Tetracyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos Patents (Class 514/284)
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Publication number: 20080306019Abstract: Provided herein is a method of protecting a neuron from dysfunction induced by an HIV neurotoxin, comprising contacting the cell with a therapeutically effective dose of a dopamine D1 receptor agonist. Also provided is a method of treating or preventing HIV-1 associated dementia (HAD) in a subject in need of such treatment or prevention, comprising administering to the subject a therapeutically effective dose of a dopamine D1 receptor agonist and estrogenic compound.Type: ApplicationFiled: May 3, 2006Publication date: December 11, 2008Inventors: Rosemarie M. Booze, Charles Mactutus
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Publication number: 20080305082Abstract: Disclosed are compounds having Formula I: and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, A, and B are as defined herein, for use in methods for treating, preventing or ameliorating hyperproliferative disorders, such as cancer and other diseases and conditions. The invention also relates to pharmaceutical compositions and formulations comprising a compound having Formula I, and in combination with one or more other active agents and/or treatments.Type: ApplicationFiled: September 14, 2005Publication date: December 11, 2008Inventors: John G. Curd, Robert L. Capizzi, John F.W. Keana
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Publication number: 20080305186Abstract: The present invention includes compositions and methods treat a patient suffering from one or more symptoms of cardiac hypertrophy, hypertension and/or ischemia by administering a pharmaceutically effective amount of a pharmaceutical composition having an anti-epileptic drug and an antibiotic to the patient, for example, the anti-epileptic drug may be carbamazepine and the antibiotic may be doxycycline.Type: ApplicationFiled: June 11, 2007Publication date: December 11, 2008Applicant: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEMInventors: Harold R. Garner, Mounir Errami
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Publication number: 20080300225Abstract: Compositions and methods are provided for a water-soluble insecticidal or pesticidal comprising at least one alkaloid, particularly at least one tetracyclo-quinolizindine alkaloid derived from sophora roots, particularly matrine and/or oxymatrine.Type: ApplicationFiled: January 23, 2008Publication date: December 4, 2008Applicant: Marrone Organic InnovationsInventor: Pamela G. Marrone
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Publication number: 20080293693Abstract: Disclosed herein is a method for preventing ovarian hyperstimulation syndrome in a subject by administering an effective amount of a dopamine agonist in a pharmaceutically acceptable carrier. Also disclosed herein is a method for treating ovarian hyperstimulation syndrome by administering an effective amount of a dopamine agonist in a pharmaceutically acceptable carrier.Type: ApplicationFiled: April 24, 2006Publication date: November 27, 2008Applicant: Ferring International Center S.A.Inventors: Antonio Pellicer-Martinez, Joan-Carles Arce, Carlos Simon-Valles, Raul Gomez-Gallego
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Publication number: 20080279961Abstract: It is demonstrated in the present invention that G-quadruplex ligands can be used to both shorten telomeres and inhibit telomerase by causing telomere uncapping. The invention relates to compositions and methods of treating cancer stem cells comprising the administration of G-quadruplex ligands, such as 3,11-difluoro-6,8,13-trimethyl-8H-quino[4,3,2-kl]acridinium methosulfate (RHPS4), which can effectively inhibit or reduce the growth of cancer stem cells. The invention also relates to a synergistic effect in inhibiting or reducing the growth cancer stem cells when a G-quadruplex ligand is combined with a mitotic spindle poison, such as paclitaxel, or other agents used in the treatment of cancer and disease. The invention also relates to RHPS4 inducing non-cancerous cell and non-cancerous stem cell proliferation.Type: ApplicationFiled: May 9, 2008Publication date: November 13, 2008Inventor: Angelika M. BURGER
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Publication number: 20080280885Abstract: The present invention relates to methods of and compositions for treating and relieving symptoms and disease associated with indications caused by a physiological drive to alleviate a sensation of anxiety. In one treatment method, methods of, and compositions for, modulating the expression of certain GABAA receptor subunits are used to treat anxiety-related disorders and depressive disorders associated with physiological tolerance to endogenous neurosteroids.Type: ApplicationFiled: April 7, 2006Publication date: November 13, 2008Applicant: Hythiam, INC.Inventors: Sanjay Sabnani, Donald Wesson
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Patent number: 7446110Abstract: Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner.Type: GrantFiled: September 2, 2004Date of Patent: November 4, 2008Assignee: Merck & Co., Inc.Inventors: Mildred L. Kaufman, Robert S. Meissner, Helen J. Mitchell
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Publication number: 20080261995Abstract: This invention relates to the combined use of a PDE5 inhibitor and a 5-alpha reductase antagonist in the treatment of lower urinary tract symptoms (LUTS), such as urgency, frequency, nocturia and urge incontinence.Type: ApplicationFiled: December 13, 2006Publication date: October 23, 2008Inventors: Carl Erik Johan Mastrell, Michael Allen Suesserman
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Publication number: 20080262016Abstract: The invention provides novel classes of Isoquinoline Derivatives. Pharmaceutical compositions and methods of making and using the compounds, are also described.Type: ApplicationFiled: June 16, 2008Publication date: October 23, 2008Applicant: Inotek Pharmaceuticals CorporationInventors: Prakash Jagtap, Erkan Baloglu, John H. van Duzer, Csaba Szabo, Andrew L. Salzman, Aloka Roy, William Williams, Alexander Nivorozhkin
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Publication number: 20080255097Abstract: The present invention relates to methods of and compositions for treating and relieving symptoms and disease associated with indications caused by a physiological drive to alleviate a sensation of anxiety. More specifically, the present invention relates to methods of and compositions for treating and relieving symptoms associated with substance abuse and withdrawal. The present invention relates to methods of and compositions for treating and relieving symptoms associated with addiction to antidepressants, opiates, nicotine or marijuana. In one method, a patient is treated with a composition that directly or indirectly modulates GABAA by modulating the expression of the GABAA receptor a4 subunit.Type: ApplicationFiled: April 7, 2006Publication date: October 16, 2008Applicant: Hythiam, Inc.Inventors: Sanjay Sabnani, Donald Wesson, Joseph Dunn
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Publication number: 20080242692Abstract: Substituted indenoisoquinolinium compounds, and pharmaceutical formulations of substituted indenoisoquinolinium compounds are described. Also described are processes for preparing substituted indenoisoquinolinium compounds. Also described are methods for treating cancer in mammals using the described substituted indenoisoquinolinium compounds or pharmaceutical formulations thereof.Type: ApplicationFiled: March 15, 2005Publication date: October 2, 2008Inventors: Mark S. Cushman, Alexandra S. Ioanoviciu, Yves G. Pommier
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Publication number: 20080214593Abstract: The present invention relates to Tetracyclic Amino Compounds and Tetracyclic Carboxamido Compounds, compositions comprising an effective amount of a Tetracyclic Amino Compound or a Tetracyclic Carboxamido Compound and methods for treating or preventing an inflammatory disease, a reperfusion injury, diabetes, a diabetic complication, reoxygenation injury resulting from organ transplantation, an ischemic condition, Parkinson's disease, renal failure, a vascular disease, a cardiovascular disease, or cancer, comprising administering to a subject in need thereof an effective amount of a Tetracyclic Amino Compound or a Tetracyclic Carboxamido Compound.Type: ApplicationFiled: December 19, 2007Publication date: September 4, 2008Inventors: Prakash JAGTAP, Csaba Szabo
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Publication number: 20080214576Abstract: Compositions and methods for treating cancer and other hyperproliferatice disease conditions with topoisomerase inhibitors and their prodrugs are disclosed.Type: ApplicationFiled: November 27, 2005Publication date: September 4, 2008Applicant: Threshold Pharmaceuticals, Inc.Inventors: Mark Matteucci, Jian-Xin Duan, Photon Rao
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Publication number: 20080207601Abstract: Compositions for reducing dependency and addiction to substances of abuse are provided. Chloride channels such as the GABAA receptors are altered under conditions of dependency and withdrawal such that the electrophysiological properties of the GABAA receptor containing neurons are altered thereby providing a pathophysiological condition resulting in symptoms of dependency and withdrawal such as anxiety. Specifically, under conditions of withdrawal the relative ratio of the a1 receptor subunit decreases relative to the a4 receptor subunit. Endogenous neurosteroid production is also associated with the molecular changes underlying the alterations of GABA-gated chloride channels. Compositions of at least two compounds including at least one inhibitor of neurosteroid production are useful for treating the pathophysiology of addiction, dependency and substance abuse withdrawal.Type: ApplicationFiled: April 6, 2006Publication date: August 28, 2008Applicant: Hythiam , Inc.Inventor: Sanjay Sabnani
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Publication number: 20080200376Abstract: The present invention relates to methods of treating and preventing obesity and obesity-related disorders in a subject comprising administering a neurokinin-1 antagonist and an anti-obesity agent, such as a melanocortin 4 receptor agonist, to said subject. The present invention further related to methods of treating or preventing sexual dysfunction, including male erectile dysfunction, in a subject comprising administering a neurokinin-1 antagonist and a sexual dysfunction therapeutic agent, such as a melanocortin 4 receptor agonist, to said subject. The present invention further provides for pharmaceutical compositions and medicaments useful in carrying out these methods.Type: ApplicationFiled: October 25, 2005Publication date: August 21, 2008Inventors: Malcolm MacCoss, Duncan E. MacIntyre, Alison M. Strack
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Patent number: 7410977Abstract: Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and 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, benign prostatic hyperplasia (BPH), cancer cachexia, Alzheimer's disease, muscular dystrophies, cognitive decline, sexual dysfunction, sleep apnea, depression, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.Type: GrantFiled: April 22, 2005Date of Patent: August 12, 2008Assignee: Merck & Co., Inc.Inventors: Robert S. Meissner, James J. Perkins
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Publication number: 20080188509Abstract: It is intended to provide pergolide-containing transdermal preparations having reduced side effects and exerting sufficient therapeutic effects. Namely, a pergolide-containing transdermal preparation which is capable of achieving a plasma AUC ratio of pergolide or the like to at least one pergolide metabolite of 1:0.5 to 1:5; and/or transdermal preparation containing pergolide and/or a pharmaceutically acceptable salt thereof which is capable of achieving a ratio (A/B) of the maximum plasma level (A) of pergolide and/or a pharmaceutically acceptable salt thereof to the plasma level (B) thereof in the next administration of less than 2.Type: ApplicationFiled: March 31, 2008Publication date: August 7, 2008Inventors: Arata TOSHIMITSU, Kazunosuke AIDA, Takaaki TERAHARA, Naruhito HIGO
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Publication number: 20080176887Abstract: A method for decreasing nicotine and other substance use in humans is disclosed. Tetrahydroberberine (THB) and its analogs, l-Tetrahydropalmatine (l-THP) and l-Stepholidine (l-SPD), are present in and can be isolated from several plants in the Magnoliidae superorder. According to the disclosed method, THB and its analogs are used to block nicotine-induced DA release, and modulate heterologous or homoeric expression of human nicotinic acetylcholine receptors (nAChR) in humans. Specifically, THB exhibits bi-directory modulation of ?4?2-nAChR-mediated currents induced by nicotine. THB also shows predominant inhibition on homologously expressed ?7-nAChR function. Thus, according to the disclosed method, THB is used to simultaneous blockade midbrain DA system function, the brain reward center, and neuronal ?4?2- and ?7-nAChR function, the major nicotine targets in the brain. Therefore, THB and its analogs serve as a novel class of natural compounds to decrease nicotine dependence in humans.Type: ApplicationFiled: January 11, 2008Publication date: July 24, 2008Applicant: ARIZONA HEALTH CONSULTING GROUP, LLCInventor: Jie Wu
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Publication number: 20080175932Abstract: A method for decreasing nicotine and other substance use in humans is disclosed. Tetrahydroberberine (THB) and its analogs, l-Tetrahydropalmatine (l-THP) and l-Stepholidine (l-SPD), are present in and can be isolated from several plants in the Magnoliidae superorder. According to the disclosed method, THB and its analogs are used to block nicotine-induced DA release, and modulate heterologous or homoeric expression of human nicotinic acetylcholine receptors (nAChR) in humans. Specifically, THB exhibits bi-directory modulation of ?4?2-nAChR-mediated currents induced by nicotine. THB also shows predominant inhibition on homologously expressed ?7-nAChR function. Thus, according to the disclosed method, THB is used to simultaneous blockade midbrain DA system function, the brain reward center, and neuronal ?4?2- and ?7-nAChR function, the major nicotine targets in the brain. Therefore, THB and its analogs serve as a novel class of natural compounds to decrease nicotine dependence in humans.Type: ApplicationFiled: January 11, 2008Publication date: July 24, 2008Applicant: ARIZONA HEALTH CONSULTING GROUP, LLCInventor: Jie Wu
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Publication number: 20080171096Abstract: A method for decreasing nicotine and other substance use in humans is disclosed. Tetrahydroberberine (THB) and its analogs, l-Tetrahydropalmatine (l-THP) and l-Stepholidine (l-SPD), are present in and can be isolated from several plants in the Magnoliidae superorder. According to the disclosed method, THB and its analogs are used to block nicotine-induced DA release, and modulate heterologous or homoeric expression of human nicotinic acetylcholine receptors (nAChR) in humans. Specifically, THB exhibits bi-directory modulation of ?4?2-nAChR-mediated currents induced by nicotine. THB also shows predominant inhibition on homologously expressed ?7-nAChR function. Thus, according to the disclosed method, THB is used to simultaneous blockade midbrain DA system function, the brain reward center, and neuronal ?4?2- and ?7-nAChR function, the major nicotine targets in the brain. Therefore, THB and its analogs serve as a novel class of natural compounds to decrease nicotine dependence in humans.Type: ApplicationFiled: January 11, 2008Publication date: July 17, 2008Applicant: ARIZONA HEALTH CONSULTING GROUP, LLCInventor: Jie Wu
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Publication number: 20080167317Abstract: This invention relates to combination therapy for the treatment of lower urinary tract symptoms (LUTS) associated with or without benign prostatic hyperplasia (BPH). The combination therapy comprises of tailored 1 adrenoceptor antagonist, which is selective for 1a over 1b subtype but non-selective for 1a over 1d subtype, in combination with muscarinic receptor antagonist, preferably bladder selective antagonist and optionally included 5-reductase inhibitor for relief of LUTS in a mammal with or without BPH.Type: ApplicationFiled: March 23, 2004Publication date: July 10, 2008Inventors: Anita Chugh, Mohammad Salman, Atul Tiwari, Gowri R. Shankar, Sandeep Sinha
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Publication number: 20080152731Abstract: The invention encompasses a formulation for hair loss prevention comprising a mixture of water and at least one nonpolar aprotic organic solvent and at least one hair loss preventive ingredient known to inhibit the hormonal mechanism underlying androgenetic hair loss and methods of using the same.Type: ApplicationFiled: October 26, 2007Publication date: June 26, 2008Inventor: Giuseppe Trigiante
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Patent number: 7381722Abstract: The present invention relates to Tetracyclic Amino Compounds and Tetracyclic Carboxamido Compounds, compositions comprising an effective amount of a Tetracyclic Amino Compound or a Tetracyclic Carboxamido Compound and methods for treating or preventing an inflammatory disease, a reperfusion injury, diabetes, a diabetic complication, reoxygenation injury resulting from organ transplantation, an ischemic condition, Parkinson's disease, renal failure, a vascular disease, a cardiovascular disease, or cancer, comprising administering to a subject in need thereof an effective amount of a Tetracyclic Amino Compound or a Tetracyclic Carboxamido Compound.Type: GrantFiled: February 15, 2006Date of Patent: June 3, 2008Assignee: Inotek Pharmaceuticals CorporationInventors: Prakash Jagtap, Csaba Szabo
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Publication number: 20080125399Abstract: Compounds of structural formula (I) are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and 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, benign prostatic hyperplasia (BPH), cancer cachexia, Alzheimer's disease, muscular dystrophies, cognitive decline, sexual dysfunction, sleep apnea, depression, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.Type: ApplicationFiled: April 4, 2005Publication date: May 29, 2008Inventors: Jiabing Wang, Carol A. McVean
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Patent number: 7354926Abstract: The invention concerns novel molecules derived from noraporphine, as well as cosmetic and dermopharmaceutical compositions containing one or several of said derivatives, alone or combined with a plant extract, in particular glaucium flavum, and particularly preparations for reducing pigmentation, with anti-ageing effect or for slimming.Type: GrantFiled: July 29, 2003Date of Patent: April 8, 2008Assignee: Sederma SASInventor: Karl Lintner
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Patent number: 7351698Abstract: Compounds of structural formula (I) as herein defined are disclosed as useful in a method for modulating the androgen receptor in a tissue selective manner in a patient in need of such modulation, as well as in a method of agonizing the androgen receptor in a patient, and in particular the method wherein the androgen receptor is antagonized in the prostate of a male patient or in the uterus of a female patient and agonized in bone and/or muscle tissue.Type: GrantFiled: May 3, 2004Date of Patent: April 1, 2008Assignee: Merck & Co., Inc.Inventors: Robert S. Meissner, James J. Perkins
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Publication number: 20080069791Abstract: The present invention relates to the use of IL-15 polynucleotides, polypeptides or compounds which bind to an antibody which specifically recognizes the IL-15 polypeptide or which specifically bind to an IL-15 receptor alpha chain for the preparation of a composition for stimulating hair growth or for treating, preventing and/or ameliorating hair loss. Moreover the present invention encompasses a transgenic non-human animal comprising an IL-15 polynucleotide. The present invention also relates to a method for stimulating hair growth in a non-human animal and to methods for manufacturing animal hair. Finally, the present invention relates to a method of treating, preventing and/or ameliorating a subject which suffers from hair loss.Type: ApplicationFiled: December 7, 2004Publication date: March 20, 2008Applicant: Universitaetsklinikum MuensterInventor: Stefan Beissert
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Patent number: 7332503Abstract: New aporphine derivatives are disclosed which have formula (I) and the physiologically acceptable salts thereof. Said derivatives may be used for the treatment of Parkinson's disease, hemicrania, restless legs syndrome (RLS), sexual dysfunction in men and women, hyperprolactemia and psychotic disorders, and/or evaluation of Parkinson's disease. Processes for the preparation of such derivatives are also disclosed.Type: GrantFiled: February 22, 2005Date of Patent: February 19, 2008Assignee: Axon Biochemicals B.V.Inventors: Hakan Wikstrom, Durk Dijkstra, Thomas Cremers, Per Erik Andren, Sandrine Marchais, Ulrik Jurva
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Patent number: 7329750Abstract: 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.Type: GrantFiled: June 25, 2004Date of Patent: February 12, 2008Assignee: Merck & Co., Inc.Inventors: William P. Danulich, Robert S. Meissner, Helen J. Mitchell
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Patent number: 7323566Abstract: A novel group of apomorphine derivatives are provided that are well suited as radioimaging agents upon incorporation of radionuclides. Through reaction of D ring sites, the less reactive sites of the apomorphine A ring is modified in ways previously unattainable.Type: GrantFiled: April 20, 2005Date of Patent: January 29, 2008Inventor: Crist N. Filer
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Patent number: 7312228Abstract: The synthesis and biological activity of benzoisoindoloisoquinolone compounds are described. The synthesis and biological activity of C-11-substituted indenoisoquinolones are also described. Indenoisoquinolones substituted at C-11 are prepared by McMurry reactions of 11-ketoindenoisoquinolones with aldehydes.Type: GrantFiled: May 11, 2004Date of Patent: December 25, 2007Assignees: Purdue Research Foundation, The United States of America as represented by the Secretary of the Department of Health and Human ServicesInventors: Mark S. Cushman, Yves G. Pommier
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Patent number: 7312229Abstract: 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.Type: GrantFiled: October 27, 2004Date of Patent: December 25, 2007Assignee: Merck & Co., Inc.Inventors: William P. Dankulich, Helen J. Mitchell
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Patent number: 7276513Abstract: There is provided a compound of formula XII, wherein G is H or a substituent, and wherein R1 is a sulphamate group.Type: GrantFiled: January 11, 2006Date of Patent: October 2, 2007Assignee: Sterix, Ltd.Inventors: Barry Victor Lloyd Potter, Michael John Reed, Lok Wai Lawrence Woo
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Patent number: 7238705Abstract: New aporphine derivatives are disclosed which have formula (I) and the physiologically acceptable salts thereof. Said derivatives may be used for the treatment of Parkinson's disease, hemicrania, restless legs syndrome (RLS), sexual dysfunction in men and women, hyperprolactemia and psychotic disorders, and/or evaluation of Parkinson's disease. Processes for the preparation of such derivatives are also disclosed.Type: GrantFiled: July 20, 2001Date of Patent: July 3, 2007Assignee: Axon Biochemicals B.V.Inventors: Hakan Wikstrom, Durk Dijkstra, Thomas Cremers, Per Erik Andren, Sandrine Marchais, Ulrik Jurva
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Patent number: 7220754Abstract: Mono-ester and asymmetrically substituted diesters of dihydrexidine, dinapsoline and A-86929 and substituted derivatives thereof are described. The novel ester/diester derivatives exhibit improved pharmacokinetic characteristics relative to their unesterified parent compounds and can be formulated into pharmaceutical compositions useful for the treatment of a wide variety of dopamine related disorders.Type: GrantFiled: February 14, 2003Date of Patent: May 22, 2007Assignee: DarPharma, Inc.Inventors: Durk Dijkstra, Hakan Wikstrom
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Patent number: 7217720Abstract: 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.Type: GrantFiled: September 2, 2004Date of Patent: May 15, 2007Assignee: Merck & Co., Inc.Inventors: Robert S. Meissner, Helen J. Mitchell
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Patent number: 7217709Abstract: The invention relates to Tetracyclic Benzamide Derivatives; compositions comprising a Tetracyclic Benzamide Derivative; and methods for treating or preventing an inflammatory disease, a reperfusion disease, an ischemic condition, renal failure, diabetes, a diabetic complication, a vascular disease, or cancer, comprising administering to a subject in need thereof an effective amount of a Tetracyclic Benzamide Derivative.Type: GrantFiled: February 26, 2004Date of Patent: May 15, 2007Assignee: Inotek Pharmaceuticals CorporationInventors: Prakash Jagtap, Csaba Szabo
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Patent number: 7208492Abstract: The invention provides compounds of formula I or formula II: wherein: the bond represented by --- is a single bond or a double bond, and R1–R5, X, and Y have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I or II, processes for preparing compounds of formula I or II, intermediates useful for preparing compounds of formula I or II, and therapeutic methods for treating cancer and other topoisomerase related conditions using compounds of formula I or II.Type: GrantFiled: May 3, 2005Date of Patent: April 24, 2007Assignee: Rutgers, The State University of New JerseyInventors: Edmond J. LaVoie, Alexander L. Ruchelman, Leroy F. Liu
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Patent number: 7186728Abstract: 17-methylene-4-azasteroid compounds of formula I: wherein R20 denotes fluoro, chloro or bromo R20a denotes hydrogen, R10 and R4 each denote a hydrogen atom or a methyl group, and R1 and R2 each denote a hydrogen atom or together denote an additional bond, are useful for treating diseases or conditions caused by excessive androgen levels, such as acne, prostate diseases, alopecia and hirsutism, as well as gynecological conditions. Methods of synthesizing the new 17-methylene-4-azasteroid compounds are described.Type: GrantFiled: August 28, 2002Date of Patent: March 6, 2007Assignee: Schering AGInventors: Bernd Menzenbach, Peter Droescher, Alexander Hillisch, Walter Elger, Hans-Udo Schweikert, Klaus Schoellkopf
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Patent number: 7138389Abstract: This invention provides methods of treating a mammalian subject in need of androgen therapy by orally administering to the subject testosterone, a testosterone ester, or a testosterone precursor in an oil vehicle and by administering to the subject a modulator such as finasteride or dutasteride which increases testosterone bioavailability in the subject.Type: GrantFiled: November 15, 2004Date of Patent: November 21, 2006Assignee: University of WashingtonInventors: John K. Amory, William J. Bremner
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Patent number: 7122534Abstract: The present invention relates to compounds of formula (I) and their pharmaceutically acceptable salts, wherein R1, R2, R3 and Z are as defined herein, intermediates in the synthesis of such compounds, pharmaceutical compositions containing such compounds and methods of using such compounds in the treatment of neurological and psychological disorders.Type: GrantFiled: January 23, 2004Date of Patent: October 17, 2006Assignee: Pfizer IncInventor: Jotham Wadsworth Coe
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Patent number: 7098218Abstract: There is provided a compound having Formula (I) wherein G is H or a substituent, and wherein R1 is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group, capable of inhibiting steroid sulphatase.Type: GrantFiled: April 16, 2004Date of Patent: August 29, 2006Assignee: Sterix LimitedInventors: Barry Victor Lloyd Potter, Michael John Reed, Lok Wai Lawrence Woo
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Patent number: 7091212Abstract: The present invention relates to the preparation of the optical isomer (R)-(+)-8,9-dihydroxy-2,3,7,11b-tetrahydro-1H-napth[1,2,3-de]isoquinoline. This invention also relates to the use of pharmaceutical compositions comprising (R)-(+)-8,9-dihydroxy-2,3,7,11b-tetrahydro-1H-napth[1,2,3-de]isoquinoline for use for the treatment of movement disorders.Type: GrantFiled: August 8, 2002Date of Patent: August 15, 2006Assignee: Purdue Research FoundationInventor: Sing-Yuen Sit
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Patent number: 7071158Abstract: A method to enhance the cytotoxic activity of an antineoplastic drug comprising administering an effective amount of the antineoplastic drug to a host exhibiting abnormal cell proliferation in combination with an effective cytotoxicity-increasing amount of an antioxidant. The invention also includes a method to decrease the toxicity to an antineoplastic agent or increase the therapeutic index of an antineoplastic agent administered for the treatment of a solid growth of abnormally proliferating cells, comprising administering an antioxidant prior to, with, or following the antineoplastic treatment.Type: GrantFiled: February 7, 2001Date of Patent: July 4, 2006Assignee: Atherogenics, Inc.Inventors: Rebecca Chinery, R. Daniel Beauchamp, Robert J. Coffey, Russell M. Medford, Brian E. Wadzinski
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Patent number: 7057044Abstract: The invention provides aporphine and oxoaporphine compounds that have endothelial nitric oxide synthase (eNOS) maintaining or enhancing activities and may be used to manufacture a medicaments for preventing or treating ischemic diseases in human and mammal, and the ischemic diseases may include ischemic cerebral apoplexy, ischemic cerebral thrombosis, ischemic cerebral embolism, hypoxic ischemic encephlopathy, ischemic cardiac disease or ischemic enteropathy etc.Type: GrantFiled: April 2, 2004Date of Patent: June 6, 2006Assignee: Lotus Pharmaceutical Co., Ltd.Inventors: MingJai Su, ShoeiSheng Lee
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Patent number: 7022854Abstract: A crystalline Form II of 17?-N-[2,5-bis (trifluoromethyl)phenyl]carbamoyl-4-aza-5-?-androst-1-en-3-one (dutasteride) is provided. The preferred crystalline Form II of dutasteride has an X-ray powder diffraction pattern, expressed in terms of d-spacing (in ° A), with peaks at about 13.42, 6.96, 6.13, 5.27, 4.77, 4.70, 4.58, 4.46 and 3.82. A process for preparation of a crystalline Form II of dutasteride is also provided and includes dissolving a crude form of dutasteride in an alcoholic solvent having from 1 to 5 carbon atoms; removing the alcoholic solvent to obtain a residue; adding an ester solvent to the residue; and filtering the resulting separated solids. The processes of the invention are believed to be simple, eco-friendly, and commercially viable.Type: GrantFiled: July 17, 2003Date of Patent: April 4, 2006Assignees: Dr. Reddy's Laboratories, Limited, Dr. Reddy's Laboratories, Inc.Inventors: Manne Satyanarayana Reddy, Chakilam Nagaraju, Gudipati Srinivasulu, Mandava Venkata Naga Brahmeshwar Rao, Bojja Ramachandra Reddy, Singamsetty Radhakrishna
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Patent number: 6992088Abstract: The invention provides compounds of formula I: wherein: R1-R5, “a” and X have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for treating cancer using compounds of formula I.Type: GrantFiled: August 11, 2003Date of Patent: January 31, 2006Assignee: Rutgers, The State University of New JerseyInventors: Edmond J. LaVoie, Sudhir K. Singh, Leroy F. Liu
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Patent number: 6956035Abstract: The invention provides novel classes of Isoquinoline Derivatives. Pharmaceutical compositions and methods of making and using the compounds, are also described.Type: GrantFiled: February 28, 2003Date of Patent: October 18, 2005Assignee: Inotek Pharmaceuticals CorporationInventors: Prakash Jagtap, Erkan Baloglu, John H. van Duzer, Csaba Szabo, Andrew L. Salzman
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Patent number: RE39056Abstract: Compounds of structural Formula (I) and pharmacologically acceptable salts and esters thereof possess 5?-reductase inhibitory activity. These compounds inhibit 5?-reductase type 1 and type 2. The compounds of structural Formula I are useful in the systemic, including oral, and parenteral, including topical, treatment and prevention of hyperandrogenic conditions including prostatic carcinoma, benign prostatic hyperplasia, acne vulgaris, seborrhea, androgenic alopecia (also called androgenetic alopecia) which includes male- and female-pattern baldness, female hirsutism, and prostatitis. A class of compounds of the present invention are also potent antiandrogens. The present invention also relates to novel compositions containing such compounds, methods of their use and methods of their manufacture.Type: GrantFiled: September 11, 1996Date of Patent: April 4, 2006Assignee: Merck & Co, Inc.Inventors: Raman K. Bakshi, Soumya P. Sahoo, Richard L. Tolman