Ring Oxygen In The Tricyclo Ring System Patents (Class 546/89)
Plural ring oxygens in the tricyclo ring system (Class 546/90)
Tropane and oxirane in the tricyclo ring system (Class 546/91)
Plural chalcogens bonded directly to ring carbons of the tricyclo ring system (Class 546/92)
  • Process of Producing Bleach Boosters
    Publication number: 20080214819
    Abstract: This invention relates to a process of producing compounds, which are useful as bleach boosters, as well as to the compounds, which are obtainable using said process, and to their use.
    Type: Application
    Filed: June 14, 2006
    Publication date: September 4, 2008
    Applicant: BASF Aktiengesellschaft
    Inventors: Ludwig Volkel, Christian Bittner, Ingo Munster, Frank Dietsche, Wolfgang Schrof
  • Substituted Tetrahydroquinolines
    Publication number: 20080194615
    Abstract: Disclosed are compounds of formula (I), wherein W, R, R1, R2, R3, R4, R5, R6, and R7 have the meanings indicated in claim 1. Said compounds can be used for the treatment of tumors, among other things.
    Type: Application
    Filed: May 17, 2006
    Publication date: August 14, 2008
    Applicant: Merck Patent GmbH
    Inventors: Kai Schiemann, Ulrich Emde, Dirk Finsinger, Christiane Amendt, Nina Heiss, Frank Zenke
  • CCR1 antagonists and methods of use therefor
    Publication number: 20080139602
    Abstract: The invention provides compounds having the formula: wherein R1 is halogen. The invention also provides compositions comprising the compounds, and methods of treating diseases or disorders that comprise administering one or more of the compounds to a subject in need thereof. The disclosed compounds have CCR1 antagonist activity.
    Type: Application
    Filed: September 13, 2007
    Publication date: June 12, 2008
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Kenneth G. Carson, Geraldine C. B. Harriman, Shomir Ghosh
  • Azabicycloalkane compounds
    Patent number: 7358244
    Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity. Such compounds are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.
    Type: Grant
    Filed: May 27, 2004
    Date of Patent: April 15, 2008
    Assignee: Theravance, Inc.
    Inventors: Mathai Mammen, Adam Hughes
  • Method for stabilizing arylcarboxylic acid, stabilizer thereof and aqueous solution containing stabilized arylcarboxylic acid
    Patent number: 7320985
    Abstract: A method for stabilizing an arylcarboxylic acid, which comprises adding a heterocyclic base to the arylcarboxylic acid or a pharmacologically acceptable salt thereof, a stabilizer thereof and an aqueous solution containing a stabilized arylcarboxylic acid. According to the stabilization method of the present invention, arylcarboxylic acid and pharmacologically acceptable salts thereof, particularly pranoprofen, can be stabilized at every temperature range, particularly at lower temperatures, thereby making the production of an aqueous solution to be used as an eye drop, nasal drop, ear drop and the like possible.
    Type: Grant
    Filed: July 23, 2003
    Date of Patent: January 22, 2008
    Assignee: Senju Pharmaceutical Co., Ltd.
    Inventor: Shirou Sawa
  • Opioid receptor antagonists
    Patent number: 7288543
    Abstract: A compound of the formula (I) (I) wherein the variables X1 to X6, Ra, Rb, R1 to R7 including R3?, E, p, j, y, z, A, B and C are as described or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases is disclosed
    Type: Grant
    Filed: March 8, 2005
    Date of Patent: October 30, 2007
    Assignee: Eli Lilly and Company
    Inventors: Howard Barff Broughton, Nuria Diaz Buezo, Charles Howard Mitch, Concepcion Pedregal-Tercero
  • Chemokine receptor antagonists and methods of use thereof
    Patent number: 7271176
    Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation.
    Type: Grant
    Filed: November 13, 2002
    Date of Patent: September 18, 2007
    Assignees: Millennium Pharmaceuticals, Inc., Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Jay R. Luly, Yoshisuke Nakasato, Etsuo Ohshima, Geraldine C. B. Harriman, Kenneth G. Carson, Shomir Ghosh, Amy M. Elder, Karen M. Mattia
  • Synthesis of cyclopentadiene derivatives
    Patent number: 7253292
    Abstract: A process for preparing cyclopentadiene derivatives comprising the steps of: a) coupling a five membered heterocycle ring with a five or six membered heterocycle ring; b) reacting the obtained compound with a carbonilating system: c) reducing the obtained compound.
    Type: Grant
    Filed: May 8, 2002
    Date of Patent: August 7, 2007
    Assignee: Basell Polyolefine GmbH
    Inventors: Ilya E. Nifant'ev, Igor A Kashulin, Pavel V. Ivchenko, Peter A. A. Klusener, Frans M. Kornorffer, Kees P. De Kloe, Jos J. H. Rijsemus
  • Methods for synthesizing heterocycles and therapeutic use of the heterocycles for cancers
    Patent number: 7250423
    Abstract: The present invention provides methods for synthesizing novel tetrahydroquinoline derivatives that are useful for cancer chemotherapy and anti-viral applications. The present invention provides compounds useful for cancer chemotherapy and methods for the preparation of these compounds. The present invention also includes cancer chemotherapy methods.
    Type: Grant
    Filed: September 24, 2002
    Date of Patent: July 31, 2007
    Inventors: Chao-Jun Li, Jianheng Zhang
  • Tiotropium-containing pharmaceutical combination for inhalation
    Patent number: 7250426
    Abstract: The present invention relates to new pharmaceutical compositions for inhalation containing one or more, preferably one, tiotropium salt combined with one or more pharmacologically acceptable acid addition salts of a compound of formula 2?, wherein the groups R1, R2, R3 and R4 may have the meanings given in the claims and in the specification, processes for preparing them and their use in the treatment of respiratory complaints.
    Type: Grant
    Filed: November 19, 2003
    Date of Patent: July 31, 2007
    Assignee: Boehringer Ingelheim Pharma GmbH & Co KG
    Inventors: Ingo Konetzki, Christopher J. Montague Meade, Michel Pairet, Michael P. Pieper
  • Pyridyl alkene and pyridyl alkine acid amides as cytostatics and immunosupressives
    Patent number: 7241745
    Abstract: The invention relates to a new pyridyl alkene and pyridyl alkine acid amides according to the general formula (I) as well as methods for their production, medicaments containing these compounds as well as their medical use, especially in the treatment of tumors or for immunosuppression.
    Type: Grant
    Filed: August 5, 2002
    Date of Patent: July 10, 2007
    Assignee: Astellas Pharma GmbH
    Inventors: Elfi Biedermann, Max Hasmann, Roland Löser, Benno Rattel, Friedemann Reiter, Barbara Schein, Klaus Seibel, Klaus Vogt
  • Quinoline 3-amino chroman derivatives
    Patent number: 7227023
    Abstract: Quinoline 3-amino chroman derivatives and compositions containing such compounds are disclosed. Methods for using the quinoline 3-amino chroman derivatives and compositions containing such compounds in the treatment of serotonin disorders are disclosed. Also disclosed are processes for preparing quinoline 3-amino chroman derivatives.
    Type: Grant
    Filed: April 29, 2004
    Date of Patent: June 5, 2007
    Assignee: Wyeth
    Inventors: Nicole Theriault Hatzenbuhler, Dahui Zhou, Gary Paul Stack, Jonathan Laird Gross
  • Chemokine receptor antagonists and methods of use thereof
    Patent number: 7186729
    Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation.
    Type: Grant
    Filed: November 13, 2002
    Date of Patent: March 6, 2007
    Assignees: Millennium Pharmaceuticals, Inc., Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Jay R. Luly, Yoshisuke Nakasato, Etsuo Ohshima, Geraldine C. B. Harriman, Kenneth G. Carson, Shomir Ghosh, Amy M. Elder, Karen M. Mattia
  • Derivatives of 1,2-dihydro-7-hydroxyquinolines containing fused rings
    Patent number: 7169922
    Abstract: The present invention describes novel dyes, including coumarins, rhodamines, and rhodols that incorporate additional fused aromatic rings. The dyes of the invention absorb at a longer wavelength than structurally similar dyes that do not possess the fused aromatic rings. Many of the dyes of the invention are useful fluorescent dyes. The invention includes chemically reactive dyes, dye-conjugates, and the use of such dyes in staining samples and detecting ligands or other analytes.
    Type: Grant
    Filed: November 13, 2003
    Date of Patent: January 30, 2007
    Assignee: Invitrogen Corporation
    Inventors: Zhenjun Diwu, Jixiang Liu, Kyle Gee
  • 4-phenyl substituted tetrahydroisoquinolines therapeutic use thereof
    Patent number: 7084152
    Abstract: Compounds are provided that, by way of their selective neurotransmitter binding useful for the treatment of various neurological and psychological disorders, e.g., ADHD. Such compounds are 4-phenyl substituted tetrahydroisoquinolines having the Formula IA, IB, IIA, IIB, IIIA or IIIC as set forth herein.
    Type: Grant
    Filed: July 11, 2001
    Date of Patent: August 1, 2006
    Assignee: AMR Technology, Inc.
    Inventors: James P. Beck, Anthony D. Pechulis, Arthur E. Harms
  • Tetrahydroquinoline derivatives
    Patent number: 7037919
    Abstract: Tetrahydroquinoline derivatives of general formula (I) or salts thereof, having a specific and strong binding affinity for AR and exhibiting AR agonism or antagonism; and pharmaceutical compositions containing the derivatives or the salts.
    Type: Grant
    Filed: October 6, 2000
    Date of Patent: May 2, 2006
    Assignee: Kaken Pharmaceutical Co. Ltd.
    Inventors: Keigo Hanada, Kazuyuki Furuya, Kiyoshi Inoguchi, Motonori Miyakawa, Naoya Nagata
  • Antidepressant azahetorocyclylmethyl derivatives of 7,8-dihydro-6H-5-oxa-1-aza-phenathrene
    Patent number: 7030245
    Abstract: Compounds of the formula useful for the treatment of such as depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder (including trichotillomania), social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa, bulimia nervosa, vasomotor flushing, cocaine and alcohol addition, sexual dysfunction (including premature ejaculation), and related illnesses.
    Type: Grant
    Filed: June 6, 2005
    Date of Patent: April 18, 2006
    Assignee: Wyeth
    Inventors: Rulin Zhao, Megan Tran, Gary P. Stack, Richard E. Mewshaw
  • Tricyclic androgen receptor modulator compounds and methods
    Patent number: 7026484
    Abstract: This invention relates to non-steroidal tricyclic compounds that are modulators of androgen receptors and to methods for making and using such compounds.
    Type: Grant
    Filed: February 22, 2002
    Date of Patent: April 11, 2006
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Lin Zhi, Cornelis Arjan Van Oeveren, Jyun-Hung Chen, Robert I. Higuchi
  • Fluorenecarboxylic acid esters, process for the manufacture thereof, and use thereof as medicaments
    Patent number: 6998406
    Abstract: Fluorenecarboxylic acid esters of general formula 1 wherein X? and the groups A, R, R1, R2, R3, R3?, R4, and R4? have the meanings given in the claims and in the specification, processes for the manufacture thereof and the use thereof as medicaments.
    Type: Grant
    Filed: August 9, 2004
    Date of Patent: February 14, 2006
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Sabine Germeyer, Helmut Meissner, Gerd Morschhaeuser, Sabine Pestel, Michael P. Pieper, Gerald Pohl, Richard Reichl, Georg Speck
  • Thieno[2,3-c]iosquinolines for use as inhibitors of PARP
    Patent number: 6989388
    Abstract: The present invention relates to compounds for the inhibition of poly(ADP-ribose) polymerase (PARP). In some embodiments, the compounds have the Formula: wherein the constituent variables are as defined herein. The invention further provides methods for the use of the compounds disclosed herein.
    Type: Grant
    Filed: October 30, 2001
    Date of Patent: January 24, 2006
    Inventors: Roberto Pellicciari, Flavio Moroni
  • Process for preparation of amidine derivatives
    Patent number: 6987187
    Abstract: A process for producing amidine derivatives represented by the following reaction scheme, characterized in that the reactions of steps 1 and 3 are conducted in acetonitrile and the reaction of step 2 is conducted in acetone.
    Type: Grant
    Filed: July 15, 2002
    Date of Patent: January 17, 2006
    Assignee: Shionogi & Co., Ltd.
    Inventors: Toshiaki Masui, Kyozo Kawata, Takayuki Kasai, Makoto Kakinuma
  • Furoisoquinoline derivatives, process for producing the same and use thereof
    Patent number: 6924292
    Abstract: A compound having a partial structure represented by Formula: or a salt thereof has an excellent phosphodiesterase (PDE) IV-inhibiting effect, and is useful as a prophylactic or therapeutic agent against inflammatory diseases, for example, bronchial asthma, chronic obstructive pulmonary disease (COPD), rheumatoid arthritis, autoimmune disease, diabetes and the like.
    Type: Grant
    Filed: March 22, 2001
    Date of Patent: August 2, 2005
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Yasuhiko Kawano, Tatsumi Matsumoto, Osamu Uchikawa, Nobuhiro Fujii, Naoki Tarui
  • Azabicyclic-substituted fused-heteroaryl compounds for the treatment of disease
    Patent number: 6911543
    Abstract: The invention provides compounds of Formula I: wherein Azabicyclo is These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals in which ?7 is known to be involved.
    Type: Grant
    Filed: October 1, 2002
    Date of Patent: June 28, 2005
    Assignee: Pfizer Inc.
    Inventors: Daniel Patrick Walker, David W. Piotrowski, Eric Jon Jacobsen, Brad A. Acker, Donn G. Wishka, Steven Charles Reitz
  • Crystalline tiotropium bromide monohydrate, processes for the preparation thereof, and pharmaceutical compositions
    Patent number: 6908928
    Abstract: Crystalline monohydrate of (1?,2?,4?,5?,7?)-7-[(hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonane bromide (tiotropium bromide monohydrate), processes for the preparation thereof, pharmaceutical compositions thereof, and their use.
    Type: Grant
    Filed: September 24, 2001
    Date of Patent: June 21, 2005
    Assignee: BI Pharma KG.
    Inventors: Rolf Banholzer, Peter Sieger, Christian Kulinna, Michael Trunk, Manfred Graulich, Peter Specht, Helmut Meissner, Andreas Mathes
  • Method of making tricyclic aminocyanopyridine compounds
    Patent number: 6909001
    Abstract: A method of making aminocyanopyridine compounds which are capable of inhibiting mitogen activated protein kinase-activated protein kinase-2 is described.
    Type: Grant
    Filed: December 5, 2003
    Date of Patent: June 21, 2005
    Assignee: Pharmacia Corporation
    Inventors: David R. Anderson, Shridhar G. Hegde, Stephen A. Kolodziej, William F. Vernier, Emily J. Reinhard
  • Antidepressant azaheterocyclylmethyl derivatives of 7,8-dihydro-6H-5-oxa-1-aza-phenanthrene
    Patent number: 6903110
    Abstract: Compounds of the formula useful for the treatment of such as depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as premenstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder (including trichotillomania), social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa, bulimia nervosa, vasomotor flushing, cocaine and alcohol addition, sexual dysfunction (including premature ejaculation), and related illnesses.
    Type: Grant
    Filed: July 24, 2002
    Date of Patent: June 7, 2005
    Assignee: Wyeth
    Inventors: Rulin Zhao, Megan Tran, Gary P. Stack, Richard E. Mewshaw
  • Polymorph forms of N-(2,3-dimethyl-5,6,7,8-tetrahydrofuro[2,3-B]quinolin-4-YL)-2-(2-oxopyrrolidin-1-YL)acetamide
    Patent number: 6884805
    Abstract: The invention relates to novel polymorph crystal forms A and B of N-(2,3-dimethyl-5,6,7,8-tetrahydrofuro[2,3-b]quinolin-4-yl)-2-(2-oxopyrrolidin-1-yl)acetamide: The compounds and pharmaceutical compositions thereof are useful for activating a malfunctioned cholinergic neuron that is associated with memory loss disturbances.
    Type: Grant
    Filed: April 19, 2002
    Date of Patent: April 26, 2005
    Assignee: Mitsubishi Pharma Corporation
    Inventors: Haruko Yamabe, Takayuki Ishige
  • Process for preparing chiral diol sulfones and dihydroxy acid HMG CoA reductase inhibitors
    Patent number: 6875867
    Abstract: A process is provided for preparing chiral diol sulfones of the structure where R3 is preferably where R4a is preferably aryl such as phenyl, and R1a is preferably alkyl such as t-butyl, which are intermediates used in preparing HMG CoA reductase inhibitors.
    Type: Grant
    Filed: May 30, 2002
    Date of Patent: April 5, 2005
    Assignee: Bristol-Myers Squibb Company
    Inventors: Paul R. Brodfuehrer, Thomas R. Sattelberg, Joydeep Kant, Xinhua Qian
  • Benzo[4,5]thieno[2,3-c]pyridine and Benzo[4,5]furo[2,3-c]pyridine Derivatives Useful as Inhibitors of Phosphodiesterase
    Patent number: 6864253
    Abstract: The present invention relates to novel ?-carboline derivatives of the general formula wherein all the variables are as described within the specification, useful as phosphodiesterase inhibitors. The present invention further relates to use of the described derivatives for the treatment of diseases and conditions related to PDE, for example male erectile dysfunction.
    Type: Grant
    Filed: October 1, 2002
    Date of Patent: March 8, 2005
    Assignee: Orth-McNeil Pharmaceutical, Inc.
    Inventors: Zhihua Sui, Mark J. Macielag
  • HMG-CoA reductase inhibitors and method
    Patent number: 6812345
    Abstract: Compounds of the following structure are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids such as lowering LDL cholesterol and/or increasing HDl cholesterol, and treating hyperlipidemia, hypercholesterolemia, hypertriglyceridemia and atherosclerosis and pharmaceutically acceptable salts thereof, wherein X is O, S, SO, SO2 or NR7; Z is n is 0 or 1; R1 and R2 are the same or different and are independently selected from alkyl, arylalkyl, cycloalkyl, alkenyl, cycloalkenyl, aryl, heteroaryl or cycloheteroalkyl; and R3 to R10 are as defined herein.
    Type: Grant
    Filed: June 24, 2003
    Date of Patent: November 2, 2004
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jeffrey A. Robl, Bang-Chi Chen, Chong-Qing Sun
  • Fluorenecarboxylic acid esters, process for the manufacture thereof, and use thereof as medicaments
    Patent number: 6790856
    Abstract: Flourenecarboxylic acid esters of general formula 1 wherein X− and the groups A, R, R1, R2, R3, R3′, R4, and R4′ have the meanings given in the claims and in the specification, processes for the manufacture thereof and the use thereof as medicaments.
    Type: Grant
    Filed: January 2, 2003
    Date of Patent: September 14, 2004
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Sabine Germeyer, Helmut Meissner, Gerd Morschhaeuser, Sabine Pestel, Michael P. Pieper, Gerald Pohl, Richard Reichl, Georg Speck
  • Crystalline tiotropium bromide monohydrate, processes for the preparation thereof, and pharmaceutical compositions
    Patent number: 6777423
    Abstract: Crystalline monohydrate of (1&agr;,2&bgr;,4&bgr;,5&agr;,7&bgr;)-7-[(hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonane bromide (tiotropium bromide monohydrate), processes for the preparation thereof, pharmaceutical compositions thereof, and their use.
    Type: Grant
    Filed: January 30, 2003
    Date of Patent: August 17, 2004
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Rolf Banholzer, Peter Sieger, Christian Kulinna, Michael Trunk, Manfred Graulich, Peter Specht, Helmut Meissner, Andreas Mathes
  • Therapeutic compounds
    Patent number: 6762191
    Abstract: The present invention provides compounds of formula (I): wherein: R1, R2, R3 R4, R5, R6, X, - - - , m, and n have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds or salts thereof. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of formula (I). The compounds are useful as 5-HT ligands.
    Type: Grant
    Filed: June 25, 2002
    Date of Patent: July 13, 2004
    Assignee: Pharmacia & Upjohn Company
    Inventors: William W. McWhorter, Jr., Valentina Badescu
  • Stable near-infrared (NIR) marker dyes based on benzopyrylium-polymethines
    Patent number: 6750346
    Abstract: The disclosure is directed to so-called laser-compatible NIR marker dyes based on polymethines for use in optical, in particular, fluorescence optical determination and detection methods, for example, in the fields of medicine, pharmaceutics and in the areas of life science, materials science and environmental science. The disclosure further discusses the aim of the invention which was to create NIR marker dyes based on polymethine which have a high degree of photostability and stability in storage as well as a high fluorescent yield and which can be excited to fluorescence in the easiest possible manner by means of laser radiation in the visible or NIR spectral range, particularly with light of an argon, helium/neon, or diode laser. Dyes based on polymethine of general formula (I) are used.
    Type: Grant
    Filed: January 22, 2002
    Date of Patent: June 15, 2004
    Assignee: Carl Zeiss Jena GmbH
    Inventors: Peter Czerney, Frank Lehmann, Bernd Schweder, Matthias Wenzel
  • 4-Anilino[2,3-b]quinoline derivatives, their preparation processes and pharmaceutical compositions comprising the same
    Patent number: 6750223
    Abstract: Disclosed herein are 4-anilino[2,3-b]quinoline derivatives of formula (I): wherein each of R1, R2, R3 and Y is given the definition as set forth in the Specification and Claims. These compounds of formula (I) have been found to have the ability to inhibit growth of a variety of tumor/cancer cells, especially leukemia, colon, melanoma and breast cancer cells. Also, disclosed are preparation processes of these compounds of formula (I) and pharmaceutical compositions comprising said compositions of formula (I).
    Type: Grant
    Filed: September 12, 2002
    Date of Patent: June 15, 2004
    Assignee: Kaohsiung Medical University
    Inventor: Cherng-Chyi Tzeng
  • CCR1 antagonists and methods of use therefor
    Publication number: 20040106639
    Abstract: The invention provides compounds having the formula: 1
    Type: Application
    Filed: November 12, 2003
    Publication date: June 3, 2004
    Applicant: Millennium Pharmaceuticals
    Inventors: Kenneth G. Carson, Geraldine C.B. Harriman
  • Cyclic hydroxamic acids as inhibitors of matrix metalloproteinases and/or TNF- &agr; converting enzyme (TACE)
    Patent number: 6740649
    Abstract: The present application describes novel cyclic hydroxamic acids of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from 0-2 heteroatoms selected from O, N, NR1, and S(O)p, and 0-1 carbonyl groups and the other variables are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-&agr; converting enzyme (TACE), aggrecanase or a combination thereof, pharmaceutical compositions containing the same, and methods of using the same.
    Type: Grant
    Filed: September 16, 2002
    Date of Patent: May 25, 2004
    Assignee: Bristol-Myers Squibb Company
    Inventors: Gregory R. Ott, Xiao-Tao Chen, Jingwu Duan, Zhonghui Lu
  • Fluorescent lanthanide chelates
    Patent number: 6740756
    Abstract: The present invention provides complexing agents of Formula I which contain novel photosensitizers and produce long-lived fluorescence for use in bioaffinity assays, especially HTRF (homogeneous time-resolved fluorescence) assays.
    Type: Grant
    Filed: June 20, 2001
    Date of Patent: May 25, 2004
    Assignee: SmithKline Beecham Corporation
    Inventors: George Wai-Kin Chan, Robert P. Hertzberg
  • Hydroxamic and carboxylic acid derivatives
    Patent number: 6734189
    Abstract: The invention relates to hydroxamic and carboxylic acid derivatives. Compounds of the formula: are disclosed. These compounds are useful for the treatment of diseases mediated by inhibitors of matrix metalloproteinase, ADAM, ADAM-TS enzymes, and/or TNF&agr;-mediated diseases including degenerative diseases and certain cancers.
    Type: Grant
    Filed: September 6, 2002
    Date of Patent: May 11, 2004
    Assignee: Darwin Discovery, Ltd.
    Inventors: Duncan Batty, Verity Margaret Sabin, Robert John Watson, Hazel Joan Dyke, Andrew Sharpe, Richard John Davenport, David Alan Owen, Andrew Douglas Baxter
  • Spiro compounds
    Patent number: 6723847
    Abstract: The present invention is directed to novel spiro compounds useful as neuropeptide Y receptor antagonists.
    Type: Grant
    Filed: June 4, 2003
    Date of Patent: April 20, 2004
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Takehiro Fukami, Akio Kanatani, Akane Ishihara, Yasuyuki Ishii, Toshiyuki Takahashi, Yuji Haga, Toshihiro Sakamoto, Takahiro Itoh
  • Compounds useful in the treatment of conditions mediated by peroxisome proliferator-activated receptors (PPAR)
    Patent number: 6723731
    Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, Ar, X, Q, A, Y and Z are as defined in the specification. These compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).
    Type: Grant
    Filed: April 13, 2001
    Date of Patent: April 20, 2004
    Assignees: Novo Nordisk A/S, Dr. Reddy's Research Foundation
    Inventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
  • Somatostatin antagonists and agonists that act at the SST subtype 2 receptor
    Patent number: 6720330
    Abstract: Compounds according to the formula A—Z—W as herein described, wherein A is selected from the groups consisting of: A′—(CH2)n—, A′—(CH2)nSO2—, and A′—(CH2)nCO—, where n is 0 to 4; and A′ is selected from (a) (C6-C10)aryl-, or (b) (C1-C9)heteroaryl-; which groups may be optionally substituted; and pharmaceutically acceptable salts, solvates or hydrates thereof; pharmaceutical compositions thereof; and methods useful to facilitate secretion of growth hormone(GH) in mammals.
    Type: Grant
    Filed: September 17, 2001
    Date of Patent: April 13, 2004
    Assignee: Pfizer Inc.
    Inventors: Bruce A. Hay, Bridget M. Cole, Anthony P. Ricketts
  • Process for stereoselective synthesis of 2-hydroxymethyl chromans
    Patent number: 6700001
    Abstract: A process for the stereoselective synthesis of 2-hydroxymethyl-chromans of formula (II) is provided where R, R1, R2 and R3 are as defined herein. The compound of formula (II) is prepared using an optically active benzene compound of formula (I) where R0 is as defined herein. The 2-hydroxymethyl-chroman compounds of formula (II) are useful as intermediates for preparing a variety of medicinal agents.
    Type: Grant
    Filed: October 4, 2002
    Date of Patent: March 2, 2004
    Assignee: Wyeth
    Inventors: Jonathan L. Gross, Gary P. Stack
  • Substituted 1,2,3,4-tetrahydroquinoline-2-carboxylic acid derivatives
    Patent number: 6699877
    Abstract: A substituted 1,2,3,4-tetrahydroquinoline-2-carboxylic acid derivative of formula I and salts thereof with pharmaceutically acceptable acids. Also disclosed are methods for making the derivative, and pharmaceutical compositions comprising the derivative. Methods for treating pain, migraine, and various other diseases using the pharmaceutical composition are also disclosed.
    Type: Grant
    Filed: August 7, 2002
    Date of Patent: March 2, 2004
    Assignee: Gruenenthal GmbH
    Inventors: Matthias Gerlach, Michael Przewosny, Werner Englberger, Elke Reissmueller, Petra Bloms-Funke, Corinna Maul, Utz-Peter Jagusch
  • Oxazolo, thiazolo and selenazolo [4,5-c]-quinolin-4-amines and analogs thereof
    Patent number: 6677334
    Abstract: Thiazolo-, oxazolo- and selenazolo[4,5-c]quinolin-4-amines and analogs thereof are described including methods of manufacture and the use of novel intermediates. The compounds are immunomodulators and induce cytokine biosynthesis, including interferon and/or tumor biosynthesis, necrosis factor, and inhibit the T-helper-type 2 immune response. The compounds are further useful in the treatment of viral and neoplastic diseases.
    Type: Grant
    Filed: September 12, 2002
    Date of Patent: January 13, 2004
    Assignee: 3M Innovative Properties Company
    Inventors: John F. Gerster, Kyle J. Lindstrom, Gregory J. Marszalek, Bryon A. Merrill, John W. Mickelson, Michael J. Rice
  • Tricyclic compounds having sPLA2-inhibitory activities
    Patent number: 6673781
    Abstract: The present invention provides a compound having sPLA2 inhibiting activity. The compound represented by the formula (I): wherein R1 is (a) C1 to C20 alkyl, C2 to C20 alkenyl, C2 to C20 alkynyl, carbocyclic groups, heterocyclic groups or the like; R2 is CONH2 or CONHNH2; one of R3 and R4 is —(L2)-(acidic group) wherein L2 is a group connecting with an acid group and the length of the connecting groups 1 to 5 atoms, and the other is a hydrogen atom; its prodrug, their pharmaceutically acceptable salt, or solvate thereof.
    Type: Grant
    Filed: February 1, 2002
    Date of Patent: January 6, 2004
    Assignee: Shionogi & Co., Ltd.
    Inventors: Mitsuaki Ohtani, Masahiro Fuji, Tetsuo Okada, Makoto Adachi, Tomoyuki Ogawa
  • 4-anilinofuro [3,2-c] quinoline derivatives, and preparation processes and uses of the same
    Patent number: 6656949
    Abstract: Disclosed herein are novel 4-anilinofuro[3,2-c]quinoline derivatives of formula (I): wherein each of the substituents is given the definition as set forth in the Specification and Claims. Also disclosed are the preparation process of these derivatives, and their uses in the manufacture of pharmaceutical compositions.
    Type: Grant
    Filed: September 12, 2002
    Date of Patent: December 2, 2003
    Assignee: Kaohsiung Medical University
    Inventor: Yeh-Long Chen
  • Tricyclic fused heterocycle compounds, process for preparing the same and use thereof
    Publication number: 20030220360
    Abstract: Compounds represented by formula (1), 1
    Type: Application
    Filed: November 12, 2002
    Publication date: November 27, 2003
    Applicant: Nippon Suisan Kaisha, Ltd., a Japan corporation
    Inventors: Shuji Jinno, Takaaki Okita, Naomi Ohtsuka, Shinya Yamashita, Junichiro Hata, Jiro Takeo
  • Thienopyridine derivatives, their production and use
    Patent number: 6653476
    Abstract: The present invention provides thienopyridine derivatives, which are useful as anti-inflammatory drugs, particularly as remedies for arthritis; processes for producing them, and pharmaceutical compositions containing them. The thienopyridine derivatives are represented by the formula (I): wherein G is a halogen atom, hydroxyl group, an optionally substituted amino group, etc.; alk is an optionally substituted lower alkylene group; X is O, S, —(CH2)q—, etc.; R is an optionally substituted amino group, etc.; ring B is an optionally substituted Y-containing 5- to 8-membered ring whose ring constituent atoms contain no nitrogen atom; Y is O, S, a group of (wherein Ra, Rb and Rc are the same or different and, each is H, a halogen atom, an optionally substituted hydrocarbon group, etc.), etc.; and ring A may be substituted.
    Type: Grant
    Filed: August 22, 2002
    Date of Patent: November 25, 2003
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Tsuneo Yasuma, Atsuo Baba, Haruhiko Makino, Isao Aoki, Toshiaki Nagata
  • N-substituted 1-(lactone) isoquinolones for treating nervous disorders
    Patent number: 6649626
    Abstract: The invention concerns compounds of general formula (I) wherein: Z represents a sulphur or oxygen atom, NH, N-alkyl or Nboc; group R′, identical or different, represent each a hydrogen atom, a OCH3 group or a OCH2O group; group R″ represents a hydrogen or a CH3 group; group X represents a carbonyl, sulphonyl or CO2 group; and group R represents an alkyl, aryl, alkenyl or aralkyl group. The invention also concerns the preparation of said compounds, pharmaceutical compositions containing them and their use for stimulating &ggr;-amino-butyric acid activity and as medicine for treating nervous disorders.
    Type: Grant
    Filed: August 15, 2002
    Date of Patent: November 18, 2003
    Assignees: Centre National de la Recherche Scientifique (CNRS), Universite de Bern, Innovationsagentur GmbH
    Inventors: Robert Dodd, Rodolphe Razet, Pierre Jean-Paul Potier, Werner Sieghart, Frantisek Jursky, Roman Furtmuller, Erwin Sigel, Urs Thomet