Hetero Ring Patents (Class 544/209)
  • Patent number: 6645915
    Abstract: The invention relates to novel substituted 1,3,5-triazines of the general formula (I) in which A represents CHR3R4 or represents C1-halogenoalkyl-substituted C3-C6-cycloalkyl, C3-C6-alkinyl or C1-C4-cyanoalkyl, where R1, R2, R3 and R4 are each as defined in the description, and to processes for their preparation, to novel intermediates, including their preparation, and to the use of the compounds of the general formula (I) as herbicides.
    Type: Grant
    Filed: July 13, 2001
    Date of Patent: November 11, 2003
    Assignees: Nihon Bayer Agrochem K. K., Bayer Aktiengesellschaft
    Inventors: Hans-Jochem Riebel, Akihiko Yanagi, Yukiyoshi Watanabe, Toshio Goto, Kristian Kather, Stefan Lehr, Katharina Voigt, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen
  • Patent number: 6645964
    Abstract: The present invention relates to cancer therapy and to novel anticancer agent having a mechanism of action which is quite specific. It also relates to novel chemical compounds as well as their therapeutic application in humans.
    Type: Grant
    Filed: November 28, 2000
    Date of Patent: November 11, 2003
    Assignee: Aventis Pharma S.A.
    Inventors: Patrick Mailliet, Jean-François Riou, Jean-Louis Mergny, Abdelazize Laoui, François Lavelle, Odile Petitgenet
  • Publication number: 20030208073
    Abstract: The invention relates to novel substituted N-aryl nitrogen-containing heterocyclic compounds of the general formula (I) 1
    Type: Application
    Filed: January 29, 2003
    Publication date: November 6, 2003
    Inventors: Karl-Heinz Linker, Kurt Findeisen, Otto Schallner, Andreas Lender, Hans-Joachim Santel, Markus Dollinger, Akihiko Yanagi, Toshio Goto
  • Patent number: 6638932
    Abstract: This invention concerns the use of the 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, C1-6alkyloxycarbonyl or substituted C1-6alkyl; 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, polyhalomethylthio, —S(═O)pR4, —NH—S(═O)pR4, —C(═O)R4, —NHC(═O)H, —C(═O)NHNH2, —NHC(═O)R4, —C(═NH)R4 or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C1-10alkyl, C2-10alk
    Type: Grant
    Filed: August 2, 2001
    Date of Patent: October 28, 2003
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Bart De Corte, Marc René de Jonge, Jan Heeres, Paul Adriaan Jan Janssen, Robert W. Kavash, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken
  • Patent number: 6638926
    Abstract: This invention provides novel pyrazole compounds that are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3. The compounds may be used to treat abnormal physiological function leading to diseases such as cancer, diabetes and Alzheimer's disease.
    Type: Grant
    Filed: September 14, 2001
    Date of Patent: October 28, 2003
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Robert J. Davies, Pan Li, Jean-Damien Charrier, David Bebbington
  • Publication number: 20030191126
    Abstract: A serotonin reuptake inhibitor containing a cyclic amine represented by the following formula, a prodrug thereof, or a pharmaceutically acceptable salt of said cyclic amine or prodrug as an active ingredient: 1
    Type: Application
    Filed: January 17, 2003
    Publication date: October 9, 2003
    Applicant: SUMITOMO PHARMACEUTICALS COMPANY LIMITED
    Inventors: Toru Kodo, Shuji Masumoto, Koji Koyama, Naoya Kinomura
  • Patent number: 6630469
    Abstract: Amino-pyrimidine and amino-triazine derivatives having 5-HT7 antagonist activity for the treatment of sleeping disorders, depression, schizophrenia, anxiety, obsessive compulsive disorders, circadian rhythm disorders, ocular disorders and/or centrally and peripherally mediated hypertension are provided.
    Type: Grant
    Filed: April 24, 2001
    Date of Patent: October 7, 2003
    Assignee: Bristol-Myers Squibb Company
    Inventors: Michael A. Poss, Ashok V. Purandare, Ronald J. Mattson, Li-Qiang Sun
  • Patent number: 6630470
    Abstract: Invented are G-CSF mimetics. Also invented are selected octacyclic compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds as G-CSF mimetics. Also invented are novel processes used in preparing these compounds.
    Type: Grant
    Filed: November 20, 2000
    Date of Patent: October 7, 2003
    Assignee: SmithKline Beecham Corporation
    Inventors: Juan I Luengo, Kevin J Duffy
  • Publication number: 20030166644
    Abstract: Use of compounds to inhibit hormone-sensitive lipase, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and novel compounds. The present compounds are inhibitors of hormone-sensitive lipase and may be useful in the treatment and/or prevention of medical disorders where a decreased activity of hormone-sensitive lipase is desirable.
    Type: Application
    Filed: December 13, 2002
    Publication date: September 4, 2003
    Inventors: Soren Ebdrup, Johannes Cornelis de Jong, Poul Jacobsen, Holger Claus Hansen, Per Vedso
  • Publication number: 20030153570
    Abstract: The invention relates to aryl triazines and uses thereof, including to inhibit lysophosphatidic acid acyltransferase &bgr; (LPAAT-&bgr;) activity and/or proliferation of cells such as tumor cells.
    Type: Application
    Filed: October 30, 2002
    Publication date: August 14, 2003
    Applicant: Cell Therapeutics, Inc.
    Inventors: Rama Bhatt, Baoqing Gong, Feng Hong, Scott A. Jenkins, J. Peter Klein, Anil M. Kumar, John Tulinsky
  • Publication number: 20030149041
    Abstract: Compounds that selectively inhibit inappropriate kinase activities and methods for their preparation are disclosed.
    Type: Application
    Filed: June 28, 2002
    Publication date: August 7, 2003
    Applicant: Pharmacopeia, Inc.
    Inventors: Shawn David Erickson, James Inglese, Jeffrey John Letourneau, Christopher Mark Riviello
  • Patent number: 6596461
    Abstract: A compound of formula (I) wherein n is e.g. a number from 2 to 50; R5′ and R5″ are e.g. a group of formula (II); G1, G2, G3 and G4 are e.g. C1-C4akyl; R1 is e.g. hydrogen or C1-C4alkyl; R2 is e.g. methylene; R3′ is e.g. hydrogen and R3″ is e.g. hydrogen or C1-C4alkyl; R4 is e.g. C2-C8alkylene; and X is e.g. —N(R7)R8) with R7 and R8 being independently of one another hydrogen or C1-C8alkyl, is useful for stabilizing an organic material against degradation induced by light, heat or oxidation.
    Type: Grant
    Filed: May 22, 2001
    Date of Patent: July 22, 2003
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Dario Lazzari, Mirko Rossi, Graziano Zagnoni, Alessandro Zedda, Valerio Borzatta, Stephen Mark Andrews
  • Publication number: 20030114451
    Abstract: The present invention describes novel isoxazolo[1,5-a]pyrimidines of formula: 1
    Type: Application
    Filed: March 27, 2002
    Publication date: June 19, 2003
    Inventor: William Eric Frietze
  • Patent number: 6576631
    Abstract: A pyrimidinylbenzimidazole or triazinylbenzimidazole derivative represented by the general formula (I): wherein A is N or CR3, and R1, R2, R3, X, Y and n are as defined in the disclosure.
    Type: Grant
    Filed: May 8, 2001
    Date of Patent: June 10, 2003
    Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.
    Inventors: Masaru Shibata, Kiyoshi Kawai, Takechi Makihara, Norihisa Yonekura, Takehiro Kawashima, Junetsu Sakai, Norimichi Muramatsu
  • Patent number: 6569856
    Abstract: This invention is directed to triazine derivatives which are selective antagonists for a NPY (Y5) receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: January 3, 2002
    Date of Patent: May 27, 2003
    Assignee: Synaptic Pharmaceutical Corporation
    Inventors: Mohammad R. Marzabadi, Stewart A. Noble, Mahesh N. Desai
  • Publication number: 20030087908
    Abstract: The invention encompasses compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions, uses and methods for prophylaxis and treatment of cancer and angiogenesis-related disease.
    Type: Application
    Filed: April 10, 2002
    Publication date: May 8, 2003
    Inventors: Stephanie D. Geuns-Meyer, Lucian V. DiPietro, Joseph L. Kim, Vinod F. Patel
  • Publication number: 20030078265
    Abstract: N-Heterocyclic derivatives of the formula (I): 1
    Type: Application
    Filed: April 12, 2002
    Publication date: April 24, 2003
    Applicant: Berlex Laboratories, Inc.
    Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
  • Publication number: 20030069245
    Abstract: This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with indoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.
    Type: Application
    Filed: December 19, 2001
    Publication date: April 10, 2003
    Inventors: Owen B. Wallace, Tao Wang, Kap-Sun Yeung, Bradley C. Pearce, Nicholas A. Meanwell, Zhilei Qiu, Haiquan Fang, Qiufen May Xue, Zhiwei Yin
  • Publication number: 20030060452
    Abstract: N-Heterocyclic derivatives of the formula (I): 1
    Type: Application
    Filed: April 12, 2002
    Publication date: March 27, 2003
    Applicant: Berlex Laboratories, Inc.
    Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
  • Publication number: 20030060608
    Abstract: Disclosed are compositions for printing recording materials, especially textile fibre materials, paper and papery substrates and plastic films and plastic transparencies by the inkjet printing process, including
    Type: Application
    Filed: September 20, 2002
    Publication date: March 27, 2003
    Inventors: Ludwig Hasemann, Reinhard Pedrazzi, Josef Geisenberger, Josef Ritter, Hans-Tobias Macholdt, Andreas Wuzik
  • Publication number: 20030027794
    Abstract: N-Heterocyclic derivatives of the formula (I): 1
    Type: Application
    Filed: April 12, 2002
    Publication date: February 6, 2003
    Applicant: Berlex Laboratories, Inc.
    Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
  • Publication number: 20030022885
    Abstract: This invention describes novel pyrazole compounds of formula II: 1
    Type: Application
    Filed: December 20, 2001
    Publication date: January 30, 2003
    Inventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Francoise Pierard
  • Patent number: 6509338
    Abstract: The present invention describes novel pyrazolo[1,5-a]triazines of formula: wherein R3 is an alkyl, alkenyl, alkynyl, or cycloalkyl group, or pharmaceutically acceptable salt forms thereof, which are useful as CRF antagonists.
    Type: Grant
    Filed: June 14, 1999
    Date of Patent: January 21, 2003
    Assignee: Bristol-Myers Squibb Company
    Inventors: Richard Eric Olson, William Eric Frietze
  • Publication number: 20030004166
    Abstract: This invention is directed to sorbitol dehydrogenase inhibitory compounds of formula I 1
    Type: Application
    Filed: March 26, 2002
    Publication date: January 2, 2003
    Inventor: Banavara L. Mylari
  • Patent number: 6492440
    Abstract: A product obtainable by 1) reacting a compound of the formula (&agr;) with a compound of the formula (&bgr;) in a molar ratio of 1.2:1 to 1.4:1; 2) reacting the end groups of the formula (&ggr;) being present in the product of the reaction 1) with e.g. dibutylamine in a molar ratio of 2:1.7 to 2:3; the reactions 1) and 2) being carried out in an organic solvent in the presence of an inorganic base; and 3) transferring the groups of the formula being present in the product of the reaction 2) to groups of the formula said transfer being carried out by reacting the product of the reaction 2) with a hydroperoxide in a hydrocarbon solvent in the presence of a peroxide decomposing catalyst. The products obtained are useful as light stabilizers, heat stabilizers and oxidation stabilizers for organic materials, in particular synthetic polymers such as polyolefins.
    Type: Grant
    Filed: June 9, 2000
    Date of Patent: December 10, 2002
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: James Peter Galbo, Nicola Lelli, Valerio Borzatta, Jean-Pierre Wolf, Michael Ackerman, Piero Piccinelli, Ivan Orban
  • Publication number: 20020183323
    Abstract: N-Heterocyclic derivatives of the formula (I): 1
    Type: Application
    Filed: April 12, 2002
    Publication date: December 5, 2002
    Applicant: Berlex Laboratories, Inc.
    Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
  • Patent number: 6489333
    Abstract: This invention relates to novel heterocycles which are useful as antagonists of the &agr;v&bgr;3 integrin, the &agr;2b&bgr;3 integrin, and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.
    Type: Grant
    Filed: April 9, 2001
    Date of Patent: December 3, 2002
    Assignee: Bristol - Meyers Squibb Pharma Company
    Inventors: William J. Pitts, Prabhakar K. Jadhav
  • Publication number: 20020165203
    Abstract: N-Heterocyclic derivatives of the formula (I): 1
    Type: Application
    Filed: April 12, 2002
    Publication date: November 7, 2002
    Applicant: Berlex Laboratories, Inc.
    Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
  • Patent number: 6476026
    Abstract: The present invention relates to novel N-cyanomethyl amides which are cysteine protease inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.
    Type: Grant
    Filed: March 15, 2000
    Date of Patent: November 5, 2002
    Assignee: Axys Pharmaceuticals, Inc.
    Inventors: Clifford M. Bryant, James T. Palmer, Robert M. Rydzewski, Eduardo L. Setti, Zong-Qiang Tian, Shankar Venkatraman, Dan-Xiong Wang
  • Patent number: 6472384
    Abstract: The present invention relates to ester, ether and N-alkylcarbamoyl derivatives of compound (Ia) and pharmaceutically acceptable salts thereof. These compounds exhibit excellent antibacterial activity and are useful for the treatment or prevention of bacterial infections. (wherein R1 is a hydrogen atom or a methyl group; R2a is a hydrogen atom, a protecting group for a hydroxy group, or a methyl group; R3 is a hydrogen atom or a protecting group for a hydroxy group; R4a is a hydrogen atom, a hydroxy group or a protected hydroxy group; R5 is a hydrogen atom or a protecting group for a hydroxy group; and X is a methylene group or a sulfur atom). The invention also includes compounds which are related to the aforeidentified compounds.
    Type: Grant
    Filed: January 9, 2001
    Date of Patent: October 29, 2002
    Assignee: Sankyo Company, Limited
    Inventors: Masatoshi Inukai, Masakatsu Kaneko, Toshio Takatsu, Hitoshi Hotoda, Masatoshi Arai, Shunichi Miyakoshi, Masaaki Kizuka, Yasumasa Ogawa
  • Patent number: 6469165
    Abstract: Polyaminotriazines represented by formula (I) can be prepared by conducting a reduction alkylamination of a tetramethylpiperidone with a diamine represented by formula (IIb), NH2—R—NH2, in the presence of a hydrogenating catalyst, removing the catalyst upon completion of the reaction to obtain an unrefined crude product (A); and, conducting a polycondensation reaction of the unrefined crude product (A) and a dichlorotriazine in an aromatic solvent and in the presence of an inorganic base.
    Type: Grant
    Filed: December 27, 1994
    Date of Patent: October 22, 2002
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Kenji Kimura, Shinya Tanaka, Manji Sasaki
  • Patent number: 6465645
    Abstract: Hindered amine compounds which are substituted by a long hydrocarbon chain are useful in a number of applications where the solubility or compatibility afforded by said substitution is needed. This is seen particularly for example with white, dyed, dipped, unscented and/or scented candle wax which is effectively stabilized against discoloration and fading by the incorporation therein of a long chain hindered amine alone or in combination with a UV absorber and/or an antioxidant.
    Type: Grant
    Filed: April 17, 2001
    Date of Patent: October 15, 2002
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Mervin G. Wood, Andrea R. Smith, James P. Galbo
  • Publication number: 20020147181
    Abstract: This invention concerns the compounds of formula 1
    Type: Application
    Filed: November 15, 2001
    Publication date: October 10, 2002
    Inventors: Paul A.J. Janssen, Jan Heeres, Henri E.L. Moereels, Michael Joseph Kukla, Donald W. Ludovici
  • Patent number: 6451737
    Abstract: The invention related to novel substituted arylsulphonyl(thio)ureas wherein: A is nitrogen or a CH grouping, Q is oxygen or sulphur, R1 is hydrogen, halogen or optionally substituted alkyl, alkoxy, alkylthio, alkylamino, dialkylamino, cycloalkyl, cycloalkyloxy or heterocyclyloxy, R2 is hydrogen, halogen or optionally substituted alkyl, alkoxy, alkylthio, alkylamino, dialkylamino, cycloalkyl, cycloalkyloxy or heterocyclyloxy, R3 is hydrogen or optionally substituted alkyl, R4 is optionally substituted alkyl, alkoxy, alkenyl, alkinyl, alkenyloxy, alkinyloxy, cycloalkyl, cycloalkyloxy or cycloalkylalkyl, and R5 is hydrogen, formyl or optionally substituted alkyl, alkylcarbonyl, alkoxycarbonyl, alkylsulphonyl, alkenyl, alkinyl, cycloalkyl, cycloalkylcarbonyl, cycloalkylsulphonyl or heterocyclyl, and salts of compounds of the formula (I), except for the compound N-(4,6-dimethyl-pyrimidin-2-yl)-N′-[2-(1,1,2,2-tetrafluoro-ethoxy)-6-methyl-phenylsulphonyl]-urea.
    Type: Grant
    Filed: August 28, 1998
    Date of Patent: September 17, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ernst Rudolf F. Gesing, Rolf Kirsten, Joachim Kluth, Klaus-Helmut Müller, Mark Wilhelm Drewes, Johannes Rudolf Jansen, Ulrich Philipp, Hans-Jochem Riebel, Otto Schallner, Markus Dollinger, Hans-Joachim Santel
  • Patent number: 6444809
    Abstract: Compounds of formula I wherein G, J, L, M, m and D have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of neurokinin A and useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
    Type: Grant
    Filed: September 22, 2000
    Date of Patent: September 3, 2002
    Assignee: Zeneca Limited
    Inventor: Scott Carson Miller
  • Patent number: 6441166
    Abstract: A product containing 5 to 85% of a group (A-1-a) and/or (A-1-b) and 15 to 95% of a group (A-2), the total sum of the groups (A-1-a), (A-1-b) and (A-2) being 100%, is useful for stabilizing an organic material against degradation induced by light, heat or oxidation.
    Type: Grant
    Filed: December 13, 1999
    Date of Patent: August 27, 2002
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Dario Lazzari, Graziano Zagnoni, Stephen Mark Andrews
  • Publication number: 20020103195
    Abstract: The invention relates to triazines and the use thereof to inhibit lysophosphatidic acid acyltransferase &bgr; (LPAAT-&bgr;) activity. The invention further relates to methods of treating cancer using said triazines. The invention also relates to methods for screening for LPAAT-&bgr; activity.
    Type: Application
    Filed: October 31, 2001
    Publication date: August 1, 2002
    Applicant: CELL THERAPEUTICS,INC.
    Inventors: Lynn Bonham, J. Peter Klein, Robert E. Finney, David M. Hollenback, Scott A. Shaffer, Norina M. Tang, Thayer H. White, David W. Leung
  • Publication number: 20020103201
    Abstract: This invention is directed to triazine derivatives which are selective antagonists for a NPY (Y5) receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: January 3, 2002
    Publication date: August 1, 2002
    Applicant: Synaptic Pharmaceutical Corporation
    Inventors: Mohammad R. Marzabadi, Stewart A. Noble, Mahesh N. Desai
  • Patent number: 6420313
    Abstract: The invention relates to novel thienylalkylamino-1,3,5-triazines of the general formula (I) in which A, R1, R2, R3, R4, R5 and Z are as defined in the description, to processes for their preparation, to their use as herbicides and to novel intermediates and their preparation.
    Type: Grant
    Filed: November 30, 2000
    Date of Patent: July 16, 2002
    Assignees: Bayer Aktiengesellschaft, Nihon Bayer Agrochem, K.K.
    Inventors: Rolf Kirsten, Hans-Jochem Riebel, Stefan Lehr, Katharina Voigt, Kristian Kather, Mark Wilhelm Drewes, Markus Dollinger, Ingo Wetcholowsky, Yukiyoshi Watanabe, Toshio Goto
  • Patent number: 6409941
    Abstract: A product obtainable by transferring groups of formula (G-I) being present in a block oligomer having a polydispersity {overscore (M)}w/{overscore (M)}n of 1 to 1.7 and corresponding to formula (I) to groups of formula (Gu-II), wherein R1 is a hydrocarbyl radical or —O—R1 is oxyl; said transfer is carried out by reaction of the block oligomer with a hydroperoxide in a hydrocarbon solvent in the presence of a peroxide decomposing catalyst; n is a number from 2 to 14; R2 is for example C2-C12alkylene; A is for example —N(R4)(R5); R4 and R5 are for example C1-C18alkyl; R is preferably a group of formula (G-I) and B and B* have one of the meanings given for A; with the proviso that in the individual recurrent units of formula (I), each of the radicals B, R and R2 has the same or a different meaning. The products are useful as light stabilizers, heat stabilizers and oxidation stabilizers for organic materials, in particular synthetic polymers.
    Type: Grant
    Filed: November 18, 1999
    Date of Patent: June 25, 2002
    Assignee: Ciba Specialty Chemicals Corp.
    Inventors: James Peter Galbo, Nicola Lelli, Valerio Borzatta, Jean-Pierre Wolf, Michael Ackerman, Piero Piccinelli
  • Patent number: 6407041
    Abstract: The invention relaters to compounds of the formula: and their use as herbicides.
    Type: Grant
    Filed: July 10, 2000
    Date of Patent: June 18, 2002
    Assignees: Bayer Aktiengesellschaft, Nihon Bayer Agrochem, K.K.
    Inventors: Katharina Voigt, Hans-Jochem Riebel, Stefan Lehr, Andreas Lender, Rolf Kirsten, Markus Dollinger, Mark Wilhelm Drewes, Ingo Wetcholowsky, Yukiyoshi Watanabe, Toshio Goto, Randy Allen Myers
  • Patent number: 6403680
    Abstract: A product obtained by 1) reacting a compound of the formula (&agr;) with a compound of the formula (&bgr;) in a stoichiometric ratio to obtain a compound of the formula (&ggr;) 2) reacting the compound of the formula (&bgr;) with the compound of the formula (&ggr;) in a molar ratio of 0.4:1 to 0.75:1; 3) reacting the end groups of the formula (&dgr;) being present in the product of the reaction 2) with e.g. dibutylamine in a molar ratio of 2:1.7 to 2:3; the reactions 1) to 3) being carried out in an organic solvent in the presence of an inorganic base; and 4) transferring the groups of the formula being present in the product of the reaction 3) to groups of the formula said transfer being carried out by reacting the product of the reaction 3) with a hydroperoxide in a hydrocarbon solvent in the presence of a peroxide decomposing catalyst; R1 is in particular a hydrocarbyl radical, B is e.g.
    Type: Grant
    Filed: November 18, 1999
    Date of Patent: June 11, 2002
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: James Peter Galbo, Nicola Lelli, Valerio Borzatta, Jean-Pierre Wolf, Michael Ackerman, Piero Piccinelli, Ivan Orban
  • Patent number: 6399620
    Abstract: There are described cycloalkyl derivatives of the formula (I) R1—Y—A—B—D—E—F—G  (I) in which R1, Y, A, B, D, E, F and G have the meaning indicated herein, their preparation and their use as medicaments. The compounds according to the invention can be used as vitronectin receptor antagonists and as inhibitors of bone resorption.
    Type: Grant
    Filed: June 29, 2000
    Date of Patent: June 4, 2002
    Assignee: Aventis Pharma S.A.
    Inventors: Volkmar Wehner, Jochen Knolle, Hans Ulrich Stilz, Jean-Francois Gourvest, Denis Carniato, Thomas Richard Gadek, Robert McDowell, Robert Maurice Pitti, Sarah Catherine Bodary
  • Patent number: 6388072
    Abstract: Hindered amines substituted on the N-atom with an —O—E—OH moiety are particularly effective in stabilizing polyolefin and automotive coating compositions against the deleterious effects of oxidative, thermal and actinic radiation where the presence of the OH group on the compounds adds important properties not attainable by the use of normal —O—E moieties.
    Type: Grant
    Filed: February 21, 2001
    Date of Patent: May 14, 2002
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: James P. Galbo, Gerald A. Capocci, Nancy N. Cliff, Robert E. Detlefsen, Michael P. DiFazio, Ramanathan Ravichandran, Peter Solera
  • Patent number: 6384032
    Abstract: The invention relates to a compound of formula (I) which can inhibit the production of IL-12. Also disclosed is a method of inhibiting IL-12 production by administering to a patient in need thereof an effective amount of a compound of formula (I).
    Type: Grant
    Filed: June 15, 2000
    Date of Patent: May 7, 2002
    Assignee: Shionogi Bioresearch Corp.
    Inventors: Mitsunori Ono, Yumiko Wada, Beatrice Brunkhorst, Tadeusz Warchol, Wojciech Wrona, Dan Zhou, Nha Huu Vo, Stephen Gillies
  • Publication number: 20020049212
    Abstract: A compound of the formula: 1
    Type: Application
    Filed: January 3, 2001
    Publication date: April 25, 2002
    Inventors: Fumitaka Ito, Hirohide Noguchi, Yoriko Ohashi, Hirohisa Shimokawa
  • Patent number: 6372729
    Abstract: This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR4 or N; n is 0, 1, 2, 3 or 4; R1 and R2 are each independently selected from hydrogen, hydroxy, C1-12alkyl, C1-12alkyloxy, C1-12alkylcarbonyl, C1-12alkyloxycarbonyl, aryl, amino, mono- or di(C1-12alkyl)amino, mono- or di(C1-12alkyl)aminocarbonyl wherein each of the aforementioned C1-12alkyl groups may optionally and each individually be substituted; or R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-12alkyl)aminoC1-4alkylidene; R3 is hydrogen, aryl, C1-6alkylcarbonyl, optionally substituted C1-6alkyl; and each R4 independently is hydroxy, halo, C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl or trihalomethyloxy; L is —X—R5 or —X-Alk-R6; wherein R5 and R6 each independently are indanyl, indolyl or phenyl; each of
    Type: Grant
    Filed: August 8, 2000
    Date of Patent: April 16, 2002
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Frederik Frans Desiré Daeyaert, Bart De Corte, Marc René De Jonge, Jan Heeres, Chih Yung Ho, Paul Adriaan Jan Janssen, Robert W. Kavash, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici
  • Patent number: 6372435
    Abstract: The present invention provides methods of correlating genetic variants in the beta-chemokine receptor 5 (CCR5) locus, more specifically CCR5 promoter alleles and genotypes, with HIV-1 transmission and/or disease progression in individuals and populations.
    Type: Grant
    Filed: August 11, 2000
    Date of Patent: April 16, 2002
    Assignee: UAB Research Foundation
    Inventors: Richard A. Kaslow, Jianming Tang
  • Patent number: 6372743
    Abstract: Disclosed are compounds of the formula: where R1, R2, R3, R4, R5, R6, and X are defined herein. These compounds are selective modulators of NPY1 receptors. These compounds are useful in the treatment of a number of CNS disorders, metabolic disorders, and peripheral disorders, particularly eating disorders and hypertension. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of NPY1 receptors and as standards in assays for NPY1 receptor binding. Methods of using the compounds in receptor localization studies are given.
    Type: Grant
    Filed: September 29, 2000
    Date of Patent: April 16, 2002
    Assignees: Neurogen Corporation, Pfizer Inc.
    Inventors: James W. Darrow, Stephane De Lombaert, Charles Blum, Jennifer Tran, Mark Giangiordano, David Andrew Griffith, Philip Albert Carpino
  • Patent number: 6346503
    Abstract: The invention relates to novel substituted 2-amino-4-alkylamino-1,3,5-triazines of the formula (I) in which R1 represents in each case optionally substituted alkyl having 2 to 6 carbon atoms or cycloalkyl having 3 to 6 carbon atoms, R2 represents hydrogen or represents alkyl having 1 to 4 carbon atoms, A represents oxygen or methylene, Ar represents in each case optionally substituted phenyl, naphthyl or heterocyclyl, and Z represents hydrogen, represents halogen or represents in each case optionally substituted alkyl, alkoxy, alkylcarboxyl, alkoxycarbonyl, alkylthio, alkylsulphinyl, alkylsulphonyl, alkenyl or alkinyl, to processes and to novel intermediates for their preparation and to their use as herbicides.
    Type: Grant
    Filed: April 6, 1999
    Date of Patent: February 12, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hans-Jochem Riebel, Stefan Lehr, Uwe Stelzer, Yukiyoshi Watanbe, Markus Dollinger