Carbocyclic Ring Containing Patents (Class 546/194)
-
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
-
Patent number: 7507753Abstract: The present invention provides a compound having melanocortin receptor agonist activity or antagonist activity, which is a novel biaryl compound represented by the formula (I): wherein ring A and ring B are optionally further substituted 6-membered aromatic rings; X is —CONR4—, —SO2NR4—, —CH2NR4— (R4 is a hydrogen atom, an optionally substituted hydrocarbon group, etc.), etc.; Y is a spacer having 1 to 12 atoms, etc.; Z is —CONR6—, —CO— (R6 is a hydrogen atom, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group), etc.; R1 is an optionally substituted amino group, etc.; R2 is an optionally substituted hydrocarbon group, etc.; R3 is an optionally substituted hydrocarbon group, etc.; and R5 is an optionally substituted hydrocarbon group, etc.; or a salt thereof.Type: GrantFiled: December 26, 2002Date of Patent: March 24, 2009Assignee: Takeda Chemical Industries Ltd.Inventors: Nobuo Cho, Kazuyoshi Aso, Satoshi Endo, Naoyuki Kanzaki, Satoshi Sasaki
-
Publication number: 20090076064Abstract: Disclosed are compounds of Formula (I) wherein G, R2, A, D and E are as described in the specification, or pharmaceutically-acceptable salts, or in vivo-hydrolysable precursors thereof. Also disclosed herein is at least one method of making, at least one pharmaceutical composition containing, and at least one method for using at least one compound in accordance with Formula I.Type: ApplicationFiled: January 3, 2007Publication date: March 19, 2009Applicant: ASTRAZENECA ABInventors: Rebecca Urbanek, Dean Brown, Gary Steelman, William Blackwell, Steven Wesolowski, Xia Wang
-
Publication number: 20090075975Abstract: Arylsulfonamide compounds of formula I are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders:Type: ApplicationFiled: November 24, 2008Publication date: March 19, 2009Inventors: Michael R. DeGraffenreid, JAY P. POWERS, Daqing Sun, Xuelei Yan
-
Patent number: 7504417Abstract: There are provided compounds having an anticoagulant action on the basis of inhibition of activated blood coagulation factor X and being useful as anticoagulants or preventive/therapeutic agents for diseases induced by thrombosis or embolism. Effective ingredients are the compounds such as 4?-bromo-2?-[(5-chloro-2-pyridyl)carbamoyl]-6?-?-D-galactopyranosyloxy-1-isopropylpiperidine-4-carboxanilide, 2?-(2-acetamido-2-deoxy-?-D-glucopyranosyloxy)-4?-bromo-6?-[(5-chloro-2-pyridyl)carbamoyl]-1-isopropylpiperidine-4-carboxanilide, etc. or salts thereof.Type: GrantFiled: November 21, 2001Date of Patent: March 17, 2009Assignee: Astellas Pharma Inc.Inventors: Tsukasa Ishihara, Fukushi Hirayama, Keizo Sugasawa, Yuji Koga, Takeshi Kadokura, Takeshi Shigenaga
-
Patent number: 7504511Abstract: The invention relates to 2-acylamino-4-phenylthiazole derivatives of general formula (I): pharmaceutically acceptable acid-addition salts thereof, hydrates or solvates of such derivatives or such pharmaceutically acceptable acid addition salts, intermediates thereto, processes for the preparation thereof, and therapeutic application thereof.Type: GrantFiled: October 19, 2005Date of Patent: March 17, 2009Assignee: Sanofi-AventisInventors: Pierre Carayon, Pierre Casellas, Daniel Floutard, Pierre Fraisse, Samir Jegham, Bernard Labeeuw
-
Publication number: 20090069335Abstract: The invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein R1-3, R5-7, a, X, Y, Y?, Y?, and Z are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.Type: ApplicationFiled: September 5, 2008Publication date: March 12, 2009Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
-
Publication number: 20090069377Abstract: The present application describes deuterium-enriched enzastaurin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: August 22, 2008Publication date: March 12, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
-
Publication number: 20090069282Abstract: The present invention relates to alkyne compounds of general formula I wherein the groups and residues A, B, W, X, Y, Z, R1 and R2 have the meanings given in claim 1. The invention further relates to pharmaceutical compositions containing at least one alkyne according to the invention. In view of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.Type: ApplicationFiled: May 15, 2008Publication date: March 12, 2009Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Dirk Stenkamp, Stephan Georg Mueller, Gerald Juergen Roth, Thorsten Lehmann-Lintz, Klaus Rudolf, Philipp Lustenberger, Kirsten Arndt, Ralf R. H. Lotz, Martin Lenter
-
Publication number: 20090069376Abstract: Substituted N—[N-(sulphonylphenyl)sulfonyl-prolyl]-phenylalanine derivatives of the present invention are antagonists of the VLA-4 integrin and are useful in the treatment, prevention and suppression of diseases mediated by VLA-4-binding and cell adhesion and activation. Moreover, the compounds of the present invention demonstrate significant receptor occupancy of VLA-4 bearing cells after oral administration and are suitable for once-, twice-, or thrice-a-day oral administration. This invention also relates to compositions containing such compounds and methods of treatment using such compounds.Type: ApplicationFiled: April 17, 2006Publication date: March 12, 2009Inventors: Ping Liu, Carrie Jones, Thomas S. Reger
-
Patent number: 7501440Abstract: The invention relates to compounds of the formula I where the radicals are as defined, and their physiologically tolerated salts. The compounds are suitable, for example, as medicaments for preventing and treating type 2 diabetes.Type: GrantFiled: March 8, 2004Date of Patent: March 10, 2009Assignee: Sanofi-Aventis Deutschland GmbHInventors: Karl Schoenafinger, Dieter Kadereit, Elisabeth Defossa, Andreas Herling, Thomas Klabunde
-
Publication number: 20090062341Abstract: The present invention relates to a novel class of selective estrogen receptor modulators (SERMs). The SERM compounds are applicable for use in the prevention and/or treatment of a variety of diseases and conditions including prevention and treatment of cancers such as prostate and breast cancer, osteoporosis, hormone-related diseases, hot flashes or vasomotor symptoms, neurological disorders, cardiovascular disease and obesity.Type: ApplicationFiled: November 28, 2006Publication date: March 5, 2009Inventors: James T. Dalton, Christina Barrett, Yali He, Seoung-Soo Hong, Duane D. Miller, Michael L. Mohler, Ramesh Narayanan, Zhongzhi Wu
-
Publication number: 20090062278Abstract: The present invention concerns 5- or 6-substituted-benzimidazole derivatives having inhibitory activity on the replication of the respiratory syncytial virus and having the formula a prodrug, N-oxide, addition salt, quaternary amine, metal complex or stereochemically isomeric form thereof wherein Q is Ar2, R6, pyrrolidinyl substituted with R6, piperidinyl substituted with R6 or homopiperidinyl substituted with R6, G is a direct bond or optionally substituted C1-10alkanediyl; R1 is Ar1 or a monocyclic or bicyclic heterocycle; one of R2a and R2b is cyanoC1-6alkyl, cyanoC2-6alkenyl, Ar3C1-6alkyl, Het1C1-6alkyl, N(R8aR8b)C1-6alkyl, Ar3C2-6alkenyl, Het1C2-6alkenyl, Ar3aminoC1-6alkyl, Het1aminoC1-6alkyl, Ar3thioC1-6alkyl, Het1thioC1-6alkyl, Ar3sulfonylC1-6alkyl, Het1sulfonylC1-6alkyl, Ar3aminocarbonyl, Het1aminocarbonyl, Ar3(CH2)naminocarbonyl, Het1(CH2)naminocarbonyl, Ar3carbonylamino, Het1carbonylamino, Ar3(CH2)ncarbonylamino, Het1(CH2)ncarbonylamino, and the other one of R2a and R2b is hydrogen; in case R2aType: ApplicationFiled: October 17, 2008Publication date: March 5, 2009Inventors: Jean-Francois Bonfanti, Koenraad Jozef Lodewijk Andries, Jerome Michel Claude Fortin, Philippe Muller, Frederic Marc Maurice Doublet, Christophe Meyer, Rudy Edmond Willebrords, Tom Valerius Josepha Gevers, Philip Maria Martha Bern Timmerman
-
Publication number: 20090062271Abstract: This application relates to a compound of formula I (or a pharmaceutically acceptable salt of the compound) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa and/or thrombin, as well as a process for its preparation and intermediates therefor.Type: ApplicationFiled: November 15, 2005Publication date: March 5, 2009Applicant: Eli Lilly And CompanyInventors: Jeffry Bernard Franciskovich, David Kent Herron, Valentine Joseph Klimkowski, Angela Lynn Marquart, John Joseph Masters, David Mendel, Andrew Michael Ratz, Gerald Floyd Smith, Michael Robert Wiley, Ying Kwong Yee
-
Publication number: 20090062260Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of liver X receptors (LXRs).Type: ApplicationFiled: November 14, 2006Publication date: March 5, 2009Applicants: IRM LLC, NOVARTIS AGInventors: Valentina Molteni, David A. Ellis, Juliet Nabakka, Donatella Chianelli, Enrique Saez, Xiaolin Li, Sylvie Chamoin, Hans-Jorg Roth
-
Publication number: 20090062261Abstract: It was found out that the nitrogen-containing heterocyclic derivative represented by the formula (I) specifically binds to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist. A compound represented by: wherein Z is N or CR1, A1 is a nitrogen-containing aromatic monocyclic group which is optionally substituted, a nitrogen-containing aromatic fused cyclic group which is optionally substituted etc., A2 is an aromatic hydrocarbon cyclic group or an aromatic heterocyclic group, each optionally having a substituent, R1, R2, Ra, Rb, Rc and Rd are each independently hydrogen, hydroxy, etc., w is 2 or 3, t is 1 or 2, X is —(CR3R4)m-, —CO(CR3R4)n-, —CONR5(CR3R4)n- etc., m is an integer of 1 to 4, n is an integer of 0 to 4, R3 and R4 are each independently hydrogen, halogen, hydroxy etc., and R5 is hydrogen or lower alkyl, or a pharmaceutically acceptable salt, or a solvate thereof.Type: ApplicationFiled: February 21, 2007Publication date: March 5, 2009Applicant: SHIONOGI & CO., LTD.Inventors: Moriyasu Masui, Makoto Adachi, Hidenori Mikamiyama, Akira Matsumura, Naoki Tsuno
-
Patent number: 7498346Abstract: The present invention relates to chemokine receptor binding compounds, pharmaceutical compositions and their use. More specifically, the present invention relates to modulators of chemokine receptor activity, preferably modulators of CCR5. These compounds demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).Type: GrantFiled: June 14, 2005Date of Patent: March 3, 2009Assignee: Genzyme CorporationInventors: Yuanxi Zhou, Gary J. Bridger, Renato T. Skerlj, David Bogucki, Wen Yang, Elyse Bourque, Jonathan Langille, Tong-Shuang Li, Markus Metz
-
Publication number: 20090054435Abstract: The present invention provides a compound represented by the formula: wherein each symbol is as defined in the specification. Since the compound of the present invention has superior hypoglycemic action and superior hypolipidemic action, it is useful as an agent for the prophylaxis or treatment of diabetes, hyperlipidemia, impaired glucose tolerance and the like.Type: ApplicationFiled: July 28, 2006Publication date: February 26, 2009Inventor: Hiroshi Imoto
-
Publication number: 20090054464Abstract: Compounds having the formula (I): wherein R1 is hydrogen, lower alkyl, lower alkenyl, lower or higher alkynyl, cyclo(lower)alkyl, cyclo(higher)alkyl, cyclo(lower)alkyl(lower)alkyl, cyclo(higher)alkyl(lower)alkyl, cyclo(lower)alkenyl(lower)alkyl, aryl-fused cyclo(lower)alkyl, lower alkoxy, acyl, aryl, ar(lower)alkoxy, ar(lower)alkyl, heteroar(lower)alkyl, amino, heteroaryl, heterocyclyl or heterocyclyl(lower)alkyl, which may be substituted with one or more suitable substituent(s), R2 is hydrogen or lower alkyl, X is pyrrolidinylene or piperidinylene, Y is pyridylene, which may be substituted with one or more suitable substituent(s), Z is lower alkenylene, which may be substituted with lower alkyl or halogen, and salts thereof are useful as a histone deacetylase inhibitors.Type: ApplicationFiled: November 4, 2008Publication date: February 26, 2009Applicant: Astellas Pharma Inc.Inventors: Naoki ISHIBASHI, Yuki SAWADA, Yasuharu URANO, Shigeki SATOH, Yoshikazu INOUE, Yoshiteru EIKYU, Koichiro MUKOYOSHI, Kazunori KAMIJO, Fumiyuki SHIRAI, Hisashi TAKASUGI
-
Publication number: 20090054451Abstract: The present invention is directed to novel piperidine derivatives and to the use of piperidine derivatives of formula I as agonists of chemokine receptor activity.Type: ApplicationFiled: August 4, 2008Publication date: February 26, 2009Applicant: Euroscreen S.A.Inventors: Jacques Huck, Frederic Ooms, Christian Tyrchan, Hamid R. Hoveyda
-
Patent number: 7494989Abstract: Achiral pyrimidine derivatives and pyridine derivatives of the following formulae or analogs thereof have selective N-type calcium channel antagonistic activity and showed analgesic action when they were taken orally. They are useful as therapeutic agents for pains and various diseases associated with the N-type calcium channels.Type: GrantFiled: September 17, 2007Date of Patent: February 24, 2009Assignee: Ajinomoto Co., Inc.Inventors: Seiji Ohno, Kayo Otani, Seiji Niwa, Satoshi Iwayama, Akira Takahara, Hajime Koganei, Yukitsugu Ono, Shinichi Fujita, Tomoko Takeda, Masako Hagihara, Akiko Okajima
-
Publication number: 20090048291Abstract: The present invention is directed to compounds of formula I compositions comprising them and their use.Type: ApplicationFiled: August 4, 2008Publication date: February 19, 2009Applicant: Euroscreen S.A.Inventors: Jacques Huck, Frederic Ooms, Julien Parcq, Regereau Yannick, Hamid R. Hoveyda, Guillaume Dutheuil
-
Publication number: 20090048299Abstract: This invention provides compounds of formula I: wherein a, b, c, m, p, s, t, W, Ar1, X1, R1, R2, R3, R4, R6, and R7 areas defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: ApplicationFiled: October 3, 2008Publication date: February 19, 2009Inventors: Mathai Mammen, Yu-Hua Ji, YongQi Mu, Trevor Mischki, Viengkham Malathong
-
Publication number: 20090048227Abstract: Substituted piperidine compounds represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.Type: ApplicationFiled: December 18, 2006Publication date: February 19, 2009Inventors: Pasun K. Chakravarty, Pengcheng Patrick Shao, Feng Ye
-
Patent number: 7491826Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: GrantFiled: July 14, 2004Date of Patent: February 17, 2009Assignee: Cytokinetics, Inc.Inventors: Bradley Paul Morgan, Kathleen A. Elias, Erica Anne Kraynack, Pu-Ping Lu, Fady Malik, Alex Muci, Xiangping Qian, Whitney Walter Smith, Todd Tochimoto, Adam Lewis Tomasi, David J. Morgans, Jr.
-
Patent number: 7491735Abstract: The present invention relates to chemokine receptor binding compounds, pharmaceutical compositions and their use. More specifically, the present invention relates to modulators of chemokine receptor activity, preferably modulators of CCR5. These compounds demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).Type: GrantFiled: December 13, 2004Date of Patent: February 17, 2009Assignee: Genzyme CorporationInventors: Yuanxi Zhou, Gary J. Bridger, Renato T. Skerlj, David Bogucki, Wen Yang, Elyse Bourque, Jonathan Langille, Tong-Shuang Li, Markus Metz, Maria R. Di Fluri, Siqiao Nan
-
Publication number: 20090043094Abstract: A process for the preparation of Compound (I) comprising reacting Compound (II) with a base in an aprotic solvent, which is represented by the following scheme: wherein R1 and R2 are each independently lower alkyl.Type: ApplicationFiled: October 7, 2008Publication date: February 12, 2009Applicant: Shionogi & Co., Ltd.Inventors: Yasuyuki KAWANISHI, Masaaki Uenaka, Munenori Matsuura
-
Publication number: 20090042841Abstract: This invention relates to novel heterocyclic compounds having selective affinity for the mGlu5 subtype of metabotropic receptors, pharmaceutical compositions thereof and uses for such compounds and compositions in the treatment of lower urinary tract disorders, such as neuromuscular dysfunction of the lower urinary tract, and in the treatment of migraine and gastroesophagael reflux disease (GERD).Type: ApplicationFiled: August 4, 2008Publication date: February 12, 2009Applicant: Recordati Ireland LimitedInventors: Amedeo Leonardi, Gianni Motta, Carlo Riva, Elena Poggesi, Davide Graziani, Matteo Longhi
-
Publication number: 20090042919Abstract: A method of modulating the activity of the GPR119 G protein-coupled receptor comprising administering to a mammalian patient in need thereof a therapeutically effective amount of at least one compound of Formula I or Formula IA and, optionally, an additional therapeutic agent.Type: ApplicationFiled: July 16, 2008Publication date: February 12, 2009Inventors: Dean A. Wacker, Karen A. Rossi, Ying Wang
-
Publication number: 20090042901Abstract: The present invention relates to an agent for the prevention/therapy of a disease caused by keratinocyte growth, which comprises, as an active ingredient, a compound represented by General Formula (1): wherein A represents a group selected from groups of the following formulas: X represents CH or N; Y represents CH2 or C?O; Z represents CH or N; R1 represents an alkoxy group; R2 and R3 each independently represent an alkyl group; R4 represents an alkyl group, and a group of the following formula: R5 each independently represent an alkoxy group or an alkylthio group; m represents an integer from 1 to 3; n represents an integer of 1 or 2; and o represents an integer of 1 or 2, or a salt thereof, or a solvate of the compound or the salt.Type: ApplicationFiled: February 1, 2006Publication date: February 12, 2009Applicant: KOWA CO., LTD.Inventors: Toshiyuki Edano, Yuichiro Tabunoki, Tomoyuki Koshi
-
Publication number: 20090036466Abstract: The present invention concerns amino-benzimidazoles having inhibitory activity on the replication of the respiratory syncytial virus and having the formula their prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms wherein Q is Ar1 or C1-6alkyl substituted with one or more substituents selected from trifluoromethyl, C3-7cycloalkyl, Ar2, hydroxy, C1-4alkoxy, C1-4alkylthio, Ar2-oxy-, Ar2-thio-, Ar2(CH2)noxy, Ar2(CH2)nthio, hydroxycarbonyl, aminocarbonyl, C1-4alkylcarbonyl, Ar2-carbonyl, C1-4alkoxycarbonyl, Ar2(CH2)ncarbonyl, aminocarbonyloxy, C1-4alkylcarbonyloxy, Ar2-carbonyloxy, Ar2(CH2)ncarbonyloxy, hydroxy-C2-4-alkyloxy, C1-4alkoxycarbonyl(CH2)noxy, mono- or di(C1-4alkyl)-aminocarbonyl, mono- or di(C1-4alkyl)aminocarbonyloxy, aminosulfonyl, mono- or di(C1-4alkyl)aminosulfonyl, dioxolanyl optionally substituted with one or two C1-6alkyl radicals, and a heterocycle selected from pyrrolidinyl, pyrrolyl, dihydropyrrolyl, thiazolidinyl, imidazolyl, triazoType: ApplicationFiled: December 20, 2004Publication date: February 5, 2009Inventors: Jean-Francois Bonfanti, Koenraad Jozef Lodewijk Andries, Frans Eduard Janssens, Francois Maria Sommen, Jerome Emile Georges Guillemont, Jean Fernand Armand Lacrampe
-
Publication number: 20090036459Abstract: The present invention relates to a class of melanocortin MCR4 agonists of general formula (I) wherein the variables and substituents are as defined herein and especially to selective MCR4 agonist compounds, to their use in medicine, particularly in the treatment of sexual dysfunction and obesity, to intermediates useful in their synthesis and to compositions containing them.Type: ApplicationFiled: February 19, 2007Publication date: February 5, 2009Inventors: Mark David Andrews, Alan Daniel Brown, Mark Ian Lansdell, Nicholas William Summerhill
-
Publication number: 20090036420Abstract: The present invention relates to methods of treating CNS disorders with a compound of formula I wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined in the specification and pharmaceutically acceptable acid addition salts thereof.Type: ApplicationFiled: July 28, 2008Publication date: February 5, 2009Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
-
Publication number: 20090036442Abstract: Disclosed are N-aroyl cyclic amine derivatives having the formula: where the variables are as define herein, and their use as pharmaceuticals, specifically as orexin receptor antagonists.Type: ApplicationFiled: October 29, 2007Publication date: February 5, 2009Inventors: Clive Leslie BRANCH, Wai Ngor Chan, Amanda Johns, Christopher Norbert Johnson, David John Nash, Riccardo Novelli, Jean-Pierre Pilleux, Roderick Alan Porter, Rachel Elizabeth Anne Stead, Geoffrey Stemp
-
Publication number: 20090036429Abstract: Chemical agents, such as derivatives of hydroxypiperidine moieties, and similar heterocyclic ring structures, including salts thereof, that act as anti-cancer and anti-tumor agents, especially where such agents modulate the activity of enzymes and structural polypeptides present in cells, such as cancer cells, or where the agents modulate levels of gene expression in cellular systems, including cancer cells, are disclosed, along with methods for preparing such agents, as well as pharmaceutical compositions containing such agents as active ingredients and methods of using these as therapeutic agents.Type: ApplicationFiled: February 16, 2007Publication date: February 5, 2009Inventors: Norman E. Ohler, Jeffrey W. Watthey, Qin Zong, Paul Young, Kathryn J. Strand
-
Publication number: 20090030012Abstract: The invention encompasses compounds of Formula I or pharmaceutically acceptable salts thereof, which are modulators of the CXCR3 chemokine receptor function useful for the treatment or prevention of pathogenic inflammatory processes, autoimmune diseases or graft rejection processes. Methods of use and pharmaceutical compositions are also encompassed.Type: ApplicationFiled: February 20, 2007Publication date: January 29, 2009Inventors: Alan D. Adams, Conrad Santini
-
Publication number: 20090030040Abstract: The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders.Type: ApplicationFiled: January 25, 2008Publication date: January 29, 2009Inventors: Michael F. Parker, Joanne J. Bronson, Mark V. Silva, Kevin W. Gillman
-
Publication number: 20090029986Abstract: Disclosed are N-aroyl cyclic amine derivatives having the formula: wherein the substituent variables are as defined herein, and their use as pharmaceuticals.Type: ApplicationFiled: October 29, 2007Publication date: January 29, 2009Inventors: Clive Leslie BRANCH, Steven Coulton, Amanda Johns, Christopher Norbert Johnson, Roderick Alan Porter, Geoffrey Stemp, Kevin Thewlis
-
Patent number: 7482468Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: n is 2-5; R is R3-aryl, R3-heteroaryl, R3-cycloalkyl, R3-heterocycloalkyl, alkyl, haloalkyl, —OR4, —SR4 or —S(O)1-2R5; R1 and R2 are H or optionally substituted phenyl or optionally substituted and X is —O— or —S—; or R1 and R2, together with the carbon atoms to which they are attached form optionally substituted and X is —O—, —S— or —NR7—; Z is and the remaining variables are as defined in the specification; also disclosed are pharmaceutical compositions comprising the compounds of formula I; also disclosed are methods of treating allergy, allergy-induced airway responses, congestion, obesity and metabolic syndrome using the compounds of Formula I, as well as combinations with other drugs useful for treating those diseases.Type: GrantFiled: January 19, 2006Date of Patent: January 27, 2009Assignee: Schering CorporationInventors: Robert G. Aslanian, Wing C. Tom, Xiaohong Zhu
-
Publication number: 20090023702Abstract: Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR 119 G protein-coupled receptor modulator therapy. These novel compounds have the structure Formula I or Formula IA.Type: ApplicationFiled: July 16, 2008Publication date: January 22, 2009Inventors: Dean A. Wacker, Karen A. Rossi, Ying Wang
-
Publication number: 20090023733Abstract: The present invention provides a compound of a formula (I): [Chemical formula should be inserted here. Please see paper copy] wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) mediated disease state.Type: ApplicationFiled: March 6, 2007Publication date: January 22, 2009Inventors: Peter Cage, Mark Furber, Christopher Luckhurst, Matthew Perry, Brian Springthorpe
-
Patent number: 7479491Abstract: The invention relates to substituted anthranylalkyl and -cycloalkyl amides of general formula (I) and to their use as medicaments for treating diseases caused by persistent angiogenesis.Type: GrantFiled: September 21, 2004Date of Patent: January 20, 2009Assignee: Novartis AGInventors: Dieter Seidelmann, Martin Krueger, Eckhard Ottow, Andreas Huth, Karl-Heinz Thierauch, Andreas Menrad, Martin Haberey
-
Patent number: 7479559Abstract: The present invention relates to novel benzyl(idene)-lactam derivatives, compounds of the formula I wherein R1 is a group of the formula G1 or G2 depicted below, wherein R1, R3, R6, R13 X, a, n and m are as defined herein, their pharmaceutically acceptable salts, and pharmaceutical compositions which include selective antagonists, inverse agonists and partial agonists of serotonin 1 (5-HT1) receptors, specifically, of one or both of the 5-HT1A and 5-HT1B receptors. The compounds of the invention are useful in treating or preventing depression, anxiety, obsessive compulsive disorder (OCD) and other disorders for which a 5-HT1 agonist or antagonist is indicated and have reduced potential for cardiac side effects, in particular QTc prolongation.Type: GrantFiled: March 17, 2005Date of Patent: January 20, 2009Assignee: Pfizer Inc.Inventors: Michael Aaron Brodney, Stephane Caron, Christopher John Helal, Jeffrey W. Raggon, Yong Tao, Nga M. Do
-
Publication number: 20090012082Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity.Type: ApplicationFiled: November 3, 2005Publication date: January 8, 2009Applicant: CURIS, INC.Inventors: Olivin M. Guicherit, Edward Andrew Boyd, Judith Boyd, Shirley Ann Brunton, Stephen Price, John Harry Alexander Stibbard, Colin H. MacKinnon
-
Publication number: 20090012083Abstract: Disclosed are N-aroyl cyclic amine derivatives having the formula: where the variables are as define herein, and their use as pharmaceuticals, specifically as orexin receptor antagonists.Type: ApplicationFiled: October 29, 2007Publication date: January 8, 2009Inventors: Clive Leslie BRANCH, Wai Ngor Chan, Amanda Johns, Christopher Norbert Johnson, David John Nash, Riccardo Novelli, Jean-Pierre Pilleux, Roderick Alan Porter, Rachel Elizabeth, Anne Stead, Geoffrey Stemp
-
Publication number: 20090012122Abstract: Disclosed are N-aroyl cyclic amine derivatives having the formula: where the variables are as define herein, and their use as pharmaceuticals, specifically as orexin receptor antagonists.Type: ApplicationFiled: October 30, 2007Publication date: January 8, 2009Inventors: Clive Leslie BRANCH, Wai Ngor Chan, Amanda Johns, Christopher Norbert Johnson, David John Nash, Riccardo Novelli, Jean-Pierre Pilleux, Roderick Alan Porter, Rachel Elizabeth, Anne Stead, Geoffrey Stemp
-
Publication number: 20090005415Abstract: Salts of 1,2-diarylimidazole-4-carboxamides and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: September 12, 2006Publication date: January 1, 2009Inventors: Matti Ahlqvist, Leifeng Cheng, Robert Lundqvist, Henrik Sorensen
-
Publication number: 20090005567Abstract: A process and new oxazolinic intermediates for the preparation of 4-(8-chloro-5,6-dihydro-11H-benzo-[5,6]-clohepta-[1,2-b]-pyridin-11-ylide-ne)-1-piperidinecarboxylic acid ethyl ester (loratadine) is described. The process starts from 2-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)-3-methyl-pyridine, a new intermediate to obtain loratadine. 2-(4,4-dimethyl-4,5-dihydro-oxazol-2-yl)-3-methyl-pyridine is condensed with 3-chloro-benzyl-chloride and the resultant product is treated with Grignard reagent of 4-chloro-N-methyl-piperidine. [3-(2-(3-chloro-phenyl)-ethyl]-pyridin-2-yl-]-1-(methyl-piperidin-4-yl)-methanone is obtained for subsequent hydrolysis. Starting from this last compound it is possible to obtain loratadine with known methods.Type: ApplicationFiled: September 9, 2008Publication date: January 1, 2009Applicant: ZaCH System S.p.A.Inventors: Vincenzo CANNATA, Livius Cotarca, Ivan Michieletto, Stefano Poli
-
Publication number: 20090005416Abstract: The present invention relates to a compound of the Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3A, R3B, R4, R5, X, m, and n are as defined herein. Such novel benzamidazole derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: June 19, 2008Publication date: January 1, 2009Inventors: Michael J. Munchhof, Lawrence A. Reiter, Susan D. La Greca, Christopher S. Jones, Qifang Li
-
Publication number: 20090005353Abstract: The present invention relates to certain novel compounds of the formula (I) to processes for preparing such compounds, to their the utility in modulation of nuclear hormone receptors Liver X Receptor (LXR) ? (NR1H3) and/or ? (NR1H2) and in treating and/or preventing clinical conditions including cardiovascular diseases such as atherosclerosis; inflammatory diseases, Alzheimer's disease, lipid disorders (dyslipidemias) whether or not associated with insulin resistance, type 2 diabetes and other manifestations of the metabolic syndrome, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: January 9, 2006Publication date: January 1, 2009Applicant: AstraZeneca ABInventors: Anders Broo, Robert Judkins, Lanna Li, Eva-Lotte Lindstedt-Alstermark, Pernilla Sandberg, Marianne Swanson, Lars Weidolf, Kay Brickmann, Patrik Holm