1,3-thiazole Ring Bonded Directly To The Six-membered Hetero Ring Patents (Class 546/270.4)
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Publication number: 20090281293Abstract: The present invention relates to processes and intermediates for the preparation of 2-fluoro 6-11 bicyclic erythromycin derivatives.Type: ApplicationFiled: May 8, 2009Publication date: November 12, 2009Inventors: Guoyou Xu, Datong Tang, In Jong Kim, Ly Tam Phan, Yat Sun Or, Zhe Wang
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Publication number: 20090281324Abstract: The present invention relates generally to novel methods for the synthesis of O-[5-(4-amino-thiazol-2-yl)-pyridin-2-ylmethyl]-hydroxylamine which is an essential reagent in the synthesis of one of the bridged erythromycin derivatives and their respective pharmaceutically acceptable salts in PCT Application WO 03/097659 A1.Type: ApplicationFiled: May 8, 2009Publication date: November 12, 2009Inventors: Datong Tang, Yinglin Han, Yanhe Huang, Ly Tam Phan, Yat Sun Or, Zhe Wang
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Publication number: 20090275751Abstract: The present invention provides a novel compound having an excellent AMPA receptor inhibitory action and/or kainate inhibitory action. A compound represented by the following formula, a salt thereof or hydrates thereof. In the formula, Q indicates NH, O or S; and R1, R2, R3, R4 and R5 are the same as or different from each other and each indicates hydrogen atom, a halogen atom, a C1-6 alkyl group or a group represented by the formula —X-A (wherein X indicates a single bond, an optionally substituted C1-6 alkylene group etc.; and A indicates an optionally substituted C6-14 aromatic hydrocarbocyclic group or 5- to 14-membered aromatic heterocyclic group etc.).Type: ApplicationFiled: February 27, 2009Publication date: November 5, 2009Inventors: Satoshi NAGATO, Kohshi Ueno, Koki Kawano, Yoshihiko Norimine, Koichi Ito, Takaisa Hanada, Masatake Ueno, Hiroyuki Amino, Makoto Ogo, Shinji Hatakeyama, Yoshio Urawa, Hiroyuki Naka, Anthony John Groom, Leanne Rivers, Terrence Smith
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Publication number: 20090270456Abstract: This invention relates to newly identified compounds for inhibiting hYAK3 and/or CK2 proteins and methods for treating diseases associated with the imbalance or inappropriate activity of hYAK3 and/or CK2 proteins.Type: ApplicationFiled: January 6, 2005Publication date: October 29, 2009Inventors: Masaichi Hasegawa, Kazuya Kano, Masato Nakano, Mariko Yamabe
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Publication number: 20090270457Abstract: The present invention discloses compounds of formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.Type: ApplicationFiled: February 18, 2009Publication date: October 29, 2009Inventors: IN JONG KIM, TONGZHU LIU, HEEJIN KIM, YANCHUN WANG, YAO-LING QIU, LY TAM PHAN, YAT SUN OR
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Publication number: 20090203745Abstract: The present invention relates to compounds of formula (I) wherein: A is a radical selected from the group comprising aromatic heterocyclic 5-membered ring systems; Ar is a radical selected from the group comprising optionally substituted 5- and 6-membered aromatic ring systems, whereby the ring system contains 0, 1, 2 or 3 heteroatoms selected from the group comprising N, O and S; Z is a linker and ? is a radical of formula (II) and their use for the inhibition of integrin.Type: ApplicationFiled: May 14, 2007Publication date: August 13, 2009Applicant: Jerini AGInventors: Gunther Zischinsky, Roland Stragies, Frank Osterkamp, Dirk Scharn, Gerd Hummel, Holger Kalkhof, Grit Zahn, Doerte Vossmeyer, Claudia Christner-Albrecht, Ulrich Reineke
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Publication number: 20090203715Abstract: The present invention relates to 2-hetarylthiazole-4-carboxamide derivatives of the formula (I), the use thereof as medicament for the treatment of various disorders, and processes for the preparation thereofType: ApplicationFiled: December 9, 2008Publication date: August 13, 2009Applicant: Bayer Schering Pharma AGInventors: Ulrich Bothe, Arne Von Bonin, Duy Nguyen, Ulf Bomer, Judith Guenther
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Patent number: 7550463Abstract: An object of the present invention provides a novel compound having the anti-viral activity, particularly, the HIV integrase inhibitory activity, and a drug containing the same, particularly, an anti-HIV drug.Type: GrantFiled: September 14, 2005Date of Patent: June 23, 2009Assignee: Shionogi & Co., Ltd.Inventor: Hiroshi Yoshida
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Publication number: 20090156615Abstract: The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: June 4, 2007Publication date: June 18, 2009Inventors: Natalie Dales, Julia Fonarev, Jianmin Fu, Duanjie Hou, Rajender Kamboj, Vishnumurthy Kodumuru, Natalia Pokrovskaia, Vandna Raina, Shaoyi Sun, Zaihui Zhang
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Publication number: 20090133319Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof wherein A1, A2 and A3 are independently selected from the group consisting of CR3 and N; B1 B2 and B3 are independently selected from the group consisting of CR2 and N; Q is a phenyl ring or a 5- or 6-membered saturated or unsaturated heterocyclic ring, each ring optionally substituted with one or more substituents independently selected from halogen, C1-C6 alkyl, C1-C6 haloalkyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsufinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, —CN, —NO2, —N(R4)R5, —C(W)N(R4)R5, —C(O)OR5 and R8; or —S(O)2N(R21)R22; —S(O)pR25 or —S(O)(?NR28)R29; R1, R2, R3, R4, R5, R8, R21, R22, R25, R28, R29; p and n are as defined in the disclosure.Type: ApplicationFiled: December 15, 2006Publication date: May 28, 2009Applicant: E. I. DU PONT DE NEMOURS AND COMPANYInventors: George Philip Lahm, Kanu Maganbhai Patel, Thomas Francis Pahutski, JR., Benjamin Kenneth Smith
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Publication number: 20090131475Abstract: The present invention relates to treatment and/or prevention of one or more metabolic disorders utilizing fatostatin A and/or a derivative and/or analog thereof. In other aspects, the compound for treatment and/or prevention of one or more metabolic disorders utilizes an A-B—C tripartite structure, wherein A, B, and C are identical or non-identical structures and are described in detail herein. In specific aspects, the metabolic disorder includes obesity or diabetes, for example.Type: ApplicationFiled: February 1, 2008Publication date: May 21, 2009Applicant: Baylor College of MedicineInventors: Motonari Uesugi, Salih J. Wakil, Lutfi Abu-Elheiga, Qian Mao, Shinji Kamisuki, Akira Kugimiya
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Publication number: 20090118506Abstract: The present invention discloses compounds of formula I, II or, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.Type: ApplicationFiled: September 17, 2008Publication date: May 7, 2009Inventors: IN JONG KIM, Tongzhu Liu, Yao-Ling Qiu, Guoqiang Wang, Jiang Long, Heejin Kim, Yanchun Wang, Ly Tam Phan, Yat Sun Or
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Publication number: 20090076009Abstract: The invention concerns thiazole derivatives of Formula I or pharmaceutically-acceptable salts thereof, wherein each of R, Ring A, m, R1, R2 and R3 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in therapy, for example in the treatment of disease mediated by a PI3K enzyme and/or a mTOR kinase.Type: ApplicationFiled: May 2, 2007Publication date: March 19, 2009Inventors: Jean-Claude (Retired) Arnould, Kevin Michael Foote, Edward Jolyon Griffen
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Publication number: 20090076275Abstract: 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, obesity, type II diabetes mellitus and metabolic syndrome.Type: ApplicationFiled: September 10, 2008Publication date: March 19, 2009Inventors: David Robert Bolin, Jianping Cai, Adrian Wai-Hing Cheung, Robert Alan Goodnow, JR., Matthew Michael Hamilton, Shiming Li, Lee Apostle McDermott, Weiya Yun
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Publication number: 20090076094Abstract: This invention relates to a novel purified compound PM181104, of formula: of molecular weight 1514 and molecular formula C69H66N18O13S5; which is obtained by fermentation of the microorganism belonging to Kocuria species (ZMA B-1/MTCC 5269). The invention includes all stereoisomeric forms and all tautomeric forms of the compound PM181104 and pharmaceutically acceptable salts and derivatives such as esters and ethers. The present invention further relates to processes for the production of the novel antibacterial compound(s), to the production of the microorganism belonging to Kocuria species (ZMA B-1/MTCC 5269), and to pharmaceutical compositions containing the novel compound(s) as an active ingredient and its/their use in medicines for treatment and prevention of diseases caused by bacterial infections.Type: ApplicationFiled: April 10, 2007Publication date: March 19, 2009Applicants: PIRAMAL LIFE SCIENCES LIMITED, COUNCIL OF SCIENTIFIC AND INDUSTRIALInventors: Girish Badrinath Mahajan, Saji David George, Prafull Vasant Ranadive, Prabhu Dutt Satyanarayan Mishra, Sreekumar Sankaranarayanan Eyyammadichiyil, Rajan Mukund Panshikar, Satish Namdeo Sawant, Sridevi Krishna, Meenakshi Sivakumar, Koteppa Pari, Becky Mary Thomas, Zarine Eruch Patel, Ram Vishwakarma, Chandrakant Govind Naik, Lisette D'Souza, Prabha Devi
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Publication number: 20090066245Abstract: The present invention is a light-emitting device material characterized by containing a pyrene compound represented by the following general formula (1): wherein R1 to R10 are specific functional groups, provided that at least one of the R1 to R10 is a substituent represented by the following general formula (2): wherein R11 to R14 are specific functional groups, provided that any one of the R11 to R14 is used for a single bond with a pyrene skeleton; X1 is a group represented by the following general formula (3): wherein R15 is a specific functional group; and Y1 to Y4 is selected from among a nitrogen atom and a carbon atom, provided that at least one of the Y1 to Y4 is a nitrogen atom and at least one thereof is a carbon atom, and no substituents exist on the nitrogen atom in the case of the nitrogen atom. This material provides a light-emitting device having high luminous efficiency and excellent durability.Type: ApplicationFiled: February 23, 2006Publication date: March 12, 2009Applicant: TORAY INDUSTRIES, INC.Inventors: Kazunori Sugimoto, Seiichiro Murase, Daisuke Kitazawa, Kazumasa Nagao, Takafumi Ogawa, Tsuyoshi Tominaga
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Patent number: 7495018Abstract: (1) A 1,3-thiazole compound of which the 5-position is substituted with a 4-pyridyl group having a substituent including no aromatic group or (2) a 1,3-thiazole compound of which the 5-position is substituted with a pyridyl group having at the position adjacent to a nitrogen atom of the pyridyl group a substituent including no aromatic group has an excellent p38 MAP kinase inhibitory activity.Type: GrantFiled: March 29, 2001Date of Patent: February 24, 2009Assignee: Takeda Pharmaceutical Company LimitedInventors: Shigenori Ohkawa, Ken-ichi Naruo, Seiji Miwatashi, Hiroyuki Kimura
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Publication number: 20090048307Abstract: An optionally N-oxidized compound represented by the formula: wherein R1 represents hydrogen, hydrocarbon, heterocycle, amino, acyl, R2 represents an aromatic group, R3 represents hydrogen, pyridyl, aromatic hydrocarbon, X represents oxygen, optionally oxidized sulfur, Y represents a bond, an oxygen, optionally oxidized sulfur, a group represented by the formula NR4 (R4 represents hydrogen, hydrocarbon or acyl) and Z represents a bond or a divalent acyclic hydrocarbon, or a salt thereof has an excellent adenosine A3 receptor antagonistic activity and is used as an agent for preventing or treating diseases related to an adenosine A3 receptor. Furthermore, the compound (I) or a salt thereof has p38 MAP kinase inhibitory activity and TNF-? inhibitory activity and is used as an agent for preventing or treating diseases related to p38 MAP kinase and diseases related to TNF-?.Type: ApplicationFiled: August 29, 2007Publication date: February 19, 2009Inventors: Shigenori Ohkawa, Naoyuki Kanzaki, Seiji Miwatashi
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Publication number: 20090048225Abstract: The present invention provides a novel compound of Formula (I) or a pharmaceutically acceptable salt thereof, having histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another, embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.Type: ApplicationFiled: August 15, 2005Publication date: February 19, 2009Inventors: Don Richard Finley, Terry Patrick Finn, Philip Arthur Hipskind, William Joseph Hornback, Cynthia Darshini Jesudason, Takako Takakuwa
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Publication number: 20090041720Abstract: The invention provides heteroaryl substituted thiazolo compounds of Formula I and II and pharmaceutically acceptable salts thereof. The variables A and R3 to R7 are defined herein. The invention also includes methods for preparing compounds and salts of Formula I and II. The present invention also includes pharmaceutical compositions containing heteroaryl substituted thiazolo compounds and methods for using heteroaryl substituted thiazolo compounds, including methods for using the compounds in the treatment of hepatitis C virus.Type: ApplicationFiled: May 22, 2008Publication date: February 12, 2009Applicant: ACHILLION PHARMACEUTICALS, INC.Inventors: Xiangzhu Wang, Souming Zhang, Venkat Gadhachanda, Cuixian Liu, Jesse Quinn, Shouming Li, Dawei Chen, Milind Deshpande, Avinash Phadke
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Publication number: 20080318954Abstract: The present invention relates to compounds of formula (I), or a pharmaceutically acceptable salts thereof, wherein: Z1: 1 is N or CH; Z2 and Z3 are each independently N or CR7; R1, R2, R3, R4, R5, R6, and R7 are each independently H, R8, or R9; each R8 is independently a hydrocarbyl group; and each R9 is independently halo, NO2, alkoxy, CN, CF3, S03H, SO2NR10R11, S02R12, NR13R14(CH2)aCOOR15, (CH2)bCONR16R17, (CH2)cCOR18 or (CH2)dOH; a, b, c and d are each independently 0, 1 2 3 or 4; R10-18 are each independently H or alkyl; provided that when R1 and R2 are both H, Z1 is CH; or Z2 is N; or Z1 is CH and Z2 is N; and wherein the compound is other than 4-(4,5-dimethylthiazol-2-yl)-N-(3,4,5trimethoxyphenyl)-2-pyrimidineamine or 4-(5-(2-hydroxyethyl)-4-methylthiazol-2-yl)N-(3,4,5-trimethoxyphenyl)-2-pyrimidineamine.Type: ApplicationFiled: February 7, 2005Publication date: December 25, 2008Applicant: Cyclacel LimitedInventors: Kenneth Duncan, Darren Gibson, Shudong Wang, Daniella I. Zheleva, Peter Martin Fischer
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Publication number: 20080262046Abstract: The present invention is directed to amidopropoxyphenyl compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.Type: ApplicationFiled: April 10, 2006Publication date: October 23, 2008Inventors: Paul J. Coleman, John Schreier
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Publication number: 20080255141Abstract: Novel compounds selected from 2-(3-aminoaryl)amino-4-aryl-thiazoles of formula (I) that selectively modulate, regulate, and/or inhibit signal transductions mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferation metabolic, allergic and degenerative disorders. More particularly, these compounds are potent and selective c-kit inhibitors.Type: ApplicationFiled: July 18, 2007Publication date: October 16, 2008Inventors: Marco Ciufolini, Camille Wermuth, Bruno Gielthen, Alain Moussy
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Patent number: 7423055Abstract: The present invention relates to novel compounds selected from 2-(3-aminoaryl)amino-4-aryl-thiazoles that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. More particularly, these compounds are potent and selective c-kit inhibitors.Type: GrantFiled: August 1, 2003Date of Patent: September 9, 2008Assignee: AB ScienceInventors: Marco Ciufolini, Camille Wermuth, Bruno Gielthen, Alain Moussy
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Publication number: 20080207641Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein A, L, Y, W1, W2, Z, X, X2, and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: ApplicationFiled: November 12, 2007Publication date: August 28, 2008Applicant: Synta Pharmaceuticals Corp.Inventors: Gary Bohnert, Shoujun Chen
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Patent number: 7414060Abstract: The invention relates to compounds of formula I: wherein R1 to R3 are as defined in the specification, to processes for their preparation, to pharmaceutical compositions containing them, and to methods for treating CNS disorders.Type: GrantFiled: February 23, 2006Date of Patent: August 19, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Georg Jaeschke, Sabine Kolczewski, Richard Hugh Philip Porter, Eric Vieira
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Publication number: 20080181866Abstract: Disclosed are compounds, stereoisomers, tautomers, pharmaceutically acceptable salts, or prodrugs thereof of having Formula (I), their preparation, use, and compositions thereof for treating an infection mediated at least in part by a virus in the Flaviviridae family of viruses, wherein A, R3, X, V, W, T, Z, R, Y1, and p are as defined herein.Type: ApplicationFiled: November 20, 2007Publication date: July 31, 2008Inventors: Martin Robert Leivers, Franz Ulrich Schmitz, Ronald Conrad Griffith, Christopher Don Roberts, Ali Dehghani Mohammad Abadi, Stephanie Anna Chan, Roopa Rai, Irina Slobodov, Tony Loc Ton
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Patent number: 7402606Abstract: Heterocycle substituted ketoamide derivatives of Formula (I), wherein the substitutes A, D, A and R are defined as in claim in, which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such heterocycle substituted ketoamide derivatives as well as method of using the same in the manufacture of medicaments for the treatment of disorders, including osteoporosis, associated with an imbalance between bone resorption and formation which can ultimately lead to fracture.Type: GrantFiled: April 1, 2003Date of Patent: July 22, 2008Assignee: SmithKline Beecham CorporationInventors: David Gene Barrett, John G. Catalano, David Norman Deaton, Aaron Bayne Miller, John A. Ray, Vicente Samano
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Patent number: 7390907Abstract: 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: September 30, 2004Date of Patent: June 24, 2008Assignee: Amgen Inc.Inventors: Ning Chen, Thomas Nixey, Mark H. Norman
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Publication number: 20080132502Abstract: The invention provides thiazole derivatives of formula (I), or pharmaceutically acceptable salts thereof in which Ring A, R1, R2 and R3 are as defined in the specification; a processes for their preparation; pharmaceutical compositions containing them; and their use in therapy, for example in the treatment of disease mediated by a PI3K enzyme and/or a mTOR kinase.Type: ApplicationFiled: November 7, 2005Publication date: June 5, 2008Inventors: Malena Bengtsson, Joakim Larsson, Grigorios Nikitidis, Peter Storm, John Peter Bailey, Edward Jolyon Griffen, Jean-Claude Arnould, Thomas Geoffrey Colerick Bird
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Publication number: 20080132546Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.Type: ApplicationFiled: December 4, 2007Publication date: June 5, 2008Applicant: AstraZeneca ABInventors: Gregory Steven Basarab, Shanta Bist, John Irvin Manchester, Brian Sherer
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Publication number: 20080108799Abstract: The present invention relates to the use of thiazolyl-pyridinium based dyes in optical layers for optical data recording, preferably for optical data recording using a laser with a wavelength up to 450 mn. The invention further relates to a write only read many (WORM) type optical data recording medium capable of recording and reproducing information with radiation of blue laser, which employs a thiazolyl-pyridinium based type dye in the optical layer. The present invention further relates to new thiazolyl-pyridinium based dyes, of formula (V), (VI) or (VIII).Type: ApplicationFiled: August 31, 2005Publication date: May 8, 2008Inventor: Andre Weiss
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Patent number: 7276527Abstract: An optionally N-oxidized compound represented by the formula: wherein R1 represents hydrogen, hydrocarbon, heterocycle, amino, acyl, R2 represents an aromatic group, R3 represents hydrogen, pyridyl, aromatic hydrocarbon, X represents oxygen, optionally oxidized sulfur, Y represents a bond, an oxygen, optionally oxidized sulfur, a group represented by the formula NR4 (R4 represents hydrogen, hydrocarbon or acyl) and Z represents a bond or a divalent acyclic hydrocarbon, or a salt thereof has an excellent adenosine A3 receptor antagonistic activity and is used as an agent for preventing or treating diseases related to an adenosine A3 receptor. Furthermore, the compound (I) or a salt thereof has p38 MAP kinase inhibitory activity and TNF-? inhibitory activity and is used as an agent for preventing or treating diseases related to p38 MAP kinase and diseases related to TNF-?.Type: GrantFiled: February 16, 2006Date of Patent: October 2, 2007Assignee: Takeda Pharmaceutical Company LimitedInventors: Shigenori Ohkawa, Naoyuki Kanzaki, Seiji Miwatashi
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Patent number: 7273866Abstract: Novel 2-arylthiazole derivatives of Formula I are described which are openers of KCNQ potassium channels and are useful in the treatment of disorders that are responsive to the opening of the KCNQ potassium channels, including pain and migraineType: GrantFiled: December 9, 2003Date of Patent: September 25, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Kenneth M. Boy, Yong-Jin Wu, Jason M. Guernon
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Publication number: 20070213376Abstract: This invention is directed to halogenated sulfonamide derivatives which are ligands at the NPY Y5 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by admixing a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression which comprises administering to the subject an amount of a compound of the subject invention.Type: ApplicationFiled: March 5, 2007Publication date: September 13, 2007Inventors: Vrej Jubian, Mathivanan Packiarajan, Emily Reinhard
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Patent number: 7253187Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein Z1 and Z2 are each independently nitrogen or CH and Ring A, TmR1, QR2, UnR3, and Sp are as described in the specification. The compounds are especially useful as inhibitors of ERK2 and for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, diabetes, and cardiovascular disease.Type: GrantFiled: February 3, 2004Date of Patent: August 7, 2007Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jingrong Cao, Jeremy Green, Michael Hale, Francois Maltais, Judy Straub, Qing Tang, Alex Aronov
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Patent number: 7226940Abstract: The present invention relates to certain substituted heterocycles of Formula (I) which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, adipocyte differentiation, uncontrolled proliferation, such as lymphoma, Hodgkin's Disease, leukemia, breast cancer, prostate cancer or cancers in general; and inflammation, such as osteoarthritis, rheumatoid arthritis, Crohn's Disease or Inflammatory Bowel DiseaseType: GrantFiled: August 24, 2005Date of Patent: June 5, 2007Assignees: Incyte San Diego, Inc., Ortho McNeil Pharmaceutical Inc.Inventors: Magnus Pfahl, Catherine Tachdjian, Hussien A. Al-Shamma, Andrea Fanjul, David P. M. Pleynet, Lyle W. Spruce
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Patent number: 7199124Abstract: The present invention relates to a c-Jun N-terminal kinase inhibitor containing an azole compound (I) substituted by a nitrogen-containing aromatic group having substituent(s)(except a compound represented by the formula: ) or a salt thereof or a prodrug thereof.Type: GrantFiled: February 1, 2002Date of Patent: April 3, 2007Assignee: Takeda Pharmaceutical Company LimitedInventors: Shigenori Ohkawa, Kenichi Naruo, Seiji Miwatashi, Hiroyuki Kimura, Tomohiro Kawamoto
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Patent number: 7183295Abstract: A compound represented by the following formula (1): (wherein each of R1 and R2, which may be identical to or different from each other, represents a hydrogen atom, a methyl group, or an ethyl group; each of R3a, R3b, R4a, and R4b, which may be identical to or different from each other, represents a hydrogen atom, a halogen atom, a nitro group, a hydroxyl group, a C1-4 alkyl group, a trifluoromethyl group, a C1-4 alkoxy group, a C1-4 alkylcarbonyloxy group, a di-C1-4 alkylamino group, a C1-4 alkylsulfonyloxy group, a C1-4 alkylsulfonyl group, a C1-4 alkylsulfinyl group, or a C1-4 alkylthio group, or R3a and R3b, or R4a and R4b may be linked together to form an alkylenedioxy group; X represents an oxygen atom, a sulfur atom, or N—R5 (R5 represents a hydrogen atom, a C1-4 alkyl group, a C1-4 alkylsulfonyl group, or a C1-4 alkyloxycarbonyl group); Y represents an oxygen atom, S(O)l (l is a number of 0 to 2), a carbonyl group, a carbonylamino group, an aminocarbonyl group, a sulfonylamino group, or an aminosuType: GrantFiled: April 20, 2006Date of Patent: February 27, 2007Assignee: Kowa Co., Ltd.Inventors: Yukiyoshi Yamazaki, Tsutomu Toma, Masahiro Nishikawa, Hidefumi Ozawa, Ayumu Okuda, Takaaki Araki, Kazutoyo Abe, Soichi Oda
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Patent number: 7166620Abstract: Compounds having general formula (I) are described, together with their use for the control of phytopathogenic fungiType: GrantFiled: December 11, 2002Date of Patent: January 23, 2007Assignee: Isagro Ricerca S.r.l.Inventors: Marilena Gusmeroli, Alessandro Ciapessoni, Franco Bettarini, Samuele Osti, Luigi Mirenna, Giovanni Camaggi, Alexia Elmini, Ramona Gironda
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Patent number: 7141672Abstract: This invention provides compounds of Formula I having the structure or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.Type: GrantFiled: January 8, 2004Date of Patent: November 28, 2006Assignee: WyethInventor: Michael S. Malamas
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Patent number: 7135488Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors.Type: GrantFiled: December 22, 2003Date of Patent: November 14, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Wolgang Guba, Wolfgang Haap, Hans Peter Marty, Robert Narquizian
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Patent number: 7119104Abstract: A compound represented by the formula (I) or a salt of the compound, and a PPAR-? activator which contains the compound or salt as the active ingredient: (wherein A represents O or S; B1 represents N, etc.; B2 represents O, etc.; each of X1 and X2 represents O, S, a bond, etc.; Y represents C1-8 alkylene chain; Z represents O or S; R1 represents aryl, etc. which can have substituents; R2 represents C1-8 alkyl, etc.; R3 represents C1-8 alkyl, C2-8 alkenyl, etc.; each of R4 and R5 represents hydrogen, C1-8 alkyl, etc.; and R6 represents hydrogen, etc.; provided that each of Z and R3 is attached to the benzene ring, and X2 is not attached to the benzene ring).Type: GrantFiled: October 9, 2002Date of Patent: October 10, 2006Assignee: Nippon Chemiphar, Co., Ltd.Inventors: Shogo Sakuma, Tomio Yamakawa, Takashi Kanda, Seiichiro Masui
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Patent number: 7105535Abstract: Compounds which are oxazolyl-pyrazole derivatives, as defined in the specification, and pharmaceutically acceptable salts thereof; are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, cell proliferative disorders, viral infections, autoimmune diseases and neurodegenerative disorders.Type: GrantFiled: January 28, 2002Date of Patent: September 12, 2006Assignee: Pfizer Italia S.R.L.Inventors: Daniela Berta, Eduard Felder, Anna Vulpetti, Marzia Villa
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Patent number: 7105556Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2, X3 and X4 are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.Type: GrantFiled: May 22, 2002Date of Patent: September 12, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Peter T. Cheng, Yoon Jeon, Wei Wang
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Patent number: 7101899Abstract: An optionally N-oxidized compound represented by the formula: wherein R1 represents hydrogen, hydrocarbon, heterocycle, amino, acyl, R2 represents an aromatic group, R3 represents hydrogen, pyridyl, aromatic hydrocarbon, X represents oxygen, optionally oxidized sulfur, Y represents a bond, an oxygen, optionally oxidized sulfur, a group represented by the formula NR4 (R4 represents hydrogen, hydrocarbon or acyl) and Z represents a bond or a divalent acyclic hydrocarbon, or a salt thereof has an excellent adenosine A3 receptor antagonistic activity and is used as an agent for preventing or treating diseases related to an adenosine A3 receptor. Furthermore, the compound (I) or a salt thereof has p38 MAP kinase inhibitory activity and TNF-? inhibitory activity and is used as an agent for preventing or treating diseases related to p38 MAP kinase and diseases related to TNF-?.Type: GrantFiled: April 20, 2000Date of Patent: September 5, 2006Assignee: Takeda Pharmaceutical Company LimitedInventors: Shigenori Ohkawa, Naoyuki Kanzaki, Seiji Miwatashi
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Patent number: 7094794Abstract: Substituted thiazole-benzoisothiazole dioxide derivatives, process for their preparation and their use. The invention relates to compounds of the formula I in which the radicals have the stated meanings, and to the physiologically tolerated salts thereof. The compounds are suitable for example as medicaments for lowering the blood glucose and for the prevention and treatment of diabetes.Type: GrantFiled: July 27, 2004Date of Patent: August 22, 2006Assignee: Sanofi-Aventis Deutschland GmbHInventors: Stefan Petry, Karl-Heinz Baringhaus, Norbert Tennagels, Guenter Mueller
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Patent number: 7067537Abstract: The present invention provides a pharmaceutical composition having a steroid C17,20-lyase inhibitory activity, which is useful as a prophylactic or therapeutic agent of prostatism, tumor such as breast cancer and the like, more particularly, a steroid C17,20-lyase inhibitor containing a compound represented by the formula: wherein A1 is an aromatic hydrocarbon group optionally having substituents or a heterocyclic group optionally having substituents, one of A2 and A3 is a hydrogen atom, a halogen atom, a C1-4 aliphatic hydrocarbon group optionally having substituents or an optionally esterified carboxyl group, the other of A2 and A3 is an aromatic hydrocarbon group optionally having substituents or a heterocyclic group optionally having substituents, and at least one of A1, A2 and A3 is a 3-pyridyl group optionally having substituents, or a salt thereof or a prodrug thereof.Type: GrantFiled: December 7, 2001Date of Patent: June 27, 2006Assignee: Takeda Pharmaceutical Company LimitedInventors: Noritaka Kuroda, Yoshi Nara, Shohei Hashiguchi, Akihiro Tasaka, Masami Kusaka, Masuo Yamaoka, Tomohiro Kaku
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Patent number: 7026316Abstract: The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: March 22, 2002Date of Patent: April 11, 2006Assignee: Merck & Co., Inc.Inventors: Wallace T. Ashton, Charles G. Caldwell, Hyun O. Ok, Emma R. Parmee, Ann E. Weber
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Patent number: 7026334Abstract: Pharmaceutical compositions containing as an active ingredient compounds of the general formula (I), prodrugs of the same, pharmaceutically acceptable salts of both, or solvates of them and exhibiting thrombopoietin receptor agonism: wherein X1 is optionally substituted heteroaryl or the like; Y1 is —NRACO— (CH2)0-2— or the like (wherein RA is a hydrogen or the like); Z1 is optionally substituted arylene or the like; and A1 is a ring represented by general formula (II) or (III):Type: GrantFiled: July 24, 2000Date of Patent: April 11, 2006Assignee: Shionogi & Co., Ltd.Inventors: Hiroshi Takemoto, Masami Takayama, Takeshi Shiota