Polycyclo Ring System Having The 1,3-oxazole Ring As One Of The Cyclos Patents (Class 546/271.7)
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Publication number: 20090082359Abstract: 5-pyridinone substituted indazoles of the formula and methods of their use are presented.Type: ApplicationFiled: July 18, 2008Publication date: March 26, 2009Applicant: AMR TECHNOLOGY, INC.Inventors: Peter Guzzo, Matthew David Surman, Alan John Henderson, Mark Hadden
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Publication number: 20090075938Abstract: There are disclosed compound of Formula (1): A1, A2, A3 and A4 which may be the same or different, represent N or CR1, X is a divalent group selected from O, S(O)n, C?W, NR4, NC(?O)R5 and CR6R7, W is O, S, NR20, Y is N or CR8, one of R4, R5, R6, R8, R9 and NR20 represents -L-R3, in which L is a single bond or a linker group, additionally, R1, R3-R9, which may be the same or different, independently represent hydrogen or a substituent and R20 represents hydrogen, hydroxyl, alkyl optionally substituted by aryl, alkoxy optionally substituted by aryl, aryl, CN, optionally substituted alkoxy, optionally substituted aryloxy, optionally substitute alkanoyl, optionally substituted aroyl, NO2, NR30R31, in which R30 and R31, which may be the same or different, represent hydrogen, optionally substituted alkyl or optionally substituted aryl; additionally, one of R30 and R31 may represent optionally substituted alkanoyl or optionally substituted aroyl, n represents an integer from 0 to 2, in addition, when an adjacent paiType: ApplicationFiled: February 9, 2007Publication date: March 19, 2009Inventors: Graham Michael Wynne, Stephen Paul Wren, Peter David Johnson, Paul Damien Price, Olivier De Moor, Gary Nugent, Richard Storer, Richard Joseph Pye, Colin Richard Dorgan
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Publication number: 20090042895Abstract: Compounds of the Formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa and bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.Type: ApplicationFiled: October 20, 2008Publication date: February 12, 2009Applicant: WyethInventors: Michael Byron Webb, Gary Paul Stack, Magda Asselin, Deborah A. Evrard
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Publication number: 20090042854Abstract: The present invention is directed to certain hexahydrpyrrolidinone compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.Type: ApplicationFiled: January 19, 2007Publication date: February 12, 2009Inventors: Jianming Bao, Robert J. DeVita, Huagang Lu, Sander G. Mills, Gregori J. Morriello
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Publication number: 20090012082Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity.Type: ApplicationFiled: November 3, 2005Publication date: January 8, 2009Applicant: CURIS, INC.Inventors: Olivin M. Guicherit, Edward Andrew Boyd, Judith Boyd, Shirley Ann Brunton, Stephen Price, John Harry Alexander Stibbard, Colin H. MacKinnon
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Publication number: 20080269191Abstract: The present invention relates to methods, compounds, and compositions for treating or preventing diseases associated with nonsense mutations in an mRNA by administering the compounds or compositions of the present invention. More particularly, the present invention relates to methods, compounds, and compositions for suppressing premature translation termination associated with a nonsense mutation in an mRNA.Type: ApplicationFiled: October 13, 2005Publication date: October 30, 2008Applicant: PTC THERAPEUTICS, INC.Inventors: Richard Wilde, Ellen Welch, Gary M. Karp
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Publication number: 20080261953Abstract: Compounds and compositions are provided for treatment or amelioration of one or more symptoms of ?-synuclein toxicity, ?-synuclein mediated diseases or diseases in which ?-synuclein fibrils are a symptom or cause of the disease. In one embodiment, the compounds for use in the compositions and methods are heteroaryl acylguanidines, heteroarylhydrazones, dihy-dropyridones, heteroaryl and aryl styryl ketones, and heteroarylpyrazoles.Type: ApplicationFiled: September 16, 2005Publication date: October 23, 2008Applicants: WHITEHEAD INSTITUTE FOR BIOMEDICAL RESEARCH, FOLDRX PHARMACEUTICALS, INC.Inventors: Susan L. Lindquist, Tiago Outeiro, Richard Labaudiniere
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Patent number: 7414046Abstract: The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates to methods for treating bacterial infections in mammala. The present invention also relates to methods for decreasing bacterial quantity in a biological sample.Type: GrantFiled: May 23, 2003Date of Patent: August 19, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Anne-Laure Grillot, Paul Charifson, Dean Stamos, Yusheng Liao, Michael Badia, Martin Trudeau
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Publication number: 20080161341Abstract: The present invention is directed to novel compounds of formula (I) wherein the variables are as defined herein. The compounds of formula (I) are useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.Type: ApplicationFiled: October 5, 2007Publication date: July 3, 2008Inventors: David J. Calderwood, Kristine E. Frank, David W. Borhani, Heather M. Davis, Nathan S. Josephsohn, Barbara S. Skinner
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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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Patent number: 7390825Abstract: Substituted oxazolidinone of the formula: wherein R2 is alkyl selected from the group consisting of methyl, ethyl, and isopropyl moieties, are described. The compounds are antibacterial.Type: GrantFiled: October 17, 2002Date of Patent: June 24, 2008Assignee: Board of Trustees of Michigan State UniversityInventors: Rawle I. Hollingsworth, Guijun Wang, Raghavakaimal Padmakumar, Jianmin Mao, Huiping Zhang, Zongmin Dai, Kanakamma Puthuparampil
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Patent number: 7378240Abstract: The present invention relates to new cyanine dyes according to the formula (I), wherein A1 and A2 are each independently O, S, or N, and R is H or a carbohydrate that may contain a hetero atom, and m is 0 to 5, and n is 0 to 5.Type: GrantFiled: November 10, 2003Date of Patent: May 27, 2008Assignee: Light Up Technologies ABInventors: Gunnar Westman, Jonas Karlsson
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Publication number: 20070244163Abstract: Fused-ring, heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein represents an optional double bond, and wherein An, En, Mn, Gn, Jn, R3, n7, R8, R9, R10, R11, R32, R33, X, Y, B and Het are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.Type: ApplicationFiled: April 11, 2007Publication date: October 18, 2007Inventors: Yan Xia, Mariappan V. Chelliah, Samuel Chackalamannil
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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: 7105680Abstract: Benzoxazole fluorescent sensor compounds and related ratiometric imaging methods for zinc metal ion.Type: GrantFiled: July 8, 2004Date of Patent: September 12, 2006Assignee: Northwestern UniversityInventors: Thomas V. O'Halloran, Masayasu Taki
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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: 6995162Abstract: Selected heterocyclic compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: January 10, 2002Date of Patent: February 7, 2006Assignee: Amgen Inc.Inventors: Guoqing Chen, Jeffrey Adams, Jean Bemis, Shon Booker, Guolin Cai, Lucian Di Pietro, Celia Dominguez, Daniel Elbaum, Julie Germain, Stephanie Geuns-Meyer, Michael Handley, Qi Huang, Joseph L. Kim, Tae-Seong Kim, Alexander Kiselyov, Xiaohu Ouyang, Vinod F. Patel, Leon M. Smith, Markian Stec, Andrew Tasker, Ning Xi, Shimin Xu, Chester Chenguang Yuan, Michael Croghan
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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
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Patent number: 6911448Abstract: The invention relates to a group of novel piperazine and piperidine derivatives of the formula wherein Y is hydrogen, halogen, alkyl (1-3C), or CN, CF3, OCF3, SCF3, alkoxy(1-3C), amino or mono- or dialkyl(1-3C) substituted amino or hydroxy, X is O, S, SO or SO2, ---Z represents —C, ?C or —N, R1 and R2 independently represent hydrogen or alkyl (1-3C), Q is benzyl or 2-, 3- or 4-pyridylmethyl, wich groups may be substited with one or more more substituents from the group halogen, nitro, cyano, amino, mono- or di (1-3C)alkylamino, (1-3C) alkoxy, CF3, OCF3, SCF3, (1-4C)-alkyl, (1-3C)alkylsulfonyl or hydroxy, and salts and prodrugs thereof.Type: GrantFiled: May 10, 2001Date of Patent: June 28, 2005Assignee: Solvay Pharmaceuticals B.V.Inventors: Roelof W. Feenstra, Johannes A. M. van der Heijden, Cornelis G. Kruse, Stephen K. Long, Gustaaf J. M. van Scharrenburg
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Patent number: 6878714Abstract: Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: July 17, 2002Date of Patent: April 12, 2005Assignee: Amgen Inc.Inventors: Benny Askew, Jeffrey Adams, Shon Booker, Guoqing Chen, Lucian V. DiPietro, Daniel Elbaum, Julie Germain, Stephanie D. Geuns-Meyer, Gregory J. Habgood, Michael Handley, Qi Huang, Tae-Seong Kim, Aiwen Li, Nobuko Nishimura, Rana Nomak, Vinod F. Patel, Babak Riahi, Joseph L. Kim, Ning Xi, Kevin Yang, Chester Chenguang Yuan
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Patent number: 6867211Abstract: The present invention relates to 4-pyridyl- and 2,4-pyrimidinyl-substituted pyrrole derivatives and their use in pharmacy, of the formula 1: in which the variables have the meanings indicated in the description. The compounds according to the invention have immunomodulating and/or cytokine release-inhibiting action and are therefore utilizable for the treatment of disorders which are connected with a disturbance of the immune system.Type: GrantFiled: January 31, 2001Date of Patent: March 15, 2005Assignee: Merckle GmbHInventors: Hans-Guenter Striegel, Stefan Laufer, Karola Tollmann, Susanne Tries
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Patent number: 6849647Abstract: The present invention provides to a novel compound having an ACAT inhibiting activity.Type: GrantFiled: September 20, 2000Date of Patent: February 1, 2005Assignee: Kowa Company, Ltd.Inventors: Kimiyuki Shibuya, Toru Miura, Katsumi Kawamine, Yukihiro Sato, Tadaaki Ohgiya, Takahiro Kitamura, Chiyoka Ozaki, Toshiyuki Edano, Mitsuteru Hirata
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Patent number: 6844295Abstract: The present invention relates to benzoxazole compounds represented by the following formula (I): wherein R1 to R4 may be the same or different from each other, and each represent a hydrogen atom, alkyl group having 1 to 6 carbon atoms, alkoxy group having 1 to 4 carbon atoms, haloalkyl group having 1 to 4 carbon atoms, haloalkoxy group having 1 to 4 carbon atoms, halogen atom, nitro group, cyano group, R12S(O)n, alkoxycarbonyl group having 1 to 4 carbon atoms, amino group, —NHCOR11 or carbonyl group, where R11 and R12 each represent an alkyl group having 1 to 6 carbon atoms, and n is an integer of 0 to 2, A represents a single bond, CHR5—Y, CR5?CR6, CR5R7—CHR6 or CHR5, where R5 represents a hydrogen atom, hydroxyl group, halogen atom or alkyl group, R6 and R7 each represent a hydrogen atom, hydroxyl group, alkyl group, halogen atom or substituted sulfonyloxy group, Y represents O, S or NH, and W represents a substituted or unsubstituted benzene ring or hetero ring, and processes for preparing the same.Type: GrantFiled: July 4, 2001Date of Patent: January 18, 2005Assignee: Ube Industries, Ltd.Inventors: Shohei Fukuda, Akira Nakamura, Motohisa Shimizu, Tatsuo Okada, Satoshi Oohida, Takehiko Asahara
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Patent number: 6825218Abstract: The invention relates to spherical telithromycin clusters and to a method for the production thereof characterized in that a telithromycin crystal suspension is prepared, said crystals are coated with a telithromycin insoluble phase which gradually crystallizes. The spherical telithromycin clusters are used in the preparation of micro-capsules.Type: GrantFiled: July 1, 2002Date of Patent: November 30, 2004Assignee: Aventis Pharma S. A.Inventors: Jean-Yves Godard, Valerie Rognon-Ravaux
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Patent number: 6800648Abstract: Compounds of the formula useful for treatment of disorders of the dopaminergic system, such as schizophrenia, schizoaffective disorder, bipolar disorder, Parkinson's disease, L-DOPA induced pychoses and dyskinesias, Tourette's syndrome and hyperprolactinemia and in the treatment of drug addiction such as the addiction to ethanol, nicotine or cocaine and related illnesses.Type: GrantFiled: April 25, 2002Date of Patent: October 5, 2004Assignee: WyethInventors: Megan Tran, Gary P. Stack
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Publication number: 20040132046Abstract: The present invention relates to new cyanine dyes according to the formula (I), wherein A1 and A2 are each independently O, S, or N, and R is H or a carbohydrate that may contain a hetero atom, and m is 0 to 5, and n is 0 to 5.Type: ApplicationFiled: November 10, 2003Publication date: July 8, 2004Applicant: Light Up Technologies ABInventors: Gunnar Westman, Jonas Karlsson
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Publication number: 20040087626Abstract: New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.Type: ApplicationFiled: March 31, 2003Publication date: May 6, 2004Inventors: Paul A. Renhowe, Savithri Ramurthy, Payman Amiri, Barry Haskell Levine, Daniel J. Poon, Skaradha Subramanian, Leonard Sung, Wendy Fantl
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Patent number: 6716987Abstract: An oxygen-containing heterocyclic compound represented by following Formula (I): wherein R1 and R2 independently represent hydrogen, lower alkyl, cyano, —(CH2)n—E1—CO—G1 (wherein E1 represents a bond, O, or NH; and G1 represents hydrogen, substituted or unsubstituted lower alkyl, OR6, or NR7R8; and n represents an integer of 0 to 4), or the like; R1 and R2 are combined to represent a saturated carbon ring together with a carbon atom adjacent thereto; or R2, and R11 or R13 described below are combined to form a single bond; R3 represents hydrogen, phenyl, or halogen; R4 represents hydroxy, lower alkoxy, or the like; A represents —C(R9)(R10)— or O; B represents O, NR11, —C(R12)(R13)—, or —C(R14)(R15)— C(R16)(R17)—; D represents (i) —C(R18)(R19)—X— (wherein X represents —C(R21)(R22)—, S, or NR23), (ii) —C(R19a)═Y— [Y represents —C(R24)—Z— (wherein Z representsType: GrantFiled: December 20, 2001Date of Patent: April 6, 2004Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Ohshima, Takashi Kawakita, Koji Yanagawa, Kyoichiro Iida, Rie Koike, Yoshisuke Nakasato, Tohru Matsuzaki, Kenji Ohmori, Soichiro Sato, Hidee Ishii, Haruhiko Manabe, Michio Ichimura, Fumio Suzuki
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Patent number: 6706711Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein R1, R2, T, n and Q are as described in the specification. The compounds are useful for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases, such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.Type: GrantFiled: April 26, 2002Date of Patent: March 16, 2004Assignee: Vertex Pharmaceuticals IncorporatedInventor: Michael R. Hale
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Patent number: 6706738Abstract: The invention is directed to physiologically active compounds of general formula (I): R1Z1—Het—L1—Ar1—L2—Y (I) wherein Het is an optionally substituted, saturated, partially saturated or fully unsaturated 8 to 10 membered bicyclic ring containing at least one heteroatom selected from O, S or N; R1 is optionally substituted aryl, heteroaryl, alkyl, alkenyl, alkynyl, cycloalkyl or heterocycloalkyl; Z1 represents a direct bond, an alkylene chain, NR4, O or S(O)n; L1 is an a —R5—R6— linkage where R5 is alkylene, alkenylene or alkynylene and R6 is a direct bond, cycloalkylene, heterocycloalkylene, arylene, heteroaryldiyl, —C(═Z3)—NR4—, —NR4—C(═Z3)—, —Z3—, —C(═O)—, —C(═NOR4)—, —NR4—, —NR4—C(═Z3)—NR4—, —SO2—NR4—, —NR4—SO2—, —O—C(═O)—, —C(═O)—O—,Type: GrantFiled: October 11, 2001Date of Patent: March 16, 2004Assignee: Aventis Pharma LimitedInventors: David Edward Clark, Paul Robert Eastwood, Neil Victor Harris, Clive McCarthy, Andrew David Morley, Stephen Dennis Pickett
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Publication number: 20040047806Abstract: A new class of alpha-cyanomethine and alpha-cyanopolymethine dyes is provided having moieties which serve for the covalent attachment to biological substrates and resulting in the fluorescent labeling of the substrates. The labeled substrates are useful in analytical techniques for the detection and measurement of biological and clinical compounds of interest. Of particular interest is a class of methine molecules which are non-fluorescent in buffer solutions but intensely fluoresce when they enter a cell.Type: ApplicationFiled: September 9, 2003Publication date: March 11, 2004Inventor: Spyros Theodoropulos
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Publication number: 20040044219Abstract: The present invention relates to a method for the manufacture of asymmetric cyanine dyes of general formula (Ia, Ib, Ic, Id), whereby the dye is produced by carrying out a solid phase condensation reaction.Type: ApplicationFiled: September 29, 2003Publication date: March 4, 2004Inventors: Jennie Sandstrom, Gunnar Westman
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Publication number: 20040029925Abstract: The present invention provides a genus of bis-benzimidazole compounds, methods and pharmaceutical compositions that are useful as modulators of potassium ion channels. The compounds of the invention are of use in both therapeutic and diagnostic methods.Type: ApplicationFiled: May 13, 2003Publication date: February 12, 2004Applicant: ICAgen, Inc.Inventors: Xiaodong Wang, Alan B. Fulp, Albert M. van Rhee, Kerry L. Spear
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Publication number: 20040014977Abstract: The present invention relates to benzoxazole compounds represented by the following formula (I): 1Type: ApplicationFiled: January 6, 2003Publication date: January 22, 2004Inventors: Shohei Fukuda, Akira Nakamura, Motohisa Shimizu, Tatsuo Okada, Satoshi Oohida, Takehiko Asahara
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Patent number: 6677341Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Substitutedamino-(n+1)-Alkanol compounds are substituted (R)-Chiral heteroaryl aminoalcohols.Type: GrantFiled: December 12, 2001Date of Patent: January 13, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Publication number: 20040006110Abstract: The present invention is directed in part towards methods of modulating the function of calcium channels with pyridine- or 1,4-dihydropyridine-based compounds. In addition, the invention describes methods of preventing and treating protein kinase-related abnormal conditions in organisms with a compound identified by the invention. Furthermore, the invention pertains to pyridine- or 1,4-dihydropyridine-based compounds and pharmaceutical compositions comprising these compounds.Type: ApplicationFiled: January 14, 2003Publication date: January 8, 2004Inventors: Phani Kumar Pullela, Paramashivappa Rangappa, Srinivasa Rao Alapati, Pillarisetti V. Subbarao, Jeffrey A. Bibbs
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Publication number: 20040002518Abstract: Organic compounds having the structural formulas I, II, and III are provided where the variables have the values described herein and R1 and R2 in structure I join together to form a 5 to 7 membered substituted or unsubstituted ring including at least one O, N, or S atom, and Z is an O, S, NH or NR group in structures I and II.Type: ApplicationFiled: June 2, 2003Publication date: January 1, 2004Applicant: Chiron CorporationInventors: Paul A. Renhowe, Cynthia M. Shafer
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Patent number: 6660751Abstract: The invention relates to novel sulfonamide compounds having 5-HT7 receptor antagonist activity, processes for their preparation, to compositions containing them and to their use in the treatment of CNS and other disorders.Type: GrantFiled: September 20, 2001Date of Patent: December 9, 2003Assignee: SmithKline Beecham p.l.c.Inventor: Peter John Lovell
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Publication number: 20030225106Abstract: Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: ApplicationFiled: July 17, 2002Publication date: December 4, 2003Applicant: Amgen Inc.Inventors: Benny Askew, Jeffrey Adams, Shon Booker, Guoqing Chen, Lucian V. DiPietro, Daniel Elbaum, Julie Germain, Stephanie D. Geuns-Meyer, Gregory J. Habgood, Michael Handley, Qi Huang, Tae-Seong Kim, Aiwen Li, Nobuko Nishimura, Rana Nomak, Vinod F. Patel, Babak Riahi, Joseph L. Kim, Ning Xi, Kevin Yang, Chester Chenguang Yuan
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Publication number: 20030225131Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: 1Type: ApplicationFiled: March 17, 2003Publication date: December 4, 2003Inventors: Christopher S. Burgey, Zhengwu J. Deng
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Patent number: 6645259Abstract: Cationic aminoanthraquinones in which at least one cationic charge is delocalized on a 5-membered unsaturated polynitrogen-containing heterocycle, their use as a direct dye in dyeing compositions for keratinous materials, in particular for human keratinous fibers such as hair, dyeing compositions containing them, and dyeing methods using these compositions.Type: GrantFiled: July 9, 2002Date of Patent: November 11, 2003Assignee: L'Oreal S.A.Inventors: Alain Genet, Alain Lagrange
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Patent number: 6632809Abstract: The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates to methods for treating bacterial infections in mammala. The present invention also relates to methods for decreasing bacterial quantity in a biological sample.Type: GrantFiled: December 12, 2001Date of Patent: October 14, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: Anne-Laure Grillot, Paul Charifson, Dean Stamos, Yusheng Liao, Michael Badia, Martin Trudeau
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Publication number: 20030191161Abstract: The invention relates to substituted and unsubstituted 3H-benzo[1,2,3]oxathiazole 2,2-dioxides, 1,3-dihydrobenzo[1,2,5]thiadiazole 2,2-dioxides and 1,3-dihydrobenzo[c]isothiazole 2,2-dioxides, to their preparation and to their use in medicaments.Type: ApplicationFiled: March 31, 2003Publication date: October 9, 2003Inventors: Stefan Petry, Karl-Heinz Baringhaus, Swen Hoelder, Guenter Mueller
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Publication number: 20030186991Abstract: The invention provides compounds which inhibit reverse transcriptase (RT) and which inhibit replication of a retrovirus, such as human immunodeficiency virus-1 (HIV-1). The compound of the invention are phenoxyethyl-thiourea-pyridines. The invention additionally provides a method for inhibiting reverse transcriptase activity of a retrovirus, such as HIV-1, comprising contacting the retrovirus with a compound of the invention. The invention additionally provides a method for inhibiting replication of a retrovirus, such as HIV-1, comprising contacting the retrovirus with a compound of the invention.Type: ApplicationFiled: April 15, 2003Publication date: October 2, 2003Applicant: Parker Hughes InstituteInventors: Fatih M. Uckun, Taracad K. Venkatachalam
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Publication number: 20030166658Abstract: The invention relates to novel 2-benzimidazolyl-, 2-benzoxazolyl- and 2-benzothiazolyl hydrazones that are derived from 2-formylpyridine, 2-acylpyridines, acetyldiazines and acetyl(iso)quinolines. The invention also relates to a novel method for producing 2-benzimidazolyl-, 2-benzoxazolyl- and 2-benzothiazolyl hydrazones and to their use as useful anti-cancer therapeutic agents. The novel compounds are also active against multidrug-resistant cancer cells.Type: ApplicationFiled: December 4, 2002Publication date: September 4, 2003Inventors: Johann Hofmann, Gottfried Heinisch, Johnny Easmon, Gerhard Purstinger, Heinz-Herbert Fiebig
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Patent number: 6608098Abstract: This invention relates to compounds represented by the general formula [I] wherein, R represents an azido group, etc., R1 and R2 are the same or different and represent hydrogen atoms, etc., R3 and R4 are the same or different and represent hydrogen atoms, etc., X1 represents an oxygen atom, etc., X2 represents an oxygen atom, etc., Y represents an oxygen atom, etc., and Z represents a condensed aryl group, etc., or a pharmaceutically acceptable salt thereof, preparation processes thereof, and an agent for treating diabetes, a prophylactic agent for chronic complications of diabetes or a drug against obesity, containing, as an effective ingredient, the compound or the pharmaceutically acceptable salt thereof.Type: GrantFiled: February 25, 2002Date of Patent: August 19, 2003Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Toshio Nagase, Tomoharu Iino, Yoshiyuki Sato, Teruyuki Nishimura, Jun-ichi Eiki
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Publication number: 20030153558Abstract: The present invention relates to 4-pyridyl- und 2,4-pyrimidinyl-substituted pyrrole derivatives and their use in pharmacy, of the formula 1 1Type: ApplicationFiled: November 5, 2002Publication date: August 14, 2003Inventors: Hans-Guenter Striegel, Stefan Laufer, Karola Tollmann, Susanne Tries
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Publication number: 20030125340Abstract: 3-(amino- or aminoalkyl) pyridinone derivatives having the formula (1) 1Type: ApplicationFiled: July 15, 2002Publication date: July 3, 2003Applicant: Centre National De La Recherche Scient.Inventors: Emile Bisagni, Valerie Dolle, Chi Hung Nguyen, Claude Monneret, David Grierson, Anne-Marie Aubertin
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Patent number: RE39198Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amounts of one of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: November 15, 2000Date of Patent: July 18, 2006Assignee: Aventis Pharmaceuticals Inc.Inventors: Joseph T. Strupczewski, Grover C. Helsley, Yulin Chiang, Kenneth J. Bordeau, Edward J. Glamkowski
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Patent number: RE40245Abstract: The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates to methods for treating bacterial infections in mammala. The present invention also relates to methods for decreasing bacterial quantity in a biological sample.Type: GrantFiled: April 28, 2004Date of Patent: April 15, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Anne-Laure Grillot, Paul S. Charifson, Dean Stamos, Yusheng Liao, Michael C. Badia, Martin Trudeau