Abstract: The invention relates to pharmaceutical compositions and methods useful in the treatment of obesity which methods comprise administering to animal, including a human or companion animal, in need of such treatment an effective amount of a compound of the structural formula
or a pharmaceutically acceptable salt, racemate or enantiomer thereof, wherein
R is hydroxy, esterified hydroxy or etherified hydroxy;
R1 and R2 are, independently, halogen, trifluoromethyl or lower alkyl;
R3 is halogen, trifluoromethyl, lower alkyl, aryl, aryl-lower alkyl, cycloalkyl or cycloalkyl-lower alkyl, carbocyclic arylmethyl, carbocyclic aroyl, carbocyclic arylhydroxymethyl; or
R3 is the radical
wherein
R8 is hydrogen, lower alkyl, aryl, cycloalkyl, aryl-lower alkyl or cycloalkyl-lower alkyl;
R9 is hydroxy or acyloxy; R10 is hydrogen or lower alkyl; or R9 and R10, taken together with the carbon atom to which they are attached, form a carbonyl group;
R4 is hydrogen, halogen, trifluorom
Type:
Grant
Filed:
October 16, 2001
Date of Patent:
April 29, 2003
Assignee:
Pfizer Inc.
Inventors:
Peter Cornelius, Diane Hargrove, Bradley P. Morgan, Andrew G. Swick
Abstract: This invention provides a method of treating obesity, generalized anxiety disorder, post-traumatic stress disorder, late luteal phase disphoric disorder (premenstrual syndrome), attention deficit disorder, with and without hyperactivity, Gilles de la Tourette syndrome, bulimia nervosa or Shy Drager Syndrome in a mammal by administering to the mammal an effective amount of a hydroxycycloalkanephenethyl amine of the following structural formula:
in which A is a moiety of the formula
where
the dotted line represents optional unsaturation;
R1 is hydrogen or alkyl;
R2 is alkyl;
R4 is hydrogen, alkyl, formyl, or alkanol;
R5 and R6 are, independently, hydrogen, hydroxyl, alkyl, alkoxy, alkanoyloxy, cyano, nitro, alkylmercapto, amino, alkylamino, dialkylamino, alkanamido, halo, trifluoromethyl, or taken together, methylene dioxy;
R7 is hydrogen or alkyl; and
n is 0, 1, 2, 3, or 4;
or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
November 30, 2001
Date of Patent:
April 29, 2003
Assignee:
Wyeth
Inventors:
Richard L. Rudolph, Albert T. Derivan, G. Virginia Upton
Abstract: The present invention relates to topical compositions for effecting an immediate improvement in the appearance and feel of skin, in addition to providing chronic improvements in skin appearance. The compositions comprise from 0.5% to 25% of a first particulate material having a refractive index of from 1.3 to 1.7, the particulate material being dispersed in the composition and having a median particle size of from 2 to 30 um, and an active effective for chronically regulating skin condition selected from Vitamin B3 compounds, retinoids, and mixtures thereof. Preferred emobodiments are oil in water emulsions further comprising a second particulate material having a larger particle size than the first.
Type:
Grant
Filed:
November 8, 2001
Date of Patent:
April 22, 2003
Assignee:
The Procter & Gamble Company
Inventors:
Petra Helga Beck, Robert Francis Date, Mario Elmen Tremblay
Abstract: Disclosed herein are methods for treating immune-mediated ear disorders, such as IMCVDs, or their symptoms, involving administration of a therapeutically-effective amount of a TNF antagonist, such as etanercept or infliximab, or a therapeutically-effective amount of a pyrimidine synthesis inhibitor, such as leflunomide.
Type:
Grant
Filed:
March 27, 2001
Date of Patent:
April 15, 2003
Assignee:
The General Hospital Corporation
Inventors:
Mahboob U. Rahman, Dennis S. Poe, Hyon K. Choi
Abstract: An effervescent sub-lingual type composition, optionally in tablet form, comprising at least one active ingredient, one ore more fruit acids, and one or more effervescing alkalis, wherein at least the acid component(s) have been coated with protective layer of polydimethylsiloxane that substantially minimizes contact between the acid(s) and atmospheric moisture until the composition is purposely mixed with water or is used sub-lingually. A method of preparation of the effervescent compositions is also dislcosed.
Abstract: A composition containing a cooling-sensation imparting substance and a cationic surfactant results in an excellent cooling sensation effect. A composition additionally containing vanilylalkyl ether, wherein the alkyl group has 1 to 6 carbon atoms, is also effective as a composition for improving cooling sensation effect. The present composition for improving cooling sensation effect improves cooling sensation effect while also sustaining that effect. In particular, the present invention provides a composition for improving cooling sensation effect that is able to impart a cooling sensation effect and sustain that effect when used after washing the hair using a shampoo containing no cooling sensation substance or a shampoo containing only a small amount of cooling sensation substance.
Abstract: The present invention provides methods of modulating or inhibiting microglia activation comprising the administration of a compound capable of inhibiting 5-LOX, FLAP, attenuating degradation of I&kgr;B&agr; or inhibiting nuclear translocation of the NF-&kgr;B active complex for the treatment of Alzheimer's disease, brain ischemia, traumatic brain injury, Parkinson's Disease, Multiple Sclerosis, ALS, subarachnoid hemorrhage or other disorders associated with excessive production of inflammatory mediators in the brain.
Type:
Grant
Filed:
July 5, 2001
Date of Patent:
April 8, 2003
Assignee:
Bristol-Myers Squibb Company
Inventors:
Rand M. Posmantur, Lav Kumar Parvathenani
Abstract: Compositions that are selective PDE III inhibitors and that are effective to treat sexual dysfunction in males and females, including, but not limited to, erectile dysfunction in males. The compositions comprise halogenated quinolines, isoquinolines, quinolones, thioquinolones and 2-oxoquinolones, including derivatives thereof. The compounds can be taken orally or by a number of different routes or can be used to coat the interior of a condom to induce erection.
Abstract: The invention relates to the use of direct or indirect selective inhibitors of factor Xa acting via antithrombin III, alone or in combination with one or more compounds with anti-platelet aggregation activity, for the preparation of medicines intended to prevent and to treat thromboembolic arterial diseases.
The subject of the invention is also pharmaceutical compositions containing one or more direct or indirect selective inhibitors of factor Xa which act via antithrombin III in combination with one or more compounds with anti-platelet aggregation activity, and optionally one or more pharmaceutically acceptable vehicles.
Type:
Grant
Filed:
February 11, 2000
Date of Patent:
April 1, 2003
Assignees:
Sanofi-Synthelabo, Akzo Nobel
Inventors:
André Bernat, Jean Marc Herbert, Maurice Petitou, Ronald Van Amsterdam
Abstract: An aqueous gel in unit dose form and suitable for topical delivery of clonidine and comprising clonidine, a water-gelling amount of a pharmaceutically acceptable gelling agent and having a pH value in the range of about 6 to about 8.5. Clonidine is present in an amount in the range of about 0.05 to about 3.5 milligrams per unit dose and at a concentration in the range of about 0.01 to about 0.5 weight percent.
Abstract: An anesthetic is provided that includes a mixture of propofol, a tonicity agent, a substantially phospholipid-free emulsifying agent, a preservative such as benzyl alcohol, and water. This anesthetic is made by combining these components and then filtering the mixture of these components through a sterilizing filter. This anesthetic may be parenterally administered to both induce and maintain anesthesia in animals.
Abstract: The present invention relates to cosmetic compositions that include one or more laked pigments. The present invention relates to improved cosmetic compositions having one or more laked pigments that include one or more metal salts. The present invention also relates to a method of improving compositions that have one or more laked pigments.
Type:
Grant
Filed:
December 27, 2001
Date of Patent:
March 4, 2003
Assignee:
Avon Products, Inc.
Inventors:
Harold Pahlck, Christian J. Lee, Dennis Cupolo
Abstract: Methods are disclosed for treating or preventing disorders such as mental diseases, inflammation and pain by inhibiting the enzyme anandamide amidohydrolase. A therapeutically effective level of an anandamide amidohydrolase inhibitor is administered such as a therapeutically effective level of a haloenol lactone. Preferably, the haloenol lactone is of the formula:
wherein R is hydrogen, R1 is a halogen, and R2 is selected from the group consisting of aryl, aryloxy, and heteroaryl radicals, derivatives of said haloenol lactones, and mixtures thereof. The haloenol lactone, E-6-(bromomethylene)tetrahydro-3-(1-naphthalenyl)-2H-pyrane-2-one, is most preferred.
Abstract: Inflammatory or neuropathic pain in both men and women patients is treated by administering, sequentially or simultaneously, (a) nalbuphine and (b) an opioid antagonist selected from naloxone, naltrexone and nalmefene, or a salt or prodrug of nalbuphine and/or the opioid antagonist. Preferably, administration is made of (a) an amount of from about 3 to about 8 mg nalbuphine and (b) from about 0.2 to about 0.8 mg of an opioid antagonist selected from naloxone, naltrexone and nalmefene, or a salt and/or prodrug of either (in an amount that produces in a patient the same blood concentration of the compound in question as would administration of said amount of the nalbuphine or opioid antagonist itself).
Treatment of both inflammatory and neuropathic pain can be achieved; side effects common with &mgr;-opioids such as morphine were not observed.
Type:
Grant
Filed:
June 8, 2001
Date of Patent:
February 25, 2003
Assignee:
The Regents of the University of California
Abstract: Treatment of hyperporliferative disorders (including tumors and psoriasis) by pulse administration of a drug (such as Vitamin D or an analog) that increases blood or tissue levels of Vitamin D. The drug is administered at a sufficient dose to have an anti-proliferative effect, but the pulsed administration of the drug avoids the development of severe symptomatic or life-threatening hypercalcemia. In particular embodiments, avoidance of hypercalcemia (as measured by serum levels of calcium above normal range) is avoided altogether. In a particular example, the drug is calcitriol administered at an oral dose of about 0.5 mcg/kg once a week.
Abstract: Lipid metabolic disorders, such as hyperlipidemia or hyperlipoproteinemia can be treated by administering to an afflicted individual an effective amount of 5-(1,2-dithiolan-3-yl) valeric acid (&agr;-lipoic acid) or one of its physiologically acceptable salts. Pharmaceutical compositions containing (&agr;-lipoic acid) and methods for making such compositions also are disclosed.
Type:
Grant
Filed:
October 9, 2001
Date of Patent:
February 11, 2003
Assignees:
BiRD Berolina innovative Research and Development GmbH, esparma GmbH
Inventors:
Rudolf-Giesbert Alken, Dieter Koegst, Gerhard Fries
Abstract: The invention relates to the use of creatine and/or creatine derivatives for treating typical disorders in women, for example PMS or dysmenorrhea, which involves the prophylactic of therapeutic use, in particular, of creatine monohydrate, creatine pyruvates, creatine ascorbates and creatine &agr;-ketoglutarates as creatine derivatives in preferred daily doses of 0.1 g to 20 g. The invention also provides for the use of creatine or its derivatives as mixtures with a pyruvate, ascorbate or &agr;-ketoglutarate. The creatine or its appropriate derivatives are not restricted to any particular form of application, which makes them all the more suitable for the many symptoms of typical female disorders.
Type:
Grant
Filed:
January 27, 2000
Date of Patent:
January 7, 2003
Assignee:
SKW Trostberg Aktiengesellschaft
Inventors:
Ivo Pischel, Helen Louise Holland, Brigitta Schwartz, Andrea Huber, Ralf Jäger
Abstract: Neural tissue edema is treated by circulating a hyperoncotic artificial cerebrospinal fluid in the cerebrospinal fluid pathway in the vicinity of edematous tissue to cause the edematous tissue to be dehydrated due to an oncotic gradient between the hypertonic artificial cerebrospinal fluid and intracellular fluid and withdrawing the fluid from the pathway after it has been so circulated.
Abstract: The present invention relates to a method of treatment of hot flushes with a 5-HT2c receptor agonist and in particular to the use of the selective 5-HT2C receptor agonists 1-[6-chloro-5-(trifluoromethyl)-2-pyridinyl]-piperazine and (S)-(+)-3-[(2,3-dihydro-5-methoxy-1H-inden-4-yl)oxy-pyrrolidine or pharmaceutically acceptable acid addition salts thereof for the manufacture of a pharmaceutical formulation adapted for the treatment of hot flushes.