Carbocyclic Ring Bonded Directly To The -c(=x)- (e.g., 3-benzoyl Pyrrolidine, Etc.) Patents (Class 548/539)
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Publication number: 20110212892Abstract: The present invention provides a hypoglycemic agent useful for treating diabetes or other similar diseases which has no adverse effects. Furthermore, the present invention provides a hypoglycemic agent comprising a combination of an antidiabetic drug and 2-methyl-2-[(4-{(1E)-3-[2-(4-methylbenzoyl)-1H-pyrrol-1-yl]prop-1-en-1-yl}benzyl)oxy]propanoic acid or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 26, 2009Publication date: September 1, 2011Applicant: Dainippon Sumitomo Pharma Co., Ltd.Inventor: Jun Nagamine
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Publication number: 20110178077Abstract: The present invention relates to small molecule compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.Type: ApplicationFiled: June 17, 2009Publication date: July 21, 2011Inventors: Priscille Brodin, Thierry Christophe, Zaesung No, Jaeseung Kim, Auguste Genovesio, Denis Philippe Cedric Fenistein, Heekyoung Jeon, Fanny Anne Ewann, Sunhee Kang, Saeyeon Lee, Min Jung Seo, Eunjung Park, Monica Contreras Dominguez, Ji Youn Nam, Eun Hye Kim
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Publication number: 20110172208Abstract: The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 and R2 are each hydrogen, lower acyl, lower alkoxycarbonyl or the like; R3 is lower alkyl, halo-lower alkyl, cycloalkyl, heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl or the like; R4 is cyano, lower alkoxycarbonyl, carboxy or the like, which exhibit potent COMT inhibitory activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.Type: ApplicationFiled: June 26, 2009Publication date: July 14, 2011Applicant: Kissei Pharmaceutical Co., Ltd.Inventors: Takehiro Ishikawa, Satoko Kobayashi, Hitoshi Inoue, Yasunori Ueno, Masako Yoshida, Nobuyuki Tanaka
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Publication number: 20110144081Abstract: The present invention relates to compounds of formula wherein R1, R2, R3, R4, Z, and n are as defined herein or to a pharmaceutically active salt thereof. Compounds of the invention are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: ApplicationFiled: December 7, 2010Publication date: June 16, 2011Inventors: Henner Knust, Andreas Koblet, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Walter Vifian
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Publication number: 20110136735Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: November 30, 2010Publication date: June 9, 2011Inventors: David BARNES, Gregory Raymond BEBERNITZ, Scott Louis COHEN, Robert Edson DAMON, Robert Francis DAY, Monish JAIN, Rajeshri Ganesh KARKI, Louise Clare KIRMAN, Tajesh Jayprakash PATEL, Brian Kenneth RAYMER, Herbert Franz SCHUSTER, Wei ZHANG
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Publication number: 20110124881Abstract: Disclosed is a process of forming a pyrrole compound. The process comprises contacting an ?-carbonyl oxime compound 1 and an ?,?-unsaturated aldehyde 2 R1 and R2 in compound 1 are independently selected from the group consisting of H, a silyl-group, an aliphatic group, an alicyclic group, an aromatic group, an arylaliphatic group, and an arylalicyclic group. The aliphatic, alicyclic, aromatic, arylaliphatic, and arylalicyclic groups comprise 0 to about 3 heteroatoms selected from the group N, O, S, Se and Si. R3 in aldehyde 2 is selected from the group consisting of H, a silyl-group, an aliphatic group, an alicyclic group, an aromatic group, an arylaliphatic group, and an arylalicyclic group. The aliphatic, alicyclic, aromatic, arylaliphatic, and arylalicyclic groups comprise 0 to about 3 heteroatoms selected from the group N, O, S, Se and Si. The ?-carbonyl oxime compound 1 an the ?,?-unsaturated aldehyde 2 are contacted in a suitable solvent in the presence of a secondary amine.Type: ApplicationFiled: May 18, 2010Publication date: May 26, 2011Inventors: Guofu Zhong, Bin Tan, Zugui Shi, Pei Juan Chua
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Publication number: 20110118262Abstract: Disclosed are compounds of formula (I) and compositions of the present invention which are inhibitors of the sodium proton exchanger isoform-1 (NHE-I). Also disclosed are methods of using and making the same.Type: ApplicationFiled: June 24, 2009Publication date: May 19, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Joerg Martin Bentzien, Stephen James Boyer, Jennifer Burke, Anne Bettina Eldrup, Xin Guo, John David Huber, Thomas Martin Kirrane, Fariba Soleymanzadeh, Alan David Swinamer
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Publication number: 20100298330Abstract: The present invention is related to the preparation and pharmaceutical In use of novel haloallylamine derivatives as SSAO/VAP-1 inhibitors having the structure of Formula I, as defined in the specification:(I). The invention also relates to methods of using invention compounds, or pharmaceutically acceptable salt or derivatives thereof, for the treatment of a variety of indications, e.g., inflammatory diseases.Type: ApplicationFiled: November 19, 2008Publication date: November 25, 2010Applicant: PHARMAXIS LTD.Inventors: Ian A. McDonald, Craig Ivan Turner, Mandar Deodhar, Jonathan Stuart Foot
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Publication number: 20100286144Abstract: A compound of the following formula (1), or its prodrug or pharmaceutically acceptable salt thereof, being useful as a diabetic medicine or preventive, or blood sugar regulator, or therapeutic agent for hyperlipemia, etc. wherein the ring Z is an optionally substituted heteroaryl, W4 is a single bond, lower alkylene, etc., Ar2 is an optionally substituted aryl, etc., W3 is a single bond, lower alkylene, etc., Ar1 is an optionally substituted arylene, etc., each of W1 and W2 is an optionally substituted lower alkylene, etc., and R1 is carboxyl, an alkoxycarbonyl.Type: ApplicationFiled: July 21, 2010Publication date: November 11, 2010Inventors: Yoko TAKAHASHI, Ryu Nagata, Kantaro Ushiroda
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Publication number: 20100286170Abstract: The present invention provides novel beta-secretase inhibitors and methods for their use, including methods of treating of Alzheimer's disease.Type: ApplicationFiled: September 24, 2008Publication date: November 11, 2010Inventors: Arun K. Ghosh, Chunfeng Liu, Thippeswamy Devasamudram, Hui Lei, Lisa M. Swanson, Sudha V. Ankala, John C. Lilly, Geoffrey M. Bilcer
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Publication number: 20100256114Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.Type: ApplicationFiled: June 17, 2010Publication date: October 7, 2010Applicant: INCYTE CORPORATIONInventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Brian W. Metcalf, Chunhong He, Ding-Quan Qian, Colin Zhang
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Publication number: 20100234364Abstract: Compounds are provided that act as potent antagonists of the CCR2 or CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2 and CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, CCR9-mediated diseases, as controls in assays for the identification of CCR2 antagonists, and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: July 10, 2007Publication date: September 16, 2010Inventors: Arindrajit Basak, Jeff Jin, Jimmie Moore, Andrew M.K. Pennell, Sreenlvas Punna, Solomon Ungashe, Zheng Wei
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Publication number: 20100210693Abstract: The present invention is directed to compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: ApplicationFiled: May 3, 2010Publication date: August 19, 2010Inventors: Philippe G. Nantermet, Hemaka Anthony Rajapakse, Harold G. Selnick
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Patent number: 7776909Abstract: Selected 2-arylacetic acids, their derivatives and pharmaceutical compositions that contain these compounds are useful in inhibiting chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2-membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. In particular, 2(ortho)-substituted arylacetic acids or their derivatives, such as amides and sulfonamides, lack cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.Type: GrantFiled: February 4, 2004Date of Patent: August 17, 2010Assignee: Dompe Pha.R.Ma S.p.A.Inventors: Alessio Moriconi, Marcello Allegretti, Riccardo Bertini, Cinzia Bizzarri, Maria Candida Cesta, Francesco Colotta
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Publication number: 20100173970Abstract: Active compounds of Formula I are described: wherein: R1 and R2 are each independently C1-C4 alkyl; or R1 and R2 together form a C2-C7 alkylene chain; and Z is a non-steroidal anti-inflammatory drug (NSAID); along with pharmaceutically acceptable salts and prodrug thereof, and methods of using the same.Type: ApplicationFiled: February 23, 2010Publication date: July 8, 2010Inventor: S. Bruce King
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Publication number: 20100168083Abstract: Novel substituted adamantane based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.Type: ApplicationFiled: March 20, 2007Publication date: July 1, 2010Inventor: Soren Ebdrup
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Publication number: 20100168088Abstract: The present invention relates to a compound of formula I wherein Ar1, Ar2, R1, R2, R3, n, o, and p are as described herein or to a pharmaceutically active salt, to all stereoisomeric forms, including individual diastereoisomers and enantiomers as well as to racemic and non-racemic mixtures thereof. Compounds of the invention are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: ApplicationFiled: October 2, 2009Publication date: July 1, 2010Inventors: Caterina Bissantz, Philippe Jablonski, Henner Knust, Matthias Nettekoven, Angélique Patiny-Adam, Hasane Ratni, Claus Riemer
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Publication number: 20100160285Abstract: The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim 1, as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.Type: ApplicationFiled: December 18, 2009Publication date: June 24, 2010Inventors: Timothy Jon Luker, Timothy Nicholas Birkinshaw, Rukhsana Tasneem Mohammed
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Patent number: 7737135Abstract: The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim 1, as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.Type: GrantFiled: August 22, 2005Date of Patent: June 15, 2010Assignee: AstraZeneca ABInventors: Timothy Jon Luker, Timothy Nicholas Birkinshaw, Rukhsana Tasneem Mohammed
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Publication number: 20100144828Abstract: The present invention provides caffeoylquinic acid derivatives and a method of preparing for the same, and also provides pharmaceutical compositions containing caffeoylquinic acid derivatives, and uses of caffeoylquinic acid derivatives in preparation of a medicament for the treatment or prophylaxis of virus diseases, in particular, uses of respiratory syncytial virus and hepatitis B virus, which has the characteristics of safety, high effectiveness and low toxicity.Type: ApplicationFiled: March 21, 2008Publication date: June 10, 2010Applicant: ZHEJIANG MEDICINE CO., LTD. XINCHANG PHARMACEUTICAInventors: Zhanggui Wu, Wei Wei
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Publication number: 20100137599Abstract: The present invention relates to a process for the preparation of 1,4-butanediol mononitrate as intermediate for large scale preparation of high purity nitrooxybutyl ester of pharmaceutically active compounds.Type: ApplicationFiled: June 18, 2008Publication date: June 3, 2010Applicant: NICOX S.A.Inventors: Achim Hack, Gunter Weingarner, Matthias Kramer
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Patent number: 7683168Abstract: Diarylmethylpiperazine compounds are described, which are useful as mu and/or delta receptor opioid compounds, without central side effects. Pharmaceutical compositions containing such compounds are variously useful for peripheral or non-centrally mediated indications, including peripherally mediated and neuropathic pain, urogenital tract disorders, overactive bladder, urinary incontinence, sexual disorders, premature ejaculation, cough, lung edema, cardiac disorders, cardioprotection, gastro-intestinal disorders, diarrhea, irritable bowl syndrome, functional distention, immuno-modulation and anti-tumor activity.Type: GrantFiled: April 14, 2006Date of Patent: March 23, 2010Assignee: Mount Cook Bio Sciences, Inc.Inventors: Shyi-Tai Jan, Kwen-Jen Chang, Kestutis P. Biciunas, Xin Ma
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Publication number: 20100056522Abstract: An object of the present invention is to find a novel pharmacological effect of a compound having an HDAC inhibitory effect. The compound having an HDAC inhibitory effect of the invention has an excellent effect of cell morphological change on trabecular meshwork cells and/or effect of intraocular pressure reduction, and is therefore useful as a preventive and/or therapeutic agent for a disease considered to be associated with aqueous humor circulation and/or intraocular pressure, particularly as a preventive and/or therapeutic agent for glaucoma or ocular hypertension.Type: ApplicationFiled: March 28, 2008Publication date: March 4, 2010Applicant: Santen Pharmaceutical Co., Ltd.Inventors: Shinji Yoneda, Koushi Fujisawa, Katsuhiko Watanabe, Junko Fujikawa, Atsushi Shimazaki, Tomoko Kirihara, Hisashi Tajima
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Patent number: 7652151Abstract: The present invention provides novel ketopyrroles having structure XXIV wherein R2 is independently at each occurrence a deuterium atom, a halogen, a nitro group, an amino group, a C3-C40 aromatic radical, a C1-C50 aliphatic radical, or a C3-C40 cyclcoaliphatic radical; “a” is an integer from 0 to 3; and X1 and X2 are independently at each occurrence a bromine atom, a hydroxy group, or the group OR10, and wherein the group R10 is independently at each occurrence a deuterium atom, a halogen, a nitro group, an amino group, a C3-C40 aromatic radical, a C1-C50 aliphatic radical, or a C3-C40 cyclcoaliphatic radical. Ketopyrroles XXIV are useful ligands for the preparation of Type (1) and Type (2) organic iridium compositions. In one aspect, the present invention provides deuterated analogs of XXIV. Organic iridium compositions are useful in the preparation optoelectronic devices, such as OLED devices and photovoltaic devices exhibiting enhanced performance characteristics.Type: GrantFiled: August 14, 2006Date of Patent: January 26, 2010Assignee: General Electric CompanyInventor: Kelly Scott Chichak
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Publication number: 20090275581Abstract: Disclosed are compounds according to Formula I: wherein the variables are defined herein. Such compounds are can bind aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also described herein are methods of antagonizing aspartic protease inhibitors in a subject in need thereof comprising administering to the subject a therapeutically effective amount of a compound according to Formula I.Type: ApplicationFiled: April 5, 2007Publication date: November 5, 2009Inventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh, Patrick T. Flaherty, Lara S. Kallander, Colin A. Leach, Brian Lawhorn, Qing Lu, Lamont R. Terrell, Bahman Ghavini-Alagha, Jing Zhang, Damiano Ghirlanda, Xiaoping Hou, Simon Semus
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Patent number: 7557136Abstract: The present invention relates to novel pyrrolidine derivatives of Formula (I), its geometrical isomers, its optically active forms as enantiomers, diastercomers, mixtures of these and its racemate forms, as well as salts thereof, wherein: R1is selected from the group comprising or consisting of H and C1-C6-alkyl; R2 is selected from the group comprising or consisting of hydrogen, C1-C6-alkyl, C1-C6 alkyl aryl, heteroaryl, C1-C6 alkyl heteroaryl, C2-C6-alkenyl, C2-C6-alkenyl aryl, C2-C6 alkenyl heteroaryl, C2-C6-alkynyl, C2-C6-alkynyl aryl, C2C6-alkynyl heteroaryl, C3-C8 cycloalkyl, heterocycloalkyl, CI-C6-alkyl cycloallcyl, CI-C6-alkyl heterocycloalkyl, CIC6 alkyl carboxy, acyl, C1-C6-alkyl acyl, C1-C6-alkyl acyloxy, C1-C6-alkyl alkoxy, alkoxycarbonyl, C1-C6-alkyl alkoxycarbonyl, aminocarbonyl, C1-C6-alkyl aminocarbonyl, C1-C6-alkyl acylarnino, C1-C6-alkyl ureido, amino, C1-C6-alkyl amino, sulfonyloxy, C1-C6 alkyl sulfonyloxy, sulfonyl, C1-C6-alkyl sulfonyl, sulfinyl, C1-C6-alkyl sulfinyl, C1-C6alkyl sulfanylType: GrantFiled: February 16, 2004Date of Patent: July 7, 2009Assignee: Laboratoires Serono SAInventors: Matthias Schwarz, Catherine Jorand-Lebrun, Delphine Valognes
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Publication number: 20090118169Abstract: A compound comprising the atom corresponding to N3 and the two or more atoms selected from N1, N2, N4 and N5, said atoms constitute the pharmacophore represented by the following formula: wherein N1 represents an atom to which a donative hydrogen atom in a hydrogen-bond donating group is bonded or a hydrogen-bond accepting atom in a hydrogen-bond accepting group; N3 represents a hydrogen-bond accepting atom in a hydrogen-bond accepting group; and N2, N4 and N5 independently represents an arbitrary carbon atom constituting a hydrophobic group and defined by the interatomic distances between N1, N2, N3, N4 and N5; and, in the optimized three-dimensional structure thereof, the distances between the atom corresponding to N3 and the two or more atoms selected from N1, N2, N4 and N5, in the optimized steric structure thereof, are the interatomic distances in a pharmacophore; or a salt thereof; inhibits the activity of transcription factor AP-1 and is useful as an agent for preventing and treating the diseases iType: ApplicationFiled: November 16, 2007Publication date: May 7, 2009Applicant: TOYAMA CHEMICAL CO., LTD.Inventors: Hisaaki Chaki, Tadakazu Takakura, Keiichi Tsuchida, Hironori Kotsubo, Yukihiko Aikawa, Shuichi Hirono, Shunichi Shiozawa
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Publication number: 20090082399Abstract: The present invention relates to new compounds which are Carbamate derivatives of formula I wherein X, B, P, Q5W, R1 and R2 are defined in the description.Type: ApplicationFiled: May 17, 2006Publication date: March 26, 2009Applicant: Addex Pharma SAInventors: Piergiuliano Bugada, Stefania Gagliardi, Giovanni Palombi, Jean-Philippe Rocher
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Publication number: 20090042896Abstract: The invention relates to a compound of formula I wherein Ar1, Ar2, R1, R2, R3, R4, n, o, p, and q are as defined herein and to a pharmaceutically active salt thereof, including all stereoisomeric forms, individual diastereoisomers and enantiomers of the compound of formula (I) as well as racemic and non-racemic mixtures thereof. The compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: ApplicationFiled: August 4, 2008Publication date: February 12, 2009Inventors: Philippe Jablonski, Kenichi Kawasaki, Henner Knust, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Xihan Wu
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Publication number: 20090012151Abstract: The present invention relates to amide compounds useful as pharmaceuticals for treating respiratory disorders such as asthma, rhinitis and COPD.Type: ApplicationFiled: July 3, 2008Publication date: January 8, 2009Inventors: Roger Victor Bonnert, Timothy Jon Luker, Anil Patel, Aaron Rigby
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Publication number: 20080260651Abstract: The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds. More specifically the iodine containing compounds are chemical compounds containing an aliphatic N-heterocyclic central moiety such as pyrrolidine or piperidine heterocycles allowing for the arrangement of three iodinated phenyl groups bound thereto. The invention also relates to the use of such diagnostic compositions as contrast agents in diagnostic imaging, in particular in X-ray imaging, and to contrast media containing such compounds.Type: ApplicationFiled: April 15, 2008Publication date: October 23, 2008Applicant: GE HEALTHCARE ASInventors: Veronique Morisson-Iveson, Joanna Marie Passmore
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Publication number: 20080255154Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.Type: ApplicationFiled: June 10, 2008Publication date: October 16, 2008Applicant: INCYTE CORPORATIONInventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Brian W. Metcalf, Chunhong He, Ding-Quan Qian, Colin Zhang
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Patent number: 7429658Abstract: A method of synthesis of a N-10 protected PBD compound of formula (I): via an intermediate of formula (II) or formula (V):Type: GrantFiled: September 10, 2004Date of Patent: September 30, 2008Assignee: Spirogen LimitedInventors: Philip Howard, Luke Masterson
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Patent number: 7425642Abstract: A heteroaryl derivative of the formula (1): (wherein Ring Z is an optionally substituted heteroaryl, R1 is a carboxyl group or an alkoxycarbonyl group, etc., W1 and W2 are an optionally substituted lower alkylene, Ar1 is an optionally substituted arylene or an optionally substituted heteroarylene, W3 is a single bond, a lower alkylene, a lower alkenylene, etc., W4 is a single bond, —NR10—, etc., Ar2 is an optionally substituted aryl or an optionally substituted heteroaryl), or a prodrug thereof, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: July 13, 2004Date of Patent: September 16, 2008Assignee: Dainippon Sumitomo Pharma Co. ,Ltd.Inventors: Ken-ichi Watanabe, Katsunori Maruta, Kantaro Ushiroda, Ryu Nagata
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Publication number: 20080217580Abstract: The present invention relates to compounds of formula (I) a process for their production and to their use for coloring high molecular weight organic materials, as fluorescent tracers, in solid dye lasers, EL lasers, in EL devices and lighting. The compounds of formula I show unique broadband luminescence in visible region.Type: ApplicationFiled: April 11, 2005Publication date: September 11, 2008Inventors: Junichi Tanabe, Hiroshi Yamamoto, Norihisa Dan
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Publication number: 20080161325Abstract: The present invention relates to compounds of formula (AA) (I) and (X): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.Type: ApplicationFiled: November 13, 2007Publication date: July 3, 2008Inventors: Yvette M. Fobian, John N. Freskos, Barbara Jagodzinska
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Publication number: 20080146607Abstract: Compounds of the formula: or pharmaceutically acceptable salts thereof, wherein m, n, Ar, R1, R2, Ra and Rb are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.Type: ApplicationFiled: December 18, 2007Publication date: June 19, 2008Inventors: Pravin Iyer, Clara Jeou Jen Lin, Stephen M. Lynch, Matthew C. Lucas, Ann Marie Madera, Kerem Erol Ozboya, Robert James Weikert, Ryan Craig Schoenfeld
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Publication number: 20080132480Abstract: The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim 1, as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.Type: ApplicationFiled: August 22, 2005Publication date: June 5, 2008Applicant: AstraZeneca ABInventors: Timothy Jon Luker, Timothy Nicholas Birkinshaw, Rukhsana Tasneem Mohammed
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Patent number: 7361663Abstract: This invention is directed to N-acylpyrrolidin-2-ylalkylbenzamidine derivatives which useful for inhibiting the activity of Factor Xa, by contacting said derivatives with a composition containing Factor Xa. The present invention is also directed to compositions containing said derivatives, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.Type: GrantFiled: October 16, 2003Date of Patent: April 22, 2008Assignee: Aventis Pharmaceuticals Inc.Inventors: Mark Czekaj, Scott I. Klein, Heinz W. Pauls
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Publication number: 20080045509Abstract: Certain substituted benzyl amine compounds are histamine H3 receptor and/or serotonin transporter modulators useful in the treatment of histamine H3 receptor- and/or serotonin-mediated diseases.Type: ApplicationFiled: June 21, 2007Publication date: February 21, 2008Inventors: Brett Allison, Michael P. Curtis, Cheryl A. Grice, John M. Keith, Michael A. Letavic, Jennifer M. B. Miller, Emily M. Stocking
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Patent number: 7329762Abstract: The present invention relates to phosphate ester prodrugs of 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 also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: June 8, 2004Date of Patent: February 12, 2008Assignee: Merck & Co., Inc.Inventors: Mark E. Fraley, Robert M. Garbaccio, George D. Hartman, William F. Hoffman
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Publication number: 20070299071Abstract: The present invention relates to compounds of formula I wherein R1, R2, R3, X, n, and m are as defined herein and to pharmaceutically acceptable acid addition salts thereof, to pharmaceutical compositions containing them, and to methods for treating neurological and neuropsychiatric disorders.Type: ApplicationFiled: June 15, 2007Publication date: December 27, 2007Inventors: Synese Jolidon, Robert Narquizian, Roger Norcross, Emmanuel Pinard
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Patent number: 7244758Abstract: Compounds that are derivatives of 3-aminomethyl-pyrrolidine generally containing at least one benzhydril moiety are useful in treating conditions which benefit from blocking calcium ion channels.Type: GrantFiled: May 28, 2004Date of Patent: July 17, 2007Assignee: Neuromed Pharmaceuticals Ltd.Inventors: Hassan Pajouhesh, Terrance P. Snutch, Hossein Pajouhesh, Yanbing Ding
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Patent number: 7189756Abstract: The present invention relates to pyrrolidine derivatives useful as inhibitors of metalloproteases, e.g. zinc proteases, and which are effective in treating disease states associated with vasoconstriction.Type: GrantFiled: June 30, 2004Date of Patent: March 13, 2007Assignee: Hoffman-La Roche Inc.Inventors: Johannes Aebi, Daniel Bur, Alexander Chucholowski, Henrietta Dehmlow, Eric Argirios Kitas, Ulrike Obst, Hans Peter Wessel
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Patent number: 7132551Abstract: One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.Type: GrantFiled: June 26, 2003Date of Patent: November 7, 2006Assignee: Sepracor Inc.Inventors: Brian M. Aquila, Thomas D. Bannister, Gregory D. Cuny, James R. Hauske, Joanne M. Holland, Paul E. Persons, Heike S. Radeke, Fengjiang Wang, Liming Shao
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Patent number: 7129266Abstract: The invention relates to a new antibiotic designated Cyan426-A, to its production by fermentation, to methods for its recovery and concentration from the crude solutions, and to a process for its purification and to semisynthetic ethers of Cyan426-A, Cyan426-A-ethers.Type: GrantFiled: December 15, 2003Date of Patent: October 31, 2006Assignee: Wyeth Holdings CorporationInventors: Haiyin He, Hui Yang, Ramunas Bigelis
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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: 7001905Abstract: Diarylamines, such as 5-amide substituted diarylamines of formula (I) or formula (II) wherein A is hydroxy, C1-6 alkoxy, or NR6OR7; X is OR12, NR13R12, or NR14; inhibitors of MEK and are useful in the treatment of a variety of proliferative disease states, such as conditions related to the hyperactivity of MEK, as well as diseases modulated by the MEK cascade.Type: GrantFiled: March 12, 2001Date of Patent: February 21, 2006Assignee: Warner-Lambert CompanyInventors: Cathlin Biwersi, Haile Tecle, Joseph Scott Warmus
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Patent number: 6897319Abstract: This invention is directed to aroyl pyrrole heteroaryl methanone and methanol compounds pharmaceutically useful as agents for treating or modulating a central nervous system disorder and methods for treating or modulating a central nervous system disorder.Type: GrantFiled: December 10, 2002Date of Patent: May 24, 2005Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: John R. Carson, Ellen E. Codd, Philip M. Pitis
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Patent number: 6890939Abstract: The present invention is directed to compounds useful as selective serine protease or dual-serine protease inhibitors, compositions thereof and methods for treating serine protease or dual-serine protease mediated disorders.Type: GrantFiled: May 16, 2003Date of Patent: May 10, 2005Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Michael N. Greco, Bruce E. Maryanoff, Michael J. Hawkins, Robert E. Boyd