Plural Hydroxy Groups Bonded Directly To The Aryl Ring Or Ring System (h Of -oh May Be Replaced By A Substituted Or Unsubstituted Ammonium Ion Or A Group Ia Or Iia Light Metal) Patents (Class 564/361)
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Publication number: 20140249180Abstract: A tau aggregation inhibitor reduces tau aggregation in cells. The tau aggregation inhibitor can include a catechol structure-containing compound or a salt thereof, and the catechol structure-containing compound can be one of isoprenaline, dopamine, dobutamine, levodopa, levodopa/carbidopa, trimetoquinol, hexoprenaline, methyldopa, and droxidopa. One example of the catechol structure-containing compound is isoprenaline, which can be d-enantiomer of isoprenaline or d/l-racemic mixture of isoprenaline. Tauopathies to be prevented or treated by the inhibitor include AD, Down's syndrome, Pick's disease, corticobasal degeneration, and progressive supranuclear palsy.Type: ApplicationFiled: October 3, 2012Publication date: September 4, 2014Applicants: National Center for Geriatrics and Gerontology, THE DOSHISHAInventors: Akihiko Takashima, Yoshiyuki Soeda, Hiroyuki Nagata, Yasuo Ihara, Tomohiro Miyasaka, Hachiro Sugimoto
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Patent number: 8771744Abstract: The invention provides a process for increasing the crystallinity of at least one solid material which is less than 100% crystalline, comprising applying ultrasound to the substantially dry solid material.Type: GrantFiled: October 20, 2010Date of Patent: July 8, 2014Assignee: Prosonix LimitedInventors: Graham Ruecroft, Dipesh Parikh
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Publication number: 20140187645Abstract: This disclosure concerns the discovery of (R,R)- and (R,S)-fenoterol analogues which are highly effective at binding ?2-adrenergic receptors. Exemplary chemical structures for these analogues are provided. Also provided are pharmaceutical compositions including the disclosed (R,R)-fenoterol and fenoterol analogues, and methods of using such compounds and compositions for the treatment of cardiac disorders such as congestive heart failure and pulmonary disorders such as asthma or chronic obstructive pulmonary disease.Type: ApplicationFiled: March 6, 2014Publication date: July 3, 2014Applicant: The USA, as represented by the Secretary, Department of Health and Human ServicesInventors: Irving William Wainer, Weizhong Zhu, Khalid Chakir, Rui-Ping Xiao, Darrel R. Abernethy, Farideh M. Beigi-Abhari
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Publication number: 20130123298Abstract: Pharmaceutical composition for the prevention of perioperative arterial hypotension in humans comprising noradrenaline for intravenous administration.Type: ApplicationFiled: July 27, 2011Publication date: May 16, 2013Applicant: LABORATOIRE AGUETTANTInventor: Jean-Michel Julia
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Publication number: 20120329879Abstract: Provided herein are methods for improving function in a retinal cell associated with a diabetic condition and for treating a diabetic retinopathic condition in a subject. The methods comprise contacting the retinal cell or administering to the subject a beta-adrenergic receptor agonist or R-isomer thereof such as have the chemical structural formula: where R1 is (CH2)n(CH3)2 or where n is 1 to 4, R2 is H or H.HX, where X is a halide and R3 is O(CH2)mCH3 at one or more of C2-C6, where m is 0 to 4. Also provided are BAR agonists having the structural where R1 is the (CH2)n-phenyl-R2 substituent and the hydroxy-benzene moiety is 1,2-benzene diol or 1,3-benzene diol.Type: ApplicationFiled: September 7, 2012Publication date: December 27, 2012Applicant: THE UNIVERSITY OF TENNESSEE RESEARCH FOUNDATIONInventors: Jena J. Steinle, Kimberly P. Williams, Jayaprakash Pagadala, Duane D. Miller
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Publication number: 20120309729Abstract: The invention provides a process for increasing the crystallinity of at least one solid material which is less than 100% crystalline, comprising applying ultrasound to the substantially dry solid material.Type: ApplicationFiled: October 20, 2010Publication date: December 6, 2012Inventors: Graham Ruecroft, Dipesh Parikh
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Patent number: 8288590Abstract: Biocompatible, bioresorbable polymers comprising a plurality of monomeric repeating units containing an amide group, wherein said amide groups are N-substituted and the N-substituent and degree of N-substitution are effective to lower the melt viscosity, the solution viscosity, or both, compared to the same polymer without N-substitution.Type: GrantFiled: July 14, 2011Date of Patent: October 16, 2012Assignee: Rutgers, The State University of New JerseyInventors: Joachim B. Kohn, Durgadas Bolikal, Jaap Schut, Ernest G. Baluca
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Publication number: 20120196938Abstract: The invention is concerned with methods, regimens and dosage forms employing a beta 2 adrenergic receptor agonist such as terbutaline sulphate, for treating nocturnal hypoglycaemia in human subjects whilst reducing incidence of hyperglycaemia in said subjects upon wakening.Type: ApplicationFiled: July 16, 2010Publication date: August 2, 2012Applicant: Jagotec AGInventor: Guy Vergnault
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Publication number: 20120157543Abstract: This disclosure concerns the discovery of (R,R)- and (R,S)-fenoterol analogues which are highly effective at binding ?2-adrenergic receptors. Exemplary chemical structures for these analogues are provided. Also provided are pharmaceutical compositions including the disclosed (R,R)-fenoterol and fenoterol analogues, and methods of using such compounds and compositions for the treatment of cardiac disorders such as congestive heart failure and pulmonary disorders such as asthma or chronic obstructive pulmonary disease.Type: ApplicationFiled: December 21, 2011Publication date: June 21, 2012Inventors: Irving W. Wainer, Weizhong Zhu, Khalid Chakir, Rui Ping Xiao, Darrell R. Abernethy, Farideh M. Beigi
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Publication number: 20120129944Abstract: A stabilised composition comprising at least one adrenergic compound and at least one antioxidant selected from the group consisting of a bisulfite, a metabisulfite and a sulfite compound.Type: ApplicationFiled: June 3, 2010Publication date: May 24, 2012Applicant: ALK AGInventors: Alan J. Baillie, Kenneth MacDonald, Pamela Porteous, Simon Hendry
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Publication number: 20120022086Abstract: Novel compounds, compositions, and methods related to the activation of the TrkB receptor are provided. The methods include administering in vivo or in vitro a therapeutically effective amount of a compound containing a catecholamine backbone and pharmaceutically acceptable salts, prodrugs, and derivatives thereof. Specifically, methods, compositions, and compounds for the treatment of disorders including neurological disorders, neuropsychiatric disorders, and metabolic disorders are provided. For example, a first method is provided of treating or reducing the risk of depression, anxiety, or obesity in a subject, which includes administering to the subject a therapeutically effective amount of the described compounds. A further method of promoting neuroprotection in a subject also is provided, which includes administering to the subject a therapeutically effective amount of the described compounds.Type: ApplicationFiled: March 17, 2010Publication date: January 26, 2012Applicant: EMORY UNIVERSITYInventor: Keqiang Ye
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Publication number: 20110269848Abstract: Biocompatible, bioresorbable polymers comprising a plurality of monomeric repeating units containing an amide group, wherein said amide groups are N-substituted and the N-substituent and degree of N-substitution are effective to lower the melt viscosity, the solution viscosity, or both, compared to the same polymer without N-substitution.Type: ApplicationFiled: July 14, 2011Publication date: November 3, 2011Applicant: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEYInventors: Joachim B. Kohn, Durgadas Bolikal, Jaap Schut, Ernest G. Baluca
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Publication number: 20110146678Abstract: This invention provides a process for increasing the crystallinity of at least one solid material which is less than 100% crystalline, comprising contacting said solid material with solvent in which the solid material is insoluble or poorly soluble (a non-solvent); and applying ultrasound to the solid material when in contact with said non-solvent.Type: ApplicationFiled: July 20, 2009Publication date: June 23, 2011Inventors: Graham Ruecroft, Dipesh Parikh
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Publication number: 20100204516Abstract: A process for the preparation of optically pure R (?) salbutamol of formula (6) and its pharmaceutically acceptable salts by using a (+) 4-nitro tartranilic acid as the resolving agent and a binary solvent system comprising alkyl acetate and C1 to C4 branched or normal chain alcohol for dissolution of the racemic mixture and resolving agent and purification of the 4-nitro tartranilic acid salt of R (?) salbutamol. 4-nitro tartranilic acid salt of R (?) salbutamol is converted into formic acid salt of R(?) 4-benzyl salbutamol followed by basification and debenzylation to form optically pure R(?) salbutamol. Optically pure (R)-salbutamol is obtained in good yield and high purity. The optically pure R(?)salbutamol is optionally converted into pharmaceutically acceptable salts.Type: ApplicationFiled: September 25, 2006Publication date: August 12, 2010Applicant: AARTI HEALTHCARE LIMITEDInventors: Parimal Desai, Narendra Salvi, Bharatkumar Patravale, Subramanian Seetharaman, Dilip Patil, Khandu Ghogare
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Publication number: 20100168245Abstract: This disclosure concerns the discovery of (R,R)- and (R,S)-fenoterol analogues which are highly effective at binding ?2-adrenergic receptors. Exemplary chemical structures for these analogues are provided. Also provided are pharmaceutical compositions including the disclosed (R,R)-fenoterol and fenoterol analogues, and methods of using such compounds and compositions for the treatment of cardiac disorders such as congestive heart failure and pulmonary disorders such as asthma or chronic obstructive pulmonary disease.Type: ApplicationFiled: August 10, 2007Publication date: July 1, 2010Inventors: Irving W. Wainer, Weizhong Zhu, Khalid Chakir, Rui Ping Xiao, Darrell R. Abernethy, Farideh M. Beigi
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Patent number: 7442839Abstract: The present invention relates to novel compounds of formula (I), to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use in the prophylaxis and treatment of respiratory diseases.Type: GrantFiled: October 24, 2003Date of Patent: October 28, 2008Assignee: Glaxo Group LimitedInventors: Alan Michael Chapman, Stephen Barry Guntrip, Brian Edgar Looker, Panayiotis Alexandrou Procopiou
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Patent number: 7087765Abstract: Method and compositions for treating a patient having a neurological disease or disorder, such as stroke, head trauma, spinal cord injury, spinal cord ischemia, ischemia- or hypoxia-induced nerve cell damage, epilepsy, anxiety, neuropsychiatric or cognitive deficits due to ischemia or hypoxia such as those that frequently occur as a consequence of cardiac surgery under cardiopulmonary bypass, or neurodegenerative diseases such as Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, or amyotrophic lateral sclerosis (ALS).Type: GrantFiled: March 9, 2004Date of Patent: August 8, 2006Assignee: NPS Pharmaceuticals, Inc.Inventors: Alan L. Mueller, Scott T. Moe
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Patent number: 6951888Abstract: A compound of formula 1 wherein: R1 is C1-C4-alkyl; R2 is C1-C4-alkyl; and R3 is C1-C4-alkyl or phenyl, each optionally mono- or polysubstituted, or R2 and R3 together are —CH2—CH2— or —CH2—CH2—CH2—, or the corresponding acid addition salt with a pharmacologically acceptable acid, processes for preparing such compounds, pharmaceutical compositions containing such compounds, and their use in the treatment of inflammatory and obstructive respiratory diseases.Type: GrantFiled: September 19, 2003Date of Patent: October 4, 2005Assignee: Boehringer Ingelheim Pharma Gmbh & Co. KGInventors: Frank Buettner, Ingo Konetzki, Kurt Schromm, Hermann Schollenberger, Sabine Pestel, Andreas Schnapp, Thierry Bouyssou, Claudia Heine
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Patent number: 6784175Abstract: The use of at least one substituted 1-amino-5-phenylpentane-3-ol and/or 1-amino-6-phenylhexane-3-ol compound and/or one of the enantiomers thereof and/or one of the diastereomers thereof and/or one of the physiologically acceptable salts thereof for producing a medicament that has an N-methyl-D-aspartate-(NMDA)-antagonistic effect.Type: GrantFiled: November 18, 2002Date of Patent: August 31, 2004Assignee: Gruenenthal GmbHInventors: Bernd Sundermann, Werner Englberger, Boris Chizh
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Patent number: 6730792Abstract: The present invention relates to a &bgr;3 adrenergic receptor agonist of formula (I) or a pharmaceutical salt thereof, which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful for treating Type II diabetes and/or obesity. The compound can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compound can be used to reduced neurogenic inflammation or as an antidepressant agent. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for decreasing gut motility are also disclosed.Type: GrantFiled: December 13, 2002Date of Patent: May 4, 2004Assignee: Eli Lilly and CompanyInventors: Britta Evers, Cynthia Darshini Jesudason, Rushad Eruch Karanjawala, David Michael Remick, Daniel Jon Sall, Miles Goodman Siegel, Wolfgang Stenzel, Russell Dean Stucky, John Arnold Werner
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Patent number: 6653508Abstract: Substituted 3-amino-2-benzyl-1-phenlypropane derivatives, methods for preparing them, pharmaceutical compositions containing them, and methods of using them to treat various medical conditions.Type: GrantFiled: January 16, 2002Date of Patent: November 25, 2003Assignee: Gruenenthal GmbHInventors: Michael Sattlegger, Helmut Buschmann, Babette-Yvonne Koegel
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Patent number: 6576793Abstract: Disclosed are multibinding compounds which are &bgr;2 adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma and bronchitis. They are also useful in the treatment of nervous system injury and premature labor.Type: GrantFiled: August 14, 2000Date of Patent: June 10, 2003Assignee: Theravance, Inc.Inventors: Edmund J. Moran, John H. Griffin, Seok-Ki Choi
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Patent number: 6495722Abstract: Provided herein are polyurethane foams which may be prepared by spray techniques. The foams of the invention are prepared using conventional isocyanates and a novel Mannich condensate polyol having a hydroxy number in the range of 250-340 and a viscosity of 3500 cps or less, and wherein the Mannich condensate polyol is derived from nonylphenol, formaldehyde, an alkanolamine, and propylene oxide as the sole alkoxylating agent. Polyurethane foams prepared according to the invention possess superior physical properties over sprayed polyurethane foams prepared using Mannich condensate polyols which are made using mixtures of propylene oxide and ethylene oxide.Type: GrantFiled: September 17, 2001Date of Patent: December 17, 2002Assignee: Huntsman Petrochemical CorporationInventors: Robert L. Zimmerman, Marshall P. Devine, Patrick L. Weaver
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Patent number: 6410791Abstract: A nitrate salt of a compound selected from the group consisting of: salbutamol having the formula (I)Type: GrantFiled: January 22, 2001Date of Patent: June 25, 2002Assignee: Nicox S.A.Inventor: Piero Del Soldato
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Patent number: 6211245Abstract: Method and compositions for treating a patient having a neurological disease or disorder, such as stroke, head trauma, spinal cord injury, spinal cord ischemia, ischemia- or hyproxia-induced nerve cell damage, epilepsy, anxiety, neuropsychiatric or cognitive deficits due to ischemia or hypoxia such as those that frequently occur as a consequence of cardiac surgery under cardiopulmonary bypass, or neurodegenerative diseases such as Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, or amyotrophic lateral sclerosis (ALS).Type: GrantFiled: November 4, 1998Date of Patent: April 3, 2001Assignee: NPS Pharmaceuticals, Inc.Inventors: Alan L. Mueller, Scott T. Moe
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Patent number: 6057371Abstract: The invention relates to methods for the treatment of central nervous system disorders, gastrointestinal disorders, drug abuse, angina, migraine, hypertension and depression by administering a pharmaceutical composition comprising an effective amount of certain sigma receptor ligands to a patient in need of such treatment. The invention further relates to novel sigma receptor ligands having high binding to the sigma receptor and pharmaceutical compositions thereof. Unexpectedly, certain of the sigma receptor ligands of the present invention have selectivity for the sigma receptor over the DA, PCP and 5-HT.sub.1A receptors.Type: GrantFiled: June 10, 1992Date of Patent: May 2, 2000Assignee: Virginia Commonwealth UniversityInventor: Richard A. Glennon
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Patent number: 5962737Abstract: Stereospecific synthesis of the racemic threo isomers of 2-nitro-1-phenylpropanols by reacting a benzaldehyde derivative with nitroalkane in the presence of a tertiary amine and reducing 2-nitro-1-phenylpropanols with, for example, lithium aluminum hydride to 2-amino-1-phenylpropanols is described. Also described are phase transfer resolution of racemic mixtures of 2-amino-1-phenylpropanol and its derivatives into their optically pure isomers by reacting a racemic mixture with the mono alkali metal salt of a tartaric acid ester in a two phase system of a hydrocarbon and water. The specification further describes therapeutically useful optically pure isomers of threo-2-amino-1-(dialkoxy or alkoxy) phenylpropanols and acid addition salts thereof.Type: GrantFiled: January 8, 1997Date of Patent: October 5, 1999Inventor: Daniel David West
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Patent number: 5910513Abstract: A compound being a substituted benzyl derivative of polyalkylene polyamine and corresponding to the following formula: ##STR1## in which: n and m=2, 3 or 4, p=2 or 3, x=0, 1 or 2, R.sub.1 and R.sub.4, which may be identical or different, represent(i) a linear or branched C.sub.1 -C.sub.4 alkyl radical or(ii) a radical of the following formula: ##STR2## in which: Z.sub.1 represents OH or OR, Z.sub.2 and Z.sub.3 represent H, OH or OR, R being a linear or branched C.sub.1 -C.sub.8 alkyl radical,R.sub.2 and R.sub.3, which may be identical or different, represent H, a linear or branched C.sub.1 -C.sub.4 alkyl radical, a radical of formula (A) or a radical of the following formula (B): ##STR3## R'.sub.1, R'.sub.4 and R'.sub.5 represent H or a linear or branched C.sub.1 -C.sub.4 alkyl radical, and R.sub.5 represents a linear or branched C.sub.1 -C.sub.4 alkyl radical or a radical of formula (A),with the proviso that at least one of the radicals R.sub.1, R.sub.2, R.sub.3, R.sub.4 or R.sub.Type: GrantFiled: June 16, 1997Date of Patent: June 8, 1999Assignee: L'OrealInventor: Jean-Baptiste Galey
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Patent number: 5775329Abstract: The present invention relates generally to methods of diagnosis, evaluation and treatment of coronary artery disease in mammals using substituted catecholamines and compounds therefore. It also relates to the preparation, use and administration of these compounds which are useful in the diagnosis, evaluation and treatment of coronary artery disease by means of a feedback controlled drug delivery system that delivers exercise simulating agents which are capable of eliciting acute responses similar to those elicited by aerobic exercise.Type: GrantFiled: June 7, 1995Date of Patent: July 7, 1998Assignee: Gensia, Inc.Inventors: Ernest K. Metzner, Mark D. Erion
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Patent number: 5750575Abstract: Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocyle. R.sub.3 may be either hydrogen or C.sub.1-3. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.Type: GrantFiled: June 7, 1995Date of Patent: May 12, 1998Assignee: Cell Therapeutics, Inc.Inventors: J. Peter Klein, Gail E. Underiner, Anil M. Kumar
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Patent number: 5686609Abstract: The invention relates to compounds of the formula ##STR1## in which: m is 2 or 3;Ar and Ar' independently are a thienyl group; a substituted or unsubstituted phenyl group; or an imidazolyl group; it also being possible for Ar' to be a benzothienyl group which is unsubstituted or substituted by a halogen; a naphthyl group which is unsubstituted or substituted by a halogen; a biphenyl group; or a substituted or unsubstituted indolyl;X is hydrogen;X' is hydrogen or a hydroxyl group or is joined to X" below to form a carbon-carbon bond, or X and X' together form an oxo group or a dialkylaminoalkoxyimino group of the formula .dbd.N--O--(CH.sub.2).sub.p --Am, in which p is 2 or 3 and Am is a dialkylamino group;Y is a nitrogen atom or a group C(X"), in which X" is hydrogen or forms a carbon-carbon bond with X';Q is hydrogen, a C.sub.1 -C.sub.4 alkyl group or an aminoalkyl group of the formula --(CH.sub.2).sub.Type: GrantFiled: March 11, 1994Date of Patent: November 11, 1997Assignee: SanofiInventors: Xavier Emonds-Alt, Pierre Goulaouic, Vincenzo Proietto, Didier Van Broeck
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Patent number: 5538999Abstract: A compacted body of powdered medicament for use in a device for the administration by inhalation of a medicament in powdered form. The compacted body is made by compressing a loose powder containing the medicament in powdered form under pressure to create sufficient structural integrity in the body to permit metering of several unit doses of the medicament by abrasion of the body in the device.Type: GrantFiled: May 23, 1995Date of Patent: July 23, 1996Assignee: Fisons plcInventors: Andrew R. Clark, John L. Hart
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Patent number: 5482523Abstract: Mannich condensation products prepared by the condensation of a compound of the formula: ##STR1## wherein R.sub.1 is hydrogen, hydroxy, lower alkyl or lower alkoxy; R.sub.3 and R.sub.4 are independently hydrogen or lower alkyl; R.sub.5 is hydrogen, alkyl, phenyl, aralkyl, alkaryl, or an acyl group of the formula: ##STR2## wherein R.sub.6 is alkyl, phenyl, aralkyl or alkaryl; R.sub.7 is alkyl; u is an integer from 1 to 10; n is an integer from 5 to 100; and x is an integer from 0 to 10;with an aldehyde and a nitrogen base selected from ammonia, lower alkylamine, a polyamine and mixtures thereof.The Mannich condensation products and their fuel soluble salts are useful as fuel additives for the prevention and control of engine deposits.Type: GrantFiled: November 2, 1994Date of Patent: January 9, 1996Assignee: Chevron Chemical CompanyInventor: Richard E. Cherpeck
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Patent number: 5468854Abstract: Conjugates of fluorescent labels with specific, selective, and high affinity ligands for receptors have been synthesized and used to directly measure binding to receptors. In the examples, fluorescein conjugates of the high-affinity benzodiazepine receptor ligands Ro 15-1788 and Ro 7-1986 were synthesized. The binding of these fluorescent ligands (BD 621, BD 623 and BD 607) to benzodiazepine receptors was characterized by direct fluorescence measurement. Both the equilibrium dissociation constants (K.sub.D) of BD 621 and BD 607 and the maximum number of binding sites (B.sub.max) estimated by fluorescence monitoring were consistent with values obtained by using radioligand binding techniques. The binding of BD 621 and BD 607 assessed by fluorescence measurement was reversible, abolished by photoaffinity labeling with Ro 15-4513, and unaffected by a variety of substances that do not bind to benzodiazepine receptors.Type: GrantFiled: July 22, 1993Date of Patent: November 21, 1995Assignee: Pharmaceutical Discovery CorporationInventors: R. Tyler McCabe, Brian R. de Costa
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Patent number: 5442118Abstract: A method for the enantioselective reduction of an .alpha.-iminoketone to an .alpha.-aminoalcohol is disclosed. The method utilizes a borane reducing agent as the reducing agent and a chiral 1,3,2-oxazaborole as the catalyst. The method is applied to the synthesis of R-albuterol from methyl 5-acetylsalicylate in high yield and high optical purity.Type: GrantFiled: April 22, 1994Date of Patent: August 15, 1995Assignee: Sepracor, Inc.Inventors: Yun Gao, Yaping Hong, Charles M. Zepp
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Patent number: 5395970Abstract: Methods and devices for the diagnosis, evaluation and treatment of coronary artery disease (CAD) by means of a closed-loop drug delivery system that delivers an exercise simulating agent, including novel exercise simulating agents which elicit both acute and adaptive cardiovascular responses similar to those elicited by aerobic activity are provided. The acute responses to the exercise simulating agent are used to diagnose and evaluate CAD in lieu of the acute responses to aerobic exercise. Due to their adaptive responses these compounds may be used to treat CAD in lieu of the adaptive responses caused by aerobic exercise training or to treat other conditions where the adaptive responses caused by aerobic exercise are desirable.Type: GrantFiled: December 15, 1993Date of Patent: March 7, 1995Assignee: Gensia Pharmaceuticals, Inc.Inventors: Ronald R. Tuttle, Clinton E. Browne, III
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Patent number: 5143938Abstract: A compound which is a propanamine of general formula (I) ##STR1## in which: R1 is a phenyl radical optionally mono-, di- or trisubstituted,or is a 5- or 6-membered monocyclic heteroaryl radical in which the single heteroatom is nitrogen, oxygen or sulfur,R2 is a lower alkyl radical,R3 and R4 are a hydrogen atom or a lower alkyl, lower alkenyl or lower cycloalkylalkyl radical,or, together with the nitrogen atom to which they are attached, form a saturated 5- to 6-membered heterocycle comprising only one heteroatom,R5 is a 5- to 7-membered cycloalkyl radical, a phenyl radical or a 5- or 6-membered monocyclic heteroaryl radical,and W representsa group .dbd.CH--QH,or a heterocycle .dbd.C[Q--(CH2)n--Q],or a group .dbd.C.dbd.Q, in which groupsQ is an oxygen or sulfur atom,n has the value 2 or 3,W being .dbd.C.dbd.Q only when R3 and R4 are not both hydrogen, and their additions salts with pharmaceutically acceptable acids.Type: GrantFiled: February 26, 1991Date of Patent: September 1, 1992Assignee: Jouveinal S.A.Inventors: Alain Calvet, Agnes Grouhel, Henri Jacobelli, Jean-Louis Junien, Xavier Pascaud
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Patent number: 5126371Abstract: Novel diarylacetylenes of the formula I ##STR1## where A, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 have the meanings stated in the description, are useful for the treatment of disorders.Type: GrantFiled: August 20, 1990Date of Patent: June 30, 1992Assignee: BASF AkteingesellschaftInventors: Hans-Heiner Wuest, Fritz-Frieder Frickel, Axel Nuerrenbach
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Patent number: 5066678Abstract: The invention relates to compounds of the general formula (I) ##STR1## and physiologically acceptable salts and solvates thereof; wherein;R.sup.1 and R.sup.2 each independently represent a hydrogen atom or a C.sub.1-3 -alkyl group with the proviso that the sum total of carbon atom in R.sup.1 and R.sup.2 is not more than 4;X represents a direct bond or a C.sub.1-7 alkylene, C.sub.2-7 alkenylene or C.sub.2-7 alkynylene group and Y represents a direct bond or a C.sub.1-6 alkylene C.sub.2-6 alkenylene or C.sub.2-6 alknylene group with the proviso that the sum total of carbon atoms in X and Y is not more than 10;W represents a group ##STR2## wherein Z represents a group R.sup.3 (CH.sub.2).sub.q where q is 0, 1 or 2 and R.sup.3 is a group R.sup.4 CONH--, R.sup.4 NHCONH--, R.sup.4 R.sup.5 NSO.sub.2 NH--, R.sup.6 SO.sub.2 NH-- or --OH;R.sup.4 and R.sup.5 each represent a hydrogen atom or a C.sub.1-3 alkyl group;R.sup.6 represents a C.sub.1-3 alkyl group;R.sup.7 represents a chlorine atom or the group --CF.sub.Type: GrantFiled: April 23, 1990Date of Patent: November 19, 1991Assignee: Glaxo Group LimitedInventors: Ian F. Skidmore, Lawrence H. C. Lunts, Harry Finch, Alan Naylor, Ian B. Campbell, Charles Willbe, William L. Mitchell, Stephen Swanson, Brian D. Judkins
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Patent number: 5023378Abstract: The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable acid addition salts, metabolically labile esters and solvates thereof in whichR.sup.1 represents a halogen atom or a methyl, ethyl, n-propyl or n-butyl group;R.sup.2, R.sup.3, R.sup.4 and R.sup.5 each represent hydrogen atoms or one or two of R.sup.2, R.sup.3, R.sup.4 and R.sup.5 represent a methy or ethyl group;X represents a C.sub.4-7 alkylene chain optionally substituted by one or more C.sub.1-4 alkyl or hydroxyl groups; or optionally containing one or two double or triple bonds; or optionally interrupted by an oxygen or sulphur atom, or by a sulphone (--SO.sub.2 --) or urea (--NHCONH--) group; andY represents a phenyl ring optionally carrying one to three substituents selected from hydroxyl, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, amino, carboxamido, C.sub.1-4 alkylsulphonylamino and nitro groups and halogen atoms with the proviso that when X is a C.sub.Type: GrantFiled: October 6, 1989Date of Patent: June 11, 1991Assignee: Glaxo Group LimitedInventors: Michael D. Dowle, David Middlemiss, Harry Finch, Alan Naylor, Lawrence H. C. Lunts
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Patent number: 4755599Abstract: The invention provides compounds of formula: ##STR1## in which R=H, halogen, alkyl, alkyloxy, alkythio, NH.sub.2, alkylamino, dialkylamino or CF.sub.3, R.sub.3 =H or alkyl,either R.sub.4 and R.sub.5 =H and R.sub.1 and R.sub.2 =H or alkyl, optionally substituted by alkenyl (2 to 4 C) or alternatively R.sub.1 and R.sub.2 form together a saturated heterocyclic ring containing 4 to 7 ring members and optionally containing another heteroatom such as O, S or N optionally substituted by alkyl,or R.sub.4 =H, R.sub.1 =H or alkyl and R.sub.2 and R.sub.5 together form an alkylene (3 to 4 C) radical and(i) either A=alkyl or phenyl which is unsubstituted or substituted by one or two substituents chosen from halogen, alkyl, alkyloxy, alkylthio, NH.sub.2, alkylamino, dialkylamino, NO.sub.2 or CF.sub.3 or alternatively A=pyridyl, benzyl or cycloalkyl (3 to 6 C), Y=S, SO or SO.sub.2 or a radical: ##STR2## in which R.sub.6 =H or alkyl and R.sub.Type: GrantFiled: February 3, 1987Date of Patent: July 5, 1988Assignee: Rhone-Poulenc SanteInventors: Jean-Claude Barriere, Jean-Pierre Corbet, Claude Cotrel, Daniel Farge, Jean-Marc Paris
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Patent number: 4725602Abstract: Acetylenes of the following formula (I): ##STR1## wherein Y, m, R.sup.1, R.sup.2, R.sup.3, n and R.sup.4 are defined herein and R.sup.5 is hydrogen, alkyl, cycloalkyl or substituted alkyl are useful vasodilators and antihypertensives.Type: GrantFiled: October 24, 1985Date of Patent: February 16, 1988Assignee: McNeilab, Inc.Inventor: John R. Carson
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Patent number: 4661635Abstract: Acetylenes of the formula (I): ##STR1## wherein Y, m, R.sup.1, R.sup.2 q, Alk, R.sup.3, n and R.sup.4 are as defined herein and Ar.sup.1 and Ar.sup.2 are aromatic, including the salts and ammonium derivatives of formula (I), in treating angina, hypertension and cardiac arrhythmias. Pharmaceutical compositions, methods of use and synthesis and novel intermediates are also part of the invention.Type: GrantFiled: October 29, 1984Date of Patent: April 28, 1987Assignee: McNeilab, Inc.Inventor: John R. Carson
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Patent number: 4582649Abstract: Compounds of formula I ##STR1## in which R.sub.1 is an aliphatic C.sub.6-22 residueR.sub.2 is an optionally substituted salicyl groupeach R.sub.3, independently, is H or an optionally substituted salicyl groupn is 0 or an integer from 1 to 10each X, independently, is --C.sub.2 H.sub.4 -- or --C.sub.3 H.sub.6 --provided that the molecule contains from 1 to 5 optionally substituted salicyl groups in free base, protonized or quaternized form, are useful as dyeing or printing after-treatment agents, particularly to improve the oxidative wet fastness of dyeings or printings on cellulose containing material.Type: GrantFiled: November 28, 1984Date of Patent: April 15, 1986Assignee: Sandoz Ltd.Inventor: Hans-Peter Baumann
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Patent number: 4453007Abstract: Provided is a method of increasing the purity of amphoteric compound compositions. The method is: (a) providing an amount of a crude amphoteric compound composition, (b) using a portion of the crude composition to prepare in solution a cationic salt of the amphoteric compound, (c) using another portion of the crude composition to prepare in solution an anionic salt of the amphoteric compound, (d) mixing together the solutions wherein a precipitate is formed, and (e) collecting the precipitate which is an amphoteric compound composition of higher purity than the crude composition.Type: GrantFiled: November 23, 1981Date of Patent: June 5, 1984Assignee: USV Pharmaceutical CorporationInventor: David Taube
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Patent number: 4408074Abstract: A process for preparing 1-(3,5-dimethoxy-4-hydroxy phenyl)-2-(N-methylamino) ethanol hydrochloride is described by reacting 2,6-dimethoxyphenol with anhydrous chloral in the presence of a catalyst, hydrolyzing 1-(3,5-dimethoxy-4-hydroxyphenyl)2,2,2-trichloro ethanol and subsequently isolating the 3,5-dimethoxy-4-hydroxyphenyl glyoxal thus obtained; finally, this compound, in the form of the bisulfite, is directly converted to the desired product by amination with methylamine in the presence of hydrogen with a hydrogenation catalyst and the final product is converted into the hydrochloride.Type: GrantFiled: November 2, 1981Date of Patent: October 4, 1983Assignee: Dr. Lo. Zambeletti S.p.A.Inventors: Massimo Signorini, Attilio Trebbi, Luigi Molteni
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Patent number: 4396627Abstract: Compounds having the formula: ##STR1## where R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, Y and X are as defined hereinbelow, are useful for the reduction of abnormally high blood glucose and lipid levels in the treatment of obesity or hyperglycaemia.Type: GrantFiled: March 15, 1982Date of Patent: August 2, 1983Assignee: Beecham Group LimitedInventors: Anthony T. Ainsworth, David G. Smith
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Patent number: 4276304Abstract: A benzylalcohol derivative of the formula: ##STR1## wherein R is hydroxy, benzyloxy, alkoxy of one to 4 carbon atoms or halogen, and Ring A is monomethoxyphenyl, dimethoxyphenyl, trimethoxyphenyl or 3,4-methylenedioxyphenyl is prepared by reducing a compound of the formula: ##STR2## wherein R' is benzyloxy, alkoxy of one to 4 carbon atoms or halogen, and Ring A is the same as defined above, and when R' is benzyloxy, if required, further subjecting the product to catalytic hydrogenation.The compounds (I) and pharmaceutically acceptable acid addition salts thereof are used as anti-diabetic agents.Type: GrantFiled: January 18, 1980Date of Patent: June 30, 1981Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Muneyoshi Ikezaki, Katsuyuki Noguchi, Hajime Iwai, Masanori Inamasu
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Patent number: RE38417Abstract: The present invention relates to anti-neoplastic and anti-psoriasis pharmaceutical compositions and methods of treatment and to insecticidal compositions and methods of controlling the growth of insects.Type: GrantFiled: August 2, 2002Date of Patent: February 3, 2004Assignee: University of Florida Research Foundation, Inc.Inventor: Raymond J. Bergeron, Jr.