The Hetero Ring Is Monocyclic Piperidine Patents (Class 514/225.5)
-
Patent number: 7652005Abstract: The invention is directed to delta opioid receptor modulators. More specifically, the invention relates to tricyclic ?-opioid modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.Type: GrantFiled: October 9, 2008Date of Patent: January 26, 2010Assignee: Janssen Pharmaceutica N.V.Inventors: Steve Coats, Scott L. Dax, Bart DeCorte, Li Liu, Mark McDonnell, James J. McNally
-
Patent number: 7648982Abstract: An opioid formulation for pulmonary administration in the treatment or management of pain, a pulmonary drug delivery device containing, method of administering, kit containing, and uses of same. The formulation contains at least one rapid-onset opioid and preferably also contains a sustained-effect opioid to reduce the frequency of administration. The invention employs the side effects of the opioid formulation to permit patients to self-limit drug intake, thereby avoiding toxicity while achieving analgesia. A pharmacokinetic and pharmacodynamic model is employed to determine optimum drug formulations and optimum parameters for administration.Type: GrantFiled: August 27, 2004Date of Patent: January 19, 2010Assignee: YM Biosciences Inc.Inventors: Steven Louis Shafer, Orlando Ricardo Hung, Diana Helen Pliura
-
Patent number: 7648981Abstract: An opioid formulation for pulmonary administration in the treatment or management of pain, a pulmonary drug delivery device containing, method of administering, kit containing, and uses of same. The formulation contains at least one rapid-onset opioid and preferably also contains a sustained-effect opioid to reduce the frequency of administration. The invention employs the side effects of the opioid formulation to permit patients to self-limit drug intake, thereby avoiding toxicity while achieving analgesia. A pharmacokinetic and pharmacodynamic model is employed to determine optimum drug formulations and optimum parameters for administration.Type: GrantFiled: March 1, 2004Date of Patent: January 19, 2010Assignee: YM Biosciences Inc.Inventors: Steven Louis Shafer, Orlando Ricardo Hung, Diana Helen Pliura
-
Publication number: 20090325942Abstract: The invention relates to compounds of the formula 1, wherein R1, R2, R3, R4, R5, R6, R7, A and B are as defined herein, the pharmaceutical compositions and the uses as pharmaceuticals.Type: ApplicationFiled: July 22, 2009Publication date: December 31, 2009Applicant: SANOFI-AVENTISInventors: Stefanie KEIL, Elisabeth DEFOSSA, Karl SCHOENAFINGER, Dieter SCHMOLL, Axel DIETRICH, Johanna KUHLMANN-GOTTKE, Karl-Christian ENGEL
-
Publication number: 20090275557Abstract: The present invention relates to inhibiting proliferation and inducing apoptosis in activated lymphocytes, including T cells and B cells. The invention also provides compositions and methods for inhibiting proliferation and inducing apoptosis in activated lymphocytes, as well methods for treating diseases associated with activated lymphocytes by administering 5-HT receptor antagonists.Type: ApplicationFiled: February 26, 2009Publication date: November 5, 2009Applicant: Immune Control, Inc.Inventors: Stephen Roth, Clayton Buck, Christopher Self, Gary Olson, Nallaganchu Rao
-
Publication number: 20080318937Abstract: The invention is directed to delta opioid receptor modulators. More specifically, the invention relates to tricyclic ?-opioid modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.Type: ApplicationFiled: August 22, 2008Publication date: December 25, 2008Inventors: Steven J. Coats, Scott L. Dax, Bart DeCorte, Li Liu, Mark McDonnell, James J. McNally
-
Publication number: 20080312219Abstract: The present invention relates to a phenothiazinium compound of Formula (I): wherein: A and B each independently is in which R? and R? each independently is a linear, branched or cyclic hydrocarbon group, or R? and R? together with the N atom to which they are attached form an optionally substituted 5-, 6- or 7-membered ring; and where XP? is a counteranion and P is 1, 2 or 3; except for the compounds in which A and B are both either —N(CH3)2 or —N(CH2CH3)2 for use in a treatment that requires removal, deactivation or killing of unwanted tissues or cells. The invention also relates to compositions comprising the compounds of Formula I, to selected compounds of Formula I, use of the compounds of Formula I as medicaments and as a PDT agent or a photodiagnostic agent, a conjugate or composite formed between a compound of Formula I and a polymer; and to a method for sterilising fluids in which the fluid is passed over the conjugate or composite whilst it is illuminated.Type: ApplicationFiled: May 12, 2008Publication date: December 18, 2008Applicant: PHOTOPHARMICA LIMITEDInventors: Stanley Beames Brown, Cassandra Claire O'Grady, John Griffiths, Kirste Joanne Mellish, Richard George Tunstall, David John Howard Roberts, David Ian Vernon
-
Publication number: 20080280886Abstract: Disclosed herein are urea-based 5-HT receptor modulators, pharmaceutically acceptable salts and prodrugs thereof, the chemical synthesis thereof, and medical use of such compounds for the treatment and/or management of 5-HT receptor-mediated disorders.Type: ApplicationFiled: May 8, 2008Publication date: November 13, 2008Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
-
Patent number: 7432257Abstract: The invention is directed to delta opioid receptor modulators. More specifically, the invention relates to tricyclic ?-opioid modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.Type: GrantFiled: January 5, 2006Date of Patent: October 7, 2008Assignee: Janssen Pharmaceutica N.V.Inventors: Steve J. Coats, Scott L. Dax, Bart DeCorte, Li Liu, Mark McDonnell, James J. McNally
-
Publication number: 20080207530Abstract: The invention provides a method for the treatment of COPD and/or gastrointestinal disease conditions ameliorated by histamine management in a subject, comprising administering to the subject an effective amount of a histidine decarboxylase inhibitor.Type: ApplicationFiled: February 12, 2008Publication date: August 28, 2008Inventors: Michalis Nicolaou, Emile Loria, Gaetan Terrasse, Yves Trehin
-
Patent number: 7407953Abstract: A phenothiazinium compound, compositions and medicaments for use in promoting wound healing and a method for promoting wound healing or cosmetic use by applying or administering a phenothiazinium compound of Formula (1) to a wound site or the skin, and optionally exposing the wound site or skin to light.Type: GrantFiled: March 20, 2007Date of Patent: August 5, 2008Assignee: Photopharmica LimitedInventors: Stanley Beames Brown, Cassandra Clare O'Grady
-
Patent number: 7358226Abstract: Methods, compositions and apparatus for localized delivery of compounds are provided. In certain embodiments, radiation force is used to direct carriers to a target site, and additional radiation is used to fragment the localized carriers, releasing associate compounds. Ultrasound radiation is preferred as the source for radiation force and for fragmentation. Also encompassed are embodiments in which targeting and fragmentations are combined with imaging of the treatment site. Alternate embodiments are disclosed in which compounds are locally delivered without use of carriers.Type: GrantFiled: August 26, 2004Date of Patent: April 15, 2008Assignee: The Regents of the University of CaliforniaInventors: Paul Dayton, Katherine W. Ferrara, Michaelann Shortencarier, Susannah Bloch
-
Publication number: 20080026081Abstract: The present invention relates to methods of treatment using the compound (+)-isopropyl 2-methoxyethyl 4-(2-chloro-3-cyano-phenyl)-1,4-dihydro-2,6-dimethyl-pyridine-3,5-dicarboxylate, as a sole active agent or in combination with other pharmacological agents.Type: ApplicationFiled: November 19, 2004Publication date: January 31, 2008Inventors: Axel Unterbeck, Michael De Vivo, Gregory M. Rose
-
Patent number: 7148216Abstract: The invention features a method for treating a patient having a cancer or other neoplasm by administering to the patient two compounds simultaneously or within 14 days of each other in amounts sufficient to treat the patient.Type: GrantFiled: December 28, 2004Date of Patent: December 12, 2006Assignee: CombinatoRx, Inc.Inventors: Alexis Borisy, Curtis Keith, Michael A. Foley, Brent R. Stockwell
-
Patent number: 7119089Abstract: Phenothiazine derivatives of formula (I) are disclosed. The compounds are inhibitors of the mitotic kinesin KSP and are useful in the treatment of cellular proliferative diseases, such as cancer, hyperplasias, restenosis, cardiac hypertrophy, immune disorders and inflammation.Type: GrantFiled: September 16, 2005Date of Patent: October 10, 2006Assignee: Cytokinetics, Inc.Inventors: Jeffrey T. Finer, John C. Chabala
-
Patent number: 7008934Abstract: Compositions and methods are provided for reducing adverse reactions as a result of parenteral administration of certain phenothiazine derivatives such as promethazine hydrochloride. The active compound may be admixed with an effective amount of one or more cyclodextrin derivatives, and if desired, one or more non-ionic surfactants such as the partial esters of sorbitol and the polyoxyethylene oxides of long chain fatty acids such as the polysorbates.Type: GrantFiled: June 26, 2002Date of Patent: March 7, 2006Assignee: Baxter International Inc.Inventor: Jianwei Yu
-
Patent number: 6992082Abstract: Phenothiazine derivatives of formula (I) are disclosed. The compounds are inhibitors of the mitotic kinesin KSP and are useful in the treatment of cellular proliferative diseases, such as cancer, hyperplasias, restenosis, cardiac hypertrophy, immune disorders and inflammation.Type: GrantFiled: January 18, 2002Date of Patent: January 31, 2006Assignee: Cytokinetics, Inc.Inventors: Jeffrey T. Finer, John C. Chabala
-
Patent number: 6846816Abstract: The invention features a method for treating a patient having a cancer or other neoplasm by administering to the patient two compounds simultaneously or within 14 days of each other in amounts sufficient to treat the patient.Type: GrantFiled: January 21, 2003Date of Patent: January 25, 2005Assignee: CombinatoRx, Inc.Inventors: Alexis Borisy, Curtis Keith, Michael A. Foley, Brent R. Stockwell
-
Patent number: 6756370Abstract: The invention relates to compounds of formula (I), wherein R1, R2 and A have the meanings given in claim 1, are potent 5-HT2A antagonists and are suitable for treating psychoses, schizophrenia, depression, neurological disorders, impaired memory, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease, Huntington's disease, eating disorders such as bulimia and anorexia nervosa, Pre-Menstrual Syndrome and/or for positively influencing obsessive-compulsive disorders, (OCD).Type: GrantFiled: February 21, 2002Date of Patent: June 29, 2004Assignee: Merck Patent GmbHInventors: Helmut Prücher, Henning Böttcher, Karl-August Ackermann, Rudolf Gottschlich, Christoph van Amsterdam, Christoph Seyfried, Jürgen Harting, Gerd Bartoszyk, Hartmut Greiner
-
Publication number: 20040097488Abstract: Therapeutic compositions of doxepin having a preponderance of the cis doxepin isomer over the trans doxepin isomer provide therapeutic effects for affective, painful, or allergic disorders without the substantial sedative effects commonly experienced with compositions having a preponderance of the trans doxepin isomer.Type: ApplicationFiled: November 14, 2002Publication date: May 20, 2004Inventor: Joel E. Bernstein
-
Publication number: 20030158097Abstract: Novel medicinal compositions aiming at delivering a medicine to a specific site of the large intestine; and preparations for intestinal administration with the use of the same. Namely, medicinal compositions, whereby a medicine can be delivered to a specific site of the large intestine, characterized by containing a P-glycoprotein modifier; and preparations for intestinal administration with the use of the same.Type: ApplicationFiled: November 21, 2002Publication date: August 21, 2003Inventors: Norifumi Tanida, Takeshi Goto, Yuji Kurosaki
-
Publication number: 20030130263Abstract: Compositions comprising both a sedative and a non-sedative antihistamine are disclosed as well as methods of inhibiting the release of histamines by administration of the compositions to a mammalian subject.Type: ApplicationFiled: December 5, 2001Publication date: July 10, 2003Applicant: PEIRCE MANAGEMENT,LLCInventor: Mark Hirsh
-
Patent number: 6583138Abstract: The invention provides a novel heterocyclic ring condensed benzothiazine compound which is effective for prevention or remedy of disease, in which histamine, leukotriene and the like participate. The heterocyclic ring condensed benzothiazine compound of the present invention or a pharmacologically acceptable salt thereof is effective for prevention or remedy of disease, in which a chemical mediator, such as histamine, leukotriene and the like, participate, for example, asthma, allergic coryza, atopic dermatitis, hives, hay fever, gastrointestinal allergy, food allergy and the like.Type: GrantFiled: January 4, 2001Date of Patent: June 24, 2003Assignee: Eisai Co., Ltd.Inventors: Mitsuaki Miyamoto, Tatsuya Yoshiuchi, Keizo Sato, Motohiro Soejima, Takashi Sato, Koichi Kikuchi, Hiroyuki Yoshimura, Katsuhiro Moriya, Yoshinori Sakuma, Shigeru Akasofu, Koji Yamada
-
Patent number: 6566389Abstract: A method for treating or preventing symptoms of tardive dyskensia comprises administering melatonin to patient exhibiting or liable to develop such symptoms. The melatonin is administered in an amount effective to ameliorate or prevent symptoms of tardive dyskensia developing in the patient.Type: GrantFiled: November 26, 2001Date of Patent: May 20, 2003Assignee: Neurim Pharmaceuticals (1991) Ltd.Inventors: Nava Zisapel, Moshe Laudon
-
Patent number: 6525100Abstract: The invention is of a topical medicament and associated methodology for use thereof, through the use of which Peyronie's disease may be effectively, cost effectively, and painlessly treated. The primary active ingredient is a calmodulin blocker, the preferred such ingredient being trifluroperizine.Type: GrantFiled: November 22, 2000Date of Patent: February 25, 2003Inventors: W. Jerry Easterling, William P. Fitch, III
-
Patent number: 6509335Abstract: This invention discloses benzoxazinone and benzothiazinone compounds which display inhibitory effects on serine proteases such as factor Xa, thrombin, and/or factor VIIa. The invention also discloses pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, and methods of using them as therapeutic agents for treating or preventing disease states in mammals characterized by abnornal thrombosis.Type: GrantFiled: August 14, 2000Date of Patent: January 21, 2003Assignee: Warner-Lambert CompanyInventors: Kent Alan Berryman, Dennis Michael Downing, Danette Andrea Dudley, Jeremy John Edmunds, Lakshmi Sourirajan Narasimhan, Stephen Taras Rapundalo
-
Patent number: 6468971Abstract: Kappa-opioid agonists prevent the impairment of renal function otherwise caused by the combination of gaseous anesthesia and surgery or severe trauma. Not only do these agents preserve renal function and maintain urine output, they also maintain plasma electrolyte concentration and osmolality by reducing renal loss of sodium and potassium when compared to other diuretic agents. The preservation of urine flow as well as the ability to retain body sodium, potassium, calcium, and osmolality during surgery or severe trauma under gaseous anesthesia are novel and unique properties associated only with kappa opioid agonists. To date, no other clinically-used diuretic agent has been shown to provide constant urine flow, or to retain electrolytes during anesthesia and surgery. The kappa opioid agonists may be used in surgical patients with normal cardiovascular function, but are particularly useful in patients with compromised cardiovascular and/or renal function.Type: GrantFiled: September 2, 1998Date of Patent: October 22, 2002Assignee: Board of Supervisors of Louisiana State University and Agricultural and Mechanical CollegeInventor: Daniel R. Kapusta
-
Patent number: RE39300Abstract: Nontoxic substances that block the N-methyl-D-aspartate (NMDA) receptor, e.g., a morphinan such as dextromethorphan or dextrorphan, or that block a major intracellular consequence of NMDA-receptor activation, e.g., a ganglioside such as GM1 or GT1b, a phenothiazine such as trifluoperazine or a naphthalenesulfonamide such as N-(6-aminohexyl)-5-chloro-1-naphthalenesulfonamide, inhibit the development of tolerance to and/or dependence on addictive drugs, e.g., narcotic analgesics such as morphine, codeine, etc.Type: GrantFiled: June 15, 2001Date of Patent: September 19, 2006Assignee: Virginia Commonwealth University Medical College of VirginiaInventors: David J. Mayer, Jianren Mao