number: 20090042844Abstract: Compounds having the structure, their salts or N-oxide derivatives: are used to treat or reduce le likelihood of acquiring androgen-dependent diseases, such as prostate cancer, benign prostatic hyperplasia, polycystic ovarian syndrome, acne, hirsutism, seborrhea, androgenic alopecia and male baldness. They can be formulated together with pharmaceutically acceptable diluent or carrier or otherwise made into any pharmaceutical dosage form. Combinations with other active pharmaceutical agents are also disclosed.Type: ApplicationFiled: April 9, 2008Publication date: February 12, 2009Inventors: Fernand LABRIE, Sylvain GAUTHIER, Julie CLOUTIER, Josee MAILHOT, Steeves POTVIN, Sylvain DION, Jean-Yves SANCEAU
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Publication number: 20090028918Abstract: The present invention relates to a kind of sodium alginate microsphere vascular embolus containing gynecological drug and its preparation. The preparation of it consists of the following steps: preparing the solution of gynecological drug, sodium alginate and dilvalent metal cations such as BaCl2, Mg Cl2 or CaCl2 etc. by order; mixing the gynecological drug solution and sodium alginate solution, and then mixing them with the curing solution of BaCl2 or CaCl2 and the like. Then the obtained is the sodium alginate microshere vascular embolus containing gynecological drug. The carrier materials of the vascular embolus according to the invention are natural extracts and have good biocompatibility and re biodegradable; the side effect of the pharmaceutic loaded by them is minimal, and it is especially suitable for myometrial gland and hysteromyoma.Type: ApplicationFiled: April 15, 2007Publication date: January 29, 2009Inventors: Congjian Xu, Xinjian Li, Hong Hong, Ge Lu
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Publication number: 20090022671Abstract: Disclosed are methods of treating rhinosinusitis of the upper airway passages in patients afflicted with said disease, which comprises administering at least once-a-day to the surfaces of said passages of said patients an amount of aerosolized particles of mometasone furoate as a monotherapy effective for treating said disease.Type: ApplicationFiled: July 11, 2008Publication date: January 22, 2009Inventors: Melvyn Bloom, Melvyn R. Danzig, Patricia Rohane, Heribert W. Staudinger
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Publication number: 20080312201Abstract: Methods of using methotrexate (MTX) active agents in which reduced host toxicity is observed are provided. In the subject methods, an effective amount of an MTX active agent is administered to the host in conjunction with the administration of an MTX toxicity reducing agent of the present invention. Also provided are compositions for use in practicing the subject methods, e.g., pharmaceutical compositions having reduced toxicity, in which the MTX active agent is combined with an MTX toxicity reducing agent that reduces the level of undesired MTX toxicity while maintaining an effective MTX anti-proliferative activity. Also provided are methods of using the subject methods and compositions in the treatment of a variety of different disease conditions.Type: ApplicationFiled: September 8, 2005Publication date: December 18, 2008Inventor: Patrick Fogarty
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Publication number: 20080293682Abstract: The invention relates to novel betulinic acid derivatives of formula (I), wherein R is C(?CH2) CH3 or CH(CH3)2; R2 together with the adjacent carbonyl group forms a carboxylic acid, carboxylic acid ester or amide or substituted amide; R3 or R4 are hydrogen or aryl with the proviso that both are not independently hydrogen or alkyl or R3 and R4 are combined together to form an aryl ring optionally substituted with a group X, wherein X is selected from halogen, alkyl, cyano, nitro, alkoxy, amino or substituted amine; Y is N or O; and R1 is zero when Y is O, and R1 is hydrogen, alkyl or aryl alkyl when Y is N, useful for inhibition of tumor cancer cells.Type: ApplicationFiled: December 29, 2005Publication date: November 27, 2008Inventors: Rama Mukherjee, Kumar Srivastava, Mohammad Jamshed Ahmed Siddioui, Manu Jaggi, Anu T. Singh, Anand Vardhan, Manoj Kumar Singh, Praveen Rajendran, Hemant Kumar Jajoo, Anand C. Burman, Vivek Kumar, Nidhi Rani, Shiv Kumar Agarwal
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Publication number: 20080287408Abstract: A pharmaceutical composition comprises at least one nonlipoidal internal phase and at least one lipoidal external phase that is bioadhesive to a vaginal mucosal surface, and comprises danazol in an amount of about 3% to about 30% by weight of the composition, wherein upon application of the composition to the vaginal mucosal surface the danazol is released over a period of about 1 to about 10 days. The composition is useful for intravaginal administration to treat a condition such as endometriosis for which danazol is indicated.Type: ApplicationFiled: April 18, 2008Publication date: November 20, 2008Applicant: DRUGTECH CORPORATIONInventors: Daniel J. Thompson, Robert C. Cuca, Thomas C. Riley, JR., Jonathan David Bortz
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Publication number: 20080280864Abstract: 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 CYP 17 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: March 2, 2006Publication date: November 13, 2008Inventors: Angela Brodie, Vincent Njar
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Publication number: 20080255075Abstract: Substituted estratriene compounds of formula (I) useful in therapy, especially in the treatment or inhibition of a steroid hormone dependent disorder requiring the inhibition of a 17?-hydroxysteroid dehydrogenase (17?-HSD) type 1, type 2 and/or type 3 enzyme, as well as their salts, pharmaceutical compositions containing such compounds and processes for preparing such compounds.Type: ApplicationFiled: November 29, 2007Publication date: October 16, 2008Applicant: Solvay Pharmaceuticals GmbHInventors: Josef MESSINGER, Uwe Schoen, Heinrich-Hubert Thole, Bettina Husen, Pasi Koskimies, Mikko Unkila
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Publication number: 20080255074Abstract: The invention provides for a combination comprising an amount of an SSRI, or a pharmaceutically acceptable salt or solvate thereof, and an amount of a GR antagonist, or a pharmaceutically acceptable salt or solvate thereof, optionally in association with one or more pharmaceutically acceptable carriers for use as therapy for depression and related disorders.Type: ApplicationFiled: November 16, 2005Publication date: October 16, 2008Applicant: N.V. OrganonInventors: Colin D. Ingram, Morag A. Grassie, Nicol Ferrier, Sasha E. Gartside, Allan E. Young
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Publication number: 20080234242Abstract: Compounds of the formula and use of the compounds as medicaments.Type: ApplicationFiled: March 19, 2008Publication date: September 25, 2008Applicant: Nicox S.A.Inventor: Piero Del Soldato
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Publication number: 20080214514Abstract: Described herein are steroid derivatives of fullerene moieties, for example fullerene derivatives in which cholesterol, or a cholesterol moiety, is attached via ester, amide, or ether bonds to one of a variety of “linkers,” e.g., chemical groups including alkyl chains and aromatic groups, which are then connected to the fullerene moiety. The steroid moiety can confers useful solubility in components of biological fluids and/or pharmacologically acceptable carriers and can also affect the biodistribution of the fullerenes which makes the derivatives useful in imaging, diagnosis and the treatment or management of disease or complications of disease states.Type: ApplicationFiled: March 3, 2008Publication date: September 4, 2008Applicant: Luna Innovations IncorporatedInventors: Darren MacFarland, Jing Zhang, Zhiguo Zhou, Robert P. Lenk, Stephen R. Wilson
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Publication number: 20080193499Abstract: 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: June 27, 2005Publication date: August 14, 2008Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Jun Liu, Curtis Chong, David J. Sullivan
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Patent number: 7407947Abstract: An amphoteric compound based on a sterol skeleton, the 3-position of the sterol ring system being substituted by one or more amphoteric groups having an isoelectric point of between about 4 and 9, together with liposomes containing such compounds and their uses.Type: GrantFiled: February 21, 2002Date of Patent: August 5, 2008Assignee: Novosom AGInventors: Steffen Panzner, Gerold Endert, Stefan Fankhaenel, Nasr El-Mokdad
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Publication number: 20080182830Abstract: An object of the present invention is to provide an agent for use in the effective treatment and prevention of endometriosis and uterine adenomyosis. The present invention relates to an agent for use in the treatment and prevention of endometriosis or uterine adenomyosis, comprising, as an active ingredient, a compound selected from the group consisting of 3-ethylpyridine, 3-methylpyridine, 2-ethylpyridine, and 2-methylpyridine.Type: ApplicationFiled: March 15, 2006Publication date: July 31, 2008Inventors: Masao Igarashi, Toshio Igarashi, Shigeo Igarashi
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Publication number: 20080167282Abstract: The invention concerns the use of one or more steroid activity inhibitors, namely androgens, such as, for example, testosterone, for the treatment of disorders related to, or resulting from use of, or induced by substances or induced by intoxication from substances or abstinence from substances, mental disorders induced by substances, substance addiction or gambling, abuse of substances or recurrent criminal behaviour.Type: ApplicationFiled: March 17, 2006Publication date: July 10, 2008Inventor: Giuseppe La Pera
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Publication number: 20080166301Abstract: The present invention comprises the design, synthesis and development of a new class of chemotherapeutic agents for prophylactic and therapeutic treatments in a mammal, particularly a human, believed to be at risk of suffering from a hormone-responsive disorder. In an aspect of the invention, such treatments include therapeutic compositions comprising novel steroidal antiestrogen and antiandrogen compounds. In a preferred aspect, such a novel compound of the present invention has an address and a message component, which are made into a single composite entity for more aggressive intervention and effective treatment of hormone-responsive disorders, thereby prolonging the disease-free interval for the patient and reducing a number of side effects.Type: ApplicationFiled: October 19, 2007Publication date: July 10, 2008Inventors: Robert N. Hanson, Carolyn Friel, Choon Young Lee
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Patent number: 7396827Abstract: The invention provides compositions comprising formula 1 steroids, e.g., 16?-bromo-3?-hydroxy-5?-androstan-17-one hemihydrate and one or more excipients, typically wherein the composition comprises less than about 3% water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16?-bromo-3?-hydroxy-5?-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen (viral) replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using certain steroids and steroid analogs. The invention also provides methods to make and use these immunomodulatory compositions and formulations.Type: GrantFiled: December 13, 2002Date of Patent: July 8, 2008Assignee: Hollis-Eden Pharmaceuticals, Inc.Inventors: Clarence N. Ahlem, William Heggie, Luis D. Carvalho
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Publication number: 20080153789Abstract: Pharmaceutical preparations for topical or local administration of drugs directly to the skin for treatment of disorders of the subcutaneous fatty tissue, in particular in cases of cellulite, are disclosed herein. In a preferred embodiment, the drug is danazol or gastrinone. In another embodiment, the drug is danazol in combination with an aromatase inhibitor or an estrogen compound. The preferred formulations contain drugs in the form of micro or nanoparticles, which may be formed of drug alone or in combination with an excipient or carrier. The excipient or carrier may modify the release rates or enhance absorption into the affected area. The drug formulation may be in the form of a cream, lotion, ointment, gel or emulsion, solution or foam.Type: ApplicationFiled: December 26, 2007Publication date: June 26, 2008Inventors: Paul Dmowski, Gerianne T. DiPiano
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Publication number: 20080146531Abstract: Estratrien-triazoles corresponding to formula (I) (shown below) which are useful in therapy, especially for the treatment and/or prevention or inhibition of a steroid hormone dependent disorder, preferably a steroid hormone dependent disease or disorder requiring the inhibition of a 17?-hydroxysteroid dehydrogenase (17?-HSD) such as 17?-HSD type 1, type 2 or type 3 enzyme.Type: ApplicationFiled: September 18, 2007Publication date: June 19, 2008Applicant: SOLVAY PHARMACEUTICALS GmbHInventors: Josef Messinger, Uwe Schoen, Heinrich-Hubert Thole, Bettina Husen, Pasi Koskimies, Lila KALLIO nee Pirkkala
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Patent number: 7381718Abstract: A process for the preparation of compounds of formula (I) in which R1, R2, R3 and n are defined as indicated in the description, use of said compounds as intermediates for the preparation of estrogen derivatives as well as the intermediates of this process.Type: GrantFiled: June 12, 2002Date of Patent: June 3, 2008Assignee: Aventis Pharma S.A.Inventors: Francoise Benedetti, Alain Mazurie, Francois Nique, Denis Prat, Christian Wehrey
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Publication number: 20080125403Abstract: A method of safely and specifically treating the combined metabolic disturbances of insulin resistance and visceral adiposity in male subject with visceral adiposity, metabolic syndrome (also known as the ‘insulin resistance syndrome’, and ‘syndrome X’), type II diabetes, or insulin resistance by administering a 5-alpha reductase inhibiting compound of structural formula I, II, III, or IV is disclosed. The method is also concerned with the use of the 5alpha reductase inhibiting compound together with antidiabetic agents, lipid lowering agents, antihypertensive agents, antiobesity agents, testosterone, testosterone precursors, testosterone prodrugs, testosterone analogs, and other androgen receptor agonists for treating visceral adiposity, metabolic syndrome, type II diabetes and insulin resistance in men.Type: ApplicationFiled: March 29, 2005Publication date: May 29, 2008Applicant: MERCK & CO., INC.Inventor: Alan Meehan
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Publication number: 20080119443Abstract: 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: ApplicationFiled: July 3, 2006Publication date: May 22, 2008Inventors: Wen-Shan Li, Yi-Ching Wang, Hsueh-Fen Juan
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Patent number: 7375098Abstract: This invention relates to 8?-vinyl-11?-(?-substituted)alkyl-estra-1,3,5(10)-trienes of general formula I with ER?-antagonistic activity, process for their production, their intermediate products, pharmaceutical preparations that contain the compounds according to the invention, as well as their use for the production of pharmaceutical agents. The new compounds can be used for contraception in men and women without influencing other estrogen-sensitive organs such as the uterus or the liver. They are also suitable for treating benign or malignant proliferative diseases of the ovary, such as ovarian cancer and granulosa cell tumors.Type: GrantFiled: April 22, 2004Date of Patent: May 20, 2008Assignee: Schering A.G.Inventors: Nico Braeuer, Olaf Peters, Alexander Hillisch, Rolf Bohlmann, Margit Richter, Hans-Peter Muhn
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Publication number: 20080090791Abstract: The invention relates to the use of compounds to ameliorate or treat an condition such as a cystic fibrosis, neutropenia or other exemplified conditions. Exemplary compounds that can be used include 3?-hydroxy-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 1?,3?-dihydroxy-4?-fluoroandrost-5-ene-17-one, 1?,3?,17?-trihydroxy-4?-fluoroandrost-5-ene, 1?,3?-dihydroxy-6?-bromoandrost-5-ene, 1?-fluoro-3?,12?-dihydroxyandrost-5-ene-17-one, 1?-fluoro-3?,4?-dihydroxyandrost-5-ene and 4?-fluoro-3?,6?,17?-trihydroxyandrostane.Type: ApplicationFiled: October 13, 2006Publication date: April 17, 2008Applicant: Hollis-Eden Pharmaceuticals, Inc.Inventors: Christopher L. Reading, Clarence N. Ahlem, Dominick L. Auci, Charles Dowding, James M. Frincke, Mei Li, Theodore Page, Dwight R. Stickney, Richard J. Trauger, Steven K. White
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Publication number: 20080085873Abstract: The invention relates to the use of compounds to ameliorate or treat a condition such as a cystic fibrosis, neutropenia or other exemplified conditions. Exemplary compounds that can be used include 3?-hydroxy-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 1?,3?-dihydroxy-4?-fluoroandrost-5-ene-17-one, 1?,3?,17?-trihydroxy-4?-fluoroandrost-5-ene, 1?,3?-dihydroxy-6?-bromoandrost-5-ene, 1?-fluoro-3?,12?-dihydroxyandrost-5-ene-17-one, 1?-fluoro-3?,4?-dihydroxyandrost-5-ene and 4?-fluoro-3?,6?, 17?-trihydroxyandrostane.Type: ApplicationFiled: October 13, 2006Publication date: April 10, 2008Applicant: Hollis-Eden Pharmaceuticals, Inc.Inventors: Christopher L. Reading, Clarence N. Ahlem, Dominick L. Auci, Charles Dowding, James M. Frincke, Mei Li, Theodore M. Page, Dwight R. Stickney, Richard J. Trauger, Steven K. White
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Patent number: 7345034Abstract: Azacyclosteroid histamine-3 receptor ligands, pharmaceutical compositions comprising such compounds, and methods for using such compounds and compositions are described herein.Type: GrantFiled: April 1, 2005Date of Patent: March 18, 2008Assignee: Abbott LaboratoriesInventors: Chen Zhao, Minghua Sun, Marlon D. Cowart, Youssef L. Bennani
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Publication number: 20080051323Abstract: This invention discloses compositions of chloroquine-coupled active agents, including methods for their preparation. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the active agent is delivered, thereby reducing the overall dosage needed. The compositions comprise a chloroquine substance coupled to an active agent directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing active agents for therapeutic or other medical uses.Type: ApplicationFiled: December 29, 2005Publication date: February 28, 2008Inventor: Kenneth M. Kosak
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Patent number: 7312206Abstract: Disclosed is a sterol derivative having a pKa value of 3.5-8 according to the general formula cation-spacer 2-Y-spacer 1-X-sterol, wherein Y and X represent bonding groups. The invention also relates to liposomes containing said sterol derivatives.Type: GrantFiled: February 21, 2002Date of Patent: December 25, 2007Assignee: Novosom AGInventors: Steffen Panzner, Gerold Endert, Stefan Fankhänel, Anja Behrens
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Publication number: 20070281914Abstract: Use of a composition comprising at least one prodrug of a steroid, preferably of a corticosteroid, for the preparation of an ophthalmic composition intended for the treatment of an ocular condition or disease of a human being or an animal.Type: ApplicationFiled: June 1, 2006Publication date: December 6, 2007Inventors: Laura Rabinovich-Guilatt, Gregory Lambert
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Publication number: 20070243238Abstract: A method for treating a mouth sore opposite a tooth by adhering an oral patch on the tooth to speed healing and relieve pain. The oral patch is placed either directly on the portion of the tooth that comes into contact with the sore or is first place onto the sore and then adhered to the tooth. The patch may be a blob of hydrophilic gums. If certain medications are applied to a mouth sore using an oral patch that delivers the medication for at least 30 minutes and the patches are used for at least two or more hours per day, the method reduces the healing time for mouth sores from typical 10-14 days to 1-5 days. The method can be used with various antimicrobials, glucocorticoids or anthihistamines incorporated into the patch that reduce inflammation or speed the healing of mouth sores.Type: ApplicationFiled: December 15, 2006Publication date: October 18, 2007Inventor: Jeffrey T. Haley
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Publication number: 20070207989Abstract: The present invention relates to useful diterpenes and pharmaceutical compositions containing them of the formula: for use in the treatment of cardiovascular and inflammatory diseases and for cancers susceptible to an NF-?B inhibitor and an endothelin receptor inhibitor. The present invention also relates to compounds and methods useful to inhibit cell proliferation and for the induction of apoptosis.Type: ApplicationFiled: March 1, 2007Publication date: September 6, 2007Applicant: SaviPu PharmaceuticalsInventors: Inderjit Kumar Dev, Ven Subbiah
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Patent number: 7265099Abstract: The invention relates to the use of chemical chelators for the preparation of a medicament for the reversal of drug-induced neuromuscular block, to a kit for providing neuromuscular block and its reversal, and to cyclophane derivatives having general formula (A) wherein R is (a), (b) or (c); or general formula (B) wherein X is (a), (b) or (d), or a pharmaceutically acceptable salt thereof.Type: GrantFiled: August 7, 2000Date of Patent: September 4, 2007Assignee: Organon N.V.Inventors: Antonius Helena Adolf Bom, Alan William Muir, David Rees
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Patent number: 7182942Abstract: A method of immunotherapy to treat cancer or a synergistic anti-cancer treatment by administering an effective amount of a natural cytokine mixture (NCM), an effective amount of cyclophosphamide (CY), or an effective amount of indomethacin (INDO), wherein the NCM, CY, or INDO are administered singly or in combinations thereof. An anti-metastatic treatment method by promoting differentiation and maturation of immature dendritic cells in a lymph node; allowing presentation thereof; and preventing development of metastasis. A method of using an NCM as a diagnostic skin test for predicting treatment outcome. A method of pre-treating dendritic cells (DC) and a method of treating monocyte defects characterized by sinus histiocytosis or a negative NCM skin test. Compositions and methods for eliciting an immune response to endogenous or exogenous tumor antigens.Type: GrantFiled: August 8, 2003Date of Patent: February 27, 2007Assignee: IRx Therapeutics, Inc.Inventor: John W. Hadden
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Patent number: 7153844Abstract: wherein X may be —CH2—O—CH2— or —CH2—, wherein n may be 1, 2, 3, 4 or 5 when X is —CH2—O—CH2—, wherein n may be 2, 3, 4, 5, 6, 7, 8, 9 or 10 when X is —CH2—, wherein o may be 1, 2 or 3, wherein Y may be O or 17?-OH, where the dotted line represents the presence or absence of a second chemical bond, wherein R1 may be selected from the group consisting of H, straight alkyl groups of 1 to 5 carbon atoms, and branched alkyl groups of 3 to 5 carbon atoms, wherein R2 may be selected for the group consisting of H, straight alkyl groups of 1 to 4 carbon atoms, branched alkyl groups of 3 or 4 carbon atoms, F, Cl, Br, I, —CF3, —NO2, —OR1, where R1 is as defined hereinabove, —COR1, where R1 is as defined hereinabove, and —CH2OH. These compounds possess anticancer activity against hormono-dependent breast, uterus as well as ovarian cancers.Type: GrantFiled: March 27, 2003Date of Patent: December 26, 2006Inventor: Gervais Bérubé
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Patent number: 7074778Abstract: This invention relates to methods for treating asthma or allergy in a mammal by administering a 3-aminosteroid compound to a mammal in need thereof. The 3-aminosteroid compound being capable of down regulating the IL-9 pathway and alleviating asthmatic responses to allergen. Exemplary 3-aminosteroid compounds used in the methods of the invention include compounds having the chemical formula (I), wherein X, R1, R2, R3, and R4 groups are as defined herein. The invention also relates to certain novel compounds of formula (I). Moreover, the invention also provides methods for identifying an immunomodulatory 3-aminosteroid compound.Type: GrantFiled: December 11, 2000Date of Patent: July 11, 2006Assignee: Genaera CorporationInventors: Roy C. Levitt, Nicholas C. Nicolaides, William A. Kinney, Steve Jones
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Patent number: 7074779Abstract: The present invention is directed to novel estrieno[3,2-b]/[3,4-c]pyrrole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and diseases mediated by an estrogen receptor.Type: GrantFiled: July 2, 2003Date of Patent: July 11, 2006Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Zhihua Sui, Xuqing Zhang
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Patent number: 7067503Abstract: There is provided a compound comprising a steroidal ring system and a group R1 selected from any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; wherein the D ring of the steroidal ring system is substituted by a group R2 of the formula —L-R3, wherein L is an optional linker group and R3 is an aromatic hydrocarbyl group.Type: GrantFiled: February 14, 2003Date of Patent: June 27, 2006Assignee: Sterix LimitedInventors: Barry Victor Lloyd Potter, Michael John Reed, Bertrand Leblond, Matthew Paul Leese
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Patent number: 7053076Abstract: Disclosed are compounds that exhibit high transport across the intestinal wall of an animal. The compounds may optionally be linked to drugs that are poorly absorbed or poorly transported across the intestinal wall after oral administration to provide for enhanced therapeutic, and optionally prolonged therapeutic, systemic blood concentrations of the drugs upon oral administration of the drug-compound conjugate. Also disclosed are pharmaceutical compositions containing and methods of using such compounds.Type: GrantFiled: August 28, 2002Date of Patent: May 30, 2006Assignee: XenoPort, Inc.Inventors: Laxminarayan Bhat, Mark A. Gallop, Bernd Jandeleit
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Patent number: 7049305Abstract: This invention is directed to compounds that provide for sustained systemic concentrations of therapeutic or prophylactic agents following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds.Type: GrantFiled: February 9, 2005Date of Patent: May 23, 2006Assignee: XenoPort, Inc.Inventors: Kenneth C. Cundy, Mark A. Gallop, Cindy X. Zhou
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Patent number: 7018991Abstract: The invention is directed to a novel class of steroids which exhibit potent antiprogestational activity.Type: GrantFiled: July 2, 2003Date of Patent: March 28, 2006Assignee: Research Triangle InstituteInventors: C. Edgar Cook, John A. Kepler, Gary S. Bartley, Rupa S. Shetty
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Patent number: 6956030Abstract: The administration of aerosolize particles of mometasone furoate in the form of dry powders, solutions, or aqueous suspension for treating corticosteroid-responsive diseases of the surfaces of upper and/or lower airway passages and/or lungs, e.g., allergic rhinitis and asthma is disclosed.Type: GrantFiled: January 22, 2004Date of Patent: October 18, 2005Assignee: Schering CorporationInventors: Joel A. Sequeira, Francis M. Cuss, Keith B. Nolop, Imtiaz A. Chaudry, Nagamani Nagabhushan, James E. Patrick, Mitchell Cayen
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Patent number: 6953785Abstract: Provided is steroid sulfatase inhibitors comprising, as the active ingredient, an estra-1,3,5(10)-triene derivative which is represented by formula (I): {wherein R1 and R2 are the same or different and represent a hydrogen atom, a lower alkyl group or, etc.; R3 represents a hydrogen atom etc.; R4 represents a hydrogen atom etc.; R5 represents a hydrogen atom etc.; R6 represents a cyano group, an amino group, COR53 (wherein R53 represents a substituted lower alkyl group etc.), a substituted or unsubstituted aryl group, a substituted or unsubstituted heterocyclic group, etc}, or pharmaceutically acceptable salts thereof.Type: GrantFiled: April 24, 2001Date of Patent: October 11, 2005Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Yoji Ino, Nobuyoshi Amishiro, Mayumi Miyata, Tsutomu Agatsuma, Kozue Muramatsu, Takeshi Takahashi, Shiro Akinaga, Chikara Murakata
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Patent number: 6949532Abstract: The administration of aerosolize particles of mometasone furoate in the form of dry powders, solutions, or aqueous suspension for treating corticosteroid-responsive diseases of the surfaces of upper and/or lower airway passages and/or lungs, e.g., allergic rhinitis and asthma is disclosed.Type: GrantFiled: January 22, 2004Date of Patent: September 27, 2005Assignee: Schering CorporationInventors: Joel A. Sequeira, Francis M. Cuss, Keith B. Nolop, Imtiaz A. Chaudry, Nagamani Nagabhushan, James E. Patrick, Mitchell Cayen
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Patent number: 6921757Abstract: Compounds of formula (I), where R is a monovalent cyclic organic group having from 3 to 15 atoms in the ring system, useful as pharmaceuticalsType: GrantFiled: June 26, 2001Date of Patent: July 26, 2005Assignee: Novartis AGInventors: Bernard Cuenoud, David Beattie, Thomas Hugo Keller, Gaynor Elizabeth Pilgrim, David Andrew Sandham, Simon James Watson
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Patent number: 6900193Abstract: The present invention relates, inter alia, to compounds having the general formula: in which: R1 is a member selected from the group consisting of —OCH3, —SCH3, —N(CH3)2, —NHCH3, —NC4H8, —NC5H10, —NC4H8O, —CHO, —CH(OH)CH3, —C(O)CH3, —O(CH2)2N(CH3)2, and —O(CH2)2NC5H10; R2 is a member selected from the group consisting of hydrogen, halogen, alkyl, acyl, hydroxy, alkoxy (e.g., methoxy, ethoxy, vinyloxy, ethynyloxy, cyclopropyloxy, etc.), acyloxy (e.g., acetoxy, glycinate, etc.), alkylcarbonate, cypionyloxy, S-alkyl, —SCN, S-acyl and —OC(O)R6, wherein R6 is a functional group including, but not limited to, alkyl (e.g., methyl, ethyl, etc.), alkoxy ester (e.g., —CH2OCH3) and alkoxy (—OCH3); R3 is a member selected from the group consisting of alkyl, hydroxy, alkoxy and acyloxy; R4 is a member selected from the group consisting of hydrogen and alkyl; and X is a member selected from the group consisting of ?O and ?N—OR5, wherein R5 is a member selected from the group consisting of hydrogen and alkyl.Type: GrantFiled: March 17, 2000Date of Patent: May 31, 2005Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Hyun K. Kim, Richard P. Blye, Pemmaraju N. Rao, James W. Cessac, Carmie K. Acosta, Anne Marie Simmons
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Patent number: 6900192Abstract: This invention is directed to compounds that provide for sustained systemic concentrations of therapeutic or prophylactic agents following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds.Type: GrantFiled: October 5, 2001Date of Patent: May 31, 2005Assignee: XenoPort, Inc.Inventors: Kenneth C. Cundy, Mark A. Gallop, Cindy X. Zhou