Plural Morpholine Rings Attached Directly Or Indirectly To Each Other By Nonionic Bonding Patents (Class 514/231.8)
  • Publication number: 20040063679
    Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R1, R2, R3, R4, R5, R6, R8, R9 and X are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds.
    Type: Application
    Filed: September 27, 2002
    Publication date: April 1, 2004
    Applicant: Boehringer Ingelheim Pharmaceuticals Inc.
    Inventors: Younes Bekkali, Denice Mary Spero, Sanxing Sun, David S. Thomson, Yancey D. Ward, Erick R.R. Young, Eugene R. Hickey, Weimin Liu, Usha R. Patel
  • Patent number: 6686467
    Abstract: The invention concerns the use of amide derivatives of formula (I) wherein: R1 and R2 are substituents such as hydroxy, C1-6alkoxy, mercapto, C1-6alkylthio, amino, C1-6alkylamino and di-(C1-6alkyl)amino; m and p are independently 0-3; R3 is C1-4alkyl; q is 0-4; and R4 is aryl or cycloalkyl; or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for use in the treatment of diseases or medical conditions mediated by cytokines
    Type: Grant
    Filed: October 8, 2002
    Date of Patent: February 3, 2004
    Assignee: Zeneca Limited
    Inventors: Dearg S Brown, George R Brown, Philip Cohen
  • Publication number: 20030191117
    Abstract: The present invention relates to acyclic piperazine and piperidine derivatives, which are especially useful for treating or preventing neuronal damage, particularly damage associated with neurological diseases. These compounds are also useful for stimulating nerve growth. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage or for stimulating nerve growth.
    Type: Application
    Filed: June 13, 2002
    Publication date: October 9, 2003
    Inventors: David Lauffer, Ronald Tomlinson, Eckhard Ottow, Martyn Botfield
  • Patent number: 6617323
    Abstract: The present invention discloses compounds useful in treating or preventing IMPDH-associated disorders, such as transplant rejection and autoimmune diseases, having the formula (I), wherein X is —C(O)—, —C(S)—, or —S(O)2—; A is an optionally-substituted saturated or unsaturated monocyclic or bicyclic ring; B is a saturated or unsaturated monocyclic or bicyclic ring system having at least one substituent Q which is selected from R7 and R8; R7 is selected from (C0-C6)alkyl, (C2-C6)alkenyl and (C2-C6)alkynyl and R7 is substituted with R8 is selected from (C0-C6)alkyl, (C2-C6)alkenyl and (C2-C6)alkynyl and R8 is substituted with and Z1 through Z5 are as defined in the specification.
    Type: Grant
    Filed: May 23, 2002
    Date of Patent: September 9, 2003
    Assignee: Bristol-Myers Squibb Co.
    Inventors: Edwin J. Iwanowicz, Katerina Leftheris, Chunjian Liu, Toomas Mitt, Scott H. Watterson
  • Patent number: 6605635
    Abstract: N-(3,5-bis-disubstituted aminomethyl-4-hydroxy)benzyl aromatic sulfonamides and N-(3,5-bis-disubstituted aminomethyl-4-hydroxy)phenyl aromatic sulfonamides compounds in accordance with the animal test, are active in the prevention and the treatment of cardiac arrhythmia. These compounds are prepared as corresponding diamines by the condensation of optionally substituted aromatic sulfochlorides with p-hydroxybenzylamine, p-aminophenol, or the like, which followed by the Mannich reaction of the resulted corresponding aromatic sulfamides with formaldehyde and secondary amines; or directly obtained by the reaction of the aromatic sulfamides with 4-amino-2,6-bis-disubstituted aminomethylphenol. Subsequently, the diamines are reacted with various acids to provide their salts.
    Type: Grant
    Filed: June 7, 2002
    Date of Patent: August 12, 2003
    Assignee: Shanghai Institute of Materia Medica Chinese Academy of Science
    Inventors: Donglu Bai, Weizhou Chen, Yunxin Bu, Yiping Wang, Yueli Dong, Aili Kang
  • Publication number: 20030130255
    Abstract: The present invention provides a compound of formula I 1
    Type: Application
    Filed: December 19, 2002
    Publication date: July 10, 2003
    Inventors: Joseph Walter Strohbach, Steven P. Tanis, Malcolm Wilson Moon, William R. Perrault
  • Publication number: 20030087890
    Abstract: The present application describes novel 1,2-disubsituted cyclic derivatives of formula I: 1
    Type: Application
    Filed: January 9, 2002
    Publication date: May 8, 2003
    Inventors: Chu-Biao Xue, Carl Decicco, Xiaohua He
  • Patent number: 6498274
    Abstract: The invention concerns the use of amide derivatives of formula (I) wherein: R1 and R2 are substituents such as hydroxy, C1-6alkoxy, mercapto, C1-6alkylthio, amino, C1-6alkylamino and di-(C1-6alkyl)amino; m and p are independently 0-3R3 is C1-4alkyl; q is 0-4; and R4 is aryl or cycloalkyl; or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for use in the treatment of diseases or medical conditions mediated by cytokines
    Type: Grant
    Filed: March 7, 2000
    Date of Patent: December 24, 2002
    Assignee: Zeneca Limited
    Inventors: Dearg S Brown, George R Brown, Philip Cohen
  • Publication number: 20020183315
    Abstract: The present invention discloses compounds useful in treating or preventing IMPDH-associated disorders, such as transplant rejection and autoimmune diseases, having the formula (I), 1
    Type: Application
    Filed: May 23, 2002
    Publication date: December 5, 2002
    Inventors: Edwin J. Iwanowicz, Katerina Leftheris, Chunjian Liu, Toomas Mitt, Scott H. Watterson
  • Publication number: 20020156061
    Abstract: Selective MMP-13 inhibitors are isophthalic acid derivatives of the formula 1
    Type: Application
    Filed: February 13, 2002
    Publication date: October 24, 2002
    Inventors: Nicole Chantel Barvian, David Thomas Connor, Richard Dennis Dyer, Adam Richard Johnson, William Chester Patt
  • Patent number: 6455520
    Abstract: The invention concerns amide derivatives of formula (I) wherein R3 is (1-6C)alkyl or halogeno; m is 0-3, p is 0-2 and q is 0-4; each of R1 and R2 is a group such as hydroxy, halogeno, trifluoromethyl and cyano; R4 is a basic group such as amino, (1-6C)alkylamino, di-[(1-6C)alkyl]amino, di-[(1-6C)alkyl]amino-(1-6C)alkyl, di-[(1-6C)alkyl]amino-(2-6C)alkoxy, heteroaryl, heteroaryloxy, heteroaryl-(1-6C)alkoxy, heterocyclyl, heterocyclyloxy and heterocyclyl-(1-6C)alkoxy; and Q2 is a group such as heteroaryl, heteroaryloxy or heteroaryl-(1-6C)alkoxy which is optionally substituted; 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: March 23, 2001
    Date of Patent: September 24, 2002
    Assignee: Astra Zeneca AB
    Inventors: Dearg S Brown, George R Brown
  • Patent number: 6451791
    Abstract: An amidoaromatic ring sulfonamide hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed, as are a treatment process that comprises administering a contemplated amidoaromatic ring sulfonamide hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.
    Type: Grant
    Filed: June 4, 1999
    Date of Patent: September 17, 2002
    Assignee: Monsanto Company
    Inventors: Robert M. Heintz, Daniel P. Getman, Joseph J. McDonald, Gary A. DeCrescenzo, Susan C. Howard, S. Zaheer Abbas
  • Publication number: 20020111340
    Abstract: Compounds of formula (I) 1
    Type: Application
    Filed: November 16, 2001
    Publication date: August 15, 2002
    Inventors: Youssef Bennani, Ramin Faghih
  • Publication number: 20020103194
    Abstract: This invention relates to a novel class of partial or full muscarinic receptor agonists intermediates for their preparation, and pharmaceutical compositions and methods of use for the treatment or prevention of diseases the treatment or prevention of which is mediated by muscarinic receptor agonism
    Type: Application
    Filed: February 15, 2000
    Publication date: August 1, 2002
    Inventors: Anabella Villalobos, Daniel Yohannes, Jolanta Nowakowski, Dane Liston
  • Publication number: 20020072520
    Abstract: Sulfonylcarboxamide derivatives of formula I, their physiologically acceptable salts and/or physiologically functional derivatives, methods of making these compounds, their use for preparing medicines for the prevention and treatment of hyperlipidemia and arteriosclerotic disorders.
    Type: Application
    Filed: September 27, 2001
    Publication date: June 13, 2002
    Inventors: Reinhard Kirsch, Hans-Ludwig Schaefer, Eugen Falk, Horst Hemmerle
  • Publication number: 20010012841
    Abstract: Ultraviolet absorbents and photostabilizers have an excellent absorption ability in a wide range of ultraviolet rays, and also have high stability and high safety.
    Type: Application
    Filed: December 15, 2000
    Publication date: August 9, 2001
    Inventors: Masaru Suetsugu, Eijiro Hara, Yuji Matsushita, Haruhiko Inoue, Haruo Ogawa, Keiko Sakai, Shigeru Mugikura
  • Patent number: 6248737
    Abstract: 1-phenyl-3 -dimethylaminopropane compounds corresponding to the formula I a method of preparing them, and the use of these substances as analgesic active ingredients in pharmaceutical compositions.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: June 19, 2001
    Assignee: Gruenenthal GmbH
    Inventors: Helmut Buschmann, Wolfgang Strassburger, Elmar Friderichs
  • Patent number: 6242446
    Abstract: Tachykinin receptor antagonists that are useful for treating or preventing attention deficit disorder, optionally associated with hyperactivity in a patient, are desclosed.
    Type: Grant
    Filed: May 31, 2000
    Date of Patent: June 5, 2001
    Assignee: Merck & Co., Inc.
    Inventors: David L. Glatt, Mark S. Kramer, Nadia Rupniak
  • Patent number: 6211175
    Abstract: This invention relates to cardiac diseases improving agents substantially free from antagonistic action to type 1 receptor of angiotensin II which participates to hypotensive action. Particularly, this invention relates to cardiac diseases improving agents composed of effective ingredients of aromatic compounds or pharmacologically acceptable salts thereof shown by below mentioned general formula. Chemical formula 1 [General formula (I)]  (wherein, substituents thereof typically include, R1, R4, R13 representing hydrogen atom, an alkyl group, a haloalkyl group and so forth, R8 representing —CO—, —SO2— or single bond, R2 representing a 3-7 membered aliphatic cyclic amino group having at least one nitrogen atom, R7 representing —CO—or —SO2—, and R12 representing N-substituted valeramido group.
    Type: Grant
    Filed: October 6, 1998
    Date of Patent: April 3, 2001
    Assignee: Kureha Chemical Industry Co., Ltd.
    Inventors: Mikiro Yanaka, Fuyuhiko Nishijima, Mikio Sugano, Hiroshi Takahashi, Shigeru Suzuki, Hiroyuki Enari, Michihito Ise