Patents by Inventor Robert T. Jacobs

Robert T. Jacobs has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Publication number: 20090291917
    Abstract: Compounds and methods of treating anti-inflammatory conditions are disclosed.
    Type: Application
    Filed: March 5, 2009
    Publication date: November 26, 2009
    Applicant: Anacor Pharmaceuticals, Inc.
    Inventors: Tsutomu Akama, Yong-Kang Zhang, Charles Z. Ding, Jacob J. Plattner, Kirk R. Maples, Yvonne Freund, Virginia Sanders, Yi Xia, Stephen J. Baker, James A. Nieman, Xiaosong Lu, Marcelo Sales, Rashmi Sharma, Rajeshwar Singh, Robert T. Jacobs, Daitao Chen, Michael Richard Kevin Alley
  • Patent number: 6355695
    Abstract: Compounds of formula I wherein Q1, Q2, Q3, Q4 and Q5 have any of the meanings given in the specification, their N-oxides, and their pharmacuetically acceptable salts are nonpeptide antagonists NKA, useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
    Type: Grant
    Filed: January 5, 2001
    Date of Patent: March 12, 2002
    Assignee: Zeneca Limited
    Inventors: Scott C. Miller, Robert T. Jacobs, Ashokkumar B. Shenvi
  • Patent number: 6235757
    Abstract: Compounds of formula I wherein Q1, Q2, Q3, Q4 and Q5 have any of the meanings given in the specification, their N-oxides, and their pharmacuetically acceptable salts are nonpeptide antagonists NKA, useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
    Type: Grant
    Filed: March 6, 2000
    Date of Patent: May 22, 2001
    Assignee: Zeneca Limited
    Inventors: Scott C. Miller, Robert T. Jacobs, Ashokkumar B. Shenvi
  • Patent number: 6051580
    Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, Q.sup.4 and Q.sup.5 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists NKA, useful for the treatment of asthma etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
    Type: Grant
    Filed: March 2, 1999
    Date of Patent: April 18, 2000
    Assignee: Zeneca Limited
    Inventors: Scott C. Miller, Robert T. Jacobs, Ashokkumar B. Shenvi
  • Patent number: 5889024
    Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, Q.sup.4 and Q.sup.5 have any of the meanings given in the specification, their N-oxides, and their pharmacuetically acceptable salts are nonpeptide antagonists NKA, useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
    Type: Grant
    Filed: April 23, 1996
    Date of Patent: March 30, 1999
    Assignee: Zeneca Limited
    Inventors: Scott C. Miller, Robert T. Jacobs, Ashokkumar B. Shenvi
  • Patent number: 5635509
    Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, and Q.sup.4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of neurokinin A and useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
    Type: Grant
    Filed: May 1, 1995
    Date of Patent: June 3, 1997
    Assignee: Zeneca Limited
    Inventors: Robert T. Jacobs, Scott C. Miller, Ashokkumar B. Shenvi, Cyrus J. Ohnmacht, Jr., Chris A. Veale
  • Patent number: 5589489
    Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, and Q.sup.4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of neurokinin A and useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
    Type: Grant
    Filed: December 12, 1994
    Date of Patent: December 31, 1996
    Assignee: Zeneca Limited
    Inventors: Ashokkumar B. Shenvi, Robert T. Jacobs, Scott C. Miller, Cyrus J. Ohnmacht, Jr., Chris A. Veale
  • Patent number: 5550136
    Abstract: Compounds of formula I ##STR1## wherein X and Y are H or halo; R.sup.2 is: [structures Ia, Ib or Ic;] ##STR2## R.sup.3 is selected from unsubstituted or substituted alkyl, aryl or heteroaryl groups;R.sup.4 is selected from H or (C1-6)alkyl,and pharmaceutically acceptable salts thereof, useful in the treatment of neuropsychiatric disoders such as psychoses; pharmaceutical compositions comprising a compound of formula I and a pharmaceutically acceptable diluent or carrier; and methods of treating neuropschiatric disorders comprising administering to a mammal (including man) in need of such treatment an effective mount of a compound of formula I, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 19, 1995
    Date of Patent: August 27, 1996
    Assignee: Zeneca Limited
    Inventors: Robert T. Jacobs, Cyrus J. Ohnmacht, Diane A. Trainor
  • Patent number: 5521199
    Abstract: The present invention concerns the novel alkyl substituted heterocycles of formula I, set out below, wherein Q, Q.sup.1, Q.sup.2 and R have the values defined herein, which antagonize the pharmacological actions of one of the endogenous neuropeptide tachykinins at the neurokinin 2 (NK.sup.2) receptor making them useful whenever such antagonism is desired, such as in the treatment of asthma and related conditions. The invention also provides pharmaceutical compositions containing the alkyl substituted heterocycles for use in such treatment, methods for their use, and processes and novel intermediates for their manufacture.
    Type: Grant
    Filed: May 16, 1994
    Date of Patent: May 28, 1996
    Assignee: Zeneca Limited
    Inventors: Robert T. Jacobs, Ashokkumar B. Shenvi
  • Patent number: 5512575
    Abstract: Compounds of formula I or I', ##STR1## wherein X and Y are independently selected from hydrogen, halo, and (1-6C)alkoxy;R.sup.1 is selected from(A) (1-6C)alkyl;(B) phenyl and naphthyl or substituted versions thereof;(C) phenyl (1-3C)alkyl and naphthyl (1-3C) alkyl;(D) five- and six-membered heteroaryl rings;(E) heteroaryl (1-3C)alkyl and pharmaceutically acceptable salts thereof, useful in the treatment of neuropsychiatric disorders such as psychoses; pharmaceutical compositions comprising a compound of formula I or I' and a pharmaceutically acceptable diluent or carrier; and methods of treating neuropsychiatric disorders comprising administering to a mammal (including man) in need of such treatment an effective amount of a compound of formula I or I', or a pharmaceutically acceptable salt thereof are claimed. The invention also relates to novel processes for producing enantiomeric methanoanthracenyl sulfoxides.
    Type: Grant
    Filed: October 19, 1993
    Date of Patent: April 30, 1996
    Assignee: Zeneca Limited
    Inventors: Robert T. Jacobs, Michael T. Klimas, Cyrus J. Ohnmacht, Marc O. Terpko
  • Patent number: 5399568
    Abstract: Compounds of formula I ##STR1## wherein X and Y are H or halo; R.sup.2 is: [structures Ia, Ib or Ic;] ##STR2## R.sup.3 is selected from unsubstituted or substituted alkyl, aryl or heteroaryl groups;R.sup.4 is selected from H or (Cl-6)alkyl,and pharmaceutically acceptable salts thereof, useful in the treatment of neuropsychiatric disoders such as psychoses; pharmaceutical compositions comprising a compound of formula I and a pharmaceutically acceptable diluent or carrier; and methods of treating neuropschiatric disorders comprising administering to a mammal (including man) in need of such treatment an effective amount of a compound of formula I, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 6, 1992
    Date of Patent: March 21, 1995
    Assignee: Imperial Chemical Industries plc
    Inventors: Robert T. Jacobs, Cyrus J. Ohnmacht, Diane A. Trainor
  • Patent number: 5334765
    Abstract: The present invention concerns novel carbamoyl derivatives of formula I, set out herein, which antagonize the pharmacological actions of one or more of the arachidonic acid metabolites known as leukotrienes, making them useful whenever such antagonism is desired, such as in the treatment of those diseases in which leukotrienes are implicated, for example, in the treatment of allergic or inflammatory diseases, or of endotoxic or traumatic shock conditions. The invention also provides pharmaceutical compositions containing the novel derivatives for use in such treatments, methods for their use and processes and intermediates for the manufacture of the novel derivatives.
    Type: Grant
    Filed: October 14, 1993
    Date of Patent: August 2, 1994
    Assignee: Imperial Chemical Industries PLC
    Inventor: Robert T. Jacobs
  • Patent number: 5286740
    Abstract: The present invention concerns novel carbamoyl derivatives of formula I, set out herein, which antagonize the pharmacological actions of one or more of the arachidonic acid metabolites known as leukotrienes, making them useful whenever such antagonism is desired, such as in the treatment of those diseases in which leukotrienes are implicated, for example, in the treatment of allergic or inflammatory diseases, or of endotoxic or traumatic shock conditions. The invention also provides pharmaceutical compositions containing the novel derivatives for use in such treatments, methods for their use and processes and intermediates for the manufacture of the novel derivatives.
    Type: Grant
    Filed: August 10, 1992
    Date of Patent: February 15, 1994
    Assignee: Imperial Chemical Industries PLC
    Inventor: Robert T. Jacobs
  • Patent number: 5280125
    Abstract: A process for the preparation of a 3-alkylated indole, which comprises:a) reacting a N-(2-nitrostyryl) enamine with an alkylating agent to afford an imine salt,b) optionally reacting the imine salt with water to afford a (2-nitrophenyl)acetaldehyde, andc) reacting the imine salt or the (2-nitrophenyl)acetaldehyde with a reducing agent capable of selectively reducing the nitro group, to afford the desired 3-alkylated indole.
    Type: Grant
    Filed: December 4, 1991
    Date of Patent: January 18, 1994
    Assignee: Imperial Chemical Industries PLC
    Inventors: Robert T. Jacobs, Gerard F. Costello, Stephen A. Brook, Peter J. Harrison
  • Patent number: 5274118
    Abstract: A process for the preparation of (2R)-methyl-4,4,4-trifluorobutylamine, or an acid addition salt thereof which comprisesa) acylating an optically active amine with 2-methyl-4,4,4-trifluorobutanoic acid or a reactive derivative thereof to afford a butyramide;b) separating (R)-diastereomeric butyramide from (S)-diastereomeric butyramide; andc) converting the (R)-diastereomeric butyramide into the desired (2R)-methyl-4,4,4-trifluorobutylamine, or an acid addition salt thereof. The product may be acylated with a carboxylic acid of formula III ##STR1## wherein U is carboxy, or a reactive derivative thereof to afford (R)-4-[5-(N-[4,4,4-trifluoro-2-methylbutyl]carbamoyl)-1-methylindol-3-yl-m ethyl]-3-methoxy-N-o-tolylsulphonylbenzamide. The indole is useful as a leukotriene antagonist, for example in the treatment of asthma or allergic rhinitis.
    Type: Grant
    Filed: December 4, 1991
    Date of Patent: December 28, 1993
    Assignee: Imperial Chemical Industries PLC
    Inventors: Robert T. Jacobs, Andrew G. Brewster, George J. Sependa