Additional Hetero Ring Containing Patents (Class 544/60)
The additional hetero ring is one of the cyclos in a bicyclo ring system (Class 544/61)
  • Microbiocidal n-phenyl-n-[4-(4-pyridyl-2-pyrimidin-2-yl]-amine derivatives
    Publication number: 20040063937
    Abstract: The invention relates to novel N-phenyl-4-(4-pyridyl)-2-pyrimidineamine derivatives of the general formula (1) wherein the sum of (m+p) together is 0, 1, 2 or 3; n and q are independently of each other 0 or 1, and the sum of (m+p+q) together is 1, 2, 3 or 4; R1 is hydrogen, halogen, alkoxy, haloalkyl, haloalkoxy or alkyl; R2 is hydrogen, C1-C6-alkyl, C1-C6-haloalkyl or C1-C6-alkoxy; R2A is hydrogen, C1-C6-alkyl, C3-C4-alkenyl or C3-C4-alkynyl; each of R3, R4, R5 and R6 is, independently of the others, hydrogen, C1-C6-alkyl, C1-C6-haloalkyl, hydroxy-C1-C6-alkyl or C1-C6-alkoxy-C1-C6-alkyl, or the ring members CR3R4 or CR5R6 or CR2R2A are independently of each other a carbonyl group (C═O) or a group C═S; X is C═O, C═S, S═O or O═S=O; Y is O, S, C═O, CH2A, —N(R8)—, —O—N(R8)—, —N(R8)—O— or NH—; R7 is hydrogen, C1-C4-alkyl, C3-C4-alkenyl, C3-C4-alkynyl, —CH2OR8, CH2SR8, —C(O)R8, —C(O)OR8,
    Type: Application
    Filed: June 25, 2003
    Publication date: April 1, 2004
    Inventors: Martin Eberle, Hugo Ziegler, Fredrik Cederbaum, Peter Ackermann, Anita Schnyder
  • Substituted heterocyclic derivatives useful as antidiabetic and antiobesity agents and method
    Publication number: 20040063700
    Abstract: 1
    Type: Application
    Filed: July 8, 2003
    Publication date: April 1, 2004
    Inventors: Peter T.W. Cheng, Sean Chen, Pratik Devasthale, Charles Z. Ding, Timothy F. Herpin, Shung Wu, Hao Zhang, Wei Wang, Xiang-Yang Ye
  • Aliphatic nitrogenous five-membered ring compounds
    Publication number: 20040063935
    Abstract: The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: 1
    Type: Application
    Filed: April 4, 2003
    Publication date: April 1, 2004
    Inventors: Kosuke Yasuda, Hiroshi Morimoto, Saburo Kawanami, Masataka Hikota, Takeshi Matsumoto, Kenji Arakawa
  • Substituted 4-amino-2-aryl-tetrahydroquinazolines, their preparation, their use and pharmaceutical preparations comprising them
    Publication number: 20040063690
    Abstract: The present invention relates to compounds of formula I: 1
    Type: Application
    Filed: October 1, 2003
    Publication date: April 1, 2004
    Applicant: AVENTIS PHARMA DEUTSCHLAND GmBH
    Inventors: Ursula Schindler, Karl Schonafinger, Hartmut Strobel
  • Pyrimidine derivatives and process for preparing the same
    Publication number: 20040063936
    Abstract: A pyrimidine derivative compound of formula (I) or a salt thereof and a method for the preparation thereof.
    Type: Application
    Filed: June 25, 2003
    Publication date: April 1, 2004
    Inventors: Tsuneyuki Sugiura, Toshihide Horiuchi, Toru Miyazaki, Tsutomu Kojima, Shinsuke Hashimoto
  • Compounds useful as reversible inhibitors of cysteine proteases
    Publication number: 20040063679
    Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R1, R2, R3, R4, R5, R6, R8, R9 and X are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds.
    Type: Application
    Filed: September 27, 2002
    Publication date: April 1, 2004
    Applicant: Boehringer Ingelheim Pharmaceuticals Inc.
    Inventors: Younes Bekkali, Denice Mary Spero, Sanxing Sun, David S. Thomson, Yancey D. Ward, Erick R.R. Young, Eugene R. Hickey, Weimin Liu, Usha R. Patel
  • Process for preparing haloalkyl pyrimidines
    Publication number: 20040063938
    Abstract: The invention is a process for producing haloalkyl pyrimidines as intermediates in the production of benzimidazole and/or pyridylimidazole derivatives having high selectivity and/or high affinity to the benzodiazepine site of GABAA receptors.
    Type: Application
    Filed: June 10, 2003
    Publication date: April 1, 2004
    Applicant: Pfizer Inc
    Inventors: Stephane Caron, Nga M. Do, Ruth E. McDermott, Robert A. Singer
  • Thiazine or pyrazine derivatives
    Patent number: 6713472
    Abstract: A compound which is a chymase inhibitor and which is represented by a formula [I] and salts thereof. In the formula [I], X is R6—(A2)n—N, R1 and R2 are H, alkyl, cycloalkyl or aryl, R3 and R4 are H, alkyl, cycloalkyl, aryl or aromatic heterocycle, R5 is H, alkyl, cycloalkyl, aryl or —A3—A4—R7, R6 is H, alkyl, cycloalkyl, OH, alkoxy, aryl, aryloxy or an aromatic heterocycle, R7 is H, alkyl, OH, alkoxy, aryl, aryloxy, amino, alkylamino, arylamino, an aromatic heterocycle or a nonaromatic heterocycle, A1 is alkylene, A2 is carbonyl or sulfonyl, A3 is alkylene, A4 is carbonyl or oxalyl and n is o or 1.
    Type: Grant
    Filed: January 18, 2002
    Date of Patent: March 30, 2004
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Kazuo Nishimura, Masakazu Ban, Ken-ichi Fujimura, Naoyuki Kobayashi, Masanori Hori, Eiko Matsumoto
  • Quinolylpropylpiperidine derivatives, preparation process and intermediates, and compositions including them
    Publication number: 20040058919
    Abstract: Quinolylpropylpiperidine derivatives of general formula (I) in which:
    Type: Application
    Filed: July 18, 2003
    Publication date: March 25, 2004
    Applicant: Aventis Pharma S.A.
    Inventors: Eric Bacque, Jean-Luc Malleron, Serge Mignani, Michel Tabart
  • Novel heterocyclic compounds having antibacterial activity: Process for their preparation and pharmaceutical compositions containing them
    Publication number: 20040059120
    Abstract: The present invention relates to novel oxazolidinone compounds of the general formula (I).
    Type: Application
    Filed: August 1, 2003
    Publication date: March 25, 2004
    Applicants: DR. REDDY'S LABORATORIES INC., DR. REDDY'S LABORATORIES LIMITED
    Inventors: Selvakumar Natesan, Jagattaran Das, Javed Iqbal, Sitaram Kumar Magadi, Srinivasa Rao Naga Venkata Mamidi, Rajagopalan Ramanujam, Baskaran Sundarababu, Braj Bhushan Lohray
  • 3-Heterocyclylpropanohydroxamic acid PCP inhibitors
    Publication number: 20040058917
    Abstract: Compounds of formula (I): 1
    Type: Application
    Filed: August 19, 2003
    Publication date: March 25, 2004
    Inventors: Paul Vincent Fish, Jackie Diane Kendall, Gavin Alistair Whitlock
  • Substituted heterocyclic compounds and methods of use
    Publication number: 20040058918
    Abstract: The present invention relates to compounds having the general formula 1
    Type: Application
    Filed: September 8, 2003
    Publication date: March 25, 2004
    Inventors: Celia Dominguez, Dawei Zhang
  • Novel cystine derivative and agent for suppressing activation of inflammatory factors
    Publication number: 20040059110
    Abstract: The present invention provides cystine derivatives, which may be in a free form, a salt form, a solvate form. The cystine derivatives of the present invention may be used to suppress activation of inflammatory factors. Accordingly, the present invention provides: compositions containing the cystine derivatives; a method for suppressing the activation of inflammatory factors by administering the composition; a method for preventing, ameliorating and/or therapeutically treating diseases, skin injuries or disorders involved in the activation of inflammatory factors by administering the composition; a method for preventing, delaying, ameliorating and/or therapeutically treating skin change via aging or aesthetically unfavorable skin change as induced or promoted by inflammatory factors by administering the composition; and pharmaceutical agents containing the cystine derivatives.
    Type: Application
    Filed: August 4, 2003
    Publication date: March 25, 2004
    Applicant: AJINOMOTO CO., INC.
    Inventors: Takashi Nakano, Manabu Kitazawa, Keiji Iwasaki, Kazutami Sakamoto
  • Pyrimidine compounds
    Patent number: 6710052
    Abstract: Pyrimidine derivatives of the formula (I) wherein: one of Q1 and Q2 or both of Q1 and Q2 is substituted on a ring carbon by one substituent of the formula (Ia) [provided that when present in Q1 the substituent of formula (Ia) is not adjacent to the —NH— link]; wherein Q1, Q2, G, R1, X, Y1, Y2, Z, n and m are as described within; and pharmaceutically acceptable salts and in vivo hydrolyzable esters thereof are described. Processes for their manufacture, pharmaceutical compositions and their use as cyclin-dependent serine/threonine kinase (CDK) and focal adhesion kinase (FAK) inhibitors are also described.
    Type: Grant
    Filed: August 8, 2002
    Date of Patent: March 23, 2004
    Assignee: AstraZeneca
    Inventors: Elizabeth Janet Pease, Gloria Anne Breault, Robert Hugh Bradbury
  • Compounds useful as reversible inhibitors of cysteine proteases
    Publication number: 20040053921
    Abstract: Disclosed are cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R2, R3, R4, R6, R8 and Y are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds.
    Type: Application
    Filed: October 24, 2002
    Publication date: March 18, 2004
    Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Younes Bekkali, Denice Mary Spero, Sanxing Sun, Yancey David Ward
  • Metabolites of prinomastat and their synthesis
    Publication number: 20040053922
    Abstract: Metabolites of a matrix metalloproteinase inhibitor prinomastat and their synthesis. These metabolites are: (3S)-N-hydroxy4-(4-((1-oxy-pyrid-4-yl)oxy)benzenesulfonyl)-2,2-dimethyl-tetrahydro-2H-1,4-thiazine-3-carboxamide (M6); (3S)-2,2-dimethyl-1,1-dioxo-4-[4-(1-oxy-pyridin-4-yloxy)-benzenesulfonyl]-thiomorpholine-3-carboxylic acid amide (M7); (3S)-2,2-dimethyl-4-[4-(1-oxypyridin-4-yloxy)-benzenesulfonyl]-thiomorpholine-3-carboxylic acid amide (M8); (3S)-2,2-dimethyl-1,1-dioxo-4-[4-(pyridin-4-yloxy)-benzenesulfonyl]-thiomorpholine-3-carboxylic acid amide (M2); and (3S)-2,2-dimethyl-4-[4-(pyridin-4yloxy)-benzenesulfonyl)-thiomorphpline-3-carboxylic acid amide (M3).
    Type: Application
    Filed: June 10, 2003
    Publication date: March 18, 2004
    Applicant: Agouron Pharmaceuticals, Inc.
    Inventors: Michael A. Ouellette, Barbara C.M. Potts, Jayaram K. Srirangam, Anthony R. Tibbetts, Kanyin E. Zhang
  • Heteroaryl-substituted pyrrole derivatives, their preparation and their therapeutic uses
    Publication number: 20040054173
    Abstract: Compounds having activity against production of an inflammatory cytokine of formula (I)′: 1
    Type: Application
    Filed: January 30, 2003
    Publication date: March 18, 2004
    Applicant: SANKYO COMPANY, LIMITED
    Inventors: Tomio Kimura, Kazumasa Aoki, Akira Nakao, Shigeru Ushiyama, Takaichi Shimozato, Nobuyuki Ohkawa, Takayoshi Nagasaki, Takanori Yamazaki
  • Processes for preparing substituted pyrimidines
    Publication number: 20040049032
    Abstract: The present invention provides a facile process for the preparation of tri- and tetra-substituted pyrimidines. The process is useful for preparing inhibitors of protein kinases, especially Aurora kinase. These inhibitors are useful for treating or lessening the severity of Aurora-mediated diseases or conditions.
    Type: Application
    Filed: June 18, 2003
    Publication date: March 11, 2004
    Inventors: Jean-Damien Charrier, Francesca Mazzei, David Kay, Andrew Miller
  • Substituted 4-amino-2-arylcyclopenta[d]pyrimidines, their preparation, their use and pharmaceutical preparations comprising them
    Publication number: 20040048850
    Abstract: The present invention relates to compounds of formula (I) wherein R1, R2 and R3 have the meanings given in the claims. Said compounds are valuable active agents in medicaments for the treatment and prophylaxis of diseases, for example cardiovascular diseases such as hypertension, angina pectoris, heart failure, thrombosis and atherosclerosis. The compounds of formula (I) arc able to modulate the body's own production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the treatment and prophylaxis ofisorders associated with an impaired cGMP balance. The invention also relates to methods for producing compounds of formula (I), to their use in the treatment and prophylaxis of the above diseases and in the preparation of medicaments for such diseases, and to pharmaceutical preparations containing the compounds of formula (I).
    Type: Application
    Filed: September 12, 2003
    Publication date: March 11, 2004
    Applicant: Aventis Pharma Deutschland GmbH
    Inventors: Ursula Schindler, Karl Schoenafinger, Hartmut Strobel
  • Acylsemicarbazides as cyclin dependent kinase inhibitors useful as anti-cancer and anti-proliferative agents
    Publication number: 20040048844
    Abstract: The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): 1
    Type: Application
    Filed: May 1, 2003
    Publication date: March 11, 2004
    Applicant: Bristol-Myers Squibb Pharma Company
    Inventors: David Nugiel, David Carini, Susan DiMeo, Anup Vidwans, Eddy Yue
  • Method for the synthesis of quinoline derivatives
    Publication number: 20040049031
    Abstract: This invention relates to novel intermediates and processes for preparing pharmaceutically active quinoline compounds, including (−)-(S)-N-(&agr;-ethylbenzyl)-3-hydroxy-2-phenylquinoline-4-carboxamide.
    Type: Application
    Filed: May 20, 2003
    Publication date: March 11, 2004
    Applicant: SmithKline Beecham Corporation
    Inventors: Mark Mellinger, Conrad Kowalski
  • Novel tyrosine kinase inhibitors
    Publication number: 20040044203
    Abstract: The present invention provides compounds of formula I 1
    Type: Application
    Filed: October 2, 2002
    Publication date: March 4, 2004
    Inventors: Mark D. Wittman, Neelakantan Balasubramanian, Upender Velaparthi, Kurt Zimmermann, Mark G. Saulnier, Peiying Liu, Xiaopeng Sang, David B. Frennesson, Karen M. Stoffan, James G. Tarrant, Anne Marinier, Stephan Roy
  • Cycloalkyl alkanoic acids as intergrin receptor antagonists
    Publication number: 20040043988
    Abstract: The present invention relates to a class of compounds represented by the Formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula (I), and methods of selectively inhibiting or antagonizing the &agr;v&bgr;3 and/or &agr;v &bgr;5 integrin.
    Type: Application
    Filed: August 21, 2003
    Publication date: March 4, 2004
    Inventors: Ish Kurmar Khanna, Michael Clare, Alan Gasiecki, Thomas Rogers, Barbara B. Chen, Mark Russell, Hwang-Fun Lu
  • Nitrogen substituted 1,2,4-triazolo[3,4-a]phthalazine derivatives for enhancing cognition
    Publication number: 20040043982
    Abstract: The present invention provides a compound of formula (I) wherein A is an optionally substituted C1-4alkylidene group or a bond, R20 and R21 are hydrogen, alkyl groups or heterocyclic groups, R1 and R2 are small substituents or hydrogen, L is O, S or substituted N, X is a 5-or 6-membered heteroaromatic ring, Y is C1-4alkylidene and Z is a 5- or 6-membered heteroaromatic ring; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising it; its use in therapy; its use in making medicaments for treating neurodegenerative disease and methods of using it to enhance cognition.
    Type: Application
    Filed: May 21, 2003
    Publication date: March 4, 2004
    Inventors: Mark Stuart Chambers, Philip Jones, Angus Murray MacLeod, Robert James Maxey, Helen Jane Szekeres
  • 4-amino-quinazolines
    Publication number: 20040044204
    Abstract: Quinazolines of the formula I, in which R, R1, R2, R3, R4 and Y have the meaning indicated in Patent claim 1, and their salts or solvates as glycoprotein IbIX antagonists.
    Type: Application
    Filed: March 20, 2003
    Publication date: March 4, 2004
    Inventors: Werner Mederski, Ralf Devant, Gerhard Barnickel, Sabine Bernotat-Danielowski, James Vickers, Bertram Cezanne, Daljit Dhanoa, Bao-Ping Zhao, James Rinker, Mark R Player, Edward Jaeger, Richard Soll
  • Analogs of indole-3-carbinol metabolites as chemotherapeutic and chemopreventive agents
    Publication number: 20040043965
    Abstract: Novel compounds useful as chemotherapeutic and chemopreventive agents are provided. The compounds are analogs of indole-3-carbinol metabolites wherein the structures and substituents of the compounds are selected to enhance the compounds' overall efficacy, particularly with respect to therapeutic activity, oral bioavailability, long-term safety, patient tolerability, and therapeutic window. The compounds are useful not only in treatment of cancer but also in prevention of cancer.
    Type: Application
    Filed: August 20, 2002
    Publication date: March 4, 2004
    Inventors: Ling Jong, Wan-Ru Chao
  • Gem-substituted alpha v beta 3 antagonists
    Publication number: 20040043994
    Abstract: The present invention relates to a class of compounds represented by the Formula I.
    Type: Application
    Filed: January 21, 2003
    Publication date: March 4, 2004
    Inventors: Ish Kumar Khanna, Yi Yu, Hwang-Fun Lu, Nizal S. Chandrakumar, Renee M. Huff, Mark Russell, Mark L. Boys, Lori A. Schretzman, Barbara B. Chen, Bipinchandra N. Desai, Srinivasan Raj Nagarajan, Alan F. Gasiecki, Thomas D. Penning, Thomas Rogers, John Adam Wendt, Albert Khilevich, Yaping Wang
  • Vanilloid receptor ligands and their use in treatments
    Publication number: 20040038969
    Abstract: Compounds having the general structure 1
    Type: Application
    Filed: May 20, 2003
    Publication date: February 26, 2004
    Inventors: Elizabeth M. Doherty, Jiawang Zhu, Markian Stec, Mark H. Norman, Vassil I. Ognyanov, Christopher H. Fotsch, Ning Chen, Partha P. Chakrabarti, Liping H. Pettus, Hui-Ling Wang, Xianghong Wang, Premilla Arasasingham
  • Compositions useful as inhibitors of GSK-3
    Publication number: 20040039007
    Abstract: The present invention provides a compound of formula I: 1
    Type: Application
    Filed: August 1, 2003
    Publication date: February 26, 2004
    Inventors: Cornelia J. Forster, Larry C. Park, Marion W. Wannamaker, Yung-Mae M. Yao
  • Novel carbapenem derivatives
    Publication number: 20040038967
    Abstract: An objective of the present invention is to provide carbapenem derivatives which have strong antibiotic activity also against MRSA, PRSP, Influenzavirus, and &bgr;-lactamase producing bacteria and are stable to DHP-1.
    Type: Application
    Filed: February 14, 2003
    Publication date: February 26, 2004
    Inventors: Yuko Kano, Yasuo Yamamoto, Takahisa Maruyama, Takehiko Sawabe, Eiki Shitara, Kazuhiro Aihara, Kunio Atsumi, Takashi Ida
  • Thiazolidinedione derivative and its use as antidiabetic
    Publication number: 20040038968
    Abstract: A compound 5-[4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl]thiazolidine-2,4-dione potassium salt or a pharmaceutically acceptable solvate thereof, a pharmaceutical composition containing such a compound and the use of such a compound in medicine, particularly in the treatment of diabetes mellitus.
    Type: Application
    Filed: July 15, 2003
    Publication date: February 26, 2004
    Inventor: Michael Millan
  • 4-fluoroalkyl-2h-benzopyrans anti-estogenic activity
    Publication number: 20040034017
    Abstract: This invention describes the new 4-fluoroalkyl-2H-benzopyrans of general formula I, 1
    Type: Application
    Filed: January 7, 2003
    Publication date: February 19, 2004
    Inventors: Hermann Kuenzer, Rolf Jautelat, Ludwig Zorn, Christa Hegele-Hartung, Uwe Kollenkirchen, Karl-Heinrich Fritzemeier
  • Piperazine and piperidine derivatives
    Publication number: 20040034019
    Abstract: The present invention relates to piperazine and piperidine derivatives, which are especially useful for treating or preventing neuronal damage, particularly damage associated with neurological diseases. These compounds are also useful for stimulating nerve growth. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage or for stimulating nerve growth.
    Type: Application
    Filed: August 8, 2002
    Publication date: February 19, 2004
    Inventors: Ronald Tomlinson, David Lauffer, Michael Mullican
  • Quinoline and quinazoline compounds useful in therapy
    Publication number: 20040034032
    Abstract: Compounds of formula I, 1
    Type: Application
    Filed: August 13, 2003
    Publication date: February 19, 2004
    Applicant: Pfizer Inc
    Inventors: Alan John Collis, David Nathan Fox
  • Derivatives of naphthalene with comt inhibiting activity
    Publication number: 20040034011
    Abstract: Compounds of formula (I′), wherein A, R1 to R3 and t are as defined in the disclosure, exhibit COMT enzyme inhibiting activity so that they are useful as COMT inhibitors.
    Type: Application
    Filed: July 9, 2003
    Publication date: February 19, 2004
    Inventors: Reijo Bckstrm, Jarmo Pystynen, Timo Lotta, Martti Ovaska, Jyrki Taskinen
  • Methods of treating periodontal disease
    Publication number: 20040034020
    Abstract: The present invention relates to methods of treating periodontal disease.
    Type: Application
    Filed: February 3, 2003
    Publication date: February 19, 2004
    Inventors: Susan Mary Daluge, Cynthia Holder Jurgensen, Michael Tolar Martin, Martin Howard Osterhout
  • Benzothiophene derivative compounds process of preparation and use thereof
    Publication number: 20040034219
    Abstract: This invention provides new benzothiophene derivatives of general formula (I) and a process for preparing them, the corresponding compositions and their use for manufacturing a medicine for the treatment of neurological disorders. These new compounds behave as serotonin reuptake inhibitors and show high affinity towards the 5-HT1A receptor.
    Type: Application
    Filed: May 27, 2003
    Publication date: February 19, 2004
    Inventors: Marisabel Mourelle Mancini, Juan Carlos Del Castillo Nieto, Berta Esperanza Lasheras Aldaz, Antonio Monge Vega, Joaquin Del Rio Zambrana
  • Pyrimidine compounds
    Patent number: 6693097
    Abstract: This invention features pyrimidine compounds of formula (I): aryl, or heteroaryl; each of R2 and R4, independently, is Rc, halogen, nitro, cyano, isothionitro, SRc, or ORc; or R2 and R4, taken together, is carbonyl; R3 is Rc, alkenyl, alkynyl, ORc, OC(O)Rc, SO2Rc, S(O)Rc, S(O2)NRcRd, SRc, NRcRd, NRcCORd, NRcC(O)ORd, NRcC(O)NRcRd, NRcSO2Rd, CORc, C(O)ORc, or C(O)NRcRd; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is O, S, S(O), S(O2), or NRc; Y is a covalent bond, CH2, C(O), C═N—Rc, C═N—ORc, C═N—SRc, O, S, S(O), S(O2), or NRc; Z is N or CH; one of U and V is N, and the other is CRc; and W is O, S, S(O), S(O2), NRc, or NC(O)Rc; in which each of Ra and Rb, independently, is H, alkyl, aryl, heteroaryl; and each of Rc and Rd, independently, is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl.
    Type: Grant
    Filed: November 30, 2001
    Date of Patent: February 17, 2004
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Mitsunori Ono, Shijie Zhang, Teresa Przewloka, K. Koya, Elena Kostik, Yuniko Wada, Lijun Sun, Weiwen Ying
  • Amonafide salts
    Patent number: 6693198
    Abstract: Disclosed is a salt of amonafide or amonafide analogs represented Structural Formula (I): R1 is —(CH2)nN+HR3R4 X− or R1 is —(CH2)nN+HR3R4 X− or —(CH2)nNR3R4 when R2 is —N+HR6R7. R2 is —OR5, halogen, —NR6R7, —N+HR6R7 X− sulphonic acid, nitro, —NR5COOR5, —NR5COR5 or —OCOR5; R3 and R4 are independently H, C1-C4 alkyl group or, taken together with the nitrogen atom to which they are bonded, a non-aromatic nitrogen-containing heterocyclic group; each R5 is independently —H or a C1-C4 alkyl group; R6 and R7 are independently H, C1-C4 alkyl group or, taken together with the nitrogen atom to which they are bonded, a non-aromatic nitrogen-containing heterocyclic group; n is an integer from 0-3; and X− is the carboxylate anion of an organic carboxylic acid compound. Also disclosed are methods of preparing certain compounds represented by Structural Formula (I).
    Type: Grant
    Filed: April 22, 2002
    Date of Patent: February 17, 2004
    Assignee: Xanthus Life Sciences, Inc.
    Inventors: Alfred M. Ajami, David O. Barlow
  • 2-(1h-indol-3-yl)-2-oxo-acetic acid amides with antitumor activity
    Publication number: 20040029858
    Abstract: 2-(III-Indol-3-yl)-2-oxo-acetamide derivatives of formula (I) having antitumor activity in particular against solid tumors, specifically colon and lung tumors.
    Type: Application
    Filed: July 10, 2003
    Publication date: February 12, 2004
    Inventors: Ernesto Menta, Nicoletta Pescalli
  • Sulfonamide and sulfamide substituted imidazoquinolines
    Publication number: 20040029877
    Abstract: Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain sulfonamide or sulfonamide functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.
    Type: Application
    Filed: December 21, 2001
    Publication date: February 12, 2004
    Inventors: Stephen L. Crooks, Kyle J. Lindstrom, Bryon A. Merrill, Michael J. Rice
  • Novel aminotriazolone compounds, method for preparing same and pharmaceutical compositions containing same
    Publication number: 20040029875
    Abstract: A compound of formula (I): 1
    Type: Application
    Filed: April 11, 2003
    Publication date: February 12, 2004
    Inventors: Jean-Luc Fauchere, Jean-Claude Ortuno, Nigel Levens, Susana Chamorro, Jean Albert Boutin
  • Acylamino cyclopropane derivatives
    Publication number: 20040029876
    Abstract: This invention relates to novel acylamino cyclopropane derivatives, processes for their preparation, pharmaceutical compositions containing them and their use as modulators of dopamine D3 receptors and for the treatment of anxiety, psychosis, substance abuse, Parkinson's disease, sexual dysfunction, and other central nervous system disorders.
    Type: Application
    Filed: July 29, 2003
    Publication date: February 12, 2004
    Applicant: Pfizer Inc
    Inventors: Anton F. J. Fliri, Anthony R. Reinhold
  • Novel flavanoids as chemotherapeutic, chemopreventive, and antiangiogenic agents
    Publication number: 20040029914
    Abstract: Novel compounds are useful as chemotherapeutic, chemopreventative, and antiangiogenic agents are provided. The compounds are flavanoids, including flavanones, flavanols, and chalcones.
    Type: Application
    Filed: April 18, 2003
    Publication date: February 12, 2004
    Inventors: Nurulain Zaveri, Wan-Ru Chao
  • Heterocyclic inhibitors of ERK2 and uses thereof
    Publication number: 20040029857
    Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: 1
    Type: Application
    Filed: April 25, 2003
    Publication date: February 12, 2004
    Inventors: Michael Robin Hale, Francois Maltais, Qing Tang, Judith Straub, Alexander Aronov
  • Pyrimidine compounds
    Publication number: 20040024206
    Abstract: This invention features pyrimidine compounds of formula (I): 1
    Type: Application
    Filed: November 26, 2002
    Publication date: February 5, 2004
    Inventors: Lijun Sun, Mitsunori Ono, Elena Kostik, Yumiko Wada
  • 9,11-cycloendoperoxide pro-drugs of prostaglandin analogues for treatment of ocular hypertension and glaucoma
    Publication number: 20040023954
    Abstract: 9,11-Cycloendoperoxide derivatives of biologically active prostaglandin analogs, and particularly of the ocular hypotensive drugs Bimatoprost, Latanaprost, Unoprostone, Travoprost and prostaglandin H2 1-ethanolamide or of structurally closely related analogs, are pro-drugs which hydrolyze under physiological conditions to provide prostaglandin analogues that are capable of providing sustained ocular and other in vivo concentrations of the respective drugs. The compounds of the invention have the formula shown below where the variables have the meaning defined in the specification.
    Type: Application
    Filed: August 5, 2002
    Publication date: February 5, 2004
    Inventors: Kah-Hiing John Ling, Wu Yang, Jinsong Ni, Haiqing Yuan, Diane D.S. Tang-Liu
  • Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases
    Publication number: 20040023963
    Abstract: The present invention provides compounds of formula I: 1
    Type: Application
    Filed: May 14, 2003
    Publication date: February 5, 2004
    Inventors: Jingrong Cao, Jeremy Green, Young-Choon Moon, Jian Wang, Mark Ledeboer, Edmund Harrington, Huai Gao
  • 1-Heterocyclylalkyl-3-sulfonyl-indole or -indazole derivatives as 5-hydroxytryptamine-6 ligands
    Publication number: 20040024023
    Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.
    Type: Application
    Filed: July 17, 2003
    Publication date: February 5, 2004
    Applicant: Wyeth
    Inventors: Ronald Charles Bernotas, Steven Edward Lenicek
  • Tricyclic-2-pyridone compounds useful as HIV reverse transcriptase inhibitors
    Publication number: 20040023955
    Abstract: The present invention relates to tricyclic 2-pyridone compounds of formula (I): 1
    Type: Application
    Filed: June 10, 2003
    Publication date: February 5, 2004
    Inventors: James D. Rodgers, Haisheng Wang, Mona Patel, Argyrios Arvanitis, Anthony J. Cocuzza