Chalcogen Bonded Directly To Piperazine Ring Carbon Patents (Class 544/384)
-
Patent number: 6911447Abstract: Disclosed are MC-3/MC-4 receptor ligands, the ligands having the following formula: wherein A is a conformationally restricted ring system selected from the group consisting of: a) non-aromatic carbocyclic rings; b) aromatic carbocyclic rings; c) non-aromatic heterocyclic rings; d) aromatic heterocyclic rings; wherein said rings comprises from 5 to 8 atoms; and W is a unit which preferable comprises D-1-fluorophenyalanine, Y comprises a heteroatom, and Z comprises an aromatic carbocyclic ring. Also disclosed are pharmaceutical compositions comprising the ligands of the invention as well as methods of treating diseases mediated through MC-3/MC-4 receptors.Type: GrantFiled: April 12, 2002Date of Patent: June 28, 2005Assignee: The Procter & Gamble CompanyInventors: Wieslaw Adam Mazur, Xinrong Tian, Xiufeng Eric Hu, Frank Hallock Ebetino
-
Patent number: 6906074Abstract: A 2-phenylpiperazine derivative represented by the formula (I) or a pharmaceutically acceptable salt, hydrate, or complex thereof: wherein each of X1 and X3 is oxygen or two hydrogen atoms, X2 O, NH, NCH3, or CH2, n is an integer of 0 or 1, R1 is hydrogen or lower alkyl and R2 is hydrogen, cyano, tetrazolyl, aminotriazolyl , mesyl, t-butoxycarbonyl, or a lower alkyl which may be optionally substituted, R3 is hydrogen, halogen, lower alkyl or lower alkoxy, each of R4 and R5 is hydrogen, lower alkoxy or trifluoromethyl, and a broken line indicates a single or double bond. The derivative may be used as a tachykinin antagonist in the treatment of diseases of the digestive system, nervous system and respiratory system, inflammation, allergy, carcinoid syndrome, chronic pain, headache, Crohn disease, depression and vomiting.Type: GrantFiled: February 20, 2003Date of Patent: June 14, 2005Assignee: Nippon Zoki Pharmaceutical Co., Ltd.Inventors: Takashi Ogino, Yukari Konishi, Kunihiko Higashiura, Kazuhito Furukawa
-
Patent number: 6858599Abstract: This invention relates to tricyclic compounds having spiro union represented by the following formula (I) or its salt which is useful as a drug, and in particular, as an inhibitor for activated blood coagulation factor X, which can be administered orally and which exhibits strong anticoagulation action. The invention also relates to a pharmacophore which was derived from the compound and is useful in molecular designing of the FXa inhibitor.Type: GrantFiled: December 27, 2001Date of Patent: February 22, 2005Assignee: Mochida Pharmaceutical Co., Ltd.Inventors: Hidemitsu Nishida, Fumihiko Saitoh, Kousuke Harada, Ikuya Shiromizu, Takafumi Mukaihira
-
Patent number: 6852855Abstract: A novel process for preparing a compound of the formula I: wherein R1 denotes substituted or unsubstituted alkyl, alkoxy, aryl, aryloxy or arylalkoxy; R2 denotes substituted or unsubstituted alkyl, alkoxy, aryl, aryloxy, arylalkoxy, tosyl, formyl, acetyl or amine; and R3 denotes substituted or unsubstituted alkyl, alkoxy, aryl, aryloxy or arylalkoxy is disclosed. These compounds are useful in the synthesis of the antidepressant mirtazapine and other tetracyclic compounds.Type: GrantFiled: August 24, 2001Date of Patent: February 8, 2005Assignee: Teva Pharmaceutical Industries Ltd.Inventor: Ben-Zion Dolitzky
-
Publication number: 20040242879Abstract: The present invention describes an industrially advantageous process to prepare highly pure 1-Methyl-3-phenylpiperazine of Formula I 1Type: ApplicationFiled: August 26, 2003Publication date: December 2, 2004Inventors: Vijay Kumar Handa, Divvela Venkata Naga Srinivasa Rao, Meenakshisunderam Sivakumaran
-
Patent number: 6818645Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: wherein X, Y, and Z are O, S, or NR4, and the other substituents are as defined in the specification; and prodrugs, individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.Type: GrantFiled: August 1, 2003Date of Patent: November 16, 2004Assignee: Syntex (U.S.A.) LLCInventors: Robert James Weikert, Ann Marie Madera, Russell Stephen Stabler
-
Publication number: 20040214832Abstract: Disclosed are piperazine derivatives, their manufacture and use as inhibitors of renin.Type: ApplicationFiled: March 26, 2004Publication date: October 28, 2004Inventors: Cuiman Cai, Emma Hazel Clay, Dennis M. Downing, Jeremy John Edmunds, Daniel Dale Holsworth, Tingsheng Li, Noel Aaron Powell
-
Patent number: 6809202Abstract: The synthesis of individual di- and tri-substituted-1,4-diazacyclic compounds having 6- to 8-atoms in the cyclic ring, their corresponding 1,6-diketo-2,5-diazacyclic compounds and similar 1,4-diazacyclic ring compounds having one ring carbonyl gorup and 6-8 atoms in the ring is disclosed, as are libraries of such compounds. Methods of preparing and using the libraries of compounds as well as individual compounds of the libraries are also disclosed.Type: GrantFiled: June 6, 2002Date of Patent: October 26, 2004Assignee: Torrey Pines Institute for Molecular StudiesInventors: Adel Nefzi, John M. Ostresh, Richard A. Houghten
-
Patent number: 6787543Abstract: A compound of the formula (I): in which Z, R1, R2, R8, R10, R11, R12, R13 and R14 are each as defined in the description, or a salt thereof. The object compound of the present invention has pharmacological activities such as Tachykinin antagonism, and is useful for manufacture of a medicament for treating or preventing Tachykinin-mediated diseases.Type: GrantFiled: December 20, 2002Date of Patent: September 7, 2004Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kazuhiko Take, Chiyoshi Kasahara, Shinji Shigenaga, Hidenori Azami, Yoshiteru Eikyu, Kazuo Nakai, Masataka Morita
-
Patent number: 6770637Abstract: Substituted 4-phenyl-pyridine compounds with activity as antagonists of Neurokinin 1 receptors, methods of making these compounds and preparing.Type: GrantFiled: August 3, 2001Date of Patent: August 3, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Thierry Godel, Torsten Hoffmann, Patrick Schnider, Heinz Stadler
-
Patent number: 6762226Abstract: Polyoxymethylene, blends of polycarbonate with acrylonitrile-butadiene-styrene terpolymer, and coatings based on a functional acrylate resin and a crosslinking agent, which are stabilized by addition of a compound of the formula I wherein s is from the range 1 to 8; R1, R2, R3 and R4, independently of each other, are C1-C4alkyl, or R1 and R2 or R3 and R4, together with the carbon atom to which they are bound, form a cyclopentyl or cyclohexyl ring; R5 is hydrogen; C1-C18alkyl; oxyl; OH; CH2CN; C1-C18alkoxy; C5-C12cycloalkoxy; C3-C8alkenyl; C3-C8alkynyl; C7-C12phenylalkyl; C7-C15phenylalkyl, which is substituted on the phenyl ring by 1, 2 or 3 radicals selected from C1-C4alkyl and C1-C4alkoxy; C7-C15phenylalkoxy; C7-C15phenylalkoxy, which is substituted on the phenyl ring by 1, 2 or 3 radicals selected from C1-C4alkyl and C1-C4alkoxy; or R5 is C1-C8alkanoyl; C3-C5alkenoyl; C1-C18alkanoyloxy; glycidyl; or a group —CH2CH(OH)-G, in which G is hydrogen, methyl or phenyl; and A is as descriType: GrantFiled: October 15, 2002Date of Patent: July 13, 2004Assignee: Ciba Specialty Chemicals CorporationInventors: Alessandro Zedda, Graziano Zagnoni, Massimiliano Sala, Dario Lazzari, Stephen Mark Andrews
-
Patent number: 6743915Abstract: A composition of matter has the formula: where n is an integer equal or greater than 1. The composition of matter possesses characteristic absorbance behavior with respect to infrared and visible energy, which is used to detect and determine the concentration of TCE. In another aspect, a method for generating the composition comprises reacting trichloroethylene (TCE) with poly(ethylenimine) in accordance with the formula: where n is an integer equal or greater than 1. Also, the invention sets forth a sensor to detect trichloroethylene (TCE) in materials. The sensor includes the composition of material that can absorb at least one of infrared (IR) or ultraviolet (UV) or visible (VIS) energies when formed by the reaction of trichloroethylene (TCE) with poly(ethylenimine).Type: GrantFiled: August 26, 2002Date of Patent: June 1, 2004Assignee: General Electric CompanyInventors: Timothy Mark Sivavec, Radislav Alexandrovich Potyrailo
-
Publication number: 20040087581Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: 1Type: ApplicationFiled: October 14, 2003Publication date: May 6, 2004Inventors: Charles Alois Dvorak, Lawrence Emerson Fisher, Keena Lynn Green, Ralph New Harris, Hans Maag, Anthony Prince, David Bruce Repke, Russell Stephen Stabler
-
Patent number: 6730783Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: April 22, 2003Date of Patent: May 4, 2004Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan
-
Publication number: 20040082786Abstract: Novel compounds of the general formulae (I) or (II), including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and the compositions are useful in vitro or in vivo for preventing or treating conditions in mammals characterized by undesired thrombosis.Type: ApplicationFiled: October 16, 2003Publication date: April 29, 2004Inventors: Bing-Yan Zhu, Zhaozhong Jon Jia, Penglie Zhang, Wenrong Huang, Yanhong Wu, Jingmei Fan Zuckett, Erik A. Goldman, Lingyan Wang, Younghong Song, Robert M. Scarborough
-
Patent number: 6677336Abstract: Novel compounds of the general formula: and pharmaceutically acceptable acid addition salts thereof, wherein the compounds are useful in therapy to protect skeletal muscles against damage resulting from trauma or to protect skeletal muscles subsequent to muscle or systemic diseases such as intermittent claudication, to treat shock conditions, to preserve donor tissue and organs used in transplants, in the treatment of cardiovascular diseases including atrial and ventricular arrhythmias, Prinzmetal's (variant) angina, stable angina, and exercise induced angina, congestive heart disease, and myocardial infarction.Type: GrantFiled: February 22, 2001Date of Patent: January 13, 2004Assignee: CV Therapeutics, Inc.Inventors: Jeff Zablocki, Elfatih Elzein, Grigory Nudelman, Tim Marquart, Brent K. Blackburn, Venkata P. Palle
-
Publication number: 20030236253Abstract: Thio-alpha-amino acids of general formula (I), wherein R1, R2 and R3 have the meanings given in the description, methods for producing them, and medicaments containing these compounds. The invention also provides methods for treating pain and other diseases using the pharmaceutical compositions comprising the thioamino acids.Type: ApplicationFiled: March 14, 2003Publication date: December 25, 2003Applicant: Gruenenthal GmbHInventors: Boris Chizh, Matthias Gerlach, Michael Haurand, Claudia Puetz, Gero Gaube, D. Enders
-
Publication number: 20030236407Abstract: The invention relates to new, perfluoroalkyl group-containing triiodoaromatic compounds, process for their production, their use as contrast media for x-ray diagnosis as well as for magnetic resonance diagnosis and magnetic resonance spectroscopy by means of fluorine measurement. Subjects of the invention are also diagnostic agents that contain these new compounds.Type: ApplicationFiled: February 28, 2003Publication date: December 25, 2003Applicant: Schering AGInventors: Markus Schafer, Bernd Raduechel, Heribert Miklautz, Franz Maier
-
Publication number: 20030212062Abstract: This invention is directed to morpholinone and morpholine derivatives which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia, sympathetic mediated pain, migraine, and for the treatment of any disease where the antagonism of the &agr;1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: ApplicationFiled: March 11, 2003Publication date: November 13, 2003Applicant: Synaptic Pharmaceutical CorporationInventors: Bharat Lagu, Dhanapalan Nagarathnam, Dake Tian, Charles Gluchowski
-
Patent number: 6642383Abstract: Compounds of the formula (I) wherein p is zero or 1; q and r, independently of each other, are an integer from 1 to 6; and s is a number ranging from 1 to 8; X is —O— or, when p is 1, X is also a group Rw, Rx, Ry and Rz are, independently of each other, C1-C18alkyl, C5-C12cycloalkyl or C1-C5hydroxyalkyl, especially methyl; R1 is hydrogen; C1-C18alkyl; oxyl; OH; CH2CN; C1-C18alkoxy; C5-C12cycloalkoxy; C3-C8alkenyl; C3-C8alkynyl; C7-C12phenylalkyl; C7-C15phenylalkyl, which is substituted on the phenyl ring by 1, 2 or 3 radicals selected from C1-C4alkyl and C1-C4alkoxy; C7-C15phenylalkoxy; C7-C15phenylalkoxy, which is substituted on the phenyl ring by 1, 2 or 3 radicals selected from C1-C4alkyl and C1-C4alkoxy; or R1 is C1-C8alkanoyl; C3-C5alkenoyl; C1-C18alkanoyloxy; glycidyl; or a group —CH2CH(OH)—G, in which G is hydrogen, methyl or phenyl; R2 is hydrogen, C1-C8alkyl, C5-C12cycloalkyl or C1-C4hydroxyalkyl; R3, R4, R5 independently of each otherType: GrantFiled: May 15, 2001Date of Patent: November 4, 2003Assignee: Ciba Specialty Chemicals CorporationInventors: Dario Lazzari, Graziano Zagnoni, Mirko Rossi, Alessandro Zedda, Valerio Borzatta, Stephen Mark Andrews
-
Publication number: 20030204089Abstract: Levorotatory and dextrorotatory enantiomers of 1-[(4-chlorophenyl)phenylmethyl]-4-[(4-methylphenyl)sulfonyl]piperazine of the formula 1Type: ApplicationFiled: March 12, 2003Publication date: October 30, 2003Inventors: Eric Cossement, Guy Bodson, Jean Gobert
-
Patent number: 6638931Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: November 28, 2000Date of Patent: October 28, 2003Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan, Thomas P. Stagnaro
-
Publication number: 20030181464Abstract: A class of phenylsulphonyl derivatives of the following formula (I) wherein Z represents halogen, cyano, nitro, trifluoromethyl, trifluoromethoxy, —Ra, —ORa, —SRa, —SORa, —SO2Ra, —SO2NRaRb, —NRaRb, —NRaCORb, —NRaCO2Rb; —CORa; —CO2Ra or —CONRaRb; or Z represents an optionally substituted five-membered heteroaromatic ring selected from furan, thiophene, pyrrole, oxazole, thiazole, isoxazole, isothiazole, imidazole, pyrazole, oxadiazole, thiadiazole, triazole and tetrazole; or Z represents an optionally substituted six-membered heteroaromatic ring selected from pyridine, pyrazine, pyrimidine and pyridazine; Ra and Rb independently represent hydrogen of C1-6 alkyl, or Ra and Rb, when linked through a nitrogen atom, together represent the residue of an azetidine, pyrrolidine, piperidine or morpholine ring; E represents a chemical bond or a straight or branched alkylene chain containing from 1 to 4 carbon atoms, optionally incorporating an oxygType: ApplicationFiled: April 21, 2003Publication date: September 25, 2003Inventors: Frank Burkamp, Susan Koon-Fung Cheng, Stephen Robert Fletcher
-
Publication number: 20030166616Abstract: Excellent tachykinin receptor antagonistic activity is provided by 2-phenylpiperazine derivatives. The piperazine derivatives exhibit a strong inhibitory action against a tachykinin-induced increase of vascular permeability in in vivo tests. Moreover, the derivatives show a preferred transfer into blood, a long half-life in blood in pharmacokinetic tests of oral administration to rats or guinea pigs, and are very stable in blood plasma of various animals. Consequently, a piperazine derivative of the present invention is very useful as a tachykinin antagonist.Type: ApplicationFiled: February 20, 2003Publication date: September 4, 2003Inventors: Takashi Ogino, Yukari Konishi, Kunihiko Higashiura, Kazuhito Furukawa
-
Publication number: 20030149020Abstract: The present invention relates to substituted bis-arylsulfonamide and arylsulfonamide compounds of the general formula (I) or the formula (II), which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous system.Type: ApplicationFiled: May 13, 2002Publication date: August 7, 2003Inventors: Ulf Bremberg, Patrizia Caldirola, Annika J. Jensen, Gary Johansson, Andrew Mott, Lori Sutin, Jan Tejbrant
-
Publication number: 20030139419Abstract: Compounds of formula (I) useful as metalloproteinase inhibitors, especially as inhibitors of MMP 13.Type: ApplicationFiled: September 27, 2002Publication date: July 24, 2003Inventors: Bernard Barlaam, Robert Dowell, Nicholas John Newcombe, Howard Tucker, David Waterson
-
Publication number: 20030134827Abstract: The present application describes novel lactams and derivatives thereof of formula I: 1Type: ApplicationFiled: March 12, 2002Publication date: July 17, 2003Inventors: Jingwu Duan, Carl P. Decicco, Zelda R. Wasserman, Thomas P. Maduskuie
-
Patent number: 6579881Abstract: A 1,4-substituted cyclic amine derivative represented by the following formula or a pharmacologically acceptable salt thereof: wherein A, B, C, D, T, Y, and Z each represent a methine or a nitrogen linkage; R1, R2, R3, R4, and R5 each represent a substituent; n represents 0 or an integer of 1 to 3; m represents 0 or an integer of 1 to 6; and p represents an integer of 1 to 3. The compounds have serotonin antagonism. They are therefore clinically useful as medicaments, in particular, for treating, ameliorating, and preventing spastic paralysis. They are also useful as central muscle relaxants for ameliorating myotonia.Type: GrantFiled: May 18, 2001Date of Patent: June 17, 2003Assignee: Eisai Co., Ltd.Inventors: Noritaka Kitazawa, Kohshi Ueno, Keiko Takahashi, Teiji Kimura, Atsushi Sasaki, Koki Kawano, Tadashi Okabe, Makoto Komatsu, Manabu Matsunaga, Atsuhiko Kubota
-
Publication number: 20030060473Abstract: A compound of formula (I) wherein A is a sulfonyl or a carbonyl; R1 is an optionally substituted aryl, an optionally substituted heterocyclic group, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; R2 is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; R3 is an optionally substituted lower alkyl, an optionally substituted lower alkoxy, an optionally substituted aryloxy, an optionally substituted lower alkenyl, an optionally substituted aryl, an optionally substituted heterocyclic group or an optionally substituted amino; R4 is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; R5 is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; and R10 is a hydroxy or a protected hydroxy, and a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 3, 2002Publication date: March 27, 2003Applicant: FUJISAWA PHARMACEUTICAL CO., LTD.Inventors: Masahiro Neya, Hitoshi Yamazaki, Natsuko Kayakiri, Kentaro Sato, Teruo Oku
-
Patent number: 6518310Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: March 16, 2001Date of Patent: February 11, 2003Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L Fedde, Carl R Illig, Thomas P. Markotan, Thomas P Stagnaro
-
Patent number: 6515159Abstract: An S,S-ethylenediamine-N,N′-disuccinic acid iron alkali salt which contains a lactam compound represented by the following general formula (1): wherein M is an ammonium ion or an alkali metal ion, and an ethylenediaminemonosuccinic acid represented by the following general formula (2): wherein M is an ammonium ion or an alkali metal ion, in an amount of 7 wt % or less, respectively.Type: GrantFiled: August 17, 2001Date of Patent: February 4, 2003Assignee: Mitsubishi Rayon Co., Ltd.Inventors: Toshitake Yamakawa, Haruo Sakai
-
Patent number: 6509337Abstract: A compound of the formula wherein R1-R9 and Ar are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration, restenosis, periodontal disease, epidemrolysis bullosa, scleritis and other disease characterized by matrix metalloproteinase activity, as well as AIDS, sepsis, septic shock and other diseases involving the production of TNF.Type: GrantFiled: September 17, 1998Date of Patent: January 21, 2003Assignee: Pfizer Inc.Inventors: Anthony Piscopio, James P. Rizzi
-
Patent number: 6498162Abstract: The invention relates to new arylglycinamide derivatives of general formula I and the pharmaceutically acceptable salts thereof, wherein R1 and R2 together with the N to which they are bound form a ring of the formula in which R3, R4, R5, Ar, R6, R7, R8, R9, R10, R11, r, s and t have the meanings given in the specification and the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin) antagonists.Type: GrantFiled: November 1, 2000Date of Patent: December 24, 2002Assignee: Boehringer Ingelheim Pharma KGInventors: Franz Esser, Gerd Schnorrenberg, Kurt Schromm, Horst Dollinger, Birgit Jung, Georg Speck
-
Publication number: 20020193382Abstract: The present invention is to provide a compound or a salt thereof represented by the formula: 1Type: ApplicationFiled: April 24, 2002Publication date: December 19, 2002Inventors: Hiroyuki Tawada, Fumio Itoh, Hiroshi Banno, Zen-Ichi Terashita
-
Publication number: 20020188120Abstract: Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflammatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states.Type: ApplicationFiled: June 28, 2002Publication date: December 12, 2002Applicant: American Cyanamid CompanyInventors: Aranapakam Mudumbai Venkatesan, Jannie Lea Baker
-
Patent number: 6472397Abstract: The compounds represented by the formula (I), and pharmacologically acceptable salts and solvates thereof are disclosed. The compound is hydrolyzed in organisms into a compound represented by the formula in which W represents a hydrogen atom, and D represents the group —V—(CH2)p—COOR, wherein R represents a hydrogen atom. The compound inhibits the aggregation of platelets via the inhibition of the linkage of the platelet membrane protein GPIIb/IIIa to fibrinogen. wherein A represents CH2 or CO, B represents the group —(CH2)k— or —(CH2)m—CO—, X and Y are different from each other and represent N or CH, W represents an ester moiety which can be removed under the physiological condition, and Z represents the groups (II) or (III): wherein D represents the group —V—(CH2)p—COOR.Type: GrantFiled: November 3, 2000Date of Patent: October 29, 2002Assignee: Meiji Seika Kaisha, Ltd.Inventors: Kazumi Ota, Kazuko Kobayashi, Tomoaki Miura, Takahiro Imai, Kazumasa Aizawa, Hisashi Suzuki, Shokichi Ohuchi, Kiyoaki Katano, Takashi Ando
-
Patent number: 6448243Abstract: A novel 1,4-substituted cyclic amine derivative represented by the following formula or a pharmacologically acceptable salt thereof: (wherein A, B, C, D, T, Y and Z represent each methine or nitrogen; R1, R2, R3, R4 and R5 represent each a substituent; n represents 0 or an integer of 1 to 3; m represents 0 or an integer of 1 to 6; and p represents an integer of 1 to 3.) The compound has a serotonin antagonism and is clinically useful as medicament, in particular, for treating, ameliorating and preventing spastic paralysis or central muscle relaxants for ameliorating myotonia.Type: GrantFiled: August 11, 1999Date of Patent: September 10, 2002Assignee: Eisai Co., Ltd.Inventors: Noritaka Kitazawa, Kohshi Ueno, Keiko Takahashi, Teiji Kimura, Atsushi Sasaki, Koki Kawano, Tadashi Okabe, Makoto Komatsu, Manabu Matsunaga, Atsuhiko Kubota
-
Patent number: 6441172Abstract: The synthesis of individual di- and tri-substituted-1,4-diazacyclic compounds having 6- to 8-atoms in the cyclic ring, their corresponding 1,6-diketo-2,5-diazacyclic compounds and similar 1,4-diazacyclic ring compounds having one ring carbonyl group and 6-8 atoms in the ring is disclosed, as are libraries of such compounds. Methods of preparing and using the libraries of compounds as well as individual compounds of the libraries are also disclosed.Type: GrantFiled: May 12, 1999Date of Patent: August 27, 2002Assignee: Torrey Pines Institute for Molecular StudiesInventors: Adel Nefzi, John M. Ostresh, Richard A. Houghten
-
Publication number: 20020082263Abstract: Compounds having the structure 1Type: ApplicationFiled: December 11, 2000Publication date: June 27, 2002Inventors: Boliang Lou, Adnan M.M. Mjalli
-
Patent number: 6387389Abstract: The present invention provides sustained-release derivatives of hydroxylated analogs of substituted 1-[2[bis(aryl)methoxy]ethyl]-piperazines and -homopiperazines, pharmaceutical compositions comprising the same, and a method of using such sustained-release derivatives to bind the dopamine transporter to achieve a desired effect, such as antagonism of dopamine reuptake inhibitors, such as cocaine, or dopamine releasers or norepinephrine and/or serotonin reuptake inhibitors, such as methamphetamine.Type: GrantFiled: June 30, 1999Date of Patent: May 14, 2002Assignee: The United States of America as represented by the Secretary of the Department of Health and Human ServicesInventors: Richard B. Rothman, Kenner C. Rice, David Lewis, Dorota Matecka, John R. Glowa
-
Patent number: 6376428Abstract: The dihalopropene compounds of the general formula [I] have excellent insecticidal/acaricidal activity, so that they are satisfactorily effective for the control of noxious insects, mites and ticks.Type: GrantFiled: May 25, 2001Date of Patent: April 23, 2002Assignee: Sumitomo Chemical Company, LimitedInventors: Noriyasu Sakamoto, Sanshiro Matsuo, Masaya Suzuki, Taro Hirose, Kazunori Tsushima, Kimitoshi Umeda
-
Patent number: 6369063Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: April 13, 1998Date of Patent: April 9, 2002Assignee: Cor Therapeutics, Inc.Inventors: Ting Su, Bing-Yan Zhu, Robert M. Scarborough
-
Patent number: 6369225Abstract: Compounds having Formula 8 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.Type: GrantFiled: August 29, 2000Date of Patent: April 9, 2002Assignee: Allergan Sales, Inc.Inventors: Jayasree Vasudevan, Alan T. Johnson, Dehua Huang, Roshantha A. Chandraratna
-
Publication number: 20020032186Abstract: Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflmatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states.Type: ApplicationFiled: July 3, 2001Publication date: March 14, 2002Applicant: American Cyanamid CompanyInventors: Aranapakam Mudumbai Venkatesan, Jannie Lea Baker, Jeremy Ian Levin
-
Patent number: 6316623Abstract: Libraries of ethylenediamine compounds having the general formula (I): wherein R1 to R6, m, n, o and p are as defined herein, are prepared using solid phase combinatorial chemistry techniques. A heterocyclic alcohol is reacted with an ethylenediamine bound to a solid support to give a scaffold having sites of diversity. Libraries of the invention are useful for screening in biological assays in order to identify pharmaceutically useful compounds.Type: GrantFiled: August 21, 1998Date of Patent: November 13, 2001Assignee: ISIS Pharmaceuticals, Inc.Inventors: Eric Edward Swayze, Elizabeth Anne Campbell Jefferson
-
Patent number: 6300510Abstract: An S,S-ethylenediamine-N,N′-disuccinic acid iron alkali salt which contains a lactam compound represented by the following general formula (1): wherein M is an ammonium ion or an alkali metal ion, and an ethylenediaminemonosuccinic acid represented by the following general formula (2): wherein M is an ammonium ion or an alkali metal ion, in an amount of 7 wt % or less, respectively.Type: GrantFiled: April 28, 2000Date of Patent: October 9, 2001Assignee: Mitsubishi Rayon Co., Ltd.Inventors: Toshitake Yamakawa, Haruo Sakai
-
Patent number: 6288038Abstract: The present invention provides a new depsipeptide derivative having a piperazinone ring within the molecule which is represented by formula (1) wherein X1 represents N(R4)—CO, N(R5)—CH2, CH2—CO, CH2—CH2, CH═CH, CH2—CH(OH) or CH(OH)—CH(OH), R1 represents a C5-C20 alkyl group or a C5-C15 alkoxy C1-C4 alkyl group, R2-R5 represent a hydrogen atom or a C1-C6 alkyl group, and A represents a group of formula (2), (3) or (4) The depsipeptide derivative has a function of accelerating the production of apolipoprotein E and is useful as an agent for the treatment of neurologic injury, an agent for the treatment of dementia and an antihyperlipidemic agent.Type: GrantFiled: April 3, 2000Date of Patent: September 11, 2001Assignee: Nisshin Seifun Group Inc.Inventors: Makoto Yanai, Masashi Suzuki, Norio Oshida, Koji Kawamura, Shigeru Hiramoto, Orie Yasuda, Nobuhiro Kinoshita, Akiko Shingai, Masako Takasu
-
Patent number: 6274584Abstract: Novel peptide derivatives, compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone are disclosed. The peptides have the formula (1): wherein a, b, A, R1, L1, D, R3, R4, R2, L2, E and G are as defined in the specification. These peptides exhibit improved resistance to proteolytic degradation, and hence, improved bioavailability.Type: GrantFiled: July 19, 2000Date of Patent: August 14, 2001Assignee: Novo Nordisk A/SInventors: Bernd Peschke, Michael Ankersen, Thomas Kruse Hansen, Henning Thøgersen
-
Patent number: 6235778Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R114 R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and mare set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: November 26, 1997Date of Patent: May 22, 2001Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan, Thomas P. Stagnaro
-
Patent number: 6211183Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: April 13, 1998Date of Patent: April 3, 2001Assignee: COR Therapeutics, Inc.Inventors: Charles K. Marlowe, Bing-Yan Zhu, Robert M. Scarborough