The Aryl Ring Or Aryl Ring System Is Bonded Directly To Another Ring Or Ring System Patents (Class 514/650)
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Patent number: 6475526Abstract: One aspect of the invention relates to anti-viral composition containing at least one zinc compound and at least one phenolic antioxidant (and optionally other ingredients such as at least one analgesic) at least one hydrocarbyl containing compound, and water. Another aspect of the invention relates to a method of treating lesionous symptoms of a viral infection involving applying an effective amount of the zinc containing anti-viral composition to the lesions.Type: GrantFiled: June 5, 2001Date of Patent: November 5, 2002Inventor: Jeffrey B. Smith
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Publication number: 20020137798Abstract: A method for treatment of neuropsychiatric symptoms or disorders emanating from primary brain or systemic impairments includes administration of an effective dose of a dopamine, serotonin, and norepinephrine reuptake inhibitor to a human in need of such treatment. The preferred reuptake inhibitor is sibutramine.Type: ApplicationFiled: March 6, 2002Publication date: September 26, 2002Inventor: Peter Sterling Mueller
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Patent number: 6448294Abstract: A method of treating symptoms linked to menopause in warm-blooded animals by administering to warm-blooded animals in need thereof an amount of a compound of the formula wherein the substituents are defined as in the application sufficient to treat said symptoms.Type: GrantFiled: February 13, 2002Date of Patent: September 10, 2002Assignee: Aventis Pharma S.A.Inventor: Dominique Lesuisse
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Publication number: 20020115727Abstract: The invention relates, in part, to making of making and using, and compositions comprising, racemic and stereomerically pure cyclobutylalkylamines, including hydroxylated sibutramine and hydroxylated metabolites of sibutramine. Methods of treating and preventing a variety of diseases and disorders are disclosed, as are pharmaceutical compositions and unit dosage forms that comprise compounds of the invention.Type: ApplicationFiled: December 3, 2001Publication date: August 22, 2002Inventors: Chris H. Senanayake, Paul D. Rubin, Thomas P. Jerussi
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Patent number: 6410564Abstract: The present invention provides a compound of formula I wherein R1 is —H, —OH, —O(C1-C4 alkyl) , —OCOC6H5, —OCO(C1-C6 alkyl), or —OSO2 (C4-C6 alkyl); R2 is —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl) or —OSO2 (C4-C6 alkyl); n is 2 or 3; and R3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino; or a pharmaceutically acceptable salt thereof. Compounds of formula I are useful in treating osteoporosis, cardiovascular related pathological conditions, and estrogen-dependent cancer.Type: GrantFiled: April 21, 1995Date of Patent: June 25, 2002Assignee: Eli Lilly and CompanyInventors: Henry U. Bryant, George J. Cullinan, Jeffrey A. Dodge, Kennan J. Fahey, Charles D. Jones, Charles W. Lugar, Brian S. Muehl
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Publication number: 20020065324Abstract: The present invention relates to methods of inducing ovulation in a female host comprising the administration of a non-polypeptide cyclic adenosine monophosphate (cAMP) level modulator to the female host. In another aspect, the invention provides for specific administration of the phosphodiesterase inhibitor prior to the luteal phase of the host's ovulatory cycle. Preferred non-polypeptide cAMP level modulator include phosphodiesterase inhibitors, particularly inhibitors of phosphodiesterase 4 isoforms.Type: ApplicationFiled: August 10, 2001Publication date: May 30, 2002Inventors: Stephen Palmer, Sean McKenna, Mark Tepper, Aliza Eshkol, Michael C. Macnamee
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Publication number: 20020055544Abstract: A regimen for the administration of tramadol for the treatment of analgesia is described. The regimen involves a slower initial titration rate of tramadol which results in a significantly lower percentage of discontinuations of therapy due to a lower incidence and severity of side effects.Type: ApplicationFiled: October 26, 2001Publication date: May 9, 2002Inventors: Marc Kamin, William Olson
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Patent number: 6380260Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof in which R1 and R2 are independently H or methyl (for example N,N-dimethyl-1-[1-(4-chlorophenyl) cyclobutyl]-3-methylbutyl amine hydrochloride optionally in the form of its monohydrate) is used for decreasing platelet adhesiveness.Type: GrantFiled: March 17, 2000Date of Patent: April 30, 2002Assignee: Knoll Pharmaceutical CompanyInventors: Carl M. Mendel, Timothy B. Seaton, Steve P. Weinstein
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Patent number: 6365631Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof in which R1 and R2 are independently H or methyl, including individual enantiomers or racemates thereof, (for example N,N-dimethyl-1-[1-(4-chlorophenyl)cyclobutyl]-3-methylbutylamine hydrochloride optionally in the form of its monohydrate) is used for treating sleeping disorders including sleep apnoea and snoring.Type: GrantFiled: March 17, 2000Date of Patent: April 2, 2002Assignee: Knoll Pharmaceutical CompanyInventors: Sharon C. Cheetham, David J. Heal, Carl M. Mendel, Timothy B. Seaton, Steve P. Weinstein, Anton Safer
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Patent number: 6365633Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof in which R1 and R2 are independently H or methyl (for example N,N-dimethyl-1-[1-(4-chlorophenyl)cyclobutyl]-3-methylbutyl amine hydrochloride optionally in the form of its monohydrate) is used for treating eating disorders, such as anorexia nervosa, bulimia nervosa, weight-gain after smoking cessation, snacking or binge eating.Type: GrantFiled: March 17, 2000Date of Patent: April 2, 2002Assignee: Knoll Pharmaceutical CompanyInventors: Sharon C. Cheetham, David J. Heal, Carl M. Mendel, Timothy B. Seaton, Steve P. Weinstein
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Patent number: 6358944Abstract: The present invention relates to methods and compositions comprising a very low dose of cyclobenzaprine or metabolite thereof for preventing and treating Generalized Anxiety Disorder. The present invention further relates to methods and compositions for treating and preventing symptoms associated with Generalized Anxiety Disorder using a very low dose of cyclobenzaprine.Type: GrantFiled: August 11, 2000Date of Patent: March 19, 2002Assignee: Vela Pharmaceuticals, Inc.Inventors: Seth Lederman, Iredell W. Iglehart, III
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Patent number: 6355685Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof in which R1 and R2 are independently H or methyl (for example N,N-dimethyl-1-[1-(4-chlorophenyl)cyclobutyl]-3-methylbutyl amine hydrochloride optionally in the form of its monohydrate), including individual enantiomers and racemates thereof, is used for treating anxiety disorders.Type: GrantFiled: March 17, 2000Date of Patent: March 12, 2002Assignee: Knoll Pharmaceutical CompanyInventors: Sharon C. Cheetham, David J. Heal, Graham P. Luscombe
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Publication number: 20020022663Abstract: A dosage form for intranasal and/or inhalation administration of an analgesic having low opioid receptor binding activity to a warm blooded animal, that includes a pharmaceutically effective amount of the analgesic. A preferred analgesic is tramadol, a tramadol and/or a pharmaceutically acceptable salt, metabolite or derivative thereof. Methods of making and using the formulation according to the invention are also provided.Type: ApplicationFiled: August 16, 2001Publication date: February 21, 2002Inventors: Mark Alfonso, Paul Goldenheim, Richard Sackler
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Publication number: 20020010198Abstract: Methods are disclosed for the treatment and prevention of disorders and conditions such as, but are not limited to: eating disorders; weight gain; obesity; irritable bowel syndrome; obsessive-compulsive disorders; platelet adhesion; apnea; affective disorders such as attention deficit disorders, depression, and anxiety; male and female sexual function disorders; restless leg syndrome; osteoarthritis; substance abuse including nicotine and cocaine addiction; narcolepsy; pain such as neuropathic pain, diabetic neuropathy, and chronic pain; migraines; cerebral function disorders; chronic disorders such as premenstrual syndrome; and incontinence.Type: ApplicationFiled: January 29, 2001Publication date: January 24, 2002Inventors: Thomas P. Jerussi, Chrisantha H. Senanayake, Qun K. Fang
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Patent number: 6335372Abstract: A method for the treatment of OCD in a mammal by administering to the mammal an effective amount of 1,7,7-trimethylbicyclo[2.2.1]heptane derivative of Formula I wherein R is hydrogen or methyl, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: November 28, 2000Date of Patent: January 1, 2002Assignee: Orion CorporationInventors: Outi Mäki-Ikola, Matti Wallin, Juha Rouru, Leena Lehtonen, Martti Jaskari
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Patent number: 6335371Abstract: A method for inducing cognition enhancement in a mammal by administering to the mammal an effective amount of 1,7,7-trimethylbicyclo[2.2.1]heptane derivative of Formula I wherein R is hydrogen or methyl, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: November 28, 2000Date of Patent: January 1, 2002Assignee: Orion CorporationInventor: Outi Mäki-Ikola
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Patent number: 6335469Abstract: The invention relates to high purity (1R,2S,4R)-(−)-2-[(2′-{N,N-dimethylamino}-ethoxy)]-2-[phenyl]-1,7,7-tri-[methyl]-bicyclo[2.2.1]heptane and pharmaceutically acceptable acid addition salts thereof containing not more than 0.2% of (1R,3S,4R)-3-[(2′-{N,N-dimethylamino}-ethyl)]-1,7,7-tri-[methyl]-bicyclo[2.2.1]heptane-2-one and/or of a pharmaceutically acceptable acid addition salt thereof. Furthermore the invention is concerned with a process for the preparation of these compounds. Moreover the invention relates to medicaments containing 1 or more of these compounds and their use.Type: GrantFiled: May 10, 2000Date of Patent: January 1, 2002Assignee: Orion CorporationInventors: Gyula Lukács, Gyula Simig, Tibor Mezei, Zoltán Budai, Márta Porcs-Makkay, György Krasznai, Kálmán Nagy, Györgyi Donáth Vereczkey, Tibor Szabó, Norbert Németh, János Szulágyi
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Patent number: 6333358Abstract: An aryloxyaniline derivative represented by the formula: wherein Ar1 and Ar2 are each a substituted or unsubstituted phenyl group, pyridyl group or naphthyl group, R1 is a hydrogen atom, an alkyl group, etc., X1 is a hydrogen atom, an alkyl group, etc., y1 is a branched or unbranched alkylene group having 1 to 6 carbon atoms or a single bond; or a pharmaceutically acceptable salt thereof can provide medicines having a high affinity for MDR, and therefore, exhibiting a therapeutic or preventive effect on anxiety, related diseases thereto, depression, etc.Type: GrantFiled: February 1, 2000Date of Patent: December 25, 2001Assignees: Taisho Pharmaceutical Co., Ltd., Nihon Nohyaku Co., Ltd.Inventors: Atsuro Nakazato, Taketoshi Okubo, Toshio Nakamura, Shigeyuki Chaki, Kazuyuki Tomisawa, Masashi Nagamine, Kenji Yamamoto, Koichiro Harada, Masanori Yoshida
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Patent number: 6329399Abstract: Novel amine derivatives having an excellent antimycotic effect represented by general formula (1) below and salts thereof are provided. [in the formula (1, R1 represents a C1-5 alkyl group which may be halogenated, R2 represents 4-(1,1-dimethylalkyl)benzyl group, 4-(1-methyl-phenylethyl)benzyl group, 1-or 2-naphthylmethyl group, or a hydrocarbon group having 3,3-dimethyl-1-butynyl group or a phenyl group at its terminal and 1 to 3 double bonds; R3 represents oxygen atom or a methylene group which may be substituted by a C1-4 alkyl group; and R4 represents 1-or 2 naphthyl group or a phenyl group which may be substituted.Type: GrantFiled: May 18, 2000Date of Patent: December 11, 2001Assignee: Pola Chemical Industries, Inc.Inventors: Takao Itoh, Takuji Nakashima, Akira Nozawa, Kouji Yokoyama, Hiroyuki Takimoto, Masayuki Yuasa, Yukio Kawazu, Toshimitsu Suzuki, Toshiro Majima
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Patent number: 6329552Abstract: The invention relates to a compound of formula (I), wherein R is an alkyl unsubstituted by one or more polar substituents or an alkenyl unsubstituted or substituted by one or more polar substituents, and X is aryl, or salts thereof. The compounds are effective e.g. against protozoa and trematodes.Type: GrantFiled: December 22, 2000Date of Patent: December 11, 2001Assignee: Novartis AGInventors: Thomas Allmendinger, Walther Helmut Wernsdorfer
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Patent number: 6284799Abstract: The present invention is concerned with the identification of compounds which increase the therapeutic index of chemotherapy drugs and which stimulate the growth of cancers, their use in the treatment of cancer and with certain novel compounds useful in such treatment.Type: GrantFiled: December 26, 1996Date of Patent: September 4, 2001Assignee: University of ManitobaInventor: Lorne J. Brandes
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Patent number: 6239175Abstract: Derivatives of mutiline of formula (1A) and pharmaceutically acceptable salts and derivatives thereof, in which R1 is ethyl or vinyl, Y is a carbamoyloxy group, in which the N-atom is unsubstituted, or mono- or di-substituted, are useful in the treatment of bacterial infections.Type: GrantFiled: December 21, 1999Date of Patent: May 29, 2001Assignee: Smithkline Beecham p.l.c.Inventors: Jeremy David Hinks, Andrew Kenneth Takle, Eric Hunt
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Patent number: 6235791Abstract: The present invention relates to the use of compounds capable of displacing tritiated cis-N-cyclohexyl-N-ethyl [3-(3-chloro-4-cyclohexylphenyl)-allyl]amine from its receptors for the preparation of pharmaceutical compositions intended to combat cell proliferation.Type: GrantFiled: April 12, 1999Date of Patent: May 22, 2001Assignee: Sanofi-SynthelaboInventors: Jean Claude Breliere, Pascual Ferrara, Christine Lebouteiller, Raymond Paul, Jorge Rosenfeld, Didier Van Broeck
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Patent number: 6232347Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof in which R1 and R2 are independently H or methyl (for example N,N-dimethyl-1-[1-(4-chlorophenyl)cyclobutyl]-3-methylbutyl amine hydrochloride optionally in the form of its monohydrate) is used for treating osteoarthritis or gout.Type: GrantFiled: March 17, 2000Date of Patent: May 15, 2001Assignee: Knoll Pharmaceutical CompanyInventors: Carl M. Mendel, Timothy B. Seaton, Steve P. Weinstein
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Patent number: 6221871Abstract: Disclosed are compounds of the formula: where S and V are various organic or inorganic substituents; G and K are the same or different and represent N or CR′ where R′ is an organic or inorganic substituent; R is hydrogen or an alkyl group; R1, X, Y, Z and T are organic or inorganic substituents; and R2 and R3 represent hydrogen or organic substituents; or NR2R3 together represents a heterocyclic ring system; and the pharmaceutically acceptable salts thereof; which are highly selective partial agonists or antagonists at brain dopamine receptor subtypes and, thus, are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.Type: GrantFiled: June 11, 1999Date of Patent: April 24, 2001Assignee: Neurogen CorporationInventors: Jun Yuan, Andrew Thurkauf
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Patent number: 6214885Abstract: The use of polymers containing &bgr;-hydroxyalkylvinylamine units, as obtainable by reacting polymers containing vinylamine units with epoxides of the formula in which R is C2-C28 alkyl, phenyl, C1-C18 alkylphenyl or C2-C18 alkenyl, as biocides.Type: GrantFiled: March 7, 2000Date of Patent: April 10, 2001Assignee: BASF AktiengesellschaftInventors: Jürgen Tropsch, Dieter Zeller, Anton Negele, Norbert Mahr, Jürgen Decker
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Patent number: 6191171Abstract: para-Aminomethylaryl carboxamides of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.Type: GrantFiled: November 13, 1998Date of Patent: February 20, 2001Assignee: Merck & Co., Inc.Inventors: Stephen E. DeLaszlo, William K. Hagmann
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Patent number: 6184239Abstract: Controlled cessation of heart beat during coronary bypass surgery and other cardiac surgeries on a beating heart improves surgical technique, and is achieved typically by electrical stimulation of the vagus nerve and administration of a combination of drugs.Type: GrantFiled: August 25, 1998Date of Patent: February 6, 2001Assignee: Emory UniversityInventor: John D. Puskas
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Patent number: 6147119Abstract: Compounds of formula (I), wherein [X] represents aromatic carbocyclic rings (A) and (B), where R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are as defined in the description, salts thereof, a method and intermediates for preparing same, the use thereof as drugs, and pharmaceutical compositions containing same, are disclosed.Type: GrantFiled: September 28, 1998Date of Patent: November 14, 2000Assignee: Hoechst Marion RousselInventor: Dominique Lesuisse
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Patent number: 6107345Abstract: A compound of formula (I): ##STR1## wherein: Z.sub.1, Z.sub.2, Z.sub.3, Z.sub.4, which may be identical or different, represent a group as defined in the description,X represents oxygen, S(O).sub.p, --(CH.sub.2).sub.n -- or --CH.sub.2 --Y--CH.sub.2 -- wherein p, n and Y are as defined in the description,A represents ##STR2## wherein m, R.sub.1, R.sub.2 and G are as defined in the description, their isomers and addition salts thereof with a pharmaceutically-acceptable acid, and medicinal products containing the same are useful in the treatment of diseases like depression, panic attacks, obsessive compulsive disorders, phobias, impulsive disorders, drug abuse or anxiety.Type: GrantFiled: March 3, 1999Date of Patent: August 22, 2000Assignee: Adir et CompagnieInventors: Jean-Louis Peglion, Aimee Dessinges, Jean-Christophe Harmange, Mark Millan, Adrian Newman-Tancredi, Mauricette Brocco
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Patent number: 6093747Abstract: The new compound of Formula (I) and salts thereof possess valuable anxiolytic properties.Type: GrantFiled: June 14, 1999Date of Patent: July 25, 2000Assignee: Egis Gyogyszergyar RT.Inventors: Istvan Gacsalyi, Imre Klebovich, Zoltan Budai, Gyula Lukacs, Erzsebet Kaufmanne Bojti, Eva Schmidt, Istvan Gyertyan, Andras Bilkei Gorzo, Gabor Blasko, Miklos Abermann, Katalin Baloghne Nemes, Gyula Grezal, Andras Egyed
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Patent number: 6080790Abstract: Compounds of formula (1) ##STR1## are described wherein Y represents a halogen atom or a group --OR.sup.1, where R.sup.1 is an optionally substituted alkyl group; R.sup.2 represents an optionally substituted cycloalkyl or cycloalkenyl group; R.sup.3 is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen or sulphur atoms or a group --N(R.sup.4)-- where R.sup.4 is a hydrogen atom or an alkyl group; X is --O--, --S--, or --N(R.sup.5)--, where R.sup.5 is a hydrogen or an alkyl group; with the proviso that when X is --O-- then R.sup.3 is not a 3-cyanamino-6-pyridazinyl or a 3-chloro-6-pyridazinyl group; and the salts, solvates, hydrates and N-oxides thereof.The compounds are selective and potent inhibitors of phosphodiesterase IV and are useful for the prophylaxis and treatment of inflammatory diseases and the alleviation of conditions associated with central nervous malfunction.Type: GrantFiled: May 30, 1997Date of Patent: June 27, 2000Assignee: Celltech Therapeutics, LimitedInventors: Ewan Campbell Boyd, Michael Anthony William Eaton, Graham John Warrellow
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Patent number: 6020368Abstract: Derivatives of mutiline of formula (1A) and pharmaceutically acceptable salts and derivatives thereof, in which R.sup.1 is ethyl or vinyl, Y is a carbamoyloxy group, in which the N-atom is unsubstituted, or mono- or di-substituted, are useful in the treatment of bacterial infections.Type: GrantFiled: December 4, 1998Date of Patent: February 1, 2000Inventors: Jeremy David Hinks, Andrew Kenneth Takle, Eric Hunt
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Patent number: 6008411Abstract: Nortriptyline functionalized compounds are provided for conjugation to antigenic compositions, particularly poly(amino acids), and enzymes. The antigenic conjugates are employed for the production of antibodies, which find use in immunoassays for the determination of nortriptyline in a sample, while the enzyme conjugates find use in an enzyme assay for the determination of nortriptyline in a sample.Type: GrantFiled: June 7, 1995Date of Patent: December 28, 1999Assignee: Dade Behring Marburg GmbHInventors: Mae W. Hu, Prithipal Singh
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Patent number: 5990151Abstract: The present invention relates to an optically active, substituted phenylalkylamine derivative represented by Formula [1]: ##STR1## wherein A is a substituted or non-substituted phenyl or thienyl; X.sup.1 is hydrogen, halogen, hydroxyl or a substituted or non-substituted C.sub.1-5 alkoxy; R.sup.1 and R.sup.2 are equally or differently hydrogen, C.sub.1-7 alkyl, C.sub.3-7 alkenyl or C.sub.3-7 alkynyl; R.sup.3 is C.sub.1-10 alkyl, C.sub.2-10 alkenyl or C.sub.2-10 alkynyl; n is an integer from 2 to 5; and m is an integer from 1 to 4,or a pharmaceutically acceptable salt thereof, and pharmaceutical use of such compound or salt. The compound of the invention is excellent in sigma 1 receptor antagonism and useful for treating schizophrenia, depression, anxiety, cerebrovascular diseases/senile troublesome behaviors, and cognitive dysfunctions and motor dysfunctions such as Alzheimer's disease, Parkinson's disease and Huntington's disease which are neurodegenerative diseases.Type: GrantFiled: May 15, 1998Date of Patent: November 23, 1999Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Atsuro Nakazato, Toshihito Kumagai, Tomoki Miyazawa, Koumei Ohta, Yutaka Kawashima, Katsuo Hatayama, deceased
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Patent number: 5985906Abstract: Use of a combination of the squalene epoxidase inhibitor terbinafine and an azole 14-alpha-methyldemethylase inhibitor (fluconazole or itraconazole) in mycotic infections caused by azole-resistant fungal strains, and corresponding pharmaceutical compositions, process and method.Type: GrantFiled: November 12, 1997Date of Patent: November 16, 1999Assignee: Novartis AGInventors: Josef Gottfried Meingassner, Neil Stewart Ryder
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Patent number: 5968908Abstract: The invention is novel analogs of 9-cis-retinoic acid which are useful for the treatment and prevention of coronary artery disease and to protect against premature atherosclerosis by increasing HDL levels. The invention includes processes for preparing the novel 9-cis-retinoic acid analogs.Type: GrantFiled: November 14, 1995Date of Patent: October 19, 1999Assignee: American Cyanamid CompanyInventors: Joseph William Epstein, Feng Ling Qing, Gary Harold Birnberg, Adam Matthew Gilbert
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Patent number: 5952350Abstract: The invention provides a compound of formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical compositions containing a compound of formula I, and methods of using a compound of formula I for inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions including hyperlipidemia, and estrogen dependent cancer.Type: GrantFiled: October 23, 1997Date of Patent: September 14, 1999Assignee: Eli Lilly and CompanyInventors: George Joseph Cullinan, Brian Stephen Muehl
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Patent number: 5935998Abstract: Use of compounds of formula (I), wherein R has various significances, in free base form or in pharmaceutically acceptable salt form, as agents against H. pylori infection and associated diseases.Type: GrantFiled: January 6, 1998Date of Patent: August 10, 1999Assignee: Novartis AGInventors: Ivan James Dalton Lindley, Neil Stewart Ryder
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Patent number: 5889000Abstract: The invention provides naphthofluorene compounds, intermediates, formulations, processes, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, cardiovascular-related pathological conditions, including hyperlipidemia, and estrogen-dependent cancer.Type: GrantFiled: September 22, 1997Date of Patent: March 30, 1999Assignee: Eli Lilly and CompanyInventors: Henry Uhlman Bryant, Jeffrey Alan Dodge, Charles Willis Lugar, III
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Patent number: 5877214Abstract: The present invention is directed to the certain polyaryl-poly(ethylene glycol) compounds ("polyaryl-PEG" compounds) which are useful as soluble polyvalent supports in the preparation of combinatorial libraries of compounds. The resultant combinatorial libraries are useful in screening for biologically active moieties in the drug discovery process or in developing compounds with desired physical and chemical properties.Type: GrantFiled: September 4, 1997Date of Patent: March 2, 1999Assignee: Merck & Co., Inc.Inventor: Ronald M. Kim
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Patent number: 5821253Abstract: The invention provides tetrahydrobenzo?a!fluorene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions, including hyperlipidemia.Type: GrantFiled: September 24, 1997Date of Patent: October 13, 1998Assignee: Eli Lilly and CompanyInventors: Henry Uhlman Bryant, George Joseph Cullinan
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Patent number: 5792762Abstract: The invention provides dihydronaphthofluorene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions.Type: GrantFiled: September 19, 1997Date of Patent: August 11, 1998Assignee: Eli Lilly and CompanyInventors: Henry Uhlman Bryant, Thomas Alan Crowell, Charles David Jones
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Patent number: 5744492Abstract: Angiogenesis is a composite of regulated proliferation and regulated invasion occuring in a variety of normal and pathologic conditions. Compound 1 and related analogs are useful for inhibiting angiogenesis in a host and offer a novel approach to the treatment of cancer, diabetic retinopathy, hemangiomata, vasculidities and other diseases associated with angiogenesis.Type: GrantFiled: March 10, 1994Date of Patent: April 28, 1998Assignee: United States of AmericaInventors: Elise C. Kohn, Lance A. Liotta, Riccardo Alessandro
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Patent number: 5723489Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof wherein: R.sup.1 to R.sup.9 are as defined herein and m is the integer 0 or 1.These compounds are beta 3 adrenergic receptor agonists and are useful, therefore for example, in the treatment of diabetes, obesity, gastrointestinal diseases and achalasia.Type: GrantFiled: May 7, 1996Date of Patent: March 3, 1998Assignee: Bristol-Myers Squibb CompanyInventors: Philip M. Sher, William N. Washburn, Kathleen M. Poss
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Patent number: 5719150Abstract: This invention relates to a 1,2-ethanediol derivative and a salt thereof, a process for producing the same, and a cerebral function-improving agent comprising the same. The cerebral function-improving agent of this invention is useful for treating cerebrovascular dementia, senile dementia, Alzheimer's dementia, sequelae of ischemic encephalopathy and cerebral apoplexy.Type: GrantFiled: November 14, 1996Date of Patent: February 17, 1998Assignee: Toyama Chemical Co., Ltd.Inventors: Satoshi Ono, Tetsuo Yamafuji, Hisaaki Chaki, Mutsuko Maekawa, Yozo Todo, Hirokazu Narita
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Patent number: 5712271Abstract: The present invention relates to a novel method for treating a mammal suffering from urinary bladder dysfunctions.Type: GrantFiled: October 3, 1996Date of Patent: January 27, 1998Inventors: Mark A. Muhlhauser, Harlan E. Shannon, Karl B. Thor
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Patent number: 5712287Abstract: The present invention relates to a novel method for treating a mammal suffering from urinary bladder dysfunctions.Type: GrantFiled: October 3, 1996Date of Patent: January 27, 1998Inventors: Mark A. Muhlhauser, Harlan E. Shannon, Karl B. Thor
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Patent number: 5710151Abstract: The present invention relates to a novel method for treating a mammal suffering from urinary bladder dysfunctions.Type: GrantFiled: October 3, 1996Date of Patent: January 20, 1998Inventors: Mark A. Muhlhauser, Harlan E. Shannon, Karl B. Thor
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Patent number: 5681846Abstract: The present invention is directed to improved pharmaceutical compositions employing paclitaxel that are formulated to increase stability and solubility. These improved formulations are useful in long-term, multi-day continuous infusion protocols, and have the advantage of reducing the number of infusion system breaks during the entire period of drug administration. Also disclosed are kits for use in preparing paclitaxel for long-term infusion and enhanced solubility.Type: GrantFiled: March 17, 1995Date of Patent: October 28, 1997Assignee: Board of Regents, The University of Texas SystemInventor: Lawrence A. Trissel