The -c(=x)- Group Is Bonded Directly To The Nitrogen Patents (Class 548/195)
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Patent number: 7105671Abstract: 2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 2-position being a substituted phenyl group and at the 3-position being a polar ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.Type: GrantFiled: April 23, 2003Date of Patent: September 12, 2006Assignee: Hoffmann-la Roche Inc.Inventors: Wendy Lea Corbett, Joseph Samuel Grimsby, Nancy-Ellen Haynes, Robert Francis Kester, Paige Erin Mahaney, Jagdish Kumar Racha, Ramakanth Sarabu, Ka Wang
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Patent number: 7105564Abstract: The present invention provides novel compounds having a dual antagonistic activity against thromboxane A2 receptor and prostaglandin D2 receptor and pharmaceutical compositions comprising them. A compound of the formula (I): wherein R1 is —CH2—CH?CH—CH2—CH2—CH2—COOR2 or —CH?CH—CH2—CH2—CH2—COOR2; R2 is hydrogen or alkyl; m is 0 or 1; p is 0 or 1; X1 and X3 each is independently optionally substituted aryl or optionally substituted heteroaryl; X2 is a bond, —CH2—, —S—, —SO2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2—, or the like; X4 is —CH2—, —CH2—CH2—, —C(?O)—, or the like, have a dual antagonistic activity against both a thromboxane A2 receptor and a prostaglandin D2 receptor.Type: GrantFiled: March 2, 2000Date of Patent: September 12, 2006Assignee: Shionogi & Co., Ltd.Inventors: Tsunetoshi Honma, Yoshiharu Hiramatsu, Akinori Arimura
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Patent number: 7101878Abstract: Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.Type: GrantFiled: August 20, 1999Date of Patent: September 5, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Mark Brian Anderson, Haresh N. Vazir, David Robert Luthin, Genevieve DeGuzman Paderes, Ved P. Pathak, Lance Christopher Christie, Yufeng Hong, Eileen Valenzuela Tompkins, Haitao Li, James Faust
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Patent number: 7067516Abstract: Compounds of formula (I) where R5, R6a, each X, L, Cy and Lp are as defined in the specification, are tryptase inhibitors useful as antiinflammatory agents.Type: GrantFiled: December 12, 2001Date of Patent: June 27, 2006Assignee: Tularik LimitedInventors: Sarah Elizabeth Lively, Martin James Harrison, Neil Jason Naylor, Christopher Neil Farthing, Bohdan Waszkowycz
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Patent number: 7037929Abstract: Compounds which are 2-amino-1,3-thiazole derivatives of formula (I) wherein R is a halogen atom, a nitro group, an optionally substituted amino group or it is a group, optionally further substituted, selected from i) straight or branched C1–C8 alkyl, C2–C6 alkenyl or C2–C6 alkynyl; ii) C3–C6 cycloalkyl; iii) aryl or arylalkyl with from 1 to 8 carbon atoms within the straight or branched alkyl chain; R1 is an optionally further substituted group selected from: i) straight or branched C1–C8 alkyl or C2–C6 alkenyl; ii) 3 to 6 membered carbocycle or 5 to 7 membered heterocycle ring; iii) aryl or arylcarbonyl; iv) arylalkyl with from 1 to 8 carbon atoms within the straight or branched alkyl chain; v) arylalkenyl with from 2 to 6 carbon atoms within the straight or branched alkenyl chain; vi) an optionally protected amino acid residue; or a pharmaceutically acceptable salt thereof; are useful for treating cell proliferative disorders associated with an altered cell dependent kinase activity.Type: GrantFiled: October 27, 1999Date of Patent: May 2, 2006Assignee: Pharmacia & Upjohn S.p.A.Inventors: Paolo Pevarello, Raffaella Amici, Gabriella Traquandi, Manuela Villa, Anna Vulpetti, Antonella Isacchi
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Patent number: 6995181Abstract: Novel non-steroidal compounds are provided which are glucocorticoid receptor modulators which are useful in treating diseases requiring glucocorticoid receptor agonist or antagonist therapy such as obesity, diabetes, inflammatory and immune disorders, and have the structure where Z is CONR1R2 or CH2NR1R2 and where R, Ra, Rb, Rc, Rd, Z, A and B are defined herein.Type: GrantFiled: July 17, 2003Date of Patent: February 7, 2006Assignee: Bristol-Myers Squibb Co.Inventors: Wayne Vaccaro, Bingwei Vera Yang, Soong-Hoon Kim, Tram Huynh, David R. Tortolani, Kenneth J. Leavitt, Wenying Li, Arthur M. Doweyko, Xiao-Tao Chen, Lidia Doweyko
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Patent number: 6987122Abstract: 2-(1H-Indol-3-yl)-2-oxo-acetamide derivatives of formula (I) having antitumor activity in particular against solid tumors, specifically colon and lung tumors.Type: GrantFiled: July 12, 2001Date of Patent: January 17, 2006Assignee: Novuspharma S.p.A.Inventors: Ernesto Menta, Nicoletta Pescalli
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Patent number: 6979694Abstract: Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.Type: GrantFiled: March 3, 2003Date of Patent: December 27, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Jagabandhu Das, Ramesh Padmanabha, Ping Chen, Derek J. Norris, Arthur M. P. Doweyko, Joel C. Barrish, John Wityak
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Patent number: 6960664Abstract: Disclosed are compounds of formula: and pharmaceutically acceptable salts and esters thereof, useful in treating and/or preventing Alzheimer's disease and other similar diseases, wherein RN, RC, R1, R2 and R20 are defined herein. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.Type: GrantFiled: May 22, 2002Date of Patent: November 1, 2005Assignee: Pharmacia & UpJohn CompanyInventors: Heinrich Schostarez, Robert Alan Chrusciel, Rebecca S. Centko
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Patent number: 6951945Abstract: 2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 3-position being a substituted phenyl group and at the 2-position being a methyl cycloalkyl ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.Type: GrantFiled: July 9, 2003Date of Patent: October 4, 2005Assignee: Hoffman-La Roche Inc.Inventors: Fred Thomas Bizzarro, Wendy Lea Corbett, Joseph Francis Grippo, Nancy-Ellen Haynes, George William Holland, Robert Francis Kester, Paige Erin Mahaney, Ramakanth Sarabu
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Patent number: 6949654Abstract: The present invention provides novel N-alkyl-N-phenylhydroxylamine derivatives containing metal chelating groups, a process for preparing the same, the use of the novel compounds as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen species (ROS) and/or excess Zn ions, in particular stroke, Parkinson's disease and Alzheimer's disease. The compounds of the invention possess similar or superior LPO inhibition activity to the reference compounds of Trolox and Ebselen. While showing lower toxicity, they also effectively inhibit the cerebral neuronal cell death caused by ROS and/or zinc ion, and show neuroprotective effects against ischemic neuronal degeneration.Type: GrantFiled: June 5, 2003Date of Patent: September 27, 2005Assignee: Sam-Sung Electronics Co., Ltd.Inventors: Eu-Gene Oh, Sung-Bo Ko, Won-Yeob Kim, Kyung-Hwa Kim, Dennis W. Choi, Laura L. Dugan, Tae-Cheon Kang, Jae-Young Koh, Kyung-Mi Kim, In-Jae Shin
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Patent number: 6936629Abstract: The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating flaviviridae viral infection.Type: GrantFiled: December 20, 2002Date of Patent: August 30, 2005Assignee: ViroChem Pharma Inc.Inventors: Laval Chan Chun Kong, Oswy Z. Pereira, Nghe Nguyen-Ba, Thumkunta Jagadeeswar Reddy, Sanjoy Kumar Das, Mohammad Arshad Siddiqui
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Patent number: 6927290Abstract: There is disclosed an advantageous mixed acid anhydride production method of formula (1): R1C(O)OY(O)n(R2)p??(1) wherein R1, R2 and Y denote the same as defined below, n and p denote an integer of 1 or 2, which is characterized by adding a carboxylic acid of formula (2); R1COOH??(2) wherein R1 denotes a hydrogen atom, an optionally substituted alkyl group or the like, an organic base to a solution of a carboxylic acid activating agent of formula (3); (R2)pY(O)nX??(3) wherein R2 denotes an optionally substituted aliphatic hydrocarbyl group or the like, Y denotes a carbon atom, a phosphorus atom, or a sulfur atom, and X denotes a chlorine atom or the like.Type: GrantFiled: May 10, 2004Date of Patent: August 9, 2005Assignee: Sumitomo Chemical Company, LimitedInventors: Takashi Miki, Hideki Ushio, Isao Kurimoto
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Patent number: 6919361Abstract: A 5-membered cyclic compound of the formula: wherein X is oxygen or sulfur, R1 is hydrogen, substituted or unsubstituted alkyl, etc., R2 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, etc., Y1 is a direct bond, substituted or unsubstituted alkylene, —CO(CH2)n—, etc., the wavy line means (E)-configuration or (Z)-configuration, R3 is substituted or unsubstituted aryl, etc., Y2 is substituted or unsubstituted alkylene, etc., R4 is hydrogen, substituted or unsubstituted alkanoyl, substituted or unsubstituted alkyl, etc., R5 is hydrogen, etc., or a salt thereof, these compound being able to inhibit infiltration of leukocytes such as eosinophils and lymphocytes, by which being useful for the treatment of various kinds of inflammation.Type: GrantFiled: June 28, 2001Date of Patent: July 19, 2005Assignee: Sumitomo Pharmaceuticals Company, LimitedInventors: Norio Fujiwara, Hitoshi Fujita, Fujio Antoku, Toshinari Sugasawa, Hajime Kawakami
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Patent number: 6908934Abstract: Compounds of Formula I and the pharmaceutically acceptable salts and esters thereof, wherein Z is selected from the group consisting of: (a) Formula Ia ?and (b) Formula Ib are novel LXR agonists and are useful in the treatment of dyslipidemic conditions particularly depressed levels of HDL cholesterol.Type: GrantFiled: May 30, 2002Date of Patent: June 21, 2005Assignee: Merck & Co., Inc.Inventors: Alan D. Adams, Aileen Bouffard, James F. Dropinski, Clare E. Gutteridge, A. Brian Jones, Weiguo Lui, John George Ondeyka, Ali Shiafee, Sheo Bux Singh
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Patent number: 6903104Abstract: The invention is based on the discovery that certain 3-oxoacetamideindolyl compounds have potent anticancer and anti-angiogenic activity. The 3-oxoacetamideindolyl compounds are of the following formula. In this formula, each R1 is independently isoxazolyl, thiazolyl, isothiazolyl, 1,3,4-thiadiazolyl, 1,3-benzothiazolyl, quinolyl, isoquinolyl, thionaphthenyl, or benzofuranyl, each being optionally substituted with 1-6 independent R5; or when taken together with R2 and the nitrogen atom to which they are attached form a 5-8 membered ring comprising C, N, S, or O atoms wherein any atom is optionally substituted with an independent R5. Each R2 is independently H, C1-C10 alkyl, or aryl, each being optionally substituted with 1-4 independent R5; or when taken together with R1 and the nitrogen atom to which they are attached form a 5-8 membered ring comprising C, N, S, or O atoms wherein any atom is optionally substituted with an independent R5.Type: GrantFiled: December 5, 2002Date of Patent: June 7, 2005Assignee: National Health Research InstitutesInventors: Chiung-Tong Chen, Shu-Jen Chen, Ming-Chu Hsu, Der-Ren Hwang, Wen-Tai Li, Chu-Chung Lin
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Patent number: 6852752Abstract: Novel hydroxamic acid compounds are disclosed. These hydroxamates inhibit peptide deformylase (PDF), an enzyme present in prokaryotes and are therefore useful as antimicrobials and antibiotics. Methods of synthesis and of use of the compounds are also disclosed.Type: GrantFiled: December 13, 2000Date of Patent: February 8, 2005Assignee: Vicuron Pharmaceuticals Inc.Inventors: Jeffrey W. Jacobs, Dinesh Patel, Jason Lewis, Zhi-Jie Ni
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Patent number: 6794392Abstract: The novel benzamide derivative represented by formula (1) and the novel anilide derivative represented by formula (13) of this invention has differentiation-inducing effect, and are, therefore, useful a therapeutic or improving agent for malignant tumors, autoimmune diseases, dermatologic diseases and parasitism. In particular, they are highly effective as an anticancer drug, specifically to a hematologic malignancy and a solid carcinoma.Type: GrantFiled: October 13, 1999Date of Patent: September 21, 2004Assignee: Schering AktiengesellschaftInventors: Tsuneji Suzuki, Tomoyuki Ando, Katsutoshi Tsuchiya, Osamu Nakanishi, Akiko Saito, Takashi Yamashita, Yoshinori Shiraishi, Eishi Tanaka
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Patent number: 6787649Abstract: A process which comprises (i) acylating a compound of formula II with a compound of formula IV to obtain a compound of formula I and (ii) deformylating said compound of formula I to obtain a compound of formula IIIType: GrantFiled: February 12, 2003Date of Patent: September 7, 2004Assignee: Sandoz GmbHInventors: Peter Kremminger, Johannes Ludescher, Siegfried Wolf
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Patent number: 6784298Abstract: Hydantoin compounds which are active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes.Type: GrantFiled: June 4, 2003Date of Patent: August 31, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Robert Alan Goodnow, Jr., Kang Le
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Patent number: 6784198Abstract: 2-amino-1,3-thiazole derivatives represented by formula (I) or (II): where R, R1, R2 and R3 are defined herein, or pharmaceutically acceptable salts thereof are useful as, for example, the treatment of cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases or neurodegenerative diseases.Type: GrantFiled: July 18, 2002Date of Patent: August 31, 2004Assignee: Pharmacia Italia S.p.A.Inventors: Paolo Pevarello, Raffaella Amici, Manuela Villa, Barbara Salom, Anna Vulpetti, Mario Varasi
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Patent number: 6780995Abstract: A series of activated iodo-benzamide derivatives are described as antineoplastic and antiviral drug compounds. The compounds generally possess a chelating group, a thiol trapping group and an activating group. The presumptive mechanism of action in preventing cancer cell and virus replication is through inhibition of the binding of transcription factors to zinc finger binding domains. The compounds are effective in inhibiting growth of a variety of human and animal tumor and leukemia cell lines at low concentrations.Type: GrantFiled: November 25, 2002Date of Patent: August 24, 2004Assignee: Isotechnika Inc.Inventors: Randall W. Yatscoff, Robert T. Foster, Selvaraj Naicker
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Patent number: 6743811Abstract: Oxazolidinones and methods for their synthesis are provided. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. Oxazolidinones as disclosed herein can be readily synthesized and used in a variety of applications including use as antimicrobial agents. In one embodiment, a variety of thioamidomethyloxazolidinones and methods for their synthesis and use are provided.Type: GrantFiled: June 27, 2002Date of Patent: June 1, 2004Assignee: Pharmacia & Upjohn CompanyInventors: Mikhail F. Gordeev, Gary W. Luehr, Dinesh V. Patel, Robert C. Gadwood
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Patent number: 6737382Abstract: Insecticidal aminothiazole derivatives and the use as an insecticide and acaricide of the compounds of formula (1): wherein R1 is cyano or fluoroalkyl, R2 is halogen, SCN or aryl, R3 is H, C1-C6 alkyl, SO2R5 or C(O)R6, R4 and R6 are, independently, aryl, phenylalkyl, alkyl, cycloalkyl groups, being optionally substituted by one or more of halogen, cyano, alkyl, alkenyl, alkynyl, haloalkyl, alkoxy, nitro, alkoxycarbonyl, alkylcarbonyloxy, alkylenedioxy, alkylcarbonyl, amino, alkylamino, haloalkoxy, alkylthio, alkylsulfonyl, haloalkenyl, alkoxycarbonylalkyl or alkoxycarbonylalkoxy; said aryl, phenylalkyl groups may additionally be fused to a cycloalkyl ring, R5 is C1-C6 alkyl, haloalkyl, X is O, S, NR7, R7 is alkyl, cycloalkyl, alkoxy, alkenylalkyloxy, alkynylalkyloxy, alkoxycarbonylalkyloxy.Type: GrantFiled: October 23, 2002Date of Patent: May 18, 2004Assignee: Nippon Soda Co. Ltd.Inventors: Isao Iwataki, Takao Iwasa, Renpei Hatano, Elizabeth Laura Moyano
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Patent number: 6727269Abstract: The invention concerns novel 2-arylimino-2,3-dihydrothiazole derivatives of general formula (I), their preparation methods and their use as medicines, in particular for treating pathological conditions or diseases wherein one (or several) somatostatin receptors is/are involved. Said pathological conditions include in particular acromegaly, pituitary adenoma or endocrine gastroenteropanceatic tumors including the carcinoid syndrome, and gastrointestinal bleeding.Type: GrantFiled: January 15, 2002Date of Patent: April 27, 2004Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventors: Christophe Moinet, Carole Sackur, Christophe Thurieau
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Patent number: 6720347Abstract: Compounds of the formula and pharmaceutically acceptable salts thereof, wherein R1 and A are defined herein, are protein kinase inhibitors and are useful in the treatment of proliferative diseases, for example, cancer, inflammation and arthritis. They may also be useful in the treatment of Alzheimer's disease and cardiovascular disease.Type: GrantFiled: March 29, 2002Date of Patent: April 13, 2004Assignee: Bristol-Myers Squibb CompanyInventors: David B. Rawlins, S. David Kimball, Kyoung S. Kim, Raj N. Misra, Kevin R. Webster
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Patent number: 6720427Abstract: The invention provides compounds of formula 1 wherein R1, R3, and R4 are as defined, and their pharmaceutically acceptable salts. Compounds of formula 1 are indicated to have activity inhibiting cdk5, cdk2, and GSK-3. Pharmaceutical compositions and methods comprising compounds of formula 1 for treating diseases and conditions comprising abnormal cell growth, such as cancer, and neurodegenerative diseases and conditions and those affected by dopamine neurotransmission are described.Type: GrantFiled: May 13, 2002Date of Patent: April 13, 2004Assignee: Pfizer Inc.Inventors: Mark A. Sanner, Chris J. Helal, Christopher B. Cooper
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Patent number: 6706735Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: June 26, 2002Date of Patent: March 16, 2004Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Paul S. Watson, Soo S. Ko, George V. DeLucca, John V. Duncia, Joseph B. Santella, III, Dean A. Wacker
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Publication number: 20040006058Abstract: The present invention is directed to novel diaminothiazoles of formula 1Type: ApplicationFiled: May 5, 2003Publication date: January 8, 2004Inventors: Xin-Jie Chu, Qingjie Ding, Nan Jiang, Kyungjin Kim, Allen John Lovey, Warren William McComas, John Guilfoyle Mullin, Jefferson Wright Tilley
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Patent number: 6673368Abstract: Remedies effective for the improvement of colonic motor dysfunction such as irritable bowel syndrome, constipation or intestinal atony without causing side effects on the central nerve system. These colonic motor dysfunction remedies comprise, as active ingredients, aminothiazole derivatives represented by the following formula (I) or a salt or hydrate thereof: wherein R1, R2 and R3 may be the same or different and each independently represent a hydrogen atom or a hydroxyl, lower alkyl, lower alkoxy, amino, nitro or cyano group, R4 and R5 may be the same or different and each independently represent a hydrogen atom or a lower alkyl group, and n stands for an integer of from 2 to 4.Type: GrantFiled: May 14, 2001Date of Patent: January 6, 2004Assignee: Zeria Phamaceutical Co., Ltd.Inventors: Shigeru Ueki, Yuko Hori, Yugo Matsunaga, Masaaki Nagasawa, Hiroyasu Nishioka, Masakazu Murata
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Patent number: 6653330Abstract: A compound of formula (I) or a pharmacologically acceptable prodrug or salt thereof which exhibits excellent antifungal activity: wherein Ar1 represents a phenyl group or the like; Ar2 represents a phenylene group or the like. X represents a sulfur atom or a methylene group. R1 represents a hydrogen atom or a C1-3 alkyl group; R2 represents a hydrogen atom or a C1-3 alkyl group; and R3 represents an optionally substituted C6-10 aryl group or the like. Fungal infections may be prevented and/or treated by administering said compound (I) or said prodrug or salt thereof.Type: GrantFiled: September 27, 2002Date of Patent: November 25, 2003Assignee: Sankyo Company, LimitedInventors: Takuya Uchida, Toshiyuki Konosu
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Publication number: 20030216427Abstract: The present invention is related to substituted amine derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such amine derivatives of formula (I). Said substituted amine derivatives are efficient modulators, in particular inhibitors, of the Bax function and/or activation. The present invention is furthermore related to novel substituted amine derivatives as well as methods of their preparation.Type: ApplicationFiled: December 26, 2002Publication date: November 20, 2003Inventors: Serge Halazy, Matthias Schwarz, Bruno Antonsson, Agnes Bombrun, Jean-Claude Martinou, Dennis Church
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Patent number: 6649643Abstract: Imidazol-4-ylmethanols and their uses for preventing and treating primary tumors, metastasis and recurrence of tumors, various symptoms accompanying tumors, prostatic hypertrophy, virilism, hirsutism, male pattern alopecia, precocious puberty, endometriosis, uterine myoma, mastopathy and polycystic ovary syndrome are disclosed.Type: GrantFiled: April 12, 2002Date of Patent: November 18, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Akihiro Tasaka, Akio Ojida, Tomohiro Kaku, Masami Kusaka, Masuo Yamaoka
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Patent number: 6620963Abstract: Compounds of the formula where the variables have the meaning defined in the specification, which bind specifically or selectively to to RAR&agr; retinoid receptors.Type: GrantFiled: September 19, 2002Date of Patent: September 16, 2003Assignee: Allergan, Inc.Inventors: Tien T. Duong, Richard Beard, Roshantha A. Chandraratna
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Patent number: 6605626Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: September 21, 2001Date of Patent: August 12, 2003Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson Jr., Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
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Patent number: 6583288Abstract: Hydantoin compounds which are active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes.Type: GrantFiled: April 26, 2001Date of Patent: June 24, 2003Assignee: Hoffman-La Roche Inc.Inventors: Robert Alan Goodnow, Jr., Kang Le
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Patent number: 6569874Abstract: The present application describes oxygen and sulfur containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is O or S and D may be C(═NH)NH2, which are useful as inhibitors of factor Xa.Type: GrantFiled: November 17, 2000Date of Patent: May 27, 2003Assignee: Bristol-Myers Squibb CompanyInventors: James Russell Pruitt, John Matthew Fevig, Mimi Lifen Quan, Donald Joseph Phillip Pinto
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Patent number: 6562373Abstract: Remedies effective for the improvement of colonic motor dysfunction such as irritable bowel syndrome, constipation or intestinal atony without causing side effects on the central nerve system. These colonic motor dysfunction remedies comprise, as active ingredients, aminothiazole derivatives represented by the following formula (I) or a salt or hydrate thereof: wherein R1, R2 and R3 may be the same or different and each independently represent a hydrogen atom or a hydroxyl, lower alkyl, lower alkoxy, amino, nitro or cyano group, R4 and R5 may be the same or different and each independently represent a hydrogen atom or a lower alkyl group, and n stands for an integer of from 2 to 4.Type: GrantFiled: May 14, 2001Date of Patent: May 13, 2003Assignee: Zeria Pharmaceutical Co., Ltd.Inventors: Shigeru Ueki, Yuko Hori, Yugo Matsunaga, Masaaki Nagasawa, Hiroyasu Nishioka, Masakazu Murata
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Patent number: 6559168Abstract: This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: where Y is ═C(R1a)— or —[N□(O)k]— where k is 0 or 1; G1 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G1 is not a discontinuous or restricted biaryl moiety as defined under G2; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; —G2 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic; or that is a 7- to 12-membered, fused polycyclic; or that is a 7- to 18-membered discontinuous or restricted biType: GrantFiled: January 31, 2002Date of Patent: May 6, 2003Assignee: Pfizer IncInventors: Anthony Marfat, Michael William McKechney
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Patent number: 6552042Abstract: The present application describes inhibitors of factor Xa of formula I: or pharmaceutically acceptable salt forms thereof, wherein W, W1, W2, and W3 may be N or C and J, Ja, and Jb combine to form a substituted carbocycle or heterocycle.Type: GrantFiled: January 29, 2001Date of Patent: April 22, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Qi Han, Celia Dominguez, Eugene C. Amparo, Jeongsook M. Park, Mimi L. Quan, Karen A. Rossi
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Patent number: 6511988Abstract: A series of activated iodo-benzamide derivatives are described as antineoplastic and antiviral drug compounds. The compounds generally possess a chelating group, a thiol trapping group and an activating group. The presumptive mechanism of action in preventing cancer cell and virus replication is through inhibition of the binding of transcription factors to zinc finger binding domains. The compounds are effective in inhibiting growth of a variety of human and animal tumor and leukemia cell lines at low concentrations.Type: GrantFiled: August 10, 2001Date of Patent: January 28, 2003Assignee: Isotechnika Inc.Inventors: Randall W. Yatscoff, Robert T. Foster, Selvaraj Naicker
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Patent number: 6489485Abstract: Para-alkyl, aryl, cycloheteroalkyl or heteroaryl [carbonyl or sulfonyl] amino substituted phenyl amides active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes.Type: GrantFiled: May 1, 2001Date of Patent: December 3, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Fred Thomas Bizzarro, Nancy-Ellen Haynes, Ramakanth Sarabu
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Patent number: 6482951Abstract: Isoindolin-1-one-substituted propionamide glucokinase activators which increase insulin secretion in the treatment of type II diabetes.Type: GrantFiled: December 6, 2001Date of Patent: November 19, 2002Assignee: Hoffmann-La Roche Inc.Inventor: Kevin Richard Guertin
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Patent number: 6448286Abstract: The current invention discloses useful pharmaceutical compositions containing amidino derivative useful as nitric oxide synthase inhibitors.Type: GrantFiled: July 28, 1998Date of Patent: September 10, 2002Assignee: G.D. Searle & Co.Inventors: Donald W. Hansen, Jr., Mark G. Currie, E. Ann Hallinan, Kam F. Fok, Timothy J. Hagen, Arija A. Bergmanis, Steven W. Kramer, Len F. Lee, Suzanne Metz, William M. Moore, Karen B. Peterson, Barnett S. Pitzele, Dale P. Spangler, R. Keith Webber, Mihaly V. Toth, Mahima Trivedi, Foe S. Tjoeng
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Patent number: 6441005Abstract: Oxazolidinones and methods for their synthesis are provided. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. Oxazolidinones as disclosed herein can be readily synthesized and used in a variety of applications including use as antimicrobial agents. In one embodiment, a variety of thioamidomethyloxazolidinones and methods for their synthesis and use are provided.Type: GrantFiled: July 26, 2000Date of Patent: August 27, 2002Assignee: Pharmacia & Upjohn CompanyInventors: Mikhail F. Gordeev, Gary W. Luehr, Dinesh V. Patel, Robert C. Gadwood
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Patent number: 6413997Abstract: 3-(Substituted phenyl)-5-(substituted heterocyclyl)-1,2,4-triazole compounds are useful as insecticides and acaricides. New synthetic procedures and intermediates for preparing the compounds, pesticide compositions containing the compounds, and methods of controlling insects and mites using the compounds are also provided.Type: GrantFiled: October 22, 1999Date of Patent: July 2, 2002Assignee: Dow AgroSciences LLCInventors: Francis E. Tisdell, Peter L. Johnson, James T. Pechacek, Robert G. Suhr, Donald H. DeVries, Carl P. Denny, Mary L. Ash
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Patent number: 6410542Abstract: The current invention discloses aminotetrazole derivatives useful as nitric oxide synthase inhibitors.Type: GrantFiled: October 13, 2000Date of Patent: June 25, 2002Assignee: G. D. Searle & Co.Inventors: E. Ann Hallinan, Donald W. Hansen, Jr., Sofya Tsymbalov
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Patent number: 6407124Abstract: Compounds of the formula and pharmaceutically acceptable salts thereof are provided.Type: GrantFiled: June 10, 1999Date of Patent: June 18, 2002Assignee: Bristol-Myers Squibb CompanyInventors: David B. Rawlins, S. David Kimball, Kyoung S. Kim, Raj N. Misra, Kevin R. Webster
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Patent number: 6388088Abstract: Tetrazolyl-phenyl acetamides are active as glucokinase activators, and are able to increase insulin secretion, which makes them useful for treating type II diabetes.Type: GrantFiled: October 11, 2001Date of Patent: May 14, 2002Assignee: Hoffman-La Roche Inc.Inventor: Achyutharao Sidduri
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Patent number: 6388071Abstract: Para-alkynyl phenyl heteroaromatic amides which are active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes.Type: GrantFiled: April 25, 2001Date of Patent: May 14, 2002Assignee: Hoffmann-La Roche Inc.Inventor: Paige Erin Mahaney