The Nitrogen Of The Hetero Ring Is Bonded Directly To Both Remaining Rings Of The Tricyclo Ring System (e.g., Dibenzo(b,e)(1,4)thiazepine, Etc.) Patents (Class 540/550)
  • Patent number: 8779126
    Abstract: A dye, having a structure represented by formula (1A): wherein A represents a group of atoms necessary for forming a ring together with the carbon-nitrogen bond; at least one of Y1A and Y2A represents an acidic group, in which when they each represent an acidic group, they may be the same as or different from each other, or when only one of them represents an acidic group, the other represents an electron-withdrawing group; D represents a group to give a dye; n represents an integer of 1 or greater; L represents a single bond or a divalent linking group; and Y3A represents an acidic group.
    Type: Grant
    Filed: October 29, 2009
    Date of Patent: July 15, 2014
    Assignee: Fujifilm Corporation
    Inventors: Katsumi Kobayashi, Keizo Kimura, Tatsuya Susuki, Hirotaka Satou, Yukio Tani
  • Patent number: 8163730
    Abstract: Compounds of formula 1: are disclosed, wherein V is CH2; W is S(O)m; m is the integer 0, 1 or 2; U is O, C(O), CR13R14 or NR15; where R13 is H, alkyl; R14 is H, OH, OR13 or OCOR13; R15 is H, alkyl, cycloalkyl, alkenyl, C(O)R13, C(O)OR13 or alkylaminocarbonyl; R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. These compounds are inhibitors of tumor necrosis factor-alpha (TNF-?) and are useful as medicaments for the treatment and prevention of disorders caused by increased TNF-? activity, in particular inflammations.
    Type: Grant
    Filed: August 11, 2010
    Date of Patent: April 24, 2012
    Assignee: Piramal Life Sciences Limited
    Inventors: Bansi Lal, Somesh Sharma, Usha Ghosh, Swati Bal-Tembe, Tulsidas More, Asha Kulkarni-Almeida, Sapna Parikh, Radha Bhaskar Panicker, Anagha Damre, Ravindra Gupte
  • Patent number: 8088918
    Abstract: The present invention relates to novel noncardiotoxic compounds and pharmaceutical compositions useful in the treatment of a variety of disorders including the treatment of depression, allergies, psychoses, cancer and gastrointestinal disorders. In particular, the present invention describes pharmaceutical compositions that mitigate life-threatening arrhythmias such as torsade de pointes. Torsade de pointes is a particular cardiac problem associated with many therapeutic agents and has been implicated as a possible cause of sudden death, particularly in those individuals with a past history of disturbances of cardiac rhythm, myocardial infarction, congenital repolarization abnormalities and cardiac risk factors such as hyperlipidemia and age. This arrhythmia is a variant of paroxysmal ventricular tachycardia associated with a prolonged QTc interval or prominent U waves on the ECG.
    Type: Grant
    Filed: August 9, 2005
    Date of Patent: January 3, 2012
    Assignee: Williamsburg Holdings LLC
    Inventor: Donald L. Barbeau
  • Publication number: 20110196147
    Abstract: This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula (I) wherein Q, J, L and Z are as defined in the specification.
    Type: Application
    Filed: April 4, 2011
    Publication date: August 11, 2011
    Inventors: Robert D├ęziel, Silvana Leit, Patrick Beaulieu, Yves Andre Chantigny, John Mancuso, Pierre Tessier, Gideon Shapiro, Richard Chesworth, David Smil
  • Publication number: 20100305094
    Abstract: Compounds of formula 1: are disclosed, wherein V is CH2; W is S(O)m; m is the integer 0, 1 or 2; U is O, C(O), CR13R14 or NR15; where R13 is H, alkyl; R14 is H, OH, OR13 or OCOR13; R15 is H, alkyl, cycloalkyl, alkenyl, C(O)R13, C(O)OR13 or alkylaminocarbonyl; R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. These compounds are inhibitors of tumor necrosis factor-alpha (TNF-?) and are useful as medicaments for the treatment and prevention of disorders caused by increased TNF-? activity, in particular inflammations.
    Type: Application
    Filed: August 11, 2010
    Publication date: December 2, 2010
    Applicant: Piramal Life Sciences Limited
    Inventors: Bansi Lal, Somesh Sharma, Usha Ghosh, Swati Bal-Tembe, Tulsidas More, Asha Kulkarni-Almeida, Sapna Parikh, Radha Panicker, Anagha Damre, Ravindra Gupte
  • Patent number: 7834001
    Abstract: Guanidine derivatives having a condensed tricyclic ring of formula 1: are disclosed, wherein U is C(O), CRaRb, O, NRa or S(O)m; V is CRaRb or NRa; W is S(O)m; wherein Ra is H, alkyl, cycloalkyl, alkenyl or aralkyl; Rb is H, alkyl, OH, ORa or OCORa, and m is the integer 0, 1 or 2; R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein with the proviso that at least one of R1, R2, R3, R4, R5, R6, R7 or R8 is guanidino or guanidino carbonyl. These derivatives are sodium-proton exchange inhibitors and are useful as medicaments for the treatment of, for example, organ disorders associated with ischemia and reperfusion, cardiac arrhythmia, cardiac hypertrophy, hypertension, cell proliferative disorders and diabetes.
    Type: Grant
    Filed: November 8, 2005
    Date of Patent: November 16, 2010
    Assignee: Piramal Life Sciences Limited
    Inventors: Bansi Lal, Swati Bal-Tembe, Usha Ghosh, Arun Kumar Jain, Tulsidas More
  • Publication number: 20090317328
    Abstract: Novel compounds of formula (I): suitable for use as in vivo imaging agents are provided as well as precursors suitable for the preparation of said compounds. The present invention also provides pharmaceuticals comprising the compounds and kits for the preparation of the pharmaceuticals. Furthermore, use of the compounds for imaging peripheral benzodiazepine receptors in a subject is provided, in particular for imaging pathological conditions in which PBR are upregulated, e.g. Parkinson's disease, multiple sclerosis, Alzheimer's disease and Huntington's disease, neuropathic pain, arthritis, asthma, atherosclerosis and cancer.
    Type: Application
    Filed: May 31, 2007
    Publication date: December 24, 2009
    Inventors: Erik Arstad, Edward George Robins, Yongjun Zhao
  • Patent number: 7320973
    Abstract: The present invention provides dihydrodiaryloxazepine derivative represented by the following formula [1], analogs thereof and pharmaceutical compositions containing them.
    Type: Grant
    Filed: December 1, 2003
    Date of Patent: January 22, 2008
    Assignee: Ajinomoto Co., Inc.
    Inventors: Katsutoshi Sakata, Takashi Tsuji, Munetaka Tokumasu, Kazuyoshi Takahashi, Shigeo Hirasawa, Junko Ezaki
  • Publication number: 20040214813
    Abstract: Disclosed herein is an antioxidant that is an alkylated iminodibenzyl of the general formula: 1
    Type: Application
    Filed: April 17, 2003
    Publication date: October 28, 2004
    Applicant: CROMPTON CORPORATION
    Inventors: Karl J. Duyck, Theodore E. Nalesnik
  • Publication number: 20040110742
    Abstract: The present invention provides dihydrodiaryloxazepine derivative represented by the following formula [1], analogs thereof and pharmaceutical compositions containing them. Those compounds have an excellent effect of improving functional diseases of gastrointestinal tracts.
    Type: Application
    Filed: December 1, 2003
    Publication date: June 10, 2004
    Applicant: Ajinomoto Co., Inc.
    Inventors: Katsutoshi Sakata, Takashi Tsuji, Munetaka Tokumasu, Kazuyoshi Takahashi, Shigeo Hirasawa, Junko Ezaki
  • Patent number: 6562808
    Abstract: 5,11-dihydrodibenzo[b,e][1,4]oxazepine derivatives of the following general formulae and analogs thereof have a calcium channel-antagonistic effect and they are effective in treating and preventing intestinal diseases such as abnormal motor function of digestive tracts, particularly, irritable bowel syndrome:
    Type: Grant
    Filed: March 10, 2000
    Date of Patent: May 13, 2003
    Assignee: Ajinomoto Co., Inc.
    Inventors: Katsutoshi Sakata, Takashi Tsuji, Noriko Sasaki, Kazuyoshi Takahashi
  • Patent number: 6528504
    Abstract: The present invention provides (R)-5,11-dihydro-5-[1-(4-methoxyphenethyl)piperidine-2-ylmethyl]dibenzo[b,e][1,4]oxazepine, (R)-5,11-dihydro-5-[1-(4-dimethylaminophenethyl)piperidine-2-ylmethyl]dibenzo[b,e][1,4]oxazepine, compounds analogous to them and pharmaceutical compositions containing such a compound. These compounds are useful for treating or preventing abnormal motor functions of gastrointestinal tracts, particularly irritable bowel syndrome.
    Type: Grant
    Filed: July 9, 2001
    Date of Patent: March 4, 2003
    Assignee: Ajinomoto Co., Inc.
    Inventors: Katsutoshi Sakata, Takashi Tsuji, Noriko Sasaki, Kazuyoshi Takahashi
  • Publication number: 20020133004
    Abstract: A process for producing a 5-substituted-5,11-dihydro-debenzo [b,e] [1,4] oxazepine compound, wherein a [2-(2-bromobenzyloxy)phenyl]amide derivative having a substituent introduced through amido bond, the substituent locating at the 5-position of the final compound, as the starting material, is subjected to the intramolecular arylation and then the obtained product is reduced. In particular, (R)-1-[(4-methoxyphenyl)acetyl]pyrrolidine-2-carboxylic acid [2-(2-bromo benzyloxy)phenyl]amide is subjected to the intramolecular arylation to obtain (R)-[[2-(5,11-dihydro-dibenzo[b,e][1,4]oxazepine-5-carbonyl)pyrrolidin]-1-yl]-2-(4-methoxyphenyl)ethanone and then this product is reduced.
    Type: Application
    Filed: March 4, 2002
    Publication date: September 19, 2002
    Applicant: AJINOMOTO CO. INC
    Inventors: Takaaki Sekiyama, Toshihiro Matsuzawa, Takashi Yamamoto, Masanobu Yatagai, Junko Ezaki
  • Patent number: 6436922
    Abstract: Disclosed are 5,11-Dihydrodibenzo[b,e][1,4]oxazepine derivatives such as (R)-(+)-5,11-dihydro-5-[1-(4-methoxyphenethyl)-2-pyrrolidinylmethyl]dibenzo[b,e][1,4]oxazepine and (R)-(+)-5,11-dihydro-5-[1-(4-fluorophenethyl)-2-pyrrolidinylmethyl]dibenzo[b,e][1,4]oxazepine, stereoisomers thereof, pharmacologically acceptable salts thereof, or hydrates thereof and a pharmaceutical composition conating the 5,11-Dihydrodibenzo[b,e][1,4]oxazepine derivatives. The derivatives have an excellent activity of improving a digestive tract moving function and are free of side effect.
    Type: Grant
    Filed: June 19, 2000
    Date of Patent: August 20, 2002
    Assignee: Ajinomoto Co., Inc.
    Inventors: Yuji Tanaka, Keiji Misumi, Yoshinari Kawakami, Masahiko Moriguchi, Kazuyoshi Takahashi, Hiroki Okamoto, Toshiaki Kamisaki, Kimihiro Inoue, Makoto Sato
  • Patent number: 6127361
    Abstract: Disclosed are 5,11-Dihydrodibenzo[b,e][1,4]oxazepine derivatives such as (R)-(+)-5,11-dihydro-5-[1-(4-methoxyphenethyl)-2-pyrrolidinylmethyl]dibenz o[b,e][1,4]oxazepine and (R)-(+)-5,11-dihydro-5-[1-(4-fluorophenethyl)-2-pyrrolidinylmethyl]dibenzo [b,e][1,4]oxazepine, stereoisomers thereof, pharmacologically acceptable salts thereof, or hydrates thereof and a phramaceutical composition conating the 5,11-Dihydrodibenzo[b,e][1,4]oxazepine derivatives. The derivatives have an excellent activity of improving a digestive tract moving function and are free of side effect.
    Type: Grant
    Filed: September 11, 1998
    Date of Patent: October 3, 2000
    Assignee: Ajinomo Co., Inc.
    Inventors: Yuji Tanaka, Keiji Misumi, Yoshinari Kawakami, Masahiko Moriguchi, Kazuyoshi Takahashi, Hiroki Okamoto, Toshiaki Kamisaki, Kimihiro Inoue, Makoto Sato
  • Patent number: 6063779
    Abstract: An objective of the present invention is to provide a compound that has antiarrhythmic activity. The present invention provides a compound of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 each represent H, halogen or lower alkyl which may be substituted by halogen; A represents H, C3-6 cycloalkyl, phenyl which may be substituted by halogen, nitro, or lower alkoxy, a 5-membered or 6-membered heterocyclic ring which may contain N and/or S, --NR.sup.3 R.sup.4 (wherein R.sup.3 and R.sup.4 each represent H or lower alkyl which may be substituted by phenyl), or COR.sup.5 (wherein R.sup.5 represents OH, amino or lower alkoxy); Q represents S or O; m represents 0-18; and n represents 0-2, and pharmaceutically acceptable salts and solvates thereof.
    Type: Grant
    Filed: May 15, 1998
    Date of Patent: May 16, 2000
    Assignee: Meiji Seika Kaisha, Ltd.
    Inventors: Kiyoaki Katano, Takahiko Satoh, Tomoko Soneda, Naoko Kamitoh, Kazuyuki Fujishima, Mitsugu Hachisu
  • Patent number: 6015797
    Abstract: The object of the present invention is a pharmaceutical composition, which comprises, as active principle, a combination of an adenosinergic agonist and a compound selected from the opiates, benzodiazepines and NMDA antagonists.
    Type: Grant
    Filed: December 7, 1998
    Date of Patent: January 18, 2000
    Assignee: Laboratoires UPSA
    Inventors: Francoise Camborde, Alix Cloarec, Timur Gungor, Jean-Marie Teulon
  • Patent number: 6008213
    Abstract: Compounds of formula (I) ##STR1## wherein A.sub.1 is C or N; E is a five- or six-membered heteroaromatic or six-membered aromatic ring optionally substituted by R.sup.3 or R.sup.4 ; X.sup.1 --X.sup.2 is CHR.sup.1 --CH, CR.sup.1 .dbd.CH, NR.sup.1 --CH, S(O).sub.u --CH or O--CH; X.sup.3 is CR.sup.5 R.sup.5 ', NR.sup.5, S(O).sub.u or O; R.sup.2 is --OR', --NR'R", --NR'SO.sub.2 R'", --NR'OR', --OCR'.sub.2 C(O)OR', --OCR'.sub.2 OC(O)--R', --OCR'.sub.2 C(O)NR'.sub.2, CF.sub.3 or --COCR'.sub.2 R.sup.2 '; R.sup.3, R.sup.4 and R.sup.7 are independently H, halo, --OR.sup.12, --SR.sup.12, --CN, --NR'R.sup.12, --NO.sub.2, --CF.sub.3, CF.sub.3 S(O).sub.r --, --CO.sub.2 R', --CONR'.sub.2, R.sup.14 --C.sub.0-6 alky-, R.sup.14 --C.sub.1-6 oxoalkyl-, R.sup.14 --C.sub.2-6 alkenyl-, R.sup.14 --C.sub.2-6 alkynyl-, R.sup.14 --C.sub.0-6 alkyloxy-, R.sup.14 --C.sub.0-6 alkylamino- or R.sup.14 --C.sub.0-6 alkyl--S(O).sub.r --; R.sup.6 is W--(CR'.sub.2).sub.q --Z--(CR'R.sup.10)--U--(CR'.sub.2).sub.s --V-- or W'--(CR'.sub.2).sub.
    Type: Grant
    Filed: December 19, 1997
    Date of Patent: December 28, 1999
    Assignee: SmithKline Beecham Corporation
    Inventors: William E. Bondinell, William H. Miller
  • Patent number: 6004983
    Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxcylic acids of the general formula wherein X, Y, Z, R.sup.1, R.sup.2 and r are as defined in the detailed part of the description, or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for treatment of indications caused by or related to the secretion and circulation of insulin antagonising peptides.
    Type: Grant
    Filed: October 3, 1997
    Date of Patent: December 21, 1999
    Assignee: Novo Nordisk A/S
    Inventors: Henrik Sune Andersen, Tine Krogh J.o slashed.rgensen, Rolf Hohlweg, Knud Erik Andersen, Zdenek Polivka, Frantisek Miksik
  • Patent number: 5846968
    Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.
    Type: Grant
    Filed: May 27, 1997
    Date of Patent: December 8, 1998
    Assignee: Novo Nordisk A/S
    Inventors: Tine Krogh J.o slashed.rgensen, Knud Erik Andersen, Henrik Sune Andersen, Rolf Hohlweg, Peter Madsen, Uffe Bang Olsen
  • Patent number: 5721254
    Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.
    Type: Grant
    Filed: October 18, 1995
    Date of Patent: February 24, 1998
    Assignee: Novo Nordisk A/S
    Inventors: Knud Erik Andersen, Uffe Bang Olsen, Hans Petersen, Frederik Christian Gr.o slashed.nvald, Ursula Sonnewald, Tine Krogh J.o slashed.rgensen, Henrik Sune Andersen
  • Patent number: 5716949
    Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.
    Type: Grant
    Filed: March 28, 1996
    Date of Patent: February 10, 1998
    Assignee: Novo Nordisk A/S
    Inventors: Henrik Sune Andersen, Knud Erik Andersen, Rolf Hohlweg, Peter Madsen, Tine Krogh J.o slashed.rgensen, Uffe Bang Olsen
  • Patent number: 5693649
    Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.
    Type: Grant
    Filed: October 18, 1995
    Date of Patent: December 2, 1997
    Assignee: Novo Nordisk A/S
    Inventors: Knud Erik Andersen, Uffe Bang Olsen, Hans Petersen, Frederik Christian Gr.o slashed.nvald, Ursula Sonnewald, Tine Krogh J.o slashed.rgensen, Henrik Sune Andersen
  • Patent number: 5688788
    Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.
    Type: Grant
    Filed: May 18, 1995
    Date of Patent: November 18, 1997
    Assignee: Novo Nordisk A/S
    Inventors: Knud Erik Andersen, Uffe Bang Olsen, Hans Petersen, Frederik Christian Gr.o slashed.nvald, Ursula Sonnewald, Tine Krogh J.o slashed.rgensen, Henrik Sune Andersen
  • Patent number: 5674116
    Abstract: An abrasive machining assembly (10) wherein a worktable (14) is rotatably supported on a frame (12) for rotation about a table axis (A) and a plurality of platens (32) are supported on the worktable (14) with each of the platens (32) being adapted for supporting a workpiece to be machined by a machining disc (38) rotating about a tool axis (B). Each platen (32) is rotatably supported for rotation about a platen axis (C) which is radially spaced from the table axis (A) a different distance than the tool axis (B) whereby each of the platens (32) rotates about a platen axis (C) which is parallel to and offset from the tool axis (B) when positioned in the workstation.
    Type: Grant
    Filed: October 9, 1996
    Date of Patent: October 7, 1997
    Assignee: CMI International Inc.
    Inventors: Daniel L. Merrill, John R. Synder, Chuck O. Eckholm, Jr., Steve M. Sunday, John L. Seaver
  • Patent number: 5668129
    Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.
    Type: Grant
    Filed: March 27, 1996
    Date of Patent: September 16, 1997
    Assignee: Novo Nordisk A/S
    Inventors: Knud Erik Andersen, Uffe Bang Olsen, Hans Petersen, Frederik Christian Gr.o slashed.nvald, Ursula Sonnewald, Tine Krogh J.o slashed.rgensen, Henrik Sune Andersen
  • Patent number: 5602120
    Abstract: Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 - - - is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--;Y is selected from CH and N;Z is cyanoR.sub.1 represents C.sub.1-4 alkyl;m is 0, 1, 2 or 3;n is 0, 1 or 2;q is 1 or 2; andD is a 5, 6 or 7-membered, saturated or unsaturated, homo- or heterocyclic ring; and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the D4 receptor is implicated, such as schizophrenia, is also described.
    Type: Grant
    Filed: December 12, 1994
    Date of Patent: February 11, 1997
    Assignee: Allelix Biopharmaceuticals, Inc.
    Inventors: Jian-Min Fu, Ashok Tehim, Robert A. Kirby
  • Patent number: 5602124
    Abstract: Described herein are 5-HT2 receptor-selective compounds of Formula I: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 - - - is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--;R.sub.1 is C.sub.1-6 alkyl optionally substituted with a substituent selected from OH, halo, C.sub.1-4 alkyl and C.sub.1-4 alkoxy; andR.sub.2, R.sub.3 and R.sub.4 are independently selected from H and R.sub.1 ;and acid addition salts, solvates and hydrates thereof.
    Type: Grant
    Filed: December 12, 1994
    Date of Patent: February 11, 1997
    Assignee: Allelix Biopharmaceuticals, Inc.
    Inventors: Ashok Tehim, Jian-Min Fu, Sumanas Rakhit
  • Patent number: 5576314
    Abstract: Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N-C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 - - - is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--;n is 1 or 2;R.sub.1 is selected from H and an amino acid side chain;R.sub.2 is selected from H, OH, C.sub.1-9 alkyl, C.sub.1-9 alkoxy, and benzyloxy; andR.sub.3 is selected from H, OH, halo, cyano, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, phenoxy, benzyloxy, .dbd.O, .dbd.S, C.sub.1-4 alkylsulfonyl, C.sub.1-4 alkylsulfonyl, C.sub.1-4 alkylthio, amino, and aminocarbonyl;and acid addition salts, solvates and hydrates thereof.
    Type: Grant
    Filed: December 12, 1994
    Date of Patent: November 19, 1996
    Assignee: Allelix Biopharmaceuticals Inc.
    Inventors: Patricia L. Power, Sumanas Rakhit
  • Patent number: 5504077
    Abstract: The present invention provides substituted dibenzoxazepine and dibenzthiazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
    Type: Grant
    Filed: February 22, 1995
    Date of Patent: April 2, 1996
    Assignee: G. D. Searle & Co.
    Inventors: Joe T. Collins, Donald W. Hansen, Jr., Karen H. Peterson, Barnett S. Pitzele, David B. Reitz
  • Patent number: 5464767
    Abstract: Immunoassay methods and reagents for the quantification of total doxepins (i.e., E-doxepin, Z-doxepin, E-desmethyldoxepin, and Z-desmethyldoxepin) in a test sample are disclosed. The quantification of total doxepins is accomplished in an immunoassay employing antibodies and labeled reagents prepared with doxepin derivatives of the Formula II: ##STR1## wherein Y-Z can be C=CH or N-CH.sub.2, R.sub.1 is a linking group, R.sub.2 can be H or CH.sub.3, and Q can be a detectable moiety or an immunogenic carrier material. The antibody reagent comprises antibodies which are capable of binding to total doxepins and which are produced with one or more immunogens prepared from the doxepin derivative of Formula II, and the labeled reagent is also prepared from the doxepin derivative of Formula II.
    Type: Grant
    Filed: April 12, 1994
    Date of Patent: November 7, 1995
    Assignee: Abbott Laboratories
    Inventors: Maciej Adamczyk, Jeffrey R. Fishpaugh, Donald Johnson, Robert E. Hruska
  • Patent number: 5204348
    Abstract: Novel heterocyclic compounds, which are represented by the following general formula, useful as anticancer drug potentiaters having a potentiating effect on the incorporation of anticancer drugs into cancer cells, the compounds each synthesized by, for example, reacting a epoxy compound obtained by reacting a heterocyclic compound with an epihalogenohydrin, with an amine derivative.
    Type: Grant
    Filed: December 3, 1991
    Date of Patent: April 20, 1993
    Assignee: Mitsui Toatsu Chemicals Inc.
    Inventors: Nobuyuki Fukazawa, Makoto Odate, Tsuneji Suzuki, Kengo Otsuka, Takashi Tsuruo, Wakao Sato
  • Patent number: 5104868
    Abstract: This invention relates to novel tricyclic derivatives of 7-substituted-6-fluoro-1,4-dihydroquinol-4-one-3-carboxylic acids and certain esters and cation salts thereof. The compounds of this invention are substituted at the 7-position by vinyl, W--CH.dbd.CH--, CH.sub.3 C.tbd.C--, W--CH.sub.2 C.tbd.C-- or ##STR1## where W is selected from certain substituted alkyl groups. This invention also relates to antibacterial compositions containing the compounds and methods of using the compounds to treat bacterial disease.
    Type: Grant
    Filed: August 29, 1990
    Date of Patent: April 14, 1992
    Assignee: Pfizer Inc.
    Inventor: Paul R. McGuirk
  • Patent number: 5071844
    Abstract: The invention provides compounds of the formula: ##STR1## wherein k is 1, 2 or 3;m is 1, 2 or 3;n is 1, 2 or 3;p is 0, 1 or 2;X is O, S or a direct link, with the proviso that when X is O or S, n is 2 or 3;R.sup.1 is H or C.sub.1-C.sub.4 alkyl; andR.sup.2 is an optionally substituted phenyl or heteroaryl group; andpharmaceutically acceptable salts thereof.These compounds are useful for the treatment of motility disorders, particularly those of the gut such as irritable bowel syndrome.
    Type: Grant
    Filed: May 23, 1990
    Date of Patent: December 10, 1991
    Assignee: Pfizer Inc.
    Inventors: David Alker, Robert J. Bass, Peter E. Cross
  • Patent number: 5026856
    Abstract: Isoindoline derivatives represented by the formula (I) and their salts are disclosed. ##STR1## There are many varieties for the compound depending on the types of residues R.sup.1 -R.sup.9 and X. The compounds can be prepared from quinoline derivatives of the formula (II) and an isoindoline derivatives of the formula (III). The compounds of formula (I) and their salts have excellent antibacterial activities against both gram positive and gram negative microorganisms. They can be used as a medicine, an agrichemical, and a food preservative.
    Type: Grant
    Filed: May 23, 1989
    Date of Patent: June 25, 1991
    Assignee: Wakunaga Seiyaku Kabushiki Kaisha
    Inventors: Takashi Yatsunami, Akira Yazaki, Satoshi Inoue, Hitoshi Yamamoto, Masaharu Yokomoto, Jun Nomiyama, Shuichiro Noda
  • Patent number: 4888335
    Abstract: Propylamines of the formula (I): ##STR1## and isomers thereof, particularly those enantiomers and racemates relative to the chiral carbon indicated by an asterisk (*). The propylamines can be used for the treatment of hypertension or angina in humans. A is pyrrolidine, piperidine or morpholine, Z is alkylene, alkenylene, oxygen or a sulfur atom and W is an oxygen or a sulfur atom.
    Type: Grant
    Filed: July 25, 1988
    Date of Patent: December 19, 1989
    Assignee: McNeilab, Inc.
    Inventors: Richard J. Mohrbacher, Philip P. Grous
  • Patent number: 4762831
    Abstract: A process for the preparation of a 1,8-bridged 4-quinolone-3-carboxylic acid of the formula ##STR1## wherein the substituents are defined hereinbelow. Some of the compound are new. The old and new compounds are antibacterials and promote animal growth.
    Type: Grant
    Filed: June 13, 1986
    Date of Patent: August 9, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus Grohe, Michael Schriewer
  • Patent number: 4668671
    Abstract: This invention describes tricyclic derivatives which are useful as histamine H.sub.1 -antagonists. A particular compound of this invention is 3-[3-(pyrido[3,2-b][1,4]-benzothiazin-10-yl)propylamino]-4-(pyrid-4-ylmeth ylamino)-1,2,5-thiadiazole-1-oxide.
    Type: Grant
    Filed: April 23, 1986
    Date of Patent: May 26, 1987
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Andrew D. Gribble, Robert J. Ife