Nitrogen, Other Than As Nitro Or Nitroso, Attached Directly To The Isoquinoline Ring System By Nonionic Bonding Patents (Class 514/310)
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Patent number: 6262074Abstract: Hetaroyl derivatives of the formula I where: R1 and R2 are each hydrogen, nitro, halogen, cyano, thiocyanato, hydroxyl, mercapto, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylthio, C1-C6-alkylsulfinyl, C1-C6-alkylsulfonyl or C1-C6-alkoxysulfonyl, where the last 6 radicals may be substituted and/or functionalized; phenyl, phenoxy, phenylthio, phenylsulfinyl or phenylsulfonyl, where the last 5 radicals may be substituted; Z is an unsubstituted or substituted four-membered unsaturated, partially or fully saturated chain consisting of three carbons and one nitrogen; Q is unsubstituted or substituted hydroxypyrazole linked at position 4; and their agriculturally useful salts. A process for preparing the hetaroyl derivatives, compositions comprising them, and the use of these derivatives or these compositions comprising them for controlling undesirable plants.Type: GrantFiled: March 17, 1999Date of Patent: July 17, 2001Assignee: BASF AktiengesellschaftInventors: Martina Otten, Norbert Götz, Wolfgang von Deyn, Stefan Engel, Uwe Kardorff, Michael Rack, Regina Luise Hill, Peter Plath, Matthias Witschel, Karl-Otto Westphalen, Helmut Walter, Ulf Misslitz
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Patent number: 6258816Abstract: A novel composition of Nimesulide and salts thereof and Cetrizine possessing antileukotriene, antihistaminic, antiallergic and antiinflammatory action is disclosed. The composition is useful in the cure of allergic disorders such as rhinitis, bronchitis, asthama, urticaria and the like.Type: GrantFiled: October 26, 1998Date of Patent: July 10, 2001Assignee: Panacea Biotec LimitedInventors: Amarjit Singh, Rajesh Jain
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Publication number: 20010005723Abstract: This invention relates to the use of eprosartan to treat isolated systolic hypertension.Type: ApplicationFiled: February 6, 2001Publication date: June 28, 2001Applicant: SmithKline Beecham CorporationInventors: David P. Brooks, Giora Z. Feuerstein, Eliot H. Ohlstein, Robert R. Ruffolo
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Publication number: 20010004638Abstract: An improved platelet gel wound healant, and methods of preparation and use thereof for healing wounds are disclosed. The improved wound healant comprises a therapeutically effective amount of activated growth factors and ascorbic acid with optional one or more additional anti-oxidant such as vitamin A and/or E, and optional one or more antibiotics.Type: ApplicationFiled: January 26, 2001Publication date: June 21, 2001Inventor: Charles E. Worden
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Patent number: 6248738Abstract: Compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein one of R1 and R2 is H and the other is N═C(NH2)2 or NHC(═NH)NH2, and the other substituents are as defined herein, are urokinase (uPA) inhibitors.Type: GrantFiled: May 30, 2000Date of Patent: June 19, 2001Assignee: Pfizer Inc.Inventors: Roger Peter Dickinson, Christopher Gordon Barber, Paul Vincent Fish
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Patent number: 6248754Abstract: The present invention relates to substituted isoquinoline derivatives and their use as anticonvulsants.Type: GrantFiled: June 15, 2000Date of Patent: June 19, 2001Assignee: SmithKline Beecham, p.l.c.Inventors: Steven Coulton, Roderick Alan Porter
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Publication number: 20010003751Abstract: A pharmaceutical composition for treating a transient ischemic attack which comprises a compound of the formula: 1Type: ApplicationFiled: January 26, 2001Publication date: June 14, 2001Inventors: Zen-ichi Terashita, Kaneyoshi Kato, Takenobu Sohma
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Patent number: 6245808Abstract: Organometallic oxovanadium (IV) complexes having potent spermicidal activity, particularly those having at least one bidentate ligand. Preferred compounds are stable oxovanadium (IV) complexes having, as ancillary ligands linked via nitrogen or oxygen-metal bonds, bis and/or mono-1,10-phenanthroline; 2,2′-bipyridyl; or 2-hydroxyacetophenone.Type: GrantFiled: November 5, 1998Date of Patent: June 12, 2001Assignee: Parker Hughes InstituteInventors: Fatih M. Uckun, Osmond D'Cruz, Wanhong Dong
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Patent number: 6245780Abstract: Compounds are provided which have the formula: wherein: R1, R2, R3, and R4 are, independently, hydrogen, halogen, alkoxy, or carboxamide; R5 is hydrogen, halogen, CF3, CN, carbamide or alkoxy; and X is (CH2)n or a 4-6 membered carbocyclic ring, wherein n is an integer of 2 to 4; or pharmaceutically acceptable salts thereof.Type: GrantFiled: April 17, 2000Date of Patent: June 12, 2001Assignee: American Home Products CorpInventors: Richard E. Mewshaw, Kristin L. Meagher
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Publication number: 20010002399Abstract: Use of low dosages of an aldosterone receptor antagonist, spironolactone, is described for treatment of circulatory disorders. This therapy would be particularly useful to treat or retard the development of congestive heart failure, while avoiding or reducing aldosterone-antagonist-induced side effects, such as hyperkalemia.Type: ApplicationFiled: January 9, 2001Publication date: May 31, 2001Applicant: G.D. Searle & Co.Inventors: Todd E. MacLaughlan, Alfonso T. Perez
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Patent number: 6235752Abstract: Disclosed are compounds that are highly selective partial agonists or antagonists of CRF1 receptors. The disclosed compounds are useful in the diagnosis and treatment of stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache, and anxiety. The compounds are represented by the formula wherein R1, R2, R3, R4, and Ar represent various inorganic and organic substituents. Also disclosed are pharmaceutical compositions and methods of treating post traumatic stress disorder, depression, headache, and anxiety.Type: GrantFiled: September 20, 1999Date of Patent: May 22, 2001Assignee: Neurogen CorporationInventors: Jun Yuan, Taeyoung Yoon
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Patent number: 6228869Abstract: This invention provides, low molecular weight, non-peptide inhibitors of matrix metalloproteinases and TNF-&agr; converting enzyme (TACE, tumor necrosis factor-&agr; converting enzyme) of formula: B wherein B is P and Q are provided that when P is Q is and vice versa; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: April 14, 1998Date of Patent: May 8, 2001Assignee: American Cyanamid CompanyInventors: Jeremy I. Levin, Arie Zask, Yansong Gu, Jay D. Albright, Xuemei Du
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Patent number: 6221866Abstract: in which R(1) to R(8) have the meanings stated in the claims, act on the Kv1.5 potassium channel, and inhibit a potassium current, referred to as “ultra-rapidly activating delayed rectifier,” in the human atrium. They are therefore very particularly suitable as novel antiarrhythmic active substances, in particular for the treatment and prophylaxis of atrial arrhythmias, e.g., atrial fibrillation or atrial flutter.Type: GrantFiled: June 23, 2000Date of Patent: April 24, 2001Assignee: Aventis Pharma Deutschland GmbHInventors: Joachim Brendel, Uwe Gerlach, Hans Ulrich Stilz, Hans-Jochen Lang
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Patent number: 6214858Abstract: A compound of formula wherein R1 is hydrogen, or C1-4 alkyl; R2 is C1-10 alkyl, optionally substituted arylC1-4alkyl, optionally substituted heteroaryl C1-4 alkyl optionally substituted C3-7 cycloalkyl, or R1 and R2 together with the nitrogen to which they are attached from a 3 to 10 membered ring which optionally contains an aditional heteroatom selected from oxygen, nitrogen or sulfur, R3 and R4 are C1-6alkyl, hydrogen, nitro, or halogen and R5 is C1-6alkyl, hydrogen, arylalkyl or heteroarylalkyl. The present invention is to the novel compounds of Formula (I), their pharmaceutical compositions, and to the novel inhibition of Caspases for use in the treatment of apoptosis, and disease states caused by excessive or inappropriate cell death.Type: GrantFiled: December 9, 1999Date of Patent: April 10, 2001Assignee: SmithKline Beecham CorporationInventors: Dennis Lee, Scott Allen Long
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Patent number: 6214841Abstract: This application relates to a novel compound of formula (I) (or a pharmaceutically acceptable salt thereof) as defined herein, processes and Intermediates for its preparation, pharmaceutical formulations comprising the novel compound of formula (I), and the use of the compound of formula (I) as an antithrombotic agent.Type: GrantFiled: November 8, 1999Date of Patent: April 10, 2001Assignee: Eli Lilly and CompanyInventors: Charles Van Jackson, Kenneth Dean Kurz, Robert Theodore Shuman
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Patent number: 6207715Abstract: Compounds of the formula: are useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpes virus.Type: GrantFiled: November 22, 1999Date of Patent: March 27, 2001Assignee: American Home Products CorporationInventors: Jonathan Bloom, Kevin Curran, Martin DiGrandi, Russell Dushin, Stanley Lang, Emily Norton, Adma Ross, Bryan O'Hara
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Patent number: 6197771Abstract: Novel N-substituted azacycloalkyl ring fused 2,3-quinoxalinediones represented by the formula: or a pharmaceutically acceptable salt thereof, are disclosed, wherein the formula variables R1, R2, X, Y, m and n are as defined herein. Also disclosed are methods of treatment using the same and intermediate compounds useful in the preparation thereof.Type: GrantFiled: February 7, 2000Date of Patent: March 6, 2001Assignee: Warner-Lambert CompanyInventors: Christopher Franklin Bigge, Thomas Charles Malone, Robert Michael Schelkun, Chung Stephen Yi
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Patent number: 6194431Abstract: Methods and pharmaceutical compositions employing a terfenadine metabolite and a leukotriene inhibitor for the treatment or prevention of inflammation or allergic disorders, such as asthma, or symptoms thereof. Also included are methods and compositions employing a terfenadine metabolite, a leukotriene inhibitor, and a decongestant for the treatment or prevention of inflammation or allergic disorders, such as asthma, or symptoms thereof.Type: GrantFiled: April 14, 1998Date of Patent: February 27, 2001Inventor: Paul D. Rubin
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Patent number: 6194409Abstract: The present invention relates to antithrombotic compounds comprising the group Q, Q having formula (I), wherein the substructure (i) is a structure selected from (a, b and c), wherein X is O or S; X′ being independently CH or N; and m is 0, 1, 2 or 3; wherein the group Q is bound through an oxygen atom or an optionally substituted nitrogen or carbon atom, or a pharmaceutically acceptable salt thereof or a prodrug thereof. The compounds of the invention are therapeutically active and in particular are antithrombotic agents.Type: GrantFiled: October 19, 1999Date of Patent: February 27, 2001Assignee: Akzo Nobel N.V.Inventors: Constant Adriaan Anton van Boeckel, Philippus Johannes Marie van Galen, Johannes Bernardus Maria Rewinkel
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Patent number: 6194427Abstract: Disclosed are compounds of the Formula: or the pharmaceutically acceptable non-toxic salts thereof wherein: the C ring is a(n) (un)substituted carbocycle; X is hydrogen, hydroxyl or lower alkyl; and W is (un)substituted alkyl, aryl, arylalkyl, or heteroaryl, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.Type: GrantFiled: February 26, 1999Date of Patent: February 27, 2001Assignee: Neurogen CorporationInventors: Robert W. DeSimone, Daniel L. Rosewater
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Patent number: 6174901Abstract: Selected novel substituted pyridine and pyridazine compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as cancer, pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, cancer, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: December 18, 1998Date of Patent: January 16, 2001Assignee: Amgen Inc.Inventors: Nathan B. Mantlo, Chan-Kou Hwang, Ulrike D. Spohr
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Patent number: 6169094Abstract: A composition is provided comprising an antipsychotic effective amount of (S)(−)-amisulpride, (S)-(−)-4-amino-N-[(1-ethylpyrrolidin-2-yl)methyl]-5-ethylsulfonyl)-2-methoxybenzamide. A preferred composition comprises the (D)-tartrate salt of (S)(−)-amisulpride. The (S)(−) enantiomer exhibits antipsychotic properties and administration of the specific enantiomer reduces adverse side effects by reducing toxicity.Type: GrantFiled: July 14, 1998Date of Patent: January 2, 2001Assignee: Sanofi-SynthelaboInventors: Ghislaine Perrault, Hans Schoemaker, Jo{umlaut over (e)}l Miget
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Patent number: 6166219Abstract: Novel benzimidazole derivatives represented by the formula (I): ##STR1## wherein R.sub.3 is a carboxyl group, a esterified carboxyl group, an amidated carboxyl group, an amino group, an amido group, or a sulfonyl group, or their pharmaceutically acceptable salts. Because of their blood sugar-depressing effect or PDE5 inhibitory effect, these compounds or salts thereof are useful as medicines for treating impaired glucose tolerance, diabetes, diabetic complications, syndrome of insulin resistance, hyperlipidemia, atherosclerosis, cardiovascular disorders, hyperglycemia, or hypertension; or stenocardia, hypertension, pulmonary hypertension, congestive heart failure, glomerulopathy, tubulointerstitial disorders, renal failure, atherosclerosis, angiostenosis, distal angiopathy, cerebral apoplexy, chronic reversible obstructions, allergic rhinitis, urticaria, glaucoma, diseases characterized by enteromotility disorders, impotence, diabetic complications, nephritis, cancerous cachexia, or restenosis after PTCA.Type: GrantFiled: November 2, 1998Date of Patent: December 26, 2000Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Noritsugu Yamasaki, Takafumi Imoto, Yoshiyuki Murai, Takahiro Hiramura, Teruo Oku, Kouzou Sawada
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Patent number: 6143762Abstract: Compounds of formula (I), wherein R.sup.1 represents a substituent selected from: a hydrogen or halogen atom; a hydroxy, cyano, nitro, trifluoromethyl, trifluoromethoxy, trifluoromethanesulfonyloxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, arylC.sub.1-4 alkoxy, C.sub.1-4 alkylthio, C.sub.1-4 alkoxyC.sub.1-4 alkyl, C.sub.3-6 cycloalkylC.sub.1-4 alkoxy, C.sub.1-4 alkanoyl, C.sub.1-4 alkoxycarbonyl, C.sub.1-4 alkylsulphonyl, C.sub.1-4 alkylsulphonyloxy, C.sub.1-4 alkylsulphonylC.sub.1-4 alkyl, arylsulphonyl, arylsulphonyloxy, arylsulphonylC.sub.1-4 alkyl, C.sub.1-4 alkylsulphonamido, C.sub.1-4 alkylamido, C.sub.1-4 alkylsulphonamidoC.sub.1-4 alkyl, C.sub.1-4 alkylamidoC.sub.1-4 alkyl, arylsulphonamido, arylcarboxamido, arylsulphonamidoC.sub.1-4 alkyl, arylcarboxamidoC.sub.1-4 alkyl, aroyl, aroylC.sub.1-4 alkyl, or arylC.sub.1-4 alkanoyl group; a group R.sup.3 OCO(CH.sub.2).sub.p, R.sup.3 CON(R.sup.4)(CH2)p, R.sup.3 R.sup.4 NCO(CH.sub.2).sub.p or R.sup.3 R.sup.4 NSO.sub.2 (CH.sub.2).sub.p where each of R.sup.3 and R.Type: GrantFiled: February 11, 1999Date of Patent: November 7, 2000Assignee: SmithKline Beecham, plcInventors: David John Nash, Geoffrey Stemp
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Patent number: 6140315Abstract: A method of decreasing atherosclerosis and its complications, such as myocardial infarction, stroke and peripheral vascular disease, wherein the method involves administering to a human or an animal an amount of goserelin acetate sufficient to decrease atherosclerosis and its complications.Type: GrantFiled: June 5, 1998Date of Patent: October 31, 2000Inventors: Kenneth M. Weisman, Michael Goldberg
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Patent number: 6139847Abstract: This invention pertains to the use of a combination of angiotensin inhibitors and nitric oxide stimulators to slow and reverse the process of fibrosis in the body. This combination of medicaments is particularly useful in the treatment of a variety of cardiovascular fibrotic pathologies, such as that associated with left ventricular hypertrophy secondary to hypertension, myocardial infarction, and myocarditis.Type: GrantFiled: February 18, 1997Date of Patent: October 31, 2000Assignee: Trustees of Boston UniversityInventors: Aram Chobanian, Peter Brecher
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Patent number: 6127379Abstract: Compounds of the general formula (I), and pharmaceutically acceptable salts thereof, ##STR1## in which X.sub.1 --(CH.sub.2).sub.x --X.sub.2 and the aromatic carbon atoms to which they are attached form a 5-7 membered ring,wherein:one of X.sub.1 and X.sub.2 is O, S or CH.sub.2 and the other is CH.sub.2 ;x is 1, 2 or 3;R.sub.1 is hydrogen, amino, halo, C.sub.1-6 alkyl, hydroxy or C.sub.1-6 alkoxy;R.sub.2 is hydrogen, halo, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, nitro, amino or C.sub.1-6 alkylthio;R.sub.3 is hydrogen, halo, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or amino;R.sub.4 and R.sub.5 are independently hydrogen or C.sub.1-6 alkyl;Y is O or NH;Z is of sub-formula (a), (b) or (c): ##STR2## wherein n.sup.1 is 1, 2, 3 or 4; n.sup.2 is 1 or 2; n.sup.3 is 2, 3, 4 or 5;q is 0, 1, 2 or 3; p is 0, 0 or 2; m is 0, 1 or 2;R.sub.a is hydrogen or a lipophilic group, such as C.sub.1-12 alkyl or aralkyl; orR.sub.a is (CH.sub.2).sub.r --R.sub.10 wherein r is 2 or 3 and R.sub.10 is selected from cyano, hydroxyl, C.sub.Type: GrantFiled: August 3, 1994Date of Patent: October 3, 2000Assignee: SmithKline Beecham p.l.c.Inventors: Francis David King, Laramie Mary Gaster, Graham Francis Joiner
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Patent number: 6127381Abstract: The invention relates to melanocortin receptor ligands and methods of using the ligands to alter or regulate the activity of a melanocortin receptor. The invention further relates to tetrahydroisoquinoline aromatic amines that function as melanocortin receptor ligands and as agents for controlling cytokine-regulated physiologic processes and pathologies, and combinatorial libraries thereof.Type: GrantFiled: April 28, 1999Date of Patent: October 3, 2000Inventors: Amaresh Basu, Timothy C. Gahman, Beverly E. Girten, Michael C. Griffith, Curtis C. Hecht, John S. Kiely, Sandra R. Slivka
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Patent number: 6117898Abstract: There are provided compounds of formula (I), ##STR1## wherein D represents a five membered heterocyclic aromatic ring containing 1 to 4 heteroatoms selected from O, N or S, optionally substituted at a carbon atom by halogen, trifluoromethyl, alkyl C1 to 6, nitro or cyano, and which is connected to the remainder of the compound of formula (I) through a carbon atom; A represents N(X) or CH(--(CH.sub.2).sub.m --NXY); U represents NH, O or CH.sub.2 ; V represents (CH.sub.2).sub.a ; W represents (CH.sub.2).sub.b ; a, b, m, X and Y are as defined in the specification, together with processes for their preparation and compositions containing them. Compounds of formula (I) are nitric oxide synthetase inhibitors and are useful in therapy.Type: GrantFiled: July 22, 1999Date of Patent: September 12, 2000Assignee: Astra AktiebolagInventors: James Edwin MacDonald, William Calvin Shakespeare, Robert John Murray, James Russell Matz
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Patent number: 6114530Abstract: Disclosed are compounds that are highly selective partial agonists or antagonists at human CRF.sub.1 receptors that are useful in the diagnosis and treatment of treating stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache and anxiety. The compounds have the formula ##STR1## or the pharmaceutically acceptable salts thereof wherein Ar, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and W are various organic and inorganic substituents.Type: GrantFiled: June 22, 1998Date of Patent: September 5, 2000Assignee: Neurogen CorporationInventors: Jun Yuan, Taeyoung Yoon
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Patent number: 6110953Abstract: A pharmaceutical composition that inhibits the growth of tumors and cancers in mammals that comprises a 1H-1,2,4-triazole derivative along with a safe and effective amount of a chemotherapeutic agent. Potentiators can be used to enhance the effectiveness of the drugs. The triazoles and potentiators compounds can also be used to treat viral infections.Type: GrantFiled: February 5, 1999Date of Patent: August 29, 2000Assignee: The Procter & Gamble CompanyInventor: James Berger Camden
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Patent number: 6103737Abstract: Corticotropin releasing factor (CRF) antagonists of formula I: ##STR1## and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress in mammals.Type: GrantFiled: July 2, 1998Date of Patent: August 15, 2000Assignee: DuPont Pharmaceuticals CompanyInventors: Anthony J. Cocuzza, Frank W. Hobbs, James P. Beck, Paul J. Gilligan
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Patent number: 6093731Abstract: Isoquinolinylguanidine compounds of formula (I): ##STR1## wherein the substituents are as defined herein, and salts thereof, are disclosed as urokinase inhibitors.Type: GrantFiled: July 22, 1999Date of Patent: July 25, 2000Inventors: Roger Peter Dickinson, Paul Vincent Fish, Christopher Gordon Barber
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Patent number: 6093727Abstract: This invention is directed to novel imidazole and imidazoline derivatives which are selective agonists for cloned human a, adrenergic receptors. This invention is also related to the use of these compounds for the treatment of any disease where modulation of the .alpha..sub.2 receptors may be useful. The invention further provides for a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: October 20, 1998Date of Patent: July 25, 2000Assignee: Synaptic Pharmaceutical CorporationInventors: Wai C. Wong, Yoon T. Jeon, Charles Gluchowski
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Patent number: 6080763Abstract: Novel aromatic heterocyclic compounds inhibit cytokines production involved in immunoregulation and inflammation such as interleukin-1 and tumor necrosis factor production. The compounds are therefore useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.Type: GrantFiled: October 29, 1998Date of Patent: June 27, 2000Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: John R. Regan, Pier F. Cirillo, Eugene R. Hickey, Neil Moss, Charles L. Cywin, Christopher Pargellis, Thomas A. Gilmore
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Patent number: 6063789Abstract: Compounds of formula I ##STR1## wherein R, R.sup.1, R.sup.2, and R.sup.3 and A are as defined herein, together with pharmaceutically acceptable salts, enantiomers or tautomers are useful as pharmaceuticals, particularly in the treatment of inflammatory disease.Type: GrantFiled: August 19, 1997Date of Patent: May 16, 2000Assignee: Astra Pharmaceuticals, Ltd.Inventors: Peter R Hamley, James E MacDonald, James R Matz, Alan C Tinker
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Patent number: 6046191Abstract: The invention relates to the co-administration of an inhibitor of induced nitric oxide synthase and an inhibitor of cyclooxygenase-2 for the treatment of inflammation and inflammatory disorders.Type: GrantFiled: October 26, 1998Date of Patent: April 4, 2000Assignee: Astra Pharmaceuticals Ltd.Inventors: Peter Hamley, Alan Tinker
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Patent number: 6046211Abstract: The current invention discloses useful pharmaceutical compositions containing amidino derivative useful as nitric oxide synthase inhibitors.Type: GrantFiled: May 6, 1998Date of Patent: April 4, 2000Assignee: G.D. Searle & Co.Inventors: Donald W. Hansen, Jr., Mark G. Currie, E. Ann Hallinan, Kam F. Fok, Timothy J. Hagen, Arija A. Bergmanis, Steven W. Kramer, Len F. Lee, Suzanne Metz, William M. Moore, Karen B. Peterson, Barnett S. Pitzele, Dale P. Spangler, R. Keith Webber, Mihaly V. Toth, Mahima Trivedi, Foe S. Tjoeng
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Patent number: 6043254Abstract: The present invention relates to indolinones of general formula ##STR1## wherein R.sub.1 to R.sub.3 are defined in claim 1, the isomers and the salts thereof, particularly the physiologically acceptable salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on various kinases and cycline/CDK complexes and on the proliferation of various tumour cells, pharmaceutical compositions containing these compounds, their use and processes for preparing them.Type: GrantFiled: March 26, 1999Date of Patent: March 28, 2000Assignee: Boehringer Ingelheim Pharma KGInventors: Wolfgang Grell, Helmut Wittneben, Jacobus Constantinus Antonius van Meel, Norbert Redemann, Rainer Walter, Armin Heckel, Frank Himmelsbach, Robert Haigh
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Patent number: 6040315Abstract: Herein is disclosed how to make and to use a nonmetallic antacid composition which is the product of the co-polymerization of guanidine and polyethylenimine. The resultant polymer is useful as an antacid.Type: GrantFiled: October 29, 1998Date of Patent: March 21, 2000Inventor: Charles E. Day
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Patent number: 6034099Abstract: A method for treating neoplasia involving the administration of certain pyrazolinone derivatives.Type: GrantFiled: November 24, 1998Date of Patent: March 7, 2000Assignee: Cell Pathways, Inc.Inventors: Rifat Pamukcu, Gary A. Piazza
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Patent number: 6027936Abstract: Disclosed herein are methods directed generally to the control of neural activity and for selectively and controllably inducing the in vivo genetic expression of one or more naturally occurring genetically encoded molecules in mammals. More particularly, the present invention selectively activates or derepresses genes encoding for specific naturally occurring molecules such as neurotrophic factors through the administration of carbon monoxide dependent guanylyl cyclase modulating purine derivatives. The methods of the present invention may be used to affect a variety of cellular and neurological activities and to therapeutically or prophylactically treat a wide variety of neurodegenerative, neurological, and cellular disorders.Type: GrantFiled: May 29, 1998Date of Patent: February 22, 2000Inventor: Alvin J. Glasky
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Patent number: 6025368Abstract: Methods are provided for treating or alleviating the symptoms of subjects with psychological disorders, metabolic disorders, chronic stress-related disorders, sleep disorders, conditions associated with sexual senescence, aging, or premature aging by treating such subjects with IGF either alone or complexed with IGFBP-3. Methods for increasing the levels of DHEA or DHEAS and treating or alleviating the symptoms of subjects with disorders characterized by low levels of DHEA or DHEAS by administering effective amounts of IGF alone or complexed with IGFBP-3 are also provided. Methods for increasing the level of T4 and treating or alleviating the symptoms of subjects with disorders characterized by low levels of T3 or T4 by administering effective amounts of IGF alone or complexed with IGFBP-3 are additionally provided.Type: GrantFiled: February 25, 1997Date of Patent: February 15, 2000Assignee: Celtrix Pharmaceuticals, Inc.Inventors: Desmond Mascarenhas, Martin Sanders
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Patent number: 5998435Abstract: The instant invention is directed to a method for the treatment of emesis comprising administering the compound [R,S]-[2-(1H-Indol-3-yl)-1-methyl-1-(1-phenyl-ethylcarbamoly)-ethyl]-carba mic acid benzofuran-2ylmethyl ester.Type: GrantFiled: December 1, 1998Date of Patent: December 7, 1999Assignee: Warner-Lambert CompanyInventors: David Christopher Horwell, John Hughes, Martyn Clive Pritchard, Lakhbir Singh
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Patent number: 5981168Abstract: Methods and compositions, useful in the treatment of amyloidosis and conditions and diseases associated therewith, such as Alzheimer's Disease (AD). These methods involve administering to a subject a pharmaceutical composition including one or more agents which modulate APP catabolism and amyloid deposition. Accordingly, the methods and compositions are useful for inhibiting amyloidosis in disorders in which amyloid deposition occurs. The methods are based, at least in part, on modulating catabolism of APP in APP-containing cells through the use of a mobile ionophore, such as carbonyl cyanide p-(trifluoromethoxy) phenylhydrazone, which does not substantially alter the viability of those cells.Type: GrantFiled: May 15, 1998Date of Patent: November 9, 1999Assignee: The University of British ColumbiaInventors: Peter B. Reiner, Bruce P. Connop
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Patent number: 5976784Abstract: A method of treating metabolic bone diseases such as osteoporosis, as well as other disease states treatable with vitamin D compounds, comprises administering an effective amount of one or more modified vitamin D compound. The modified compound contains a typical vitamin D nucleus but with in vivo hydrolyzable groups at one or more of the 1, 3 and 25 carbon positions. The time of conversion of the modified compound to its active form, such as calcitriol, can be regulated to thus provide controlled release of the compound in vivo over time, by changing or modifying the hydrolyzable groups.Type: GrantFiled: May 22, 1998Date of Patent: November 2, 1999Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Heinrich K. Schnoes, Zu Y. Cai, Mary E. Phelps, Connie M. Smith
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Patent number: 5972975Abstract: Substituted 2-aminopyridine compounds of Formula (I) and pharmaceutically acceptable salts which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders.Type: GrantFiled: May 22, 1997Date of Patent: October 26, 1999Assignee: Merck & Co., Inc.Inventors: Craig Esser, William Hagmann, William Hoffman, Shrenik Shah, Kenny Wong, Renee Chabin, Ravindra Guthikonda, Malcolm Maccoss, Charles Caldwell, Philippe Durette
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Patent number: 5972937Abstract: The invention relates to heterocyclic families of compounds having pharmacological activity, in particular possessing 5HT.sub.2C receptor antagonist activity processes for their preparation, to compositions containing them and to their use in the treatment of CNS disorders.Type: GrantFiled: September 16, 1997Date of Patent: October 26, 1999Assignee: SmithKline Beecham p.l.c.Inventors: Laramie Mary Gaster, Paul Adrian Wyman, Keith Raymond Mulholland, David Thomas Davies
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Patent number: 5968950Abstract: A hydrochloride salt of an Apo B secretion/MTP inhibitor, methods of making the salt, methods of using the salt and pharmaceutical compositions containing the salt are disclosed.Type: GrantFiled: March 2, 1998Date of Patent: October 19, 1999Assignee: Pfizer IncInventors: George J. Quallich, George Chang, Lewin T. Wint
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Patent number: 5955472Abstract: Amyloid aggregation in animals is inhibited by administering a naphthylazo compound of formula (I), wherein R1 and R2 are hydrogen, alkyl, substituted alkyl, or complete a heterocyclic ring, R3 is hydrogen or alkyl, R4, R5, R6, and R7 are substitutent groups. The compounds are especially useful in preventing and treating Alzheimer's disease.Type: GrantFiled: April 29, 1998Date of Patent: September 21, 1999Assignee: Warner-Lambert CompanyInventors: Sheryl Jeanne Hays, Harry LeVine, III, Jeffery David Scholten