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: 8779126Abstract: 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: GrantFiled: October 29, 2009Date of Patent: July 15, 2014Assignee: Fujifilm CorporationInventors: Katsumi Kobayashi, Keizo Kimura, Tatsuya Susuki, Hirotaka Satou, Yukio Tani
-
Patent number: 8163730Abstract: 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: GrantFiled: August 11, 2010Date of Patent: April 24, 2012Assignee: Piramal Life Sciences LimitedInventors: 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: 8088918Abstract: 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: GrantFiled: August 9, 2005Date of Patent: January 3, 2012Assignee: Williamsburg Holdings LLCInventor: Donald L. Barbeau
-
Publication number: 20110196147Abstract: 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: ApplicationFiled: April 4, 2011Publication date: August 11, 2011Inventors: Robert Déziel, Silvana Leit, Patrick Beaulieu, Yves Andre Chantigny, John Mancuso, Pierre Tessier, Gideon Shapiro, Richard Chesworth, David Smil
-
Publication number: 20100305094Abstract: 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: ApplicationFiled: August 11, 2010Publication date: December 2, 2010Applicant: Piramal Life Sciences LimitedInventors: Bansi Lal, Somesh Sharma, Usha Ghosh, Swati Bal-Tembe, Tulsidas More, Asha Kulkarni-Almeida, Sapna Parikh, Radha Panicker, Anagha Damre, Ravindra Gupte
-
Patent number: 7834001Abstract: 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: GrantFiled: November 8, 2005Date of Patent: November 16, 2010Assignee: Piramal Life Sciences LimitedInventors: Bansi Lal, Swati Bal-Tembe, Usha Ghosh, Arun Kumar Jain, Tulsidas More
-
Publication number: 20090317328Abstract: 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: ApplicationFiled: May 31, 2007Publication date: December 24, 2009Inventors: Erik Arstad, Edward George Robins, Yongjun Zhao
-
Patent number: 7320973Abstract: The present invention provides dihydrodiaryloxazepine derivative represented by the following formula [1], analogs thereof and pharmaceutical compositions containing them.Type: GrantFiled: December 1, 2003Date of Patent: January 22, 2008Assignee: Ajinomoto Co., Inc.Inventors: Katsutoshi Sakata, Takashi Tsuji, Munetaka Tokumasu, Kazuyoshi Takahashi, Shigeo Hirasawa, Junko Ezaki
-
Publication number: 20040214813Abstract: Disclosed herein is an antioxidant that is an alkylated iminodibenzyl of the general formula: 1Type: ApplicationFiled: April 17, 2003Publication date: October 28, 2004Applicant: CROMPTON CORPORATIONInventors: Karl J. Duyck, Theodore E. Nalesnik
-
Publication number: 20040110742Abstract: 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: ApplicationFiled: December 1, 2003Publication date: June 10, 2004Applicant: Ajinomoto Co., Inc.Inventors: Katsutoshi Sakata, Takashi Tsuji, Munetaka Tokumasu, Kazuyoshi Takahashi, Shigeo Hirasawa, Junko Ezaki
-
Patent number: 6562808Abstract: 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: GrantFiled: March 10, 2000Date of Patent: May 13, 2003Assignee: Ajinomoto Co., Inc.Inventors: Katsutoshi Sakata, Takashi Tsuji, Noriko Sasaki, Kazuyoshi Takahashi
-
Patent number: 6528504Abstract: 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: GrantFiled: July 9, 2001Date of Patent: March 4, 2003Assignee: Ajinomoto Co., Inc.Inventors: Katsutoshi Sakata, Takashi Tsuji, Noriko Sasaki, Kazuyoshi Takahashi
-
Publication number: 20020133004Abstract: 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: ApplicationFiled: March 4, 2002Publication date: September 19, 2002Applicant: AJINOMOTO CO. INCInventors: Takaaki Sekiyama, Toshihiro Matsuzawa, Takashi Yamamoto, Masanobu Yatagai, Junko Ezaki
-
Patent number: 6436922Abstract: 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: GrantFiled: June 19, 2000Date of Patent: August 20, 2002Assignee: Ajinomoto Co., Inc.Inventors: Yuji Tanaka, Keiji Misumi, Yoshinari Kawakami, Masahiko Moriguchi, Kazuyoshi Takahashi, Hiroki Okamoto, Toshiaki Kamisaki, Kimihiro Inoue, Makoto Sato
-
Patent number: 6127361Abstract: 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: GrantFiled: September 11, 1998Date of Patent: October 3, 2000Assignee: Ajinomo Co., Inc.Inventors: Yuji Tanaka, Keiji Misumi, Yoshinari Kawakami, Masahiko Moriguchi, Kazuyoshi Takahashi, Hiroki Okamoto, Toshiaki Kamisaki, Kimihiro Inoue, Makoto Sato
-
Patent number: 6063779Abstract: 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: GrantFiled: May 15, 1998Date of Patent: May 16, 2000Assignee: Meiji Seika Kaisha, Ltd.Inventors: Kiyoaki Katano, Takahiko Satoh, Tomoko Soneda, Naoko Kamitoh, Kazuyuki Fujishima, Mitsugu Hachisu
-
Patent number: 6015797Abstract: 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: GrantFiled: December 7, 1998Date of Patent: January 18, 2000Assignee: Laboratoires UPSAInventors: Francoise Camborde, Alix Cloarec, Timur Gungor, Jean-Marie Teulon
-
Patent number: 6008213Abstract: 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: GrantFiled: December 19, 1997Date of Patent: December 28, 1999Assignee: SmithKline Beecham CorporationInventors: William E. Bondinell, William H. Miller
-
Patent number: 6004983Abstract: 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: GrantFiled: October 3, 1997Date of Patent: December 21, 1999Assignee: Novo Nordisk A/SInventors: Henrik Sune Andersen, Tine Krogh J.o slashed.rgensen, Rolf Hohlweg, Knud Erik Andersen, Zdenek Polivka, Frantisek Miksik
-
Patent number: 5846968Abstract: 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: GrantFiled: May 27, 1997Date of Patent: December 8, 1998Assignee: Novo Nordisk A/SInventors: Tine Krogh J.o slashed.rgensen, Knud Erik Andersen, Henrik Sune Andersen, Rolf Hohlweg, Peter Madsen, Uffe Bang Olsen
-
Patent number: 5721254Abstract: 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: GrantFiled: October 18, 1995Date of Patent: February 24, 1998Assignee: Novo Nordisk A/SInventors: 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: 5716949Abstract: 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: GrantFiled: March 28, 1996Date of Patent: February 10, 1998Assignee: Novo Nordisk A/SInventors: Henrik Sune Andersen, Knud Erik Andersen, Rolf Hohlweg, Peter Madsen, Tine Krogh J.o slashed.rgensen, Uffe Bang Olsen
-
Patent number: 5693649Abstract: 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: GrantFiled: October 18, 1995Date of Patent: December 2, 1997Assignee: Novo Nordisk A/SInventors: 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: 5688788Abstract: 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: GrantFiled: May 18, 1995Date of Patent: November 18, 1997Assignee: Novo Nordisk A/SInventors: 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: 5674116Abstract: 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: GrantFiled: October 9, 1996Date of Patent: October 7, 1997Assignee: CMI International Inc.Inventors: Daniel L. Merrill, John R. Synder, Chuck O. Eckholm, Jr., Steve M. Sunday, John L. Seaver
-
Patent number: 5668129Abstract: 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: GrantFiled: March 27, 1996Date of Patent: September 16, 1997Assignee: Novo Nordisk A/SInventors: 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: 5602120Abstract: 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: GrantFiled: December 12, 1994Date of Patent: February 11, 1997Assignee: Allelix Biopharmaceuticals, Inc.Inventors: Jian-Min Fu, Ashok Tehim, Robert A. Kirby
-
Patent number: 5602124Abstract: 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: GrantFiled: December 12, 1994Date of Patent: February 11, 1997Assignee: Allelix Biopharmaceuticals, Inc.Inventors: Ashok Tehim, Jian-Min Fu, Sumanas Rakhit
-
Patent number: 5576314Abstract: 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: GrantFiled: December 12, 1994Date of Patent: November 19, 1996Assignee: Allelix Biopharmaceuticals Inc.Inventors: Patricia L. Power, Sumanas Rakhit
-
Patent number: 5504077Abstract: 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: GrantFiled: February 22, 1995Date of Patent: April 2, 1996Assignee: G. D. Searle & Co.Inventors: Joe T. Collins, Donald W. Hansen, Jr., Karen H. Peterson, Barnett S. Pitzele, David B. Reitz
-
Patent number: 5464767Abstract: 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: GrantFiled: April 12, 1994Date of Patent: November 7, 1995Assignee: Abbott LaboratoriesInventors: Maciej Adamczyk, Jeffrey R. Fishpaugh, Donald Johnson, Robert E. Hruska
-
Patent number: 5204348Abstract: 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: GrantFiled: December 3, 1991Date of Patent: April 20, 1993Assignee: Mitsui Toatsu Chemicals Inc.Inventors: Nobuyuki Fukazawa, Makoto Odate, Tsuneji Suzuki, Kengo Otsuka, Takashi Tsuruo, Wakao Sato
-
Patent number: 5104868Abstract: 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: GrantFiled: August 29, 1990Date of Patent: April 14, 1992Assignee: Pfizer Inc.Inventor: Paul R. McGuirk
-
Patent number: 5071844Abstract: 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: GrantFiled: May 23, 1990Date of Patent: December 10, 1991Assignee: Pfizer Inc.Inventors: David Alker, Robert J. Bass, Peter E. Cross
-
Patent number: 5026856Abstract: 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: GrantFiled: May 23, 1989Date of Patent: June 25, 1991Assignee: Wakunaga Seiyaku Kabushiki KaishaInventors: Takashi Yatsunami, Akira Yazaki, Satoshi Inoue, Hitoshi Yamamoto, Masaharu Yokomoto, Jun Nomiyama, Shuichiro Noda
-
Patent number: 4888335Abstract: 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: GrantFiled: July 25, 1988Date of Patent: December 19, 1989Assignee: McNeilab, Inc.Inventors: Richard J. Mohrbacher, Philip P. Grous
-
Patent number: 4762831Abstract: 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: GrantFiled: June 13, 1986Date of Patent: August 9, 1988Assignee: Bayer AktiengesellschaftInventors: Klaus Grohe, Michael Schriewer
-
Patent number: 4668671Abstract: 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: GrantFiled: April 23, 1986Date of Patent: May 26, 1987Assignee: Smith Kline & French Laboratories LimitedInventors: Andrew D. Gribble, Robert J. Ife