Thiadiazines Patents (Class 544/8)
-
Publication number: 20100298278Abstract: The invention relates to the substituted 1,2-ethylenediamines of general formula (I), wherein the groups R1 to R13, A, B, L and i are defined as in the description and the claims. The invention also relates to the use thereof in the treatment of Alzheimer's disease (AD) and similar diseases.Type: ApplicationFiled: August 8, 2006Publication date: November 25, 2010Inventors: Christian Eickmeier, Klaus Fuchs, Niklas Heine, Stefan Peters, Cornelia Dorner-Ciossek, Sandra Handschuh, Herbert Nar, Klaus Klinder
-
Publication number: 20100286129Abstract: The present invention relates to novel benzimidazole-dihydrothiadiazinone derivatives as fructose-1,6-bisphosphatase inhibitors, to processes for the preparation thereof and to the use thereof in therapy, especially for the treatment of diabetes.Type: ApplicationFiled: October 13, 2008Publication date: November 11, 2010Inventors: Gerard Botton, Caroline Leriche, Annick Arbellot De Vacqueur, Annick Audet, Johannes Gleitz
-
Publication number: 20100260711Abstract: The present invention relates to 3-Aminosulfonyl Substituted Indole Derivatives, compositions comprising at least one 3-Aminosulfonyl Substituted Indole Derivative, and methods of using the 3-Aminosulfonyl Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: November 13, 2008Publication date: October 14, 2010Applicant: Schering CorporationInventors: Kevin X. Chen, Stuart B. Rosenblum, F. George Njoroge, Joseph A. Kozlowski
-
Publication number: 20100190777Abstract: Compounds of formula I active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases. Formula (I) wherein Ar is optionally substituted heteroaryl; R2 is hydrogen, lower alkyl or halogen; U is selected from the group consisting of —S(O)2—, —C(X)—, —C(X)—N(R10)—, and —S(O)2—N(R10)—; R3 is optionally substituted lower alkyl, optionally substituted C3.6 cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl or optionally substituted heteroaryl; and wherein R1, R3, R4, m, L1, X R10 are as described herein.Type: ApplicationFiled: July 16, 2008Publication date: July 29, 2010Applicant: PLEXXIKON INC.Inventors: Guoxian Wu, Jiazhong Zhang, Yong-Liang Zhu, Chao Zhang, Prabha N. Ibrahim, Songyuan Shi, Wayne Spevak, Dean R. Artis, James Tsai
-
Publication number: 20100168070Abstract: The invention relates to substituted 1,2-ethylenediamines of general formula (I), wherein the radicals R1-R13, A, B, L and i are as defined in the description and in the claims. The invention also relates to the use thereof for treating Alzheimer's disease (AD) and similar diseases.Type: ApplicationFiled: August 8, 2006Publication date: July 1, 2010Inventors: Niklas Heine, Klaus Fuchs, Christian Eickmeier, Stefan Peters, Cornelia Dorner-Ciossek, Sandra Handschuh, Herbert Nar, Klaus Klinder
-
Publication number: 20100144681Abstract: The invention relates to substituted 1,2-ethylenediamines of general formula (I), wherein the radicals R1-R13, A, B, L and i are as defined in the description and the claims. The invention also relates to the use thereof for treating Alzheimer's disease (AD) and similar diseases.Type: ApplicationFiled: August 8, 2006Publication date: June 10, 2010Inventors: Klaus Fuchs, Christian Eickmeier, Niklas Heine, Stefan Peters, Cornelia Dorner-Ciossek, Sandra Handschuh, Herbert Nar, Klaus Klinder
-
Patent number: 7713961Abstract: The present invention relates to substituted 1,2-ethylenediamines of general formula (I) wherein the groups R1 to R15, A, B, L, i as well as X1—X4 are defined as in the specification and claims and the use thereof for the treatment of Alzheimer's disease (AD) and similar diseases.Type: GrantFiled: March 30, 2006Date of Patent: May 11, 2010Assignee: Boehringer Ingelheim International GmbHInventors: Christian Eickmeier, Stefan Peters, Klaus Fuchs, Niklas Heine, Sandra Handschuh, Cornelia Dorner-Ciossek, Klaus Klinder, Marcus Kostka
-
Publication number: 20100035865Abstract: The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula (I), as defined in the specification. The invention is also directed to compositions containing the compounds of formula (I).Type: ApplicationFiled: March 26, 2008Publication date: February 11, 2010Inventors: Kimberly Gail Estep, Anton F.J. Fliri, Christopher J. O'Donnell
-
Publication number: 20090324511Abstract: 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: ApplicationFiled: May 20, 2009Publication date: December 31, 2009Inventors: Bradley P. Morgan, Alex Muci, Erica Kraynack, Pu-Ping Lu, Todd Tochimoto, David J. Morgans, JR.
-
Publication number: 20090325940Abstract: The present invention relates to substituted 1,2-ethylenediamines of general formula (I) wherein the groups R1 to R15, A, B, L, i as well as X1-X4 are defined as in the specification and claims and the use thereof for the treatment of Alzheimer's disease (AD) and similar diseases.Type: ApplicationFiled: July 29, 2009Publication date: December 31, 2009Applicant: Boehringer Ingelheim International GmbHInventors: Christian Eickmeier, Stefan Peters, Klaus Fuchs, Niklas Heine, Sandra Handschuh, Cornelia Dorner-Ciossek, Klaus Klinder, Marcus Kostka
-
Patent number: 7534785Abstract: Compounds of the formula I, in which R1, R2, Q and B have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: GrantFiled: October 25, 2006Date of Patent: May 19, 2009Assignee: Merck Patent GesellschaftInventors: Oliver Schadt, Dieter Dorsch, Melanie Schultz, Andree Blaukat
-
Patent number: 7531533Abstract: A compound represented by the general formula (I) or a salt thereof: [T represents oxygen atom and the like; V represents CH2 and the like; R01 to R04 represent hydrogen atom and the like; A represents a linear alkylene group or linear alkenylene group having 2 to 8 carbon atoms and the like; D represents carboxyl group and the like; X represents ethylene group, trimethylene group and the like; E represents —CH(OH)— group and the like; and W represent —U1—(RW1)(RW2)—U2—U3 group (U1 represents a single bond, an alkylene group having 1 to 4 carbon atoms and the like; RW1 and RW2 represent hydrogen atom and the like; U2 represents a single bond, an alkylene group having 1 to 4 carbon atoms and the like; and U3 represent an alkyl group having 1 to 8 carbon atoms and the like), or a residue of a carbon ring or heterocyclic compound], which can be utilized as an active ingredient of medicaments effective for prophylactic and/or therapeutic treatment of skeletal diseases such as osteoporosis and fracture, glaucoType: GrantFiled: January 26, 2006Date of Patent: May 12, 2009Assignee: Asahi Kasei Pharma CorporationInventors: Motoshi Shoda, Toshinori Ishizuya
-
Patent number: 7524874Abstract: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritis, vitiligo, general gastrointestinal disorders, gastric ulceration, dType: GrantFiled: August 1, 2005Date of Patent: April 28, 2009Assignee: Amgen Inc.Inventors: Elizabeth M. Doherty, Jiawang Zhu, Markian Stec, Mark H. Norman, Vassil I. Ognyanov, Christopher H. Fotsch, Ning Chen, Partha P. Chakrabarti, Liping H. Pettus, Hui-Ling Wang, Xianghong Wang, Premilla Arasasingham
-
Patent number: 7514430Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: July 28, 2005Date of Patent: April 7, 2009Assignee: Bristol-Myers Squibb Pharma CompanyInventor: George V. DeLucca
-
Publication number: 20090042867Abstract: The invention relates to substituted 1,2-ethylenediamines of general formula (I), wherein the radicals R1 to R13, A, B, L, and i are defined as indicated in the description and the claims, as well as the use thereof for treating Alzheimer's disease (AD) and similar diseases.Type: ApplicationFiled: August 8, 2006Publication date: February 12, 2009Inventors: Klaus Fuchs, Christian Eickmeier, Niklas Heine, Stefan Peters, Cornelia Dorner-Ciossek, Sandra Handschuh, Herbert Nar, Klaus Klinder
-
Publication number: 20090023713Abstract: The invention is concerned with novel heterocyclyl compounds of formula (I) wherein A, X, Y, R3, R4, R5, R6, R7, R8, R9, R10, m and n are as herein defined, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR2 receptor, CCR5 receptor and/or CCR3 receptor and can be used as medicaments.Type: ApplicationFiled: July 10, 2008Publication date: January 22, 2009Inventors: Johannes Aebi, Alfred Binggeli, Luke Green, Guido Hartmann, Hans P. Maerki, Patrizio Mattei, Fabienne Ricklin
-
Patent number: 7476667Abstract: The invention relates to indole acetic acid compounds which function as antagonists of the CRTH2 receptor. The invention also relates to the use of these compounds to inhibit the binding of prostaglandin D2 and its metabolites or certain thromboxane metabolites to the CRTH2 receptor and to treat disorders responsive to such inhibition.Type: GrantFiled: June 2, 2008Date of Patent: January 13, 2009Assignee: WyethInventors: Youssef L. Bennani, Lawrence Nathan Tumey, Elizabeth Ann Gleason, Michael Joseph Robarge
-
Publication number: 20080318936Abstract: Compounds of the formula (I), in which R1, R2, m, Q and B have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: October 25, 2006Publication date: December 25, 2008Inventors: Oliver Schadt, Dieter Dorsch, Melanie Schultz, Andree Blaukat
-
Publication number: 20080306052Abstract: Compounds of the formula I, in which R1, R2, Q and B have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: October 25, 2006Publication date: December 11, 2008Inventors: Oliver Schadt, Dieter Dorsch, Melanie Schultz, Andree Blaukat
-
Publication number: 20080275031Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.Type: ApplicationFiled: June 16, 2008Publication date: November 6, 2008Inventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Renee Louise DesJarlais, Sanath K. Meegalla, Mark Wall, Kenneth Wilson
-
Patent number: 7414050Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.Type: GrantFiled: April 18, 2007Date of Patent: August 19, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Carl R. Illig, Shelly K. Ballentine, Jinsheng Chen, Renee Louise DesJarlais, Sanath K. Meegalla, Mark Wall, Kenneth Wilson
-
Patent number: 7371743Abstract: The present invention relates to new substituted carboxylic acid amides of general formula wherein A, B and R1 to R5 are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.Type: GrantFiled: February 11, 2005Date of Patent: May 13, 2008Assignee: Boehringer Ingelheim International GmbHInventors: Henning Priepke, Kai Gerlach, Roland Pfau, Norbert Hauel, Iris Kauffmann-Hefner, Georg Dahmann, Herbert Nar, Sandra Handschuh, Wolfgang Wienen, Annette Schuler-Metz
-
Patent number: 7358239Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q isType: GrantFiled: March 14, 2005Date of Patent: April 15, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
-
Patent number: 7335672Abstract: Substituted pyridines and pyrimidines and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenType: GrantFiled: September 13, 2005Date of Patent: February 26, 2008Assignee: Amgen Inc.Inventors: Mark H. Norman, Liping H. Pettus, Xianghong Wang, Jiawang Zhu
-
Patent number: 7332511Abstract: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, dType: GrantFiled: August 1, 2005Date of Patent: February 19, 2008Assignee: Amgen Inc.Inventors: Elizabeth M. Doherty, Jiawang Zhu, Markian Stec, Mark H. Norman, Hui-Ling Wang, Christopher H. Fotsch, Ning Chen, Partha P. Chakrabarti, Celia Dominguez, James Richard Falsey, Christopher Hulme, Jodie Katon, Thomas Nixey, Vassil I. Ognyanov, Liping H. Pettus, Robert Michael Rzasa
-
N-(substituted benzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamides useful as HIV integrase inhibitors
Patent number: 7323460Abstract: N-(Substituted benzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamides are inhibitors of HIV integrase and inhibitors of HIV replication. The naphthyridine carboxamides are of Formula (I): wherein R1?, R2? and R3? are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are described.Type: GrantFiled: March 12, 2003Date of Patent: January 29, 2008Assignee: Merck & Co., Inc.Inventors: Melissa Egbertson, H. Marie Langford, Jeffrey Y. Melamed, John S. Wai, Wei Han, Debbie S. Perlow, Linghang Zhuang, Mark Embrey -
Publication number: 20070249593Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.Type: ApplicationFiled: April 18, 2007Publication date: October 25, 2007Inventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Renee Louise DesJarlais, Sanath K. Meegalla, Mark Wall, Kenneth Wilson
-
Patent number: 7273862Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk1 and Alk2 are optionally substituted C1-6alkanediyl; R6 is hydrogen or phenylmethyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a bivalent radical.Type: GrantFiled: November 29, 2004Date of Patent: September 25, 2007Assignee: Janssen Pharmaceutica N.V.Inventors: Kristof Van Emelen, Marcel Frans Leopold De Bruyn
-
Patent number: 7259163Abstract: Novel anti-viral agents of Formula wherein: A represents OR1, NR1R2, or R1 wherein R1 and R2 are hydrogen, C1-6alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; or R1 and R2 together with the nitrogen atom to which they are attached form a 5 or 6 membered saturated cyclic group; B represents C(O)R3 wherein R3 is C1-6alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; C represents C1-6alkyl, aryl, heteroaryl or heterocyclyl; D represents a saturated or unsaturated optionally substituted 6-membered heterocyclic ring; E represents hydrogen or C1-6alkyl; F represents hydrogen, C1-6alkyl, aryl or heteroaryl; and G represents hydrogen, C1-6alkyl, heterocyclylalkyl, arylalkyl or heteroarylalkyl; and salts, solvates and esters thereof, processes for their preparation and methods of using them in HCV treatment are provided.Type: GrantFiled: October 30, 2002Date of Patent: August 21, 2007Assignee: Glaxo Group LimitedInventors: Gianpaolo Bravi, Rossella Guidetti, David Haigh, Charles David Hartley, Peter David Howes, Deborah Lynette Jackson, Victoria Lucy Helen Lovegrove, Pritom Shah, Martin John Slater, Katrina Jane Wareing
-
Patent number: 7229988Abstract: The present invention provides novel dialkylhydroxybenzoic acid derivatives containing metal chelating groups and the use of the novel compounds as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen species and/or excess Zn ions, in particular stroke, Parkinson's disease, Alzheimer's disease. The compounds of the invention have not only low toxicity but also similar or superior LPO inhibition activity to references. They also effectively inhibit the cerebral neuronal cell death by ROS and/or zinc ion, and show neuroprotective effects against ischemic neuronal degeneration.Type: GrantFiled: June 5, 2003Date of Patent: June 12, 2007Assignee: Samsung Electronics Co., Ltd.Inventors: Eu-Gene Oh, Sung-Bo Ko, Kyung-Hwa Kim, In-Kyu Chang, Dennis W. Choi, Laura L. Dugan, Jae-Young Koh, In-Jae Shin, Moo-Ho Won
-
Patent number: 7217706Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.Type: GrantFiled: February 14, 2002Date of Patent: May 15, 2007Assignee: Astellas Pharma Inc.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
-
Dye-forming coupler, silver halide photographic light-sensitive material and azomethine dye compound
Patent number: 7196194Abstract: A yellow dye-forming coupler represented by formula (I): wherein Q represents a group of nonmetallic atoms that form a 5- to 7-membered ring in combination with the —N?C—N(R1)—; R1 and R2 each represent a substituent; R4 represents an alkyl group; m represents an integer of 0 to 4; and X represents a hydrogen atom, or a group capable of being split-off upon a coupling reaction with an oxidized product of a developing agent; and when R4 represents a primary alkyl group, R1 represents —(CH2)3O—R101 in which R101 is an alkyl group having 4 to 8 carbon atoms. A silver halide color photographic light-sensitive material having at least one yellow dye-forming coupler represented by formula (I) in at least one layer provided on a support.Type: GrantFiled: October 7, 2003Date of Patent: March 27, 2007Assignee: Fuji Photo Film Co., LtdInventors: Kiyoshi Takeuchi, Shigeki Uehira, Mario Aoki, Jun Ogasawara, Yasuhiro Shimada, Seiji Ichijima, Yasuaki Deguchi, Naoto Matsuda, Akira Ikeda, Hisashi Mikoshiba, Masaharu Sugai, Taiji Katsumata -
Patent number: 7081453Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharma-ceutically acceptable acid addition salt thereof, wherein —a1?a2—a3?a4— is a bivalent radical wherein one or two of a1 to a4 are nitrogen and the remaining a1 to a4 are —CH?; —Z1—Z2— is a bivalent radical; —A— is a bivalent radical of formula —N(R6)—Alk2— or a 5, 6 or 7-membered saturated heterocycle containing one or two nitrogen atoms; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; Alk1 and Alk2 are optionally substituted C1-6alkanediyl; R5 is a radical of formula (d-1), (d-2), (d-3), (d-4), (d-5) wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y2 is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonylType: GrantFiled: June 13, 2001Date of Patent: July 25, 2006Assignee: Janssen Pharmaceutica N.V.Inventors: Kristof Van Emelen, Marcel Frans Leopold De Bruyn, Manuel Jesús Alcázar-Vaca, José Ignacio Andrés-Gil, Francisco Javier Fernández-Gadea, Maria Encarnacion Matesanz-Ballesteros, José Manuel Bartolomé-Nebreda
-
Patent number: 7064201Abstract: Compounds represented by the following structure (I) are disclosed: as are methods for making such compounds, wherein said methods comprise reacting a diacyldiketopiperazine with a first aldehyde to produce an intermediate compound; and reacting the intermediate compound with a second aldehyde to produce the class of compounds with the generic structure, where the first aldehyde and the second aldehydes are selected from the group consisting of an oxazolecarboxaldeyhyde, imidazolecarboxaldehyde, a benzaldehyde, imidazolecarboxaldehyde derivatives, and benzaldehyde derivatives, thereby forming the above compound wherein R1, R1?, R1?, R2, R3, R4, R5, and R6, X1 and X2, Y, Z, Z1, Z2, Z3, and Z4 may each be separately defined in a manner consistent with the accompanying description. Compositions and methods for treating cancer and fungal infection are also disclosed.Type: GrantFiled: August 1, 2003Date of Patent: June 20, 2006Assignee: Nereus Pharmaceuticals, Inc.Inventors: Yoshio Hayashi, Michael A. Palladino, Jr., Jennifer Grodberg
-
Patent number: 7015216Abstract: Disclosed are a series of heteroaryl-?-alanine derivatives, compositions containing them, processes for their preparation and their use in medicine.Type: GrantFiled: July 19, 2001Date of Patent: March 21, 2006Assignees: Elan Pharmaceuticals, Inc., WyethInventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis, Darren B. Dressen, Francine S. Grant, Christopher Semko, Ying-Zi Xu
-
Patent number: 7015321Abstract: A practical and high-yielding method for the efficient, one-step synthesis of diverse classes of N,N?-differentiated sulfamides employs a wide range of amino alcohols and simple amines using Burgess-type reagents. This methodology extends the application and availability of sulfamides within the fields of chemical biology, medicinal chemistry, asymmetric synthesis, and supramolecular chemistry.Type: GrantFiled: October 14, 2003Date of Patent: March 21, 2006Assignee: The Scripps Research InstituteInventors: Kyriacos C. Nicolaou, Deborah Longbottom, Scott A. Snyder, Xianhai Huang
-
Patent number: 6974869Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: September 18, 2002Date of Patent: December 13, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventor: George V. DeLucca
-
Patent number: 6921759Abstract: Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described. These compounds are inhibitors of HIV integrase and inhibitors of HIV replication, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.Type: GrantFiled: October 10, 2001Date of Patent: July 26, 2005Assignee: Merck & Co., Inc.Inventors: Neville J. Anthony, Robert P. Gomez, Steven D. Young, Melissa Egbertson, John S. Wai, Linghang Zhuang, Mark Embrey, Jeffrey Y. Melamed, H. Marie Langford, James P. Guare, Thorsten E. Fisher, Samson M. Jolly, Michelle S. Kuo, Debra S. Perlow, Jennifer J. Bennett, Timothy W. Funk
-
Patent number: 6900222Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereon wherein —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is aType: GrantFiled: May 23, 2000Date of Patent: May 31, 2005Assignee: Janssen Pharmaceutica N.V.Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
-
Patent number: 6878702Abstract: The use of mitochondrial KATP channel openers, particularly compounds of general formula (I), for the treatment or prevention of inflammation by inducing apoptosis of inflammatory cells.Type: GrantFiled: November 16, 2001Date of Patent: April 12, 2005Assignee: Orion CorporationInventors: Heimo Haikala, Minja Hyttilä-Hopponen, Erkki Nissinen, Minna Ruotsalainen, Aino Pippuri, Kari Lönnberg
-
Patent number: 6867298Abstract: The present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of an amide or amine moiety and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In additional embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between a nitrogen atom of an acyl hydrazine and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In other embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of a nitrogen-containing heteroaromatic, e.g., indole, pyrazole, and indazole, and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate.Type: GrantFiled: May 8, 2003Date of Patent: March 15, 2005Assignee: Massachusetts Institute of TechnologyInventors: Stephen L. Buchwald, Artis Klapars, Jon C. Antilla, Gabriel E. Job, Martina Wolter, Fuk Y. Kwong, Gero Nordmann, Edward J. Hennessy
-
Publication number: 20040259863Abstract: The invention relates to the use of type 4 phosphodiesterase inhibitors (PDE IV inhibitors) to treat diseases and to combinations of PDE IV inhibitors with other drugs.Type: ApplicationFiled: April 30, 2004Publication date: December 23, 2004Inventors: Hans-Michael Eggenweiler, Michael Wolf
-
Patent number: 6828317Abstract: The present invention provides certain thiadiazinone derivatives of oxazolidinones of the following formula I: or pharmaceutically acceptable salts thereof that are antibacterial agents, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.Type: GrantFiled: February 4, 2003Date of Patent: December 7, 2004Assignee: Pharmacia & Upjohn CompanyInventors: Gary W. Leuhr, Mikhail F. Gordeev, Dinesh V. Patel
-
Publication number: 20040242568Abstract: Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound comprising the formula: 1Type: ApplicationFiled: March 24, 2004Publication date: December 2, 2004Applicant: Syrrx, Inc.Inventors: Jun Feng, Stephen L. Gwaltney, Stephen W. Kaldor, Jeffrey A. Stafford, Michael B. Wallace, Zhiyuan Zhang
-
Patent number: 6825192Abstract: The present invention provides a hetrodiazinon compound having 2-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptor antagonistic action, which is represented by the following formula (I), a pharmacologically acceptable salt thereof or hydrates thereof. Wherein A represents O, S or a group represented by the formula NR3 (wherein R3 represents hydrogen atom or a lower alkyl group); R1 and R2 are the same as or different from each other and each represents an optionally substituted (hetero)aryl group etc.; and R4 and R5 are the same as or different from each other and each represents hydrogen atom, hydroxy, a halogen atom, nitrile group, nitro group, a lower alkyl group, a (hetero)aryl group etc.Type: GrantFiled: August 15, 2001Date of Patent: November 30, 2004Assignee: Eisai Co., Ltd.Inventors: Koichi Ito, Noritaka Kitazawa, Satoshi Nagato, Akiharu Kajiwara, Tatsuto Fukushima, Shinji Hatakeyama, Takahisa Hanada, Masataka Ueno, Kohshi Ueno, Koki Kawano
-
Patent number: 6780868Abstract: Compounds of formula (I): wherein: V represents a single bond or a linear or branched (C1-C6)alkylene chain, M represents a single bond or a linear or branched (C1-C6)alkylene chain, A and E each represents nitrogen or CH, but at least one of the two groups A or E represents nitrogen, W represents a group of formula (i): X represents carbonyl, G1 represents a linear C3 alkylene chain optionally containing a double bond and/or being optionally substituted by a hydroxyl group, their isomers, their hydrates, their solvates, and additional salts thereof with a pharmaceutically acceptable acid, and medicinal products containing the same which are useful in the treatment of diseases or pathological conditions in which endothelial dysfunction is known.Type: GrantFiled: February 20, 2003Date of Patent: August 24, 2004Assignee: Les Laboratoires ServierInventors: Jean-Louis Peglion, Christophe Poitevin, Jean-Paul Vilaine, Nicole Villeneuve, Marie-Pierre Bourguignon, Catherine Thollon
-
Publication number: 20040138448Abstract: A practical and high-yielding method for the efficient, one-step synthesis of diverse classes of N,N′-differentiated sulfamides employs a wide range of amino alcohols and simple amines using Burgess-type reagents. This methodology extends the application and availability of sulfamides within the fields of chemical biology, medicinal chemistry, asymmetric synthesis, and supramolecular chemistry.Type: ApplicationFiled: October 14, 2003Publication date: July 15, 2004Applicant: The Scripps Research InstituteInventors: Kyriacos C. Nicolaou, Deborah Longbottom, Scott A. Snyder, Xianhai Huang
-
Patent number: 6756370Abstract: The invention relates to compounds of formula (I), wherein R1, R2 and A have the meanings given in claim 1, are potent 5-HT2A antagonists and are suitable for treating psychoses, schizophrenia, depression, neurological disorders, impaired memory, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease, Huntington's disease, eating disorders such as bulimia and anorexia nervosa, Pre-Menstrual Syndrome and/or for positively influencing obsessive-compulsive disorders, (OCD).Type: GrantFiled: February 21, 2002Date of Patent: June 29, 2004Assignee: Merck Patent GmbHInventors: Helmut Prücher, Henning Böttcher, Karl-August Ackermann, Rudolf Gottschlich, Christoph van Amsterdam, Christoph Seyfried, Jürgen Harting, Gerd Bartoszyk, Hartmut Greiner
-
Patent number: 6693191Abstract: Described is a process for the preparation of a particulate tetrahydro-3,5-dimethyl-1,3,5-thiadiazine-2-thione product by combining a first aqueous solution comprising methylammonium N-methyldithiocarbamate with a second aqueous solution comprising formaldehyde, followed by separation and drying of the resulting solid, which comprises combining the first and the second aqueous solutions in such a way that the ratio between the concentrations of dithiocarbamate functions and of formaldehyde is essentially constant in the reaction mixture over time during the duration of the reaction.Type: GrantFiled: February 6, 2003Date of Patent: February 17, 2004Assignee: BASF AktiengesellschaftInventors: Heinz Isak, Norbert Sendhoff, Franz Schütz, Jörg Therre, Michael Drögemüller, Dirk Franke, Manfred Munzinger, Alexander Weck, Kirsten Burkart
-
Publication number: 20040014746Abstract: The present invention provides certain thiadiazinone derivatives of oxazolidinones of the following formula I: 1Type: ApplicationFiled: February 4, 2003Publication date: January 22, 2004Inventors: Gary W. Leuhr, Mikhail F. Gordeev, Dinesh V. Patel