Ring Nitrogen Shared By Two Of The Cyclos Patents (Class 514/230.2)
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Publication number: 20080207538Abstract: This invention provides methods for enhancing production in a subject of a functional protein from a gene disrupted by a mutation, for example by the presence of a premature stop codon or by an exon skipping mutation, comprising administering to the subject an amount of an agent effective to suppress the mutation and an amount of an agent effective to increase transcription of the gene.Type: ApplicationFiled: March 7, 2005Publication date: August 28, 2008Inventors: David S. Lawrence, Biao Xi
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Patent number: 7414051Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.Type: GrantFiled: April 11, 2007Date of Patent: August 19, 2008Assignee: WyethInventors: Hassan Mahmoud Elokdah, Alexander Alexei Greenfield, Cristina Grosanu, Albert Jean Robichaud
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Publication number: 20080146553Abstract: Compositions including a quinolone component in an amount effective as an antibiotic when the composition is placed in a mammalian eye, and a carrier component in an amount effective to act as a carrier for the quinolone component are provided. The present compositions are substantially free of other components effective as preservatives. Preferably the quinolone component has fungistatic activity. In one very useful embodiment, the compositions include a NSAID component in an amount effective to reduce inflammation or pain when the composition is placed in a mammalian eye. Methods of using the present compositions, for example, to resolve microbial infections and/or to reduce inflammation and/or pain in a mammalian eye are included within the scope of the present invention.Type: ApplicationFiled: February 20, 2008Publication date: June 19, 2008Applicant: Allergan, Inc.Inventors: Christopher A. Muller, Elizabeth A. Bancroft, Janet K. Cheetham, Harold G. Jensen, Teresa H. Kuan, David F. Power, Kevin D. Skule
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Publication number: 20080139472Abstract: This invention provides methods of preserving, improving, or restoring cognitive function in mammal having one or more mutations in the FMR1 gene (e.g. at risk for or having fragile x syndrome), where the methods involve the brain derived neurotrophic factor (BDNF) level or activity in the brain of said mammal. In certain embodiments the methods involve administering one or more AMPA potentiators (e.g., ampakines) to the mammal in an amount sufficient to increase BDNF levels in the brain of the mammal.Type: ApplicationFiled: October 5, 2007Publication date: June 12, 2008Inventors: JULIE LAUTERBORN, GARY LYNCH, CHRISTINE GALL, CHRISTOPHER REX
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Publication number: 20080139545Abstract: The present invention provides a pharmaceutical composition that includes: (a) at least one of a non-aminoglycoside antibiotic and an anti-inflammatory agent; and (b) a biofilm-dissolving agent.Type: ApplicationFiled: May 22, 2007Publication date: June 12, 2008Inventors: Won-Taek Choe, Joseph Baxter Roberson, Michael T. Murray
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Publication number: 20080132457Abstract: Efflux pump inhibitors are co-administered with antimicrobial agents for the treatment of ophthalmic or otic infections. The agents may be co-administered directly to the site of infection (e.g., the eye or ear).Type: ApplicationFiled: September 17, 2007Publication date: June 5, 2008Inventors: Keith Bostian, Thomasz Glinka, Olga Lomovskaya, Mark Surber, Neil Berkley, David Griffith
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Publication number: 20080125422Abstract: The invention relates to the use of a 5-HT4 receptor antagonist in the manufacture of a medicament for the prophylaxis or treatment of atrial remodelling in a mammal. Preferably, the antagonist is N-[(1-nbutyl-4-piperidinyl)methyl]-3,4-dihydro-2H-[1,3]oxazino[3,2-a]indole-10-carboxamide (SB 207266) or a pharmaceutically acceptable salt thereof. The invention also relates to the use of SB 207266 or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for the treatment or prophylaxis of atrial fibrillation in a mammal by administering to the mammal a daily oral or parenteral dosage regimen of about 0.2 mg to 1.0 mg of the SB 207266 or salt thereof per kg of total body weight (measured as the free base). The invention also relates to the use of SB 207266 or a pharmaceutically acceptable salt thereof in the prophylaxis or treatment of atrial arrhythmia in a mammal by administration of the SB 207266 or salt thereof on the first day at a loading dose of about 1.2 to about 2.Type: ApplicationFiled: October 31, 2007Publication date: May 29, 2008Inventors: Mireille Marguerite Jeanne Bonhomme, Antoine Michel Alain Bril, Bernard Emile Joseph Gout, Bela Rajiv Patel, Gillian Louise Shepherd, Neeta Balkrishan Amin, Bernard Enno Ilson
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Publication number: 20080124385Abstract: Methods for treating and preventing middle ear infections by transmembrane administration of medicament-containing transmembrane carrier compositions, such as liposomes and other lipid vesicles, to the tympanic membrane. Medicaments useful for treating pain, inflammation or infection in the outer ear may be co-administered. If utilized for transmembrane administration, the liposomes or other lipid vesicles will usually not be sterically stabilized. The medicaments delivered according to the methods of the invention include antibiotic, anti-viral, anti-fungal and anti-inflammatory agents that are useful in treatment and/or prophylaxis of middle ear infections and their sequelae.Type: ApplicationFiled: September 2, 2005Publication date: May 29, 2008Inventor: William R. Campbell
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Patent number: 7358245Abstract: The administration of cannabinoid receptor agonists for inhibition of transient lower esophageal sphincter relaxations, gastroesophageal reflux disease and regurgitation is disclosed.Type: GrantFiled: November 20, 2002Date of Patent: April 15, 2008Assignee: AstraZenca ABInventor: Anders Lehmann
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Patent number: 7326703Abstract: The present invention realtes to 5H-pyrazolo[1,5-c][1,3]benzoxazin-5-yl)phenyl methanone derivatives as inhibitors of the viral replication of the HIV virus, processes for their preparation as well as pharmaceutical compositions, their use as medicines, and diagnostic kits comprising them. The present invention also concerns combinations of the present HIV inhibitors with other anti-retroviral agents. It further relates to their use in assays as reference compounds or as reagents. The compounds of the present invention are useful for preventing or treating infection by HIV and for treating AIDS.Type: GrantFiled: May 4, 2005Date of Patent: February 5, 2008Assignee: Tibotec Pharmaceuticals LtdInventors: Abdellah Tahri, Lieve Emma Jan Michiels, Koenraad Lodewijk August Van Acker, Dominique Louis Nestor Ghislain Surleraux
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Publication number: 20080027040Abstract: The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:Type: ApplicationFiled: December 20, 2004Publication date: January 31, 2008Applicant: Morphochem Aktiengesellschaft Fur KombinatorischeInventors: Christian Hubschwerlen, Jean-Luc Specklin, Daniel Baeschlin, Christine Schmitt, Stefan Muller, Michael W. Cappi
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Publication number: 20070244106Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.Type: ApplicationFiled: April 11, 2007Publication date: October 18, 2007Applicant: WyethInventors: Hassan Mahmoud Elokdah, Alexander Alexei Greenfield, Cristina Grosanu, Albert Jean Robichaud
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Publication number: 20070244105Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.Type: ApplicationFiled: April 11, 2007Publication date: October 18, 2007Applicant: WyethInventors: Alexander Alexei Greenfield, Cristina Grosanu, Hassan Mahmoud Elokdah, Albert Jean Robichaud
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Patent number: 7273859Abstract: The invention encompasses a series of pyrimidinone compounds which inhibit HIV integrase and thereby prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses intermediates useful for making the pyrimidone compounds.Type: GrantFiled: April 20, 2005Date of Patent: September 25, 2007Assignee: Bristol-Myers Squibb CompanyInventor: B. Narasimhulu Naidu
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Patent number: 7235550Abstract: The invention relates to compounds of formula (I): wherein: G1 represents an alkylene chain as defined in the description, A represents R2 and R3 represent hydrogen, alkyl, alkoxy or hydroxy or together form oxo, R4 and R5 represent hydrogen, R1 is as defined in the description, and medicinal products containing the same which are useful in treating or preventing melatoninergic disorders.Type: GrantFiled: October 9, 2002Date of Patent: June 26, 2007Assignee: Les Laboratoires ServierInventors: Gérald Guillaumet, Marie-Claude Viaud, Hervé Van de Poel, Philippe Delagrange, Caroline Bennejean, Pierre Renard
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Patent number: 7208490Abstract: The invention includes tetrahydroquinoline and related compounds of formula I, and pharmaceutical compositions thereof, that exhibit useful antibacterial activity against a wide range of human and veterinary pathogensType: GrantFiled: October 2, 2003Date of Patent: April 24, 2007Assignee: Pharmacia & Upjohn Company LLCInventors: Michael Robert Barbachyn, Gordan L. Bundy, Paul Joseph Dobrowolski, Alexander Ross Hurd, Gary E. Martin, Dennis Joseph McNamara, John Raymond Palmer, Donna L. Romero, Arthur Glenn Romero, J. Craig Ruble, Debra Ann Sherry, Lisa Marie Thomasco, Peter Laurence Toogood
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Patent number: 7179805Abstract: The present invention relates to compounds having a structure according to Formula I wherein n, m, z, R, R2, R3, R4, R5, R6, A, E, X, Y, a and b are as defined above; or an optical isomer, diastereomer or enantiomer thereof; a pharmaceutically acceptable salt, hydrate, or prodrug thereof.Type: GrantFiled: September 9, 2004Date of Patent: February 20, 2007Assignee: Janssen Pharmaceutica N.V.Inventors: Eugene B. Grant, III, Mark J. Macielag, Xiaoqing Xu, Steven David Paget, Michele Ann Weidner-Wells
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Patent number: 7160899Abstract: This invention relates to the use of the combined action of a compound with neurotrophic activity and an adenosine A2A receptor antagonist for the treatment of Parkinson's disease.Type: GrantFiled: April 4, 2002Date of Patent: January 9, 2007Assignee: Neurosearch A/SInventors: Dan Peters, Lars Christian B. Rønn, Karin Sandager Nielsen
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Patent number: 7153851Abstract: A compound as represented by the general formula (I) shown below exhibits high antibacterial activity against gram-positive bacteria, in particular, such drug-resistant bacteria as mRNA, PRSP and VRE: wherein R1 is a methyl group, a fluoromethyl group, a methoxymethyl group, an acetoxymethyl group, a hydroxymethyl group or a methylene; R2 is a hydrogen atom, a lower alkyl group having 1 to 3 carbon atoms, or a pharmaceutically acceptable cation and an ester of a prodrug; R3 is a hydrogen atom or a halogen atom; R4 is a hydrogen atom, a lower alkyl group having 1 to 3 carbon atoms, a fluoromethyl group, a trifluoromethyl group or a fluorine atom; and R5 is a hydrogen atom or a fluorine atom, with exceptions where R1 is a methyl group, R4 and R5 are at the same time a hydrogen atom, and R3 is a fluorine atom.Type: GrantFiled: March 13, 2003Date of Patent: December 26, 2006Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Yoshikazu Asahina, Masaya Takei
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Patent number: 6958333Abstract: The present invention relates to a compound of Formula (I) and the manufacturing method(s) thereof and the use thereof: ? wherein: Ar is a nitrogen-containing heteroaromatic ring group; X and Z are each a carbon atom, and so on; Y is CO, and so on; R1 is a hydrogen atom, and so on; R2 and R3 are each a hydrogen atom, and so on; R4 and R5 are each a hydrogen atom, and so on; and the formula is a single bond or a double bond. According to the present invention, the compound of the present invention can provide Cdk4 and/or Cdk6 inhibitors for treating malignant tumors, because the compounds of the present invention exhibit a prominent growth inhibitory activity against tumor cells.Type: GrantFiled: July 26, 2000Date of Patent: October 25, 2005Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Takashi Hayama, Kyoko Hayashi, Teruki Honma, Ikuko Takahashi
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Patent number: 6919334Abstract: Compounds of the formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa and bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.Type: GrantFiled: September 10, 2003Date of Patent: July 19, 2005Assignee: WyethInventors: Hong Gao, Gary Paul Stack
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Patent number: 6887868Abstract: The present invention provides compounds of Formula (I): wherein: R1, R2, R3, R4, R5, R6 R7, R8, n, m, and X have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of Formula (I). The compounds are 5-HT ligands and are useful for treating diseases wherein modulation of 5-HT activity is desired.Type: GrantFiled: September 19, 2002Date of Patent: May 3, 2005Assignee: Pharmacia & Upjohn CompanyInventor: Jian-Min Fu
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Publication number: 20040259809Abstract: The present invention provides pharmaceutical compositions including a sedating antihistamine and a stimulant, and methods of use thereof. The stimulant reduces the sedation caused by the antihistamine, thereby allowing potent, but sedating, antihistamines to be used effectively.Type: ApplicationFiled: June 17, 2003Publication date: December 23, 2004Applicant: PediaMed Pharmaceuticals, Inc.Inventor: Gilbert Rene Gonzales
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Publication number: 20040259871Abstract: This invention related to the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for higher order behaviors. These brain networks are involved in cognitive abilities related to memory impairment, such as is observed In a variety of dementias, and in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson's disease, schizophrenia and affective disorders. In a particular aspect, the present invention relates to compounds useful for treatment of such conditions and methods of using these compounds for such treatment.Type: ApplicationFiled: August 3, 2004Publication date: December 23, 2004Inventors: Gary A. Rogers, Matthew Allan, Clayton Harris, Jianjie Huang, Christopher M. Marrs, Rudolf Mueller, Stanislaw Rachwal
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Patent number: 6821969Abstract: The present invention provides a compound of formula I These compounds are useful as antiviral agents, in particular, as agents against viruses of the herpes family.Type: GrantFiled: December 27, 2001Date of Patent: November 23, 2004Assignee: Pharmacia & UpJohn CompanyInventor: Atli Thorarensen
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Publication number: 20040198726Abstract: CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke. The CRF receptor antagonists of this invention have the following structure of formula (I): including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, R1, R2, R4, R5, R6, A, X, and Y are as defined herein. Compositions containing a CRF receptor antagonist in combination with a pharmaceutically acceptable carrier are also disclosed, as well as methods for use of the same.Type: ApplicationFiled: May 28, 2004Publication date: October 7, 2004Inventors: Romano Di Fabio, Gabriella Gentile, Mustapha Haddach, Yves St Denis, John Patrick Williams
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Patent number: 6794391Abstract: The invention provides compounds or salts thereof of the general formula (I): wherein each of R1 and R2 independently represents a C1-6 alkyl or C2-7 acyl group; X represents OCH2 or a group CR3R4; wherein each of R3 or R4 independently represents a hydrogen atom or a C1-3 alkyl group; R5 represents a hydrogen atom or a C1-3 alkyl, C2-3 alkenyl or C2-3 alkynyl group; R6 represents a hydrogen atom or a C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, amino, C1-6 alkylamino, di(C1-6) alkylamino or C2-7 acylamino group; each of R7 and R8 independently represents a hydrogen or halogen atom or a hydroxy, trifluoromethyl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C2-7 acyl, C1-6 alkylthio, C1-6 alkoxy, C3-6 cycloalkyl; and R9 represents a hydrogen or halogen atom or a hydroxy, trifluoromethyl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C2-7 acyl, C1-6 alkylthio, C1-6 alkoxy or C3-6 cycloalkyl group. The compounds or salts thereof are useful for treatment of respiratory disorders such as asthma.Type: GrantFiled: September 26, 2001Date of Patent: September 21, 2004Assignee: Vernalis LimitedInventors: Alexander William Oxford, David Jack
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Publication number: 20040176370Abstract: 3,4-Dihydro-N-[[1-(3-hydroxybutyl-4-piperidinyl]methyl]-2H-[1,3]oxazino[3,2-&agr;]indole-10-carboxamide and its use as 5-HT4 receptor antagonist for example in the treatment or prophylaxis of gastrointestinal disorders, cardiovascular disorders and CNS disorders.Type: ApplicationFiled: March 16, 2004Publication date: September 9, 2004Applicant: SmithKline Beecham p.l.c.Inventors: Frank Hossner, David Austin Ryan
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Publication number: 20040170654Abstract: A method for systemic administration of a hydrophobic dopamine agonist to a mammal is disclosed. The method involves delivering the hydrophobic dopamine agonist to the dermis of the mammal whereby improved systemic absorption is obtained compared to absorption produced upon delivering the substance subcutaneously by bolus administration.Type: ApplicationFiled: December 15, 2003Publication date: September 2, 2004Inventor: Thomas C. Pinkerton
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Publication number: 20040147504Abstract: The invention relates to the use of compound of Formula I in treating patients for inflammatory or neuropathic pain as well as various symptoms of multiple sclerosis.Type: ApplicationFiled: December 16, 2003Publication date: July 29, 2004Applicant: Aventis Pharmaceuticals Inc.Inventors: Bin Zhu, Joseph Wettstein, Margaret A. Petty
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Patent number: 6762181Abstract: This invention provides a quinolone derivative having potent antibacterial activity against various bacteria including drug-resistant strains which is a compound of the following formula wherein R1 is an optionally substituted aromatic group, a salt of the same or a hydrate of both.Type: GrantFiled: September 7, 2001Date of Patent: July 13, 2004Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Makoto Takemura, Hisashi Takahashi, Katsuhiro Kawakami, Toshiyuki Takeda, Rie Miyauchi
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Patent number: 6756368Abstract: A method of treating a subject infected with a virus or a method of preventing viral infection of a subject comprising administering to the subject an effective amount of a compound having the structure: wherein L=L′=2-methylimidazole.Type: GrantFiled: July 6, 2000Date of Patent: June 29, 2004Assignee: The Trustees of Columbia University in the City of New YorkInventors: Saul J. Silverstein, Erik K. Lium, Jennifer A. Schwartz
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Patent number: 6716830Abstract: Ophthalmic, otic and nasal compositions containing a new class of antibiotics (e.g., moxifloxacin) are disclosed. The compositions preferably also contain one or more anti-inflammatory agents. The compositions may be utilized to treat ophthalmic, otic and nasal conditions by topically applying the compositions to the affected tissues.Type: GrantFiled: July 22, 2002Date of Patent: April 6, 2004Assignee: Alcon, Inc.Inventors: Gerald Cagle, Robert L. Abshire, David W. Stroman, John M. Yanni
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Patent number: 6713468Abstract: Methods of using compounds of formula (I): their racemates, enantiomers, diastereoisomers and inorganic acid salts and organic acid salts thereof.Type: GrantFiled: July 25, 2002Date of Patent: March 30, 2004Assignee: Aventis Pharma S.A.Inventors: Jean-Claude Hardy, Jean Bouquerel, Patrick Nemecek, Jean-Claude Aloup, Serge Mignani, Jean-François Peyronel
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Patent number: 6699989Abstract: Disclosed are guanidine and biguanidine derivatives which have anti-viral and anti-bacterial activity. Also disclosed are pharmaceutical compositions containing such compounds as an active ingredient, and anti-viral and anti-bacterial methods utilizing such compounds.Type: GrantFiled: August 28, 2000Date of Patent: March 2, 2004Inventor: B. Vithal Shetty
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Patent number: 6673793Abstract: The present invention provides a compound of formula I which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.Type: GrantFiled: June 28, 2001Date of Patent: January 6, 2004Assignee: Pharmacia & Upjohn Co.Inventors: Steven Ronald Turner, Suvit Thaisrivongs, Atli Thorarensen
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Publication number: 20030229026Abstract: The present invention provides selective kinase inhibitors of formula (I).Type: ApplicationFiled: December 2, 2002Publication date: December 11, 2003Inventors: Rima Salim Al-Awar, Kyle Andrew Hecker, James Edward Ray, Jianping Huang, Sajan Joseph, Tiechao Li, Michael Paal, Radhakrishnan Rathnachalam, Chuan Shih, Philip Parker Waid, Xun Zhou, Guoxin Zhu
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Publication number: 20030225070Abstract: This invention relates to the treatment of mGluR5 receptor mediated disorders, which comprises administering to a person in need of treatment a compound having the formula 1Type: ApplicationFiled: April 4, 2003Publication date: December 4, 2003Inventors: Vincent Mutel, Jens-Uwe Peters, Juergen Wichmann
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Patent number: 6624159Abstract: The present invention provides a compound of formula I which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.Type: GrantFiled: June 22, 2001Date of Patent: September 23, 2003Assignee: Pharmacia & Upjohn CompanyInventors: David John Anderson, Gordon L. Bundy, Fred L. Ciske, David R. Graber, Michael J. Genin, Thomas M. Judge, Malcolm Wilson Moon, Mark E. Schnute, Joseph Walter Strohbach, Suvit Thaisrivongs, Atli Thorarensen, Steven Ronald Turner, Valerie A. Vaillancourt, Allison J. Wolf
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Patent number: 6620808Abstract: Methods for modulating the endocrine system of a mammal are provided. In the subject methods, a positive allosteric modulator of AMPA receptors of the hypothalamus are administered to the host. The subject methods find use in applications where it is desired to increase the circulatory level of a hormone in a mammalian host, such as diseased states characterized by abnormally depressed circulatory levels of the hormone.Type: GrantFiled: September 25, 2001Date of Patent: September 16, 2003Assignee: The Regents of the University of CaliforniaInventors: Peter Van Der Klish, Gary Lynch
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Patent number: 6602868Abstract: The invention provides methods and use of heterocyclic amines, and phenylazacycloalkane compounds, and their pharmacologically acceptable salts for the treatment of Restless Legs Syndrome (RLS).Type: GrantFiled: October 29, 2001Date of Patent: August 5, 2003Assignee: Pharmacia & Upjohn CompanyInventors: Sylvia McBrinn, Richard Wayne Anderson
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Publication number: 20030134847Abstract: The invention relates to compound of formula (I): 1Type: ApplicationFiled: October 9, 2002Publication date: July 17, 2003Inventors: Gerald Guillaumet, Marie-Claude Viaud, Herve Van De Poel, Philippe Delagrange, Caroline Bennejean, Pierre Renard
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Patent number: 6573260Abstract: This invention provides a quinolone derivative which exerts strong antibacterial action upon various bacteria and has high safety, and it relates to a compound having a structure of formula (I), its salts and hydrates thereof: {R1 and R2: hydrogen, alkyl; n: 1 to 4; Q: following structure (Ia): [R3: alkyl, alkenyl, halogenoalkyl, cyclic alkyl, aryl, heteroaryl, alkoxyl, alkylamino; R4: hydrogen, alkylthio; R5: hydrogen, amino, hydroxyl, thiol, halogenomethyl, alkyl, alkenyl, alkynyl, alkoxyl; X1: halogen, hydrogen, A1: nitrogen, structure of formula (II): (X2: hydrogen, amino, halogen, cyano, halogenomethyl, halogenomethyl, alkyl, alkenyl, alkynyl, alkoxyl; R4 and R3 or X2 and R3 may together form a cyclic structure; Y: hydrogen, various ester forming groups]}.Type: GrantFiled: May 24, 2001Date of Patent: June 3, 2003Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Makoto Takemura, Hisashi Takahashi, Rie Miyauchi, Toshiyuki Takeda, Isao Hayakawa
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Publication number: 20030092711Abstract: Methods of using compounds which are progesterone receptor agonists for contraception and the treatment of progesterone-related maladies alone or in combination with an estrogen receptor agonist or progesterone receptor antagonist are provided.Type: ApplicationFiled: May 6, 2002Publication date: May 15, 2003Inventors: Puwen Zhang, Andrew Fensome, Eugene A. Terefenko, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley, Jay E. Wrobel, Mark A. Collins
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Publication number: 20030092676Abstract: 1Type: ApplicationFiled: May 21, 2002Publication date: May 15, 2003Inventors: Rima Salim Al-Awar, Kyle Andrew Hecker, Jianping Huang, Sajan Joseph, James Edward Ray, Philip Parker Waid
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Publication number: 20030087883Abstract: The present invention provides compounds of Formula (I): 1Type: ApplicationFiled: September 19, 2002Publication date: May 8, 2003Inventor: Jian-Min Fu
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Patent number: 6552018Abstract: The present invention relates to cis- and trans-forms of pyrazole derivatives, salts thereof, or agents containing the same, and represented by the general formula (I): wherein G represents a nitrogen containing saturated heterocyclic structure represented by the following formula: These compounds exhibit anti-tumor activity on 5-FU-resistant tumors and effects on P glycoprotein expressing, multiple-drug resistant tumors. An example of a pyrazole derivative which demonstrates 50% inhibition of tumor cell growth is 3-[4-(3-chloro-5-fluorophenyl)-1piperazinyl]-1-[1-(3-chloro-2-pyridyl)-5-methyl-4-pyrazolyl)-1-trans-propene hydrochloride. Synthesis of the compounds represented by formula (I) can be prepared by any one of various routes such as a Mannich reaction, a Wittig reaction, reductive amination or substitution by allylation.Type: GrantFiled: October 17, 2000Date of Patent: April 22, 2003Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Akio Ejima, Satoru Ohsuki, Hitoshi Ohki, Hiroyuki Naito
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Publication number: 20030045520Abstract: This invention relates to tricyclic compounds having spiro union represented by the following formula (I) or its salt which is useful as a drug, and in particular, as an inhibitor for activated blood coagulation factor X, which can be administered orally and which exhibits strong anticoagulation action.Type: ApplicationFiled: December 27, 2001Publication date: March 6, 2003Inventors: Hidemitsu Nishida, Fumihiko Saitoh, Kousuke Harada, Ikuya Shiromizu, Takafumi Mukaihira
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Publication number: 20030008894Abstract: Compounds of the following formula: 1Type: ApplicationFiled: December 14, 2001Publication date: January 9, 2003Applicant: The Procter & Gamble CompanyInventors: Benoit Ledoussal, Xiufeng Eric Hu, Ji-In Kim Almstead, Jeffrey Lyle Gray
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Publication number: 20030004152Abstract: The present invention is a method of treating sexual disturbances in humans and inducing mating in non-human mammals using the compounds of formula (A) 1Type: ApplicationFiled: July 30, 2002Publication date: January 2, 2003Inventors: Robert B. McCall, Martin Durham Meglasson