Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To Pyridine Or Partially Hydrogenated Pyridine Ring Patents (Class 546/262)
  • Patent number: 7371747
    Abstract: The present invention is directed to novel cyanoalkylamino derivatives that are inhibitors of cysteine protease such as cathepsins K, S, B and L, in particular cathepsin K Pharmaceutical composition comprising these compounds, method of treating diseases mediated by unregulated cysteine protease activity, in particular cathepsin K utilizing these compounds and methods of preparing these compounds are also disclosed.
    Type: Grant
    Filed: November 13, 2002
    Date of Patent: May 13, 2008
    Assignee: Merck Frosst Canada & Co.
    Inventors: Cameron Black, Sheldon N. Crane, Dana Davis, Eduardo L. Setti
  • Publication number: 20080108594
    Abstract: This application relates to a compound of formula I (or a pro-drug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa and/or thrombin, as well as a process for its preparation and intermediates therefor (I).
    Type: Application
    Filed: April 13, 2004
    Publication date: May 8, 2008
    Applicant: Eli Lilly and Company
    Inventors: Jeffry Bernard Franciskovich, David Kent Herron, Jared Harris Linebarger, Angela Lynn Marquart, John Joseph Masters, David Mendel, Leander Merritt, Andrew Michael Ratz, Gerald Floyd Smith, Leland Otto Weigel, Michael Robert Wiley, Ying Kwong Yee
  • Patent number: 7288124
    Abstract: Disclosed herein are novel heteroaromatic binuclear direct dyes, dye compositions containing these dyes and also a process for dyeing keratin fibers using them. In particular, the invention relates to heteroaromatic binuclear direct dyes comprising a pyridine nucleus. With these novel dyes, black shades that show good fastness can be obtained, and they also may show good stability in dye compositions.
    Type: Grant
    Filed: September 8, 2005
    Date of Patent: October 30, 2007
    Assignee: L'Oreal S.A.
    Inventor: Aziz Fadli
  • Publication number: 20070249683
    Abstract: The invention is concerned with dicarboxamide derivatives of formula (I) wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used in pharmaceutical compositions.
    Type: Application
    Filed: April 11, 2007
    Publication date: October 25, 2007
    Inventors: Katrin Groebke Zbinden, Wolfgang Haap, Hans Hilpert, Narendra Panday, Fabienne Ricklin
  • Patent number: 7157580
    Abstract: Aminopyrimidine and aminopyridine (I) compounds, compositions and methods useful in the treatment of inflammatory, metabolic or malignant conditions, are provided herein
    Type: Grant
    Filed: October 18, 2004
    Date of Patent: January 2, 2007
    Assignee: Roche Palo Alto LLC
    Inventors: Ronald Charles Hawley, Sharada Shenvi Labadie, Eric Brian Sjogren, Francisco Xavier Talamas
  • Patent number: 7135472
    Abstract: The present invention provides novel 3-heterocyclic benzylamides and related derivatives having the general Formula I wherein R1, R2, R3, R4, R5, R6, A and Het are as defined in the specification, or a nontoxic pharmaceutically acceptable salt, solvate or hydrate thereof which are openers or activators of KCNQ potassium channels. The present invention also provides pharmaceutical compositions comprising said novel 3-heterocyclic benzylamides and to the method of treatment of disorders sensitive to KCNQ potassium channel opening activity such as migraine or a migraine attack, bipolar disorders, epilepsy, acute and chronic pain and anxiety.
    Type: Grant
    Filed: November 21, 2003
    Date of Patent: November 14, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Yong-Jin Wu, Alexandre L'Heureux, Huan He
  • Patent number: 7109220
    Abstract: The present invention provides amino substituted pyridinyl methanone compounds; pharmaceutical compositions comprising the compounds and methods of synthesis thereof. The compounds, which are cyclin dependent kinase (CDK) inhibitors, can be used to treat or ameliorate CDK mediated disorders. The invention thus also provides the therapeutic or prophylactic use of the compounds and/or pharmaceutical compositions to treat such disorders.
    Type: Grant
    Filed: November 4, 2004
    Date of Patent: September 19, 2006
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Ronghui Lin, Steven K. Wetter, Yanhua Lu, Peter J. Connolly, Stuart Emanuel, Robert H. Gruninger, Steven A. Middleton
  • Patent number: 7074742
    Abstract: Compounds of Formula (I), their N-oxides and agriculturally suitable salts are disclosed which are useful as fungicides formula (I), (II) wherein A is a substituted pyridinyl ring; B is a substituted pyridinyl ring; W is C=L or SOn is O or S; R1 and R2 are each independently H; or C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl or C3-C6 cycloalkyl, each optionally substituted; R3 is H; or C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl or C3-C6 cycloalkyl, C2-C6 alkylcarbonyl, C2-C6 alkoxycarbonyl, C2-C6 alkylaminocarbonyl or C3-C8 dialkylaminocarbonyl; R4 is C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl or C3-C6 cycloalkyl, each optionally substituted; X is O or S; and n is 1 or 2; provided that when W is C?O and R1, R2 and R3 are H; then B is other than 4-trifluoromethyl-3-pyridinyl, 2-chloro-4-pyridinyl and 2,6-dihalo-4-pyridinyl.
    Type: Grant
    Filed: September 17, 2001
    Date of Patent: July 11, 2006
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Timothy Donald Neubert, David Walter Piotrowski, Michael Paul Walker
  • Patent number: 7034035
    Abstract: The present invention relates to compounds of Formula I: wherein: a) ?represents a 6-membered heterocyclic aromatic ring in which X1 is N and X2, X3 and X4 are each independently CR?; R? is independently H, halogen, cyano, hydroxy, C1-C3 alkyl, C1-C3 haloalkyl, cyclopropyl, C1-C3 alkoxy, C1-C3 haloalkoxy, C1-C3 alkylthio, aryl, C1-C3 NHC(O)alkyl, NHC(O)H, C1-C3 haloalkylthio, C2-C4 alkenyl, C2-C4 haloalkenyl, C2-C4 alkynyl, C2-C4 haloalkynyl or nitro wherein adjacent R? substituents may form a ring; b) Z is O, S or NORZ in which RZ is H or C1-C3 alkyl; and c) A represents (i) C3-C14 cycloalkyl, containing 1 or 3 heteroatoms and 0-2 unsaturations, which may be unsubstituted or substituted with halogen, hydroxy, C1-C6 alkyl, C1-C6 haloalkyl, cyano, nitro, aroyl, aryloxy, heteroaryloxy, C1-C6 alkylthio, arylthio, heteroarylthio, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C8 acyloxy, aryl, heteroaryl, C1-C6 acyl, C1-C6 carboalkoxy or amido unsubstituted or substituted with one or two C1 -C6 alkyl groups, o
    Type: Grant
    Filed: December 2, 2002
    Date of Patent: April 25, 2006
    Assignee: Dow AgroSciences LLC
    Inventors: Michael J. Ricks, William H. Dent, III, Richard B. Rogers, Chenglin Yao, Bassam S. Nader, John L. Miesel, Gina M. Fitzpatrick, Kevin G. Meyer, Noormohamed M. Niyaz, Irene M. Morrison, Robert P. Gajewski
  • Patent number: 6995162
    Abstract: Selected heterocyclic compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Grant
    Filed: January 10, 2002
    Date of Patent: February 7, 2006
    Assignee: Amgen Inc.
    Inventors: Guoqing Chen, Jeffrey Adams, Jean Bemis, Shon Booker, Guolin Cai, Lucian Di Pietro, Celia Dominguez, Daniel Elbaum, Julie Germain, Stephanie Geuns-Meyer, Michael Handley, Qi Huang, Joseph L. Kim, Tae-Seong Kim, Alexander Kiselyov, Xiaohu Ouyang, Vinod F. Patel, Leon M. Smith, Markian Stec, Andrew Tasker, Ning Xi, Shimin Xu, Chester Chenguang Yuan, Michael Croghan
  • Patent number: 6949655
    Abstract: A compound having the formula (I): wherein: each R1, R2, R3 and R4 are independently selected from (C1-C10)-straight or branched alkyl, Ar-substituted- (C1-C10)-straight or branched alkyl, (C2-C10)-straight or branched alkenyl or alkynyl, or Ar-substituted-(C2-C10)-straight or branched alkenyl or alkynyl; wherein one to two CH2 groups of said alkyl, alkenyl, or alkynyl chains in each of R1, R2, R3 and R4 are optionally and independently replaced with O, S, S(O), S(O), S(O)2, C(O) or N(R5) in a chemically stable arrangement, wherein the CH2 group of R1 and R2 bound directly to said nitrogen cannot be replaced with C(O); or R1 and R2 taken together form a 4 to 7 membered ring; or R3 and R4 taken together form a 3 to 7 membered ring; wherein a CH2 in either the R1 and R2 ring system or the R3 and R4 ring system is independently and optionally replaced with O, C(O), N(R5), S, S(O), S(O)2 in a chemically stable arrangement; or wherein either or both of the R1 and R2 ring system and the R3 and R4 ring sy
    Type: Grant
    Filed: June 13, 2002
    Date of Patent: September 27, 2005
    Inventors: David Lauffer, Ronald Tomlinson, Eckhard Ottow, Martyn Botfield
  • Patent number: 6943180
    Abstract: Compounds of formula (I) are antagonists of VLA-4 and/or alpha4/beta7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, rhinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.
    Type: Grant
    Filed: March 15, 2002
    Date of Patent: September 13, 2005
    Assignee: Merck & Co., Inc.
    Inventors: George Doherty, Linus S Lin, William K. Hagmann, Ginger Xu-qiang Yang, Linda L. Chang, Shrenik K. Shah, Richard A. Mumford, Theodore Kamenecka
  • Patent number: 6936597
    Abstract: Polymeric prodrugs of the formula: wherein B is selected from the group consisting of OH, leaving groups, residues of amine-containing moieties and a residues of hydroxyl-containing moieties; Y1 is selected from the group consisting of O, S, and NR5; M is NR3, O or S; Ar is a moiety which when included in Formula I forms a multi-substituted aromatic or heteroaromatic hydrocarbon or a multi-substituted heterocyclic group; (m) is zero or a positive integer; R1-3 and R5 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls, substituted C1-6 heteroalkyls, C1-6 alkoxy, phenoxy and C1-6 heteroalkoxy; and R4 is a polymeric residue; as well as methods of making and using the same are disclosed.
    Type: Grant
    Filed: March 21, 2002
    Date of Patent: August 30, 2005
    Assignee: Enzon, Inc.
    Inventors: Richard B. Greenwald, Yun H. Choe
  • Patent number: 6878714
    Abstract: Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Grant
    Filed: July 17, 2002
    Date of Patent: April 12, 2005
    Assignee: Amgen Inc.
    Inventors: Benny Askew, Jeffrey Adams, Shon Booker, Guoqing Chen, Lucian V. DiPietro, Daniel Elbaum, Julie Germain, Stephanie D. Geuns-Meyer, Gregory J. Habgood, Michael Handley, Qi Huang, Tae-Seong Kim, Aiwen Li, Nobuko Nishimura, Rana Nomak, Vinod F. Patel, Babak Riahi, Joseph L. Kim, Ning Xi, Kevin Yang, Chester Chenguang Yuan
  • Patent number: 6849621
    Abstract: Disclosed are novel compounds of the formula Also disclosed are pharmaceutical compositions comprising the compounds of Formula I. Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I. Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I in combination with a H. receptor antagonist.
    Type: Grant
    Filed: March 11, 2002
    Date of Patent: February 1, 2005
    Assignees: Schering Corporation, Pharmacopeia Drug Discovery, Inc.
    Inventors: Stuart B. Rosenblum, Qingbei Zeng, Mwangi Wa Mutahi, Robert G. Aslanian, Pauline C. Ting, Neng-Yang Shih, Daniel M. Solomon, Jianhua Cao, Henry A. Vaccaro, Kevin D. McCormick, John J. Baldwin, Ge Li
  • Publication number: 20040266770
    Abstract: Substituted cyanoanthranilamide derivatives, their production and use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis are described. The compounds according to the invention can be used as or in the case of psoriasis, Kaposi's sarcoma, restenosis, such as, e.g., stent-induced restenosis, endometriosis, Crohn's disease, Hodgkin's disease, leukemia; arthritis, such as rheumatoid arthritis, hemangioma, angiofibroma; eye diseases, such as diabetic retinopathy, neovascular glaucoma; renal diseases, such as glomerulonephritis, diabetic nephropathy, malignant nephrosclerosis, thrombic microangiopathic syndrome, transplant rejections and glomerulopathy; fibrotic diseases, such as cirrhosis of the liver, mesangial cell proliferative diseases, arteriosclerosis, injuries to nerve tissue, and inhibition of the reocclusion of vessels after balloon catheter treatment, in vascular prosthetics or after mechanical devices are used to keep vessels open, such as, e.g.
    Type: Application
    Filed: August 25, 2004
    Publication date: December 30, 2004
    Inventors: Alexander Ernst, Andreas Huth, Martin Krueger, Karl-Heinz Thierauch, Andreas Menrad, Martin Haberey
  • Patent number: 6833378
    Abstract: Corticotropin-releasing factor (CRF) antagonists having the formulae wherein the dashed lines, A, B, Y, Z, G, R3, R4, R5, R6, R16 and R17 are as defined in the application, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment disorders including CNS and stress-related disorders.
    Type: Grant
    Filed: January 17, 2001
    Date of Patent: December 21, 2004
    Assignee: Pfizer Inc
    Inventor: Yuhpyng L. Chen
  • Patent number: 6800619
    Abstract: Described herein are compounds that are useful as caspase inhibitors having the formula: wherein Ring A is an optionally substituted piperidine, tetrahydroquinoline or tetrahydroisoquinoline ring; R1 is hydrogen, CN, CHN2, R, or CH2Y; R is an optionally substituted group selected from an aliphatic group, an aryl group, or an aralkyl group; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; and R3 is hydrogen, an optionally substituted aryl group, an optionally substituted aralkyl group, or an optionally substituted C1-6 aliphatic group, R4 is an optionally substituted group selected from an aryl group or a heterocyclyl group, or R3 and R4 taken together with the nitrogen to which they are attached optionally form a substituted or unsubstituted monocyclic, bicyclic or tricyclic ring.
    Type: Grant
    Filed: September 12, 2001
    Date of Patent: October 5, 2004
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Ronald Knegtel, Michael Mortimore
  • Patent number: 6794396
    Abstract: A class of substituted pyridines that are useful for inhibiting the activity of cholesteryl ester transfer protein, and have the structural formula (IA), wherein R2, R3, R4, R5, and R6 are defined in the claims.
    Type: Grant
    Filed: March 31, 2003
    Date of Patent: September 21, 2004
    Assignee: Pharmacia Corporation
    Inventors: Len F. Lee, Kevin C. Glenn, Daniel T. Connolly, David G. Corley, Daniel L. Flynn, Ashton T. Hamme, Shridhar G. Hegde, Michele A. Melton, Roger J. Schilling, James A. Sikorski, Nancy N. Wall, Jeffery A. Zablocki
  • Patent number: 6794380
    Abstract: The invention concerns amide derivatives of the Formula I wherein X is CH or N; Y is CH or N; m is 0-3; R1 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and carbamoyl; n is 0-3; R2 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and (1-6C)alkoxycarbonyl; R3 is hydrogen, halogeno, (1-6C)alkyl or (1-6C)alkoxy; q is 0-4; and Q is a group such as aryl, aryloxy, aryl-(1-6C)alkoxy, arylamino, N-(1-6C)alkyl-arylamino and aryl-(1-6C)alkylamino; or pharmaceutically-acceptable salts or in-vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.
    Type: Grant
    Filed: January 29, 2003
    Date of Patent: September 21, 2004
    Assignee: AstraZeneca AB
    Inventor: Dearg S Brown
  • Patent number: 6787546
    Abstract: The object of the invention is to provide an excellent compound as a drug. The invention relates to a heterocyclic compound shown by the following formula: A—B—D—E  [1] wherein A is heteroaryl or its oxide; B is ethenylene; D is optionally substituted phenylene; and E is a group of the formula:  wherein G is optionally substituted phenyl; and R is heteroaryl or heteroarylmethyl, or a group of the formula: wherein n is an integer of 1 to 5; R5 and R6 are same or different and are independently selected from the group consisting of hydrogen, C1—C6 alkyl, hydroxyalkyl, aminoalkyl; or R5 and R6 taken together with the adjacent nitrogen atom may form 5- to 7-membered cyclic amino group for —NR5R6 or a salt thereof.
    Type: Grant
    Filed: June 12, 2002
    Date of Patent: September 7, 2004
    Assignee: Nippon Shinyaku Co., Ltd.
    Inventors: Toshiyuki Suzuki, Tomiyoshi Aoki
  • Publication number: 20040138257
    Abstract: The present invention relates to cancer therapy and to novel anticancer agents 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: Application
    Filed: November 25, 2003
    Publication date: July 15, 2004
    Applicant: Aventis Pharma S.A.
    Inventors: Herve Bouchard, Augustin Hittinger
  • Patent number: 6759414
    Abstract: This application relates to a compound of formula I (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
    Type: Grant
    Filed: July 29, 2003
    Date of Patent: July 6, 2004
    Assignee: Eli Lilly and Company
    Inventors: Douglas Wade Beight, Trelia Joyce Craft, Carl Penman Denny, Jeffry Bernard Franciskovich, Theodore Goodson, Jr., Steven Edward Hall, David Kent Herron, Sajan Joseph, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milet, Marta Maria Piñeiro-Nuñez, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
  • Publication number: 20040067982
    Abstract: The present invention relates to novel CD40:CD154 binding interrupter compounds and use of these compounds and pharmaceutical compositions comprising them, to treat conditions associated with inappropriate CD154 activation in a subject. Specifically, this invention provides compounds which are identified by screening a library of small molecules for those that are capable of specifically binding CD154 and interrupting CD40:CD154 interaction.
    Type: Application
    Filed: February 28, 2003
    Publication date: April 8, 2004
    Inventors: Zhongli Zheng, Mary-Beth Carter, YuSheng Liao, Lihong Sun, Leonid Kirkovsky, Susan Mrose, Yen-Ming Hsu, David Thomas, Gerald W. Shipps, Satish Jindal, George R. Lenz, Huw M. Nash
  • Patent number: 6680383
    Abstract: A process for making nevirapine, comprising the following steps: (a) reacting a 2-halo-3-pyridinecarbonitrile of the formula wherein X is a fluorine, chlorine, bromine or iodine atom, preferably chlorine or bromine, with cyclopropylamine, to yield 2-(cyclopropylamino)-3-pyridinecarbonitrile; (b) hydrolyzing the 2-(cyclopropylamino)-3-pyridinecarbonitrile to yield 2-(cyclopropylamino)-3-pyridine carboxylic acid; (c) isolating the 2-(cyclopropylamino)-3-pyridine carboxylic acid from the reaction medium; (e) treating the 2-(cyclopropylamino)-3-pyridine carboxylic acid with a chlorinating agent, to yield 2-(cyclopropylamino)-3-pyridinecarbonyl chloride; (f) reacting the 2-(cyclopropylamino)-3-pyridine carbonyl chloride with a 2-halo-4-methyl-3-pyridinamine of the formula wherein X is a fluorine, chlorine, bromine or iodine atom, preferably chlorine or bromine, to produce an N-(2-halo-4-methyl-3-pyridinyl)-2-(cyclopropylamino)-3-pyridinecarboxamide; and (g) cyclizing the N-
    Type: Grant
    Filed: June 5, 2003
    Date of Patent: January 20, 2004
    Assignee: Boehringer Ingelheim Chemicals, Inc.
    Inventors: Robert Frederick Boswell, Bernard Franklin Gupton, Young Sek Lo
  • Patent number: 6677452
    Abstract: The present invention relates to novel pyridine carboxamide or sulfonamide derivative compounds of the following formula: wherein R1 to R6 have the meanings provided herein. The invention further relates to combinatorial libraries containing two or more such compounds, as well as methods of preparing pyridine carboxamide or sulfonamide derivative compounds.
    Type: Grant
    Filed: September 30, 1999
    Date of Patent: January 13, 2004
    Assignee: Lion Bioscience AG
    Inventors: Yuewu Chen, Hengyuan Lang, Yazhong Pei
  • Publication number: 20030225106
    Abstract: Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Application
    Filed: July 17, 2002
    Publication date: December 4, 2003
    Applicant: Amgen Inc.
    Inventors: Benny Askew, Jeffrey Adams, Shon Booker, Guoqing Chen, Lucian V. DiPietro, Daniel Elbaum, Julie Germain, Stephanie D. Geuns-Meyer, Gregory J. Habgood, Michael Handley, Qi Huang, Tae-Seong Kim, Aiwen Li, Nobuko Nishimura, Rana Nomak, Vinod F. Patel, Babak Riahi, Joseph L. Kim, Ning Xi, Kevin Yang, Chester Chenguang Yuan
  • Patent number: 6656958
    Abstract: The present invention is directed to a series of substituted pyridine compounds, a method for selectively controlling neurotransmitter release in mammals using these compounds, and pharmaceutical compositions containing these compounds. Preferred compounds are 3′-(5′- and/or 6′-substituted) pyridyl ethers.
    Type: Grant
    Filed: February 1, 2001
    Date of Patent: December 2, 2003
    Assignee: Abbott Laboratories
    Inventors: Nan-Horng Lin, Liming Dong
  • Patent number: 6635657
    Abstract: This application relates to a compound of formula I (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
    Type: Grant
    Filed: June 8, 2001
    Date of Patent: October 21, 2003
    Assignee: Eli Lilly and Company
    Inventors: Douglas Wade Beight, Trelia Joyce Craft, Carl Penman Denny, Jeffry Bernard Franciskovich, Theodore Goodson, Steven Edward Hall, David Kent Herron, Sajan Joseph, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Marta Maria Piñeiro-Núñez, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
  • Publication number: 20030186989
    Abstract: Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructive pulmonary disease, of Formula (1.0.
    Type: Application
    Filed: July 24, 2002
    Publication date: October 2, 2003
    Inventors: Anthony Marfat, Robert James Chambers
  • Patent number: 6624178
    Abstract: The invention discloses novel compounds of the pyridinium series useful for the management of diabetes and aging-related vascular complications, including kidney disease, nerve damage, atherosclerosis, retinopathy, dermatological disorders and discoloration of teeth, by breaking preformed AGE, of the general formula I, or pharmaceutically acceptable salts thereof, wherein, R1, R2, R3, X and m are as defined in the specification.
    Type: Grant
    Filed: August 9, 2002
    Date of Patent: September 23, 2003
    Assignee: Torrent Pharmaceuticals Ltd.
    Inventor: Alangudi Sankaranarayanan
  • Patent number: 6610717
    Abstract: Dihydropyridine derivatives represented by the following formula: analogs thereof and pharmaceutically acceptable salts thereof have an activity of selectively inhibiting the action of N-type calcium channel, and they are used as therapeutic agents for various diseases relating to N-type calcium channel.
    Type: Grant
    Filed: December 21, 2001
    Date of Patent: August 26, 2003
    Assignee: Ajinomoto Co., Inc.
    Inventors: Akira Nakajo, Munetaka Tokumasu, Morikazu Kito, Akira Takahara, Yukitsugu Ono, Tomoko Takeda, Yuki Kajigaya, Hajime Koganei
  • Patent number: 6608060
    Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
    Type: Grant
    Filed: June 14, 1999
    Date of Patent: August 19, 2003
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Guy W. Bemis, Francesco Gerald Salituro, John Patrick Duffy, John E. Cochran, Edmund Martin Harrington, Mark A. Murko, Keith P. Wilson, Michael Su, Vincent P. Galullo
  • Patent number: 6605624
    Abstract: A class of substituted pyridines that are useful for inhibiting the activity of cholesteryl ester transfer protein, and have the structural formula (IA), wherein R2, R3, R4, R5, and R6 are defined in the claims.
    Type: Grant
    Filed: December 11, 2000
    Date of Patent: August 12, 2003
    Assignee: Pharmacia Corporation
    Inventors: Len F. Lee, Kevin C. Glenn, Daniel T. Connolly, David G. Corley, Daniel L. Flynn, Ashton T. Hamme, Shridhar G. Hegde, Michele A. Melton, Roger J. Schilling, James A. Sikorski, Nancy N. Wall, Jeffery A. Zablocki
  • Publication number: 20030144262
    Abstract: This invention relates to a series of N-heterocyclyl hydrazides of Formula I, 1
    Type: Application
    Filed: October 4, 2002
    Publication date: July 31, 2003
    Inventors: Zhihua Sui, Mark Macielag, James Lanter
  • Publication number: 20030139397
    Abstract: Compounds of Formula (I), and their N-oxides and agriculturally suitable salts, are disclosed which are useful as arthropodicides wherein A is H; E is H or C1-C3 alkyl; or A and E can be taken together to form —CH2—, —CH2CH2—, —O—, —S—, —S(O)—, —S(O)2—, —NR8—, —OCH2—, —SCH2—, —N(R8)CH2—, substituted —CH2— and substituted —CH2CH2—, the substituents independently selected from 1-2 halogen and 1-2 methyl; W is N or CR4;X is CR5R6, O, S, NR7 or a direct bond, provided that when W is N, then X is other than a direct bond; Y is H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C3 alkylsulfonyl, C3-C6 cycloalkyl, C3-C6 cycloalkylalkyl, NR9R10, N═CR11R12, OR7, COR13, CO2R14 or C1-C6 alkyl substituted by at least one group selected from halogen, C1-C3 alkoxy, CN, NO2, S(O)1R15, COR13, CO2R14 and optionally substituted phenyl; Z is O or S; and R2, R3, R4, R5, R6, R7, R8, R9
    Type: Application
    Filed: August 28, 2002
    Publication date: July 24, 2003
    Inventor: David Walter Piotrowski
  • Publication number: 20030114311
    Abstract: 4-Aminopicolinic acids having aryl or heteroaryl substituents in the 6-position and their amine and acid derivatives are potent herbicides demonstrating a broad spectrum of weed control.
    Type: Application
    Filed: July 30, 2002
    Publication date: June 19, 2003
    Inventors: Terry William Balko, Ann Marie Buysse, Jeffrey Brian Epp, Stephen Craig Fields, Christian Thomas Lowe, Renee Joan Keese, John Sanders Richburg, James Melvin Ruiz, Monte Ray Weimer, Renard Antonio Green, Roger Eugene Gast, Kristy Bryan
  • Patent number: 6566527
    Abstract: A five-step process for preparing 1-(6-methylpyridin-3-yl)-2-[4-methylsulfonyl)phenyl]ethanone of formula (I): The process involves the following steps: (a) 4-(methylthio)benzyl alcohol is converted into 4-(methylthio)benzyl chloride; (b) 4-(methylthio)benzyl chloride is converted with an alkali metal cyanide into 4-(methylthio)phenylacetonitrile; (c) 4-(methylthio)phenylacetonitrile is condensed with a 6-methyinicotinic ester to give 3-[2-(2-(methylthio)phenyl)-2-cyanoacetyl](6-methyl)pyridine; (d) 3-[2-(4-(methylthio)phenyl-2-cyanoacetyl](6-methyl)pyridine is hydrolyzed and decarboxylated under acidic conditions to give 3-[2-(4-(methylthio)-phenyl)acetyl](6-methyl)pyridine is hydrolyzed and decarboxylated under acidic conditions to give 3-[2-(4-(methylthio)phenyl)acetyl(6-methyl)pyridine; and (e) 3-[2(4-(methylthio)phenyl)acetyl](6-methyl)pyridine is oxidized to give the end product.
    Type: Grant
    Filed: March 14, 2002
    Date of Patent: May 20, 2003
    Assignees: Merck & Co., Inc., Lonza AG
    Inventors: Yves Bessard, James Edward Leresche
  • Publication number: 20030083269
    Abstract: Disclosed are compounds that inhibit the microbial NAD synthetase enzyme. For example, disclosed are compounds of the formula Ar1—X—Ar2—Y—L—Z—Q, wherein Q is Q1Ar3 or Ar3Q1; Ar1, Ar2, and Ar3 are independently aryl or heteroaryl, optionally substituted with one or more substituents; X, Y, and Z are independently selected from the group consisting of a covalent bond or groups containing one or more of C, H, N, O, S atoms; L is a linker and Q1 is an alkylenyl, alkylenyl carbonyloxy alkyl, or alkylenyl carbonylamino alkyl group, optionally having a substituent; a covalent bond; a group containing amidine or guanidine function wherein the amidine or guanidine may be optionally N-substituted with an alkyl; or a zwitterion; or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: February 22, 2002
    Publication date: May 1, 2003
    Applicant: Virtual Drug Development, Inc.
    Inventors: Wayne J. Brouillette, Lawrence DeLucas, Christie Brouillette, Sadanandan E. Velu, Yong-Chul Kim, Liyuan Mou, R. Stephen Porter
  • Patent number: 6548514
    Abstract: The invention concerns amide derivatives of the Formula I wherein X is CH or N; Y is CH or N; m is 0-3; R1 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and carbamoyl; n is 0-3; R2 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and (1-6C)alkoxycarbonyl; R3 is hydrogen, halogeno, (1-6C)alkyl or (1-6C)alkoxy; q is 0-4; and Q is a group such as aryl, aryloxy, aryl-(1-6C)alkoxy, arylamino, N-(1-6C)alkyl-arylamino and aryl-(1-6C)alkylamino; or pharmaceutically-acceptable salts or in-vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.
    Type: Grant
    Filed: September 17, 2001
    Date of Patent: April 15, 2003
    Assignee: Astrazeneca AB
    Inventor: Dearg S. Brown
  • Publication number: 20030065011
    Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating COX-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I.
    Type: Application
    Filed: October 30, 2001
    Publication date: April 3, 2003
    Applicant: Merck Frosst Canada & Co.
    Inventors: Daniel Dube, Rejean Fortin, Richard Friesen, Zhaoyin Wang, Jacques Yves Gauthier
  • Publication number: 20030055259
    Abstract: The invention relates to a process for the preparation of 5-arylnicotinaldehydes by reduction of the corresponding 5-arylnicotinic acids by catalytic hydrogenation in the presence of carboxylic anhydrides in which the catalyst used is a palladium/ligand complex, characterized in that the molar ratio between palladium and ligand is from 1:5 to 1:15 in the case of monodentate ligands and from 1:2.5 to 1:7.5 in the case of bidentate ligands.
    Type: Application
    Filed: August 6, 2002
    Publication date: March 20, 2003
    Inventors: Andreas Bathe, Heinz Bokel, Thomas Keil, Ralf Knieriemen, Christoph Murmann
  • Patent number: 6521626
    Abstract: Compounds of formula (1): wherein R1 is a hydrogen atom or an optionally substituted cycloaliphatic, polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; Alk1 is an optionally substituted aliphatic or heteroaliphatic chain; L1 is a linker atom or group; r and s is each zero or an integer 1; R2 and R3, which may be the same or different, is each a hydrogen or halogen atom or a straight or branched alkyl, haloalkyl, alkoxy, haloalkoxy, hydroxyl or nitro group; Alk2 is a straight or branched alkylene chain; m is zero or an integer 1; R4 is a hydrogen atom or a methyl group; R5 is a hydrogen atom or a straight or branched alkyl group; R6 is a group —(CH2)tR7 in which t is zero or the integer 1 and R7 is an optionally substituted polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; R is a carboxylic acid (—CO2H) or a derivative thereof; and the salts, solvates and hydrates the
    Type: Grant
    Filed: March 23, 1999
    Date of Patent: February 18, 2003
    Assignee: Celltech R&D Limited
    Inventors: Sarah Catherine Archibald, John Clifford Head, Graham John Warrellow, John Robert Porter
  • Publication number: 20030013743
    Abstract: The present invention is directed to substituted N′-(arylcarbonyl)-benzhydrazides, N′-(arylcarbonyl)-benzylidene-hydrazides and analogs thereof, represented by the Formulae I and II: 1
    Type: Application
    Filed: May 10, 2002
    Publication date: January 16, 2003
    Applicant: Cytovia, Inc.
    Inventors: Sui Xiong Cai, Shailaja Kasibhatla, John Drewe, P. Sanjeeva Reddy, Han-Zhong Zhang
  • Patent number: 6503928
    Abstract: Compounds of the formula wherein R1, R2, R3, R4, X and n are defined in the specification, are useful for the treatment of anxiety, depression and related CNS disorders, and other related conditions such as the treatment of alcohol and drug withdrawal, sexual dysfunction and Alzheimer's disease.
    Type: Grant
    Filed: September 18, 2001
    Date of Patent: January 7, 2003
    Assignee: Wyeth
    Inventors: Michael G. Kelly, Gan Zhang, Yvette L. Palmer, Wayne E. Childers
  • Publication number: 20020193605
    Abstract: Dihydropyridine derivatives represented by the following formula: 1
    Type: Application
    Filed: December 21, 2001
    Publication date: December 19, 2002
    Applicant: AJINOMOTO CO. INC
    Inventors: Akira Nakajo, Munetaka Tokumasu, Morikazu Kito, Akira Takahara, Yukitsugu Ono, Tomoko Takeda, Yuki Kajigaya, Hajime Koganei
  • Publication number: 20020193409
    Abstract: Polymeric prodrugs of the formula: 1
    Type: Application
    Filed: March 21, 2002
    Publication date: December 19, 2002
    Inventors: Richard B. Greenwald, Yun H. Choe
  • Patent number: 6486183
    Abstract: Compounds of formula (I): wherein Rx is cyano or bromo; R1 is halo; R2 is C1-C3 alkyl, and pharmaceutically acceptable salts and prodrugs thereof have activity as antiretrovirals.
    Type: Grant
    Filed: November 13, 2000
    Date of Patent: November 26, 2002
    Assignee: Medivir AB
    Inventors: Christer Salhberg, Rolf Noréen, Marita Högberg, Per Engelhardt
  • Patent number: 6465471
    Abstract: Compounds of formula (1) are described: in which Het is a heteroaromatic group, Alk1 is an optionally substituted aliphatic or heteroaliphatic chain and R is a carboxylic acid or a derivative thereof. The compounds are able to inhibit the binding of &agr;4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.
    Type: Grant
    Filed: July 1, 1999
    Date of Patent: October 15, 2002
    Assignee: Celltech Therapeutics Limited
    Inventors: Graham John Warrellow, John Clifford Head, John Robert Porter, Sarah Catherine Archibald
  • Patent number: RE38506
    Abstract: The present invention provides the compound having the structure: wherein each of R1 and R2 are independently the same as or different from each other; when R1 and R2 are the same, each is a substituted or unsubstituted arylamino, cycloalkylamino, pyridineamino, piperidino, 9-purine-6-amine, or thiozoleamino group; when R1 and R2 are different, R1=R3—N—R4, wherein each of R3 and R4 are independently the same as or different from each other and are a hydrogen atom, a hydroxyl group, a substituted or unsubstituted, branched or unbranched alkyl, alkenyl, cycloalkyl, aryl, alkyloxy, aryloxy, arylalkyloxy, or pyridine group, or R3 and R4 bond together to form a piperidine group and R2 is a hydroxylamino, hydroxyl, amino, alkylamino, dialkylamino or alkyloxy group; and n is an integer from about 4 to about 8. The present invention also provides a method of selectively inducing terminal differentiation of neoplastic cells and thereby inhibiting proliferation of such cells.
    Type: Grant
    Filed: November 2, 2001
    Date of Patent: April 20, 2004
    Assignees: Sloan-Kettering Institute for Cancer Research, The Trustees of Columbia University in the City of New York
    Inventors: Ronald Breslow, Paul A. Marks, Richard A. Rifkind, Branko Jursic