Diazine Ring Patents (Class 544/114)
  • Publication number: 20030198608
    Abstract: Providing an ultraviolet absorbent or photostabilizer with excellent absorption over a wide ultraviolet wavelength range and great stability and a high safety profile, as well as an ultraviolet-absorbing composition, a photostabilized composition and an external preparation for skin, where the pyridazine derivative of the following general formula and/or a salt thereof is included as the effective component of the ultraviolet absorbent or photostabilizer, or is included in the ultraviolet-absorbing composition, the photostabilized composition and the external preparation for skin: 1
    Type: Application
    Filed: June 13, 2002
    Publication date: October 23, 2003
    Applicant: Shiseido Co., Ltd.
    Inventors: Masaru Suetsugu, Eijiro Hara
  • Patent number: 6610677
    Abstract: This invention describes novel pyrazole compositions comprising a pharmaceutically acceptable carrier and a compound of formula VIII: wherein Z1 is N or C—R9, Z2 is N or CH, and Z3 is N or C—Rx, provided that one of Z1 and Z3 is nitrogen; G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said Ring C has one or two ortho substituents independently selected from —R1; Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; and Rx, R1, R2, R2′, R3, and R9 are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.
    Type: Grant
    Filed: September 14, 2001
    Date of Patent: August 26, 2003
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Robert Davies, Pan Li, Julian M. C. Golec, Jean-Damien Charrier, Ronald Knegtel, David Bebbington
  • Publication number: 20030119811
    Abstract: Compounds represented by Formula (I): 1
    Type: Application
    Filed: April 2, 2002
    Publication date: June 26, 2003
    Inventors: Nigel J. Liverton, John W. Butcher, Charles McIntyre, Christopher F. Claiborne, David A. Claremon, John A. McCauley, Joseph J. Romano, Wayne Thompson, Peter M. Munson
  • Publication number: 20030105094
    Abstract: The present invention discloses compounds which, are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.
    Type: Application
    Filed: March 19, 2002
    Publication date: June 5, 2003
    Applicant: Schering Corporation
    Inventors: John W. Clader, Hubert B. Josien, Anandan Palani, Tin Yau Chan
  • Patent number: 6570013
    Abstract: This invention relates to [4-oxo-(5-trifluoromethyl-benzothiazol-2-ylmethyl)-3,4-dihydro-phthalazin-1-yl]-acetic acid ethanolamine salt, pharmaceutical compositions thereof and methods of treating diabetic complications in mammals comprising administering to said mammals said salt and said compositions. This invention is also directed to combinations of said diethylamine salt with NHE-1 inhibitors, selective serotonin retuptake inhibitors (SSRIs), glycogen phosphorylase inhibitors (GPIs), sorbitol dehydrogenase inhibitors (SDIs) and antihypertensive agents. Said combinations are useful in treating diabetic complications in mammals.
    Type: Grant
    Filed: February 13, 2001
    Date of Patent: May 27, 2003
    Assignee: Pfizer Inc
    Inventor: Banavara L. Mylari
  • Patent number: 6562843
    Abstract: This invention provides novel substituted 3-pyridyl-4-arylpyrroles, and pharmaceutical compositions comprising same, useful for treating disorders ameliorated by reducing TNF-&agr; production and/or p38 activity in appropriate cells. This invention also provides therapeutic and prophylactic methods using the instant pharmaceutical compositions.
    Type: Grant
    Filed: April 28, 2000
    Date of Patent: May 13, 2003
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventor: James L. Bullington
  • Patent number: 6562817
    Abstract: The present invention provides a compound of the formula (I):   wherein A ring, B ring and C ring are each independently optionally substituted aromatic carbocycle or optionally substituted 5- or 6-membered heterocycle which may fuse with benzene ring, W1, W2 and/or W3 represents a bond when A ring, B ring and/or C ring is optionally substituted 5-membered heterocycle, X is —O—, —NR1— wherein R1 is hydrogen, lower alkyl etc. or the like, Y is hydrogen, lower alkyl, lower alkenyl or the like, one of V1 and V2 is a bond, and the other is a bond, —O— or the like, and a pharmaceutical composition comprising the same.
    Type: Grant
    Filed: July 21, 2000
    Date of Patent: May 13, 2003
    Assignee: Shionogi & Co., Ltd.
    Inventors: Norihiko Tanimoto, Yasushi Hasegawa, Nobuhiro Haga
  • Patent number: 6562822
    Abstract: The present invention provides a compound of formula I which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.
    Type: Grant
    Filed: June 22, 2001
    Date of Patent: May 13, 2003
    Assignee: Pharmacia & Upjohn Company
    Inventor: Mark E. Schnute
  • Publication number: 20030087901
    Abstract: Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective modulators for ER-&bgr; over ER-&agr;. Methods are disclosed for modulating ER-&bgr; in cell and/or tissues expressing the same, including cells and/or tissue that preferentially express ER-&bgr;. More generally, methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natural hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.
    Type: Application
    Filed: February 27, 2002
    Publication date: May 8, 2003
    Applicant: Signal Pharmaceuticals, Inc.
    Inventors: Shripad S. Bhagwat, Leah M. Gayo-Fung, Qi Chao
  • Patent number: 6534503
    Abstract: Methods for treating sexual dysfunction, such as erectile dysfunction or sexual arousal disorder, with a compound having the generic formula X1—X2-(D)Phe-Arg-(D)Trp-X3. A particularly useful compound is HP-228, which has the formula Ac-Nle-Gln-His-(D)Phe-Arg-(D)Trp-Gly-NH2. The invention also provides methods for selecting melanocortin receptor-3 ligands by determining whether a compound modulates the activity of MC-3 as an agonist or antagonist. These methods can be used to screen compound libraries for ligands to treat MC-3-associated conditions. Such conditions include sexual dysfunction, including erectile dysfunction and sexual arousal disorder.
    Type: Grant
    Filed: July 13, 2000
    Date of Patent: March 18, 2003
    Assignee: Lion Bioscience AG
    Inventors: Kevin C. Dines, Timothy C. Gahman, Beverly E. Girten, Douglas L. Hitchin, Kevin R. Holme, Hengyuan Lang, Sandra R. Slivka, Karen J. Watson-Straughan, Ronald R. Tuttle, Yazhong Pei
  • Publication number: 20030036543
    Abstract: This invention describes novel pyrazole compounds of formula IIIa: 1
    Type: Application
    Filed: December 19, 2001
    Publication date: February 20, 2003
    Inventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Andrew Miller, Ronald Knegtel
  • Publication number: 20030028017
    Abstract: Disclosed is a novel method of producing heteroaryl amines of the formula(I): 1
    Type: Application
    Filed: July 11, 2001
    Publication date: February 6, 2003
    Inventors: Nathan Yee, Suresh R. Kapadia, Jinhua J. Song
  • Patent number: 6506939
    Abstract: A process for the preparation of a mixture comprising a compound of formula (1) and a compound of formula (2) wherein R1 is an optionally substituted C1-20 alkyl, optionally substituted C3-4 alkenyl, optionally substituted C5-7 cycloalkyl or optionally substituted benzyl, R2 is an optionally substituted C1-20 alkyl, optionally substituted C3-4 alkenyl or optionally substituted C5-7 cycloalkyl, A is either S or NR3, R3 is an optionally substituted C1-20 alkyl, optionally substituted C3-4 alkenyl or optionally substituted C5-7 cycloalkyl, or R2 and R3 together form a 5-7 membered ring which can contain an oxygen atom, R4 is hydrogen or methyl, R5 is an optionally substituted C1-20 alkyl, optionally substituted C3-4 alkenyl, optionally substituted C5-7 cycloalkyl or optionally substituted benzyl and, R6 is hydrogen or an optionally substituted C1-20 alkyl, optionally substituted C3-4 alkenyl or optionally substituted C5-7 cycloalkyl, or R5 and R6 together form a 5-7 membered ring which can cont
    Type: Grant
    Filed: July 13, 2001
    Date of Patent: January 14, 2003
    Assignee: Ciba Specialty Chemicals Water Treatments Ltd.
    Inventors: Peter Stuart Littlewood, Michael Singh
  • Patent number: 6486332
    Abstract: Compounds of formula A(B)x,  (I) wherein x is an integer from 1 to 4, A is the radical of a chromophore of the quinacridone, anthraquinone, perylene, indigo, quinophthalone, isoindolinone, isoindoline, dioxazine, phthalocyanine or azo series, which radical contains x N-atoms attached to B, preferably with at least one directly adjacent or conjugated carbonyl group, B is a group of formula  and, if x is 2, 3 or 4, may also be one, two or three hydrogen atoms. The symbols Q, R1, R2, R3, R4, X, Y, Z, m and n, are as defined in claim 1. These carbamate group-containing soluble chromophores are distinguished by outstanding solid state fluorescence in the UV range as well as the by ease with which they can be converted to the corresponding pigments in the substrate in which they are incorporated.
    Type: Grant
    Filed: February 6, 2001
    Date of Patent: November 26, 2002
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Zhimin Hao, John S. Zambounis, Abul Iqbal
  • Patent number: 6403791
    Abstract: A compound of the formula wherein R1 is C1-3 alkyl optionally substituted with one or more fluorines; R2 is C1-6 alkyl, cycloalkyl or NR4R5; R3 is a pyrazole, imidazole or isoxazole group of partial formula (A), (B) or (C) NR4R5 is a nitrogen-containing heterocyclic ring; R6 is C1-3 alkyl; and R7 and R8, which are the same or different, each represents C1-3 alkyl, halogen, CF3 or CN; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: February 9, 2001
    Date of Patent: June 11, 2002
    Assignee: Darwin Discovery, Ltd.
    Inventors: Hazel Joan Dyke, Alan Findlay Haughan, Christopher Lowe, George Martin Buckley, Richard John Davenport, Andrew Sharpe, Hannah Jayne Kendall, Verity Margaret Sabin, John Gary Montana, Catherine Louise Picken
  • Publication number: 20020058809
    Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (I), (II), (Ia) and (Ib) further defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for making such novel compounds.
    Type: Application
    Filed: November 2, 2001
    Publication date: May 16, 2002
    Inventors: Michel Jose Emmanuel, Eugene R. Hickey, Weimin Liu, Denice Mary Spero, Sanxing Sun, David S. Thomson, Yancey David Ward, Erick Richard Roush Young
  • Patent number: 6355640
    Abstract: The present invention relates to a novel pyrazolopyridine compound of the following formula: wherein R1 is aryl, and R2 is cyclo(lower)alkyl which may have one or more suitable substituent(s), etc; and a pharmaceutically acceptable salt thereof, which is useful as a medicament; the processes for the preparation of said pyrazolopyridine compound or a salt thereof; a pharmaceutical composition comprising said pyrazolopyridine compound or a pharmaceutically acceptable salt thereof; etc.
    Type: Grant
    Filed: May 6, 1998
    Date of Patent: March 12, 2002
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Atsushi Akahane, Shintaro Nishimura, Hiromichi Itani, Kieran P. M. Durkin
  • Patent number: 6348468
    Abstract: This invention relates to pyridazine derivatives represented by the formula (1): wherein R1 represents a (substituted) aryl group, R2 represents a phenyl group substituted at 4-position by a lower alkoxyl group or a lower alkylthio group, R3 represents a lower alkoxyl group, a halogenated lower alkyl group, a lower cycloalkyl group, a (subsituted) aryl group, a (substituted) aryloxy group, a (substituted) nitrogen-containing heterocyclic ring residue, a (substituted) aminocarbonyl group or a lower alkylcarbonyl group, A represents a single bond, a lower alkylene group or a lower alkenylene group, X represents O or S, and the dashed line indicates that the carbon-carbon bond between the 4-position and the 5-position is a single bond or a double bond, or salts thereof; and also to medicines containing them as effective ingredients.
    Type: Grant
    Filed: May 15, 2000
    Date of Patent: February 19, 2002
    Assignee: Kowa Co., Ltd.
    Inventors: Masao Ohkuchi, Yoshinori Kyotani, Hiromichi Shigyo, Tomoyuki Koshi, Takahiro Kitamura, Tadaaki Ohgiya, Takayuki Matsuda, Yukiyoshi Yamazaki, Natsuyo Kumai, Kyoko Kotaki, Hideo Yoshizaki, Yuriko Habata
  • Publication number: 20020010177
    Abstract: The present invention is concerned with the compounds of formula 1
    Type: Application
    Filed: March 19, 2001
    Publication date: January 24, 2002
    Inventors: Eddy Jean Edgard Freyne, Jean Fernand Armand Lacrampe, Frederik Dirk Deroose, Marc Gaston Venet
  • Patent number: 6297274
    Abstract: Novel nonpeptide endothelin I antagonists of Formula are described wherein R1 is unsubstituted or substituted cycloalkyl, phenyl, naphthyl or heteroaryl, R2 is unsubstituted or substituted alkyl, aryl or heteroaryl, R3 is unsubstituted or substituted alkyl, cycloalkyl, aryl or heteroayl, and R1 and/or R2 and/or R3 are independently substituted by a total of from 1 to 4 substituents which enhance aqueous solubility with the proviso that when R2 is alkyl and is substituted, the substituent is not oxygen at the &agr;-position of the furanone ring.
    Type: Grant
    Filed: August 4, 1998
    Date of Patent: October 2, 2001
    Assignee: Warner-Lambert Company
    Inventors: Xue-Min Cheng, Annette Marian Doherty, William Chester Patt, Joseph Thomas Repine
  • Patent number: 6271401
    Abstract: Compounds of formula A(B)x,  (I), wherein x is an integer from 1 to 4, A is the radical of a chromophore of the quinacridone, anthraquinone, perylene, indigo, quinophthalone, isoindolinone, isoindoline, dioxazine, phthalocyanine or azo series, which radical contains x N-atoms attached to B, preferably with at least one directly adjacent or conjugated carbonyl group, B is a group of formula and, if x is 2, 3 or 4, may also be one, two or three hydrogen atoms. The symbols Q, R1, R2, R3, R4, X, Y, Z, m and n, are as defined in claim 1. These carbamate group-containing soluble chromophores are distinguished by outstanding solid state fluorescence in the UV range as well as the by ease with which they can be converted to the corresponding pigments in the substrate in which they are incorporated.
    Type: Grant
    Filed: July 9, 1996
    Date of Patent: August 7, 2001
    Assignee: Ciba Specialty Chemicals Corp.
    Inventors: Zhimin Hao, John S. Zambounis, Abul Iqbal
  • Patent number: 6156891
    Abstract: Carboxylic acids of formula (1): ##STR1## wherein R.sup.2 and R.sup.3 are independently hydrogen or C.sub.1 -C.sub.3 alkyl, and Q is optionally substituted phenyl, can be easily converted by ring closing into pyridazin-3-one derivatives of formula (7): ##STR2## The carboxylic acids of formula (1) can be produced by reacting hydrazone compounds of formula (5): ##STR3## wherein R.sup.3 and Q are as defined above, with malonic acid derivatives of formula (6):R.sup.2 CH(COOH).sub.2wherein R.sup.2 is as defined above in the presence of a base.
    Type: Grant
    Filed: April 9, 1999
    Date of Patent: December 5, 2000
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Takashi Furukawa
  • Patent number: 6121251
    Abstract: Compounds with fungicidal and insecticidal properties having formula I ##STR1## wherein W is ##STR2## n is 0 or 1; Y is O, S, NR.sub.1, or R.sub.6 ;the ring bond containing R.sub.4 and R.sub.5 is a single or double bond;X is independently selected from hydrogen, halo, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy and --HC.dbd.CH--CH.dbd.CH-- thereby forming a napthyl ring;R is independently selected from (C.sub.1 -C.sub.12)alkyl and halo(C.sub.1 -C.sub.12)alkyl;R.sub.1 is independently selected from (C.sub.1 -C.sub.12)alkyl, (C.sub.2 -C.sub.8)alkenyl and aryl;R.sub.2 is independently selected from hydrogen, (C.sub.1 -C.sub.12)alkyl (C.sub.1 -C.sub.12)alkoxy, halo(C.sub.1 -C.sub.12)alkyl, halo(C.sub.1 -C.sub.12)alkoxy, hydroxy(C.sub.1 -C.sub.12)alkyl, (C.sub.1 -C.sub.12)alkoxy(C.sub.1 -C.sub.12)alkyl, (C.sub.1 -C.sub.12)alkoxycarbonyl(C.sub.1 -C.sub.12)alkyl, (C.sub.2 -C.sub.8)alkenyl, halo(C.sub.2 -C.sub.8)alkenyl, (C.sub.3 -C.sub.10)alkynyl, halo(C.sub.3 -C.sub.10)alkynyl, (C.sub.3 -C.sub.
    Type: Grant
    Filed: September 26, 1997
    Date of Patent: September 19, 2000
    Assignee: Rohm and Haas Company
    Inventors: Steven Howard Shaber, Edward Michael Szapacs, Ronald Ross
  • Patent number: 6100258
    Abstract: Compounds antagonistic of the pain enhancing effects of prostaglandins are disclosed. The compounds comprise an optionally-substituted A ring with a --CH(R.sup.3)N(R.sup.2)B--R.sup.1 and --OD groups positioned in a 1,2 relationship to one another on ring carbon atoms. The 3-position ring-atom is not substituted. B is also an optionally-substituted ring and the group R.sup.1 is positioned on B in a 1,3 or 1,4 relationship with the --CH(R.sup.3)N(R.sup.2)-- linking group. R.sup.1, R.sup.2 and R.sup.3 and D can be a number of different organic or halogen moieties. N-oxides of --NR.sup.2 and S-oxides of sulphur containing rings are disclosed as are processes for the preparation of the compounds, intermediates in their preparation, pharmaceutical compositions containing them, and their use as therapeutic agents.
    Type: Grant
    Filed: December 16, 1997
    Date of Patent: August 8, 2000
    Assignee: Zeneca Limited
    Inventor: Gloria Anne Breault
  • Patent number: 6090753
    Abstract: Novel pyridazin-3-one derivatives of formula [1] are provided, which are useful as active ingredients of herbicides, wherein R.sup.1 is haloalkyl; R.sup.2 and R.sup.3 are the same or different and are hydrogen, alkyl, haloalkyl, or alkoxyalkyl; and Q is [Q-1], [Q-2], [Q-3], [Q-4], or [Q-5]. Also provided are their use and intermediates for their production.
    Type: Grant
    Filed: January 30, 1998
    Date of Patent: July 18, 2000
    Assignee: Sumitomo Chemical Company Limited
    Inventors: Tadashi Katayama, Shinichi Kawamura, Yuzuru Sanemitsu, Yoko Mine
  • Patent number: 5922706
    Abstract: Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
    Type: Grant
    Filed: November 13, 1997
    Date of Patent: July 13, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Conrad P. Dorn, Jeffrey J. Hale, Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Tamara Ladduwahetty
  • Patent number: 5886178
    Abstract: Compounds of formula I: ##STR1## where: R.sub.10 is a group represented by formula (A), (B), or (C): ##STR2## and the other substituents are as defined in the specification; and their pharmaceutically acceptable salts are inhibitors of prostaglandin G/H synthase and are anti-inflammatory and analgesic agents.
    Type: Grant
    Filed: May 28, 1997
    Date of Patent: March 23, 1999
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Darin A. Allen, James P. Dunn, Eric B. Sjogren, David B. Smith
  • Patent number: 5869659
    Abstract: The present invention relates to heteroatom-containing cyclopentanopyridyl-oxazolidinones, processes for their preparation and their use as medicaments, in particular as antibacterial medicaments.
    Type: Grant
    Filed: January 13, 1997
    Date of Patent: February 9, 1999
    Assignee: Bayer Aktiengesellschaft
    Inventors: Andreas Stolle, Dieter Habich, Bernd Riedl, Martin Ruppelt, Stephen Bartel, Walter Guarnieri, Hanno Wild, Rainer Endermann, Hein-Peter Kroll
  • Patent number: 5837702
    Abstract: Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein X is alkyl, Y is a single bond, --CH.sub.2 --, --C(O)--, --O--, --S-- or --N(R.sup.8)-- where R.sup.8 is hydrogen, alkyl, haloalkyl, aryl, arylalkyl, cycloalkyl or (cycloalkyl)alkyl, and R.sup.1 to R.sup.7 are as defined herein. These compounds have potassium channel activating activity and are useful, therefore for example, as cardiovascular agents.
    Type: Grant
    Filed: August 30, 1994
    Date of Patent: November 17, 1998
    Assignee: Bristol-Myers Squibb Co.
    Inventors: George C. Rovnyak, Karnail S. Atwal, Dinos P. Santafianos, Charles Z. Ding
  • Patent number: 5777113
    Abstract: The invention relates to novel compounds of formula I ##STR1## wherein the general symbols are as defined in claim 1, as stabilizers for organic materials against oxidative, thermal or light-induced degradation.
    Type: Grant
    Filed: October 10, 1995
    Date of Patent: July 7, 1998
    Assignee: Ciba Specialty Chemicals Corporation
    Inventor: Rita Pitteloud
  • Patent number: 5776858
    Abstract: 1-Azinyl-tetraozolinones of the following formulae (I) and (II): ##STR1## wherein R.sup.1 and R.sup.2 are independently represent alkyl, haloalkyl, cycloalkyl, alkenyl, haloalkenyl, alkynyl or optionally substituted phenyl, orR.sup.1 and R.sup.2, together with the nitrogen atom to which they are bonded, may form a 5- or 6-membered heterocyclic ring which may optionally contain a further heteroatom, and said heterocyclic ring may optionally be benzo-condensed and/or be substituted by one or more of C.sub.1-4 alkyl(s), andR.sup.3 is a 6-membered heterocyclic aromatic group consisting of carbon atoms and 2 or 3 nitrogen atoms, which may optionally be substituted by halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, di(C.sub.1-4 alkyl)amino or phenyl.The compounds of the formula (I) exhibit an excellent herbicidal activity and the compounds of the formula (II) are useful as starting materials in the production of the compounds of the formula (I).
    Type: Grant
    Filed: October 25, 1996
    Date of Patent: July 7, 1998
    Assignee: Nihon Bayer Agrochem K.K.
    Inventors: Toshio Goto, Seishi Ito, Natsuko Minegishi, Tatsuya Yamaoka, Chieko Ueno, Koichi Moriya, Fritz Maurer, Ryo Watanabe
  • Patent number: 5773530
    Abstract: The present invention relates to a novel pyrazolopyridine compound of the following formula: ##STR1## wherein R.sup.1 is aryl, andR.sup.2 is cyclo(lower)alkyl which may have one or more suitable substituent(s), etc; and a pharmaceutically acceptable salt thereof, which is useful as a medicament; the processes for the preparation of said pyrazolopyridine compound or a salt thereof; a pharmaceutical composition comprising said pyrazolopyridine compound or a pharmaceutically acceptable salt thereof; etc.
    Type: Grant
    Filed: September 13, 1996
    Date of Patent: June 30, 1998
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Atsushi Akahane, Shintaro Nishimura, Hiromichi Itani, Kieran P. M. Durkin
  • Patent number: 5763618
    Abstract: A method of manufacturing a sulfide comprises the steps of (a) dissolving a thiol in a solvent to form a solution; (b) oxidizing the thiol to a disulfide in the presence of a first oxidizing agent in the solution; (c) reacting the disulfide with a coupler in the presence of a base and a second oxidizing agent, without isolation of said disulfide from the solution, to form a reaction mixture in which the sulfide is produced; and (d) obtaining said sulfide.
    Type: Grant
    Filed: April 29, 1996
    Date of Patent: June 9, 1998
    Assignee: Konica Corporation
    Inventors: Ryuzou Watanabe, Shinri Tanaka, Katsuji Ota, Michiko Nagato, Tomio Horiuchi
  • Patent number: 5739132
    Abstract: Disclosed are a pyridazinone compound represented by the formula: ##STR1## wherein (1) R.sup.1 is a substituted or unsubstituted C.sub.1-10 alkyl, a C.sub.3-6 cycloalkyl, a lower alkenyl, a heterocyclic group having N, O or S atom or camphor-10-yl; R.sup.3 is hydrogen, a substituted or unsubstituted lower alkyl or a lower alkenyl; or R.sup.1 and R.sup.3 are bonded at terminal ends thereof to form a lower alkylene; and Z is a group represented by the formula: ##STR2## where n is 1 or 2; and D is hydrogen or a halogen; or (2) R.sup.1 is a substituted or unsubstituted C.sub.1-10 alkyl, a substituted or unsubstituted phenyl, a C.sub.3-6 cycloalkyl, a lower alkenyl, a heterocyclic group having N, O or S atom or camphor-10-yl; R.sup.3 is hydrogen, a substituted or unsubstituted lower alkyl or a lower alkenyl; or R.sup.1 and R.sup.3 are bonded at terminal ends thereof to form a lower alkylene; and Z is a group represented by the formula: ##STR3## and R.sup.
    Type: Grant
    Filed: December 16, 1996
    Date of Patent: April 14, 1998
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Akihiko Ishida, Koichi Homma, Harumichi Kono, Koji Tamura, Yasuhiko Sasaki
  • Patent number: 5723411
    Abstract: Compounds of Formula I, and their N-oxides and agriculturally-suitable salts, are disclosed which are useful for controlling undesired vegetation ##STR1## wherein Q, W, R.sup.1, R.sup.2 and R.sup.3 are as defined in the disclosure.Also disclosed are compositions containing the compounds of Formula I and a method for controlling undesired vegetation which involves contacting the vegetation or its environment with an effective mount of a compound of Formula I.
    Type: Grant
    Filed: October 16, 1996
    Date of Patent: March 3, 1998
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Thomas Martin Stevenson
  • Patent number: 5719147
    Abstract: Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
    Type: Grant
    Filed: September 8, 1995
    Date of Patent: February 17, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Conrad P. Dorn, Paul E. Finke, Jeffrey J. Hale, Malcolm MacCoss, Sander G. Mills, Shrenik K. Shah, Mark Stuart Chambers, Timothy Harrison, Tamara Ladduwahetty, Brian John Williams
  • Patent number: 5686588
    Abstract: A stoichiometric acid moiety transfer reaction for the preparation of an acid salt of an amine compound is disclosed. The acid moiety transfer reaction provides amine acid salts of high purity and having crystalline structure of uniform size and shape.
    Type: Grant
    Filed: August 16, 1995
    Date of Patent: November 11, 1997
    Inventor: Seo Hong Yoo
  • Patent number: 5681954
    Abstract: A compound represented by formula (I): ##STR1## wherein Q represents an aryl group, a heterocyclic group, a diarylmethyl group, an aralkyl group composed of an aryl group and an alkylene group, an alkyl group or a cycloalkyl group, in which the aryl group, heterocyclic group, and the aryl moiety of the diarylmethyl group and aralkyl group may be substituted with one or more substituents; R represents a bicyclic, substituted, nitrogen-containing heterocyclic group or a substituted phenyl group, in which the nitrogen-containing heterocyclic group is composed of a 5-membered, substituted, aromatic or saturated ring containing one or two nitrogen atoms and a 6-membered ring; and Z represents an alkylene group, an alkenylene group, an alkylene group, a carbonyl group, an alkylene group containing a carbonyl group or an oxalyl group, or a salt thereof.
    Type: Grant
    Filed: April 4, 1995
    Date of Patent: October 28, 1997
    Assignee: Daiichi Pharmaceutical Co., Ltd.
    Inventors: Kenjiro Yamamoto, Atsushi Hasegawa, Hideki Kubota, Masahiro Ando, deceased, Hitoshi Yamaguchi
  • Patent number: 5643908
    Abstract: Compounds having inhibitory activity against inhibitory activity against type IV collagenase and are useful as angiogenesis, cancer infiltration or cancer metastasis inhibitors. The compounds have the formula: ##STR1## in which R.sup.1 represents a group of formula: --OR.sup.3 (wherein R.sup.3 represents a hydrogen atom or an alkyl group),--NR.sup.4 R.sup.5 (wherein R.sup.4 and R.sup.5 each represents a hydrogen atom, an alkyl or alkoxy group),--NHCH(R.sup.6 COR.sup.7 (wherein R.sup.6 represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms, and R.sup.7 represents an alkyl group),--NHCH(R.sup.6)COOR.sup.8 (wherein R.sup.8 represents an alkyl group) or--NHCH(R.sup.6)CONR.sup.9 R.sup.10 (wherein R.sup.9 and R.sup.10 each represents a hydrogen atom or an alkyl group, or NR.sup.9 R.sup.10 together represent a heterocyclic ring group); andR.sup.2 represents a hydrogen atom, an alkyl or aralkyl group.
    Type: Grant
    Filed: June 27, 1994
    Date of Patent: July 1, 1997
    Assignee: Sankyo Company, Limited
    Inventors: Yukio Sugimura, Kazuhiko Tamaki, Tomowo Kobayashi, Kazuhiko Tanzawa
  • Patent number: 5637699
    Abstract: Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
    Type: Grant
    Filed: May 22, 1995
    Date of Patent: June 10, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Conrad P. Dorn, Jeffrey J. Hale, Paul E. Finke, Malcolm MacCoss, Sander G. Mills, Shrenik K. Shah, Mark S. Chambers, Timothy Harrison, Tamara Ladduwahetty, Brian J. Williams
  • Patent number: 5635494
    Abstract: Compounds with fungicidal and insecticidal properties having formula I ##STR1## wherein W is CH.sub.3 --O-A.dbd.C--CO(V)CH.sub.3 ; n is 0 or 1;A is N or CH;V is O or NH;whereinY is O, S, NR.sub.1, or R.sub.6, the ring bond containing R.sub.4 and R.sub.5 is a single or double bond and R.sub.4 and R.sub.5 are independently selected from hydrogen and substituted or unsubstituted alkyl and aryl groups.
    Type: Grant
    Filed: April 21, 1995
    Date of Patent: June 3, 1997
    Assignee: Rohm and Haas Company
    Inventors: Ronald Ross, Steven H. Shaber, Edward M. Szapacs
  • Patent number: 5633248
    Abstract: A compound of the formula: ##STR1## wherein Ar.sup.1 and Ar.sup.2 independently represent an optionally substituted aromatic group; P and Q independently represent a divalent aliphatic hydrocarbon group having at least 2 carbon atoms and optionally having either oxygen or sulfur in the carbon chain; R.sup.1 and R.sup.3 independently represent --CO--R, --CONH--R (R represents a hydrocarbon group or a heterocyclic group) or a hydrocarbon group; R.sup.2 and R.sup.4 independently represent hydrogen or an alkyl group; R.sup.2 and R.sup.4 independently represent hydrogen or an alkyl group; R.sup.1 and R.sup.2 or R.sup.3 and R.sup.4, taken together with the adjacent nitrogen atom, may form a nitrogen-containing heterocyclic group; and j represents 0 or 1, or a salt thereof, has excellent GnRH-receptor antagonizing activity and is useful as a prophylactic and therapeutic agent for hormone-dependent and other diseases.
    Type: Grant
    Filed: November 21, 1995
    Date of Patent: May 27, 1997
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Kaneyoshi Kato, Yoshihiro Sugiura, Koichi Kato
  • Patent number: 5623072
    Abstract: Disclosed are certain 3-phenylpyridazines, compositions thereof which are herbicidal and methods of using such compositions for controlling undesired plants. Intermediates useful in preparing the 3-phenylpyridazines are disclosed.
    Type: Grant
    Filed: October 11, 1994
    Date of Patent: April 22, 1997
    Assignee: Monsanto Company
    Inventors: Michael S. South, Terri L. Jakuboski
  • Patent number: 5622948
    Abstract: Pyrrole pyridazine and pyridazinone compounds are described. These compounds are useful as anti-inflammatory agents in the treatment of inflammation and pain. The preparation of these compounds, their pharmaceutically acceptable salts, and pharmaceutical compositions containing these compounds, is also described.
    Type: Grant
    Filed: December 1, 1994
    Date of Patent: April 22, 1997
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: James P. Dunn, Chakk S. Ramesha, Jim W. Barnett, Denis J. Kertesz, Aaron B. Miller, David Morgans, Jr., C. Elliott Sigal, Eric B. Sjogren, David B. Smith, Francisco X. Talamas
  • Patent number: 5580871
    Abstract: There are provided novel 1,4-dihydropyridine compounds, compositions containing them and methods of using them to treat congestive heart failure.
    Type: Grant
    Filed: March 9, 1995
    Date of Patent: December 3, 1996
    Assignee: The Dupont Merck Pharmaceutical Company
    Inventor: Richard A. Earl
  • Patent number: 5506227
    Abstract: Compounds having the formula I: ##STR1## are antagonists of the actions of leukotrienes. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.
    Type: Grant
    Filed: April 13, 1992
    Date of Patent: April 9, 1996
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Robert Zamboni, Daniel Guay, Jacques-Yves Gauthier
  • Patent number: 5502059
    Abstract: The invention relates to substituted 1-naphthyl-3-pyrazolecarboxamides of formula I: ##STR1## Application: These compounds are useful for the treatment of neuropsychiatric disorders, especially those associated with a dysfunction of the dopaminergic systems.
    Type: Grant
    Filed: October 11, 1994
    Date of Patent: March 26, 1996
    Assignee: Sanofi
    Inventors: Bernard Labeeuw, Danielle Gully, Francis Jeanjean, Jean-Charles Molimard, Robert Boigegrain
  • Patent number: 5489603
    Abstract: An insecticidal composition containing a guanidine derivative of the formula: ##STR1## wherein R.sup.1 is an optionally substituted homocyclic or heterocyclic group, n is 0 or 1, R.sup.2 is a hydrogen atom or an optionally substituted hydrocarbon group, R.sup.3 is a primary, secondary or tertiary amino group, X is an electron attractive group such as nitro or trifluoroacetyl group, provided that when n is 0, R.sup.1 is an optionally substituted heterocyclic group or a salt thereof.
    Type: Grant
    Filed: July 15, 1993
    Date of Patent: February 6, 1996
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hideki Uneme, Koichi Iwanaga, Noriko Higuchi, Isao Minamida, Tetsuo Okauchi
  • Patent number: 5461053
    Abstract: The present invention relates to pyridazine derivatives of formula: ##STR1## which are useful as ligands of cholinergic receptors, in particular, receptors of the M.sub.1 type.
    Type: Grant
    Filed: October 22, 1992
    Date of Patent: October 24, 1995
    Assignee: Sanofi
    Inventors: Robert Boigegrain, Roger Brodin, Jean P. Kan, Dominique Olliero, Camille G. Wermuth, Jean-Jacques Bourguignon, Paul Worms
  • Patent number: 5418233
    Abstract: Heterobiaryl derivatives of the formulaR.sub.1 NH--X.sub.1 --X.sub.2 --X.sub.3 --Y.sub.1 --Y.sub.2 --Y.sub.3 --Y.sub.4 --E (I)whereinR.sub.1, X.sub.1 to X.sub.3 and Y.sub.1 to Y.sub.4 are as defined herein, the tautomers, stereoisomers and mixtures thereof, and the salts, particularly the physiologically acceptable salts, thereof with organic or inorganic acids or bases. The derivatives have valuable pharmacological properties, such as inhibiting cell-cell aggregation and cell-matrix interactions.
    Type: Grant
    Filed: October 14, 1992
    Date of Patent: May 23, 1995
    Assignee: Karl Thomae GmbH
    Inventors: Guenter Linz, Helmut Pieper, Frank Himmelsbach, Austel: Volkhard, Thomas Mueller, Johannes Weisenberger, Elke Seewaldt-Becker