Plural Nitrogens In The Polycyclo Ring System Patents (Class 540/577)
-
Publication number: 20030153552Abstract: An essentially pure noribogaine compound having the formula: 1Type: ApplicationFiled: February 14, 2002Publication date: August 14, 2003Inventors: Deborah C. Mash, Juan Sanchez-Ramos, William Lee Hearn
-
Publication number: 20030060458Abstract: The present invention provides compounds of Formula (I): 1Type: ApplicationFiled: July 11, 2002Publication date: March 27, 2003Inventors: Jian-Min Fu, Jeanette Kay Morris, Arthur Glenn Romero
-
Publication number: 20030018023Abstract: The present application describes 5-6 or 5-7 heterobicyclics of Formula I: 1Type: ApplicationFiled: March 25, 2002Publication date: January 23, 2003Inventors: Donald Joseph Philip Pinto, Renhua Li
-
Patent number: 6472403Abstract: The present invention relates to novel imidazolidinone derivatives thereof, their synthesis, and their use as &agr;v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3 and/or &agr;v&bgr;5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, inflammatory arthritis, viral disease, cancer, and metastatic tumor growth.Type: GrantFiled: January 19, 2001Date of Patent: October 29, 2002Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, Wasyl Halczenko, John H. Hutchinson, Aiwen Li, Robert S. Meissner, James J. Perkins, Thomas G. Steele, Jiabing Wang, Michael A. Patane
-
Publication number: 20020128475Abstract: The present invention are substituted 9-arylsulfone- 1,2,3,4,5,6-hexahydroazepino [4,5-b] indoles (X) and unsubstituted 9-arylsulfone- 1,2,3,4,5,6- hexahydroazepino[4,5-b]indoles (XI) such as the compound of EXAMPLE 13 which are useful in treating depression, obesity and other CNS disorders.Type: ApplicationFiled: October 30, 2001Publication date: September 12, 2002Applicant: Pharmacia & Upjohn CompanyInventors: Eric Jon Jacobsen, Susan Fax Jacobsen
-
Patent number: 6410526Abstract: The present invention relates to novel nonanoic acid derivatives, their synthesis, and their use as &agr;v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3 and &agr;v&bgr;5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, inflammatory arthritis, viral disease, cancer, and metastatic tumor growth.Type: GrantFiled: May 31, 2000Date of Patent: June 25, 2002Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, George D. Hartman, Robert S. Meissner, James J. Perkins
-
Publication number: 20020077318Abstract: The invention provides compounds of Formula (I): 1Type: ApplicationFiled: September 20, 2001Publication date: June 20, 2002Inventors: Kristine E. Frank, Brad A. Acker, Michael D. Ennis, Jed F. Fisher, Jian-min Fu, Eric Jon Jacobsen, William W. McWhorter, Jeanette K. Morris, Donald Joseph Rogier
-
Patent number: 6407092Abstract: The present invention provides compounds of formula I: wherein R1, R2, X and Y have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of formula (I).Type: GrantFiled: April 20, 2000Date of Patent: June 18, 2002Assignee: Pharmacia & Upjohn CompanyInventors: Jackson B. Hester, Bruce N. Rogers, Eric Jon Jacobsen, Michael D. Ennis, Brad A. Acker, Susan L. Vander Velde, Kristine E. Frank
-
Patent number: 6369222Abstract: The invention relates to nitro- and cyano-1,2,4,5-tetrahydro-heterocycloazepinyl pyrimidine derivatives as well as their pharmaceutically acceptable salts. The invention further relates to medicaments containing such compounds and a process for the preparation of such compounds. The compounds of the invention are group I mGluR antagonists and are therefore useful for the control or prevention of acute and/or chronic neurological disorders.Type: GrantFiled: July 11, 2001Date of Patent: April 9, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Alfred Binggeli, Hans-Peter Maerki, Vincent Mutel, Wolfgang Wostl
-
Publication number: 20020019390Abstract: This invention is directed to novel imidazole and imidazoline derivatives which are selective agonists for cloned human &agr;2 adrenergic receptors. This invention is also related to the use of these compounds for the treatment of any disease where modulation of the &agr;2 receptors may be useful. The invention further provides for a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: ApplicationFiled: August 20, 2001Publication date: February 14, 2002Applicant: Synaptic Pharmaceutical CorporationInventors: Wai C. Wong, Yoon T. Jeon, T.G. Murali Dhar, Charles Gluchowski
-
Patent number: 6340753Abstract: A novel optically active quarternary ammonium salt with an axial chirality is provided. The quarternary ammonium salt can act as a phase-transfer catalyst to convert glycine derivatives into optically active &agr;-amino acid derivatives by stereoselectively alkylating the glycine derivatives. Furthermore, according to the present invention, intermediates useful for producing the novel quarternary ammonium can be produced.Type: GrantFiled: July 13, 2000Date of Patent: January 22, 2002Assignee: Nagase & Co., Ltd.Inventor: Keiji Maruoka
-
Publication number: 20010051718Abstract: The present invention is directed to methods for the preparation of piperazine ring-containing compounds, particularly mirtazapine. According to the present invention, the mirtazapine intermediate 1-(3-carboxypyridyl-2)-4-methyl-2-phenyl-piperazine is made by hydrolyzing 1-(3-cyanopyridyl-2)-4-methyl-2-phenyl-piperazine with a base where the base is present in a ratio of up to about 12 moles of the base per one mole of 1-(3-cyanopyridyl-2)-4-methyl-2-phenyl-piperazine. The mirtazapine intermediate 1-(3-carboxypyridyl-2)-4-methyl-2-phenyl-piperazine may be made by hydrolyzing 1-(3-cyanopyridyl-2)-4-methyl-2-phenyl-piperazine with potassium hydroxide at a temperature of at least about 130° C.Type: ApplicationFiled: July 6, 2001Publication date: December 13, 2001Inventors: Claude Singer, Anita Liberman, Nina Finkelstein
-
Patent number: 6153608Abstract: The invention relates to a compound of the following general formula [I] or a medicinally acceptable salt thereof, or a solvate thereof, ##STR1## wherein R.sup.1 represents alkyl, alkenyl, alkynyl, alkoxy, hydroxy, cyano, or halogen; R.sup.2 represents hydrogen, hydroxy, or halogen; R.sup.3 represents hydrogen, alkyl, or amidino; Ring A represents a 5 to 11-membered cyclic amino group which may be substituted, which cyclic amino group may be bridged between two carbon atoms in optional positions. The compound of this invention is useful for the prevention or treatment of cerebral tissue impairment due to the vasospasm following cerebral hemorrhage.Type: GrantFiled: July 29, 1998Date of Patent: November 28, 2000Assignee: Nippon Shinyaku Co., Ltd.Inventors: Hiroyoshi Hidaka, Akira Matsuura, Takushi Matsuzaki
-
Patent number: 6130229Abstract: Compounds of Formula I: ##STR1## wherein: X.sup.1 is hydrogen, halogen, CF.sub.3, nitro, NH.sub.2 or lower alkyl;each X.sup.2 is independently selected from the group consisting of hydrogen, halogen, lower alkoxy and lower alkyl;n is 1 or 2;Y is selected from the group consisting of S(O).sub.p, O, and NR.sup.5, wherein p is 0, 1 or 2, and R.sup.5 is hydrogen, alkyl, aryl, cycloalkyl, loweralkoxycarbonyl, aminocarbonyl or acyl;R.sup.1 and R.sup.2, which may be the same or different, are selected from the group consisting of hydrogen and lower alkyl groups, or taken together can form an oxygen atom when Y is NR.sup.5 ;A . . . is C=, CH-- or N--;R is --CZ--Y.sup.1 --Y.sup.2 --R.sup.3, wherein:Z is O, =CH--CN, or =N--CN;one of Y.sup.1 and Y.sup.2 is a bond, --CO--, O, S, or --NR.sup.4 --, and the other is (CH.sub.2).sub.m, where m is 0 or an integer of 1 to 4, and R.sup.4 is H or alkyl, with the proviso that when Z is O and m is 0 then Y.sup.1 or Y.sup.2 is selected from --CO--, O, S, or --NR.sup.4 ;R.sup.Type: GrantFiled: October 7, 1997Date of Patent: October 10, 2000Assignee: Schering CorporationInventors: Adriano Afonso, Joseph M. Kelly, Stuart B. Rosenblum, Ronald L. Wolin, Jay Weinstein
-
Patent number: 5849731Abstract: The present invention relates to indole derivatives represented by the following compound 1 and the pharmacologically acceptable acid addition salt thereof. ##STR1## The compounds of the present invention were found to exhibit strong antitussive and analgesic actions as a result of pharmacological evaluation, and can be used in the pharmaceutical field as effective antitussives and analgesics.Type: GrantFiled: May 16, 1997Date of Patent: December 15, 1998Assignee: Toray Industries, Inc.Inventors: Hiroshi Nagase, Koji Kawai, Takashi Endo, Shinya Ueno, Masayuki Maeda, Satoshi Sakami
-
Patent number: 5808060Abstract: Disclosed are biologically active, non-indole-containing compounds referred to as fused isoindolones, which are represented by the following general formula: ##STR1## The fused indolones can be obtained by complete chemical synthesis. Methods for making and using the fused isoindolones are disclosed.Type: GrantFiled: December 9, 1996Date of Patent: September 15, 1998Assignee: Cephalon, Inc.Inventors: Robert L. Hudkins, Neil W. Johnson
-
Patent number: 5723606Abstract: This invention relates to nitrogen-containing aromatic 5-membered ring-condensed benzazepine derivatives represented by the general formula (I) ##STR1## (symbols in the formula have the following meanings; ring B: a nitrogen-containing aromatic 5-membered ring having at least 1 nitrogen atom and optionally one oxygen or sulfur atom, which may optionally have substituent(s), R.sup.1 and R.sup.2 : these may be the same or different from each other and each represents a hydrogen atom, a halogen atom, a lower alkyl group, an amino group which may optionally be substituted by lower alkyl group(s), or a lower alkoxy group,A: a single bond; a group represented by the formula--NHCO--(CR.sup.3 R.sup.4).sub.n --,n: 0 or an integer of from 1 to 3,R.sup.3 and R.sup.4 : these may be the same or different from each other and each represents a hydrogen atom, a lower alkyl group (provided that R.sup.3 and R.sup.Type: GrantFiled: January 19, 1996Date of Patent: March 3, 1998Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Akihiro Tanaka, Hiroyuki Koshio, Nobuaki Taniguchi, Akira Matsuhisa, Ken-ichiro Sakamoto, Atsuki Yamazaki, Takeyuki Yatsu
-
Carbocyclic and heterocyclic fused-ring quinolinecarboxylic acids useful as immunosuppressive agents
Patent number: 5639759Abstract: This invention relates to carbocyclic and heterocyclic fused-ring quinolinecarboxylic acid compounds, to pharmaceutical compositions comprising such compounds, and to methods of using such compounds for the treatment and/or prevention of organ transplantation rejection, graft versus host disease, autoimmune diseases, chronic inflammatory diseases, including but not limited to psoriasis and rheumatoid arthritis, and cancer in a mammal.Type: GrantFiled: March 27, 1995Date of Patent: June 17, 1997Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Ronald Louis Magolda, William John Pitts, Irina Cipora Jacobson, Carl Henry Behrens, Michael James Orwat, Douglas Guy Batt -
Patent number: 5594152Abstract: This invention comprises a process for production of a compound of the formula: ##STR1## in which R.sup.1 is selected from the group consisting of H, lower alkyl(C.sub.1 -C.sub.3), alkoxy(C.sub.1 -C.sub.3), bromo, chloro, fluoro, iodo, --COlower alkyl(C.sub.1 -C.sub.3), and --CF.sub.3 ;R.sup.2 is selected from the group consisting of H, lower alkyl(C.sub.1 -C.sub.3), alkoxy(C.sub.1 -C.sub.3), amino, bromo, chloro, fluoro, iodo, and --COlower alkyl(C.sub.1 -C.sub.3);or R.sup.1 and R.sup.2 taken together are methylenedioxy or ethylenedioxy;R.sup.3 is an aldehyde or carboxcylic acid moiety;the moiety ##STR2## wherein Z represents substituted or unsubstituted phenyl ring or an optionally substituted 5 or 6-membered aromatic heterocyclic ring.Type: GrantFiled: March 10, 1995Date of Patent: January 14, 1997Assignee: American Cyanamid CompanyInventors: Aranapakam M. Venkatesan, Jay D. Albright
-
Patent number: 5436333Abstract: Compounds of the formula: ##STR1## in which R.sup.1 is H, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, amino, bromo, chloro, fluoro, iodo, C.sub.1 -C.sub.3 alkylcarbonyl or trifluoromethyl; R.sup.2 is H, C.sub.1 -C.sub.3 alkyl, C.sub.1 --C.sub.3 alkoxy, bromo, chloro, fluoro, iodo, or C.sub.1 -C.sub.3 alkylcarbonyl; or R.sup.1 and R.sup.2 taken together are methylenedioxy or ethylenedioxy; the structure ##STR2## represents, as described in the specification, an ortho-fused phenyl moiety; an aromatic 5-membered heterocycle containing N, O, or S; or an aromatic 6-membered heterocycle containing N; all of which may be optionally substituted, are produced by reaction of ##STR3## where R.sup.3 is a masked aldehyde or carboxyl group, with 2-nitro-benzyl bromide followed by removal of the mask, reduction and cyclization.Type: GrantFiled: August 8, 1994Date of Patent: July 25, 1995Assignee: American Cyanamid CompanyInventors: Aranapakam M. Venkatesan, Jay D. Albright
-
Patent number: 5258511Abstract: Heterocyclic compounds of the formula ##STR1## in which R represents hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted hetaryl,A represents C--R.sup.1, N,R.sup.1 represents substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted hetaryl,X, Y represent O, NH,Z represents hydrogen, --CN, substituted or unsubstituted aryl, substituted or unsubstituted hetaryl,W represents O, N--R.sup.5,R.sup.5 represents hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, a substituted or unsubstituted heterocyclic radical andB represents a substituted or unsubstituted carbocyclic-aromatic or heterocyclic ring onto which one or more further rings can be fused,and the use of these compounds as dyestuffs or pigments.Type: GrantFiled: July 20, 1992Date of Patent: November 2, 1993Assignee: Bayer AktiengesellschaftInventor: Hans Hochstetter
-
Patent number: 5250681Abstract: A piperidine compound of the formula (I): ##STR1## wherein A is a fused aromatic ring; R is hydrogen, chloro or methoxy; X is (CH.sub.2).sub.n, which may be substituted, in which n is 0 or an integer of 1 to 10, --CH.dbd.CH--, --C.dbd.C--, --O--, --S--, --NH--, --N(COCH.sub.3)--, --N(COOC.sub.2 H.sub.5)--, --N(CHO)--, --N(CH.sub.3)--, --CO--, --SO--, or --SO.sub.2 --; Y is --CH.dbd.CH--, --CH.sub.2 CH.sub.2 --, --CH.sub.2 CO--, --O--, --S--, --NH--, --OCH.sub.2 --, --SCH.sub.2 --, --NHCH.sub.2 --, --CH(OH)CH.sub.2 -- or --CH(OH)CH(OH)--; and Q is substituted or unsubstituted n-hexyl, carboxypropyl, ethoxycarbonylpropyl, cyanopropyl, cyclohexyl, phenyl, indanyl, naphthyl, tetrahydronaphthyl, benzocycloheptyl, piperidinyl, tetrahydroisoquinolinyl, indolyl, pyrolyl, furyl, thienyl, thiazolyl, oxazolyl or N-methylpyrolyl, wherein any one or more of the --(CH.sub.2)-groups of the hexyl, carboxypropyl, ethoxycarbonylpropyl and cyanopropyl groups may be replaced by --CH.dbd.CH--, --C.dbd.Type: GrantFiled: February 15, 1991Date of Patent: October 5, 1993Assignee: Ajinomoto Co., Inc.Inventors: Masataka Shoji, Kozo Toyota, Chikahiko Eguchi, Ryota Yoshimoto, Yoshikatsu Koyama, Hideki Domoto, Akira Kamimura
-
Patent number: 4971964Abstract: A pyridine derivative represented by formula (I): ##STR1## wherein the symbols are as defined in the specification, which exhibits selective, potential, and long-lasting inhibitory activity on biosynthesis of thromboxane A.sub.2 and is useful in the treatment and prevention of a broad range of diseases.Type: GrantFiled: June 15, 1989Date of Patent: November 20, 1990Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Koji Suzuki, Obase Hiroyuki, Akira Karasawa, Shiro Shirakura, Kubo Shizuoka, Ichiro Miki, Akio Ishii
-
Patent number: 4869895Abstract: A compound of the formula: ##STR1## wherein T is tritium; is described as well as intermediates for its preparation. The compound of formula I is useful in vivo for detecting the presence of benzodiazepine receptor occupiers in a warmblooded animal.Type: GrantFiled: August 5, 1988Date of Patent: September 26, 1989Assignee: Hoffmann-La Roche Inc.Inventors: Walter Burger, Arnold A. Liebman, Clark W. Berry
-
Patent number: 4866057Abstract: Compounds of the formula ##STR1## where R.sup.1, R.sup.2, R.sup.3, R.sup.4 and A have the meanings stated in the specification, as well as the use thereof for controlling diseases, are described.Type: GrantFiled: May 20, 1988Date of Patent: September 12, 1989Assignee: BASF AktiengesellschaftInventors: Gerd Steiner, Juergen Pfister, Hans-Juergen Teschendorf, Liliane Unger, Rudolf Binder
-
Patent number: 4843079Abstract: There are disclosed compounds having the formula ##STR1## wherein n is 1-4; R is hydrogen, loweralkyl or loweralkylcarbonyl; R.sub.1 is hydrogen, loweralkyl, loweralkylcarbonyl, aryl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, oxygen-bridge arylloweralkyl, or oxygen-bridged diaryllowerallyl; A is a direct bond or (CHR.sub.3).sub.m, m being 1-3; X is hydrogen, loweralkyl, cycloalkyl,, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, formyl, loweralkylcarbonyl, arylcarbonyl, --SH, loweralkylthio, --NHCOR.sub.4 or --NR.sub.5 R.sub.6, R.sub.4 being hydrogen or loweralkyl, and R.sub.6 and R.sub.6 being independently hydrogen, loweralkyl or cycloalkyl; Y is O, S or NR.sub.7 ; and each R.sub.2, each R.sub.3 and R.sub.Type: GrantFiled: April 4, 1988Date of Patent: June 27, 1989Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Gregory M. Shutske, Richard C. Effland
-
Patent number: 4820835Abstract: A compound of the formula: ##STR1## wherein T is tritium; is described as well as intermediates for its preparation. The compound of formula I is useful in an assay for detecting the presence of benzodiazepine receptor occupiers in a warmblooded animal.Type: GrantFiled: June 30, 1986Date of Patent: April 11, 1989Assignee: Hoffmann-La Roche Inc.Inventors: Walter Burger, Arnold A. Liebman, Clark W. Perry
-
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