Diuretic Patents (Class 514/869)
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Patent number: 9938236Abstract: The present invention provides novel compounds of formula (I) and methods of use thereof. In certain embodiments, the compounds of the invention are useful as nucleocapsid assembly inhibitors. In other embodiments, the compounds of the invention are useful as pregenomic RNA encapsidation inhibitors of Hepatitis B virus (HBV). In yet other embodiments, the compounds of the invention are useful for the treatment of viral infection, including HBV and related viral infections.Type: GrantFiled: December 27, 2013Date of Patent: April 10, 2018Assignees: Drexel University, Baruch S. Blumberg Institute, Arbutus Biopharma, Inc.Inventors: Xiaodong Xu, Ju-Tao Guo, Tong Xiao, Yanming Du, Timothy Block, Simon David Peter Baugh, Hong Ye
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Patent number: 9586957Abstract: Compounds of Formula I, including pharmaceutically acceptable salts thereof: I useful as HIV attachment inhibitors.Type: GrantFiled: March 25, 2014Date of Patent: March 7, 2017Assignee: ViiV Healthcare UK (No.5) LimitedInventors: Tao Wang, Zhiwei Yin, Zhongxing Zhang, John A. Bender, Barry L. Johnson, John F. Kadow, Nicholas A. Meanwell
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Patent number: 9464079Abstract: Methods employing chemiluminescent agents as therapeutically active agents in the treatment of proliferative disorders are disclosed. The chemiluminiscent agents are used in the disclosed method without a therapeutically effective amount of a photosensitizer. Novel chemiluminescent agents having the general formula: are also disclosed, wherein X, Y, Z, R3 and R5-R9 are as defined herein.Type: GrantFiled: March 22, 2012Date of Patent: October 11, 2016Assignees: Semorex Technologies Ltd., Ariel-University Research and Development Company Ltd.Inventors: Bernard S. Green, Galia Luboshits, Michael A. Firer
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Patent number: 9023894Abstract: The invention relates to a combination comprising the renin inhibitor of formula (I) or a pharmaceutically acceptable salt thereof.Type: GrantFiled: September 19, 2011Date of Patent: May 5, 2015Assignee: Novartis AGInventors: William Hewitt, Daniel L Vasella, Randy L Webb
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Patent number: 9023893Abstract: The invention relates to a combination comprising the renin inhibitor of formula (I) or a pharmaceutically acceptable salt thereof.Type: GrantFiled: September 19, 2011Date of Patent: May 5, 2015Assignee: Novartis AGInventors: William Hewitt, Daniel L Vasella, Randy L Webb
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Patent number: 8889115Abstract: The present invention provides methods and compositions for the treatment of ion imbalances. In particular, the invention provides compositions comprising potassium binding polymers and pharmaceutical compositions thereof. Methods of use of the polymeric and pharmaceutical compositions for therapeutic and/or prophylactic benefits are disclosed herein. Examples of these methods include the treatment of hyperkalemia, such as hyperkalemia caused by renal failure and/or the use of hyperkalemia causing drugs.Type: GrantFiled: October 9, 2012Date of Patent: November 18, 2014Assignee: Relypsa, Inc.Inventors: Dominique Charmot, Han-Ting Chang, Gerrit Klaerner, Jerry M. Buysse, Mingjun Liu
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Patent number: 8409561Abstract: The present invention provides methods and compositions for the treatment of ion imbalances. In particular, the invention provides compositions comprising sodium-binding polymers and pharmaceutical compositions thereof. Methods of use of the polymeric and pharmaceutical compositions for therapeutic and/or prophylactic benefits are disclosed herein. Examples of these methods include the treatment of hypertension, chronic heart failure, end stage renal disease, liver cirrhosis, chronic renal insufficiency, fluid overload, or sodium overload.Type: GrantFiled: August 16, 2010Date of Patent: April 2, 2013Assignee: Relypsa, Inc.Inventors: Dominique Charmot, Han-Ting Chang, Mingjun Liu, Futian Liu, Gerrit Klaerner
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Patent number: 8377911Abstract: A compound having the structure formula (I) or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.Type: GrantFiled: September 20, 2010Date of Patent: February 19, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Michael Man-Chu Lo, Lin Yan
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Patent number: 8354394Abstract: A compound having the structure (I) wherein R is selected from the group consisting of 1) and 2), or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.Type: GrantFiled: October 22, 2010Date of Patent: January 15, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Christopher Franklin, Ravi Nargund, Michael Man-Chu Lo, Lin Yan, Pei Huo
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Patent number: 8173596Abstract: A method for treating a disorder characterized by salt retention, fluid retention, and combinations thereof. A method for determining the presence of or the progression of a disorder characterized by salt retention, fluid retention, salt loss, fluid loss, and combinations thereof. An immunoassay kit for detecting a level of prouroguanylin in a sample.Type: GrantFiled: May 16, 2005Date of Patent: May 8, 2012Assignee: The University of North Carolina at Chapel HillInventors: Michael F. Goy, Nicholas G. Moss, Xun Qian
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Patent number: 7776319Abstract: The present invention provides methods and compositions for the treatment of ion imbalances. In particular, the invention provides compositions comprising sodium-binding polymers and pharmaceutical compositions thereof. Methods of use of the polymeric and pharmaceutical compositions for therapeutic and/or prophylactic benefits are disclosed herein. Examples of these methods include the treatment of hypertension, chronic heart failure, end stage renal disease, liver cirrhosis, chronic renal insufficiency, fluid overload, or sodium overload.Type: GrantFiled: March 30, 2005Date of Patent: August 17, 2010Assignee: Relypsa, Inc.Inventors: Robert Alpern, Jerry Buysse, Han Ting Chang, Dominique Charmot, Michael James Cope, John Fordtran, Gerrit Klaerner, Eric Connor, Mingjun Liu, Futian Liu, Jun Shao
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Patent number: 6784179Abstract: A compound of formula (I) and salts and solvates thereof, in which: R0 represents hydrogen, halogen or C1-6 alkyl; R1 represents hydrogen, C1-6alkyl, C2-6alkenyl, C2-6 alkynyl, halo C1-6alkyl, C3-8cycloalkyl, C3-8cycloalkylC1-3alkyl, arylC1-3alkyl or heteroaryl C1-3alkyl; R2 represents an optionally substituted monocyclic aromatic ring selected from benzene, thiophene, furan and pyridine or an optionally substituted bicyclic ring attached to the rest of the molecule via one of the benzene ring carbon atoms and wherein the fused ring A is a 5- or 6-membered ring which may be saturated or partially or fully unsaturated and comprises carbon atoms and optionally one or two heteroatoms selected from oxygen, sulphur and nitrogen; and R3 represents hydrogen or C1-3 alkyl, or R1 and R3 together represent a 3- or 4-membered alkyl or alkenyl chain.Type: GrantFiled: February 5, 2002Date of Patent: August 31, 2004Assignee: ICOS CorporationInventor: Alain Claude-Marie Daugan
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Patent number: 6503883Abstract: The invention relates to a pharmaceutical preparation, which contains an immunosuppressive active agent in dissolved form in a starch capsule, or hard or soft gelatin capsule which has been coated with one or several polymer films. The invention further relates to a process for the production of the pharmaceutical preparation.Type: GrantFiled: November 28, 2000Date of Patent: January 7, 2003Assignee: Novartis AGInventor: Ulrich Posanski
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Patent number: 6420358Abstract: This invention provides methods of increasing urine flow in humans while minimizing the loss of electrolytes or ions, the methods comprising administering to a human in need thereof a combination of N-[4-(5H-pyrrolo[2,1-c][1,4]benzodiazepin-10(11H)ylcarbonyl)-3-chlorophenyl]-5-fluoro-2-methylbenzamide (or a pharmaceutically acceptable salt thereof), also known as VPA-985, and one or more diuretic agents, as well as pharmaceutical compositions and kits or packages for such combinations.Type: GrantFiled: September 25, 2000Date of Patent: July 16, 2002Assignee: American Cyanamid CompanyInventors: Evelyn Ellis-Grosse, Gayle P. Orczyk
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Patent number: 6369059Abstract: A compound of formula (I) and salts and solvates thereof, in which: R0 represents hydrogen, halogen or C1-6 alkyl; R1 represents hydrogen, C1-6alkyl, C2-6alkenyl, C2-6 alkynyl, haloC1-6alkyl, C3-8cycloalkyl, C3-8cycloalkylC1-3alkyl, arylC1-3alkyl or heteroarylC1-3alkyl; R2 represents an optionally substituted monocyclic aromatic ring selected from benzene, thiophene, furan and pyridine or an optionally substituted bicyclic ring attached to the rest of the molecule via one of the benzene ring carbon atoms and wherein the fused ring A is a 5- or 6-membered ring which may be saturated or partially or fully unsaturated and comprises carbon atoms and optionally one or two heteroatoms selected from oxygen, sulphur and nitrogen; and R3 represents hydrogen or C1-3 alkyl, or R1 and R3 together represent a 3- or 4-membered alkyl or alkenyl chain.Type: GrantFiled: August 7, 2000Date of Patent: April 9, 2002Assignee: ICOS CorporationInventor: Alain Claude-Marie Daugan
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Patent number: 6329428Abstract: The present invention is drawn to a therapeutic drug for micturition disorders and diseases of the lower urinary tract system, containing an organic acid salt of [2-[4-(3-ethoxy-2-hydroxypropoxy)phenylcarbamoyl]ethyl]-dimethylsulfonium. The invention enables treatment of diseases of the lower urinary tract system which cause urinary disorders, such as interstitial cystitis and prostatitis, which arise from unelucidated causes and thus are regarded intractable diseases.Type: GrantFiled: July 5, 2000Date of Patent: December 11, 2001Assignee: Taiho Pharmaceutical Co., Ltd.Inventors: Tamio Yamauchi, Tomohiro Ueda
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Patent number: 5948799Abstract: This invention relates to a method for reducing morbidity and/or mortality in a mammal with congestive heart failure due to non-ischemic etiology comprising administering amlodipine or a pharmaceutically acceptable amlodipine acid addition salt, and, optionally, a diuretic and/or digoxin. The invention further relates to methods for treating patients with congestive heart failure due to non-ischemic etiology, comprising administering a non-ischemic congestive heart failure treating amount of amlodipine or a pharmaceutically acceptable amlodipine salt and, optionally, a diuretic and/or digoxin. The invention also provides a kit which comprises a container means and a) amlodipine and a diuretic, b) amlodipine and digoxin, or c) amlodipine, digoxin and a diuretic; and a kit which comprises a container means and a) amlodipine, an angiotensin converting enzyme (ACE) inhibitor and a diuretic, b) amlodipine, an ACE inhibitor and digoxin, or c) amlodipine, an ACE inhibitor, digoxin and a diuretic.Type: GrantFiled: March 12, 1997Date of Patent: September 7, 1999Assignee: Pfizer Inc.Inventor: Anne Barbara Cropp
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Patent number: 5914336Abstract: A method of controlling the serum solubility of orally administered torasemide is disclosed. A new crystallin modification of torasemide, called modification III which has significantly higher rates of solubilization than the known crystallin form of torasemide, modification I, is blended with amounts of modification I to produce a preselected level of torasemide in serum at a given time following administration. Compositions containing amounts of modification I and modification III, sufficient to achieve the desired serum levels of torasemide, are also disclosed.Type: GrantFiled: June 2, 1998Date of Patent: June 22, 1999Assignee: Boehringer Mannheim GmbHInventor: Bruno Dreckmann-Behrendt
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Patent number: 5843476Abstract: Compositions containing a first dispersion of lipid vesicles which are capable of penetrating into the deep layers of the skin and which contain at least one active agent chosen from lipolytic agents, draining agents and firming agents, for treating these deep layers, and a second dispersion of lipid vesicles which are capable of penetrating into the surface layers of the skin and which contain at least one active agent chosen from cutaneous surface treatment agents, exfoliation agents, smoothing agents and softening agents for the skin, for treating these surface layers, are effective as slimming agents for combating plumpness.Type: GrantFiled: February 19, 1997Date of Patent: December 1, 1998Assignee: L'OrealInventors: Alain Ribier, Jean-Thierry Simonnet, Chantal Fanchon, Evelyne Segot, Herve Cantin
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Patent number: 5843452Abstract: A composition for use in immunosuppression therapy is disclosed. The composition includes an immunosuppressant drug, such as cyclosporin A, and an ethanol extract of the root xylem of Tripterygium wilfordii. The extract is effective alone, or in combination with such an immunosuppressant, in the treatment of transplantation rejection. Also disclosed is a method of immunosuppression that includes administering to a subject a pharmaceutically effective amount of an immunosuppressant drug and an extract of the type above, in an amount effective to potentiate the action of the drug.Type: GrantFiled: June 2, 1994Date of Patent: December 1, 1998Assignee: Pharmagenesis, Inc.Inventors: Tien-Wen Tao Wiedmann, Jian Wang, Nathan B. Pliam, Hank C. K. Wuh
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Patent number: 5728678Abstract: The present invention provides a composition as well as method for providing nutrition to renal patients. Pursuant to the present invention, the enteral composition includes an effective amount of a protein source including whey protein and free amino acids that provide essential as well as nonessential amino acids. The composition is calorically dense and has a moderate osmolality.Type: GrantFiled: June 6, 1995Date of Patent: March 17, 1998Assignee: Nestec Ltd.Inventors: Susan Trimbo, Diana Twyman, David Madsen, Shen-Youn Chang, Hugh N. Tucker
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Patent number: 5668157Abstract: Cyanoguanidine compounds of formula (I) and its pharmaceutically acceptable acid addition salts wherein R.sub.1 is hydrogen or methyl; R.sub.2 is C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.5 cycloalkyl, C.sub.3 -C.sub.5 cycloalkenyl hydroxy methyl, methoxy-C.sub.1 -C.sub.5 alkyl, or R.sub.1 and R.sub.2 are combined to form a C.sub.3 -C.sub.6 carbocyclic ring; R.sub.3 and R.sub.4 are each independently selected to be hydrogen, C.sub.1 -C.sub.4 alkyl, F, Cl, Br, I or CF.sub.3 ; R.sub.5 is hydrogen, F or Cl; R.sub.6 is hydrogen, --NH.sub.2, --NHCH.sub.3, --NHC.sub.2 H.sub.5, --NHCH(CH.sub.3).sub.2, --N(CH.sub.3).sub.2, --N(C.sub.2 H.sub.5).sub.2, NH(CH.sub.2).sub.m, --OC.sub.1 -C.sub.3 alkyl (where m is 2 or 3), --NHC(O)C.sub.1 -C.sub.3 alkyl, Cl or Br; and n is 0 or 1. The compounds of formula (I) are potassium channel blockers useful in the treatment of cardiovascular disorders such as congestive heart failure and hypertension and as a diuretic.Type: GrantFiled: June 25, 1996Date of Patent: September 16, 1997Assignee: Pharmacia & Upjohn CompanyInventors: Stephen J. Humphrey, Kaushik D. Meisheri, James H. Ludens, Jackson B. Hester, Jr.
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Patent number: 5565485Abstract: Phenoxyphenylacetic acids and derivatives of the general structural formula I ##STR1## have endothelin antagonist activity and are useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, benign prostatic hyperplasia, inflammatory diseases including Raynaud's disease and asthma.Type: GrantFiled: August 22, 1994Date of Patent: October 15, 1996Assignee: Merck & Co., Inc.Inventors: Scott W. Bagley, Theodore P. Broten, Prasun K. Chakravarty, Daljit S. Dhanoa, Kenneth J. Fitch, William J. Greenlee, Nancy J. Kevin, Douglas J. Pettibone, Ralph A. Rivero, Thomas F. Walsh, David L. Williams, Jr., Richard B. Toupence, Jay M. Matthews
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Patent number: 5508044Abstract: A solid oral dosage form comprising diltiazem (or a pharmaceutically acceptable salt thereof) in controlled release form and hydrochlorothiazide in immediate release form. Preferably, the controlled release component comprises a plurality of spheroids comprising diltiazem and a spheronizing agent.Type: GrantFiled: July 22, 1994Date of Patent: April 16, 1996Assignee: Euro-Celtique, S.A.Inventors: Ian R. Buxton, Adrian Brown, Helen Critchley, Stewart T. Leslie, Sandra T. A. Malkowska, Derek A. Prater, Ronald B. Miller
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Patent number: 5504099Abstract: Aqueous injection solution that is ready-for-injection of a water-soluble, physiologically well-tolerated azosemide salt of an organic amide, which contains an organic solvent and if desired, a physiologically well-tolerated buffer and it concerns a process for the production of such an injection solution in which the salt is dissolved in a mixture which contains water, an organic solvent and, if desired, a physiologically well-tolerated buffer.Type: GrantFiled: February 24, 1995Date of Patent: April 2, 1996Assignee: Boehringer Mannheim GmbHInventors: Heinrich Woog, Werner Gruber
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Patent number: 5475031Abstract: This invention relates to the use of the succinic acid molecule to stimulate the Citric Acid Cycle in humans and animals and thus relieve those metabolic disorders caused by a deficiency in the Citric Acid Cycle in humans and animals.Type: GrantFiled: September 3, 1993Date of Patent: December 12, 1995Inventor: William H. Livingston
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Patent number: 5422393Abstract: A purified naturally occurring natriuretic compound, identified as Natriuretic Hormone, and a method for isolation of the compound. The natriuretic compound has a molecular weight of about 360, a molecular formula of C.sub.21 H.sub.28 O.sub.5 and with a steroidal nucleus. The compound is useful as a diuretic in the treatment of diseases such as heart disease and hypertension.Type: GrantFiled: October 12, 1993Date of Patent: June 6, 1995Assignee: Naturon Pharmaceutical CorporationInventors: Neal S. Bricker, William J. Wechter
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Patent number: 5395836Abstract: There is provided a novel xanthine Compound(I) ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each represent hydroxy-substituted, oxo-substituted or unsubstituted lower alkyl, Y is a single bond or alkylene, and Q is ##STR2## wherein R.sup.3 and R.sup.4 are the same or different and each represent hydrogen or hydroxy, n is 0 or 1; provided that when both of R.sup.3 and R.sup.4 are hydrogen, at least one of R.sup.1 and R.sup.2 is hydroxy-substituted or oxo-substituted lower alkyl; or a pharmaceutically acceptable salt thereof.The xanthine compound has adenosine A.sub.1 receptor antagonizing activity, and thus shows diuretic effect, renal-protecting effect, bronchodilatory effect, cerebral function improving effect and anti-dementia effect.Type: GrantFiled: April 5, 1994Date of Patent: March 7, 1995Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Junichi Shimada, Takashi Kuwabara, Tohru Yasuzawa, Hiroshi Magara, Hiromi Nonaka, Hideaki Kusaka, Fumio Suzuki
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Patent number: 5364879Abstract: The present invention provides a method of medical treatment for a medical condition in a mammal. In this method, a pharmacologically effective amount for treatment of the condition of a trioxolane or a diperoxide of a non-terpene unsaturated hydrocarbon is applied to the mammal. The invention also provides methods of modulating the immune system in a mammal, of treating inflammation of a tissue in a mammal, and of treating bacterial, fungal, protozoal and viral infections in a mammal.Type: GrantFiled: February 14, 1994Date of Patent: November 15, 1994Assignee: Cliveden Ltd.Inventor: Stephen Herman
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Patent number: 5266596Abstract: DL- or L-threo-3-(3,4-dihydroxyphenyl)serine is effective for the treatment of urinary incontinence, shows no side effects such as urine discharge disturbance, palpitation and hypertension, and has low toxicity.Type: GrantFiled: March 26, 1992Date of Patent: November 30, 1993Assignee: Sumitomo Pharmaceuticals Co., Ltd.Inventors: Kiyoshi Yokokawa, Shuji Takaori
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Patent number: 5256687Abstract: The invention relates to a pharmaceutical composition comprising an angiotensin converting enzyme inhibitor (trandolpril or pamipril) and a loop diuretic (Furosemide or piretanide), and to their use for the treatment of high blood pressure.Type: GrantFiled: November 19, 1992Date of Patent: October 26, 1993Assignee: Hoechst AktiengesellschaftInventors: Reinhard Becker, Rolf Geiger, Rainer Henning, Volker Teetz, Hansjorg Urbach
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Patent number: 5164401Abstract: A method of treating a mammal in need of diruetic treatment by administering an effective diuretic amount of a diuretically active 3,7,9,9-tetrasubstituted 3,7-diazabicyclo[3,3,1]nonane compound, diuretic pharmaceutical compositions containing an effective diuretic amount of a diuretically active 3,7,9,9-tetrasubstituted 3,7-diazabicyclo[3,3,1]nonane compound; and previously unknown diuretically active 3,7,9,9-tetrasubstituted 3,7-diazabicyclo[3,3,1]nonane compounds containing an optionally substituted phenylalkyl group in the 3-position.Type: GrantFiled: June 17, 1991Date of Patent: November 17, 1992Assignee: Kali-Chemie Pharma GmbHInventors: Kurt Burow, Gerd Buschmann, Arman Farjam, Ulrich Kuehl, Gerda Varchmin, Deiter Ziegler, Uwe Schoen
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Patent number: 5143937Abstract: Compounds of the formula I ##STR1## where R.sup.1 to R.sup.5 have the meaning indicated, a process for their preparation and their use as medicaments are described. They are effective lipid-lowering agents with antioxidative properties from the benzenesulfonamide series. They do not have hypotensive and diuretic properties.Type: GrantFiled: February 16, 1990Date of Patent: September 1, 1992Assignee: Hoechst AktiengesellschaftInventors: Hans-Jochen Lang, Ernold Granzer, Bela Kerekjarto
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Patent number: 5132298Abstract: A method for improvement in diuresis which comprises administering, to a subject in need of such improvement, a cyclodextrin or a derivative thereof in an amount effective to cause such improvement.Type: GrantFiled: October 18, 1990Date of Patent: July 21, 1992Assignee: K.K. Ueno Seiyaku OyoInventor: Ryuji Ueno
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Patent number: 5124152Abstract: There are described pharmaceutical compositions comprising aqueous solutions of 7 c l r - ,2,3,4-tetrahydro-2-methyl-3-2-methylphenyl)-4-oxo-6-quinazolinesulfonamid e. ethanol and a cosolvent selected from propylene glycol or polyethylene glycols suitable for parenteral administration to a patent suffering from refractory edema.Type: GrantFiled: January 7, 1991Date of Patent: June 23, 1992Assignee: Fisons CorporationInventors: Jennifer M. Biringer, Martin L. Eichman
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Patent number: 5118615Abstract: Disclosed is a DNA fragment comprising a base sequence coding for a peptide occurring in human atrium cordis and having diuretic action or a precursor of the peptide, plasmids containing the DNA fragment, microorganisms transformed with the plasmid, and a process for production of the peptide using the transformant.Also disclosed is a new peptide consisting of 126 amino acids occurring in human atrium cordis and a precursor thereof. The peptide has notable diuretic action and hypotensive or antihypertensive actions.Type: GrantFiled: March 9, 1987Date of Patent: June 2, 1992Assignee: Suntory LimitedInventors: Hisayuki Matsuo, Kenji Kangawa, Yujiro Hayashi, Shinzo Oikawa, Takehiro Oshima, Shoji Tanaka, Hiroshi Nakazato, Yasunori Tawaragi
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Patent number: 5106630Abstract: A purified naturally occurring natriuretic compound, identified as Natriuretic Hormone, and a method for isolation of the compound. The natriuretic compound has a molecular weight of about 360, a molecular formula of C.sub.21 H.sub.28 O.sub.5 and with a steroidal nucleus. The compound is useful as a diuretic in the treatment of diseases such as heart disease and hypertension.Type: GrantFiled: June 13, 1990Date of Patent: April 21, 1992Assignee: Neal S. BrickerInventors: Neal S. Bricker, William J. Wechter
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Patent number: 5106610Abstract: A method for determining the diuretic potency of candidate drugs as inhibitors of ADH-elicited water channels is disclosed. In a preferred embodiment, such diuretic potency of candidate drugs is determined by suspending vesicles containing ADH water channels in an aqueous suspending medium, incorporating the candidate into the suspension, rapidly changing the pH of the suspending medium and thereafter detecting the proton permeability of the water channels. The proton permeability in the presence of the candidate drug can then be compared to the proton permeability of water channels under similar conditions without the presence of the candidate drug to determine the diuretic potency of the candidate drug to inhibit ADH-elicited water channels.Type: GrantFiled: December 29, 1989Date of Patent: April 21, 1992Assignee: Childrens Medical Center CorporationInventors: H. William Harris, Mark L. Zeidel
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Patent number: 5104887Abstract: High potency carbonic anhydrase inhibitors derived from methazolamide.Type: GrantFiled: August 28, 1991Date of Patent: April 14, 1992Assignee: University of Iowa Research FoundationInventors: Ronald D. Schoenwald, Charles F. Barfknecht
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Patent number: 5100646Abstract: A method of determining the glomerular filtration rate of a subject comprises (1) obtaining a serum sample S.sub.pre and a urine sample U.sub.pre from a subject; (2) administering to the subject an amount of a paramagnetic substance that is filtered by the kidneys and is readily detectable by NMR in serum and urine; (3) allowing for the concentration of the substance to equilibrate between the blood and the extravascular spaces; (4) separating an aliquot of the urine sample v.sub.A and obtaining a serum sample from the subject at the time t.sub.A ; (5) calculating a urine rate (v/a).sub.A from the formula (v/a).sub.A =V.sub.A /a.sub.Type: GrantFiled: July 25, 1990Date of Patent: March 31, 1992Assignee: The United States of America as represented by the Secretary of the Department of Health and Human ServicesInventors: Peter L. Choyke, Joseph A. Frank, Howard A. Austin
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Patent number: 5100647Abstract: Methods for the therapy of cystic fibrosis, Bartter's syndrome, and secretory diarrheas, and for diuretic treatment, by administering to a patient dodecahydro-7,14-methano-2H,6H-di-pyrido[1,2-a:1',2'-e][1,5]diazocine or a pharmaceutically acceptable derivative thereof are disclosed. The formulations include an aerosol formulation comprising the active ingredient in association with an aerosol propellant.Type: GrantFiled: October 2, 1990Date of Patent: March 31, 1992Assignee: The Trustees of the University of PennsylvaniaInventors: Zalman S. Agus, Ellie Kelepouris, Martin Morad
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Patent number: 5087630Abstract: Compounds of formula (Ia), or pharmaceutically acceptable salts or solvates thereof, ##STR1## in which A, together with the nitrogen atom, represents --(CH.sub.2)p--, where p is an integer from 3 to 6, or an optionally substituted tetrahydroisoquinoline ring system;each of R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl C.sub.3-6 cycloalkyl or C.sub.4-12 cycloalkylalkyl, or together form a C.sub.2-6 polymethylene or C.sub.2-6 alkenylene group, optionally substituted with a hetero-atom,R.sub.x is hydrogen, C.sub.1-6 alkyl or phenyl, or together with R.sub.1 forms a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 -- group; and R comprises a substituted or unsubstituted carbocyclic or heterocyclic aromatic group;and compounds of formula (Ib) ##STR2## in which: R, R.sub.1, R.sub.2 and X are as defined in formula (Ia)R.sub.a is C.sub.1-6 alkyl or phenyl;R.sub.b is hydrogen or together with R.sub.a forms a --(CH.sub.2).sub.Type: GrantFiled: October 16, 1989Date of Patent: February 11, 1992Assignee: Dr. Lo. Zambeletti SpAInventors: Roberto Colle, Antonio Pizzi, Geoffrey D. Clarke
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Patent number: 5011688Abstract: A liquid composition for the relief of premenstrual and menstrual discomfort comprising, as active pharmaceutical agents, an effective amount of an analgesic, an antihistamine, and a diuretic, said active agents being dissolved in a liquid vehicle, said composition containing 5-25 percent by volume alcohol and being flavored with active flavoring elements selected from the group consisting of citrus, vanilla, and mint, said active flavoring ingredients being present in an amount sufficient to mask the unpleasant taste of the pharmaceutically active agents.Type: GrantFiled: May 8, 1990Date of Patent: April 30, 1991Inventors: Henry D. Calam, Hans A. Schaeffer
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Patent number: 5010092Abstract: Drug treatment therapies and kits for use therewith are disclosed. They involve the use of methimazole and/or its pro-drug carbimazole to reduce nephrotoxic effects of chemical exposure. In one embodiment, a patient receives cisplatin and then is treated with methimazole. The time delay in providing methimazole prevents the methimazole from being substantially expelled by the kidney prior to cisplatin reaching the kidney.Type: GrantFiled: December 22, 1989Date of Patent: April 23, 1991Assignee: Wisconsin Alumni Research FoundationInventor: Adnan A. Elfarra
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Patent number: 4981852Abstract: A diuretic pharmaceutically acceptable solution of triamterene and solutions of triamterene and hydrochlorothiazide to provide an antihypertensive and diuretic effect for those in need thereof. Triamterene is solubilized in a combination of a glycol and lactic acid present in an amount sufficient to maintain the triamterene in solution. A pharmaceutically acceptable diluent, such as glycerin is also present.Type: GrantFiled: May 13, 1988Date of Patent: January 1, 1991Assignee: Multilan AGInventor: Kap S. Ahn
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Patent number: 4980352Abstract: Certain gem-dimethyl substituted bicyclic phenolic pyrazines of formula III possess eukalemic diuretic properties. They are of value in treating those diseases and conditions in which a eukalemic diuretic effect is required, for example in treating edema, hypertension and/or related conditions.Type: GrantFiled: May 19, 1989Date of Patent: December 25, 1990Assignee: ICI Americas Inc.Inventor: John A. Schwartz
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Patent number: 4973600Abstract: Novel benzodioxole derivative of the formula: ##STR1## wherein R.sup.1 is a lower alkyl group, a lower alkoxy-lower alkyl group, phenyl group or pyridyl group, R.sup.2 is hydrogen atom or a halogen atom and R.sup.3 is hydrogen atom or a lower alkyl group, and a salt thereof are disclosed.Said derivative (I) and a salt thereof have potent diuretic, saluretic and uricosuric activities.Type: GrantFiled: January 31, 1989Date of Patent: November 27, 1990Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Norio Takamura, Isao Inoue, Masaru Inage, Isao Yamaguchi
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Patent number: 4968673Abstract: The use is described of [1R-[1.alpha.(Z),2.beta.,3.beta.,5.alpha.]]-(+)-7-[5-[[(1,1'-biphenyl)-4-y l]methoxy]-3-hydroxy-2-(1-piperidinyl)cyclopentyl]-4-heptenoic acid or a physiologically acceptable salt, solvate or cyclodextrin complex thereof in the manufacture of medicaments for the therapy or prophylaxis of chronic glomerular diseases including glomerulonephritis, lupus nephritis and systemic lupus erythematosus, renal failure, renal hypertension, hepatorenal syndrome, proteinurea (e.g. albuminurea and microalbuminurea), haemolytic uraemic syndrome and renal impairment following ureteral obstruction.Type: GrantFiled: June 20, 1989Date of Patent: November 6, 1990Assignee: Glaxo Group LimitedInventor: Patrick P. A. Humphrey
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Patent number: 4952410Abstract: Pharmaceutical composition containing moxonidine (4-chloro-6-methoxy-2-methyl-5-(2-imidazolin-2-yl)aminopyrimidine) or its pharmaceutically acceptable salts and hydrochlorothiazide (6-chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulphonamide-1,1-dioxide ) and, if appropriate, triamterene (2,4,7-triamino-6-phenylpteridine).Type: GrantFiled: November 17, 1988Date of Patent: August 28, 1990Assignee: Beiersdorf AGInventors: Ben Armah, Wolfgang Stenzel, Vera Planitz
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Patent number: RE34222Abstract: A pharmaceutical composition comprises magnesium oxide, hydroxide or a non-toxic salt of magnesium in a slow-release carrier; this material may be combined with or co-prescribed with a diuretic or cardiac glycoside or adrenergic receptor blocking agent or a calcium antagonist for the treatment of hypertension or angina pectoris.Type: GrantFiled: November 28, 1990Date of Patent: April 13, 1993Inventor: Maurice Bloch