Patents Examined by Robert Gerstl
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Patent number: 6667412Abstract: The present invention provides a novel nitrile compound useful as an intermediate for the production of, for example, N,N-substituted cyclic amine derivatives or phenylacetonitrile derivatives that are useful as a medicine. Specifically it provides a nitrile carboxylic acid compound, nitrile ester compound and nitrile alcohol compound. That is, it provides a nitrile compound represented by the following formula (I): wherein R1 and R2 means substituents; m means 0 or an integer of from 1 to 6; n means 0 or an integer of from 1 to 5; and R3 means carboxyl group, a lower alkoxycarbonyl group or hydroxymethyl group.Type: GrantFiled: August 27, 2001Date of Patent: December 23, 2003Assignee: Eisai Co., Ltd.Inventors: Yuichi Suzuki, Noboru Yamamoto, Koki Kawano, Teiji Kimura, Koichi Ito, Satoshi Nagato, Yoshihiko Norimine, Yoichi Iimura
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Patent number: 6664281Abstract: A peroxisome proliferator activated receptor regulator containing a carboxylic acid derivative of formula (I) (wherein all symbols are as defined in the specification), a non-toxic acid thereof or a hydrate thereof as active ingredient. Because of having an effect of regulating PPAR, a compound of formula (I) is useful as a hypoglycemic agent, a hypolipidemic agent, a preventive and/or a remedy for diseases associating metabolic disorders (diabetes, obesity, syndrome X, hypercholesterolemia, hyperlipoproteinemia, etc.), hyperlipemia, atherosclerosis, hypertension, circulatory diseases, overeating, coronary heart diseases, etc., an HDL cholesterol-elevating agent, an LDL cholesterol and/or VLDL cholesterol-lowering agent and a drug for relief from risk factors of diabetes or syndrome X.Type: GrantFiled: February 26, 2001Date of Patent: December 16, 2003Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Hisao Tajima, Yoshisuke Nakayama, Daikichi Fukushima
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Patent number: 6660758Abstract: Epothilone A, epothilone B, analogs of epothilone and libraries of epothilone analogs are synthesized. Epothilone A and B are known anticancers agents that derive their anticancer activity by the prevention of mitosis through the induction and stabilization of microtubule assembly. The analogs of epothilone are novel. Several of the analogs are demonstrated to have a superior cytotoxic activity as compared to epothilone A or epothilone B as demonstrated by their enhanced ability to induce the polymerization and stabilization of microtubules.Type: GrantFiled: September 24, 1999Date of Patent: December 9, 2003Assignee: The Scripps Research InstituteInventors: Kyriacos C. Nicolaou, Yun He, Sacha Ninkovic, Joaquin Pastor, Frank Roschangar, Francisco Sarabia, Hans Vallberg, Dionisios Vourloumis, Nicolas Winssinger, Zhen Yang, Nigel Paul King, M. Ray Finlay
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Patent number: 6660760Abstract: Heterocyclic aromatic compounds are provided which are useful in stimulating endogenous production or release of growth hormone and in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength. The heterocyclic aromatic compounds have the structure including pharmaceutically acceptable salts thereof and all stereoisomers thereof, wherein Xa is heteroaryl, preferably, and R1, R1a, R6, Y, Xb, A, B, Z, R3, R4, R4a, R5 and R5a are as defined herein.Type: GrantFiled: October 28, 2002Date of Patent: December 9, 2003Assignee: Bristol-Myers Squibb Co.Inventors: Jeffrey A. Robl, Joseph A. Tino, Andres S. Hernandez, Jun Li
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Patent number: 6657083Abstract: Disclosed is a 2-amino-5-acylamino-4-substituted-phenol compound having the structural formula I: wherein Y is a substituent group, and R′ is a ballast group. Also disclosed is a simplified method for preparing a photographic coupler using this compound.Type: GrantFiled: December 3, 2001Date of Patent: December 2, 2003Assignee: Eastman Kodak CompanyInventor: Chang-Kyu Kim
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Patent number: 6642266Abstract: This invention is directed to methods of treating conditions which present with low bone mass, particularly osteoporosis, frailty, an osteoporotic fracture, a bone defect, childhood idiopathic bone loss, alveolar bone loss, mandibular bone loss, bone fracture, osteotomy, bone loss associated with periodontitis, or prosthetic ingrowth comprising administering prostaglandin agonists which are EP4 receptor selective prostaglandin agonists. This invention is especially directed to those methods wherein the EP4 receptor selective agonist is a compound of Formula I: wherein the variables are as defined in the specification.Type: GrantFiled: November 16, 2001Date of Patent: November 4, 2003Assignee: Pfizer Inc.Inventors: Kimberly O. Cameron, HuaZhu Ke, Bruce A. Lefker, David D. Thompson
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Patent number: 6642391Abstract: A compound named Amycomycin of the formula: is described, as well as its pharmaceutically acceptable salts and derivatives, in all their stereoisomeric and tautomeric forms. The compound is obtained by growing the microorganism Amycolatopsis species ST101170 (DSM 12216) and is useful as a pharmaceutical, particularly as an antibiotic.Type: GrantFiled: December 7, 2000Date of Patent: November 4, 2003Assignee: Aventis Pharma Deutschland GmbHInventors: Cordula Hopmann, Michael Kurz, Heinrich Decker, Dominique Le Beller, Jozsef Aszodi
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Patent number: 6639074Abstract: The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-azacycloalkanoylaminothiazole compounds of formula I or a pharmaceutically acceptable salt thereof, wherein: R is alkyl, aryl or heteroaryl; R1, R2, R3, R4 and R5 are each independently hydrogen, alkyl, aryl or heteroaryl; R6 and R7 are each independently hydrogen, alkyl, aryl, heteroaryl, halogen, hydroxy or alkoxy; R8 is hydrogen, alkyl, aryl, heteroaryl, CONR9R10, COR11 or COOR12; R9, R10, R11 and R12 are each independently hydrogen, alkyl or aryl; m equals 0 to 5; and n equals 0 to 5, which are novel, potent inhibitors of cyclin dependent kinases (cdks). The present invention further concerns new key intermediate compounds, a quaternary ammonium salt of formula III′ and a 2-oxazolylalkyl derivative of formula IX.Type: GrantFiled: March 18, 2002Date of Patent: October 28, 2003Assignee: Bristol Myers Squibb CompanyInventors: Bang-Chi Chen, Kyoung S. Kim, S. David Kimball, Raj N. Misra, Mark E. Salvati, Joseph E. Sundeen, Hai-Yun Xiao, Rulin Zhao
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Patent number: 6635621Abstract: This invention relates to derivatives of alpha-amino acid amides, to pharmaceutical compositions containing such compounds, and to their use in medicine as inhibitors of cysteine proteases, particularly the cathepsins. A compound of formula (I) is described or a pharmaceutically acceptable salt, hydrate or solvate thereof. Pharmaceutically acceptable salts of the compounds of this invention include the sodium, potassium, magnesium, calcium, hydrogen chloride, tartaric acid, succinic acid, fumaric acid and p-toluenesulfonic acid salts.Type: GrantFiled: January 30, 2002Date of Patent: October 21, 2003Assignee: Naeja Pharmaceutical Inc.Inventors: Rajeshwar Singh, Nian Zhou, Andhe V. N. Reddy, George Thomas, Qizhu Ding, Jadwiga Kaleta, Ronald George Micetich, Mark Whittaker
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Patent number: 6632831Abstract: The invention relates to BCAT inhibitors and the use thereof for treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the overstimulation of the excitatory amino acids, treating anxiety, psychosis, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headache, chronic pain, neuropathic pain, Parkinson's disease, diabetic retinopathy, glaucoma, CMV retinitis, urinary incontinence, opioid tolerance or withdrawal, and inducing anesthesia, as well as for enhancing cognition.Type: GrantFiled: November 26, 2002Date of Patent: October 14, 2003Assignee: Pfizer Inc.Inventors: Sheryl Jeanne Hays, Lain-Yen Hu, Huangshu Lei, Jeffrey David Scholten, David Juergen Wustrow
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Patent number: 6630506Abstract: Acyl guanidines are provided which are sodium/proton exchange (NHE) inhibitors which have the structure wherein n is 0 to 4; X is a bond, O, S, SO, SO2, CO, or NR7; Y is a bond, O, S, SO, SO2, CO, or NR7′ wherein at least one of X and Y is other than a bond; and R1, R2, R3, R4, R5, R6, R7 and Ra, Rb, Rc, Rd are as defined herein, and are useful as antianginal, cardioprotective agents, antiischemic agents, and agents for peripheral vascular disease including intermittent claudication. In addition, a method is provided for preventing or treating angina pectoris, cardiac dysfunction, myocardial necrosis, arrhythmia, peripheral vascular diseases (PVD), including peripheral atherosclerotic disease (PAD), including intermittent claudication, Raynaud's diseases, and LeRiches Syndrome, pain, parethesia or discomfort in the lower limb and gluteal regions produced by vascular (e.g.Type: GrantFiled: April 21, 2000Date of Patent: October 7, 2003Assignee: Bristol-Myers Squibb Co.Inventors: Sundeep Dugar, Steven V. O'Neil
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Patent number: 6630485Abstract: The present invention relates to compounds of Formula (I) that are p-38 MAP kinase inhibitors, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.Type: GrantFiled: April 19, 2001Date of Patent: October 7, 2003Assignee: Syntex (U.S.A.) LLCInventors: Soan Cheng, David Michael Goldstein, Teresa Alejandra Trejo Martin, Eric Brian Sjogren
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Patent number: 6624310Abstract: The invention relates to compounds which are obtained by fermenting DSM 6773, especially epothilones A1, A2, A8, A9, B10, C1, C2, C3, C4, C5, C6, C7, C8, C9, D1, D2, D5, G1, G2, H1, H2, I1, I2, I3, I4, I5, I6 and K and trans-epothilones C1 and C2.Type: GrantFiled: March 21, 2001Date of Patent: September 23, 2003Assignee: Gesellschaft fuer Biotechnologische Forschung, mbH (GBF)Inventors: Gerhard Hoefle, Hans Reichenbach, Klaus Gerth, Ingo Hardt, Florenz Sasse, Heinrich Steinmetz
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Patent number: 6624314Abstract: A pyrrolesulfonamide derivative having the following formula (I): wherein the ring P represented by is a pyrrole ring having the following structure: wherein R represents alkyl, cycloalkyl, cycloalkylalkyl or aralkyl; the dashed line indicates the presence or absence of a bond; l stands for 0 or 1; A represents alkylene, alkenylene or alkynylene; and Y represents a group in which W represents CH, C═ or N; m stands for 0 or 1 when W is CH or N, or m stands for 1 when W is C═; B represents a specific divalent group; E1 and E2 each independently represents H or lower alkyl; and D represents an aromatic hydrocarbon group or heterocyclic group. The compound (I) has strong serotonin-2 receptor antagonistic action and low toxicity and less side effects, and is useful as a therapeutic for circulatory diseases such as ischemic heart diseases, cerebrovascular disturbances and peripheral circulatory disturbances.Type: GrantFiled: June 4, 2001Date of Patent: September 23, 2003Assignee: Daiichi Suntory Pharma Co., Ltd.Inventors: Akira Mizuno, Makoto Shibata, Tomoe Kamei, Harukazu Fukami, Norio Inomata
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Patent number: 6620831Abstract: The present invention relates to an indazole derivative, pharmaceutically acceptable salt, solvated product and isomer thereof substituted with 1,1-dioxoisothiazolidine which are useful as inhibitors for Cyclin Dependent Kinase(CDK). The present invention also relates to an agent for inhibiting and treating diseases involving cell proliferation, e.g., cancer, inflammation, restenosis, angiogenesis, etc. which comprises the compound of formula (1) as an active ingredient together with a pharmaceutically acceptable carrier.Type: GrantFiled: November 4, 2002Date of Patent: September 16, 2003Assignee: LG Life Sciences Ltd.Inventors: Jin-Ho Lee, Chang-Yong Hong, Tae-Sik Park, Jong-Hyun Kim, Sei-Hyun Choi, Sook-Kyung Yoon, Hyun-Ho Chung, Shin-Wu Jeong, Kwang-Yeon Hwang, Dong-Kyu Shin
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Patent number: 6620830Abstract: The invention provides thiazolidinedione, oxadiazolidinedione, and triazolone compounds of Formula (I) which compounds are thyroid receptor ligands. The invention further provides pharmaceutical compositions and kits comprising such compounds and methods of treating obesity, overweight condition, hyperlipidemia, glaucoma, cardiac arrhythmias, skin disorders, thyroid disease, hypothyroidism, thyroid cancer, diabetes, atherosclerosis, hypertension, coronary heart disease, congestive heart failure, hypercholesterolemia, depression, and osteoporosis using such compounds.Type: GrantFiled: April 17, 2001Date of Patent: September 16, 2003Assignee: Pfizer, Inc.Inventor: Yuan-Ching P. Chiang
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Patent number: 6620828Abstract: Diaminothiazole compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction in order to modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.Type: GrantFiled: February 15, 2001Date of Patent: September 16, 2003Assignee: Agouron Pharmaceuticals, Inc.Inventors: Shao Song Chu, Larry Andrew Alegria, Steven Lee Bender, Suzanne Pritchett Benedict, Allen J. Borchardt, Robert Steve Kania, Mitchell David Nambu, Anna Maria Tempczyk-Russell, Sepehr Sarshar, Dilip Bhumralkar, Zhengwei Peng, Michelle Yang
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Patent number: 6617341Abstract: A novel 2-iminothiazole derivatives and the use as an insecticide and acaricide of the compounds of formula (1): wherein R1 is CN or fluoroalkyl (especially C1-C4 fluoroalkyl), R2 is H, halogen or CN, R3 is aryl, phenylalkyl, alkyl, cycloalkyl groups; being optionally substituted by one or more substituents, alkylthiocarbamoyl, or aroyl; being optionally substituted by one or more substituents, R4 is aryl; being optionally substituted by one or more substituents, X is O, SOn, n is 0, 1 or 2 or X is N(R5) wherein, R3 and R5 are, independently, H or alkyl, alkoxy, acyl, alkylamino, aryl groups; being optionally substituted by one or more substituents or arylamino, being optionally substituted by one or more substituents or R3 and R5 may additionally be fused to a heteroaromatic ring.Type: GrantFiled: December 30, 2002Date of Patent: September 9, 2003Assignee: Nippon Soda Co. Ltd.Inventors: Isao Iwataki, Asiye Meric, Elizabeth Laura Moyano, Renpei Hatano
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Patent number: 6613932Abstract: A prostaglandin derivative represented by the formula: [wherein X is CH2, O or S(O)q1, Y is an ethylene group, a vinylene group, an ethynylene group, O(CH2)t1 or S(O)q2(CH2)t1, Z is an ethylene group, a vinylene group or an ethynylene group, R1 is a hydrogen atom, a C1-10 alkyl group or a C3-10 cycloalkyl group, R2 is a C1-10 alkyl group, a C2-10 alkenyl group, a C2-10 alkynyl group, a C3-10 cycloalkyl group, a C1-5 alkyl-C3-10 cycloalkyl group, a C3-10 cycloalkyl-C1-5 alkyl group, a hydroxy-C1-5 alkyl group, a halogeno-C1-5 alkyl group, a C1-5 alkoxy-C1-5 alkyl group, a C2-4 alkoxycarbonyl-C1-5 alkyl group, a carboxyl-C1-5 alkyl group, a cyano-C1-5 alkyl group, a C1-5 alkyl group substituted with a group represented by the formula: —NR7R8, an acyl group, a group represented by the formula: —(CH2)t2CH(NH2)COOR9, etc., and R3 is a hydrogen atom, a C1-10 alkyl group, etc.], a pharmaceutically acceptable salt thereof or a hydrate thereof.Type: GrantFiled: March 11, 2002Date of Patent: September 2, 2003Assignees: Taisho Pharmaceutical Co., Ltd., Fumie SatoInventors: Fumie Sato, Tohru Tanami, Hideo Tanaka, Naoya Ono, Makoto Yagi, Hitomi Hirano
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Patent number: 6613943Abstract: Disclosed is a 4-acylamino-2-hydroxy-5-substituted-acylanilide compound having the structural formula I: wherein R is hydrogen or an alkyl group, Y is a group linked to the rest of the compound by a —O—, —S—, or —N— atom; and R′ is a substituent group. Also disclosed is a method of using the compound in making a cyan dye-forming photographic coupler.Type: GrantFiled: December 3, 2001Date of Patent: September 2, 2003Assignee: Eastman Kodak CompanyInventor: Chang-Kyu Kim