Plural 1,3-diazine Rings Patents (Class 544/296)
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Patent number: 6890926Abstract: The invention relates to novel quinoline derivatives of the formula 1, to their preparation and to their use as medicaments, in particular for treating tumors.Type: GrantFiled: July 20, 2001Date of Patent: May 10, 2005Assignee: Zentaris AGInventors: Peter Emig, Eckhard Günther, Jürgen Schmidt, Bernd Nickel, Bernhard Kutscher
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Patent number: 6887875Abstract: Diarylpyrimidine compounds of Formula I are provided, wherein.Type: GrantFiled: May 22, 2002Date of Patent: May 3, 2005Assignee: Neurogen CorporationInventors: Jianhua Huang, Kevin Hodggetts, Dario Doller, Ping Ge, Yasuchika Yamaguchi
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Patent number: 6878717Abstract: This invention concerns the use of compounds of formula: the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein -a1=-a2-a3=a4- forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxy-carbonyl, substituted C1-6alkyl, or substituted C1-6alkyloxyC1-6alkylcarbonyl; each R2 independently is hydroxy, halo, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalo-methylthio, —S(?O)pR6, —NH—S(?O)pR6, —C(?O)R6, —NHC(?O)H, —C(?O)NHNH2, —NHC(?O)R6, —C(?NH)R6 or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or L is —X—R3 wherein R3 is optionally subsType: GrantFiled: November 1, 1999Date of Patent: April 12, 2005Inventors: Bart De Corte, Marc Rene De Jonge, Jan Heeres, Chih Yung Ho, Paul Adriaan Jan Janssen, Robert W. Kavash, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken
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Patent number: 6861417Abstract: Novel pyridin-4-yl or pyrimidin-4-yl substituted pyrazine compounds and compositions for use in therapy.Type: GrantFiled: April 14, 2003Date of Patent: March 1, 2005Assignee: SmithKline Beecham CorporationInventors: Jerry L. Adams, Ralph F. Hall, Jeffrey C. Boehm
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Patent number: 6849627Abstract: The present invention relates to compounds which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the formula: wherein R1 is substituted aryl; R4 is substituted or unsubstituted aryl or heteroaryl.Type: GrantFiled: March 17, 2003Date of Patent: February 1, 2005Assignee: The Procter & Gamble CompanyInventors: Michael Philip Clark, Matthew John Laufersweiler, Adam Golebiowski, Mark Sabat, Todd Andrew Brugel
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Patent number: 6849622Abstract: The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein A represents —CH2— or —S—, R1 represents hydrogen atom, a lower alkyl group, a hydroxy lower alkyl group or a lower alkoxy lower alkyl group, X represents —N(R3)—, —O— or —CO—, where R3 represents hydrogen atom or a lower alkyl group, and R2 represents (1) a cyclic group which may be substituted, or (2) an amino group which may be substituted, or a pharmaceutically acceptable salt thereof, a method for preparing the above-mentioned compound and a pharmaceutical composition comprising the above-mentioned compound as an effective ingredient.Type: GrantFiled: October 5, 2001Date of Patent: February 1, 2005Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Kosuke Yasuda, Hiroshi Morimoto, Saburo Kawanami, Masataka Hikota, Takeshi Matsumoto, Kenji Arakawa
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Patent number: 6838461Abstract: Compounds of the formula I in which R1, R2, R4 and R5 have the meanings indicated in claim 1, are potent 5-HT2A antagonists and are suitable for the treatment of psychoses, schizophrenia, depression, neurological disorders, memory disorders, Parkingson's disease, amyotrophic lateral sclerosis, Alzheimer's disease, Huntington's disease, eating disorders such as bulimia, nervous anorexia, premenstrual syndrome and/or for positively affecting compulsive behavior (obsessive-compulsive disorder, OCD).Type: GrantFiled: July 7, 2000Date of Patent: January 4, 2005Assignee: Merck Patent GmbHInventors: Henning Boettcher, Christoph Seyfried
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Patent number: 6833364Abstract: The present invention relates to novel substituted pyrazole derivatives of the general formula (I) in which the substituents R1, R2, R3, A, X and Y are each as defined, and to processes for their preparation and to their use as medicaments, in particular as medicaments for the treatment of cardiovascular disorders.Type: GrantFiled: March 26, 2001Date of Patent: December 21, 2004Assignee: Bayer HealthCare AGInventors: Alexander Straub, Achim Feurer, Cristina Alonso-Alija, Elke Stahl, Johannes-Peter Stasch, Elisabeth Perzborn, Joachim Hütter, Klaus Dembowsky
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Patent number: 6833378Abstract: Corticotropin-releasing factor (CRF) antagonists having the formulae wherein the dashed lines, A, B, Y, Z, G, R3, R4, R5, R6, R16 and R17 are as defined in the application, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment disorders including CNS and stress-related disorders.Type: GrantFiled: January 17, 2001Date of Patent: December 21, 2004Assignee: Pfizer IncInventor: Yuhpyng L. Chen
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Patent number: 6821971Abstract: The present invention relates to compound which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the formula: wherein R comprises ethers or amines; R1 is: a) substituted or unsubstituted aryl; or b) substituted or unsubstituted heteroaryl; R2a and R2b units are each independently hydrogen, ethers, amines, amides, carboxylates, or said units can form a double bond, a carbonyl, or R2a and R2b can be taken together to form a substituted or unsubstituted ring comprising from 4 to 8 atoms, said ring selected from the group consisting of: i) carbocyclic; ii) heterocyclic; iii) aryl; iv) heteroaryl; v) bicyclic; and vi) heterobicyclic.Type: GrantFiled: September 18, 2002Date of Patent: November 23, 2004Assignee: The Procter & Gamble CompanyInventors: Michael Philip Clark, Matthew John Laufersweiler, Jane Far-Jine Djung, Biswanath De
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Publication number: 20040219390Abstract: Benzoxazinone and quinazolinone compounds useful in organic light emitting devices (OLEDS) are described.Type: ApplicationFiled: January 23, 2004Publication date: November 4, 2004Applicant: Honeywell International, Inc.Inventors: Thomas Potrawa, John Magno, Ilyas Khayrullin, Susanne Hoyer
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Patent number: 6811595Abstract: Compounds of the formulae wherein, provided that at least one of R1, R2, and R3 is not a hydrogen atom, R1, R2 and R3 each, independently of the other, is hydrogen, alkyl, aryl, arylalkyl, or alkylaryl, and wherein R1 and R2 can also be alkoxy, aryloxy, arylalkyloxy, alkylaryloxy, polyalkyleneoxy, polyaryleneoxy, polyarylalkyleneoxy, polyalkylaryleneoxy, silyl, siloxane, polysilylene, polysiloxane, or a group of the formula wherein r and s are integers representing a number of repeat —CH2— groups, and wherein X is a direct bond, oxygen, sulfur, —NR40— wherein R40 is hydrogen, alkyl, aryl, arylalkyl, or alkylaryl, or —CR50R60— wherein R50 and R60 each, independently of the other, is hydrogen, alkyl, aryl, arylalkyl, or alkylaryl, and R10 and R11 each, independently of the other, is alkylene, arylene, arylalkylene, or alkylarylene, and wherein R10 can also be polyalkyleneoxy, polyaryleneoxy, polyarylalkyleneoxy, polyalkylaryleneoxy, silylenType: GrantFiled: September 4, 2002Date of Patent: November 2, 2004Assignee: Xerox CorporationInventors: Danielle C. Boils-Boissier, Marcel P. Breton, Jule W. Thomas, Jr., Donald R. Titterington, Jeffrey H. Banning, H. Bruce Goodbrand, James D. Wuest, Marie-Eve Perron, Hugues Duval
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Patent number: 6794386Abstract: The present invention relates to a compound of the general formula (I), wherein R1 together with the C atom to which it is attached, and R2 together with the N atom to which it is attached, form a piperidinyl ring; X represents a bond, oxygen or —NR12—; and Y represents oxygen; pharmaceutical compositions containing such a compound, as well as the use of such a compound for the production of pharmaceutical compositions, and for the treatment of inflammatory, auto-immune and immune diseases.Type: GrantFiled: November 19, 2002Date of Patent: September 21, 2004Assignee: Bayer AktiengesellschaftInventors: Markus Albers, Thomas Lehmann, Thomas Rölle, Gerhard Müller, Gerhard Hessler, Masaomi Tajimi, Karl Ziegelbauer, Hiromi Okigami, Haruki Hasegawa
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Publication number: 20040176384Abstract: The present invention is directed to curcumin analogs exhibiting anti-tumor and anti-angiogenic properties, pharmaceutical formulations including such compounds and methods of using such compounds.Type: ApplicationFiled: October 21, 2003Publication date: September 9, 2004Applicant: Emory UniversityInventors: James P. Snyder, Matthew C. Davis, Brian Adams, Mamoru Shoji, Dennis C. Liotta, Eva M. Ferstl, Ustun B. Sunay
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Patent number: 6787546Abstract: The object of the invention is to provide an excellent compound as a drug. The invention relates to a heterocyclic compound shown by the following formula: A—B—D—E [1] wherein A is heteroaryl or its oxide; B is ethenylene; D is optionally substituted phenylene; and E is a group of the formula: wherein G is optionally substituted phenyl; and R is heteroaryl or heteroarylmethyl, or a group of the formula: wherein n is an integer of 1 to 5; R5 and R6 are same or different and are independently selected from the group consisting of hydrogen, C1—C6 alkyl, hydroxyalkyl, aminoalkyl; or R5 and R6 taken together with the adjacent nitrogen atom may form 5- to 7-membered cyclic amino group for —NR5R6 or a salt thereof.Type: GrantFiled: June 12, 2002Date of Patent: September 7, 2004Assignee: Nippon Shinyaku Co., Ltd.Inventors: Toshiyuki Suzuki, Tomiyoshi Aoki
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Patent number: 6787539Abstract: The invention relates to compounds of the formula wherein R1 is lower alkyl, lower alkoxy, pyridinyl, pyrimidinyl, phenyl, —S-lower alkyl, —S(O)2-lower alkyl, —N(R)—(CH2)n—N(R)2, —O—(CH2)n—N(R)2, —N(R)2, or a cyclic tertiary amine of the group which may contain one additional heteroatom, selected from N, O or S, and wherein this group may be connected with the pyrimidine ring via the linker —O(CH2)n—; R2 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R3/R3′ is, independently from each other, hydrogen or lower alkyl; R4 is independently from each other halogen, trifluoromethyl or lower alkoxy; R5 is hydrogen or lower alkyl; R is, independently from each other, hydrogen or lower alkyl; X is —C(O)N(R)— or —N(R)C(O)—; Y is —O—, —S—, —SO2—, - or —N(R)—; n is 1,2,3 or 4; and m is 0,1 or 2; or a pharmaceuticType: GrantFiled: October 15, 2001Date of Patent: September 7, 2004Assignee: Hoffmann-La Roche Inc.Inventor: Heinz Stadler
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Patent number: 6787542Abstract: The present invention relates to novel heterocyclyl-containing diaryl sulfide compounds that are useful for treating inflammatory and immune diseases, to pharmaceutical compositions comprising these compounds, and to methods of inhibiting inflammation or suppressing immune response in a mammal.Type: GrantFiled: June 25, 2001Date of Patent: September 7, 2004Assignee: ICOS CorporationInventors: Gary T. Wang, Sheldon Wang, Robert Gentles
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Publication number: 20040162302Abstract: Novel crystals of a potassium salt of (E)-N-[6-methoxy-5-(2-methoxyphenoxy)-2-(pyrimidin-2-yl)pyrimidin-4-yl]-2-phenylethenesulfonamide, a preparation process thereof, and novel solvates of (E)-N-[6-methoxy-5-(2-ethoxyphenoxy)-2-(pyrimidin-2-yl)pyrimidin-4-yl]-2-phenylethenesulfonamide.Type: ApplicationFiled: January 26, 2004Publication date: August 19, 2004Inventors: Yoshinori Kato, Hironori Harada, Masahiro Kurotani, Haruhiko Toda, Kenichirou Sakamoto
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Publication number: 20040138244Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.Type: ApplicationFiled: October 14, 2003Publication date: July 15, 2004Inventors: James T. Dalton, Duane D. Miller
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Publication number: 20040122015Abstract: A compound of Formula (I): 1Type: ApplicationFiled: November 25, 2003Publication date: June 24, 2004Inventors: David W. Boykin, Richard R. Tidwell, Mohamed A. Ismail, Reto Brun
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Publication number: 20040116445Abstract: The present invention is directed to chemical compositions of substituted thioacetamides, processes for the preparation thereof and uses of the compositions in the treatment of diseases.Type: ApplicationFiled: November 18, 2003Publication date: June 17, 2004Inventors: Edward R. Bacon, Sankar Chatterjee, Derek Dunn, John P. Mallamo, Matthew S. Miller, Rabindranath Tripathy, Jeffry L. Vaught
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Patent number: 6750342Abstract: The invention relates to substituted polycyclic aryl and heteroaryl pyrimidinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.Type: GrantFiled: May 18, 2000Date of Patent: June 15, 2004Assignee: Pharmacia CorporationInventors: Michael South, Ashton T. Hamme, II, William L. Neumann, Darin E. Jones, Melvin L. Rueppel
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Publication number: 20040106622Abstract: An aryl-substituted alicyclic compound of the formula (I): 1Type: ApplicationFiled: September 22, 2003Publication date: June 3, 2004Inventors: Toshiya Morie, Seiji Iwama, Mitsue Notake, Tomoko Kitano
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Publication number: 20040097529Abstract: Novel use of N-[6-methoxy-5-(2-methoxyphenoxy)-2-(pyrimidin-2-yl)pyrimidin-4-yl]-2-phenylethenesulfonamide or a pharmaceutically acceptable salt thereof. Improvement of the following particular condition in a diabetic patient: (1) Elevation of blood glucose level; (2) Elevation of blood lipid level after the onset of early-stage nephropathy; (3) Renal dysfunction after the onset of early-stage nephropathy; (4) Increase of urinary albumin excretion after the onset of early-stage nephropathy; (5) Glomerular hyperfiltration after the onset of early-stage nephropathy; (6) Renal dysfunction after the progress toward chronic renal failure; (7) Increase of urinary protein excretion after the progress toward chronic renal failure.Type: ApplicationFiled: September 26, 2003Publication date: May 20, 2004Inventors: Akira Fujimori, Hironori Yuyama, Atsuo Tahara, Rie Sonoda, Kumiko Shibasaki
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Publication number: 20040087604Abstract: The present invention provides a compound of the formula (I): 1Type: ApplicationFiled: July 3, 2003Publication date: May 6, 2004Inventors: Tatsuo Tsuri, Shozo Takechi, Isao Horibe
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Patent number: 6720322Abstract: The present invention relates to novel butyne diol derivatives of the general formula I and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more compounds of the general formula I and especially their use as endothelin receptor antagonists.Type: GrantFiled: June 24, 2002Date of Patent: April 13, 2004Assignee: Actelion Pharamceuticals Ltd.Inventors: Martin Bolli, Christoph Boss, Martine Clozel, Walter Fischli
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Patent number: 6716845Abstract: The present invention pertains to derivatives of 5,5-disubstituted pyrimidine-2,4,6,-trianones having the formula: wherein R1, R2, R3, and R4 are described herein. These compounds have antitumor and antimetastatic activity.Type: GrantFiled: February 25, 2002Date of Patent: April 6, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Dagmar Geppert, Frank Grams, Hans-Willi Krell, Herbert Leinert, Ernesto Menta, Gerd Zimmermann
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Publication number: 20040060474Abstract: Disclosed are compounds of the formulae 1Type: ApplicationFiled: September 4, 2002Publication date: April 1, 2004Applicant: Xerox CorporationInventors: Danielle C. Boils-Boissier, Marcel P. Breton, Jule W. Thomas, Donald R. Titterington, Jeffrey H. Banning, H. Bruce Goodbrand, James D. Wuest, Marie-Eve Perron, Hugues Duval
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Patent number: 6699862Abstract: Novel indolyl-2-phenyl bisamidines are described which are DNA methyltransferase inhibiting agents, and pharmaceutical compositions containing them are used as antiproliferative agents for treating a disease, especially a neoplastic disease, characterized by abnormally rapid proliferation of tissue involved in said disease; said indolyl-2-phenyl bisamidines comprising a and a pharmaceutically acceptable salt thereof, wherein: R1 is hydrogen or (C1-C3)alkyl; R3, R4, R5, R8, R9, and R10 are hydrogen or (C1-C3)alkyl, or R3 and R4 may be taken together, or R8 and R9 may be taken together with the nitrogen atoms to which they are attached, to form an imidazolinyl group; R14 is —H; —NHC(═O)(CH2)mR20; —(CH2)mR20; —CH(CH3)R20; —(CH2)m(C6H3)—R17; —(CH2)m(C6H3)—R20; —(CH2)m(heterocyclyl)—R17; —(CH2)m(heterocyclyl)—R20; —CH2CH═CHR20; —(CH2)mC(═O)NH—CHR20R21; or —(CH2)mC(═O)NH—CH2&mType: GrantFiled: March 24, 2000Date of Patent: March 2, 2004Assignee: Pfizer Inc.Inventors: Steven W. Goldstein, Banauara L. Mylari, Jose R. Perez, Edward A. Glazer
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Publication number: 20040038971Abstract: The present invention relates to compounds which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the formula: 1Type: ApplicationFiled: March 17, 2003Publication date: February 26, 2004Applicant: The Procter & Gamble CompanyInventors: Michael Philip Clark, Matthew John Laufersweiler, Adam Golebiowski, Mark Sabat, Todd Andrew Brugel
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Publication number: 20040009975Abstract: Pyrimidinedione derivatives of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them are useful for the treatment of inflammation and immunological diseases.Type: ApplicationFiled: April 9, 2003Publication date: January 15, 2004Applicant: ORCHID CHEMICALS & PHARMACEUTICALS LIMITEDInventors: Shiv Kumar Agarwal, Ravikumar Tadiparthi, Pawan Aggarwal, Savithiri Shivakumar
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Publication number: 20040010056Abstract: A colored dispersion comprising a polymer and a dye represented by General Formula (1):Type: ApplicationFiled: June 20, 2003Publication date: January 15, 2004Applicant: KONICA CORPORATIONInventors: Mari Takahashi, Satoru Ikesu, Takatugu Suzuki, Kyoko Iwamoto
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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: 20040006094Abstract: This invention provides novel neuroprotective 4-pyrimidineamine derivatives and neuroprotective pharmaceutical compositions comprising 4-pyrimidinamines. This invention also provides methods of using these compositions to prevent ischemic cell death, particularly neuronal cell death, and reduce the likelihood of neuronal cell death in a subject due to a traumatic event. Finally, this invention provides an apparatus for administering to a subject the instant pharmaceutical compositions.Type: ApplicationFiled: March 25, 2003Publication date: January 8, 2004Inventors: Elfrida R. Grant, Frank K. Brown, Robert Allan Zivin, Michael McMillian, Zhong Zhong, Malcolm Scott, Allen B. Reitz, Tina Morgan Ross
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Publication number: 20040002123Abstract: Methods and compositions are provided for detecting changes in membrane potential in membranes biological systems.Type: ApplicationFiled: December 31, 2002Publication date: January 1, 2004Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Roger Y. Tsien, Jesus E. Gonzalez
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Patent number: 6667330Abstract: Furanone derivatives and the pharmaceutically acceptable salts thereof have cytoprotective activity and protective activity for neuroinflammation, and neurodegenerative disorders; they are useful in the treatment of stroke, cerebral ischemia, myocardial infarction, myocardial ischemia, chronic heart failure, inflammation and other oxidative stress-related conditions, as well as Alzheimer's disease and senile dementia; they are also useful in the manufacture of pharmaceutical formulations for the treatment of such conditions.Type: GrantFiled: January 28, 2003Date of Patent: December 23, 2003Assignee: Galileo Pharmaceuticals, Inc.Inventors: Bing Wang, Wei Zhang, Jiangao Song, Ughetta del Balzo, Lesley Brown, Gail Walkinshaw
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Publication number: 20030232813Abstract: The present invention relates to novel amino substituted pyrimidinone derivatives of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. The present invention more particularly provides novel amino substituted pyrimidinone derivatives of the general formula (I) and a method thereof.Type: ApplicationFiled: April 9, 2003Publication date: December 18, 2003Applicant: ORCHID CHEMICALS & PHARMACEUTICALS LIMITEDInventors: Shiv Kumar Agarwal, Ravikumar Tadiparthi, Pawan Aggarwal, Savithiri Shivakumar
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Patent number: 6664272Abstract: The present invention is directed to curcumin analogs exhibiting anti-tumor and anti-angiogenic properties, pharmaceutical formulations including such compounds and methods of using such compounds.Type: GrantFiled: December 4, 2000Date of Patent: December 16, 2003Assignee: Emory UniversityInventors: James P. Snyder, Matthew C. Davis, Brian Adams, Mamoru Shoji, Dennis C. Liotta, Eva M. Ferstl, Ustun B. Sunay
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Patent number: 6660738Abstract: The present invention relates to pyrrolidine derivatives useful as inhibitors of metalloproteases, e.g. zinc proteases, and which are effective in treating disease states associated with vasoconstriction.Type: GrantFiled: July 17, 2001Date of Patent: December 9, 2003Assignee: Hoffmann-La Roche Inc.Inventors: Johannes Aebi, Daniel Bur, Alexander Chucholowski, Henrietta Dehmlow
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Publication number: 20030225088Abstract: The invention relates to substituted aromatic polycyclic tertiary-heteroalkylamine 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.Type: ApplicationFiled: September 26, 2002Publication date: December 4, 2003Applicant: G.D. Searle & Co.Inventors: James A. Sikorski, Richard C. Durley, Mark A. Massa, Jane L. Wang, Deborah A. Mischke, Barry L. Parnas, Melvin L. Rueppel
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Publication number: 20030220359Abstract: The invention relates to novel aryl-ethene-sulfonamides and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as endothelin receptor antagonists.Type: ApplicationFiled: January 3, 2003Publication date: November 27, 2003Inventors: Christoph Boss, Martin Bolli, Martine Clozel, Walter Fischli, Thomas Weller
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Patent number: 6653300Abstract: This invention describes novel pyrazole compounds of formula I′: wherein Q′ is —O—, —C(R6′)2—, 1,2-cyclopropanediyl, 1,2-cyclobutanediyl, or 1,3-cyclopropanediyl, and R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T—R3 or L—Z—R3, or Rx and Ry are taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-7 membered ring having 0-3 heteroatoms; and R2 and R2′ are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.Type: GrantFiled: December 19, 2001Date of Patent: November 25, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Jeremy Green, David Kay, Ronald Knegtel, Andrew Miller, Ronald Tomlison, Pan Li
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Publication number: 20030216574Abstract: New bicyclic based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as in the treatment of diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.Type: ApplicationFiled: May 28, 2003Publication date: November 20, 2003Inventors: John M. Nuss, Savithri Ramurthy
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Publication number: 20030216404Abstract: The invention encompasses novel compounds which are inhibitors of matrix metalloproteinase, ADAM or ADAM-TS enzymes, and which are useful for the treatment of diseases mediated by those enzymes, including degenerative diseases and certain cancers.Type: ApplicationFiled: June 12, 2003Publication date: November 20, 2003Inventors: Duncan Robert Hannah, Hazel Joan Dyke, Andrew Sharpe, Andrew Douglas Baxter
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Publication number: 20030216382Abstract: The present invention provides compounds of formula (I) 1Type: ApplicationFiled: February 10, 2003Publication date: November 20, 2003Inventors: Markus Boehringer, Bernd Michael Loeffler, Jens-Uwe Peters, Matthias Steger, Peter Weiss
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Patent number: 6649760Abstract: Phenyluracils of the general formula (I) in which Q, R1, R2, R3, R4, R5 and R6 each have one of the meanings given in the description, and processes for their preparation and their use as herbicides.Type: GrantFiled: February 20, 2002Date of Patent: November 18, 2003Assignee: Bayer AktiengesellschaftInventors: Roland Andree, Hans-Georg Schwarz, Karl-Heinz Linker, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen
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Publication number: 20030212079Abstract: This invention provides novel neuroprotective 4-pyrimidineamine derivatives and neuroprotective pharmaceutical compositions comprising 4-pyrimidinamines. This invention also provides methods of using these compositions to prevent ischemic cell death, particularly neuronal cell death, and reduce the likelihood of neuronal cell death in a subject due to a traumatic event. Finally, this invention provides an apparatus for administering to a subject the instant pharmaceutical compositions.Type: ApplicationFiled: March 25, 2003Publication date: November 13, 2003Inventors: Elfrida R. Grant, Frank K. Brown, Robert Allan Zivin, Michael McMillian, Zhong Zhong, Malcolm Scott, Allen B. Reitz, Tina Morgan Ross
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Publication number: 20030207248Abstract: Methods and compositions are provided for detecting changes in membrane potential in membranes biological systems.Type: ApplicationFiled: December 31, 2002Publication date: November 6, 2003Inventors: Roger Y. Tsien, Jesus E. Gonzalez
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Publication number: 20030199526Abstract: The present invention provides a compound of formula (I): 1Type: ApplicationFiled: December 9, 2002Publication date: October 23, 2003Inventors: Deborah Choquette, Robert J. Davies, Marion W. Wannamaker
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Patent number: RE38330Abstract: The present invention relates to compositions and methods for inhibiting and reversing nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises a thiazolium compound capable of inhibiting, and to some extent reversing, the formation of advanced glycosylation endproducts of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated. A novel immunoassay for detection of the reversal of the nonenzymatic crosslinking is also disclosed.Type: GrantFiled: August 12, 1999Date of Patent: November 25, 2003Assignee: Alteon Inc.Inventors: Anthony Cerami, Peter C. Ulrich, Dilip R. Wagle, San-Bao Hwang, Sara Vasan, John J. Egan