The Chalcogen, X, Is In A -c(=x)- Group (e.g., 1-phenyl -2-pyrrolidino Hexanone-1, Etc.) Patents (Class 548/571)
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Patent number: 8940718Abstract: The disclosure is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: GrantFiled: November 16, 2012Date of Patent: January 27, 2015Assignee: Gilead Pharmasset LLCInventors: Elizabeth M. Bacon, Jeromy J. Cottell, Ashley Anne Katana, Darryl Kato, Evan S. Krygowski, John O. Link, James Taylor, Chinh Viet Tran, Teresa Alejandra Trejo Martin, Zheng-Yu Yang, Sheila Zipfel
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Patent number: 8940776Abstract: A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The subject has type 2 diabetes; renal hypertrophy or hyperplasia associated with diabetic nephropathy; Tay-Sachs; Gaucher's; or Fabry's disease. Methods of decreasing plasma TNF-?, lowering blood glucose levels, decreasing glycated hemoglobin levels, inhibiting glucosylceramide synthase, and lowering glycosphingolipid concentrations in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.Type: GrantFiled: August 27, 2012Date of Patent: January 27, 2015Assignee: Genzyme CorporationInventors: Craig Siegel, Cecilia M. Bastos, David J. Harris, Angeles Dios, Edward Lee, Richard Silva, Lisa M. Cuff, Mikaela Levine, Cassandra A. Celatka, Frederic Vinick, Thomas H. Jozefiak, Yibin Xiang, John Kane, Junkai Liao
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Patent number: 8921341Abstract: The disclosure is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: GrantFiled: October 8, 2013Date of Patent: December 30, 2014Assignee: Gilead Pharmasset LLCInventors: Elizabeth M. Bacon, Jeromy J. Cottell, Ashley Anne Katana, Darryl Kato, Evan S. Krygowski, John O. Link, James Taylor, Chinh Viet Tran, Teresa Alejandra Trejo Martin, Zheng-Yu Yang, Sheila Zipfel
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Patent number: 8791076Abstract: The invention relates to compounds of Formula I: and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, and R3 are defined as set forth in the specification. The compounds are agonists of neurotrophin (such as nerve growth factor) receptors.Type: GrantFiled: August 31, 2011Date of Patent: July 29, 2014Inventors: Pablo Villoslada, Angel Messeguer
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Publication number: 20140080833Abstract: Intracellular kinase inhibitors and their therapeutic uses for patients with T cell malignancies, B cell malignancies, autoimmune disorders, and transplanted organs.Type: ApplicationFiled: November 11, 2013Publication date: March 20, 2014Applicant: MannKind CorporationInventors: Gary A. Flynn, Sandra A. Lee, Mary Faris, David W. Brandt, Subrata Chakravarty
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Patent number: 8669252Abstract: Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.Type: GrantFiled: May 12, 2011Date of Patent: March 11, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Dong-Ming Shen, John S. Debenham, Thomas H. Graham, Matthew J. Clements, Yong Zhang
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Patent number: 8575135Abstract: The disclosure is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: GrantFiled: March 1, 2013Date of Patent: November 5, 2013Assignee: Gilead Sciences, Inc.Inventors: Elizabeth M. Bacon, Jeromy J. Cottell, Ashley Anne Katana, Darryl Kato, Evan S. Krygowski, John O. Link, James Taylor, Chinh Viet Tran, Teresa Alejandra Trejo Martin, Zheng-Yu Yang, Sheila Zipfel
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Publication number: 20130281664Abstract: The present invention relates to novel Ruthenium catalysts and related borohydride complexes, and the use of such catalysts, inter alia, for (1) hydrogenation of amides (including polyamides) to alcohols and amines; (2) preparing amides from alcohols with amines (including the preparation of polyamides (e.g., polypeptides) by reacting dialcohols and diamines and/or by polymerization of amino alcohols); (3) hydrogenation of esters to alcohols (including hydrogenation of cyclic esters (lactones) or cyclic di-esters (di-lactones) or polyesters); (4) hydrogenation of organic carbonates (including polycarbonates) to alcohols and hydrogenation of carbamates (including polycarbamates) or urea derivatives to alcohols and amines; (5) dehydrogenative coupling of alcohols to esters; (6) hydrogenation of secondary alcohols to ketones; (7) amidation of esters (i.e.Type: ApplicationFiled: October 11, 2011Publication date: October 24, 2013Inventors: David Milstein, Ekambaram Balaraman, Chidambaram Gunanathan, Boopathy Gnanaprakasam, Jing Zhang
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Patent number: 8552051Abstract: The use of mesembrenone and medicaments and dietary supplements containing mesembrenone. The applicant has surprisingly found that mesembrenone exhibits potent PDE-4 inhibition properties and, in addition to being useful in treating conditions that respond to treatment with a PDE-4 inhibitor, has dual activity on account of its serotonin-uptake inhibition properties. Mesembrenone is extracted and isolated, for example as a pure compound, from plant material of the plant family Mesembryanthemaceae. Preferably a plant or plants from the genus Sceletium, more preferably, Sceletium tortuosum(L) N.E.Br is used.Type: GrantFiled: March 16, 2010Date of Patent: October 8, 2013Assignee: H. L. Hall & Sons LimitedInventors: Alan Harvey, Nigel Gericke, Alvaro Viljoen
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Publication number: 20130203815Abstract: The present invention provides compounds represented by general formula (I): wherein, R1, R2, R3, L and T are as defined in the specification, in all their stereoisomeric and tautomeric forms and mixtures thereof in all ratios, and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, and prodrugs thereof. The invention also relates to processes for the manufacture of compounds of formula (I) and pharmaceutical compositions containing them. The compounds and the pharmaceutical compositions of the present invention are useful in the treatment of a condition or disorder mediated by one or more cytokines selected from Tumor Necrosis Factor-alpha (TNF-?) and interleukins such as IL-1, IL-6, and IL-8. The present invention further provides a method of treatment of inflammatory disorders by administering a therapeutically effective amount of the said compound of formula (I) or its pharmaceutical composition, to a mammal in need thereof.Type: ApplicationFiled: March 25, 2011Publication date: August 8, 2013Applicant: PIRAMAL ENTERPRISES LIMITEDInventors: Babasaheb Pandurang Bandgar, Jalindar Vasant Totre
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Patent number: 8283367Abstract: The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly or indirectly with proteasome activity.Type: GrantFiled: November 6, 2008Date of Patent: October 9, 2012Assignee: Cephalon, Inc.Inventors: Raffaella Bernardini, Alberto Bernareggi, Paolo G. Cassara, Germano D'Arasmo, Ernesto Menta, Ambrogio Oliva
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Patent number: 8129547Abstract: The present invention relates to a method for the anticoagulation of human blood ex vivo in which blood calcium concentration remains the same, no thrombin is formed and thrombocyte function is not affected. The invention further relates to a blood coagulation factor Xa inhibitor that can be advantageously used in this method, an agent that contains an inhibitor of the blood coagulation factor Xa, and a kit for diagnosing cellular blood components. The anticoagulated blood obtained according to the invention can be used for examining cellular blood components, for example for the diagnosis of thrombocyte function.Type: GrantFiled: January 26, 2007Date of Patent: March 6, 2012Inventors: Peter Hellstern, Jörg Stürzebecher, Uta Stürzebecher, legal representative
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Patent number: 8071604Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions of compounds of Formula (A): wherein Ar, X, Y, R1, R2, R3, and q are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness, promotion of wakefulness, treatment of Parkinson's disease, cerebral ischemia, stroke, sleep apneas, eating disorders, stimulation of appetite and weight gain, treatment of attention deficit hyperactivity disorder (“ADHD”), enhancing function in disorders associated with hypofunctionality of the cerebral cortex, including, but not limited to, depression, schizophrenia, fatigue, in particular, fatigue associated with neurologic disease, such as multiple sclerosis, chronic fatigue syndrome, and improvement of cognitive dysfunction.Type: GrantFiled: November 8, 2007Date of Patent: December 6, 2011Assignees: Cephalon France, Cephalon, Inc.Inventors: Brigitte Lesur, Philippe Louvet, Rabindranath Tripathy
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Patent number: 8044048Abstract: Derivatives of sulindac are provided along with pharmaceutical compositions containing them and use for precancerous conditions and treating cancer. Derivatives of sulindac are also suitable for treating chronic inflammatory conditions. A method for preparing the derivatives is also provided.Type: GrantFiled: January 4, 2007Date of Patent: October 25, 2011Assignee: Southern Research InstituteInventors: Gary Piazza, Robert Reynolds
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Publication number: 20110232870Abstract: Nitrogen-containing fluorochemical ketones are provided that can be useful in apparatuses that includes a device and a mechanism for transferring heat. The provided fluorochemical ketones are stable at temperatures above 170° C., are environmentally friendly, and are economical to produce. The provided apparatuses can be useful for vapor phase soldering of electronic devices.Type: ApplicationFiled: March 26, 2010Publication date: September 29, 2011Inventors: Richard M. FLYNN, Michael G. COSTELLO, Michael J. BULINSKI, Daniel R. VITCAK, Phillip E. TUMA
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Patent number: 7888386Abstract: In one aspect, the invention relates to compounds of formula I: where a and R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: July 23, 2009Date of Patent: February 15, 2011Assignee: Theravance, Inc.Inventors: Eric L. Stangeland, Priscilla Van Dyke, Timothy J. Church, Lori Jean Patterson, Daisuke Roland Saito
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Publication number: 20110034461Abstract: The invention relates to novel compounds of formula I where R1, R2, R3, R4, R5, R9, Ar, Q1, Q2 and Q3 are each as defined below. The compounds of the formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of the formula I and to the use thereof as a medicament.Type: ApplicationFiled: August 5, 2010Publication date: February 10, 2011Applicant: sanofi-aventisInventors: Uwe HEINELT, Volkmar WEHNER, Matthias HERRMANN, Karl SCHOENAFINGER, Henning STEINHAGEN
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Publication number: 20100184996Abstract: A process for the formation of 2-(methyloxy)-N-[2-methyl-1-phenyl-2-(1-pyrrolidinyl)propyl]-4,6-bis(trifluoromethyl)benzamide is disclosed, comprising treatment of 2,4-ditrifluoromethyl-6-methoxy-benzoic acid with an arylsulphonyl halide, C1-6alkylsulphonyl halide or di-C1-6alkylphosphoryl chloride, in the presence of a base and an aprotic solvent; followed by reaction with [2-methyl-1-phenyl-2-(1-pyrrolidinyl)propyl]amine or a salt thereof. Also disclosed is a process for the formation of [2-methyl-1-phenyl-2-(1-pyrrolidinyl)propyl]amine comprising: i) treatment of an ?-haloketone with an alcohol in the presence of a base followed by reaction with pyrrolidine; ii) treatment of the product of stage i) with Ar—CH(R5)N H2 wherein R5 is C1-4alkyl and Ar is optionally substituted phenyl, followed by reduction with a sodium borohydride derivative; and iii) reduction of the product of stage ii) with hydrogen and a palladium catalyst.Type: ApplicationFiled: June 18, 2008Publication date: July 22, 2010Applicant: GLAXO GROUP LIMITEDInventors: Alcide Perboni, Nicola Giubellina
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Patent number: 7700587Abstract: Haloperidol analogs that conforms to the structural formulae: wherein: R is H, or —(CH2)n—OH, n is an integer from 0 to 2, and A is a heterocyclic bridging group, consisting essentially of carbon and at least one nitrogen atom, which effectively maintains the distance between the moieties connected thereby such that the compound (1) is incapable of metabolizing to BCPP+ like species, (2) has an affinity for the D2 receptor subtype of 15<D2<250 and (3) functions as a dopamine receptor antagonist, or the structural formulae: wherein: R1 is H, or —(CH2)n—OH, n is an integer from 0 to 2, B is an aza- or diaza-bicyclo group, which effectively maintains the distance between the moieties connected thereby such that the compound is incapable of metabolizing to BCPP+ like species; and Z is —CH— or N; and pharmaceutically acceptable salts, esters, derivatives, metal complexes, conjugates and prodrugs thereof.Type: GrantFiled: September 7, 2004Date of Patent: April 20, 2010Assignee: Florida A&M UniversityInventors: Seth Y. Ablordeppey, Donald M. N. Sikazwe
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Publication number: 20100022616Abstract: In one aspect, the invention relates to compounds of formula I: where a and R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: July 23, 2009Publication date: January 28, 2010Inventors: Eric Stangeland, Priscilla Van Dyke, Timothy J. Church, Lori Jean Patterson, Daisuke Roland Saito
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Publication number: 20090312392Abstract: The present invention provides amino ceramide-like compounds which inhibit glucosyl ceramide (GlyCer) formation by inhibiting the enzyme GlyCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.Type: ApplicationFiled: April 30, 2009Publication date: December 17, 2009Inventors: James A. Shayman, David J. Harris, Craig Siegel, Carol A. Nelson, Diane P. Copeland
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Publication number: 20090292000Abstract: Substituted pyrrolidine compounds are provided, and methods of treatment and pharmaceutical composition that utilize or comprise one or more such compounds. Compounds of the invention are useful for a variety of therapies, including treating or preventing preterm labor, dysmenorrhea, asthma, hypertension, infertility or fertility disorder, undesired blood clotting, preeclampsia or eclampsia, an eosinophil disorder, sexual dysfunction, osteoporosis and other destructive bone disease or disorder, and other diseases and disorders associated with the prostaglandin family of compounds. In a preferred aspect, a substituted pyrrolidine compound is administered to a subject in coordination with a phosphodiesterase inhibitor compound.Type: ApplicationFiled: August 3, 2009Publication date: November 26, 2009Applicant: LABORATOIRES SERONO S.A.Inventors: Yihua Liao, Zhong Zhao, Gian Luca Araldi
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Patent number: 7524880Abstract: The invention provides a crystalline naphthalene-1,5-disulfonic acid salt of 2-[(S)-1-(8-methylaminooctyl)pyrrolidin-3-yl]-2,2-diphenylacetamide or a solvate thereof. This invention also provides pharmaceutical compositions comprising the salt or prepared using the salt; processes and intermediates for preparing the salt; and methods of using the salt to treat a pulmonary disorder.Type: GrantFiled: June 9, 2005Date of Patent: April 28, 2009Assignee: Theravance, Inc.Inventors: Li Li, Robert Chao, Adam Hughes, Yu-Hua Ji, Davar Khossravi, Weijiang Zhang
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Patent number: 7521552Abstract: There is provided a process for the preparation of substituted amino alcohols HO—(CH2)n—NR1R2 from haloalcohols HO—(CH2)n—X, where X is Cl, Br or I, by reaction with an amine HNR1R2, in water as solvent at a temperature range of about 20° C. to about 90° C. optionally in the presence of a catalytic amount of an iodide source metal iodides. The haloalcohols are useful in the preparation of 6-[(substituted)phenyl]-triazolopyrimidine compounds which are useful in the treatment of cancer.Type: GrantFiled: December 8, 2004Date of Patent: April 21, 2009Assignee: WyethInventors: Yanzhong Wu, Arkadiy Rubezhov, Jean Schmid, Jay Thomas Afragola
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Publication number: 20090048454Abstract: Novel intermediates for the production of aminoacetyl pyrrolidine carbonitrile derivatives ensure the safe and efficient production of the compounds. Specifically, the present invention provides a sulfonyloxyacetyl pyrrolidine derivative, represented by the following formula: (Chemical Formula 1) (wherein R1 is a substituted or unsubstituted C1-C6 alkyl group, a substituted or unsubstituted C3-C6 cycloalkyl group, a substituted or unsubstituted arylmethyl group, a substituted or unsubstituted aromatic hydrocarbon, a substituted or unsubstituted aromatic heterocyclic ring or a substituted or unsubstituted aliphatic heterocyclic ring; R2 is CONH2 or CN; and X is CH2, CHF or CF2.Type: ApplicationFiled: February 2, 2007Publication date: February 19, 2009Inventors: Yoshikazu Asahina, Yasumichi Fukuda, Futoshi Shiga
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Patent number: 7468383Abstract: The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly or indirectly with proteasome activity.Type: GrantFiled: February 9, 2006Date of Patent: December 23, 2008Assignee: Cephalon, Inc.Inventors: Raffaella Bernardini, Alberto Bernareggi, Paolo G. Cassara, Germano D'Arasmo, Ernesto Menta, Ambrogio Oliva
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Patent number: 7459472Abstract: This invention provides aryl and heteroaryl compounds of Formula (I) as described herein, and methods of their preparation. Also provided are pharmaceutical compositions made with the compounds of Formula (I) and methods for making such compositions. Compounds of Formula (I) may be useful for treating viral infections including orthopox viruses, either alone or in combination with other therapeutic agents.Type: GrantFiled: August 6, 2004Date of Patent: December 2, 2008Assignee: TransTech Pharma, Inc.Inventors: Adnan M. M. Mjalli, Robert C. Andrews, Murty N. Arimilli, Mohan Rao, Mustafa Guzel, Muralidhar Bondlela, Xiao-Chuan Guo, Guoxiang Huang
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Publication number: 20080262075Abstract: This invention relates to pyrrolidine derivatives, which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. Processes for the preparation of described compounds, pharmaceutical compositions containing the described compounds and the methods for treating the diseases mediated through muscarinic receptors are also provided.Type: ApplicationFiled: August 18, 2005Publication date: October 23, 2008Applicant: RANBAXY LABORATORIES LIMITEDInventors: Mohammad Salman, Pakala Kumara Savithru Sarma, Sandeep Y. Shelke, Anita Chugh, Suman Gupta
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Patent number: 7429586Abstract: Substituted aryloxyalkylamines of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.Type: GrantFiled: June 15, 2006Date of Patent: September 30, 2008Assignee: Ortho-McNeil Pharmaceuticlas, Inc.Inventors: Richard Apodaca, Nicholas I. Carruthers, Curt A. Dvorak, Dale A. Rudolph, Chandravadan R. Shah, Wei Xiao
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Patent number: 7358271Abstract: The present invention relates to pharmaceutical compositions containing sulpiride compounds having the general formula: where R1 is branched or straight chain alkyl having from 1 to about 7 carbon atoms, a substituted or unsubstituted aryl, a substituted or unsubstituted cycloalkyl, a substituted or unsubstituted aralkyl, a substituted or unsubstituted alkylcycloalkyl, or a group having the formula (CH2)n R2 where R2 is a substituted or unsubstituted aryl or a substituted or unsubstituted cycloalkyl, and n is an alkyl group having from 0 to about 6 carbon atoms and pharmaceutically acceptable salts or diluents.Type: GrantFiled: September 4, 2004Date of Patent: April 15, 2008Assignee: Williamsburg Holdings LLCInventor: Donald L. Barbeau
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Patent number: 7335680Abstract: Substituted pyrrolidine compounds are provided, and methods of treatment and pharmaceutical composition that utilize or comprise one or more such compounds. Compounds of the invention are useful for a variety of therapies, including treating or preventing preterm labor, dysmenorrhea, asthma, hypertension, infertility or fertility disorder, undesired blood clotting, preeclampsia or eclampsia, an eosinophil disorder, sexual dysfunction, osteporosis and other destructive bone disease or disorder, and other diseases and disorders associated with the prostaglandin family of compounds. In a preferred aspect, a substituted pyrrolidine compound is administered to a subject in coordination with a phosphodiesterase inhibitor compound.Type: GrantFiled: December 19, 2002Date of Patent: February 26, 2008Assignee: Laboratoires Serono SAInventors: Yihua Liao, Zhong Zhao, Gian Luca Araldi
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Patent number: 7332512Abstract: The present invention relates to novel halonitrobutadienes, to processes for their preparation and to their use for controlling animal pests.Type: GrantFiled: October 23, 2002Date of Patent: February 19, 2008Assignee: Bayer CropScience AGInventors: Reiner Fischer, Peter Jeschke, Angelika Lubos-Erdelen, legal representative, Peter Lösel, Udo Reckmann, Dieter Kaufmann, Viktor Zapolskil, Christoph Erdelen
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Patent number: 7291753Abstract: The invention relates to a process for the reduction of compounds comprising a carbon-carbon (C?C), carbon-oxygen (C?O), or carbon-nitrogen (C?N) double bond, to a corresponding hydrogenated alkane, alcohol or amine, comprising contacting a compound comprising the C?C, C?O or C?N double bond with a hydrogen donor solvent and a catalyst comprising a metal complex having a tridentate aminodiphosphine ligand under transfer hydrogenation conditions.Type: GrantFiled: November 10, 2004Date of Patent: November 6, 2007Inventor: Kamaluddin Abdur-Rashid
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Patent number: 7235580Abstract: The present invention relates to dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention is also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: October 14, 2003Date of Patent: June 26, 2007Assignee: Merck & Co., Inc.Inventors: Michael J. Breslin, Paul J. Coleman, Christopher D. Cox, George D. Hartman, Brenda J. Mariano
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Patent number: 7229803Abstract: The invention relates to methods for reacting (di)amines as substrates in the presence of a lysine oxidase arid a reducing agent, resulting in alcohols, diols or cyclic secondary amines. In a particular embodiment, the invention is directed to methods of preparing cyclic secondary amines suitable for ultimately synthesizing piperidine-2-carboxylic acid and proline derivatives, useful, for example as thrombin inhibitors.Type: GrantFiled: April 8, 2002Date of Patent: June 12, 2007Assignee: BASF AktiengesellschaftInventors: Thomas Friedrich, Norbert Zimmermann, Rainer Stürmer
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Patent number: 7220773Abstract: A novel pyrrole derivative represented by the following formula (1) and a salt thereof: wherein R1 means substituted alkenyl, etc.; R2 means substituted benzoyl, etc.; and R3 to R5 each means hydrogen, alkyl, halogeno, etc. The derivative and salt have antidiabetic activity.Type: GrantFiled: April 17, 2002Date of Patent: May 22, 2007Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Ryu Nagata, Katsunori Maruta, Kiyotaka Iwai, Makoto Kitoh, Kantaro Ushiroda, Kozo Yoshida
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Patent number: 7176229Abstract: Novel pyrrolidine compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.Type: GrantFiled: November 7, 2005Date of Patent: February 13, 2007Assignee: ICOS CorporationInventors: Timothy J. Martins, Kerry W. Fowler, Joshua Odingo, Edward A. Kesicki, Amy Oliver, Laurence Edward Burgess, John Joseph Gaudino, Zachary S. Jones, Bradley J. Newhouse, Stephen T. Schlachter
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Patent number: 7173129Abstract: The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the application.Type: GrantFiled: June 7, 2004Date of Patent: February 6, 2007Assignee: Athero Genics, Inc.Inventors: Kimberly J. Worsencroft, Liming Ni, Zhihong Ye, Charles Q. Meng, M. David Weingarten, Jacob E. Simpson, James A. Sikorski
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Patent number: 7115754Abstract: The present invention relates to novel pyrrolidine derivative of formula (I), its geometrical isomers, its optically active forms as enantiomers, diastereomers, mixtures of these and its racemate forms, as well as salts thereof, wherein R1 is selected from the group comprising or consisting of H and C1–C6-alkyl, for the prevention and/or treatment of preterm labor, premature birth or dysmenorrheaType: GrantFiled: July 4, 2003Date of Patent: October 3, 2006Assignee: Applied Research Systems ARS Holding N.V.Inventors: Catherine Jorand-Lebrun, Jerome Dorbais, Anna Quattropani, Matthias Schwarz, Delphine Valognes
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Patent number: 7078535Abstract: The invention relates to a process for the preparation of 6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-ylacetic acid, in which 5-benzyl-3,3-dimethyl-3,4-dihydro-2H-pyrrole is reacted with ?-bromo-4-chloroacetophenone with formation of 6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizine and the acetic acid group is introduced into the 5-position, 5-benzyl-3,3-dimethyl-3,4-dihydro-2H-pyrrole being obtained by hydrogenation of 2,2-dimethyl-4-oxo-5-phenylvaleronitrile or a ketal thereof. The invention also relates to processes for the preparation of intermediates occurring in the above process.Type: GrantFiled: August 21, 2002Date of Patent: July 18, 2006Assignee: Merckle GmbHInventors: Gerd Dannhardt, Thomas Kammermeier, Philipp Merckle, Hans-Günter Striegel, Stefan Laufer
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Patent number: 6995284Abstract: The present invention relates to a synthetic process for the preparation of a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor.Type: GrantFiled: October 22, 2002Date of Patent: February 7, 2006Assignee: The University of Tennessee Research FoundationInventors: James T. Dalton, Duane D. Miller, Yali He, Donghua Yin
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Patent number: 6965038Abstract: The present invention discloses an acylated derivative of an aminothiol compound having a general formula II wherein R1-R4 and R6 are substitutable ligands. Such compounds can perform as superior catalysts in asymmetric addition reactions of organic zinc and aldehyde. According to the present invention, only less than 0.02% of the acylated derivative is needed to obtain high enantioselectivity over 99% enantiomeric excess.Type: GrantFiled: August 26, 2003Date of Patent: November 15, 2005Assignee: National Chung-Hsing UniversityInventors: Teng-Kuei Yang, Nan-Kuang Chen, To Liu
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Patent number: 6864270Abstract: Composition, article of manufacture for and method of treating malaria in a human having an infestation of Plasmodium protozoans are described. The method comprises administering a therapeutically-effective amount of a compound of formula (I) or (IV), i.e. sufficient quantity to reduce the population of Plasmodium. The composition of the invention is a compound of formula (I) or (IV) with a pharmaceutical excipient. The article of manufacture is the composition in combination with labeling for treating malaria. The substituents are detailed in the specification.Type: GrantFiled: August 8, 2002Date of Patent: March 8, 2005Assignee: University of Florida Research Foundation, Inc.Inventor: Raymond J. Bergeron, Jr.
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Publication number: 20040266822Abstract: The present invention provides amine derivatives represented by formula I, its isomers, racemes or optical isomers, pharmaceutical salts thereof, its amides or esters, pharmaceutical compositions containing said compounds and the preparation methods thereof. The invention also relates to the use of the above mentioned compounds in the preparation of drugs for the prophylaxis or treatment of cardiovascular diseases, diabetes, bronchial and urinary smooth muscle spasm as well as ischemic and anoxic nerve injury. The above compounds can be used to treat hypertension, angina diaphragmatic, myocardial infarction, congestive heart failure, arrhythmia, diabetes, spasmodic bronchial diseases, spasmodic bladder or ureter diseases, and depression.Type: ApplicationFiled: August 12, 2004Publication date: December 30, 2004Inventors: Hai Wang, Liuhong Yun, Huasong Feng, Fulin Li, Xingehun Tang, Huamei He, Rifang Yang, Wenyu Cui, Qixiu Gao, Gang Hu, Rusheng Zhao, Wei Liu, Chaoliang Long, Lin Wang, Xinqiang Lu, Lijun Liu, Yuan Yan
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Publication number: 20040266008Abstract: This invention relates to a novel class of linear polyene polyketides, their pharmaceutically acceptable salts and derivatives, and to methods for their production. The compounds may be obtained by cultivation of Streptomyces melanosporafaciens species and isolation of the polyene polyketide, followed by optional chemical production of the isolated polyene polyketide. The compounds may also be produced by other known bacteria. The invention further includes the use of these compounds as inhibitors of fungal cell growth and inhibitors of cancer cell growth. Finally, the invention encompasses pharmaceutical compositions comprising these novel polyketide compounds, or their pharmaceutically acceptable salts or derivatives thereof.Type: ApplicationFiled: May 13, 2004Publication date: December 30, 2004Applicant: Ecopia BioSciences, Inc.Inventors: Brian O. Bachmann, James B. McAlpine, Emmanuel Zazopoulos, Chris M. Farnet
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Publication number: 20040267022Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: ApplicationFiled: January 2, 2004Publication date: December 30, 2004Applicant: G. D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
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Publication number: 20040266698Abstract: Compounds of the formula (I), wherein R1, R1-R7 and alk have meaning as defined, pharmaceutical compositions thereof, and use thereof for the treatment and/or prevention of cardiovascular disorders responsive to ACE and NEP inhibition and/or ECE inhibition.Type: ApplicationFiled: February 24, 2004Publication date: December 30, 2004Inventor: Cynthia Anne Fink
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Publication number: 20040259868Abstract: Compounds of formula (I) 1Type: ApplicationFiled: July 6, 2004Publication date: December 23, 2004Inventors: John Walter Liebeschuetz, Christopher William Murray, Stephen Clinton Young, Nicholas Paul Camp, Stuart Donald Jones, William Alexander Wylie, John Joseph Masters, Michael Robert Wiley, Scott Martin Sheehan, David Birenbaum Engel, Brian Morgan Watson
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Patent number: RE39558Abstract: Compounds of this formula are useful for treating or preventing, obesity, breast cancer, osteoporosis, endometriosis, cardiovascular disease and prostatic disease.Type: GrantFiled: December 23, 2004Date of Patent: April 10, 2007Assignee: Pfizer Inc.Inventors: Kimberly O. Cameron, Paul A. DaSilva Jardine, Robert L. Rosati
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Patent number: RE40525Abstract: A racemate diastereoisomer and optical isomer of a compound of formula (I): wherein B is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of which may be optionally substituted with C1-6 alkyl; C1-6 alkoxy; C1-6 alkanoyl; hydroxy; hydroxyalkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with C1-6 alkyl; amido; or (lower alkyl)amide; or B is an acyl derivative of formula R4—C(O)—; a carboxyl derivative of formula R4—O—C(O)—; an amide derivative of formula R4—N(R5)—C(O)—; a thioamide derivative of formula R4—N(R5)—C(S)—; or a sulfonyl of formula R4—SO2; R5 is H or C1-6 alkyl; and Y is H or C1-6 alkyl; R3 is C1-8 alkyl, C3-7 cycloalkyl, or C4-10 alkylcycloalkyl, all optionally substituted with hydroxy, C1-6 alkoxy, C1-6 thioalkyl, amido, (lower alkyl)amido, C6 or C10 aryl, or C7-16 aralkyl; R2 is C2—R20, NH—R20, O—R20 or S—R20, wherein R20 is a saturated or unsaturated C3-7 cycloalkyl or C4-10 (alkylcycloalkyl), all of which being optionally mono-, di- or tri-Type: GrantFiled: September 30, 2005Date of Patent: September 30, 2008Assignee: Boehringer Ingelheim (Canada) Ltd.Inventors: Montse Llinas-Brunet, Murray D. Bailey, Dale R. Cameron, Anne-Marie Faucher, Elise Ghiro, Nathalie Goudreau, Teddy Halmos, Marc-André Poupart, Jean Rancourt, Youla S. Tsantrizos, Dominik M. Wernic