Patents by Inventor Xiao-shu He

Xiao-shu He 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: 20020052496
    Abstract: Disclosed are compounds of the formula 1
    Type: Application
    Filed: June 20, 2001
    Publication date: May 2, 2002
    Applicant: Neurogen Corporation
    Inventors: Xiao-Shu He, Brian de Costa, Jan W.F. Wasley
  • Publication number: 20020045624
    Abstract: Certain aralkl diazabicycloalkyl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions.
    Type: Application
    Filed: September 4, 2001
    Publication date: April 18, 2002
    Inventors: Wayne D. Bowen, Brian R. De Costa, Celia Dominguez, Xiao-Shu He, Kenner C. Rice
  • Patent number: 6313141
    Abstract: Disclosed are compounds of the formula or the pharmaceutically acceptable salts thereof wherein: A represents an optionally substituted alkylene group of from 2-5 carbon atoms; W is COH or CH; Y and Z are nitrogen or CH; and R1, R2, R3, R4, R5, R6 are defined herein. Pharmaceutical compositions and preparations containing such compounds are also provided. The invention further relates to the use of such compounds in the treatment of neuropsychological diseases such as schizophrenia and other central nervous system diseases.
    Type: Grant
    Filed: March 8, 2000
    Date of Patent: November 6, 2001
    Assignee: Neurogen Corporation
    Inventor: Xiao-Shu He
  • Patent number: 6310064
    Abstract: Certain aralkyl diazabicycloalkyl compounds are disclosed for treatment of CNS disorders, such as cerebral ischemia, psychosis, and convulsions.
    Type: Grant
    Filed: July 6, 1999
    Date of Patent: October 30, 2001
    Assignee: The United States of America as represented by the of Department of Health and Human Services
    Inventors: Wayne Bowen, Brian R. de Costa, Celia Dominguez, Xiao-Shu He, Kenner C. Rice
  • Patent number: 6288230
    Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable acid addition salts thereof wherein: n is an integer; R1 represents an organic or inorganic group; R2 represents halogen or C1-C6 alkyl; RN is an alkylene carrying a substituted piperazine, piperidine, or tetrahydropyridine; and R4 is hydrogen or C1-C6 alkyl, which compounds are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents.
    Type: Grant
    Filed: September 29, 1999
    Date of Patent: September 11, 2001
    Assignee: Neurogen Corporation
    Inventors: Xi Chen, Xiao-shu He
  • Patent number: 6284759
    Abstract: Disclosed are compounds of the formula: or pharmaceutically acceptable salts thereof, wherein: A is (un)substituted alkylene; R1 and R2 are the same or different and represent hydrogen, halogen, alkyl, alkoxy, alkylthio, hydroxy, (un)substitutedamino, cyano, nitro, sulfonamide, trifluoromethyl or trifluoromethoxy; R3, R4, R5, R6, and R8 are independently hydrogen or alkyl; and X is sulfur, oxygen or NR7 where R8 is defined herein; m is an integer chosen from 0, 1 or 2; and Ar is an aryl or heteroaryl group as further defined herein, which compounds are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents.
    Type: Grant
    Filed: September 30, 1999
    Date of Patent: September 4, 2001
    Assignee: Neurogen Corporation
    Inventor: Xiao Shu He
  • Patent number: 6252077
    Abstract: Disclosed are compounds of the formula or the pharmaceutically acceptable salts thereof wherein the 6-membered A ring may be optionally substituted with up to four groups independently selected from halogen, hydroxy, lower alkyl, or lower alkoxy; Ar represents optionally substituted aryl or heteroaryl Z represents carbon or nitrogen provided that where Z is carbon, R11 represents hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy, or phenyl optionally substituted with one or two groups selected from hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy; and where Z is nitrogen, R11 represents an electron pair; R5 is hydrogen or lower alkyl; m represents an integer; n is 0, or an integer; R12 and R13 independently represent lower alkyl; CR′R″ represent a methylene group optionally substituted with lower alkyl; and k is 1, which compounds are useful in treating various neuropsychological disorders including, for example, schizophrenia, dementia, depression, anxi
    Type: Grant
    Filed: December 22, 1999
    Date of Patent: June 26, 2001
    Assignee: Neurogen Corporation
    Inventors: Xiao-shu He, Brian de Costa, Jan W. F. Wasley
  • Patent number: 6245768
    Abstract: Disclosed are compounds of the formula or the pharmaceutically acceptable salts thereof wherein the 6-membered A ring may be optionally substituted with up to four groups independently selected from halogen, hydroxy, lower alkyl, or lower alkoxy; Ar represents optionally substituted aryl or heteroaryl Z represents carbon or nitrogen provided that where Z is carbon, R11 represents hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy, or phenyl optionally substituted with one or two groups selected from hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy; and where Z is nitrogen, R11 represents an electron pair; R5 is hydrogen or lower alkyl, L and m represent integers; n is 0, or an integer; R12 and R13 independently represent lower alkyl; or together may together form an optionally substituted 5-11 membered ring with the nitrogen atoms to which they are bonded;CR′R″ represents a methylene group optionally substituted with lower alkyl;and k is an integer of from 1
    Type: Grant
    Filed: August 3, 1999
    Date of Patent: June 12, 2001
    Assignee: Neurogen Corporation
    Inventors: Xiao-shu He, Brian de Costa, Jan W. F. Wasley
  • Patent number: 6100255
    Abstract: Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof, wherein:Ar represents aryl or heteroaryl;R.sub.1 and R.sub.2 are the same or different and represent organic or inorganic substituents;R.sub.5 is hydrogen or C.sub.1 -C.sub.6 alkyl;W represents CH or nitrogen;X is oxygen or sulfur; andA represents an alkylene group,which compounds bind selectively with high affinity to the dopamine D.sub.4 receptor subtype and are therefore of use in treatment of various neuropsychological disorders.
    Type: Grant
    Filed: October 28, 1998
    Date of Patent: August 8, 2000
    Assignee: Neurogen Corporation
    Inventor: Xiao-shu He
  • Patent number: 6031097
    Abstract: Disclosed are compounds of the formula ##STR1## or the pharmaceutically acceptable salts thereof wherein the 6-membered A ring may be optionally substituted with up to four groups independently selected from halogen, hydroxy, lower alkyl, or lower alkoxy;Ar represents optionally substituted aryl or heteroarylZ represents carbon or nitrogen provided thatwhere Z is carbon, R.sub.11 represents hydrogen, halogen, hydroxy, lower alkyl, or loweralkoxy, or phenyl optionally substituted with one or two groups selected from hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy; andwhere Z is nitrogen, R.sub.11 represents an electron pair;R.sub.5 is hydrogen or lower alkyl;L and m represent integers;n is 0, or an integer;R.sub.12 and R.sub.
    Type: Grant
    Filed: October 26, 1998
    Date of Patent: February 29, 2000
    Assignee: Neurogen Corporation
    Inventors: Xiao-shu He, Brian de Costa, Jan W.F. Wasley
  • Patent number: 5972945
    Abstract: Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable salts thereof wherein: R.sub.1, R.sub.2, and R.sub.3 are as defined herein;R.sub.6 is hydrogen or C.sub.1 -C.sub.6 alkyl, andQ represents a substituted azacycloalkylalkyl group,which compounds are useful in treating psychotic disorders such as schizophrenia and other central nervous system diseases.
    Type: Grant
    Filed: June 12, 1998
    Date of Patent: October 26, 1999
    Assignee: Neurogen Corporation
    Inventor: Xiao-Shu He
  • Patent number: 5958920
    Abstract: Certain aralkyl diazabicycloalkyl compounds are disclosed for treatment of CNS disorders, such as cerebral ischemia, psychosis and convulsions.
    Type: Grant
    Filed: October 20, 1997
    Date of Patent: September 28, 1999
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Wayne Bowen, Brian R. de Costa, Celia Dominguez, Xiao-Shu He, Kenner C. Rice
  • Patent number: 5932729
    Abstract: Disclosed are compounds of the formula ##STR1## or the pharmaceutically acceptable salts thereof wherein the 6-membered A ring may be optionally substituted with up to four groups independently selected from halogen, hydroxy, lower alkyl, or lower alkoxy;Ar represents optionally substituted aryl or heteroaryl;Z represents carbon or nitrogen provided thatwhere Z is carbon, R.sub.11 represents hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy, or phenyl optionally substituted with one or two groups selected from hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy; andwhere Z is nitrogen, R.sub.11 represents an electron pair;R.sub.5 is hydrogen or lower alkyl;L and m represent integers;n is 0, or an integer;R.sub.12 and R.sub.
    Type: Grant
    Filed: August 7, 1997
    Date of Patent: August 3, 1999
    Assignee: Neurogen Corporation
    Inventors: Xiao-shu He, Brian de Costa, Jan W. F. Wasley
  • Patent number: 5856318
    Abstract: Certain nitrogen-containing cyclohetero cycloalkylaminoaryl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein each of R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrido, lower alkyl, benzyl, and haloloweralkyl;wherein each of R.sup.2, R.sup.3 and R.sup.8 through R.sup.11 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein n is an integer of from four to six; wherein m is an integer of from two to four; wherein A is selected from phenyl, naphthyl, benzothienyl, benzofuranyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 11, 1997
    Date of Patent: January 5, 1999
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Wayne Bowen, Brian R. de Costa, Celia Dominguez, Xiao-Shu He, Kenner C. Rice
  • Patent number: 5744472
    Abstract: Disclosed are compounds of the formula ##STR1## or the pharmaceutically acceptable salts thereof wherein the 6-membered A ring may be optionally substituted with up to four groups independently selected from halogen, hydroxy, lower alkyl, or lower alkoxy;Ar represents optionally substituted aryl or heteroarylZ represents carbon or nitrogen provided thatwhere Z is carbon, R.sub.11 represents hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy, or phenyl optionally substituted with one or two groups selected from hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy; andwhere Z is nitrogen, R.sub.11 represents an electron pair;R.sub.5 is hydrogen or lower alkyl;L and m represent integers;n is 0, or an integer;R.sub.12 and R.sub.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: April 28, 1998
    Assignee: Neurogen Corporation
    Inventors: Xiao-shu He, Brian de Costa, Jan W. F. Wasley
  • Patent number: 5679679
    Abstract: Certain aralkyl diazabicyloalkyl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein: each of R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from the group consisting of hydrido, loweralkyl, benzyl and haloloweralkyl;each of R.sup.2, R.sup.3, and R.sup.8 through R.sup.
    Type: Grant
    Filed: December 2, 1994
    Date of Patent: October 21, 1997
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Wayne Bowen, Brian R. de Costa, Celia Dominguez, Xiao-Shu He, Kenner C. Rice
  • Patent number: 5679673
    Abstract: Certain aralkyl diazabicycloalkyl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein each of R, R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrido, lower-alkyl, benzyl, and haloloweralkyl; wherein each of R.sup.2, R.sup.3 and R.sup.10 through R.sup.13 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein each of R.sup.8 and R.sup.
    Type: Grant
    Filed: November 21, 1994
    Date of Patent: October 21, 1997
    Assignee: The United States of America, represented by the Department of Health and Human Services
    Inventors: Wayne Bowen, Brian R. de Costa, Celia Dominguez, Xiao-Shu He, Kenner C. Rice
  • Patent number: 5656632
    Abstract: Disclosed are compounds of the formula ##STR1## or the pharmaceutically acceptable salts thereof wherein the 6-membered A ring may be optionally substituted with up to four groups independently selected from halogen, hydroxy, lower alkyl, or lower alkoxy;Ar represents optionally substituted aryl or heteroarylZ represents carbon or nitrogen provided thatwhere Z is carbon, R.sub.11 represents hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy, or phenyl optionally substituted with one or two groups selected from hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy; andwhere Z is nitrogen, R.sub.11 represents an electron pair;R.sub.5 is hydrogen or lower alkyl;L and m represent integers;n is 0, or an integer;R.sub.12 and R.sub.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: August 12, 1997
    Assignee: Neurogen Corporation
    Inventors: Xiao-shu He, Brian de Costa, Jan W. F. Wasley
  • Patent number: 5656625
    Abstract: Certain nitrogen-containing cyclohetero cycloalkylaminoaryl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein each of R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrido, lower alkyl, benzyl, and haloloweralkyl;wherein each of R.sup.2, R.sup.3 and R.sup.8 through R.sup.11 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein n is an integer of from four to six; wherein m is an integer of from two to four; wherein A is selected from phenyl, naphthyl, benzothienyl, benzofuranyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 17, 1995
    Date of Patent: August 12, 1997
    Assignees: The United States of America as represented by the Department of Health and Human Services, Brown University Research Foundation
    Inventors: Wayne Bowen, Brian R. de Costa, Celia Dominguez, Xiao-Shu He, Kenner C. Rice
  • Patent number: 5602168
    Abstract: Disclosed are compounds of the formula ##STR1## or the pharmaceutically acceptable salts thereof wherein the 6-membered A ring may be optionally substituted with up to four groups independently selected from halogen, hydroxy, lower alkyl, or lower alkoxy;Ar represents optionally substituted aryl or heteroarylZ represents carbon or nitrogen provided thatwhere Z is carbon, R.sub.11 represents hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy, or phenyl optionally substituted with one or two groups selected from hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy; andwhere Z is nitrogen, R.sub.11 represents an electron pair;R.sub.5 is hydrogen or lower alkyl;L and m represent integers;n is 0, or an integer;R.sub.12 and R.sub.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: February 11, 1997
    Assignee: Neurogen Corporation
    Inventors: Xiao-shu He, Brian de Costa, Jan W. F. Wasley