The Nitrogen Is Bonded Directly To A -c(=x)- Group, Wherein X Is Chalcogen Patents (Class 549/441)
-
Patent number: 7776922Abstract: The invention relates to substituted [(phenylethanoyl)amino]benzamides and methods for their preparation, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, in particular of inflammatory disorders such as, for example, cutaneous, respiratory tract and cardiovascular disorders such as, for example, arteriosclerosis and coronary heart disease.Type: GrantFiled: November 17, 2005Date of Patent: August 17, 2010Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Ulf Brüggemeier, Petros Gatsios, Mark Meininghaus, Leila Telan, Elisabeth Woltering, Martina Wuttke, Hartmut Beck, Nils Griebenow, Frank Süβmeier, Niels Svenstrup, Axel Kretschmer, Marcus Bauser, Johannes Köbberling, Wahed Moradi, Siegfried Zaiss, Claudia Hirth-Dietrich, Barbara Albrecht
-
Publication number: 20100113423Abstract: The present disclosure provides compounds that function as modulators of aldehyde dehydrogenase (ALDH) enzymatic activity, as well as compositions and formulations comprising the compounds. The present disclosure provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition.Type: ApplicationFiled: October 19, 2009Publication date: May 6, 2010Inventors: Daria Mochly-Rosen, Che-Hong Chen, Wenjin Yang
-
Publication number: 20100093733Abstract: Compounds of formula (I): or pharmaceutically acceptable salts and esters thereof, are useful for the treatment of obesity, type II diabetes and the metabolic syndrome.Type: ApplicationFiled: February 15, 2008Publication date: April 15, 2010Applicant: PROSIDION LIMITEDInventors: Oscar Barba, Graham Dawson, William Gattrell, Martin James Procter, Chrystelle Marie Rasamison, Colin Peter Sambrook-Smith, Philippe Wong-Kai-In
-
Patent number: 7691902Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: GrantFiled: December 28, 2006Date of Patent: April 6, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara S. Hadida Ruah, Mark Miller, Peter D. J. Grootenhuis, Brian Bear, Jason McCartney
-
Publication number: 20090280499Abstract: The invention provides a hapten, an immunogen comprising the hapten coupled to an antigenicity-conferring carrier material, a conjugate comprising the hapten coupled to a labelling agent, as well as, antibodies raised against the aforementioned immunogen and capable of binding with MDMA.Type: ApplicationFiled: April 3, 2007Publication date: November 12, 2009Inventors: Robert Ivan McConnell, Elouard Benchikh, Stephen Peter Fitzgerald, John Victor Lamont
-
Patent number: 7601712Abstract: A compound represented by formula (I) wherein the symbols in the formula are the same meanings as those in specification, salts thereof, solvates thereof, or prodrugs thereof binds to DP receptor and shows antagonistic activity for DP receptor. Thus, it is useful for prevention and/or treatment of diseases such as allergic disease (e.g., allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, urticaria, eczema, diseases accompanied by itch (e.g., atopic dermatitis and urticaria), diseases (e.g., cataract, retinal detachment, inflammation, infection and sleeping disorders) which is generated secondarily as a result of behavior accompanied by itch (e.g.Type: GrantFiled: September 16, 2004Date of Patent: October 13, 2009Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Atsushi Naganawa, Maki Iwahashi, Atsushi Kinoshita, Atsushi Shimabukuro, Seiji Ogawa, Koji Yano, Kaoru Kobayashi, Yutaka Okada, Yoko Kishida, Shouji Kawauchi, Kohki Tsukamoto, Yoko Matsunaga, Fumio Nambu
-
Publication number: 20090253684Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, COPD.Type: ApplicationFiled: December 2, 2008Publication date: October 8, 2009Inventors: Romyr Dominique, Robert Alan Goodnow, JR., Agnieszka Kowalczyk, Qi Qiao, Achyutharao Sidduri, Jefferson Wright Tilley
-
Publication number: 20090110796Abstract: The present invention relates to the use of a compound or a mixture consisting of two or more compounds or containing one or more compounds selected from the group consisting of compounds of Formulae (I) and (ent-I) wherein in Formulae (I) and (ent-I) the following applies: the aromatic radical Ar is selected from the group consisting of: wherein in the aromatic radicals A and B the following applies: R1 and R2 are selected independently of one another from the group consisting of H, OH, OCH3, OCH2CH3, OCH(CH3)2, COOCH3, COOCH2CH3, COOCH(CH3)2, or R1 and R2 are adjacent and jointly form an OCH2O group, and wherein in the aromatic radical C the following applies: X is O or S as a flavoring substance or flavoring substance mixture.Type: ApplicationFiled: October 30, 2008Publication date: April 30, 2009Applicant: SYMRISE GmbH & Co. KGInventors: Michael Backes, Tobias Vossing, Ingo Wohrle
-
Publication number: 20090099239Abstract: The present invention relates to novel compounds and compositions having antiviral activity. The invention also relates to methods for the therapeutic or prophylactic treatment of viral infections in mammals.Type: ApplicationFiled: June 23, 2006Publication date: April 16, 2009Inventors: Gary Dinneen Ewart, Wayne Morris Best
-
Publication number: 20090082431Abstract: The present invention provides compounds that function as modulators of mitochondrial aldehyde dehydrogenase-2 (ALDH2) activity; and pharmaceutical compositions comprising the compounds. The present invention provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition. The present invention further provides assays for identifying agonists of ALDH2.Type: ApplicationFiled: March 7, 2008Publication date: March 26, 2009Inventors: Daria Mochly-Rosen, Che-Hong Chen, Xiaohu Ouyang
-
Publication number: 20080312237Abstract: Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.Type: ApplicationFiled: July 18, 2008Publication date: December 18, 2008Inventors: Michael G. Kelly, Satyanarayana Janagani, Ravindra B. Upasani
-
Patent number: 7423154Abstract: An asymmetric synthesis of diarylmethylpiperazines is described. The synthetic route enables preparation of a variety of enatiomerically pure amines with different N-alkyl groups. The invention includes an asymmetric addition of organometallic compounds to chiral sulfinimine to give adducts in predominantly one diastereomer can subsequently be transferred into pure enantiomers of by cleavage of the chiral auxilliary which is followed by synthesis of the piperazine ring by alkylation procedures.Type: GrantFiled: November 22, 2005Date of Patent: September 9, 2008Assignee: AstraZeneca ABInventors: William Brown, Niklas Plobeck
-
Publication number: 20080194650Abstract: The invention provides well-defined aryl fluoroethyl ureas that are useful as selective alpha2 adrenergic agonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of alpha2 adrenergic receptors.Type: ApplicationFiled: December 5, 2007Publication date: August 14, 2008Inventors: Ken Chow, Wenkui K. Fang, Evelyn G. Corpuz, Daniel W. Gil, Michael E. Garst
-
Patent number: 7291621Abstract: Substituted biaryl amides of Formula I are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5a receptor activation in humans, domesticated companion animals and livestock animals.Type: GrantFiled: January 3, 2006Date of Patent: November 6, 2007Assignee: Neurogen CorporationInventors: Yang Gao, Andrew Thrukauf, He Zhao
-
Patent number: 7141674Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure:Type: GrantFiled: October 21, 2003Date of Patent: November 28, 2006Assignee: Johnson & Johnson Consumer Companies, Inc.Inventors: Malcolm K. Scott, Pauline J. Sanfilippo, Louis J. Fitzpatrick, III, Richard Cordova, Kevin Pan, Joseph Meschino
-
Patent number: 7122561Abstract: The present invention provides piperine and analogues or derivatives thereof for the treatment of skin conditions treatable by stimulation of melanocyte proliferation, such as vitiligo, and also for treating skin cancer. The piperine and analogues or derivatives thereof may also be used to cosmetically promote or enhance the natural coloration of the skin.Type: GrantFiled: July 31, 2003Date of Patent: October 17, 2006Assignee: BTG International LimitedInventors: Amala Raman, Zhixiu Lin, Robert C. Hider, Radhakrishnan Venkatasamy
-
Patent number: 7119049Abstract: This invention relates to novel oxathiinecarboxamides of the formula (I) in which R, R1 and m are as defined in the disclosure, to a plurality of processes for preparing these substances and to their use for controlling unwanted micro-organisms.Type: GrantFiled: May 15, 2003Date of Patent: October 10, 2006Assignee: Bayer Cropscience AGInventors: Heiko Rieck, Ralf Dunkel, Hans-Ludwig Elbe, Ulrike Wachendorff-Neumann, Astrid Mauler-Machnik, Karl-Heinz Kuck
-
Patent number: 7078565Abstract: Disclosed are phenyl-alkylene benzamides useful as orexin antagonistsType: GrantFiled: October 30, 2002Date of Patent: July 18, 2006Assignee: SmithKline Beecham plcInventors: Wai Ngor Chan, Amanda Johns, Roderick Alan Porter, Rachel Elizabeth Anne Stead, Mythily Vimal
-
Patent number: 7067551Abstract: The present invention provides hydroxamate compounds which are deacetylase inhibitors. The compounds are suitable for pharmaceutical compositions having anti-proliferative properties.Type: GrantFiled: November 9, 2004Date of Patent: June 27, 2006Assignee: Novartis AGInventors: Stacy W Remiszewski, Kenneth W Bair, Richard W Versace, Lawrence B Perez, Michael A Green, Lidia C Sambucetti, Sushil Sharma
-
Patent number: 7026339Abstract: The present invention relates to compounds, process for their synthesis, compositions and methods for the treatment and prevention of hepatitis C virus (HCV) infection. In particular, the present invention provides novel compounds, pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment or prevention of HCV infection. The present invention also provides processes and intermediates for the synthesis of these compounds.Type: GrantFiled: November 3, 2004Date of Patent: April 11, 2006Inventors: Fan Yang, Bo Zhang, Nancy Anne Wicnienski, Jeffrey Allen Pfefferkorn, Meredith L. Greene, Ke Chen, Richard A. Nugent, Matthew Todd Reding, Robert Charles Kelly, Mark A. Mitchell, Lee A. Funk, Richard Frederick Heier, III, Rebecca Merry Anderson
-
Patent number: 7019028Abstract: The invention relates to compounds of the formula (I) process for their preparation starting from the plant Beilschmiedia fulva, PLA 101037, and the use thereof for producing a medicament, in particular for the treatment of allergic disorders, of asthmatic disorders, of inflammatory concomitant symptoms of asthma and/or of diseases which can be treated by inhibiting c-maf and NFAT.Type: GrantFiled: July 25, 2003Date of Patent: March 28, 2006Assignees: Aventis Pharma Deutschland GmbH, Aventis Pharmaceuticals Inc.Inventors: Claudia Eder, Herbert Kogler, Sabine Haag-Richter
-
Patent number: 7019024Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 9, 2001Date of Patent: March 28, 2006Assignee: Allelix Neuroscience Inc.Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
-
Patent number: 6878706Abstract: Compounds according to the following formula (I): wherein the variables Q and R1 to R6 are as described herein, which reversibly inhibit the cysteine proteases, such as cathepsins K, S, F, L and B; pharmaceutical compositions containing such compounds, and method of treating diseases and pathological conditions exacerbated by these cysteine proteases such as, but not limited to rheumatoid arthritis, multiple sclerosis and other autoimmune diseases, osteoporosis, asthma, Alzheimer's disease, atherosclerosis and endometriosis.Type: GrantFiled: March 27, 2003Date of Patent: April 12, 2005Assignee: Boehringer Ingelheim Pharmaceuticals Inc.Inventors: Thomas A. Gilmore, Eugene Richard Hickey, Weimin Liu, Peter Allen Nemoto, Denice M. Spero
-
Patent number: 6858648Abstract: A compound having the following Formula: wherein R1, R2, Z, and Y are defined herein, and methods of preparation and application for treating mental disorders and inflammation are provided therewith.Type: GrantFiled: July 10, 2003Date of Patent: February 22, 2005Assignees: Fudan University, Shanghai Institute of Pharmaceutical IndustryInventors: Sheng-li Pan, Fu-gang Qian, Ren Wen, Jing Xie, Jun Wang, Yi-ci Shao
-
Patent number: 6849649Abstract: The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R1 is optionally substituted C1-6alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C1-6alkoxy, —NR2R3 or —NR4SO2R5; X is the linkage —(CH2)n— or —(CH2)q—O— (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C1-4alkoxy; hydroxy; hydroxy(C1-3alkyl); C3-7cycloalkyl; carbocyclyl; heterocyclyl; or by C1-4alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R8 groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.Type: GrantFiled: October 28, 2003Date of Patent: February 1, 2005Assignee: Pfizer Inc.Inventors: Stephen Challenger, Andrew Simon Cook, Adam Thomas Gillmore, Donald Stuart Middleton, David Cameron Pryde, Alan Stobie
-
Patent number: 6767921Abstract: The subject of the present invention is the various polymorphic forms I, II, III, IV of benzyl (S,S)-2-(2-acetylsulphanylmethyl-3-benzo[1,3]dioxol-5-ylpropionyl-amino)propionate, hereinafter called Fasidotril, their methods of preparation and novel pharmaceutical compositions containing them.Type: GrantFiled: March 26, 2003Date of Patent: July 27, 2004Assignee: BioprojectInventors: Marc Capet, Gérard Coquerel, Denis Danvy, Jeanne-Marie Lecomte, Marie-Noëlle Petit, Jean-Charles Schwartz
-
Patent number: 6762318Abstract: Novel compounds that act to antagonize the action of the glucagon peptide hormone on the glucagon receptor. More particularly, it relates to glucagon antagonists or inverse agonists.Type: GrantFiled: December 3, 2002Date of Patent: July 13, 2004Assignee: Novo Nordisk A/SInventors: Janos Tibor Kodra, Peter Madsen, Jesper Lau, Anker Steen Jorgensen, Inge Thoger Christensen
-
Patent number: 6730705Abstract: The invention relates to new alkoximinoacetic acid amides, a process for their preparation and their use as agents for combating pests.Type: GrantFiled: June 30, 2000Date of Patent: May 4, 2004Assignee: Bayer AktiengesellschaftInventors: Thomas Seitz, Gerd Hänssler, Klaus Stenzel
-
Publication number: 20040053994Abstract: A compound having the following Formula: 1Type: ApplicationFiled: July 10, 2003Publication date: March 18, 2004Inventors: Sheng-Ii Pan, Fu-gang Qian, Ren Wen, Jing Xie, Jun Wang, Yi-ci Shao
-
Patent number: 6680391Abstract: The present invention provides piperine and analogues or derivatives thereof for the treatment of skin conditions treatable by stimulation of melanocyte proliferation, such as vitiligo, and also for treating skin cancer. The piperine and analogues or derivatives thereof may also be used to cosmetically promote or enhance the natural coloration of the skin.Type: GrantFiled: January 22, 2002Date of Patent: January 20, 2004Assignee: BTG International LimitedInventors: Amala Raman, Zhixiu Lin, Robert C. Hider, Radhakrishnan Venkatasamy
-
Patent number: 6677456Abstract: This invention is to provide a novel taxol derivative useful as an antitumor compound having respective substituent groups, represented by the following formula (I) which can be orally administeredType: GrantFiled: March 6, 2002Date of Patent: January 13, 2004Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Tsunehiko Soga, Kouichi Uoto, Yasuyuki Takeda
-
Patent number: 6660756Abstract: The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R1 is optionally substituted C1-6alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C1-6alkoxy, —NR2 R3 or —NR4SO2R5; X is the linkage —(CH2)n— or —(CH2)q—O— (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C1-4alkoxy; hydroxy; hydroxy(C1-3alkyl); C3-7cycloalkyl; carbocyclyl; heterocyclyl; or by C1-4alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R8 groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.Type: GrantFiled: March 12, 2002Date of Patent: December 9, 2003Assignee: Pfizer Inc.Inventors: Stephen Challenger, Andrew Simon Cook, Adam Thomas Gillmore, Donald Stuart Middleton, David Cameron Pryde, Alan Stobie
-
Patent number: 6638970Abstract: Novel compounds of the general formula: and pharmaceutically acceptable acid addition salts thereof, wherein the compounds are useful in therapy to protect skeletal muscles against damage resulting from trauma or to protect skeletal muscles subsequent to muscle or systemic diseases such as intermittent claudication, to treat shock conditions, to preserve donor tissue and organs used in transplants, in the treatment of cardiovascular diseases including atrial and ventricular arrhythmias, Prinzmetal's (variant) angina, stable angina, and exercise induced angina, congestive heart disease, and myocardial infarction.Type: GrantFiled: February 22, 2001Date of Patent: October 28, 2003Assignee: CV Therapeutics, Inc.Inventors: Elfaith Elzein, Jeff Zablocki, Tim Marquart
-
Patent number: 6603044Abstract: The present invention provides a phthalamide derivative of the formula (I): wherein A1 is (substituted) C1-C8 alkylene, (substituted) C3-C8 alkenylene, (substituted) C3-C8 alkynylene, etc., R1 is H, (halo) C3-C6 cycloalkyl, (substituted) phenyl, (substituted) heterocycle, —A2—R4, etc., R2 and R3 are H, C3-C6 cycloalkyl, —A2—R4, etc., A2 is —C(═O)—, —C(═S)— or —C(═NR5)—, R4 is H, alkyl, (substituted) phenyl, (substituted) heterocycle, etc., X and Y are halogen, cyano, nitro, (halo) C1-C6 alkyl, (halo) C1-C6 alkoxy, etc., l is 0-4, m is 0-5, n is 0-2; and an agrohorticultural insecticide containing said compound as active ingredient and exhibiting an excellent insecticidal effect.Type: GrantFiled: November 29, 1999Date of Patent: August 5, 2003Assignee: Nihon Nohyaku Co., Ltd.Inventors: Masanori Tohnishi, Hayami Nakao, Eiji Kohno, Tateki Nishida, Takashi Furuya, Toshiaki Shimizu, Akira Seo, Kazuyuki Sakata, Shinsuke Fujioka, Hideo Kanno
-
Patent number: 6515124Abstract: Aromatic dehydroamino acids are disclosed that are active as LFA-1 arnagonists This activity enables these compounds to prevent inflammation which is a consequence of T cell activation and accordingly reduce or eliminate inflammatory skin disease psoriasis.Type: GrantFiled: January 5, 2001Date of Patent: February 4, 2003Assignee: Hoffman-La Roche Inc.Inventors: Nader Fotouhi, Paul Gillespie, Robert William Guthrie, Sherrie Lynn Pietranico-Cole, Weiya Yun
-
Patent number: 6509369Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure:Type: GrantFiled: January 8, 2002Date of Patent: January 21, 2003Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Malcolm K. Scott, Pauline J. Sanfilippo, Louis J. Fitzpatrick, III, Richard Cordova, Kevin Pan, Joseph Meschino
-
Patent number: 6509379Abstract: Phenylacetic acid derivatives of the formula I where the variables are as disclosed herein, their salts, processes and intermediates for their preparation, and their use for controlling harmful fungi and animal pests.Type: GrantFiled: April 23, 1998Date of Patent: January 21, 2003Assignee: BASF AktiengesellschaftInventors: Herbert Bayer, Hubert Sauter, Klaus Oberdorf, Wassilios Grammenos, Thomas Grote, Reinhard Kirstgen, Bernd Müller, Ruth Müller, Franz Röhl, Eberhard Ammermann, Volker Harries, Gisela Lorenz, Siegfried Strathmann, Norbert Götz, Albrecht Harreus
-
Patent number: 6472414Abstract: Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure including pharmaceutically acceptable salts thereof or prodrug esters thereof, wherein q is 0, 1 or 2; Rx is H, alkyl, aryl or halogen; A is (1) a bond; (2) —O—; or (3) B is: and wherein L2, L1, R1, R2, R3, R3′, R3a, R3b, R4, R4′, R5, X, are as defined herein.Type: GrantFiled: May 18, 1999Date of Patent: October 29, 2002Assignee: Bristol-Myers Squibb CompanyInventors: Scott A. Biller, John K. Dickson, R. Michael Lawrence, David R. Magnin, Michael A. Poss, Jeffrey A. Robl, William A. Slusarchyk, Richard B. Sulsky, Joseph A. Tino
-
Patent number: 6458801Abstract: A compound of the formula wherein the substituents are as defined in the specification and its pharmaceutically acceptable salts and its prodrug useful for treating osteoporosis.Type: GrantFiled: June 29, 2001Date of Patent: October 1, 2002Assignees: Aventis Pharma S.A., Genentech, Inc.Inventors: Denis Carniato, Thomas R. Gadek, Jean-Francois Gourvest, Jochen Knolle, Anurschirwan Peyman, Sarah C. Bodary
-
Publication number: 20020103192Abstract: Substituted trifluoromethyl ketones, ketooxazoles, ketoamides, ketoesters, and diketones having the formula 1Type: ApplicationFiled: March 14, 2001Publication date: August 1, 2002Inventors: Michael L. Curtin, Steven K. Davidsen, Robin R. Frey, Howard R. Heyman, Michael R. Michaelides, Anil Vasudevan, Carol K. Wada
-
Patent number: 6376538Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.Type: GrantFiled: September 19, 1997Date of Patent: April 23, 2002Assignee: Biogen, Inc.Inventors: Steven P. Adams, Ko-Chung Lin, Wen-Cherng Lee, Alfredo C. Castro, Craig N. Zimmerman, Charles E. Hammond, Yu-Sheng Liao, Julio Hernan Cuervo, Juswinder Singh
-
Patent number: 6372779Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure:Type: GrantFiled: December 28, 1998Date of Patent: April 16, 2002Assignee: Ortho Pharmaceutical CorporationInventors: Malcolm K. Scott, Pauline J. Sanfilippo, Louis J. Fitzpatrick, III, Richard Cordova, Kevin Pan, Joseph Meschino
-
Patent number: 6344570Abstract: Compounds of formula (II) where R1 is in the para or meta position and is (A); R2 and R3 are each independently selected from hydrogen, nitro, C1-6alkyl, C3-6cycloalkyl, C2-6alkenyl, C2-6alkynyl, C1-4alkoxyl, C1-6alkylamino, C1-6dialkylamino, C1-6akylC1-4alkoxyl, C1-6alkylaminoC1-6alkyl, amino, cyano, halogeno, trifluoromethyl, —CO2R12 and —CONR12R13, where R12 and R13 are independently selected from hydrogen or C1-6alkyl, or R2 and R3 together with the phenyl to which they are attached form a 9 or 10 membered bicyclic ring system; R4 is C1-4alkyl; R5 is selected from hydrogen and C1-4alkyl; R6 is selected from C1-6alkyl, C1-4alkyl(C4-6)cycloalkyl, C1-6alkyl(C1-6)alkoxyl, C1-6alkylS(C1-6)alkyl, C1-4alkylsulphonyl(C1-4)alkyl; (B) where q is an integer from 1 to 6 and R14 is halogeno; R7 is selected from C1-6alkyl, C1-8alkoxylcarbonyl, C2-6alkenyl, 1,3-benzodioxol-5-yl and aryl each optionally substituted by one or more substituents selected from C1-4alkoxy, C1-6alkyl, cyano, halogType: GrantFiled: July 11, 2000Date of Patent: February 5, 2002Assignee: AstraZeneca UK LimitedInventors: David R Brittain, Craig Johnstone
-
Patent number: 6340704Abstract: The present invention provides a compound represented by the formula: wherein R1 is an amino group which may be substituted; R2 is a hydrogen atom or a lower alkyl group which may be substituted; X is a methyne group which may be substituted or N(O)m (m is 0 or 1); a ring A is a homo- or hetero-cycle which is substituted by a halogen atom, lower alkyl, lower alkoxy or lower alkylenedioxy; and a ring B is a homo- or hetero-cycle which may be substituted; or a salt thereof, which exhibits excellent cell differentiation-inducing action and cell differentiation-inducing factor action-enhancing action, and is useful in the treatment and prevention of various nerve diseases or bone/joint diseases.Type: GrantFiled: July 19, 1999Date of Patent: January 22, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Shogo Marui, Masatoshi Hazama, Kohei Notoya, Koki Kato
-
Patent number: 6323227Abstract: This invention relates to compounds of formula which inhibit Factor Xa, to pharmaceutical compositions containing the compounds, and to the use of the compounds for the treatment of patients suffering from conditions which can be ameliorated by the administration of an inhibitor of Factor Xa.Type: GrantFiled: February 26, 1999Date of Patent: November 27, 2001Assignee: Aventis Pharmaceuticals Products Inc.Inventors: Scott I. Klein, Kevin R. Guertin, Alfred P. Spada, Heinz W. Pauls, Yong Gong, Daniel G. McGarry
-
Publication number: 20010039357Abstract: The present invention provides N-alkylaspartyl dipeptideester compounds and salts thereof, such as N-[N-[3-(3-hydroxy-4-methoxyphenyl)-3-methylbutyl]-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester, which provide high degrees of sweetness in comparison to conventional products, compositions and products containing the novel aspartyl dipeptide ester compounds and method of producing the novel aspartyl dipeptide ester compounds.Type: ApplicationFiled: March 16, 2001Publication date: November 8, 2001Applicant: AJINOMOTO CO., INC.Inventors: Yusuke Amino, Kazuko Yuzawa, Tadashi Takemoto, Ryoichiro Nakamura
-
Publication number: 20010036961Abstract: Novel compounds of the general formula: 1Type: ApplicationFiled: February 22, 2001Publication date: November 1, 2001Inventors: Elfatih Elzein, Jeff Zablocki, Tim Marquart
-
Patent number: 6306873Abstract: This invention relates to compounds of general formula (I): in which Ar is a group selected from: A1, A2, B, C, D, E, Q1-Q3, R1-R9, Z1 and Z2 are as defined in the disclosure, and Y represents carboxy or an acid bioisostere. These compounds inhibit the production or physiological effects of TNF and inhibit cyclic AMP phosphodiesterase. The invention is also directed to pharmaceutical compositions comprising compounds of formula (I), their pharmaceutical use and methods for their preparation.Type: GrantFiled: July 20, 1999Date of Patent: October 23, 2001Assignee: Aventis Pharmaceuticals Products Inc.Inventors: Christopher J. Burns, Richard Labaudiniere, Stephen Condon, Robert D. Groneberg, Rose M. Mathew, Joseph M. Salvino
-
Patent number: 6303799Abstract: Novel aryl derivatives comprising an aryl olefin moiety linked to a non-nucleosidic backbone moiety are disclosed. The resulting molecules are typically used as photoactivated crosslinking groups when incorporated into oligonucleotides to crosslink nucleic acid strands.Type: GrantFiled: November 10, 1998Date of Patent: October 16, 2001Assignee: NaxcorInventors: Peter C. Cheng, David Albagli, Michael L. Wood
-
Patent number: 6271399Abstract: Indane and indene compounds are described which are endothelin receptor antagonists.Type: GrantFiled: June 2, 1995Date of Patent: August 7, 2001Assignee: SmithKline Beecham CorporationInventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff