Plural Morpholine Rings Attached Directly Or Indirectly To Each Other By Nonionic Bonding Patents (Class 514/231.8)
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Methods and compositions for the treatment or prevention of abnormal bone formation in a soft tissue
Patent number: 10369152Abstract: Provided herein are methods and compositions for the treatment and/or prevention of abnormal bone formation in a soft tissue. In certain embodiments, the methods and compositions treat and/or prevent a disease or disorder comprising abnormal bone formation in soft tissue. Exemplary diseases or disorders that can be treated with the methods and compositions described herein include, but are not limited to, heterotopic ossification diseases such as fibrodysplasia ossificans progressive, anklyosing spondylosis, traumatic heterotopic ossification, burn- or blast-injury associated heterotopic ossification, and joint replacement surgery associated heterotopic ossification.Type: GrantFiled: February 12, 2016Date of Patent: August 6, 2019Assignee: THE BRIGHAM AND WOMEN'S HOSPITAL, INC.Inventors: Paul B. Yu, Jana Bagarova, Devaveena Dey -
Patent number: 9458086Abstract: Modified stilbenoids and formulations thereof are provided. The modified stilbenoids can include one or more amino or amino-alkyl substituents. The formulation can be for the treatment or prevention of obesity and the modified stilbenoid present in an effective amount to alleviate or prevent the onset of one or more symptoms of obesity. Methods of making the modified stilbenoids and formulations thereof are provided. Methods are provided for treating a subject with a modified stilbenoid in an effective amount to alleviate or prevent one or more symptoms associated with diabetes, cardiovascular disease, high blood pressure, deep vein thrombosis, osteoarthritis, obstructive sleep apnea, cancer, and non-alcoholic fatty liver disease. The administration of the modified stilbenoids can result in decreased levels of PKC?II, PKC?VIII, substantially unaltered expression of PKC?I; a decreased number of adipocytes; increased weight and/or fat loss; or a combination thereof.Type: GrantFiled: July 2, 2014Date of Patent: October 4, 2016Assignees: University of South Florida (A Florida Non-Profit Corporation), The United States of America as Represented by the Department of Veterans Affairs Office of General Counsel—PSG IV (024)Inventors: Niketa A. Patel, Rekha S. Patel, Kirpal S. Bisht
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Patent number: 9067875Abstract: Disclosed are nordihydroguaiaretic acid derivative compounds including various end groups bonded by a carbon atom or heteroatom though a side chain bonded to the respective hydroxy residue O groups by an ether bond or a carbamate bond, pharmaceutical compositions, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, a metabolic disease, such as diabetes, a vascular disease, such as hypertension and macular degeneration, or a proliferative disease, such as diverse types of cancers.Type: GrantFiled: May 14, 2012Date of Patent: June 30, 2015Assignee: ERIMOS PHARMACEUTICALS LLCInventors: Qingqi Chen, Rocio Alejandra Lopez, Jonathan Daniel Heller, Amanda Jean Morris
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Publication number: 20150141417Abstract: Disclosed are nordihydroguaiaretic acid derivative compounds including various end groups bonded by a carbon atom or heteroatom though a side chain bonded to the respective hydroxy residue O groups by an ether bond or a carbamate bond, pharmaceutical compositions, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, a metabolic disease, such as diabetes, a vascular disease, such as hypertension and macular degeneration, or a proliferative disease, such as diverse types of cancers.Type: ApplicationFiled: May 14, 2012Publication date: May 21, 2015Inventors: Qingqi Chen, Rocio Alejandra Lopez, Jonathan Daniel Heller, Amanda Jean Morris
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Patent number: 8952006Abstract: Morpholinoalkyl fumarates, pharmaceutical compositions comprising the morpholinoalkyl fumarates, and methods of using morpholinoalkyl fumarates and pharmaceutical compositions for treating neurodegenerative, inflammatory, and autoimmune disorders including multiple sclerosis, psoriasis, irritable bowel disorder, ulcerative colitis, arthritis, chronic obstructive pulmonary disease, asthma, Parkinson's disease, Huntington's disease, and amyotrophic lateral sclerosis are disclosed.Type: GrantFiled: February 7, 2013Date of Patent: February 10, 2015Assignee: XenoPort, Inc.Inventors: Kenneth C. Cundy, Suresh K. Manthati, David J. Wustrow
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Publication number: 20140309185Abstract: This document relates to inhibitors of G protein coupled receptor 6 kinase (GRK6) polypeptides as well as methods and materials for using such inhibitors to treat hematological malignancies, inflammation diseases, and autoimmune disorders.Type: ApplicationFiled: October 26, 2012Publication date: October 16, 2014Inventors: Alexander Keith Stewart, Artem Plekhov, Robert Greenhouse
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Publication number: 20140243324Abstract: The present invention relates to uses of small molecule mimetics of hematopoietic growth factors. In particular the present invention relates to uses of small molecule mimetics of erythropoietin.Type: ApplicationFiled: November 17, 2011Publication date: August 28, 2014Applicant: LIGAND PHARMACEUTICALS INCORPORATEDInventors: Reid P. Bissonnette, Andrew R. Hudson, Keith B. Marschke, Deepa Rungta, Lin Zhi
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Publication number: 20140206629Abstract: The invention relates to inhibition of SDF-1? expression in subacromial bursa cells by CXCR-4 inhibitors. Bursal cell migration in response to SDF-? stimulation is also decreased in the presence of CXCR4 inhibitors. Accordingly, provided are methods for treating or ameliorating a musculoskeletal disorder.Type: ApplicationFiled: February 17, 2012Publication date: July 24, 2014Applicant: RHODE ISLAND HOSPITALInventor: Theodore A. Blaine
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Publication number: 20140187546Abstract: Cystine analogs that improve the solubility of L-cystine in urine for treatment of cystinuria and which have the structure: and pharmaceutically acceptable salts, solvates and prodrugs thereof, wherein each R and R? pair are independently selected from (i) or (ii); (i) R and R? are independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alcohol, substituted or unsubstituted aryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocyclic, and substituted or unsubstituted heteroaryl, or (ii) R and R? together form a substituted or unsubstituted heterocyclic ring structure, or a substituted or unsubstituted heteroaryl ring structure; X is hydrogen, or an alkyl; and Y is O or S.Type: ApplicationFiled: January 2, 2014Publication date: July 3, 2014Applicant: Rutgers, The State University of New JerseyInventors: Longqin Hu, Amrik Sahota
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Publication number: 20140142067Abstract: The present invention is directed to use of a series of compounds and compositions comprising the same for activating telomerase and treating diseases, disorders and/or conditions related thereto.Type: ApplicationFiled: November 12, 2013Publication date: May 22, 2014Applicant: BEN-GURION UNIVERSITY OF THE NEGEV RESEARCH AND DEVELOPMENT AUTHORITYInventors: Aviv GAZIT, Shimon SLAVIN, Esther PRIEL, Sara YITZCHAK
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Publication number: 20130303531Abstract: Disclosed are nordihydroguaiaretic acid derivative compounds including various end groups bonded by a carbon atom or heteroatom though a side chain bonded to the respective hydroxy residue O groups by an ether bond or a carbamate bond, pharmaceutical compositions, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, a metabolic disease, such as diabetes, a vascular disease, such as hypertension and macular degeneration, or a proliferative disease, such as diverse types of cancers.Type: ApplicationFiled: May 14, 2012Publication date: November 14, 2013Inventors: Qingqi Chen, Rocio Alejandra Lopez, Jonathan Daniel Heller, Amanda Jean Morris
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Patent number: 8546386Abstract: Provided are additives of formula I for use in hydrocarbonaceous compositions, such as petroleum or liquid fuels: (I) wherein R1, R2, R3, R4, and R5 are as defined herein. The additives improve the corrosion resistance of the compositions. The additives also enhance the antimicrobial efficacy of any added biocides contained in such compositions.Type: GrantFiled: April 29, 2009Date of Patent: October 1, 2013Inventors: G. David Green, Sheila M. Tinetti, Patrick E. Brutto, John Pohlman
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Publication number: 20130203753Abstract: Morpholinoalkyl fumarates, pharmaceutical compositions comprising the morpholinoalkyl fumarates, and methods of using morpholinoalkyl fumarates and pharmaceutical compositions for treating neurodegenerative, inflammatory, and autoimmune disorders including multiple sclerosis, psoriasis, irritable bowel disorder, ulcerative colitis, arthritis, chronic obstructive pulmonary disease, asthma, Parkinson's disease, Huntington's disease, and amyotrophic lateral sclerosis are disclosed.Type: ApplicationFiled: February 7, 2013Publication date: August 8, 2013Applicant: XENOPORT, INC.Inventor: XENOPORT, INC.
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Publication number: 20130203745Abstract: The present invention relates to bisaryl(thio)morpholine derivatives of the formula (I) wherein R1 is an aryl substitutent selected from phenyl, pyridyl, pyrimidinyl, biphenyl and naphthyl, each optionally substituted with one or more substituents independently selected from halogen, (1-6C)alkyl optionally substituted with one or more fluoro atoms, (1-4C)alkoxy optionally substituted with one or more fluoro atoms, amino, di(1-4C)alkylamino, —SO2-(1-4C)alkyl, —CO-(1-4C)alkyl, —CO—O-(1-4C)alkyl and —NH—CO-(1-4C)alkyl, or substituted with phenoxy, benzyl, benzyloxy, phenylethyl or morpholinyl, each optionally substituted with (1-4C)alkyl, and (8-10C)bicyclic group, bicyclic heterocycle, each optionally substituted with (1-4C)alkyl optionally substituted with one or more fluoro atoms or oxo; A is selected from —CO—, —NH—, —O—, —S—, —SO— or —SO2—; ring structure B optionally contains one nitrogen atom; R2 is H, (1-4C)alkyl optionally substituted with one or more fluoro atoms, (1-4C)alkoxy optionally substitType: ApplicationFiled: July 8, 2011Publication date: August 8, 2013Applicant: AbbVie B.V.Inventors: Wouter I. Iwema Bakker, Raymond Bronger
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Publication number: 20130071444Abstract: Amphiphilic cationic polymers comprising a biocompatible amphiphile linked to an organic cation are provided. The polymers complex with therapeutic agents and facilitate delivery of such therapeutic agents, particularly therapeutic nucleic acids, both in vitro and in vivo. Accordingly, the invention further provides methods of facilitating delivery of therapeutic and/or diagnostic agents to a cell and methods of treating a condition, such as a disease or infection, in an organism using the amphiphilic cationic polymers of the invention.Type: ApplicationFiled: September 14, 2012Publication date: March 21, 2013Applicant: The Charlotte-Mecklenburg Hospital Authority d/b/a Carolinas HealthCare SystemInventors: Mingxing Wang, Qilong Lu, Bo Wu, Peijuan Lu
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Publication number: 20130065842Abstract: Heterocyclic compounds, and pharmaceutical compositions thereof, are disclosed as ROR?t modulators that have a formula represented by the following: and wherein n1, n2, R1, R2, R3, and R4 are as described herein. These compounds may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune disorders, cancer, and graft-versus-host disease.Type: ApplicationFiled: March 11, 2011Publication date: March 14, 2013Inventors: Dan Littman, Jun R. Huh, Wenwei Huang, Ruili Huang
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Publication number: 20130053378Abstract: The present invention relates to nordihydroguaiaretic acid derivative compounds, namely, butane bridge modified nordihydroguaiaretic acid (NDGA) compounds and butane bridge modified tetra-O-substituted NDGA compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, metabolic diseases, such as diabetes and hypertension, or a proliferative disease, such as diverse types of cancers.Type: ApplicationFiled: July 30, 2012Publication date: February 28, 2013Applicant: Erimos Pharmaceuticals LLCInventors: Qingqi Chen, Jonathan Daniel Heller, Rocio Alejandra Lopez, Amanda Jean Morris
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Publication number: 20120149673Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases, disorders or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: February 17, 2012Publication date: June 14, 2012Applicant: CalciMedica, Inc.Inventors: Jeffrey P. Whitten, Yazhong Pei, Kenneth A. Stauderman, Jack Roos
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Publication number: 20120129837Abstract: Chemical agents, such as disulfonamide derivatives of fluorene, anthracene, xanthene, dibenzosuberone and acridine, and similar heterocyclic ring structures, including salts thereof, that act as anti-cancer and anti-tumor agents, especially where such agents modulate the activity of the Wnt/?-catenin signaling pathway, and serve to reduce ?-catenin levels present in cells, such as cancer cells, or where the agents modulate levels of gene expression in cellular systems, including cancer cells, are disclosed, along with methods for preparing such agents, as well as pharmaceutical compositions containing such agents as active ingredients and methods of using these as therapeutic agents.Type: ApplicationFiled: January 30, 2012Publication date: May 24, 2012Inventors: Wieslaw M. Cholody, Yi Zang, Norman E. Ohler, Sheela Chellappan, Janak Padia, Karina Zuck, Jeffrey W.H. Watthey, Zoe Ohler, Jeffrey Strovel
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Patent number: 8178527Abstract: Disclosed are nordihydroguaiaretic acid derivative compounds including various end groups bonded by a carbon atom or heteroatom though a side chain bonded to the respective hydroxy residue O groups by an ether bond or a carbamate bond, pharmaceutical compositions, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, a metabolic disease, such as diabetes, a vascular disease, such as hypertension and macular degeneration, or a proliferative disease, such as diverse types of cancers.Type: GrantFiled: October 2, 2007Date of Patent: May 15, 2012Assignee: Erimos Pharmaceuticals LLCInventors: Qingqi Chen, Rocio Alejandra Lopez, Jonathan Daniel Heller, Amanda Jean Morris
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Publication number: 20120040976Abstract: Disclosed are methods for identifying individuals suffering from a CNS disorder (including Alzheimer's Disease, ALS, behavioral disorders, and the like) that could be treated with a CNS drug with greater therapeutic efficacy and lower side effects and the compounds useful for such treatment. Also disclosed are methods for predicting the efficacy of a drug candidate for the treatment of a CNS disorder. The technology is also applicable to drug discovery for evaluation in animal models of neurodegenerative diseases.Type: ApplicationFiled: December 11, 2009Publication date: February 16, 2012Applicant: HUMAN BIOMOLECULAR RESEARCH INSTITUTEInventors: John R. Cashman, Kenneth J. Abel
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Publication number: 20110301159Abstract: The disclosure relates to novel compounds that are capable of modulating Jak2 kinase activities, compounds that have therapeutic use in treating or preventing a subject suffering from or susceptible to a Jak2 mediated disease or disorder, and methods of use and compositions thereof.Type: ApplicationFiled: December 9, 2009Publication date: December 8, 2011Applicants: UNIVERSITY OF SOUTH FLORIDA, UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC.Inventors: Peter P. Sayeski, Gyorgy M. Keseru, Kirpal Bisht
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Publication number: 20110281850Abstract: Intracellular kinase inhibitors and their therapeutic uses for patients with T cell malignancies, B cell malignancies, autoimmune disorders, and transplanted organs.Type: ApplicationFiled: July 7, 2011Publication date: November 17, 2011Applicant: MANNKIND CORPORATIONInventors: Gary A. Flynn, Sandra Aeyoung Lee, Mary Faris, David William Brandt, Subrata Chakravarty
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Publication number: 20110135650Abstract: The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt or a solvate thereof. The present invention also provides pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.Type: ApplicationFiled: June 1, 2010Publication date: June 9, 2011Inventors: Samuel CHACKALAMANNIL, Tin-Yau CHAN, Mariappan V. CHELLIAH, Martin C. CLASBY, Michael DWYER, William J. GREENLEE, Tomokazu HIRABAYASHI, Santhosh NEELAMKAVIL, Hidemitsu NISHIDA, Fumihiko SAITOH, Unmesh SHAH, Yan XIA
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Publication number: 20110117055Abstract: Provided herein are hepatitis C virus entry inhibitor oxoacetamide compounds, pharmaceutical compositions thereof, and methods for their use in treatment or prevention of hepatitis C virus infection in a subject in need thereof.Type: ApplicationFiled: November 18, 2010Publication date: May 19, 2011Inventors: James E. MacDonald, McKelvy F. Jeffrey, Flossie Wong-Staal
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Publication number: 20110039819Abstract: The present invention relates to substituted phenoxybenzamide compounds of general formula (I): in which R1, R2, R3, R4, R5, X, R6 and q are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: April 9, 2009Publication date: February 17, 2011Inventors: Marion Hitchcock, Ingo Hartung
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Publication number: 20110039841Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPAR? subtype.Type: ApplicationFiled: May 3, 2005Publication date: February 17, 2011Applicants: Novo Nordisk A/SInventors: Zdenék Polivka, Karel Sindelar, Per Sauerberg, Ingrid Pettersson
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Patent number: 7872002Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and modulating GABAA, and use of the compound of formula I for the treatment of GABAA receptor associated disorders. The general structure of formula I is shown below and can exist in tautomeric forms: The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).Type: GrantFiled: June 6, 2008Date of Patent: January 18, 2011Assignee: Helicon Therapeutics, Inc.Inventors: Alan P. Kaplan, Varsha Gupta, Jan W. F. Wasley
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Patent number: 7863266Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and modulating GABAA, and use of the compound of formula I for the treatment of GABAA receptor associated disorders. The general structure of formula I is shown below: The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).Type: GrantFiled: June 6, 2008Date of Patent: January 4, 2011Assignee: Helicon Therapeutics, Inc.Inventors: Alan P. Kaplan, Varsha Gupta
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Patent number: 7858614Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and negatively modulating the ?5 subtype of GABAA, and use of the compound of formula I for the treatment of GABAA receptor associated disorders. The general structure of formula I is shown below: The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).Type: GrantFiled: June 6, 2008Date of Patent: December 28, 2010Assignee: Helicon Therapeutics, Inc.Inventors: Alan P. Kaplan, Varsha Gupta, Jan W.F. Wasley
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Publication number: 20100087425Abstract: This invention discloses novel gamma secretase inhibitors of the formula: wherein: L is —O—, —N(R6)—, —S—, —S(O)—, or —S(O2)—; R1 is selected from the group consisting of aryl and heteroaryl; R2 is selected from the group consisting of alkyl, —C(O)—Y, —X—C(O)—Y, -alkylene-X—C(O)—Y, -alkylene-C(O)—Y, -alkylene-cycloalkylene-X—C(O)—Y, -alkylene-cycloalkylene-C(O)—Y, -cycloalkylene-alkylene-X—C(O)—Y, -cycloalkylene-alkylene-C(O)—Y, -cycloalkylene-X—C(O)—Y, -cycloalkylene-C(O)—Y, -alkylene-cycloalkylene-alkylene-X—C(O)—Y, -alkylene-cycloalkylene-alkylene-C(O)—Y, aryl, and heteroaryl; R3 is selected from the group consisting of aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, and alkoxyalkyl; each R4 and R5 is independently selected from the group consisting of H and alkyl; and Y is selected from the group consisting of —NR8R9, —N(R6)—(CH2)b—NR8R9, aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heterType: ApplicationFiled: December 8, 2009Publication date: April 8, 2010Inventors: Hubert B. Josien, John W. Clader, Thomas A. Bara, Ruo Xu, Hongmei Li, Dmitri A. Pissarnitaki, Zhiqiang Zhao
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Publication number: 20100022528Abstract: Disclosed are nordihydroguaiaretic acid derivative compounds including various end groups bonded by a carbon atom or heteroatom though a side chain bonded to the respective hydroxy residue O groups by an ether bond or a carbamate bond, pharmaceutical compositions, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, a metabolic disease, such as diabetes, a vascular disease, such as hypertension and macular degeneration, or a proliferative disease, such as diverse types of cancers.Type: ApplicationFiled: October 2, 2007Publication date: January 28, 2010Applicant: ERIMOS PHARMACEUTICALS LLC.Inventors: Qingqi Chen, Rocio Alejandra Lopez, Jonathan Daniel Heller, Amanda Jean Morris
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Publication number: 20090306070Abstract: The present invention relates to nordihydroguaiaretic acid derivative compounds, namely, butane bridge modified nordihydroguaiaretic acid (NDGA) compounds and butane bridge modified tetra-O-substituted NDGA compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, metabolic diseases, such as diabetes and hypertension, or a proliferative disease, such as diverse types of cancers.Type: ApplicationFiled: October 2, 2007Publication date: December 10, 2009Applicant: Erimos Pharmaceuticals LLCInventors: Jonathan Daniel Heller, Qingqi Chen, Rocio Alejandra Lopez, Amanda Jean Morris
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Publication number: 20090176776Abstract: The present invention provides novel methods of treating HIV infections employing small molecule inhibitors identified by chemical library (DIVERSet™ library). These small molecule inhibitors may specifically bind to HIV-1 capsid protein thereby interfering with capsid assembly. The small molecule inhibitors of the present invention can be potential drug targets in the treatment of HIV infection.Type: ApplicationFiled: October 23, 2006Publication date: July 9, 2009Applicant: UNIVERSITY OF ALABAMA AT BIRMINGHAMInventor: Peter Prevelige
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Patent number: 7531536Abstract: This invention describes novel pyrazole compounds of formula IIIa: wherein R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx, Ry, R2; and R2? are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.Type: GrantFiled: August 1, 2003Date of Patent: May 12, 2009Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Andrew Miller, Ronald Knegtel
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Publication number: 20090118270Abstract: PDE4 inhibition is achieved by novel compounds, e.g., N-substituted diarylamine analogs. The compounds of the present invention are of Formulas I-III: wherein A, B, D, E, G, J, K, R1, R2, R3, R4, R11, R12, R13, R14, R21, R22, R23 and R24 are as defined herein.Type: ApplicationFiled: December 5, 2008Publication date: May 7, 2009Inventors: Francisco Xavier Talamas, Joan Marie Caroon, Robert Dunn, Allen Hopper, Erik Kuester, Richard Schumacher, Ashok Tehim
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Publication number: 20090023718Abstract: The present invention relates to a novel class of hydroxamic acid derivatives having a diamine or iminodiacetic acid backbone. The hydroxamic acid compounds can be used to treat cancer. The hydroxamic acid compounds can also inhibit histone deacetylase and are suitable for use in selectively including terminal differentiation, arresting cell growth and/or apoptosis of neo-plastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compound of the invention are also useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: November 23, 2004Publication date: January 22, 2009Applicant: Aton Pharma, Inc.Inventors: Thomas A. Miller, David J. Witter, Sandro Belvedere
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Publication number: 20080255105Abstract: A compound which is a biphenyl derivative of formula (I), or a pharmaceutically acceptable salt thereof wherein: R1 is a C1-C6 alkyl group or a moiety -A1, -L1-A1, -A1-A1?, -L1-A1-A1?, -A1-L1-A1?, -A1-Y1-A1?, -A1-Het1-A1?, -L1-A1-Y1-A1?, -L1-A1-Het1-A1?, -L1-Het1-A1, -L1-Y1-A1, -L1-Y1-Het1-A1, -L1-Het1-Y1-A1, -L1-Y1-Het1-L1?, -A1-Y1-Het1-A1?, -A1-Het1-Y1-A1?, -A1-Het1-L1-A1?, -A1-L1-Het1-A1? or -L1-Het1-L1?; -A and B are the same or different and each represent a direct bond or a —CO—NR?—, —NR?—CO—, —NR?—CO2—, —CO—, —NR?—CO—NR?—, —NR?—S(O)2—, —S(O)2—NR?—, —SO2—, —NR?—, —NR?—CO—CO—, —CO—O—, —O—CO—, —(C1-C2 alkylene)-NR?— or —(C1-C2 hydroxyalkylene)-NR?-moiety, wherein R? and R? are the same or different and each represent hydrogen or C1-C4 alkyl; —R2 and R3 are the same or different and each represent C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy or halogen; n and m are the same or different and each represent 0 or 1; R4 is a C1-C6 alkyl group or a moiety -A4, -L4-A4, -A4-A4?, -L4-A4-A4?, -A4-L4Type: ApplicationFiled: September 18, 2006Publication date: October 16, 2008Inventors: Christopher James Wheelhouse, Alexander James Floyd Thomas, David John Bushnell, James Lumley, James Iain Salter, Malcolm Clive Carter, Neil Mathews, Christopher John Pilkington, Richard Martyn Angell
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Patent number: 7410965Abstract: A delayed release pharmaceutical formulation containing 1-dimethylamino-3-(3-methoxyphenyl)-2-methylpentan-3-ol or a pharmaceutically acceptable salt thereof in a matrix; said matrix containing from 1 to 80 wt. % of at least one pharmaceutically acceptable, matrix-forming, hydrophilic or hydrophobic polymer and having the following in vitro dissolution rate relative to 100 wt. % of the 1-dimethylamino-3-(3-methoxyphenyl)-2-methylpentan-3-ol contained in the formulation: 3-35 wt. % released after 0.5 hour, 5-50 wt. % released after 1 hour, 10-75 wt. % released after 2 hours, 15-82 wt. % released after 3 hours, 30-97 wt. % released after 6 hours, more than 50 wt. % released after 12 hours, more than 70 wt. % released after 18 hours, and more than 80 wt. % released after 24 hours.Type: GrantFiled: November 29, 2004Date of Patent: August 12, 2008Assignee: Gruenenthal GmbHInventors: Johannes Bartholomaeus, Iris Ziegler
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Patent number: 7365067Abstract: The present invention provides a compound having the following general formula (I) which is useful as a neurokinin receptor antagonist: (wherein, R1, R2: optionally substituted (hetero)aryl, R3: —CO—R4, —CO—O—R4, etc., R4: alkyl, cycloalkyl, etc., A: CH2, CO, SO2, B: a single bond, etc., D: oxygen, CH2, E: alkylene, alkenylene, n: 1 to 3).Type: GrantFiled: February 24, 2005Date of Patent: April 29, 2008Assignee: Sankyo Company, LimitedInventors: Takahide Nishi, Toshiyasu Takemoto, Takuya Ikeda, Kiyoshi Morimoto
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Patent number: 7358247Abstract: Provided is an impurity of mycophenolate mofetil, processes for its preparation and its use as a reference.Type: GrantFiled: April 26, 2005Date of Patent: April 15, 2008Assignee: TEVA Gyógyszergyár Zártköruen Muködö RészvénytársaságInventors: Sandor Molnar, Tivadar Tamas, Janos Hajko, Beáta Kosztya, Amihai Eisenstadt
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Patent number: 7329765Abstract: Benzothiophene compounds such as are DNA binding compounds exhibiting antibacterial activity.Type: GrantFiled: November 30, 2004Date of Patent: February 12, 2008Assignee: GeneSoft Pharmaceuticals, Inc.Inventors: Roland W. Burli, Eldon E. Baird, Matthew J. Taylor, Jacob A. Kaizerman, Wenhao Hu
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Patent number: 7186714Abstract: The present invention provides compounds of formula (I) wherein all variables are as defined herein, pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agentsType: GrantFiled: June 10, 2002Date of Patent: March 6, 2007Assignee: SmithKline Beecham CorporationInventors: Kristjan Gudmundsson, Brian A. Johns
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Patent number: 6995151Abstract: Selective MMP-13 inhibitors are isophthalic acid derivatives of the formula wherein: R1, R2, and R3 independently are hydrogen, halo, hydroxy, C1–C6 alkyl, C1–C6 alkoxy, C2–C6 alkenyl, C2–C6 alkynyl, NO2, NR4R5, CN, or CF3; E is independently O or S; A and B independently are OR4 or NR4R5; each R4 and R5 independently are H, C1–C6 alkyl, C2–C6 alkenyl, C2–C6 alkynyl, (CH2)n aryl, (CH2)n cycloalkyl, (CH2)n heteroaryl, or R4 and R5 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring, optionally containing a heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted; n is 0 to 6; or a pharmaceutically acceptable salt thereof. The compounds are useful for treating diseases in a mammal that are mediated by MMP enzymes.Type: GrantFiled: February 13, 2002Date of Patent: February 7, 2006Assignee: Warner-Lambert CompanyInventors: Nicole Chantel Barvian, David Thomas Connor, Richard Dennis Dyer, Adam Richard Johnson, William Chester Patt
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Patent number: 6899864Abstract: The present invention provides a kit and a method for targeting of a diagnostic or therapeutic agent to a target site in a mammal having a pathological condition. The kit comprises, in separate containers, (a) a first conjugate comprising a targeting moiety and a Morpholino oligomer, wherein the targeting moiety selectively binds to a primary, target-specific binding site of the target site or to a substance produced by or associated with the target site; (b) optionally, a clearing agent; and (c) a second conjugate comprising a complementary Morpholino oligomer and a diagnostic agent or therapeutic agent. The method comprises administering (a), optionally (b), and (c) to a mammal.Type: GrantFiled: April 1, 2002Date of Patent: May 31, 2005Assignee: Immunomedics, Inc.Inventors: Donald J. Hnatowich, Mary Rusckowski, Guozheng Liu
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Publication number: 20040157837Abstract: The invention features methods and compositions for treating a patient diagnosed with, or at risk for developing, a fungal infection.Type: ApplicationFiled: November 7, 2003Publication date: August 12, 2004Inventors: George N. Serbedzija, Lisa M. Johansen, Todd W. Chappell, Curtis Keith, Grant R. Zimmermann, M. James Nichols, Benjamin A. Auspitz
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Patent number: 6770641Abstract: The present invention provides a pharmaceutical composition which is useful as a phosphatidylinositol 3 kinase (PI3K) inhibitor and an antitumor agent, and it provides a novel bicyclic or tricyclic fused heteroaryl derivative or a salt thereof which possesses an excellent PI3K inhibiting activity and cancer cell growth inhibiting activity.Type: GrantFiled: June 10, 2003Date of Patent: August 3, 2004Assignees: Yamanouchi Pharmaceutical Co., Ltd., Ludwig Institute for Cancer Research, Imperial Cancer Research Technology Ltd.Inventors: Masahiko Hayakawa, Hiroyuki Kaizawa, Hiroyuki Moritomo, Ken-Ichi Kawaguchi, Tomonobu Koizumi, Mayumi Yamano, Koyo Matsuda, Minoru Okada, Mitsuaki Ohta
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Patent number: 6743788Abstract: Disclosed are novel aromatic compounds of the formula(I) described herein, wherein G, E, W, Ar, X, Y and Z are disclosed herein. The compounds are useful for treating cytokine mediated diseases or conditions such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.Type: GrantFiled: May 17, 2002Date of Patent: June 1, 2004Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier Francesco Cirillo, Victor Kamhi, John Robinson Regan, Michele Tsang
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Patent number: 6723719Abstract: Compounds of formulae (IA) and (IB) or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein R1 is C1 to C3 alkyl substituted with C3 to C6 cycloalkyl, CONR5R6 or a N-linked heterocyclic group; (CH2)nHet or (CH2)nAr; R2 is C1 to C6 alkyl; R3 is C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy; R4 is SO2NR7R8; R5 and R6 are each independently selected from H and C1 to C4 alkyl optionally substituted with C1 to C4 alkoxy, or, together with the nitrogen atom to which they are attached, form a 5- or 6-membered heterocyclic group; R7 and R8, together with the nitrogen atom to which they are attached, form a 4-R10-piperazinyl group; R10 is H or C1 to C4 alkyl optionally substituted with OH, C1 to C4 alkoxy or CONH2; H is an optionally substituted C-linked 5- or 6-membered heterocyclic group; Ar is optionally substituted phenyl; and n is 0 or 1; are potent and selective cGMP PDE5 inhibitors useful in the treatment of, inType: GrantFiled: September 29, 1999Date of Patent: April 20, 2004Assignee: Pfizer IncInventors: Mark Edward Bunnage, John Paul Mathias, Stephen Derek Albert Street, Anthony Wood
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Patent number: RE38761Abstract: A method of inhibiting cell proliferation in a patient suffering from such disorder comprising administering to said patient an effective amount of a composition comprising, in admixture with a pharmaceutically acceptable carrier, a compound, or a pharmaceutically acceptable salt thereof, which is a substituted styrene compound which can also be a naphthalene, an indane or a benzoxazine; including nitrile and molononitrile compounds, and pharmaceutical compositions comprising, in admixture with a pharmaceutically acceptable carrier, a pharmaceutically-effective amount of such compound.Type: GrantFiled: October 14, 1994Date of Patent: July 19, 2005Assignee: Yissum Research Development Company of the Hebrew University of JerusalemInventors: Alexander Levitzki, Chaim Gilon, Michael Chorev, Aviv Gazit