The Additional Hetero Ring Is A Cyclo In A Polycyclo Ring System Patents (Class 548/364.4)
-
Patent number: 7514461Abstract: The invention relates to novel chroman derivatives, stereoisomers and pharmaceutically acceptable salts of Formula I wherein the substituents are as defined in the specification. They are useful in the treatment of disorders mediated by lipoxygenase, such as immune diseases, respiratory diseases and cardiovascular diseases, as well as in the treatment of neurodegenerative disorders and/or mitochondrial disorders. They are also useful in the manufacture of pharmaceutical formulations for the treatment of such conditions.Type: GrantFiled: September 15, 2004Date of Patent: April 7, 2009Assignee: Edison Pharmaceuticals, Inc.Inventors: Bing Wang, Gail Walkinshaw, Sekhar Boddupalli, Arkadij M. Elizarov, Xianming Jin, Xianfeng Li, Donald R. James, Jiangao Song, Jian Chen, Wei Zhang
-
Publication number: 20090082308Abstract: The present invention relates to a novel class of benzothiophene amide derivatives. The hydroxamic acid compounds can be used to treat cancer. The benzothiophene amide compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: April 14, 2006Publication date: March 26, 2009Inventors: Jed Lee Hubbs, Dawn M. Mampreian, Joey L. Methot, Thomas A. Miller, Karin M. Otte, Phieng Siliphaivanh, David L. Sloman, Matthew G. Stanton, Kevin J. Wilson, David J. Witter
-
Publication number: 20090062365Abstract: The present invention relates to novel pyrazole derivatives having a positive allosteric GABAB receptor (GBR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS). The compounds are represented by the general formula (I) wherein R1, R2, R3 and Y are as defined in the description. For example, R1 may be hydrogen or alkyl, R2 may be hydrogen or alkyl, R3 may be alkoxy and Y may be a carbonylamino linked substituent containing an aryl group.Type: ApplicationFiled: December 21, 2006Publication date: March 5, 2009Inventor: Udo Bauer
-
Publication number: 20090061143Abstract: A recording layer including a novel organic compound for a high density optical recording medium is provided. The information may be recorded on the recording layer at a 2× speed or higher speed with a relatively lower writing power so that heat distribution of the recording layer in the irradiated area is not likely to become steep both in time and space. The organic compound incorporated in the recording layer has the following general chemical structural formula (I).Type: ApplicationFiled: September 5, 2007Publication date: March 5, 2009Applicant: INDUSTRIAL TECHNOLOGY RESEARCH INSTITUTEInventors: Ming-Chia Li, An-Tse Lee, Chien-Liang Huang, Chung-Ta Cheng, Kuo-Chi Chiu, Tzuan-Ren Jeng
-
Patent number: 7482449Abstract: This invention relates to a process for making spirolactone compounds analogous to formula I.Type: GrantFiled: March 19, 2008Date of Patent: January 27, 2009Assignees: Merck & Co., Inc., Banyu Pharmaceutical Co., Ltd.Inventors: Ralph P. Volante, David M. Tschaen, Steven A. Weissman, Matthew Heileman, Toshiaki Mase, Takehiko Iida, Kenji Maeda, Toshihiro Wada, Hiroki Sato, Kenichi Asakawa
-
Publication number: 20090012075Abstract: The present invention relates to a novel class of fluorinated arylamide derivatives. The instant compounds can be used to treat cancer. The fluorinated arylamide derivatives can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: January 8, 2007Publication date: January 8, 2009Inventors: Thomas A. Miller, David L. Sloman, Matthew G. Stanton, Kevin J. Wilson, David J. Witter
-
Patent number: 7468386Abstract: The present invention relates to compounds of the Formula wherein R1, R3, R4, R5, R6, R7 and R8 are as defined. Compounds of the Formula I have activity inhibiting production of A?-peptide. The invention also relates to pharmaceutical compositions and methods of treating disorders and diseases, for example, neurodegenerative and/or neurological disorders, e.g., Alzheimer's disease, in a mammal comprising compounds of the Formula I.Type: GrantFiled: July 5, 2007Date of Patent: December 23, 2008Assignee: Pfizer Inc.Inventors: Yuhpyng L. Chen, Lei Zhang
-
Patent number: 7465808Abstract: There are provided by the present invention certain pyrazole based CCK-1 receptor modulators.Type: GrantFiled: September 19, 2005Date of Patent: December 16, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Terrance D. Barrett, J. Guy Breitenbucher, Laurent Gomez, Michael D. Hack, Liming Huang, Kelly J. McClure, Magda F. Morton, Clark A. Sehon, Nigel P. Shankley
-
Publication number: 20080280875Abstract: The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein: Ring A is (4-12)-membered heterocyclyl; Ring B is a fused benzene ring selected from the group consisting of: Ring A, ring B, ring C, R1, R1a, R2, R3, R4, L2, n, t, w, and z are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of glucokinase, the method comprising administering to a mammal an effective amount of a compound of formula (I).Type: ApplicationFiled: May 9, 2007Publication date: November 13, 2008Inventors: Hao Bai, Simon Bailey, Dilip Ramakant Bhumralkar, Feng C. Bi, Fengli Guo, Mingying He, Paul Stuart Humphries, Anthony Lai Ling, Jihong Lou, Seiji Nukul, Ru Zhou
-
Patent number: 7432287Abstract: Compounds represented by formula (I): as well as their pharmaceutically acceptable salts are disclosed. The compounds are useful as glucokinase activating agents for the treatment of diabetes and related conditions. Compositions and methods of treatment are also included.Type: GrantFiled: February 26, 2004Date of Patent: October 7, 2008Assignee: Banyu Pharmeceutical Co., Ltd.Inventors: Tomoharu Iino, Noriaki Hashimoto, Hiroshi Nakashima, Keiji Takahashi, Teruyuki Nishimura, Jun-ichi Eiki
-
Publication number: 20080207725Abstract: A compound of formula (I): wherein A represents 2,3-dihydro-1-benzofuran-7-yl, 5-fluoro-2-methoxy-phenyl or 5-fluoro-2-hydroxy-phenyl; and R1 and R2 each independently represent hydrogen, fluorine or chlorine; or a physiologically functional derivative thereof.Type: ApplicationFiled: June 27, 2006Publication date: August 28, 2008Inventors: Michael David Barker, David House, Haydn Terence Jones, Simon John Fawcett MacDonald, Iain McFarlane Mclay
-
Publication number: 20080194607Abstract: The present invention relates to the use of compounds of the general Formula (I): wherein in Formula (I), R is H, alkyl, cycloalkyl, aryl or heteroaryl; R1 is H, alkyl, cycloalkyl, aryl or heteroaryl; R2 is H, alkyl, cycloalkyl, aryl or heteroaryl; A1 and A2 each independently represent an optionally substituted C1-C20-alkyl group which may contain one or more group(s) Z, or a monocyclic or polycyclic optionally substituted aromatic or non-aromatic ring system which may contain one or more group(s) X, and in case of a polycyclic ring system, said system contains at least one aromatic ring; Z is selected from the group consisting of S, O, N, NR4, CO, CO2, CS, SO or SO2 X is selected from the group consisting of S, O, N, NR4, SO or SO2;Type: ApplicationFiled: December 28, 2007Publication date: August 14, 2008Inventors: Aldo Ammendola, Katharina Aulinger-Fuchs, Astrid Gotschlich, Bernd Kramer, Martin Lang, Wael Saeb, Udo Sinks, Andreas Wuzik
-
Patent number: 7407977Abstract: There are presented compounds of the formula or a pharmaceutically acceptable salt thereof, which are useful in the treatment of diabetes, diabetic retinopathy, asthma and diarrhea.Type: GrantFiled: July 29, 2005Date of Patent: August 5, 2008Assignee: Hoffman-La Roche Inc.Inventors: Jianping Cai, Adrian Wai-Hing, Fariborz Firooznia, Kevin Richard Guertin, Lida Qi
-
Publication number: 20080153816Abstract: Indole compounds corresponding to the formula (I): as defined in the claims, pharmaceutically acceptable addition salts of such compounds, pharmaceutical compositions containing such compounds, the process for their preparation, and their use as pharmacologically active substances, especially in the treatment of hypertriglyceridemia, hyperlipidemia, hypercholesterolemia, diabetes, endothelial dysfunction, cardiovascular disease, inflammatory disease and neurodegeneration.Type: ApplicationFiled: February 28, 2008Publication date: June 26, 2008Applicant: Laboratoires Fournier S.A.Inventors: Jean BINET, Benaissa Boubia, Pierre Dodey, Christiane Legendre, Martine Barth, Olivia Poupardin-Olivier
-
Patent number: 7368569Abstract: This invention relates to a process for making spirolactone compounds analogous to formula IType: GrantFiled: October 14, 2003Date of Patent: May 6, 2008Assignees: Merck & Co., Inc., Banyu Pharmaceutical Co., Ltd.Inventors: Ralph P. Volante, David M. Tschaen, Steven A. Weissman, Matthew Heileman, Toshiaki Mase, Takehiko Iida, Kenji Maeda, Toshihiro Wada, Hiroki Sato, Kenichi Asakawa
-
Patent number: 7358248Abstract: Disclosed are compounds and pharmaceutically acceptable salts of formula (I): which are useful in the treatment of metabolic disorders related to insulin resistance, leptin resistance, or hyperglycemia. Compounds of the invention include inhibitors of Protein tyrosine phosphatases, in particular Protein tyrosine phosphatase-1B (PTP-1B), that are useful in the treatment of diabetes and other PTP mediated diseases, such as cancer, neurodegenerative diseases and the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.Type: GrantFiled: April 30, 2004Date of Patent: April 15, 2008Assignee: The Institute for Pharmaceutical Discovery LLCInventors: Darren Whitehouse, Shaojing Hu, Michael C. Van Zandt, Garrett Parker, Thomas G. Meskill
-
Patent number: 7332149Abstract: The present invention describes novel compounds of the formula: (Q)d—Ln—Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The present invention also provides novel compounds useful for imaging atherosclerosis, restenosis, cardiac ischemia, and myocardial reperfusion injury. The present invention also provides novel compounds useful for the treatment of rheumatoid arthritis. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety.Type: GrantFiled: June 21, 2000Date of Patent: February 19, 2008Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Milind Rajopadhye, John A. Barrett, Alan P. Carpenter, Jr., Edward H. Cheesman, Thomas D. Harris
-
Patent number: 7321045Abstract: The present invention describes novel compounds of the formula: (Q)d-Ln-Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The present invention also provides novel compounds useful for imaging atherosclerosis, restenosis, cardiac ischemia, and myocardial reperfusion injury. The present invention also provides novel compounds useful for the treatment of rheumatoid arthritis. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety.Type: GrantFiled: February 2, 2004Date of Patent: January 22, 2008Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Milind Rajopadhye, Thomas D. Harris, Edward H. Cheesman
-
Patent number: 7304072Abstract: Compounds represented by the general formula (I) wherein Ar1 represents an aryl or heteroaryl which may be substituted; n represents 0 or 1; T, U, V and W each independently represent a nitrogen atom or a methine group which may have a substituent selected from the group consisting of halogen, lower alkyl, hydroxy and lower alkoxy, wherein at least two of which represent said methine group; X represents methine, hydroxy substituted methine or nitrogen atom; Y represents an imino which may be substituted with lower alkyl, or oxygen; and a salt, ester or N-oxide derivative thereof. The compounds exhibit NPY antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders, central nervous system disorders, metabolic diseases, sexual and reproductive dysfunctions, gastro-intestinal disorders, respiratory disorders, inflammation or glaucoma, and the like.Type: GrantFiled: August 23, 2004Date of Patent: December 4, 2007Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Takehiro Fukami, Akio Kanatani, Akane Ishihara, Yasuyuki Ishii, Toshiyuki Takahashi, Yuji Haga, Toshihiro Sakamoto, Takahiro Itoh, Masato Chiba
-
Patent number: 7244757Abstract: The present invention relates to compounds of the Formula wherein R1, R3, R4, R5, R6, R7 and R8 are as defined. Compounds of the Formula I have activity inhibiting production of A?-peptide. The invention also relates to pharmaceutical compositions and methods of treating disorders and diseases, for example, neurodegenerative and/or neurological disorders, e.g., Alzheimer's disease, in a mammal comprising compounds of the Formula I.Type: GrantFiled: March 11, 2005Date of Patent: July 17, 2007Assignee: Pfizer IncInventors: Yuhpyng L. Chen, Lei Zhang
-
Patent number: 7235584Abstract: Novel non-psychotropic cannabinoids are disclosed and pharmaceutical compositions comprising these novel compounds are described for preventing neurotoxicity, neuroinflammation, immune or inflammatory disorders comprising as active ingredient the stereospecific (+) enantiomer, having (3S,4S) configuration of ?6 tetrahydrocannabinol type compounds. The compositions are particularly effective in alleviating and even preventing neurotoxicity due to acute injuries to the central nervous system, including mechanical trauma, compromised or reduced blood supply as may occur in cardiac arrest or stroke, or poisonings. They are also effective in the treatment of certain inflammatory disorders and chronic degenerative diseases characterized by neuronal loss and chronic pain including neuropathic pain.Type: GrantFiled: June 25, 2003Date of Patent: June 26, 2007Assignee: Pharmos CorporationInventors: Aaron Garzon, George Fink
-
Patent number: 7211597Abstract: The present invention relates to compounds of Formula I: wherein A is (CH2)m-Q-(CH2)n, wherein each CH2 may be independently substituted with one or more substitution selected from the group consisting of: hydroxy, halo, alkoxy, lower alkyl, amino, aminoalkyl, alkylamino, alkenyl, and alkynyl; B is a 5 or 6 membered heteroaryl, or aryl, optionally saturated, or optionally substituted with R1, R2, or R12; X is selected from the group consisting of: N and C; and Y and Z are independently selected from the group consisting of: N, C, CH, CR3, S, and O; compositions comprising such compounds, intermediates thereof, methods of making such compounds, and methods for treating cancer, inflammation, and inflammation-associated disorders, such as arthritis.Type: GrantFiled: September 19, 2002Date of Patent: May 1, 2007Inventors: Suzanne Metz, Michael Clare, Joyce Z. Crich, Timothy J. Hagen, Gunnar J. Hanson, He Huang, Stephen C. Houdek, Michael A. Stealey, Michael L. Vazquez, Richard M. Weier, Xiangdong Xu
-
Patent number: 7211335Abstract: A red organic light-emitting compound which has a superior heat-resistance and is capable of adjusting the color of the emitted light, and an organic light-emitting device including the same are disclosed.Type: GrantFiled: March 19, 2003Date of Patent: May 1, 2007Assignee: Neoviewkolon Co., Ltd.Inventors: Ha-Geun Hwang, Ki-Seok Kim
-
Patent number: 7208169Abstract: The invention relates to novel biphenylcarboxamides of the formula (I) in which R1, R2, m, n, R3, Y and A are as defined in the disclosure, to a plurality of processes for preparing these substances and their use for controlling unwanted microorganisms, and to novel intermediates and their preparation.Type: GrantFiled: April 16, 2003Date of Patent: April 24, 2007Assignee: Bayer CropScience LPInventors: Ralf Dunkel, Hans-Ludwig Elbe, Heiko Rieck, Robert Markert, Ulrike Wachendorff-Neumann, Astrid Mauler-Machnik, Karl-Heinz Kuck, Martin Kugler, Thomas Jaetsch
-
Patent number: 7157454Abstract: The invention relates to compounds of formula: These compounds show affinity for the bradykinin receptors with selectivity towards the B1 receptors; they may be used for the preparation of medicinal products intended for treating or preventing inflammation pathologies and persistent or chronic inflammatory diseases.Type: GrantFiled: March 27, 2002Date of Patent: January 2, 2007Assignee: Sanofi-AventisInventors: Bernard Ferrari, Jean Gougat, Yvette Muneaux, Pierre Perreaut, Lionel Sarran
-
Patent number: 7105513Abstract: The present invention relates to acylated, heteroaryl-condensed cycloalkenylamines, to pharmaceutical compositions comprising such compounds, to methods for the stimulation of the expression of endothelial NO synthase, and methods of treatment comprising administering such compounds.Type: GrantFiled: July 31, 2003Date of Patent: September 12, 2006Assignee: Sanofi-Avertis Deutschland GmbHInventors: Hartmut Strobel, Paulus Wohlfart
-
Patent number: 7034049Abstract: Compounds which are 3-amino-pyrazole derivatives represented by formula (I) wherein R is C3–C6 cycloalkyl group optionally substituted by a straight or branched C1–C6 alkyl or arylalkyl group; R1 is a straight or branched C1–C6 alkyl, C2–C4 alkenyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl, arylalkyl, arylcarbonyl, aryloxyalkyl or arylalkenyl group, each of which may be optionally further substituted as indicated in the description; or a pharmaceutically acceptable salt thereof. The compounds are useful for the treatment of cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases or neurodegenerative diseases.Type: GrantFiled: May 5, 2000Date of Patent: April 25, 2006Assignees: Pharmacia Italia S.p.A., Pharmacia & Upjohn Company LLCInventors: Paolo Pevarello, Paolo Orsini, Gabriella Traquandi, Mario Varasi, Edward L. Fritzen, Martha A. Warpehoski, Betsy S. Pierce, Maria Grabriella Brasca
-
Patent number: 6995262Abstract: The invention relates to a novel polymethine dyes containing at least one acylsulfonamido group of the formula (I) in which n, Y, A and R have the meaning given in the claims, and at least one compound of the formulae (a) to (n) given in the claims. The polymethine dyes according to the invention are suitable for use as dyes and/or labels, in particular for staining or labeling biomolecules.Type: GrantFiled: July 24, 2000Date of Patent: February 7, 2006Assignee: Bayer CropScience AGInventors: Geert Deroover, Michael Missfeldt, Lydia Simon
-
Patent number: 6958356Abstract: The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein rings D-E represent guanidine mimics, which are useful as inhibitors of factor Xa.Type: GrantFiled: March 13, 2002Date of Patent: October 25, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Patrick Y. Lam, Charles G. Clark, Celia Dominguez, John M. Fevig, Amy Qi Han, Renhua Li, Donald J. Pinto, James R. Pruitt, Mimi L. Quan
-
Patent number: 6949540Abstract: Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S are described.Type: GrantFiled: March 28, 2003Date of Patent: September 27, 2005Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Hui Cai, James P. Edwards, Steven P. Meduna, Barbara A. Pio, Jianmei Wei
-
Patent number: 6949550Abstract: The present application describes substituted-aminomethyl substituted compounds and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.Type: GrantFiled: November 26, 2002Date of Patent: September 27, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Mimi L. Quan, Ruth R. Wexler
-
Patent number: 6916798Abstract: The present invention relates to compounds of formula I that are useful as GSK-3 inhibitors. The invention also relates to methods of using compounds of formula I or pharmaceutical compositions comprising compounds of formula I to inhibit GSK-3 activity. The invention further provides methods of utilizing these compounds and pharmaceutical compositions in the treatment and prevention of various disorders, such as diabetes and Alzheimer's disease. The invention also relates to methods for inhibiting Aurora-2 activity and for treating or preventing Aurora-2-mediated diseases using compounds of formula I or pharmaceutical compositions comprising compounds of formula I. The invention also relates to methods for inhibiting cyclin-dependent kinase-2 activity and for treating or preventing inhibiting cyclin-dependent kinase-2-mediated diseases using compounds of formula I or pharmaceutical compositions comprising compounds of formula I.Type: GrantFiled: August 2, 2002Date of Patent: July 12, 2005Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jeremy Green, Michael J. Arnost, Albert Pierce
-
Patent number: 6906070Abstract: The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein rings D-E represent guanidine mimics, which are useful as inhibitors of factor Xa.Type: GrantFiled: August 8, 2001Date of Patent: June 14, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Patrick Y. Lam, Charles G. Clark, Celia Dominguez, John M. Fevig, Qi Han, Renhua Li, Donald J. P. Pinto, James R. Pruitt, Mimi L. Quan
-
Patent number: 6894173Abstract: Disclosed are novel processes and novel intermediate compounds for preparing aryl-and heteroaryl-substituted urea compounds of the formula(I) wherein Ar1, Ar2, L, Q and X are described herein. The product compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.Type: GrantFiled: February 10, 2003Date of Patent: May 17, 2005Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Lin-Hua Zhang, Lei Zhu
-
Publication number: 20040229918Abstract: Selective PDE4 inhibition is achieved by aryl and heteroaryl pyrazole compounds. The compounds exhibit improved PDE4 inhibition as compared to compounds such as rolipram and show selectivity with regard to inhibition of other classes of PDEs.Type: ApplicationFiled: April 16, 2004Publication date: November 18, 2004Inventors: Allen Hopper, Erik Kuester, Robert Dunn, Richard Conticello
-
Patent number: 6809206Abstract: The method of this invention prepares acylated cyclic compounds by contacting phenyl esters as acylating agents with cyclic compounds in the presence of a cyanide or fluoride catalyst.Type: GrantFiled: March 24, 2003Date of Patent: October 26, 2004Assignee: E. I. du Pont de Nemours and CompanyInventor: Paul Walter Wojtkowski
-
Patent number: 6803372Abstract: Compounds of the general formula (I): wherein Ar1 represents optionally substituted aryl or heteroaryl; n represents 0 or 1; T, U, V, and W each independently represent nitrogen atom or optionally substituted methine group, where at least two of them represent the said methine group; X represents methine or hydroxy substituted methine; Y represents an optionally substituted imino or oxygen atom are described and claimed. These novel spiro compounds are useful as neuropeptide Y receptor antagonists and as agents for the treatment of various kinds of cardiovascular disorders, central nervous system disorders, metabolic diseases and the like.Type: GrantFiled: March 8, 2002Date of Patent: October 12, 2004Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Takehiro Fukami, Akio Kanatani, Akane Ishihara, Yasuyuki Ishii, Toshiyuki Takahashi, Yuji Haga, Toshihiro Sakamoto, Takahiro Itoh
-
Publication number: 20040138265Abstract: The invention concerns novel carboxamides of formula (I) wherein A is (A1), (A2), (A3), (A4), (A5); Q is (Q1), (Q2), (Q3), (Q4), (Q5), (Q6); R1 is CH2 R2, CH2CH═CHR2, CH═C═CHR2 or COR3; R2 is hydrogen, C1-C6alkyl, C1-C6haloalkyl, C2-C6alkenyl, C2-C6alkynyl, C3-C7cycloalkyl, COOC1-C4alkyl, COOC3-C6alkenyl, COOC3-C6alkynyl or CN; R3 is C1-C6alkyl, C1-C6alkyl substituted by halogen, C1-C6alkoxy or C1-C6haloalkoxy; or is C1-C6alkylthio, C1-C6haloalkylthio, C1-C6alkoxy, C1-C6haloalkoxy; C3-C6alkenyloxy or C3-C6haloalkenyloxy; C3-C6haloalkenyloxy; C3-C6alkynyloxy or C3-C6haloalkynyloxy; R4 is methyl, CF2Cl, CF3, CF2H, CFH2, Cl or Br, R5 is methyl, CF3, CH2OCH3 or CH2OCF3; R6 is hydrogen, fluoro, CF3 or methyl; R7 is hydrogen, methyl or halogen; and Z is phenyl, halophenyl, C5-C7cycloalkyl, C5-C7acycloalkyl substituted by C1-C3alkyl, C1C3haloalkyl or halogen, or a group of the form —CHR8—CH2—CHR9R10 wherein R8, R9 and R10 are independently of each other C1-C3alkyl.Type: ApplicationFiled: January 12, 2004Publication date: July 15, 2004Inventors: Harald Walter, Stephan Trah
-
Publication number: 20040110750Abstract: Compounds of formula (I′) wherein the two OH— substituents in the phenyl moiety are in a position ortho to one another and R1 in a position ortho to one of the hydroxy groups; and X, R1 to R6 are as defined in claims, exhibit COMT enzyme inhibiting activity so that they are useful as COMT inhibitors.Type: ApplicationFiled: March 31, 2003Publication date: June 10, 2004Inventors: Jarmo Pystynen, Martti Ovaska, Jukka Vidgren, Timo Lotta, Marjo Yliperttula-Ikonen
-
Publication number: 20040097733Abstract: Compounds of the formula 1Type: ApplicationFiled: July 2, 2003Publication date: May 20, 2004Inventors: Richard L. Beard, Thong Vu, Diana F. Colon, Vidyasagar Vuligonda, Roshantha A. Chandraratna
-
Patent number: 6716850Abstract: Compounds of the formula I: where; R1 is O, S; R2 is an optionally substituted nitrogen-containing heterocycle, wherein the nitrogen is located at the 2 position relative to the (thio)urea bond; R3 is H, C1-C3 alkyl, R4-R7 are independently selected from H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, haloC1-C6 alkyl, C1-C6 alkanoyl, haloC1-C6 alkanoyl, C1-C6 alkoxy, haloC1-C6 alkoxy, C1-C6 alkyloxy-C1-C6 alkyl, haloC1-C6 alkyloxy-C1-C6 alkyl hydroxy-C1-C6 alkyl, amino-C1-C6 alkyl, carboxy-C1-C6 alkyl, cyano-C1-C6 alkyl, amino, carboxy, carbamoyl, cyano, halo, hydroxy, keto; X is —(CHR8)n-—D—(CHR8)m—; D is —NR9—, —O—, —S—, —S(═O)— or —S(═O)2—; R8 is independently H, C1-C3 alkyl, halo substitutedC1-C3alkyl; R9 is H, C1-C3 alkyl; n and m are independently 0, 1 or 2; and prodrugs and pharmaceutically acceptable salts thereof, have utility as inhibitors of HIV-1 reverse transcriptase, particularType: GrantFiled: March 5, 2002Date of Patent: April 6, 2004Assignee: Medivir ABInventors: Stefan Lindström, Christer Sahlberg, Hans Wallberg, Genaidy Kalyanov, Lourdes Salvador Odén, Lotta Naeslund
-
Patent number: 6716257Abstract: The new diaminopyrazole compounds are bridged 4,5-diaminopyrazole compounds or salts thereof.Type: GrantFiled: December 14, 2001Date of Patent: April 6, 2004Assignee: Wella AktiengesellschaftInventors: Otto Goettel, Aline Pirrello, André Hayoz, Emmanuel Morand
-
Publication number: 20040058931Abstract: Indanes, benzopyrans and analogues thereof are potassium channel inhibitors and blockers of IKur and have the structure 1Type: ApplicationFiled: November 15, 2002Publication date: March 25, 2004Inventors: John Lloyd, Heather J. Finlay, Wayne Vaccaro, Karnail S. Atwal, Michael F. Gross, Kerry L. Spear
-
Patent number: 6699860Abstract: This invention is related to novel di-substituted aminomethyl chroman derivatives which are useful in the treatment of beta-3 receptor-mediated conditions.Type: GrantFiled: December 7, 2001Date of Patent: March 2, 2004Assignee: Bayer Pharmaceuticals CorporationInventors: Gaetan H. Ladouceur, William H. Bullock, Steven R. Magnuson, Stephen J. O'Connor, Roger A. Smith, Quanrong Shen, Qingjie Liu, Ning Su, Emil J. Velthuisen, Ann-Marie Campbell, Paul P. Ehrlich
-
Patent number: 6677460Abstract: An aromatic carboxylic acid bicyclic sulfur compound of the formula (II): wherein X1 is a C1 to C4 alkyl, a halogen, a C1 to C4 haloalkyl, a C2 to C4 alkoxyalkyl, a C1 to C4 alkoxy or a C1 to C4 haloalkoxy; X2 is a hydrogen, a C1 to C4 alkyl or a C1 to C4 haloalkyl, or X2 forms a bond with X5; X3 is a hydrogen, a C1 to C4 alkyl or a C1 to C4 haloalkyl; X4 is a hydrogen, a halogen, a C1 to C4 alkyl, a C1 to C4 haloalkyl or a C1 to C4 alkoxy; X5 forms a bond with X2 or X5 forms a bond with X7; each of X6 and X8 is independently a hydrogen or a C1 to C4 alkyl or forms a bond with X5; p is 1; and n is 0, 1 or 2; or a salt thereof.Type: GrantFiled: May 20, 2003Date of Patent: January 13, 2004Assignee: Idemitsu Kosan Company, LimitedInventors: Kazufumi Nakamura, Masashi Sakamoto, Ichiro Nasuno
-
Publication number: 20030236421Abstract: The present invention relates to pyrazole derivatives of the formula (I), 1Type: ApplicationFiled: May 20, 2003Publication date: December 25, 2003Applicant: IDEMITSU KOSAN COMPANY, LIMITEDInventors: Kazufumi Nakamura, Masashi Sakamoto, Ichiro Nasuno
-
Publication number: 20030220199Abstract: Disclosed are novel pyrazole derivatives which are free of phytotoxicity to corn and can control a broad range of cropland weeds at a low dosage and herbicides containing them, and the present invention provides pyrazole derivatives of the general formula (I), or salts thereof, 1Type: ApplicationFiled: February 4, 2003Publication date: November 27, 2003Applicant: IDEMITSU KOSAN CO., LTD.Inventors: Kazufumi Nakamura, Kazuyoshi Koike, Masashi Sakamoto, Ichiro Nasuno
-
Publication number: 20030216258Abstract: Condensed heterocyclic compounds of the general formula: 1Type: ApplicationFiled: April 25, 2003Publication date: November 20, 2003Applicant: Sumitomo Chemical Company, LimitedInventors: Minoru Takano, Shinichi Kawamura, Takashi Komori
-
Patent number: RE39663Abstract: The invention provides compositions electron-deficient nitrogen heterocycle-substituted fluorescein dyes and methods in which the dyes are conjugated to substrates and used as detection labels in molecular biology experiments. The electron-deficient nitrogen heterocycles include pyridine, quinoline, pyrazine, and the like. Substrates include polynucleotides, nucleosides, nucleotides, peptides, proteins, carbohydrates, and ligands.Type: GrantFiled: April 6, 2004Date of Patent: May 29, 2007Assignee: Applera CorporationInventors: Krishna G. Upadhva, Steven M. Menchen, Weiguo Zhen
-
Patent number: RE39681Abstract: Compounds of the formula wherein: X is selected from the group consisting of trihalomethyl, C1-C6 alkyl, and a group of formula II: wherein: R3 and R4 are independently selected from the group consisting of hydrogen; halogen; hydroxyl; nitro; C1-C6 alkyl; C1-C6 alkoxy; carboxy; C1-C6 trihaloalkyl; and cyano; Z is selected from the group consisting of substituted and unsubstituted aryl; or a pharmaceutically acceptable salt thereof. The compounds are inhibitors of cyclooxygenase-2 activity. They are useful for treating cyclooxygenase-mediated disorders, including, for example, inflamation, neoplastic disorders and angiogenesis-mediated disorders.Type: GrantFiled: July 29, 2003Date of Patent: June 5, 2007Assignee: Temple University - of the Commonwealth System of Higher EducationInventors: E. Premkumar Reddy, M. V. Ramana Reddy