Tricyclo Ring System Having The Seven-membered Hetero Ring A One Of The Cyclos Patents (Class 514/217)
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Publication number: 20020045610Abstract: The present invention relates to the use of N-substituted azaheterocyclic compounds or salts thereof, for the treatment of conditions related to angiogenesis.Type: ApplicationFiled: June 1, 2001Publication date: April 18, 2002Inventors: Anker Jon Hansen, Tine Krogh Jorgensen, Uffe Bang Olsen
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Publication number: 20020037890Abstract: A pharmaceutical composition comprising synergistically effective amounts of cefpirome and dalfopristine/quinupristine combination. A method of treating a patient comprising the administration of synergistically effective amounts of cefpirome and a dalfopristine/quinupristine combination. Kits comprising synergistically effective amounts of cefpirome and a dalfopristine/quinupristine combination are also disclosed.Type: ApplicationFiled: August 3, 2001Publication date: March 28, 2002Inventors: Celine Feger, Philippe Moreillon, Jacques Vouillamoz
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Publication number: 20020037877Abstract: Stable aqueous pharmaceutical suspension compositions containing lecithin as a stabilizing additive and lacking a polymeric suspending agent are disclosed.Type: ApplicationFiled: July 16, 2001Publication date: March 28, 2002Applicant: Alcon Universal Ltd.Inventor: Onkar N. Singh
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Publication number: 20020037926Abstract: Methods of treating or preventing chronic pain or convulsion are disclosed by administering to an animal a sodium channel blocker and at least one of gabapentin and pregabalin. Also disclosed are pharmaceutical compositions and kits for the treatment or prevention of chronic pain or convulsion.Type: ApplicationFiled: October 5, 2001Publication date: March 28, 2002Inventor: Nancy C. Lan
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Publication number: 20020035104Abstract: Provided are compounds of formula (I) 1Type: ApplicationFiled: August 16, 2001Publication date: March 21, 2002Applicant: GENENTECH, INC.Inventors: Dean R. Artis, David Y. Jackson, Thomas E. Rawson, Mark E. Reynolds, Daniel P. Sutherlin, Mark S. Stanley
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Patent number: 6358941Abstract: The present invention relates to the use of pharmaceutically acceptable cholinesterase inhibitors for the preparation of a pharmaceutical composition for the treatment or prophylaxis of arthritic disorders, including osteoarthritis, rheumatoid arthritis and other rheumatoid diseases such as Juvenile Arthritis, Systemic Lupus Erythematosis, Sjogren's Syndrome, Progressive Systemic Sclerosis, Polymyositis, Dermatomyositis, Ankylosing Spondilitis, Reiter's Syndrome, Psoriatic Arthritis, Relapsing Polychondritis, Relapsing Panniculitis, Crohn's Disease, Ulcerative Colitis, Heredity Complement Deficiencies, Collagen Vascular Diseases, Felty's Syndrome, rheumatological manifestations associated with bacterial and viral endocarditis or myocarditis and other rheumatological manifestations such as anaemia of chronic disorders. The invention also relates to a novel method of treatment or prophylaxis of such diseases and manifestations.Type: GrantFiled: May 3, 1999Date of Patent: March 19, 2002Inventors: Ernir Snorrason, James Murray
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Publication number: 20020028803Abstract: This invention provides caspase inhibitors of formula I: 1Type: ApplicationFiled: March 29, 2001Publication date: March 7, 2002Inventors: David Bebbington, Ronald Knegtel, Michael Mortimore, David Kay, Julian M.C. Golec
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Publication number: 20020028804Abstract: Cosmetic methods and compositions containing selected iminodibenzyl or fluorene derivatives. When used for skin or hair care, the inventive compositions provide control of sebum secretion from sebocytes, improved oil control and improved feel, and prevent shine and stickiness.Type: ApplicationFiled: June 1, 2001Publication date: March 7, 2002Applicant: Unilever Home & Personal Care USA, Division of Conopco, Inc.Inventors: John Steven Bajor, David Joseph Pocalyko
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Publication number: 20020010171Abstract: The present invention relates to compounds of the general formula (I) 1Type: ApplicationFiled: June 11, 2001Publication date: January 24, 2002Inventors: Lone Jeppesen, Per Sauerberg, Anthony Murray, Paul Stanley Bury
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Patent number: 6335323Abstract: Methods and compositions for treatment of a patient suffering from a form of peripheral neuropathy are disclosed. The method comprises administering to the patient any one of the following combinations of components: I. A, B and C; II. A and B; III. B and C; IV. A and C, wherein A is an antidepressant or a monoamine oxidase inhibitor, B is vitamin B12, and C is a precursor or inducer of a neurotransmitter, e.g. L-phenylalanine.Type: GrantFiled: March 4, 1999Date of Patent: January 1, 2002Assignee: The WWK TrustInventor: Andrew Peter Worsley
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Publication number: 20010056091Abstract: A method of inhibiting effects of exogenous neurotoxic or neurotoxinic products in warm-blooded animals comprising administering to warm-blooded animals before exposure to said products an inhibitorily effective amount of reversible cholinesterase inhibitor selected from the group consisting of pyridostigmine and physostigmine followed by administration of an inhibitorily effective amount of 2-methyl-1-(1-piperidinyl)-1-(2-thienyl)-cyclohexane in substantially pure racemic, diastereoisomeric or enantiomeric form.Type: ApplicationFiled: April 13, 2001Publication date: December 27, 2001Applicant: SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES (S.C.R.A.S)Inventors: Guy Lallement, Pierre D'Arbigny, Jean-Marc Kamenka
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Patent number: 6319937Abstract: This invention relates to novel isoxazolines of formula (I): or a pharmaceutically acceptable salt form thereof. This invention also relates to novel isoxazolines of formula (I) which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.Type: GrantFiled: November 17, 1999Date of Patent: November 20, 2001Assignee: DuPont Pharmaceuticals CompanyInventors: John Wityak, Prabhakar K. Jadhav
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Patent number: 6316417Abstract: The invention is concerned with a parenteral formulation comprising a 5H-dibenz(b,f)azepine-5-carboxamide and an aqueous-based solvent. The parenteral formulation is useful in the treatment of seizures resulting from, e.g. epileptic attack.Type: GrantFiled: May 2, 2000Date of Patent: November 13, 2001Assignee: Novartis AGInventor: Peter Van Hoogevest
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Publication number: 20010036943Abstract: Pharmaceutical compositions are disclosed for the treatment of acute, chronic and/or neuropathic pain. The pharmaceutical compositions are comprised of a therapeutically effective combination of a nicotine receptor partial agonist and an analgesic agent and a pharmaceutically acceptable carrier. The analgesic agent is selected from opioid analgesics, NMDA antagonists, substance P antagonists, COX 1 and COX 2 inhibitors , tricyclic antidepressants (TCA), selective serotonin reuptake inhibitors (SSRI), capsaicin receptor agonists, anesthetic agents, benzodiazepines, skeletal muscle relaxants, migraine therapeutic agents, anti-convulsants, anti-hypertensives, anti-arrythmics, antihistamines, steroids, caffeine, and botulinum toxin. The method of using these compounds and a method of treating acute, chronic and/or neuropathic pain and migraine in a mammal including a human is also disclosed.Type: ApplicationFiled: December 18, 2000Publication date: November 1, 2001Inventors: Jotham W. Coe, Steven B. Sands, Edmund P. Harrigan, Brian T. O'Neill, Eric J. Watsky
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Publication number: 20010029256Abstract: The present invention relates to compounds of formula (I) 1Type: ApplicationFiled: March 14, 2001Publication date: October 11, 2001Inventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
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Patent number: 6291449Abstract: A method and product for treating and preventing diarrhea and scours is provided. The method involves treating a subject who has diarrhea, or scours, or is at risk of getting diarrhea or scours with an aromatic compound of the invention. The products of the invention are a veterinary preparation of the aromatic compound of the invention and an anti-scours agent, and a pharmaceutical preparation of the aromatic compound of the invention and an anti-diarrheal agent.Type: GrantFiled: September 23, 1998Date of Patent: September 18, 2001Assignees: Children's Medical Center Corporation, Beth Israel Deaconess Medical CenterInventors: Wayne I. Lencer, Carlo Brugnara, Seth Alper
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Patent number: 6281212Abstract: Disclosed is a method of treating a subject with a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to the subject a therapeutically effective amount of a compound represented by the following structural formula: and physiologically acceptable salts thereof. Z is a substituted or unsubstitured aromatic group. Y is a covalent bond, —O— or —CO—. n is an integer from one to about five. X is a covalent bond or —CO—. Ra is an aliphatic or a substituted aliphatic group; Rb is an aliphatic group substituted with an aromatic group or substituted aromatic group; and, taken together with the nitrogen atom bonded to Ra and Rb, can form a substituted or unsubstituted non-aromatic heterocyclic ring.Type: GrantFiled: July 11, 1997Date of Patent: August 28, 2001Assignee: Millennium Pharmaceuticals, Inc.Inventors: Charles F. Schwender, Charles R. Mackay, Julia C. Pinto, Walter Newman
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Publication number: 20010016569Abstract: Non-antibody multimeric receptor ligands, methods for making and identifying them and their use for agonizing or antagonizing multimeric receptors.Type: ApplicationFiled: March 13, 2001Publication date: August 23, 2001Applicant: SmithKline Beecham CorporationInventors: Martin Rosenberg, Katherine Louisa Widdowson
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Patent number: 6251894Abstract: This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 0, 1 or 2; m is 1 or 2, provided that if m is 2, then n is 1; ═Q is ═O or ═NR3; X is a covalent bond or —O—, —S—, —NR3—; R1 is Ar1, Ar1C1-6alkyl or di(Ar1)C1-6alkyl, wherein each C1-6alkyl group is optionally substituted; R2 is Ar2, Ar2C1-6alkyl, Het or HetC1-6alkyl; R3 is hydrogen or C1-6alkyl; L is a piperidine derivative of formula (a-1) or a spiro piperidine derivative of formula (a-2); Ar1 is phenyl or substituted phenyl; Ar2 is naphtalenyl; phenyl or substituted phenyl; and Het is a monocyclic or bicyclic heterocycle; each monocyclic and bicyclic heterocycle may optionally be substituted on a carbon atom; as substance P antagonists; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: June 22, 1998Date of Patent: June 26, 2001Assignee: Janssen Pharmaceuticals N.V.Inventors: Frans Eduard Janssens, Joseph Elisabeth Leenaerts, Yves Emiel Maria Van Roosbroeck
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Patent number: 6239128Abstract: The present invention relates to the use of indole-2,3-dione-3-oxime derivatives in a method of combating diseases and disorders associated with or mediated by the release of excitatory amino acids.Type: GrantFiled: September 29, 2000Date of Patent: May 29, 2001Assignee: Neurosearch A/SInventors: Frank Watjen, Jorgen Drejer
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Patent number: 6235730Abstract: 3-piperidyl-4-oxoquinazoline derivatives are provided, which is represented by the formula (I): wherein R represents an amino group or a cyclic amino group such as dibenzoazepine, each of which is substituted with a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group, or the like, n is an integer of 1 to 3, R3 and R4 independently represents a hydrogen atom, a lower alkyl group, or the like, or a pharmaceutically acceptable salt thereof. Compounds (I) of the present invention have excellent MTP-inhibitory activity. Thus, these compounds not only inhibit formation of LDL that is a cause of arteriosclerotic diseases but also regulate TG, cholesterol, and lipoproteins such as LDL in the blood and regulate cellular lipids through regulation of MTP activity. They can also be used as a new type of preventive or therapeutic agents for hyperlipemia or arteriosclerotic diseases.Type: GrantFiled: October 26, 1999Date of Patent: May 22, 2001Assignee: Japan Tobacco, Inc.Inventors: Motohide Sato, Takeo Katsushima, Hajime Kinoshita
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Patent number: 6214816Abstract: The compounds are N-substituted azaheterocyclic compounds of formula I wherein R1 and R2 independently are hydrogen, halogen, trifluoromethyl, hydroxy, C1-6-alkyl or C1-6-alkoxy; and Y is >N—CH2— wherein only the underscored atom participates in the ring system; and X is —C(R6R7)—, —CH2CH2—, —CH═CH—CH2—, —CH2—CH═CH—, —CH2—(C═O)—, —(C═O)—CH2—, —CH2CH2CH2—, —CH═CH—, CH(R10)CH2—, —CH2CH(R10) or —(C═O)— wherein R6 and R7 independently are hydrogen or C1-6-alkyl and wherein R10 is C1-6-alkyl or phenyl; and r is 0, 1 or 2; and Z is selected from wherein A is —CH2—, —O—, —S— or —N(R5)— wherein R5 is H or C1-6-alkyl; and R3 is —(CH2)pCOR4 wherein p is 1, 2, 3 or 4 and R4 is OH, NH2, NHOH or C1-6-alkoxy; or a pharmaceutically acceptable salt thType: GrantFiled: March 10, 1999Date of Patent: April 10, 2001Assignee: Novo Nordisk A/SInventors: Rolf Hohlweg, Tine Krogh Jørgensen, Knud Erik Andersen, Uffe Bang Olsen, Zdenék Polivka, Karel Sindelar
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Patent number: 6211229Abstract: The invention is directed to a method for the treatment of a patient suffering from transient or short term insomnia. The claimed method comprises the administration of a compound selected from the group consisting of the pharmaceutically acceptable forms of doxepin, amitriptyline, trimipramine, trazodone and mixtures thereof in dosages ranging from about 0.5 to about 20.0 milligrams.Type: GrantFiled: February 17, 2000Date of Patent: April 3, 2001Inventor: Neil B. Kavey
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Patent number: 6211174Abstract: The present invention is directed to certain naphtho-fused lactams of the general structural formula: wherein and R1, R1a, R1b, R2a, R2b, R3a, R4, R5, R6, A, L, X, n, p and w are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone.Type: GrantFiled: September 24, 1998Date of Patent: April 3, 2001Assignee: Merck & Co., Inc.Inventors: Robert J. Devita, Matthew J. Wyvratt
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Patent number: 6211171Abstract: When administered locally, tricyclic, second generation and third generation antidepressants, such as amitriptyline and desipramine, have been shown to produce analgesia in a subject having a site of local discomfort. The analgesic effect of such antidepressants, when administered locally is equal to that achieved by systemic administration and lasts longer. The invention provides compositions containing tricyclic, second generation, and third generation antidepressants for local administration, such as those formulated for topical application, or for injection in slow release delivery vehicles, and methods for their use for producing local analgesia.Type: GrantFiled: May 19, 1998Date of Patent: April 3, 2001Assignee: Dalhousie UniversityInventors: Jana Sawynok, Mike Esser, Allison Reid
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Patent number: 6191117Abstract: Methods are disclosed for the acute and chronic treatment of obesity using drugs whose mechanism includes the interaction and antagonism of the kainate/AMPA receptor. Methods are disclosed for employing the drug topiramate (topomax) as monotherapy or in combination therapy with lamotrigene, valproic acid, valproic acid and carbamezepine combination, or felbamate (felbatol).Type: GrantFiled: July 10, 2000Date of Patent: February 20, 2001Inventor: Walter E. Kozachuk
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Patent number: 6184218Abstract: The invention relates to a composition comprising a first component (a) which is (R)-3N,N-dicyclobutylamino-8-fluoro-3,4-dihydro-2H-1-benzopyran-5-carboxamide hydrogen (2R,3R)-tartrate monohydrate and a second component (b) which is 1-[3-(dimethylamino)propyl]-1-(p-fluorophenyl)-5-phthalancarbonitrile, as the racemate or an enantiomer thereof, in the form of the free base, or a pharmaceutically acceptable salt and/or solvate thereof The invention further concerns the preparation of the composition, pharmaceutical formulations containing said composition, and a method of treatment of affective disorders such as mood disorders and anxiety disorders with said composition, as well as a kit containing said composition.Type: GrantFiled: July 9, 1999Date of Patent: February 6, 2001Assignee: Astra AktiebolagInventors: John Evenden, Seth-Olov Thorberg
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Patent number: 6184219Abstract: The invention relates to a composition comprising a first component (a) which is (R)-5-carbamoyl-8-fluoro-3-N,N-dicyclobutylamino-3,4-dihydro-2H-1-benzopyran in the form of the free base, or a pharmaceutically acceptable salt and/or solvate thereof, and a second component (b) which is (+)-1-[3-(dimethylamino)propyl]-1-(p-fluorophenyl)-5-phthalancarbonitrile in the form of the free base, or a pharmaceutically acceptable salt and/or solvate thereof. The invention is further directed to the preparation of the composition, pharmaceutical formulations containing said composition, and a method of treatment of affective disorders such as mood disorders and anxiety disorders with said composition, as well as a kit containing said composition.Type: GrantFiled: July 9, 1999Date of Patent: February 6, 2001Assignee: Astra AktiebolagInventors: John Evenden, Seth-Olov Thorberg
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Patent number: 6174880Abstract: A method for treating painful fibromuscular disorders comprising topical application to the skin of a therapeutically effective amount of a tricyclic antidepressant compound in a pharmaceutically acceptable vehicle.Type: GrantFiled: December 1, 1998Date of Patent: January 16, 2001Assignee: Winston Laboratories, Inc.Inventor: Joel E. Bernstein
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Patent number: 6172105Abstract: The invention relates to a composition comprising a first component (a) which is (R)-3-N,N-dicyclobutylamino-8-fluoro-3,4-dihydro-2H-1-benzopyran-5-carboxamide hydrogen (2R,3R)-tartrate monohydrate and a second component (b) which is a 5-HT reuptake inhibitor, excluding citalopram and paroxetine. The invention is further directed to the preparation of the composition, pharmaceutical formulations containing said composition, and a method of treatment of affective disorders such as mood disorders and anxiety disorders with said composition, as well as a kit containing said composition.Type: GrantFiled: July 9, 1999Date of Patent: January 9, 2001Assignee: Astra AktiebolagInventors: John Evenden, Seth-Olov Thorberg
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Patent number: 6172058Abstract: A pharmaceutical compound of the formula in which R1 is C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-10 cycloalkyl, C3-10 cycloalkyl-C1-10 alkyl, C3-10 cycloalkyl-C2-10 alkenyl, C3-10 cycloalky-C2-10 alkynyl, optionally substituted phenyl-C1-10 alkyl, optionally substituted phenyl-C2-10 alkenyl, optionally substituted phenyl-C2-10 alkynyl, optionally substituted naphthyl, optionally substituted naphthyl-C1-10 alkyl, C1-10 alkoxy-C1-10 alkyl, C3-10 cycloalkoxy-C1-10 alkyl, optionally substituted heterocyclyl, optionally substituted heterocyclyl-C1-10 alkyl, optionally substituted phenyl fused to C5-10 cycloalkyl, optionally substituted tricyclic, optionally substituted tricyclic-C1-10 alkyl, or [optionally substituted phenyl(CH2)n]2-C1-10 alkyl, where n is 0 or 1 to 4, and R2 is hydrogen or one of the values for R1; or a salt or ester thereof.Type: GrantFiled: April 3, 1998Date of Patent: January 9, 2001Assignee: Lilly, SAInventors: Concepci{acute over (o)}n Pedregal Tercero, Ivan Collado Cano, Angel Maz{acute over (o)}n Ruiz
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Patent number: 6159971Abstract: The invention relates to a combination of a first component (a) which is a 5-HT reuptake inhibitor and a second component (b) which is selective h5-HT.sub.1B antagonist or partial agonist having the formula I ##STR1## wherein X is CH.sub.2, O; Y is CONH, NHCO;R.sub.1 is H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl;R.sub.2 is H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, halogen;R.sub.3 is ##STR2## R.sub.4 and R.sub.5 independently are H or C.sub.1 -C.sub.4 alkyl, as racemate, R-enantiomer or S-enantiomer, and said components (a) and (b) being in the form of free bases, solvents or pharmaceutically acceptable salts thereof, the preparation thereof, pharmaceutical formulations containing said combination, use of and method of treatment of affective disorders such as depression, anxiety and OCD with said combination as well as a kit containing said combination.Type: GrantFiled: October 21, 1998Date of Patent: December 12, 2000Assignee: Astrazeneca ABInventors: Stefan Berg, Svante Ross, Seth-Olov Thorberg
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Patent number: 6150355Abstract: A phenylpiperidine derivative or pharmaceutical acceptable salt thereof represented by formula (I): ##STR1## wherein X represents CH or N; Y--Z represents CH.sub.2 --O, CH.sub.2 --S, CH.sub.2 --CH.sub.2, CH.dbd.CH or CONR.sup.5 (wherein R.sup.5 represents hydrogen or lower alkyl); R.sup.1 represents hydrogen, lower alkyl, halogen, lower alkoxy or trifluoromethyl; and R.sup.2, R.sup.3 and R.sup.4 are the same or different and each represents hydrogen, lower alkyl or QR.sup.6 (wherein Q represents a single bond or lower alkylene, and R.sup.6 represents hydroxy, lower alkoxyalkoxy, lower alkoxy, lower alkylthio, nitro, halogen, lower alkanoyloxy, lower alkoxycarbonyl, lower alkanoyl or carboxyl).The present invention provides novel phenylpiperidine derivatives useful as analgesics.Type: GrantFiled: March 13, 1998Date of Patent: November 21, 2000Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Toshiaki Kumazawa, Hirokazu Koshimura, Shigeru Aono, Shunji Ichikawa, Shigeto Kitamura
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Patent number: 6096737Abstract: The use of a combination of a tricyclic or tetracyclic antidepressant, a serotonin reuptake inhibitor, or a monoamine oxidase inhibitor with a neurotransmitter-inducing or precursor compound is proposed in the preparation of medication for the treatment or prevention of multiple sclerosis or other demyelinating conditions. For use in treatment to ameliorate the effects of a demyelinating condition, a daily regime is proposed of from 10 to 220 mg lofepramine and from 100 mg to 5 g of L-phenylalanine, optionally supplemented with injections of vitamin B.sub.12.Type: GrantFiled: June 27, 1997Date of Patent: August 1, 2000Inventor: Cari Loder
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Patent number: 6096738Abstract: A method for preventing and treating headache pain comprising administering a tricyclic antidepressant compound locally to the nasal mucosa to a patient suffering from headaches.Type: GrantFiled: January 28, 1999Date of Patent: August 1, 2000Assignee: Winston Laboratories, Inc.Inventor: Joel E. Bernstein
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Patent number: 6071901Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids andy esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.Type: GrantFiled: April 1, 1998Date of Patent: June 6, 2000Assignee: Novo Nordisk A/SInventors: Florenzio Zaragossa Dorwald, Knud Erik Andersen, Rolf Hohlweg, Peter Madsen, Tine Krogh J.o slashed.rgensen, Uffe Bang Olsen, Henrik Sune Andersen, Svend Treppendahl, Polivka Zdenek, Silhankova Alexandra, Sindelar Karel
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Patent number: 6066632Abstract: The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula ##STR1## wherein X, Y, Z, R.sup.1, R.sup.2 and r are as defined in the detailed part of the present description, or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for treatment of indications caused by or related to the secretion and circulation of insulin antagonising peptides, e.g. non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.Type: GrantFiled: August 17, 1999Date of Patent: May 23, 2000Assignee: Novo Nordisk A/SInventors: Knud Erik Andersen, Tine Krogh J.o slashed.rgensen, Rolf Hohlweg, Erik Fischer, Uffe Bang Olsen, Zdenek Polivka, Karel Sindelar, Vladimir Valenta
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Patent number: 6054448Abstract: Compounds of the formula ##STR1## in which R.sup.1 is Y or Y--C.sub.1-6 alkyl, where Y is carboxy, tetrazolyl, --SO.sub.2 H, --SO.sub.3 H, --OSO.sub.3 H, --CONHOH, or --P(OH)OR', --PO(OH)OR', --OP(OH)OR' or --OPO(OH)OR' where R' is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or optionally substituted phenyl-C.sub.1-6 alkyl,and R.sup.2, R.sup.3, R.sup.4, X and Z are as defined in the specification, possess affinity for metabotropic glutamate receptors and are useful in the treatment of disorders of the central nervous system.Type: GrantFiled: October 17, 1997Date of Patent: April 25, 2000Assignee: Eli Lilly and Company LimitedInventors: Barry Peter Clark, John Richard Harris
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Patent number: 6048856Abstract: The present invention relates to novel N-substituted azaheterocyclic compounds of the formula ##STR1## wherein X, Y, R.sup.1, R.sup.1a, R.sup.2, R.sup.2a, R.sup.12, R.sup.13, A, r and s are as defined in the detailed part of the present description, or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation. These compounds are also useful for treating indications caused by or related to the secretion and circulation of insulin antagonizing peptides, e.g., non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.Type: GrantFiled: December 14, 1998Date of Patent: April 11, 2000Assignee: Novo Nordisk A/SInventors: Tine Krogh J.o slashed.rgensen, Erik Fischer, Rolf Hohlweg, Knud Erik Andersen, Uffe Bang Olsen, Karel Sindelar, Alexandra Silhankova, Otylie Konigova, Zdenek Polivka
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Patent number: 6043238Abstract: A compound of the formula ##STR1## wherein a, V, X, Y, Z, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined above, useful in (a) the treatment of myelosuppression including suppression associated with cancer chemotherapy as well as activation of the immune system for the treatment of cancer or (b) prevention and treatment of viral, fungal, bacterial and parasitic infectious diseases.Type: GrantFiled: August 15, 1997Date of Patent: March 28, 2000Assignee: Pfizer Inc.Inventors: Christopher B. Cooper, Joseph P. Lyssikatos, Donald W. Mann, Scott J. Hecker
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Patent number: 6040302Abstract: The present invention relates to 1,4-disubstituted piperazines of the general formula ##STR1## wherein X, Y, Z, R.sup.1, R.sup.2 and r are as defined in the detailed part of the present description or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for the treatment of indications caused by or related to the secretion and circulation of insulin antagonising peptides, e.g. non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.Type: GrantFiled: March 18, 1999Date of Patent: March 21, 2000Assignee: Novo Nordisk A/SInventors: Rolf Hohlweg, Peter Madsen, Tine Krogh J.o slashed.rgensen, Knud Erik Andersen, Brett Watson, Zdenek Polivka, Otylie Konigova, Martina Kovandova, Alexandra Silhankova, Vladimir Valenta
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Patent number: 6030967Abstract: A compound of the formula: whereinQ is an optionally substituted carbon atom or N(O)p wherein p is 0 or 1;Y is an optionally substituted methylene group, S(O)q wherein q is an integer of 0 to 2, or an optionally substituted imino group;Z.sup.1 is a C.sub.1-3 alkylene group which may have an oxo group or a thioxo group and may contain etherified oxygen or sulfur within the carbon chain;Z.sup.2 is an optionally substituted C.sub.1-3 alkylene group;Ar is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group;one of R.sup.1 and R.sup.2 is a hydrogen atom, a halogen atom, a hydroxyl group, an optionally substituted lower alkyl group, or an optionally substituted lower alkoxy group;the other is a halogen atom, a hydroxyl group, an optionally substituted lower alkyl group, or an optionally substituted lower alkoxy group; orR.sup.1 and R.sup.2 taken together with adjacent --c.dbd.c-- form a ring; andring A is a benzene ring which may be substituted in addition to R.sup.1 and R.Type: GrantFiled: October 30, 1997Date of Patent: February 29, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Shogo Marui, Masatoshi Hazama, Kohei Notoya, Masaki Ogino
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Patent number: 6008213Abstract: Compounds of formula (I) ##STR1## wherein A.sub.1 is C or N; E is a five- or six-membered heteroaromatic or six-membered aromatic ring optionally substituted by R.sup.3 or R.sup.4 ; X.sup.1 --X.sup.2 is CHR.sup.1 --CH, CR.sup.1 .dbd.CH, NR.sup.1 --CH, S(O).sub.u --CH or O--CH; X.sup.3 is CR.sup.5 R.sup.5 ', NR.sup.5, S(O).sub.u or O; R.sup.2 is --OR', --NR'R", --NR'SO.sub.2 R'", --NR'OR', --OCR'.sub.2 C(O)OR', --OCR'.sub.2 OC(O)--R', --OCR'.sub.2 C(O)NR'.sub.2, CF.sub.3 or --COCR'.sub.2 R.sup.2 '; R.sup.3, R.sup.4 and R.sup.7 are independently H, halo, --OR.sup.12, --SR.sup.12, --CN, --NR'R.sup.12, --NO.sub.2, --CF.sub.3, CF.sub.3 S(O).sub.r --, --CO.sub.2 R', --CONR'.sub.2, R.sup.14 --C.sub.0-6 alky-, R.sup.14 --C.sub.1-6 oxoalkyl-, R.sup.14 --C.sub.2-6 alkenyl-, R.sup.14 --C.sub.2-6 alkynyl-, R.sup.14 --C.sub.0-6 alkyloxy-, R.sup.14 --C.sub.0-6 alkylamino- or R.sup.14 --C.sub.0-6 alkyl--S(O).sub.r --; R.sup.6 is W--(CR'.sub.2).sub.q --Z--(CR'R.sup.10)--U--(CR'.sub.2).sub.s --V-- or W'--(CR'.sub.2).sub.Type: GrantFiled: December 19, 1997Date of Patent: December 28, 1999Assignee: SmithKline Beecham CorporationInventors: William E. Bondinell, William H. Miller
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Patent number: 6004983Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxcylic acids of the general formula wherein X, Y, Z, R.sup.1, R.sup.2 and r are as defined in the detailed part of the description, or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for treatment of indications caused by or related to the secretion and circulation of insulin antagonising peptides.Type: GrantFiled: October 3, 1997Date of Patent: December 21, 1999Assignee: Novo Nordisk A/SInventors: Henrik Sune Andersen, Tine Krogh J.o slashed.rgensen, Rolf Hohlweg, Knud Erik Andersen, Zdenek Polivka, Frantisek Miksik
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Patent number: 5998399Abstract: Method of treating or reducing the risk of human disease or condition in which the synthesis or oversynthesis of nitric oxide forms a contributory part wherein a therapeutically effective amount of the compound of formula (I) as defined in the specification is administered to a person suffering from or susceptible to such disease or condition.Type: GrantFiled: November 16, 1998Date of Patent: December 7, 1999Assignee: Astra AktiebolagInventors: James E. Macdonald, Robert Gentile, Robert J. Murray
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Patent number: 5962449Abstract: The present invention relates to novel N-substituted amino acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.Type: GrantFiled: March 28, 1996Date of Patent: October 5, 1999Assignee: Novo Nordisk A/SInventors: Peter Madsen, Knud Erik Andersen, Rolf Hohlweg, Florenzio Zaragossa Dorwald, Tine Krogh J.o slashed.rgensen, Uffe Bang Olsen, Henrik Sune Andersen
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Patent number: 5962514Abstract: The invention relates to a combination of a first component (a) which is a 5-HT reuptake inhibitor and a second component (b) which is selective 5-HT.sub.1A antagonist of the general formula ##STR1## wherein R.sub.1 is n-propyl or cyclobutyl;R.sub.2 is isopropyl, tertiary butyl, cyclobutyl, cyclopentyl or cyclohexyl;R.sub.3 is hydrogen;R.sub.4 is hydrogen or methyl;as (R)-enantiomer in the form of free base or pharmaceutically acceptable salts thereof, the preparation thereof, pharmaceutical formulations containing said combination, use of and method of treatment of affective disorders such as depression, anxiety and OCD with said combination as well as a kit containing said combination.Type: GrantFiled: May 9, 1997Date of Patent: October 5, 1999Assignee: Astra AktiebolagInventors: John Evenden, Seth-Olov Thorberg
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Patent number: 5929069Abstract: A compound represented by the formula (I) or (II) or a salt thereof wherein R.sup.1 represents hydrogen atom or a C.sub.1-6 alkyl group; R.sup.2 and R.sup.3 independently represent a hydrogen atom or a C.sub.1-6 alkyl group, or R.sup.2 and R.sup.3 may combine together to represent a 5- or 6-membered cycloalkyl group; R.sup.4 represents, for example, a hydrogen atom or a C.sub.1-6 alkyl group; R.sup.5 represents, for example, a hydrogen atom or a C.sub.1-6 alkyl group; R.sup.6 represents a hydrogen atom or a C.sub.1-6 alkyl group; x represents --NR.sup.7 --, --O--, --CHR.sup.7 -- or --S-- in which R.sup.7 represents, for example, a hydrogen atom or a C.sub.1-6 alkyl group; and Y represents a phenylene group or a pyridinediyl group. The compounds are useful as agents for enhancing the activities of retinoid compounds.Type: GrantFiled: September 20, 1996Date of Patent: July 27, 1999Assignee: Institute of Medicinal Molecular Design, Inc.Inventor: Koichi Shudo
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Patent number: 5929085Abstract: There are provided novel compounds of formula (I) ##STR1## wherein X, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are as defined in the specification and optical isomers and racemates thereof and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy.Type: GrantFiled: January 22, 1997Date of Patent: July 27, 1999Assignee: Astra AktiebolagInventors: James MacDonald, James Matz, William Shakespeare
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Patent number: RE37029Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: November 5, 1998Date of Patent: January 23, 2001Assignee: Aventis Pharmaceuticals Inc.Inventors: Joseph T. Strupczewski, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegler