Tetracyclo Ring System Having The Diazine Ring As One Of The Cyclos (e.g., Benzophenazines, Etc.) Patents (Class 544/343)
  • Patent number: 7265119
    Abstract: The present invention is directed to the tartrate salts of 5,8,14-triazatetracyclo[10.3.1.02,11.04,9]-hexadeca-2(11),3,5,7,9-pentaene: and pharmaceutical compositions thereof. The present invention in particular is directed to the L-tartrate salt, and further to the various polymorphs of the L-tartrate salt, including two distinct anhydrous polymorphs (referred to herein as Forms A and B) and a hydrate polymorph (referred to herein as Form C). In addition, the present invention is also directed to the D-tartrate salt of 5,8,14-triazatetracyclo[10.3.1.02,11.04,9]-hexadeca-2(11),3,5,7,9-pentaene and the various polymorphs thereof; as well as the D,L-tartrate salt thereof and its polymorphs, and the meso-tartrate salt thereof and its polymorphs.
    Type: Grant
    Filed: February 28, 2005
    Date of Patent: September 4, 2007
    Assignee: Pfizer Inc
    Inventors: David E. Bogle, Glenn R. Williams, Peter R. Rose
  • 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
  • Patent number: 7235662
    Abstract: Novel non-steroidal compounds are provided which are glucocorticoid receptor modulators which are useful in treating diseases requiring glucocorticoid receptor agonist or antagonist therapy such as obesity, diabetes, inflammatory and immune disorders, and have the structure where R1–R9, X, Y and Z are defined herein.
    Type: Grant
    Filed: June 10, 2004
    Date of Patent: June 26, 2007
    Assignee: Bristol-Myers Squibb Company
    Inventors: Sara Sabine Hadida-Ruah, Xiaohui He, Johnny Yasuo Nagasawa
  • Patent number: 7223863
    Abstract: The present invention relates an improved process for the preparation of tetrahydro-?-carboline derivative of formula (V) which is useful as an intermediate for the preparation of Tadalafil of formula (I).
    Type: Grant
    Filed: July 25, 2006
    Date of Patent: May 29, 2007
    Assignee: Alembic Limited
    Inventors: Pandurang Balwant Deshpande, Bharat Becharbhai Boda, Sachin Surendra Surti, Pranay Pravinchandra Shah
  • Patent number: 7205300
    Abstract: This invention is directed to compounds of the formula (I): and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are as defined herein; intermediates for the synthesis of such compounds, pharmaceutical compositions containing such compounds; and methods of using such compounds in the treatment of neurological and psychological disorders.
    Type: Grant
    Filed: January 3, 2003
    Date of Patent: April 17, 2007
    Assignee: Pfizer Inc
    Inventors: Jotham Wadsworth Coe, Paige Roanne Palmer Brooks
  • Patent number: 7183282
    Abstract: The present invention is directed to compounds useful for treating addictive behavior and sleep disorders represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6a, R6b, R7, R8, R9, X, b, k, m, and n, and the dashed lines are described herein. The compounds used in the method of treatment of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including addictive behavior and sleep disorders.
    Type: Grant
    Filed: March 14, 2006
    Date of Patent: February 27, 2007
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Albert J. Robichaud, Taekyu Lee, Wei Deng, Ian S. Mitchell, Michael G. Yang, Simon Haydar, Wenting Chen, Christopher D. McClung, Emilie J. Calvello, David M. Zawrotny
  • Patent number: 7144882
    Abstract: This invention is directed to compounds of the formula (I): and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are as defined herein; intermediates for the synthesis of such compounds, pharmaceutical compositions containing such compounds; and methods of using such compounds in the treatment of neurological and psychological disorders.
    Type: Grant
    Filed: January 3, 2003
    Date of Patent: December 5, 2006
    Assignee: Pfizer Inc
    Inventors: Jotham Wadsworth Coe, Paige Roanne Palmer Brooks
  • Patent number: 7132419
    Abstract: A compound which is a benzo[a]phenazine-11-carboxamide derivative of formula (I) wherein each of R1 to R4, which are the same or different, is selected from hydrogen, halogen, hydroxyl, C1–C6 alkoxy which is unsubstituted or substituted, heteroaryloxy, C1–C6 alkyl which is unsubstituted or substituted, nitro, cyano, azido, amidoxime, CO2R10, CON(R12)2, OCON(R12), SR10, SOR11, SO2R11, SO2N(R12)2, N(R12)2, NR10SO2R11, N(SO2R11)2 NR10(CH2)nCN, NR10COR11, OCOR11 or COR10; each of R5 to R7, which are the same or different, is selected from hydrogen, halogen, hydroxy, C1–C6 alkoxy, C1–C6 alkyl, SR10 and N(R12)2; Q is C1–C6 alkylene which is unsubstituted or substituted by (i) C1–C6 alkyl which is unsubstituted or substituted, (ii) hydroxy, provided that the hydroxy group is not ? to either of the N atoms adjacent to Q in formula (I), (iii) CO2R10, or (iv) CON(R12); R8 and R9, which are the same or different, are each hydrogen or C1–C6 alkyl, or R8 and R9 together with the nitrogen atom to which they are attach
    Type: Grant
    Filed: December 30, 2004
    Date of Patent: November 7, 2006
    Assignee: Xenova Limited
    Inventors: John Milton, Nigel Vicker, Adrian Folkes, Shouming Wang, William Alexander Denny
  • Patent number: 7098209
    Abstract: Compounds of the general structural formula (I), and use of the compounds and salts and solvates thereof, as thereapeutic agents.
    Type: Grant
    Filed: April 15, 2002
    Date of Patent: August 29, 2006
    Assignee: Lilly Icos LLC
    Inventors: Mark W. Orme, Jason S. Sawyer, Lisa M. Schultze
  • Patent number: 7034027
    Abstract: Compounds of general structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents.
    Type: Grant
    Filed: July 9, 2001
    Date of Patent: April 25, 2006
    Assignee: Lilly Icos LLC
    Inventors: Mark W. Orme, Jason Scott Sawyer, Lisa M. Schultze
  • Patent number: 6984641
    Abstract: Selective inhibitors of cGMP-specific PDE, and use of the compounds and salts and solvates thereof as therapeutic agents, are disclosed.
    Type: Grant
    Filed: May 2, 2002
    Date of Patent: January 10, 2006
    Assignee: Lilly Icos LLC.
    Inventors: Mark W. Orme, Jason S. Sawyer, Alain C. Daugan, Agnes Bombrun, Françoise Gellibert, Lisa M. Schultze, Raymond F. Brown, Romain L. Gosmini
  • Patent number: 6962918
    Abstract: Compounds of the general structural formula (I), and use of the compounds and salts and solvates thereof, as therapeutic agents.
    Type: Grant
    Filed: September 17, 2001
    Date of Patent: November 8, 2005
    Assignee: Lilly Icos LLC.
    Inventors: Mark W. Orme, Lisa M. Schultze, Jason Scott Sawyer, Alain Claude-Marie Daugan, Raymond Brown
  • Patent number: 6962936
    Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: where Ht, R2, T, and m are as described in the specification. The compounds are useful for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.
    Type: Grant
    Filed: April 26, 2002
    Date of Patent: November 8, 2005
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Michael R. Hale, Francois Maltais
  • Patent number: 6960585
    Abstract: Compounds of formula (I), or pharmaceutically-acceptable salts thereof, are useful in treating inflammatory and immune diseases and disorders, wherein X, Y1, Y2, and R2-4 are as defined in the specification.
    Type: Grant
    Filed: September 27, 2001
    Date of Patent: November 1, 2005
    Assignee: Bristol-Myers Squibb Company
    Inventors: Francis Beaulieu, Carl Quellet, Makonen Belema, Yuping Qiu, Xuejie Yang, Fred C. Zusi
  • Patent number: 6951938
    Abstract: Pharmaceutical compositions comprising compounds of the formula and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are defined as in the specification, in combination with another therapeutic agent and methods of using such combinations in the treatment of neurological and psychological disorders.
    Type: Grant
    Filed: April 22, 2002
    Date of Patent: October 4, 2005
    Assignee: Pfizer Inc.
    Inventors: Jotham Wadsworth Coe, Paige Roanne Palmer Brooks
  • Patent number: 6933387
    Abstract: The present invention is directed to 1,2,3,4,10,10a-hexahydropyrazino [1,2-a]indole derivatives of formula (I): as well as pharmaceutically acceptable salts, hydrates and esters thereof, wherein the substituents have the meanings provided in the specification. Compounds of the present invention may be used in the treatment or prevention of obesity or Type II diabetes.
    Type: Grant
    Filed: March 25, 2003
    Date of Patent: August 23, 2005
    Assignees: Hoffmann-La Roche Inc., Vernalis Research Limited
    Inventors: Jonathan Mark Bentley, Paul Hebeisen, Marc Muller, Hans Richter, Stephan Roever
  • Patent number: 6911542
    Abstract: Compounds of the general structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents.
    Type: Grant
    Filed: May 15, 2001
    Date of Patent: June 28, 2005
    Assignee: Lilly Icos LLC.
    Inventors: Mark W. Orme, Jason Scott Sawyer, Lisa M. Schultze, Alain Claude-Marie Daugan, Francoise Gellibert
  • Patent number: 6903099
    Abstract: Compounds of the general structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents.
    Type: Grant
    Filed: May 15, 2001
    Date of Patent: June 7, 2005
    Assignee: Lilly Icos LLC
    Inventors: Mark W. Orme, Jason Scott Sawyer, Lisa M. Schultze
  • Patent number: 6897310
    Abstract: Pharmaceutical compositions comprising compounds of the formula and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are defined as in the specification, in combination with another therapeutic agent and methods of using such combinations in the treatment of neurological and psychological disorders.
    Type: Grant
    Filed: April 23, 2002
    Date of Patent: May 24, 2005
    Assignee: Pfizer Inc
    Inventors: Jotham Wadsworth Coe, Paige Roanne Palmer Brooks
  • Patent number: 6897311
    Abstract: A process for the preparation of compound of formula (I A), decahydro-2a,4a,6a,8a-tetraazacyclopent[fg]accnaphthylene and the corresponding functionalized compounds of general formula (I), intermediates for the preparation of 1,4,7,10-tetraazacyclododecane (II A) and corresponding derivatives (II), by preparation of compounds of general formula (III) and subsequent reduction thereof.
    Type: Grant
    Filed: April 10, 2001
    Date of Patent: May 24, 2005
    Assignee: Bracco International BV
    Inventors: Maria Argese, Marino Brocchetta, Giuseppe Manfredi, Fabrizio Rebasti, Giorgio Ripa
  • Patent number: 6890927
    Abstract: The present invention is directed to the tartrate salts of 5,8,14-triazatetracyclo[10.3.1.02,11.04,9]-hexadeca-2(11),3,5,7,9-pentaene: and pharmaceutical compositions thereof. The present invention in particular is directed to the L-tartrate salt, and further to the various polymorphs of the L-tartrate salt, including two distinct anhydrous polymorphs (referred to herein as Forms A and B) and a hydrate polymorph (referred to herein as Form C). In addition, the present invention is also directed to the D-tartrate salt of 5,8,14-triazatetracyclo[10.3.1.02,11.04,9]-hexadeca-2(11),3,5,7,9-pentaene and the various polymorphs thereof; as well as the D,L-tartrate salt thereof and its polymorphs, and the meso-tartrate salt thereof and its polymorphs.
    Type: Grant
    Filed: May 6, 2002
    Date of Patent: May 10, 2005
    Assignee: Pfizer Inc
    Inventors: David E. Bogle, Peter R. Rose, Glenn R. Williams
  • Patent number: 6878711
    Abstract: Compounds of the general structural formula and use of the compounds and salts and solvates thereof, as therapeutic agents.
    Type: Grant
    Filed: October 9, 2001
    Date of Patent: April 12, 2005
    Assignee: Lilly Icos LLC
    Inventors: Mark W. Orme, Jason Scott Sawyer, Lisa M. Schultze
  • Patent number: 6872721
    Abstract: Compounds of the general structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents.
    Type: Grant
    Filed: May 15, 2001
    Date of Patent: March 29, 2005
    Assignee: Lilly ICOS LLC
    Inventors: Mark W. Orme, Jason Scott Sawyer, Alain Claude-Marie Daugan
  • Patent number: 6844345
    Abstract: The present invention provides piperazine derivatives in accordance with formula (I) as well as salts, hydrates and esters thereof. The substituent designations are as provided in the specification. The compounds of the present invention can be used in the treatment of type II diabetes or obesity.
    Type: Grant
    Filed: March 7, 2002
    Date of Patent: January 18, 2005
    Assignees: Hoffman-La Roche Inc., Vernal Research Limited
    Inventors: Paul Hebeisen, Patrizio Mattei, Marc Muller, Hans Richter, Stephan Roever, Sven Taylor
  • Publication number: 20040266758
    Abstract: Novel non-steroidal compounds are provided which are glucocorticoid receptor modulators which are useful in treating diseases requiring glucocorticoid receptor agonist or antagonist therapy such as obesity, diabetes, inflammatory and immune disorders, and have the structure 1
    Type: Application
    Filed: June 10, 2004
    Publication date: December 30, 2004
    Inventors: Sara Sabine Hadida-Ruah, Xiaohui He, Johnny Yasuo Nagasawa
  • Patent number: 6821975
    Abstract: A compound of structural formula (I), and pharmaceutically acceptable salts and solvates thereof, wherein the compound is in free drug particulate form, is disclosed.
    Type: Grant
    Filed: July 19, 2002
    Date of Patent: November 23, 2004
    Assignee: Lilly ICOS LLC
    Inventors: Neil R. Anderson, Kerry J. Hartauer, Martha A. Kral, Gregory A. Stephenson
  • Publication number: 20040209864
    Abstract: The present invention is directed to methods of treating addictive behavior and sleep disorders by administering compounds represented by structural Formula (I) 1
    Type: Application
    Filed: February 25, 2004
    Publication date: October 21, 2004
    Inventors: Albert J. Robichaud, Taekyu Lee, Wei Deng, Ian S. Mitchell, Wenting Chen, Christopher D. McClung, Emilie J. Calvello, David M. Zawrotny
  • Patent number: 6794388
    Abstract: The present invention is directed to the succinate salts of 5,7,13-triazatetracyclo[9.3.1.02,10.04,8]-pentadeca-2(10),3,5,8-tetraene and pharmaceutical compositions thereof. The invention is also directed to a process for preparation of the succinate salts.
    Type: Grant
    Filed: November 27, 2002
    Date of Patent: September 21, 2004
    Assignee: Pfizer Inc.
    Inventors: George J. Quallich, Lewin T. Wint
  • Patent number: 6787549
    Abstract: The present invention is directed to the citrate salt of 5,8,14-triazatetracyclo[10.3.1.02,11.04,9]-hexadeca-2(11),3,5,7,9-pentaene: and pharmaceutical compositions thereof. The present invention is also directed to the various forms of the citrate salt, particularly its hydrate and its anhydrous/nearly anhydrous polymorph. The invention is also directed to processes for preparation of these citrate salt forms.
    Type: Grant
    Filed: May 6, 2002
    Date of Patent: September 7, 2004
    Assignee: Pfizer Inc.
    Inventors: Phillip J. Johnson, Peter R. Rose, Glenn R. Williams, Lewin T. Wint
  • Publication number: 20040169175
    Abstract: The present invention relates to electronic devices comprising an organic compound acting to inject or transport holes with p-type semi-conducting characteristics. The present invention provides for electronic devices comprising at least one or more layers selected from a group composed of a hole injecting layer, a hole transporting layer, and a hole injecting and transporting layer which comprises hexaazatriphenylene based organic compound represented by chemical formula (1), wherein the devices can use low drive-voltage, and can improve a light-emitting life.
    Type: Application
    Filed: March 10, 2004
    Publication date: September 2, 2004
    Applicant: LG CHEMICAL CO., LTD.
    Inventors: Se-Hwan Son, Ok-Hee Kim, Seok-Hee Yoon, Kong-Kyeom Kim, Youn-Gu Lee, Jae-Soon Bae
  • Publication number: 20040171830
    Abstract: Selective inhibitors of cGMP-specific PDE, and use of the compounds and salts and solvates thereof as therapeutic agents, are disclosed.
    Type: Application
    Filed: November 25, 2003
    Publication date: September 2, 2004
    Inventors: Mark W Orme, Jason S Sawyer, Alain C Daugan, Agnes Bombrun, Francois Gellibert, Lisa M Schultze, Raymond E Brown, Romain L Gosmini
  • Publication number: 20040162291
    Abstract: Compounds of structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents.
    Type: Application
    Filed: November 25, 2003
    Publication date: August 19, 2004
    Inventors: Mark W. Orme, Jason S. Sawyer, Lisa M. Schultze
  • Patent number: 6777406
    Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein is R1, R6a, R6b, R7, R8, R9, X, b, m, and n are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.
    Type: Grant
    Filed: December 19, 2001
    Date of Patent: August 17, 2004
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: John M. Fevig, Ian S. Mitchell, Taekyu Lee, Wenting Chen, Joseph Cacciola
  • Publication number: 20040157831
    Abstract: The present invention provides compounds of Formula (I): 1
    Type: Application
    Filed: February 3, 2004
    Publication date: August 12, 2004
    Applicant: Pharmacia & Upjohn Company
    Inventor: William W. McWhorter
  • Publication number: 20040152705
    Abstract: Compounds of the general structural formula (I), and use of the compounds and salts and solvates thereof, as thereapeutic agents. In particular, the invention relates to compounds that are potent and selective inhibitors of cyclic guanosine 3′, 5′-monophosphate specific phosphodiesterase (cGMP-specific PDE), in particular PDE5, and have utility in a variety of therapeutic areas wherein such inhibition is considered beneficial, including the treatment of cardiovascular disorders and erectile dysfunction.
    Type: Application
    Filed: November 24, 2003
    Publication date: August 5, 2004
    Inventors: Mark W. Orme, Jason S. Sawyer, Lisa M. Schultze
  • Publication number: 20040092502
    Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) 1
    Type: Application
    Filed: December 19, 2001
    Publication date: May 13, 2004
    Inventors: John M. Fevig, Ian S. Mitchell, Taekyu Lee, Wenting Chen, Joseph Cacciola
  • Patent number: 6723445
    Abstract: Electron transporting materials and organic light emitting devices utilizing the electron transporting materials, wherein the electron transporting materials are dibenzoquinoxaline compounds, and the devices utilize at least one layer incorporating a dibenzoquinoxaline compound. Dibenzoquinoxaline compounds include dipyridyl substituted dibenzoquinoxaline compounds, diphenyl substituted dibenzoquinoxaline compounds, naphthalene substituted dibenzoquinoxaline compounds, anthrene-dibeanzoquinoxaline compounds, bis(methoxy)phenyl substituted dibenzoquinoxaline compounds, dithiophen-dibenzoquinoxaline compounds, and dibenzoquinoxaline compounds.
    Type: Grant
    Filed: December 31, 2001
    Date of Patent: April 20, 2004
    Assignee: Canon Kabushiki Kaisha
    Inventors: Xiao-Chang Charles Li, Bing R. Hsieh
  • Patent number: 6699899
    Abstract: Imido and amido substituted acylhydroxamic acids which reduce the levels of TNF&agr; and inhibit phosphodiesterase in a mammal. A typical embodiment is (3-(1,3-dioxoisoindolin-2-yl)-3-(3-ethoxy-4-methoxyphenyl)propanoylamino)propanoate.
    Type: Grant
    Filed: December 21, 1999
    Date of Patent: March 2, 2004
    Assignee: Celgene Corporation
    Inventors: Hon-Wah Man, George W Muller, Shaei Y Huang
  • Patent number: 6689290
    Abstract: A mixture comprising a molecule of formula (I); in which A1, A2, A3, A4, A5 and A6, which may be the same or different, are each N or —CH; Y1, Y2, Y3, Y4, Y5 and Y6, which may be the same or different, are each hydrogen or C1 to C12 alkoxy; X1, X2, X3, X4, X5 and X6, which may be the same or different, are each hydrogen, C1 to C12 alkoxy or alkyl C1 to C12; and R7, R8, R9, R10, R11 and R12 are each hydrogen, or each of R7 and R8, R9 and R10 and R11 and R12 may form a bond; and a molecule of formula (II); in which R1, R2, R3, R4, R5 and R6, which may be the same or different, are each alkyl or substituted (and/or chiral) alkyl C1 to C16, acyl C1 to C16, polyethyleneoxy, a flexible connection to a polymer backbone or part of a polymer backbone in homopolymers, copolymers or block copolymers; and B1, B2, B3, B4, B5 and B6a, which may be the same or different, are each, hydrogen, alkyl C1 to C16, alkoxy C1 to C16, nitro, halogeno, cyano, amido, diazo or ester, e.g. alkyl C1 to C16 ester.
    Type: Grant
    Filed: January 13, 2003
    Date of Patent: February 10, 2004
    Assignee: The University of Leeds
    Inventors: Neville Boden, Richard James Bushby, Gareth Headdock, Owen Roger Lozman, Andrew Wood, Ekaterina Olegovna Arikanien, Andrew Paul McNeill, Zhibao Lu, Quayling Liu
  • Patent number: 6686349
    Abstract: The invention relates to novel tetracyclic pyrroloquinolone derivatives of the formula (I) or (II): wherein all variables are as herein defined, pharmaceutical compositions containing the compounds and their use for the treatment of sexual dysfunction.
    Type: Grant
    Filed: November 12, 2002
    Date of Patent: February 3, 2004
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Weiqin Jiang, Zhihua Sui
  • Publication number: 20040014974
    Abstract: A process for the preparation of compound of formula (I A), decahydro-2a,4a,6a,8a-tetraazacyclopent[fg]accnaphthylene and the corresponding functionalized compounds of general formula (1), intermediates for the preparation of 1,4,7,10-tetraazacyclododecane (II A) and corresponding derivatives (II), by preparation of compounds of general formula (III) and subsequent reduction thereof.
    Type: Application
    Filed: November 25, 2002
    Publication date: January 22, 2004
    Inventors: Maria Argese, Marino Brocchetta, Giuseppe Manfredi, Fabrizio Rebasti, Giorgio Ripa
  • Patent number: 6680326
    Abstract: Novel polycyclic compounds of the formula [I], wherein R1, R2, R3, R4, R5, R6, R7, ring A, ring B, X, Y and Z are as defined herein and the pharmaceutically acceptable salts thereof. These compounds have antitumor activity and useful for the treatment of cancer.
    Type: Grant
    Filed: September 25, 2002
    Date of Patent: January 20, 2004
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Tsunehisa Aoyama, Kenichi Kawasaki, Miyako Masubuchi, Tatsuo Ohtsuka, Kiyoaki Sakata
  • Patent number: 6673798
    Abstract: A purified tyrphostin of a general formula: wherein, for Compound I, R6 is either at position 6 or at position 7, or, for Compound II, R6 is either at position 6 or at position 8.
    Type: Grant
    Filed: April 9, 2001
    Date of Patent: January 6, 2004
    Assignee: Yissum Research Development Company of the Hebrew University of Jerusalem
    Inventors: Alexander Levitzki, Aviv Gazit, Shmuel Banai, David S. Gertz, Gershon Golomb, Frank D. Boehmer, Johannes Waltenberger
  • Publication number: 20030236263
    Abstract: Compounds of the general structural formula (I), and use of the compounds and salts and solvates thereof, as therapeutic agents.
    Type: Application
    Filed: February 27, 2003
    Publication date: December 25, 2003
    Inventors: Mark W. Orme, Lisa M. Schultze, Jason Scott Sawyer, Alain Claude-Marie Daugan, Raymond Brown
  • Patent number: 6667405
    Abstract: Disclosed is a compound represented by the following formula (I): wherein Z1 represents an atomic group necessary to form a 5- or 6-membered nitrogen-containing heterocyclic ring; Z2 represents an atomic group necessary to form a 5- or 6-membered heterocyclic ring, Z2 may further be substituted, or may be condensed with a hetero ring or a benzene ring; R1 represents a hydrogen atom, a halogen atom, a mercapto group, an alkyl group, an alkenyl group, an aryl group, an alkylthio group, an alkenylthio group, or an arylthio group; L1 and L2 each represents a methine group; p1 represents 0 or 1; V1 represents a substituent; and n represents 0, 1 or 2, and when n represents 2, a plurality of V1 may be the same or different.
    Type: Grant
    Filed: November 1, 2001
    Date of Patent: December 23, 2003
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Katsumi Kobayashi, Takashi Katoh, Junji Nishigaki
  • Publication number: 20030229080
    Abstract: Compounds of the general structural formula and use of the compounds and salts and solvates thereof, as therapeutic agents.
    Type: Application
    Filed: April 9, 2003
    Publication date: December 11, 2003
    Inventors: Mark W Orme, Jason Scott Sawyer, Lisa M Schultze
  • Publication number: 20030225092
    Abstract: Compounds of the general structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents.
    Type: Application
    Filed: December 3, 2002
    Publication date: December 4, 2003
    Inventors: Mark W. Orme, Jason Scott Sawyer, Alain Claude-Marie Daugan
  • Publication number: 20030225094
    Abstract: Compounds of the general structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents.
    Type: Application
    Filed: December 6, 2002
    Publication date: December 4, 2003
    Inventors: Mark W Orme, Jason scott Sawyer, LIsa M Schultze, Alain Claude-Marie Daugan, Francoise Gellibert
  • Patent number: 6653470
    Abstract: 1,4,7,10-Tetraazacyclodecane, a precursor for the synthesis of macrocylic chelating agents for metal ions such as gadolinium, is prepared efficiently as a highly pure product on an industrial scale.
    Type: Grant
    Filed: October 11, 2001
    Date of Patent: November 25, 2003
    Assignee: Bracco International B.V.
    Inventors: Maria Argese, Giuseppe Manfredi, Fabrizio Rebasti, Giorgio Ripa
  • Patent number: RE39680
    Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6a, R6b, R7, R8, R9, X, b, k, m, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.
    Type: Grant
    Filed: February 16, 2006
    Date of Patent: June 5, 2007
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Albert J. Robichaud, Taekyu Lee, Wei Deng, Ian S. Mitchell, Michael Guang Yang, Simon Haydar, Wenting Chen, Christopher D. McClung, Emile J. B. Calvello, David M. Zawrotny, Parthasarathl Rajagopalan