Tricyclo Ring System Having The Seven-membered Hetero Ring A One Of The Cyclos Patents (Class 514/217)
  • Publication number: 20020045610
    Abstract: The present invention relates to the use of N-substituted azaheterocyclic compounds or salts thereof, for the treatment of conditions related to angiogenesis.
    Type: Application
    Filed: June 1, 2001
    Publication date: April 18, 2002
    Inventors: Anker Jon Hansen, Tine Krogh Jorgensen, Uffe Bang Olsen
  • Publication number: 20020037890
    Abstract: 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: Application
    Filed: August 3, 2001
    Publication date: March 28, 2002
    Inventors: Celine Feger, Philippe Moreillon, Jacques Vouillamoz
  • Publication number: 20020037877
    Abstract: Stable aqueous pharmaceutical suspension compositions containing lecithin as a stabilizing additive and lacking a polymeric suspending agent are disclosed.
    Type: Application
    Filed: July 16, 2001
    Publication date: March 28, 2002
    Applicant: Alcon Universal Ltd.
    Inventor: Onkar N. Singh
  • Publication number: 20020037926
    Abstract: 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: Application
    Filed: October 5, 2001
    Publication date: March 28, 2002
    Inventor: Nancy C. Lan
  • Publication number: 20020035104
    Abstract: Provided are compounds of formula (I) 1
    Type: Application
    Filed: August 16, 2001
    Publication date: March 21, 2002
    Applicant: GENENTECH, INC.
    Inventors: Dean R. Artis, David Y. Jackson, Thomas E. Rawson, Mark E. Reynolds, Daniel P. Sutherlin, Mark S. Stanley
  • Patent number: 6358941
    Abstract: 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: Grant
    Filed: May 3, 1999
    Date of Patent: March 19, 2002
    Inventors: Ernir Snorrason, James Murray
  • Publication number: 20020028803
    Abstract: This invention provides caspase inhibitors of formula I: 1
    Type: Application
    Filed: March 29, 2001
    Publication date: March 7, 2002
    Inventors: David Bebbington, Ronald Knegtel, Michael Mortimore, David Kay, Julian M.C. Golec
  • Publication number: 20020028804
    Abstract: 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: Application
    Filed: June 1, 2001
    Publication date: March 7, 2002
    Applicant: Unilever Home & Personal Care USA, Division of Conopco, Inc.
    Inventors: John Steven Bajor, David Joseph Pocalyko
  • Publication number: 20020010171
    Abstract: The present invention relates to compounds of the general formula (I) 1
    Type: Application
    Filed: June 11, 2001
    Publication date: January 24, 2002
    Inventors: Lone Jeppesen, Per Sauerberg, Anthony Murray, Paul Stanley Bury
  • Patent number: 6335323
    Abstract: 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: Grant
    Filed: March 4, 1999
    Date of Patent: January 1, 2002
    Assignee: The WWK Trust
    Inventor: Andrew Peter Worsley
  • Publication number: 20010056091
    Abstract: 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: Application
    Filed: April 13, 2001
    Publication date: December 27, 2001
    Applicant: SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES (S.C.R.A.S)
    Inventors: Guy Lallement, Pierre D'Arbigny, Jean-Marc Kamenka
  • Patent number: 6319937
    Abstract: 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: Grant
    Filed: November 17, 1999
    Date of Patent: November 20, 2001
    Assignee: DuPont Pharmaceuticals Company
    Inventors: John Wityak, Prabhakar K. Jadhav
  • Patent number: 6316417
    Abstract: 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: Grant
    Filed: May 2, 2000
    Date of Patent: November 13, 2001
    Assignee: Novartis AG
    Inventor: Peter Van Hoogevest
  • Publication number: 20010036943
    Abstract: 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: Application
    Filed: December 18, 2000
    Publication date: November 1, 2001
    Inventors: Jotham W. Coe, Steven B. Sands, Edmund P. Harrigan, Brian T. O'Neill, Eric J. Watsky
  • Publication number: 20010029256
    Abstract: The present invention relates to compounds of formula (I) 1
    Type: Application
    Filed: March 14, 2001
    Publication date: October 11, 2001
    Inventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
  • Patent number: 6291449
    Abstract: 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: Grant
    Filed: September 23, 1998
    Date of Patent: September 18, 2001
    Assignees: Children's Medical Center Corporation, Beth Israel Deaconess Medical Center
    Inventors: Wayne I. Lencer, Carlo Brugnara, Seth Alper
  • Patent number: 6281212
    Abstract: 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: Grant
    Filed: July 11, 1997
    Date of Patent: August 28, 2001
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Charles F. Schwender, Charles R. Mackay, Julia C. Pinto, Walter Newman
  • Publication number: 20010016569
    Abstract: Non-antibody multimeric receptor ligands, methods for making and identifying them and their use for agonizing or antagonizing multimeric receptors.
    Type: Application
    Filed: March 13, 2001
    Publication date: August 23, 2001
    Applicant: SmithKline Beecham Corporation
    Inventors: Martin Rosenberg, Katherine Louisa Widdowson
  • Patent number: 6251894
    Abstract: 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: Grant
    Filed: June 22, 1998
    Date of Patent: June 26, 2001
    Assignee: Janssen Pharmaceuticals N.V.
    Inventors: Frans Eduard Janssens, Joseph Elisabeth Leenaerts, Yves Emiel Maria Van Roosbroeck
  • Patent number: 6239128
    Abstract: 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: Grant
    Filed: September 29, 2000
    Date of Patent: May 29, 2001
    Assignee: Neurosearch A/S
    Inventors: Frank Watjen, Jorgen Drejer
  • Patent number: 6235730
    Abstract: 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: Grant
    Filed: October 26, 1999
    Date of Patent: May 22, 2001
    Assignee: Japan Tobacco, Inc.
    Inventors: Motohide Sato, Takeo Katsushima, Hajime Kinoshita
  • Patent number: 6214816
    Abstract: 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 th
    Type: Grant
    Filed: March 10, 1999
    Date of Patent: April 10, 2001
    Assignee: Novo Nordisk A/S
    Inventors: Rolf Hohlweg, Tine Krogh Jørgensen, Knud Erik Andersen, Uffe Bang Olsen, Zdenék Polivka, Karel Sindelar
  • Patent number: 6211229
    Abstract: 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: Grant
    Filed: February 17, 2000
    Date of Patent: April 3, 2001
    Inventor: Neil B. Kavey
  • Patent number: 6211174
    Abstract: 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: Grant
    Filed: September 24, 1998
    Date of Patent: April 3, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Robert J. Devita, Matthew J. Wyvratt
  • Patent number: 6211171
    Abstract: 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: Grant
    Filed: May 19, 1998
    Date of Patent: April 3, 2001
    Assignee: Dalhousie University
    Inventors: Jana Sawynok, Mike Esser, Allison Reid
  • Patent number: 6191117
    Abstract: 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: Grant
    Filed: July 10, 2000
    Date of Patent: February 20, 2001
    Inventor: Walter E. Kozachuk
  • Patent number: 6184218
    Abstract: 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: Grant
    Filed: July 9, 1999
    Date of Patent: February 6, 2001
    Assignee: Astra Aktiebolag
    Inventors: John Evenden, Seth-Olov Thorberg
  • Patent number: 6184219
    Abstract: 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: Grant
    Filed: July 9, 1999
    Date of Patent: February 6, 2001
    Assignee: Astra Aktiebolag
    Inventors: John Evenden, Seth-Olov Thorberg
  • Patent number: 6174880
    Abstract: 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: Grant
    Filed: December 1, 1998
    Date of Patent: January 16, 2001
    Assignee: Winston Laboratories, Inc.
    Inventor: Joel E. Bernstein
  • Patent number: 6172105
    Abstract: 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: Grant
    Filed: July 9, 1999
    Date of Patent: January 9, 2001
    Assignee: Astra Aktiebolag
    Inventors: John Evenden, Seth-Olov Thorberg
  • Patent number: 6172058
    Abstract: 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: Grant
    Filed: April 3, 1998
    Date of Patent: January 9, 2001
    Assignee: Lilly, SA
    Inventors: Concepci{acute over (o)}n Pedregal Tercero, Ivan Collado Cano, Angel Maz{acute over (o)}n Ruiz
  • Patent number: 6159971
    Abstract: 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: Grant
    Filed: October 21, 1998
    Date of Patent: December 12, 2000
    Assignee: Astrazeneca AB
    Inventors: Stefan Berg, Svante Ross, Seth-Olov Thorberg
  • Patent number: 6150355
    Abstract: 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: Grant
    Filed: March 13, 1998
    Date of Patent: November 21, 2000
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Toshiaki Kumazawa, Hirokazu Koshimura, Shigeru Aono, Shunji Ichikawa, Shigeto Kitamura
  • Patent number: 6096737
    Abstract: 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: Grant
    Filed: June 27, 1997
    Date of Patent: August 1, 2000
    Inventor: Cari Loder
  • Patent number: 6096738
    Abstract: 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: Grant
    Filed: January 28, 1999
    Date of Patent: August 1, 2000
    Assignee: Winston Laboratories, Inc.
    Inventor: Joel E. Bernstein
  • Patent number: 6071901
    Abstract: 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: Grant
    Filed: April 1, 1998
    Date of Patent: June 6, 2000
    Assignee: Novo Nordisk A/S
    Inventors: 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
  • Patent number: 6066632
    Abstract: 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: Grant
    Filed: August 17, 1999
    Date of Patent: May 23, 2000
    Assignee: Novo Nordisk A/S
    Inventors: Knud Erik Andersen, Tine Krogh J.o slashed.rgensen, Rolf Hohlweg, Erik Fischer, Uffe Bang Olsen, Zdenek Polivka, Karel Sindelar, Vladimir Valenta
  • Patent number: 6054448
    Abstract: 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: Grant
    Filed: October 17, 1997
    Date of Patent: April 25, 2000
    Assignee: Eli Lilly and Company Limited
    Inventors: Barry Peter Clark, John Richard Harris
  • Patent number: 6048856
    Abstract: 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: Grant
    Filed: December 14, 1998
    Date of Patent: April 11, 2000
    Assignee: Novo Nordisk A/S
    Inventors: Tine Krogh J.o slashed.rgensen, Erik Fischer, Rolf Hohlweg, Knud Erik Andersen, Uffe Bang Olsen, Karel Sindelar, Alexandra Silhankova, Otylie Konigova, Zdenek Polivka
  • Patent number: 6043238
    Abstract: 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: Grant
    Filed: August 15, 1997
    Date of Patent: March 28, 2000
    Assignee: Pfizer Inc.
    Inventors: Christopher B. Cooper, Joseph P. Lyssikatos, Donald W. Mann, Scott J. Hecker
  • Patent number: 6040302
    Abstract: 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: Grant
    Filed: March 18, 1999
    Date of Patent: March 21, 2000
    Assignee: Novo Nordisk A/S
    Inventors: 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
  • Patent number: 6030967
    Abstract: 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: Grant
    Filed: October 30, 1997
    Date of Patent: February 29, 2000
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Shogo Marui, Masatoshi Hazama, Kohei Notoya, Masaki Ogino
  • Patent number: 6008213
    Abstract: 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: Grant
    Filed: December 19, 1997
    Date of Patent: December 28, 1999
    Assignee: SmithKline Beecham Corporation
    Inventors: William E. Bondinell, William H. Miller
  • Patent number: 6004983
    Abstract: 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: Grant
    Filed: October 3, 1997
    Date of Patent: December 21, 1999
    Assignee: Novo Nordisk A/S
    Inventors: Henrik Sune Andersen, Tine Krogh J.o slashed.rgensen, Rolf Hohlweg, Knud Erik Andersen, Zdenek Polivka, Frantisek Miksik
  • Patent number: 5998399
    Abstract: 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: Grant
    Filed: November 16, 1998
    Date of Patent: December 7, 1999
    Assignee: Astra Aktiebolag
    Inventors: James E. Macdonald, Robert Gentile, Robert J. Murray
  • Patent number: 5962449
    Abstract: 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: Grant
    Filed: March 28, 1996
    Date of Patent: October 5, 1999
    Assignee: Novo Nordisk A/S
    Inventors: Peter Madsen, Knud Erik Andersen, Rolf Hohlweg, Florenzio Zaragossa Dorwald, Tine Krogh J.o slashed.rgensen, Uffe Bang Olsen, Henrik Sune Andersen
  • Patent number: 5962514
    Abstract: 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: Grant
    Filed: May 9, 1997
    Date of Patent: October 5, 1999
    Assignee: Astra Aktiebolag
    Inventors: John Evenden, Seth-Olov Thorberg
  • Patent number: 5929069
    Abstract: 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: Grant
    Filed: September 20, 1996
    Date of Patent: July 27, 1999
    Assignee: Institute of Medicinal Molecular Design, Inc.
    Inventor: Koichi Shudo
  • Patent number: 5929085
    Abstract: 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: Grant
    Filed: January 22, 1997
    Date of Patent: July 27, 1999
    Assignee: Astra Aktiebolag
    Inventors: James MacDonald, James Matz, William Shakespeare
  • Patent number: RE37029
    Abstract: 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: Grant
    Filed: November 5, 1998
    Date of Patent: January 23, 2001
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Joseph T. Strupczewski, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegler