Ureido, Guanido, Or Hydrazine Patents (Class 562/439)
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Patent number: 8487129Abstract: Compounds of Formula (Ia) wherein R is a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl, a C1-C6 substituted or unsubstituted alkyl or —NR?R?, Q is C(O), O, NR?, S, S(O)2, C(O)2 (CH2)p Y is C(O), O, NR?, S, S(O)2, C(O)2 (CH2)p Z is H or C1-C4 alkyl, R? is H, C(O), S(O)2, C(O)2, a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl or a C1-C6 substituted or unsubstituted alkyl, when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C6-C12 heteroaryl, —NR?R? or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition. Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage.Type: GrantFiled: November 11, 2011Date of Patent: July 16, 2013Assignee: Molecular Insight Pharmaceuticals, Inc.Inventors: John W. Babich, Craig N. Zimmerman, Kevin P. Maresca
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Publication number: 20130116324Abstract: The present invention relates to the novel use (anti-inflammatory activity) of Ramalin isolated from the Antarctic lichen Ramalina terebrata, and more specifically to a pharmaceutical composition containing Ramalin as an active ingredient. Ramalin of the invention is a compound derived from natural material, has no toxicity or side effects, and inhibits the expression of inducible nitric oxide synthase (iNOS) in the transcription stage to significantly inhibit the production of nitric oxide (NO) that is a key mediator of inflammatory responses. In addition, it inhibits the activation of the inflammatory mediator NF-?B, inhibits p38 MAPK, ERK1/2 and JNK signaling pathways, and inhibits the expression of the LPS receptor TLR4, suggesting that Ramalin has an excellent anti-inflammatory effect. Thus, the composition containing Ramalin can be effectively used to fundamentally treat or prevent inflammatory diseases or immune diseases and to relieve or alleviate the symptoms of the diseases.Type: ApplicationFiled: June 2, 2011Publication date: May 9, 2013Applicant: KOREA OCEAN RESEARCH AND DEVELOPMENT INSTITUTEInventors: Joung Han Yim, Il Chan Kim, Sung Gu Lee, Doc Kyu Kim, Se Jong Han, Hyoung Seok Lee, Sung Jin Kim, Tai Kyoung Kim, Pil-Sung Kang, Heeyong Park, Ha Ju Park, Suhkneung Pyo
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Publication number: 20130109866Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.Type: ApplicationFiled: October 23, 2012Publication date: May 2, 2013Applicant: ALLERGAN, INC.Inventor: ALLERGAN, INC.
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Patent number: 8357819Abstract: The invention relates to a process for the synthesis of (Z)-3-[2-butoxy-3?-(3-heptyl-1-methylureido)biphenyl-4-yl]-2-methoxyacrylic acid of formula (I): and also to the process for the synthesis of the reaction intermediates of general formula (XII), and to the said compounds when R2 is chosen from the methyl, trifluoromethyl, phenyl and 4-tolyl radicals:Type: GrantFiled: April 18, 2008Date of Patent: January 22, 2013Assignee: Galderma Research & DevelopmentInventor: Jean-Guy Boiteau
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Publication number: 20120329724Abstract: The present invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as opioid agonists.Type: ApplicationFiled: September 7, 2012Publication date: December 27, 2012Inventors: Christopher Gordon Barber, Dafydd Rhys Owen, Lisa Rosemary Thompson
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Publication number: 20120329716Abstract: The instant invention relates to peptides obtained from the enzymatic hydrolysis of yellow pea seed proteins that are capable of lowering the blood pressure and reducing the effects of kidney disease in a subject b\ inhibiting or reducing the affinity of the enzymes in the renin-angiotensin system for their substrates, specifically renin, to compositions comprising said peptides and to uses thereof.Type: ApplicationFiled: October 28, 2010Publication date: December 27, 2012Inventors: Rotimi Aluko, Jianping Wu, Harold Aukema
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Patent number: 8318208Abstract: The present disclosure generally relates to nanoparticles having about 0.2 to about 35 weight percent of a therapeutic agent; and about 10 to about 99 weight percent of biocompatible polymer such as a diblock poly(lactic) acid-poly(ethylene)glycol. Other aspects of the invention include methods of making such nanoparticles.Type: GrantFiled: July 19, 2012Date of Patent: November 27, 2012Assignee: Bind Biosciences, Inc.Inventors: Stephen E. Zale, Greg Troiano, Mir Mukkaram Ali, Jeff Hrkach, James Wright
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Publication number: 20120289554Abstract: This invention relates to novel 4-dimethylaminobutyric acid derivatives of the formula wherein A1, A2, R1, m and n are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds inhibit carnitine palmitoyl transferase (CPT) activity, in particular CPT2 activity, and can be used as medicaments in methods for the treatment of diseases modulated by CPT2 inhibitors.Type: ApplicationFiled: July 24, 2012Publication date: November 15, 2012Inventors: Mirjana Andjelkovic, Simona M. Ceccarelli, Odile Chomienne, Gerald Lewis Kaplan, Patrizio Mattei, Jefferson Wright Tilley
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Publication number: 20120277223Abstract: The present invention relates to compounds of formula (I): wherein Q, G1, G2, and G3, are defined herein. Pharmaceutical compositions and methods for treating DGAT-1 related diseases or conditions are also disclosed.Type: ApplicationFiled: July 16, 2012Publication date: November 1, 2012Inventors: Andrew S. Judd, Mathew M. Mulhern, Rajesh R. lyengar, Philip R. Kym, Andrew J. Souers
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Publication number: 20120269864Abstract: The present invention is a compound of formula (I) or formula (II) which are suitable as NP-1 antagonists.Type: ApplicationFiled: June 11, 2012Publication date: October 25, 2012Inventors: Haiyan Jia, Ian ZACHARY, Michelle TICKNER, Lili CHENG, Chris CHAPMAN, Katie ELLARD, Basil HARTZOULAKIS, Ashley JARVIS, Rosemary LYNCH, Jamie NALLY, David SELWOOD, Mark STEWART
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Patent number: 8273363Abstract: The present invention generally relates to polymers and macromolecules, in particular, to polymers useful in particles such as nanoparticles. One aspect of the invention is directed to a method of developing nanoparticles with desired properties. In one set of embodiments, the method includes producing libraries of nanoparticles having highly controlled properties, which can be formed by mixing together two or more macromolecules in different ratios. One or more of the macromolecules may be a polymeric conjugate of a moiety to a biocompatible polymer. In some cases, the nanoparticle may contain a drug. Other aspects of the invention are directed to methods using nanoparticle libraries.Type: GrantFiled: May 17, 2011Date of Patent: September 25, 2012Assignee: Bind Biosciences, Inc.Inventors: Stephen E. Zale, Mir Mukkaram Ali
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Publication number: 20120232120Abstract: A compound of the formula: where X is phenyl substituted at the 3, 4 and 5 positions with R1, R2 or R3 which are selected from hydrogen, chloro, lower alkyl of 1 to 5 carbons, phenoxy, phenyl, naphthyl, or phenyl (lower) alkyl where the lower alkyl group has 1-5 carbon atoms and m is 0 or 1; Y is —CONH— or —NHCONH— where the nitrogen atoms are unsubstituted or substituted with other phenoxyisobutyric acid derivatives, or the residue of a phenoxyisobutyric acid and n is 0 or 1; Z is unsubstituted phenyl when m is 1 and n is 1; when Y is 0, X is 0; Z is also substituted.Type: ApplicationFiled: March 8, 2012Publication date: September 13, 2012Inventors: IRAJ LALEZARI, JILL FABRICANT
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Patent number: 8246968Abstract: The present invention generally relates to polymers and macromolecules, in particular, to polymers useful in particles such as nanoparticles. One aspect of the invention is directed to a method of developing nanoparticles with desired properties. In one set of embodiments, the method includes producing libraries of nanoparticles having highly controlled properties, which can be formed by mixing together two or more macromolecules in different ratios. One or more of the macromolecules may be a polymeric conjugate of a moiety to a biocompatible polymer. In some cases, the nanoparticle may contain a drug. Other aspects of the invention are directed to methods using nanoparticle libraries.Type: GrantFiled: March 31, 2008Date of Patent: August 21, 2012Assignee: Bind Biosciences, Inc.Inventors: Stephen E. Zale, Mir Mukkaram Ali
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Publication number: 20120208988Abstract: Compounds of Formula (Ia) wherein R is a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl, a C1-C6 substituted or unsubstituted alkyl or —NR?R?, Q is C(O), O, NR?, S, S(O)2, C(O)2 (CH2)p Y is C(O), O, NR?, S, S(O)2, C(O)2 (CH2)p Z is H or C1-C4 alkyl, R? is H, C(O), S(O)2, C(O)2, a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl or a C1-C6 substituted or unsubstituted alkyl, when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C6-C12 heteroaryl, —NR?R? or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition. Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage.Type: ApplicationFiled: November 11, 2011Publication date: August 16, 2012Applicant: MOLECULAR INSIGHTS PHARMACEUTICALS, INC.Inventors: John W. Babich, Craig N. Zimmerman, Kevin P. Maresca
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Patent number: 8242145Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the antagonists of PGD2 receptors described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: GrantFiled: February 12, 2009Date of Patent: August 14, 2012Assignee: Panmira Pharmaceuticals, LLCInventors: John Howard Hutchinson, Thomas Jonathan Seiders, Brian Andrew Stearns, Bowei Wang, Yen Pham Truong, Jeannie M. Arruda
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Patent number: 8236330Abstract: The present invention generally relates to polymers and macromolecules, in particular, to polymers useful in particles such as nanoparticles. One aspect of the invention is directed to a method of developing nanoparticles with desired properties. In one set of embodiments, the method includes producing libraries of nanoparticles having highly controlled properties, which can be formed by mixing together two or more macromolecules in different ratios. One or more of the macromolecules may be a polymeric conjugate of a moiety to a biocompatible polymer. In some cases, the nanoparticle may contain a drug. Other aspects of the invention are directed to methods using nanoparticle libraries.Type: GrantFiled: May 17, 2011Date of Patent: August 7, 2012Assignee: Bind Biosciences, Inc.Inventors: Stephen E. Zale, Mir Mukkaram Ali
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Publication number: 20120178666Abstract: Prodrugs of guanfacine with amino acids or short peptides, pharmaceutical compositions containing such prodrugs and a method for providing therapeutic benefit in the treatment of ADHD/ODD (attention deficient hyperactivity disorder and oppositional defiance disorder) with guanfacine prodrugs are provided herein. Additionally, methods for minimizing or avoiding the adverse gastrointestinal side effects associated with guanfacine administration, as well as improving the pharmacokinetics of guanfacine are provided herein.Type: ApplicationFiled: September 15, 2010Publication date: July 12, 2012Applicant: SHIRE LLCInventors: Richard Franklin, Robert G. Tyson, Bernard T. Golding, Rhys Whomsley
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Patent number: 8206747Abstract: The present disclosure generally relates to nanoparticles having about 0.2 to about 35 weight percent of a therapeutic agent; and about 10 to about 99 weight percent of biocompatible polymer such as a diblock poly(lactic) acid-poly(ethylene)glycol. Other aspects of the invention include methods of making such nanoparticles.Type: GrantFiled: June 16, 2009Date of Patent: June 26, 2012Assignee: BIND Biosciences, Inc.Inventors: Stephen E. Zale, Greg Troiano, Mir Mukkaram Ali, Jeff Hrkach, James Wright
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Patent number: 8207373Abstract: HPV inhibitors with formula (I) where G1 represents a hydrocarbonated bond or chain possibly substituted by one or two alkyl groups, G2 represents a group (see formula Ia+Ib) or R represents a hydrogen, an alkyl, halogenoalkyl, or a prodrug radical such as carbamate, acetyl or dialkylaminomethyl, G represents a bond or a hydrocarbonated chain possibly substituted by one or two alkyls, W represents an oxygen or sulphur, R1 and R2 each represent a group chosen from among hydrogen, halogen, hydroxyl, thio, alkoxy, halogenoalkoxy, alkylthio, halogenoalkylthio, amino, monoalkylamino, dialkylamino, cycloalkyl, alkyl or halogenoalkyl, R3 represents an acid or a prodrug radical of the acid function or a bioisostere of the acid function, A represents an aryl, cycloalkyl, cycloalkenyl or a heterocycle, each possibly substituted, and B represents an aryl or a heterocycle with 6 chains, each possibly substituted, and pharmaceutically acceptable salts.Type: GrantFiled: May 18, 2007Date of Patent: June 26, 2012Assignee: Anaconda PharmaInventors: Marta Blumenfeld, Delphine Compere, Jean-Michel Gauthier
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Publication number: 20120122862Abstract: The present invention is a compound of formula (I) or formula (II) which are suitable as NP-1 antagonists.Type: ApplicationFiled: January 30, 2012Publication date: May 17, 2012Inventors: Haiyan Jia, Ian Zachary, Michelle Tickner, Lili Cheng, Chris Chapman, Katie Ellard, Basil Hartzoulakis, Ashley Jarvis, Rosemary Lynch, Jamie Nally, David Selwood, Mark Stewart
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Publication number: 20120101157Abstract: Disclosed are 4,5-diamino-3-halo-2-hydroxybenzoic acid derivatives and manufactures thereof. The 4,5-diamino-3-halo-2-hydroxybenzoic acid derivatives are presented by formula (I): wherein R1 group is H, CH3, or C2H5; R2 group is H, or Br; R3 group is CH3, or C3H7; and R4 group is H, or C(?NH)—NH2. 4,5-diamino-3-halo-2-hydroxybenzoic acid derivatives provided here were non-toxic to MDCK cells, particularly compounds 6a, 6b, 6c, 6e, 6f, 7a, 7b and 8 had better anti-H1N1 activity. In the future, these compounds can be used to focus on viral neuraminidases as targets to develop effective anti-influenza drugs.Type: ApplicationFiled: October 24, 2011Publication date: April 26, 2012Applicant: NATIONAL DEFENSE MEDICAL CENTERInventors: AN-RONG LEE, WEN-HSIN HUANG, CHI-HONG CHU, WEN-LIANG CHANG, CHEN-WEN YAO, I-LING CHEN
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Publication number: 20120088300Abstract: Certain embodiments disclosed herein are directed to a method of producing endoderm cells, such as definitive endoderm cells by exposing stem cells such as embryonic stem cells or induced pluripotent stem (iPS) cells to an effective amount of at least one compound described herein to differentiate the stem cells into the endoderm cells such as definitive endoderm cells. Differentated endoderm cells produced by the methods disclosed herein can be differentiated into pancreatic epithelium, and other endoderm derivatives such as thymus, liver, stomach, intestine and lung. Another aspect of the present invention relates to a method of producing pancreatic progenitor cells, such as Pdx1-positive pancreatic progenitor cells by exposing endoderm cells, such as definitive endoderm cells to an effective amount of at least one compound described herein to differentiate the definitive endoderm cells into Pdx1-positive pancreatic progenitor cells.Type: ApplicationFiled: February 5, 2010Publication date: April 12, 2012Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGEInventors: Douglas A. Melton, Malgorzata Borowiak, Rene Maehr, Shuibing Chen, Weiping Tang, Julia L. Fox, Stuart L. Schreiber
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Publication number: 20120077876Abstract: This invention relates to a prodrug comprising a partial structure having the general formula (I) or (II), where R1 and R2 are hydrogen, alkyl, or aryl radicals.Type: ApplicationFiled: January 8, 2010Publication date: March 29, 2012Applicant: Dritte Patentportfolio Beteiligungsgesellschaft Mbh & Co. KGInventors: Bernd Clement, Dennis Schade
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Publication number: 20120059055Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions that include the compounds described herein, and methods of using such antagonists of PGD2 receptors, alone or in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: ApplicationFiled: November 15, 2011Publication date: March 8, 2012Applicant: PANMIRA PHARMACEUTICALS, LLCInventors: John Howard HUTCHINSON, Brian Andrew Stearns, Jill Melissa Scott, Yen Pham Truong, Jeffrey Roger Roppe, Nicholas Simon Stock, Jeannie M. Arruda, Thomas Jon Seiders, Bowei Wang
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Patent number: 8114857Abstract: The present invention provides new derivatives of 4- or 5-aminosalicylic acid, and a pharmaceutical composition containing these derivatives of 4- or 5-aminosalicylic acid as active ingredients, useful for the treatment of intestinal diseases such as inflammatory bowel disease (IBD) and irritable bowel syndrome (IBS) and for the prevention/treatment of colon cancer. More particularly, these derivatives comprise a hydrogen sulfide releasing moiety linked via an azo, an ester, an anhydride, a thioester or an amide linkage to a molecule of 4- or 5-aminosalicylic acid. Furthermore, the present invention provides a process for preparing these compounds and their use for treating IBD and IBS and the prevention/treatment of colon cancer.Type: GrantFiled: December 29, 2010Date of Patent: February 14, 2012Assignee: Antibe Therapeutics Inc.Inventors: John L. Wallace, Giuseppe Cirino, Giuseppe Caliendo, Anna Sparatore, Vicenzo Santagada, Stefano Fiorucci
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Publication number: 20120028985Abstract: The present invention relates to the treatment and prevention of immunological and inflammatory disorders with a compound of formula (I) in combination with methotrexate,Type: ApplicationFiled: November 6, 2009Publication date: February 2, 2012Applicant: 4SC AGInventors: Manfred Gröppel, Johann Leban
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Publication number: 20110294741Abstract: The present invention relates to derivatives of L-Tyrosyl-L-Arginine and the use of said derivatives in the prevention and/or treatment of a tau-induced cytotoxicity.Type: ApplicationFiled: April 1, 2009Publication date: December 1, 2011Applicant: Bioalvo-Servicos, Investigacao e Desenvolvimento em Biotecnologia S.A.Inventors: Alexandra Maria Barros Dos Santos, Catia Santana Reverendo Rodrigues, Christophe Francois Aime Roca, Helena Margarida Moreira de Oliveira Vieira, Jose Manuel Bernardo de Sousa, Marta Isabel Heitor Cerejo, Patricia Ramalhete Mendes da Silva Calado, Ricardo Filipe Antunes Pinheiro, Sukalyan Chatterjee, Marta Maria Batista Ribeiro, Miguel Augusto Rico Botas Castanho, Eduard Bardaji Rodriguez, Montserrat Heras Corominas, Isaura Ferreira Tavares, Marta Sofia Carvalho Teixeira Pinto
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Patent number: 8067445Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein that are antagonists of PGD2 receptors. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: GrantFiled: January 29, 2009Date of Patent: November 29, 2011Assignee: Panmira Pharmaceuticals, LLCInventors: John Howard Hutchinson, Brian Andrew Stearns, Jill Melissa Scott, Yen Pham Truong, Jeffrey Roger Roppe, Nicholas Simon Stock, Jeannie M. Arruda, Thomas Jon Seiders, Bowei Wang, Deborah Volkots
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Patent number: 8058449Abstract: Compounds of Formula (Ia) wherein R is a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl, a C1-C6 substituted or unsubstituted alkyl or —NR?R?, Q is C(O), O, NR?, S, S(O)2, C(O)2 (CH2)p Y is C(O), O, NR?, S, S(O)2, C(O)2 (CH2)p Z is H or C1-C4 alkyl, R? is H, C(O), S(O)2, C(O)2, a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl or a C1-C6 substituted or unsubstituted alkyl, when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C6-C12 heteroaryl, —NR?R? or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition. Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage.Type: GrantFiled: November 7, 2007Date of Patent: November 15, 2011Assignee: Molecular Insight Pharmaceuticals, Inc.Inventors: John W. Babich, Craig N. Zimmerman, Kevin P. Maresca
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Publication number: 20110251216Abstract: The present invention relates to therapeutic targets for cancer. In particular, the present invention relates to small molecules and nucleic acids that target EZH2 expression in cancer (e.g., prostate cancer, breast cancer, other solid tumors, multiple myeloma).Type: ApplicationFiled: February 10, 2011Publication date: October 13, 2011Applicant: The Regents of The University of MichiganInventors: Arul M. Chinnaiyan, Sooryanaryana Lnu, Qi Cao
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Publication number: 20110207654Abstract: The present invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as opioid agonists.Type: ApplicationFiled: February 24, 2011Publication date: August 25, 2011Inventors: Christopher Gordon Barber, Dafydd Rhys Owen, Lisa Rosemary Thompson
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Patent number: 7973063Abstract: Novel biaromatic compounds having the following structural formula (I): are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine, in particular in dermatology as well as in the fields of cardiovascular diseases, immune diseases and/or diseases related to the metabolism of lipids, or, alternatively, into cosmetic compositions.Type: GrantFiled: October 9, 2009Date of Patent: July 5, 2011Assignee: Galderma Research & DevelopmentInventors: Jerome Aubert, Laurence Clary, Pascale Mauvais, Michel Rivier, Etienne Thoreau, Jean-Guy Boiteau
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Publication number: 20110130391Abstract: The invention encompasses ureido substituted benzoic acid compounds, compositions comprising the compounds and methods for treating or preventing diseases associated with nonsense mutations of mRNA by administering these compounds or compositions.Type: ApplicationFiled: December 29, 2010Publication date: June 2, 2011Inventors: Richard G. Wilde, James J. Takasugi, Seongwoo Hwang, Ellen M. Welch, Guangming Chen
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Publication number: 20110098322Abstract: The present invention provides compounds that can inhibit the activity of soluble epoxide hydrolases. In particular, the present invention provides compounds of Formula I.Type: ApplicationFiled: August 5, 2008Publication date: April 28, 2011Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: James R. Sanborn, Bruce D. Hammock, Sung Hee Hwang, Paul D. Jones, Christophe Morisseau
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Publication number: 20110098352Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions that include the compounds described herein, and methods of using such antagonists of PGD2 receptors, alone or in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: ApplicationFiled: January 29, 2009Publication date: April 28, 2011Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: John Howard Hutchinson, Brian Andrew Stearns, Jill Melissa Scott, Yen Pham Truong, Jeffrey Roger Roppe, Nicholas Simon Stock, Jeannie M. Arruda, Thomas Jon Seiders, Bowei Wang
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Publication number: 20110082109Abstract: The present invention provides a pharmaceutical which possesses an excellent inhibitory effect on NHE3 (Na+/H+ exchanger type 3) and effectively improves diseases or conditions of organs in which NHE3 is expressed.Type: ApplicationFiled: October 1, 2010Publication date: April 7, 2011Applicant: AJINOMOTO CO., INC.Inventors: Wataru MIYANAGA, Yoichiro Shima, Misato Noguchi, Akiko Oonuki, Yayoi Kawato, Hiroshi Iwata, Eri Harada, Ryuta Takashita, Hirokazu Ueno, Tadakiyo Nakagawa
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Publication number: 20110065796Abstract: Prodrugs of guanfacine with amino acids or short peptides, pharmaceutical compositions containing such prodrugs and a method for providing therapeutic benefit in the treatment of ADHD/ODD (attention deficient hyperactivity disorder and oppositional defiance disorder) with guanfacine prodrugs are provided herein. Additionally, methods for minimizing or avoiding the adverse gastrointestinal side effects associated with guanfacine administration, as well as improving the pharmacokinetics of guanfacine are provided herein.Type: ApplicationFiled: September 15, 2010Publication date: March 17, 2011Applicant: SHIRE LLCInventors: Rhys Whomsley, Richard Franklin, Bernard T. Golding, Robert G. Tyson
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MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
Publication number: 20110053958Abstract: The present invention relates to amide derivatives of Formula (XIIIa) and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.Type: ApplicationFiled: March 17, 2009Publication date: March 3, 2011Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Thuy-Anh Tran, Weichao Chen, Bryan A. Kramer, Abu J.M. Sadeque, Anna Shifrina, Young-Jun Shin, Pureza Vallar, Ning Zou -
Publication number: 20110034558Abstract: Described herein is the DP2 antagonist [2?-(3-benzyl-1-ethyl-ureidomethyl)-6-methoxy-4?-trifluoromethyl-biphenyl-3-yl]-acetic acid, or a pharmaceutically acceptable salt thereof. Also described are methods of preparing the DP2 antagonist, or a pharmaceutically acceptable salt thereof. Also described herein are pharmaceutical compositions suitable for administration to a mammal that include the DP2 antagonist, or a pharmaceutically acceptable salt thereof, and methods of using such pharmaceutical compositions for treating respiratory diseases or conditions, allergic diseases or conditions, inflammatory diseases or conditions, as well as other prostaglandin D2-dependent or prostaglandin D2-mediated diseases or conditions.Type: ApplicationFiled: July 29, 2010Publication date: February 10, 2011Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: Jason Edward BRITTAIN, Brian Andrew STEARNS, Christopher David KING, Kevin Ross HOLME
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Patent number: 7879827Abstract: The present invention provides new derivatives of 4- or 5-aminosalicylic acid, and a pharmaceutical composition containing these derivatives of 4- or 5-aminosalicylic acid as active ingredients, useful for the treatment of intestinal diseases such as inflammatory bowel disease (IBD) and irritable bowel syndrome (IBS) and for the prevention/treatment of colon cancer. More particularly, these derivatives comprise a hydrogen sulfide releasing moiety linked via an azo, an ester, an anhydride, a thioester or an amide linkage to a molecule of 4- or 5-aminosalicylic acid. Furthermore, the present invention provides a process for preparing these compounds and their use for treating IBD and IBS and the prevention/treatment of colon cancer.Type: GrantFiled: February 10, 2009Date of Patent: February 1, 2011Assignee: Antibe Therapeutics Inc.Inventors: John L. Wallace, Giuseppe Cirino, Giuseppe Caliendo, Anna Sparatore, Vincenzo Santagada, Stefano Fiorucci
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Publication number: 20110008253Abstract: A manufacturing process for the preparation of radiolabeled compounds of formula (I) includes reacting compounds of formula (II) with a source of readionuclide of a halogen in the presence of an oxidant under acidic condition, wherein: *I is 123I, 124I, 125I or 131I; R is lower alkyl, optionally substituted with one or more fluorine atoms; Q is C(O), O, NR?, S, S(O)2, C(O)2, (CH2)p; Y is C(O), O, NR?, S, S(O)2, C(O)2, (CH2)p; R? is H, C(O), S(O)2, C(O)2; Z is H, C1-C4 alkyl, benzyl, substituted benzyl or trialkylsilyl; m is 0, 1, 2, 3, 4 or 5; n is 0, 1, 2, 3, 4, 5 or 6; and p is 0, 1, 2, 3, 4, 5 or 6.Type: ApplicationFiled: June 15, 2010Publication date: January 13, 2011Inventors: John W. Babich, Craig Zimmerman, Kevin P. Maresca
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Patent number: 7863332Abstract: Novel biaromatic compounds having the general formula (I): and cosmetic/pharmaceutical compositions comprised thereof are useful in human or veterinary medicine (in dermatology and also in the fields of cardiovascular diseases, of immune diseases and/or of diseases related to the metabolism of lipids) or, alternatively, in cosmetic compositions.Type: GrantFiled: February 16, 2007Date of Patent: January 4, 2011Assignee: Galderma Research & DevelopmentInventors: Laurence Clary, Jean-Guy Boiteau, Corinne Millois Barbuis
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Publication number: 20100305207Abstract: This invention relates to a novel compound which is a glycogen phosphorylase inhibitor and its use in the treatment of diabetes and other conditions associated therewith. The invention further relates to a pharmaceutical composition containing the compound and to processes for preparing the compound and pharmaceutical composition.Type: ApplicationFiled: September 25, 2008Publication date: December 2, 2010Inventors: Pierette Banker, Eric Eugene Boros, Scott Howard Dickerson, Istvan Kaldor, Cecilia S. Koble, Michael Tolar Martin, Steven Meagher Sparks, Stephen Andrew Thomson
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Publication number: 20100298429Abstract: Disclosed herein are compositions that include for example the arginine salt of carbidopa, and methods for treating neurological or movement diseases or disorders such as restless leg syndrome, Parkinson's disease, secondary parkinsonism, Huntington's disease, Parkinson's like syndrome, PSP, MSA, ALS, Shy-Drager syndrome and conditions resulting from brain injury including carbon monoxide or manganese intoxication, using substantially continuous administration of carbidopa or salt thereof together with administration of levodopa.Type: ApplicationFiled: July 14, 2010Publication date: November 25, 2010Inventors: Oron Yacoby-Zeevi, Mara Nemas
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Publication number: 20100286430Abstract: The invention relates to a process for the synthesis of (Z)-3-[2-butoxy-3?-(3-heptyl-1-methylureido)biphenyl-4-yl]-2-methoxyacrylic acid of formula (I): and also to the process for the synthesis of the reaction intermediates of general formula (XII), and to the said compounds when R2 is chosen from the methyl, trifluoromethyl, phenyl and 4-tolyl radicals:Type: ApplicationFiled: April 18, 2008Publication date: November 11, 2010Applicant: GALDERMA RESEARCH & DEVELOPMENTInventor: Jean-Guy Boiteau
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Patent number: 7750049Abstract: The invention relates to compounds of formula (I) in which R is selected from halogen, alkyl, alkoxy, aryl and heteroaryl; R1 is selected from 2-hydroxyethyl, 2,3-dihydroxypropyl, 3-hydroxypropyl, 2,2-dihydroxyethyl, 3,3-dihydroxypropyl, 1,3-dioxolane-ethyl, 1,3-dioxane-methyl, 1,3-dioxolane-methyl, 1,3-dioxane-ethyl, 3-fluoro-2-hydroxypropyl, 3-carboxy-2-hydroxy-propyl, 3-chloro-2-hydroxypropyl, 2-hydroxypropyl, 2-hydroxy-propen-2-yl, morpholinoethyl, piperazinoethyl, hydroxymethyl, benzyl, 4-(hydroxymethyl)benzyl, 4-chlorobenzyl, 4-fluorobenzyl, and 4-hydroxybenzyl. R2 is te/t-butyl or trifluoromethyl; R3 is independently selected from hydrogen, carboxy, cyano, alkyl or hydroxyalkyl, The compounds of formula (I) can be used for the preparation of pharmaceutical compositions for the therapy of inflammatory states, such as chronic neuropathic pain, over-active bladder syndrome, tumor pain, hemorrhoids, inflammatory hyperalgesia, post-intervention pain, dental extraction, airway and gastro-intestinal diseases.Type: GrantFiled: December 6, 2007Date of Patent: July 6, 2010Assignee: Pharmeste S.R.L.Inventors: Pier Giovanni Baraldi, Pier Andrea Borea, Pierangelo Geppetti, Francesca Fruttarolo, Maria Giovanna Pavani, Marcello Trevisani
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Publication number: 20090312286Abstract: The invention provides a new class of compounds capable of inhibiting carnitine palmitoyl transferase (CPT) having formula (I) The invention also relates to pharmaceutical compositions, which comprise at least one new compound according to the invention, and their therapeutic use in the treatment of hyperglycaemic conditions such as diabetes and the pathologies associated with it, such as for example congestive heart failure and obesity.Type: ApplicationFiled: July 10, 2007Publication date: December 17, 2009Applicant: SIGMA-TAU INDUSTRIE FARMACEUTICHE RIUNITE S.P.A.Inventors: Fabio Giannessi, Emanuela Tassoni, Natalina Dell' Uomo, Roberto Conti, Maria Ornella Tinti
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Patent number: 7626054Abstract: Novel biaromatic compounds having the following structural formula (I): are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine, in particular in dermatology as well as in the fields of cardiovascular diseases, immune diseases and/or diseases related to the metabolism of lipids, or, alternatively, into cosmetic compositions.Type: GrantFiled: November 3, 2006Date of Patent: December 1, 2009Assignee: Galderma Research & DevelopmentInventors: Jerome Aubert, Laurence Clary, Pascale Mauvais, Michel Rivier, Etienne Thoreau, Jean-Guy Boiteau
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Patent number: 7619115Abstract: Novel ortho-substituted N?-benzylidene-(3-hydroxyphenyl)acetohydrazides of the formula (I), in which R1-R9 have the meanings indicated in claim 1, are SGK inhibitors and can be used for the treatment of SGK-induced diseases and conditions, such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and kidney diseases, generally in fibroses and inflammatory processes of any type.Type: GrantFiled: June 6, 2005Date of Patent: November 17, 2009Assignee: Merck Patent GmbHInventors: Rolf Gericke, Dieter Dorsch, Werner Mederski, Norbert Beier, Florian Lang
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Publication number: 20090233886Abstract: The present invention provides new derivatives of 4- or 5-aminosalicylic acid, and a pharmaceutical composition containing these derivatives of 4- or 5-aminosalicylic acid as active ingredients, useful for the treatment of intestinal diseases such as inflammatory bowel disease (IBD) and irritable bowel syndrome (IBS) and for the prevention/treatment of colon cancer. More particularly, these derivatives comprise a hydrogen sulfide releasing moiety linked via an azo, an ester, an anhydride, a thioester or an amide linkage to a molecule of 4- or 5-aminosalicylic acid. Furthermore, the present invention provides a process for preparing these compounds and their use for treating IBD and IBS and the prevention/treatment of colon cancer.Type: ApplicationFiled: February 10, 2009Publication date: September 17, 2009Applicant: ANTIBE THERAPEUTICS INC.Inventors: John L. Wallace, Giuseppe Cirino, Giuseppe Caliendo, Anna Sparatore, Vincenzo Santagada, Stefano Fiorucci