Tetracyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos Patents (Class 514/284)
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Patent number: 6313134Abstract: The present invention discloses thaliporphine and its derivatives for the treatment and/or prophylaxis of cardiac diseases, including cardiac arrhythmia, myocardial ischemia or myocardial infarction, and sudden death caused by cardiac arrhythmia or acute myocardial infarction.Type: GrantFiled: August 23, 2000Date of Patent: November 6, 2001Assignee: National Science CouncilInventors: Ming-Jai Su, Shoei-Sheng Lee
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Patent number: 6306437Abstract: Psychogenic impotence can be ameliorated without substantial undesirable side effects by administration of apomorphine and an antiemetic agent in an amount sufficient to substantially reduce nausea symptoms associated with the use of apomorphine.Type: GrantFiled: June 29, 2000Date of Patent: October 23, 2001Assignee: Pentech Pharmaceuticals, Inc.Inventors: Ragab El-Rashidy, Bruce Ronsen
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Publication number: 20010031762Abstract: The present invention relates to compounds of formula (I) 1Type: ApplicationFiled: April 13, 2001Publication date: October 18, 2001Inventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
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Patent number: 6297286Abstract: Substantially single-enantiomer(−)-tramadol, and its metabolites and structural and/or functional analogues, are useful for the prevention and/or treatment of one or more symptoms selected from nausea, vomiting, dizziness, blurred vision, drowsiness, somnolence, hallucinations, respiratory depression, constipation and euphoria. In particular, substantially single enantiomer (−)-tramadol, and its o-desmethyl metabolite, have been found to be potent anti-emetics.Type: GrantFiled: November 8, 2000Date of Patent: October 2, 2001Assignee: Darwin Discovery, Ltd.Inventor: Richard Michael Huckle
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Patent number: 6291471Abstract: A method of treating organic erectile dysfunction, particularly vasculogenic erectile dysfunction comprises administering to a male in need of such treatment a therapeutically effective amount of apomorphine or a pharmaceutically acceptable salt or pro-drug thereof.Type: GrantFiled: December 17, 1998Date of Patent: September 18, 2001Assignee: ABB Holdings, Inc.Inventors: Karen Kling, Renee J. Perdok, Dustin D. Ruff
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Publication number: 20010020002Abstract: The present invention relates to the treatment of conditions characterized by loss of appetite (anorexia) and/or pathological weight loss by administering a therapeutically effective amount of an agent that modulates androgen activity. The present invention further relates to the treatment and prevention of anorexia nervosa with such agents.Type: ApplicationFiled: April 13, 2001Publication date: September 6, 2001Applicant: VELA PHARMACEUTICALS INC.Inventors: Seth Lederman, Donald W. Landry
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Publication number: 20010020038Abstract: A method for inhibiting hair loss and/or promoting hair growth in chemotherapy and/or radiation therapy patients wherein the (R)-enantiomer of 4-[[(cyanoimino)-[(1,2,2-trimethylpropyl)amino]methyl]amino]benzonitrile is administered prior to, simultaneous with and/or after chemotherapy and/or radiation treatment.Type: ApplicationFiled: March 13, 2001Publication date: September 6, 2001Inventor: Karnail S. Atwal
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Patent number: 6284770Abstract: This invention relates to the use of 5-HT3 receptor antagonists in the treatment of nonconstipated female IBS patients.Type: GrantFiled: April 5, 2000Date of Patent: September 4, 2001Assignee: Glaxo Wellcome Inc.Inventors: Allen Wayne Mangel, Allison Ruth Northcutt
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Patent number: 6277416Abstract: The present invention relates to a chemical composition useful in the chemical management of plant disease. The pesticides of the present invention incorporate benzophenanthridine alkaloids into formulations that are (1) residual and active for a period of time, (2) are adhesive to plant surfaces, (3) have good spreading properties, (4) are stable against photodeactivation, (5) have low phytoxicity, and (6) are capable of penetrating plant tissues.Type: GrantFiled: July 29, 1999Date of Patent: August 21, 2001Assignee: Camas Technologies, Inc.Inventors: Ronald J. Harkrader, Donald L. Meyer
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Patent number: 6271246Abstract: This application relates to a pharmaceutical composition for the prevention, treatment, and management of scalp conditions, such as dandruff, seborrheic dermatitis, psoriasis, folliculitis, and hair thinning including a therapeutically effective amount of an acidic component of a hydroxyacid or tannic acid, or a pharmaceutically acceptable salt thereof. A preferred anti-dandruff composition and method of managing dandruff includes a therapeutically effective amount of the acid component, a vitamin A component, and an anti-growth agent. A preferred anti-hair thinning composition and method of managing thinning hair includes a therapeutically effective amount of the acidic component, a niacin component present in an amount sufficient to locally increase blood circulation, and a 5-&agr; reductase inhibitor.Type: GrantFiled: August 3, 1999Date of Patent: August 7, 2001Inventor: Howard Murad
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Patent number: 6268377Abstract: The present invention provides for the combined use of 5&agr;-reductase inhibitors together with calcium channel blockers for the treatment of benign prostatic hyperplasia (BPH), prostate cancer, prostatitis, hematuria, and other androgen related disorders, including prostatitis and the prevention of prostate cancer. This invention provides a method of treatment which is useful in the treatment of benign prostatic hyperplasia, prostatitis, and/or the prevention and treatment of prostatic cancer, as well as in the treatment of prostatitis and hematuria. This invention also provides a pharmaceutical composition which is useful in the treatment of benign prostatic hyperplasia, prostatitis, hematuria and/or the prevention and treatment of prostatic cancer, wherein the pharmaceutical composition comprises the combination of a 5&agr;-reductase inhibitor and a calcium channel blocking agent.Type: GrantFiled: September 22, 1999Date of Patent: July 31, 2001Assignee: Merck & Co., Inc.Inventors: Joanne Waldstreicher, Daniel Z. Wang
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Patent number: 6268376Abstract: 17&bgr;-N-monosubstituted-carbamoyl-4-aza-5&agr;-androst-1-en-3-ones of the formula wherein R1 is selected from hydrogen, methyl and ethyl and R2 is a straight or branched chain alkyl, cycloalkyl, aralkyl of from 1-12 carbons, or monocyclic aryl optionally containing 1 or more lower alkyl substituents of 1-2 carbon atoms and/or 1 or more halogens, and R′, R″, R″′ are hydrogen or methyl are useful for the prevention of prostatic carcinoma.Type: GrantFiled: December 27, 1994Date of Patent: July 31, 2001Assignee: Merck & Co., Inc.Inventors: Glenn J. Gormley, Elizabeth Stoner
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Publication number: 20010008895Abstract: 17&bgr;-(N-tert-butylcarbamoyl)-3-one-4-aza-steroids (I) can be obtained by a process which comprises the reaction of 17&bgr;-(alkoxycarbonyl)-3-one-4-aza-steroid with lithium tert-butylamide in an organic solvent. Some compounds of formula (I), for example, finasteride, are useful as inhibitors of 5&agr;-reductase, and can be used in the treatment of benign prostatic hyperplasia and alopecia.Type: ApplicationFiled: March 5, 2001Publication date: July 19, 2001Applicant: Raga Consultores, S.L.Inventors: Luis Octavio Silva Guisasola, Cristina Blanco Fernandez, Antonio Lorente Bonde-Larsen, Jorge Martin Juarez
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Patent number: 6251915Abstract: A method for treatment or prevention of prostate cancer by administering an effective amount of a compound of the formula (I) or a pharmaceutically acceptable salt or ester thereof. In formula (I) (which follows) , each of R1 and R2 is a hydrogen atom, a hydroxyl group, a protected hydroxyl group or a lower alkoxy group.Type: GrantFiled: June 8, 2000Date of Patent: June 26, 2001Assignee: Sankyo Company, LimitedInventors: Koichi Kojima, Tomowo Kobayashi
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Patent number: 6239139Abstract: The present invention provides a cholesterol biosynthesis inhibitor which specifically inhibits the sterol 14-reductase which is involved in the distal pathway of cholesterol biosynthesis, a compound of formula (1) below and the use of an extract or the compound of formula (1) for treating hypercholesterolaemia or hyperlipidaemia. The inhibitor comprises an extract obtained by extracting Corydalis Turtschaninowii Besser with a solvent, or an organic layers obtained by partitioning an extract from Corydalis Turtschaninowii Besser with an organic solvent. The extract contains 7,8,13,13&agr;-tetrahydrocoridaline or its derivative, as the active ingredients, which specifically inhibits the enzyme which is involved in the distal pathway of the cholesterol biosynthesis.Type: GrantFiled: January 20, 1999Date of Patent: May 29, 2001Assignee: Hanwha Chemical CorporationInventors: Jung Ho Kim, Tae Neung Jhong, Young Ki Paik, Joon Seo Park, Eui Deok Kim, You Suk Lee, Seung Un Kim
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Patent number: 6204273Abstract: Compounds of the Formula I are inhibitors of the 5&agr;-reductase 1 isozyme, and are useful alone, or in combination with a 5&agr;-reductase 2 inhibitor, for the treatment of androgenic sensitive disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, and benign prostatic hyperplasia.Type: GrantFiled: January 29, 1999Date of Patent: March 20, 2001Assignee: Merck & Co., Inc.Inventors: Philippe L. Durette, William K. Hagmann, Thomas J. Lanza, Jr., Soumya P. Sahoo, Gary H. Rasmusson, Richard L. Tolman, Derek Von Langen
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Patent number: 6200983Abstract: Psychogenic impotence or erectile dysfunction can be identified in psychogenic male patients and can be ameliorated, without substantial undesirable side effects, by sublingual administration of apomorphine dosage forms so as to maintain a plasma concentration of apomorphine of no more than about 5.5 nanograms per milliliter.Type: GrantFiled: November 15, 1999Date of Patent: March 13, 2001Assignees: Pentech Pharmaceuticals, Inc., Queen's University at KingstonInventors: Ragab El-Rashidy, Jeremy P. W. Heaton, Alvaro Morales, Michael A. Adams
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Patent number: 6200965Abstract: Androgen synthesis inhibitors, as well as methods for the use of the same to reduce plasma levels of testosterone and/or dyhydrotestosterone, and to treat prostate cancer and benign prostatic hypertrophy, are disclosed.Type: GrantFiled: May 27, 1999Date of Patent: March 13, 2001Assignee: The University of Marylsnd, BaltimoreInventors: Angela Brodie, Vincent C. O. Njar
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Patent number: 6197768Abstract: The invention relates to novel pyridocarbazole derivatives having highly selective action in inhibiting cyclic GMP-phosphodiesterase (hereinafter abbreviated as cGMP-PDE), processes for producing such derivatives, agents containing at least one of such derivatives as an active ingredient for preventing and/or treating pulmonary hypertension, ischemic heart diseases or diseases against which the cGMP-PDE inhibitory action is effective, and intermediates useful for the production of pyridocarbazole derivatives.Type: GrantFiled: September 10, 1999Date of Patent: March 6, 2001Assignee: Mochida Pharmaceutical Co., Ltd.Inventors: Masayuki Ohashi, Toshiyuki Shudo, Kazumi Nishijima, Tatsuto Notsu, Akira Kikuchi, Kazutoshi Yanagibashi, Hidemitsu Nishida
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Patent number: 6194423Abstract: The present invention is directed to a novel dopamine receptor ligands of the formula: pharmaceutical formulations of such compounds, and a method using such compounds for treating a patient suffering from dopamine-related dysfunction of the central or peripheral nervous system.Type: GrantFiled: August 13, 1999Date of Patent: February 27, 2001Assignees: Purdue Research Foundation, University of North Carolina at Chapel HillInventors: David E. Nichols, Richard Mailman, Debasis Ghosh
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Patent number: 6184228Abstract: The present invention is directed to a method for selecting compounds for use in treating sickle cell disease in a patient. The method comprises the steps of selecting a first set of HbS ligands from a first group of chemical compounds, selecting from the first set of HbS ligands a seconds set that exhibit inhibition of HbS polymerization, and selecting from the second set a third set that display anti-sickling activity of red blood cells when in the presence thereof. The method may include the step of performing a methemoglobin S proteolysis assay measuring a percent protease protection for each compound. The method may additionally include the steps of measuring HbS aggregation, inhibition of protease, deoxy-HbS gelation inhibition activity, O2 affinity of HbS, and cytotoxic effect to cell activity. The method may further include assessing red blood cell morphology, and eliminating compounds that contain moieties that bind to heme.Type: GrantFiled: May 25, 1999Date of Patent: February 6, 2001Assignee: ANADYS Pharmaceuticals, Inc.Inventors: Alan F. Corin, Andrew A. Pakula, Julianne Bryan
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Patent number: 6174892Abstract: The instant invention involves a method of treating and/or reversing androgenic alopecia and promoting hair growth, and methods of treating acne vulgaris, seborrhea, and female hirsutism, by administering to a patient in need of such treatment a 5&agr;-reductase 2 inhibitor, such as finasteride, in a dosage amount under 5 mgs/day.Type: GrantFiled: November 24, 1999Date of Patent: January 16, 2001Assignee: Merck & Co., Inc.Inventors: Glenn J. Gormley, Keith D. Kaufman, Elizabeth Stoner, Joanne Waldstreicher
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Patent number: 6143757Abstract: Compounds of the general structural formula ##STR1## and use of the compounds and salts and solvates thereof, as therapeutic agents.Type: GrantFiled: September 16, 1998Date of Patent: November 7, 2000Assignee: ICOS CorporationInventors: Alain Claude-Marie Daugan, Richard Frederick LaBaudiniere
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Patent number: 6133288Abstract: The present invention provides compounds of formula I and II: ##STR1## wherein X is --O--, --S--, or --NR.sup.5 --;Y is --O--, --S--, --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, or --NR.sup.5 --;B is --CH.sup.2 -- or --CO--;R.sup.1, R.sup.2, and R.sup.3 are each independently --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl), --OSO.sub.2 CF.sub.3, Cl, or F;n is 1 or 2;W is CH.sub.2 or C.dbd.O;R.sup.4 is 1-piperidinyl, 2-oxo-1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 2-oxo-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino;R.sup.5 is C.sub.1 -C.sub.3 alkyl, --COC.sub.6 H.sub.5, --CO(C.sub.1 -C.sub.6 alkyl), --C(O)OC.sub.6 H.sub.5, --C(O)O(C.sub.1 -C.sub.6 alkyl), --SO.sub.2 (C.sub.1 -C.sub.6 alkyl), --SO.sub.2 C.sub.6 H.sub.5, or --SO.sub.2 CF.sub.3 ;or a pharmaceutically acceptable salt or solvate thereof.Type: GrantFiled: November 9, 1999Date of Patent: October 17, 2000Assignee: Eli Lilly and CompanyInventor: Timothy Alan Grese
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Patent number: 6133280Abstract: This invention relates to novel inhibitors of androgen synthesis that are useful in the treatment of prostate cancer and benign prostatic hypertrophy. The present invention also provides methods of synthesizing these novel compounds, pharmaceutical compositions containing these novel compounds, and methods of treating prostate cancer and benign prostatic hypertrophy using the androgen synthesis inhibitors of the present invention.Type: GrantFiled: May 10, 1999Date of Patent: October 17, 2000Assignee: University of Maryland at BaltimoreInventors: Angela Brodie, Yangzhi Ling
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Patent number: 6130228Abstract: Compounds of Formula (I), methods for their preparation, pharmaceutical formulations and use thereof.Type: GrantFiled: August 25, 1998Date of Patent: October 10, 2000Assignee: University of StrathclydeInventors: George Rennet Proctor, Alan Lang Harvey, Maureen Theresa McKenna, Steven John Mullins
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Patent number: 6127378Abstract: Compounds of the formula I in which R1, R2, R3, R31, R4, R5, R51 and R6 have the meanings indicated in the description, are novel efficacious bronchial therapeutics.Type: GrantFiled: September 3, 1998Date of Patent: October 3, 2000Assignee: Byk Gulden Lomberg Chemische Fabrik GmbHInventor: Beate Gutterer
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Patent number: 6124282Abstract: Various compounds that can inhibit the enzyme CYP2D6 are disclosed. The compounds are useful in increasing the effectiveness and reducing the abuse potential of drugs that are metabolised by CYP2D6.Type: GrantFiled: May 22, 1998Date of Patent: September 26, 2000Inventors: Edward M. Sellers, Rachel F. Tyndale
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Patent number: 6121277Abstract: The present invention relates to camptothecin-skeleton alkaloids isolated from Mappia foetida or obtained by semi-synthesis from said alkaloids.Mappia foetida, a plant growing in the Indian subcontinent, is known to contain in its various parts, mainly in the seeds, camptothecin, mappicine and foetidine I and II (EP-A-685481).The alkaloids of the invention have the following general formula: ##STR1## in which R is a hydrogen atom or a methoxy group; R.sub.1 is hydroxy, an OM group wherein M is an alkali cation, preferably sodium or potassium, a C.sub.1 -C.sub.6 alkoxy group, an optionally substituted phenoxy group, an amino, C.sub.1 -C.sub.6 monoalkylamino or C.sub.2 -C.sub.12 dialkylamino group in which the alkyl moiety is optionally substituted by amino groups, an arylamino group; R.sub.2 is a C.sub.1 -C.sub.6 alkyl group or a group of formula COR.sub.3 wherein R.sub.3 is alkyl C.sub.1 -C.sub.6 or optionally substituted phenyl or benzyl.Type: GrantFiled: October 6, 1998Date of Patent: September 19, 2000Assignee: Indena S.p.A.Inventors: Ezio Bombardelli, Luisella Verotta
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Patent number: 6121275Abstract: The present invention provides protoberberine alkaloid derivatives useful as anticancer agents, and methods of use thereof. The invention also provides protoberberine derivatives useful as topoisomerase inhibitors. The invention further provides coralyne and nitidine derivatives which are topoisomerase I-targeted therapeutics effective against camptothecin resistant cancer cells, and are especially effective against CNS tumors.Type: GrantFiled: July 31, 1998Date of Patent: September 19, 2000Assignee: Rutgers, The State University of New JerseyInventors: Edmond J. LaVoie, Leroy Fong Liu, Darshan B. Makhey
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Patent number: 6121276Abstract: Psychogenic impotence can be ameliorated without substantial undesirable side effects by administration of apomorphine and an antiemetic agent in an amount sufficient to substantially reduce nausea symptoms associated with the use of apomorphine.Type: GrantFiled: June 22, 1998Date of Patent: September 19, 2000Assignee: Pentech Pharmaceuticals, Inc.Inventors: Ragab El-Rashidy, Bruce Ronsen
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Patent number: 6114326Abstract: The present invention provides for the use of cabergoline and other agents for the treatment of restless legs syndrome (RLS).Type: GrantFiled: March 24, 1999Date of Patent: September 5, 2000Assignee: Pharmacia & Upjohn CompanyInventor: Peter Schueler
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Patent number: 6114345Abstract: Compounds of formula (I), wherein: the symbol ---- represents a single or a double bond; R is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group; R.sub.f and R'.sub.f, each independently, are C.sub.1 -C.sub.4 alkyl groups substituted by one or more fluorine atoms; and R.sub.1 and R.sub.2, each independently, are selected from: a hydrogen atom; a phenyl group; a C.sub.1 -C.sub.4 alkyl group unsubstituted or substituted by one or more fluorine atoms; a halogen atom; a cyano (CN) group; a group OR.sub.4, wherein R.sub.4 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group; a group SR.sub.5, wherein R.sub.5 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group; and a group COR.sub.6, wherein R.sub.6 is a group OR.sub.4 in which R.sub.4 is as defined above or a C.sub.1 -C.sub.4 alkyl group unsubstituted or substituted by one or more fluorine atoms. They are useful as testosterone 5a-reductase inhibitors.Type: GrantFiled: April 28, 1999Date of Patent: September 5, 2000Assignee: Pharmacia & Upjohn, S.p.A.Inventors: Achille Panzeri, Marcella Nesi, Enrico Di Salle
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Patent number: 6107499Abstract: The invention involves the formation of a prodrug from a fatty acid carrier and a neuroactive drug. The prodrug is stable in the environment of both the stomach and the bloodstream and may be delivered by ingestion. The prodrug passes readily through the blood brain barrier. Once in the central nervous system, the prodrug is hydrolyzed into the fatty acid carrier and the drug to release the drug.In a preferred embodiment, the carrier is 4, 7, 10, 13, 16, 19 docosahexa-enoic acid and the drug is dopamine. Both are normal components of the central nervous system. The covalent bond between the drug and the carrier preferably is an amide bond, which bond may survive the conditions in the stomach. Thus, the prodrug may be ingested and will not be hydrolyzed completely into the carrier molecule and drug molecule in the stomach.Type: GrantFiled: June 6, 1995Date of Patent: August 22, 2000Assignee: Neuromedica, Inc.Inventor: Victor E. Shashoua
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Patent number: 6093722Abstract: A method for treatment or prevention of prostate cancer by administering an effective amount of a compound of the formula (I) or a pharmaceutically acceptable salt or ester thereof. In formula (I) (which follows), each of R.sup.1 and R.sup.2 is a hydrogen atom, a hydroxyl group, a protected hydroxyl group or a lower alkoxy group.Type: GrantFiled: August 23, 1999Date of Patent: July 25, 2000Assignee: Sankyo Company, LimitedInventors: Koichi Kojima, Tomowo Kobayashi
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Patent number: 6087362Abstract: The treatment of sexual dysfunction in human patients by an oral therapy regimen of administration of apomorphine and sildenafil is disclosed. This treatment optimizes the efficacy of each drug and substantially minimizes the undesirable side effects associated individually therewith. Apomorphine and sildenafil can be co-administered with a combination dosage unit or administered sequentially in separate dosage units, substantially prior to sexual activity. Other erectogenic agents can be administered along with apomorphine and sildenafil.Type: GrantFiled: March 16, 1999Date of Patent: July 11, 2000Assignee: Pentech Pharmaceuticals, Inc.Inventor: Ragab El-Rashidy
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Patent number: 6087347Abstract: Estratriene derivatives of the following formula have a powerful inhibitory effect on estrone sulfatase and are hence useful for the prophylaxis or treatment of diseases caused by estrogens, such as breast cancer, uterine cancer, ovarian cancer, endometriosis, adenomyosis uteri and mastopathy. ##STR1## wherein one of A and B represents C.dbd.O or CH.sub.2 and the other represents O or NH; and R represents --SO.sub.2 NR.sup.1 R.sup.2 or --PO(OM).sub.2 in which R.sup.1 and R.sup.2 each independently represent a hydrogen atom or a lower alkyl group and M represents a hydrogen atom or an alkali metal; provided that, when one of A and B represents NH, the other represents C.dbd.O.Type: GrantFiled: March 12, 1999Date of Patent: July 11, 2000Assignee: Teikoku Hormone Mfg. Co., Ltd.Inventors: Naoyuki Koizumi, Shigehiro Takegawa, Shigeki Iwashita, Tomoko Kawachi, Mamoru Mieda, Tomohito Fujii
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Patent number: 6075005Abstract: The present invention relates to a hair growth compositions which contain relaxin or a relaxin analog and an anti-androgenic agent such as finasteride, SKL-105657, estrogen, cyproterone acetate, spironolactor, flutamide, minoxidil or RU58841 as well as to methods for treating androgenic alopecia using such compositions.Type: GrantFiled: July 6, 1999Date of Patent: June 13, 2000Inventor: Raziel Lurie
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Patent number: 6048849Abstract: This invention provides for pharmaceutical formulations of compounds which are useful as protective agents when administered to patients also receiving antineoplastic drugs. The invention also includes methods of reducing the toxicity of various antineoplastic agents by administering an effective amount of the protective agent to a patient receiving one or more antineoplastic agents. The compounds useful as protective agents have either a sulfhydryl moiety or are reducible disulfides.Type: GrantFiled: January 6, 1999Date of Patent: April 11, 2000Assignee: BioNumerik Pharmaceuticals, Inc.Inventors: Frederick H. Hausheer, Thomas J. Dodd
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Patent number: 6037348Abstract: The present invention provides a method of inhibiting influenza and flaviviral replication based on a mechanism of action in which HA-mediated fusion or E protein mediated fusion is inhibited by a fusion inhibiting agent which binds, complexes or otherwise becomes associated with HA or E protein during the translation of the target protein and/or its vesicular transport.Type: GrantFiled: February 5, 1997Date of Patent: March 14, 2000Assignee: Eli Lilly and CompanyInventors: Joseph Matthew Colacino, Steven Duane Hatch, William Joseph Hornback, Mark Ayer Muesing, John Edwin Munroe, Kirk Alan Staschke, Joseph Chiou-Chung Tang
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Patent number: 6030979Abstract: The present invention provides a pharmaceutical composition comprising 5,6-dihydrodibenzo[a,g]quinolizinium derivative and the salts thereof of formula (I) which specifically inhibits the sterol 14-reductase which is involved in the distal pathway of cholesterol biosynthesis, and the use of the compound of formula (I) for treating hypercholesterolaemia or hyperlipidaemia.Type: GrantFiled: January 22, 1999Date of Patent: February 29, 2000Assignee: Hanwha CorporationInventors: Jung Ho Kim, Tae Neung Jhong, Young Ki Paik, Joon Seo Park, Eui Deok Kim, You Suk Lee, Seung Un Kim
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Patent number: 6030981Abstract: The invention relates to phenanthridine derivatives of the general formula I and II ##STR1## and also its salts, in which R.sub.1 means a hydrogen atom, an aromatic, carbocyclic or hetercyclic or heterocyclic residue and in which R.sub.2 and R.sub.3, which can be the same or different, mean a hydrogen atom, an alkyloxy residue, an alkylenoxy residue, a halogen atom or a nitro group.Type: GrantFiled: April 13, 1998Date of Patent: February 29, 2000Inventors: Bernd Clement, Matthias Weide
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Patent number: 6030978Abstract: The antifungal formulation comprising the novel compounds of the following chemical formulae (I) and (II) exhibit in vitro antifungal activity against fungi including cutaneous filamentous fungus, such as Epidermophyton, Microsporum, Trichophyton, Sporothrix schenckii, Aspergillus or Candida. The formulation of the present invention exhibit in vitro antifungal activity at the concentration of 1-100 .mu.g/ml. ##STR1## wherein R.sup.1, R.sup.2, and R.sup.4 may be the same or different, and represent C.sub.1 -C.sub.5 alkoxy, R.sup.3 represents hydrogen or C.sub.1 -C.sub.10 alkyl, A.sup.- represents inorganic acid ion, organic acid ion or halide, R.sup.5 represents hydrogen, pyridylmethyl, substituted pyridylmethyl or a group having the following chemical formula(XI) ##STR2## wherein Z.sup.1, Z.sup.2, Z.sup.3, Z.sup.4 and Z.sup.5 may be the same or different and represent hydrogen, halogen, C.sub.1 -C.sub.5 alkyl, trifluoromethyl, phenyl, substituted phenyl, nitro, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.Type: GrantFiled: December 10, 1998Date of Patent: February 29, 2000Assignee: Hanwha CorporationInventors: Jung Ho Kim, Tae Neung Jhong, Young Ki Paik, Joon Seo Park, Eui Deok Kim, You Suk Lee, Seung Un Kim
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Patent number: 6028079Abstract: A condensed-indan derivative represented by formula (1) and a pharmaceutically acceptable salt thereof: wherein ring A represents an optionally substituted benzene ring or naphthalene ring, or a benzene ring having a lower alkylenedioxy group, ring B represents an optionally substituted benzene ring or a benzene ring having a lower alkylenedioxy group. Y represents --N.dbd.CR-- or --CR.dbd.N--, R represents a --NR.sub.1 R.sub.2 group, an optionally substituted nitrogen-containing heterocyclic group or a --OR.sub.3 group, wherein R.sub.1 and R.sub.2 are the same or different and each is a hydrogen atom; a phenyl group; an optionally substituted nitrogen-containing heterocyclic group; or a lower alkyl group which may be substituted by at least one selected from the group consisting of an optionally substituted amino group, a lower alkoxy group, a phenyl group, a nitrogen-containing heterocyclic group, an amine oxide group substituted by a lower alkyl group or a hydroxyl group(s); R.sub.Type: GrantFiled: August 12, 1997Date of Patent: February 22, 2000Assignee: Taiho Pharmaceutical Co., LtdInventors: Shinji Okazaki, Tetsuji Asao, Motoji Wakida, Keisuke Ishida, Masato Washinosu, Teruhiro Utsugi, Yuji Yamada
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Patent number: 6004971Abstract: The present invention provides compounds of formula I and II: ##STR1## wherein X is --O--, --S--, or --NR.sup.5 --;Y is --O--, --S--, --CH.sub.2 --, --Ch.sub.2 CH.sub.2 --, --CH.dbd.CH--, or --NR.sup.5 --;B is --CH.sup.2 -- or --CO--;R.sup.1, R.sup.2, and R.sup.3 are each independently --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl), --OSO.sub.2 CF.sub.3, Cl, or F;n is 1 or 2;W is CH.sub.2 or C.dbd.O;R.sup.4 is 1-piperidinyl, 2-oxo-1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 2-oxo-1-pyrrolidinyl, 4-morpholino, dimechylamino, diethylamino, or 1-hexamethyieneimino;R.sup.5 is C.sub.1 -C.sub.3 alkyl, --COC.sub.6 H.sub.5, --CO(C.sub.1 -C.sub.6 alkyl), --C(O)OC.sub.6 H.sub.5, --C(O)O(C.sub.1 -C.sub.6 alkyl), --SO.sub.2 (C.sub.1 -C.sub.6 alkyl), --SO.sub.2 C.sub.6 H.sub.5,or --SO.sub.2 CF.sub.3 ; or a pharmaceutically acceptable salt or solvate thereof.Type: GrantFiled: June 19, 1997Date of Patent: December 21, 1999Assignee: Eli Lilly and CompanyInventor: Timothy Alan Grese
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Patent number: 6001844Abstract: Compounds of structural Formula (I) ##STR1## and pharmacologically acceptable salts and esters thereof possess 5.alpha.-reductase inhibitory activity. These compounds inhibit 5.alpha.-reductase type 1 and type 2. The compounds of structural Formula I are useful in the systemic, including oral, and parenteral, including topical, treatment and prevention of hyperandrogenic conditions including prostatic carcinoma, benign prostatic hyperplasia, acne vulgaris, seborrhea, androgenic alopecia (also called androgenetic alopecia) which includes male- and female-pattern baldness, female hirsutism, and prostatitis. A class of compounds of the present invention are also potent antiandrogens. The present invention also relates to novel compositions containing such compounds, methods of their use and methods of their manufacture.Type: GrantFiled: March 11, 1998Date of Patent: December 14, 1999Assignee: Merck & Co., Inc.Inventors: Raman K. Bakshi, Soumya P Sahoo, Richard L. Tolman
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Patent number: 6001848Abstract: Disclosed are dopamine agonist and opioidergic compositions and methods for their use in the treatment of alcoholism. The invention discloses compounds and therapeutic kits useful in the treatment of alcoholics having the A1 allele of the dopamine receptor D2 gene. Also disclosed are methods of treating alcoholics having the A1/A1 or A1/A2 DRD2 genotype comprising administration of dopamine agonists such as aporphines, ergolines, related compounds, and their analogs, in combination with opioidergic compounds such as naloxone.Type: GrantFiled: March 24, 1997Date of Patent: December 14, 1999Assignee: The Regents of the University of CaliforniaInventor: Ernest P. Noble
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Patent number: 6001845Abstract: A method of treating sexual dysfunction comprising administering a therapeutically effective amount of a combination of phentolamine and apomorphine, as well as pharmaceutical compositions and kits useful in those methods, are disclosed.Type: GrantFiled: June 10, 1999Date of Patent: December 14, 1999Assignee: Schering CorporationInventor: Thomas Mark Estok
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Patent number: 5998427Abstract: The present invention relates to compounds of formula (I), wherein carbons 1 and 2 are joined by either a single or a double bond; R.sup.1 is hydrogen or methyl; R.sup.2 is hydrogen or methyl; R.sup.3 is (B) wherein X, R.sup.6, R.sup.7 and R.sup.8 are various groups, and pharmaceutically acceptable solvates thereof and their use in the treatment of androgen responsive and mediated diseases.Type: GrantFiled: May 14, 1998Date of Patent: December 7, 1999Assignee: Glaxo Wellcome Inc.Inventors: Kenneth William Batchelor, Stephen Vernon Frye
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Patent number: 5998377Abstract: A regime for therapeutic management of a benign prostatic hyperplasia and prostatic cancer employs Cetrorelix alone or in combination with .alpha.-reductase inhibitors or .alpha.-receptor blocking agents. The regimen reduces the volume of the prostate and avoids the side effects associated with testosterone levels being in a castration range. Cetrorelix is administered at dosages between 0,5 mg/day and 20 mg/week or about 0.014 mg/kg body weight per day to 0,30 mg/kg body weight per week or at levels of about 25 to 120 mg of Cetrorelix per month or 0.376 mg/kg to 1.71 mg/kg per month. Cetrorelix can be administered with .alpha.-reductase inhibitors or .alpha.-receptor blocking agents.Type: GrantFiled: April 9, 1998Date of Patent: December 7, 1999Assignee: ASTA Medica AktiengesellschaftInventors: Jurgen Engel, Thomas Reissmann, Hilde Riethmuller-Winzen, Jurgen Rawert