Diazine Ring Patents (Class 544/114)
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Publication number: 20030198608Abstract: 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: 1Type: ApplicationFiled: June 13, 2002Publication date: October 23, 2003Applicant: Shiseido Co., Ltd.Inventors: Masaru Suetsugu, Eijiro Hara
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Patent number: 6610677Abstract: 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: GrantFiled: September 14, 2001Date of Patent: August 26, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: Robert Davies, Pan Li, Julian M. C. Golec, Jean-Damien Charrier, Ronald Knegtel, David Bebbington
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Publication number: 20030119811Abstract: Compounds represented by Formula (I): 1Type: ApplicationFiled: April 2, 2002Publication date: June 26, 2003Inventors: 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
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Publication number: 20030105094Abstract: 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: ApplicationFiled: March 19, 2002Publication date: June 5, 2003Applicant: Schering CorporationInventors: John W. Clader, Hubert B. Josien, Anandan Palani, Tin Yau Chan
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Patent number: 6570013Abstract: 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: GrantFiled: February 13, 2001Date of Patent: May 27, 2003Assignee: Pfizer IncInventor: Banavara L. Mylari
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Patent number: 6562843Abstract: 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: GrantFiled: April 28, 2000Date of Patent: May 13, 2003Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventor: James L. Bullington
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Patent number: 6562817Abstract: 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: GrantFiled: July 21, 2000Date of Patent: May 13, 2003Assignee: Shionogi & Co., Ltd.Inventors: Norihiko Tanimoto, Yasushi Hasegawa, Nobuhiro Haga
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Patent number: 6562822Abstract: 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: GrantFiled: June 22, 2001Date of Patent: May 13, 2003Assignee: Pharmacia & Upjohn CompanyInventor: Mark E. Schnute
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Publication number: 20030087901Abstract: 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: ApplicationFiled: February 27, 2002Publication date: May 8, 2003Applicant: Signal Pharmaceuticals, Inc.Inventors: Shripad S. Bhagwat, Leah M. Gayo-Fung, Qi Chao
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Patent number: 6534503Abstract: 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: GrantFiled: July 13, 2000Date of Patent: March 18, 2003Assignee: Lion Bioscience AGInventors: 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
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Publication number: 20030036543Abstract: This invention describes novel pyrazole compounds of formula IIIa: 1Type: ApplicationFiled: December 19, 2001Publication date: February 20, 2003Inventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Andrew Miller, Ronald Knegtel
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Publication number: 20030028017Abstract: Disclosed is a novel method of producing heteroaryl amines of the formula(I): 1Type: ApplicationFiled: July 11, 2001Publication date: February 6, 2003Inventors: Nathan Yee, Suresh R. Kapadia, Jinhua J. Song
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Patent number: 6506939Abstract: 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 contType: GrantFiled: July 13, 2001Date of Patent: January 14, 2003Assignee: Ciba Specialty Chemicals Water Treatments Ltd.Inventors: Peter Stuart Littlewood, Michael Singh
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Patent number: 6486332Abstract: 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: GrantFiled: February 6, 2001Date of Patent: November 26, 2002Assignee: Ciba Specialty Chemicals CorporationInventors: Zhimin Hao, John S. Zambounis, Abul Iqbal
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Patent number: 6403791Abstract: 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: GrantFiled: February 9, 2001Date of Patent: June 11, 2002Assignee: 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
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Publication number: 20020058809Abstract: 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: ApplicationFiled: November 2, 2001Publication date: May 16, 2002Inventors: Michel Jose Emmanuel, Eugene R. Hickey, Weimin Liu, Denice Mary Spero, Sanxing Sun, David S. Thomson, Yancey David Ward, Erick Richard Roush Young
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Patent number: 6355640Abstract: 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: GrantFiled: May 6, 1998Date of Patent: March 12, 2002Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Atsushi Akahane, Shintaro Nishimura, Hiromichi Itani, Kieran P. M. Durkin
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Patent number: 6348468Abstract: 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: GrantFiled: May 15, 2000Date of Patent: February 19, 2002Assignee: 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
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Publication number: 20020010177Abstract: The present invention is concerned with the compounds of formula 1Type: ApplicationFiled: March 19, 2001Publication date: January 24, 2002Inventors: Eddy Jean Edgard Freyne, Jean Fernand Armand Lacrampe, Frederik Dirk Deroose, Marc Gaston Venet
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Patent number: 6297274Abstract: 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: GrantFiled: August 4, 1998Date of Patent: October 2, 2001Assignee: Warner-Lambert CompanyInventors: Xue-Min Cheng, Annette Marian Doherty, William Chester Patt, Joseph Thomas Repine
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Patent number: 6271401Abstract: 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: GrantFiled: July 9, 1996Date of Patent: August 7, 2001Assignee: Ciba Specialty Chemicals Corp.Inventors: Zhimin Hao, John S. Zambounis, Abul Iqbal
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Patent number: 6156891Abstract: 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: GrantFiled: April 9, 1999Date of Patent: December 5, 2000Assignee: Sumitomo Chemical Company, LimitedInventor: Takashi Furukawa
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Patent number: 6121251Abstract: 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: GrantFiled: September 26, 1997Date of Patent: September 19, 2000Assignee: Rohm and Haas CompanyInventors: Steven Howard Shaber, Edward Michael Szapacs, Ronald Ross
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Patent number: 6100258Abstract: 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: GrantFiled: December 16, 1997Date of Patent: August 8, 2000Assignee: Zeneca LimitedInventor: Gloria Anne Breault
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Patent number: 6090753Abstract: 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: GrantFiled: January 30, 1998Date of Patent: July 18, 2000Assignee: Sumitomo Chemical Company LimitedInventors: Tadashi Katayama, Shinichi Kawamura, Yuzuru Sanemitsu, Yoko Mine
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Patent number: 5922706Abstract: 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: GrantFiled: November 13, 1997Date of Patent: July 13, 1999Assignee: Merck & Co., Inc.Inventors: Conrad P. Dorn, Jeffrey J. Hale, Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Tamara Ladduwahetty
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Patent number: 5886178Abstract: 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: GrantFiled: May 28, 1997Date of Patent: March 23, 1999Assignee: Syntex (U.S.A.) Inc.Inventors: Darin A. Allen, James P. Dunn, Eric B. Sjogren, David B. Smith
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Patent number: 5869659Abstract: The present invention relates to heteroatom-containing cyclopentanopyridyl-oxazolidinones, processes for their preparation and their use as medicaments, in particular as antibacterial medicaments.Type: GrantFiled: January 13, 1997Date of Patent: February 9, 1999Assignee: Bayer AktiengesellschaftInventors: Andreas Stolle, Dieter Habich, Bernd Riedl, Martin Ruppelt, Stephen Bartel, Walter Guarnieri, Hanno Wild, Rainer Endermann, Hein-Peter Kroll
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Patent number: 5837702Abstract: 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: GrantFiled: August 30, 1994Date of Patent: November 17, 1998Assignee: Bristol-Myers Squibb Co.Inventors: George C. Rovnyak, Karnail S. Atwal, Dinos P. Santafianos, Charles Z. Ding
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Patent number: 5777113Abstract: 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: GrantFiled: October 10, 1995Date of Patent: July 7, 1998Assignee: Ciba Specialty Chemicals CorporationInventor: Rita Pitteloud
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Patent number: 5776858Abstract: 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: GrantFiled: October 25, 1996Date of Patent: July 7, 1998Assignee: Nihon Bayer Agrochem K.K.Inventors: Toshio Goto, Seishi Ito, Natsuko Minegishi, Tatsuya Yamaoka, Chieko Ueno, Koichi Moriya, Fritz Maurer, Ryo Watanabe
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Patent number: 5773530Abstract: 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: GrantFiled: September 13, 1996Date of Patent: June 30, 1998Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Atsushi Akahane, Shintaro Nishimura, Hiromichi Itani, Kieran P. M. Durkin
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Patent number: 5763618Abstract: 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: GrantFiled: April 29, 1996Date of Patent: June 9, 1998Assignee: Konica CorporationInventors: Ryuzou Watanabe, Shinri Tanaka, Katsuji Ota, Michiko Nagato, Tomio Horiuchi
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Patent number: 5739132Abstract: 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: GrantFiled: December 16, 1996Date of Patent: April 14, 1998Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Akihiko Ishida, Koichi Homma, Harumichi Kono, Koji Tamura, Yasuhiko Sasaki
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Patent number: 5723411Abstract: 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: GrantFiled: October 16, 1996Date of Patent: March 3, 1998Assignee: E. I. du Pont de Nemours and CompanyInventor: Thomas Martin Stevenson
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Patent number: 5719147Abstract: 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: GrantFiled: September 8, 1995Date of Patent: February 17, 1998Assignee: 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
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Patent number: 5686588Abstract: 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: GrantFiled: August 16, 1995Date of Patent: November 11, 1997Inventor: Seo Hong Yoo
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Patent number: 5681954Abstract: 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: GrantFiled: April 4, 1995Date of Patent: October 28, 1997Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Kenjiro Yamamoto, Atsushi Hasegawa, Hideki Kubota, Masahiro Ando, deceased, Hitoshi Yamaguchi
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Patent number: 5643908Abstract: 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: GrantFiled: June 27, 1994Date of Patent: July 1, 1997Assignee: Sankyo Company, LimitedInventors: Yukio Sugimura, Kazuhiko Tamaki, Tomowo Kobayashi, Kazuhiko Tanzawa
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Patent number: 5637699Abstract: 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: GrantFiled: May 22, 1995Date of Patent: June 10, 1997Assignee: 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
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Patent number: 5635494Abstract: 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: GrantFiled: April 21, 1995Date of Patent: June 3, 1997Assignee: Rohm and Haas CompanyInventors: Ronald Ross, Steven H. Shaber, Edward M. Szapacs
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Patent number: 5633248Abstract: 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: GrantFiled: November 21, 1995Date of Patent: May 27, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Kaneyoshi Kato, Yoshihiro Sugiura, Koichi Kato
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Patent number: 5623072Abstract: 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: GrantFiled: October 11, 1994Date of Patent: April 22, 1997Assignee: Monsanto CompanyInventors: Michael S. South, Terri L. Jakuboski
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Patent number: 5622948Abstract: 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: GrantFiled: December 1, 1994Date of Patent: April 22, 1997Assignee: 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
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Patent number: 5580871Abstract: There are provided novel 1,4-dihydropyridine compounds, compositions containing them and methods of using them to treat congestive heart failure.Type: GrantFiled: March 9, 1995Date of Patent: December 3, 1996Assignee: The Dupont Merck Pharmaceutical CompanyInventor: Richard A. Earl
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Patent number: 5506227Abstract: 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: GrantFiled: April 13, 1992Date of Patent: April 9, 1996Assignee: Merck Frosst Canada, Inc.Inventors: Robert Zamboni, Daniel Guay, Jacques-Yves Gauthier
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Patent number: 5502059Abstract: 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: GrantFiled: October 11, 1994Date of Patent: March 26, 1996Assignee: SanofiInventors: Bernard Labeeuw, Danielle Gully, Francis Jeanjean, Jean-Charles Molimard, Robert Boigegrain
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Patent number: 5489603Abstract: 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: GrantFiled: July 15, 1993Date of Patent: February 6, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Hideki Uneme, Koichi Iwanaga, Noriko Higuchi, Isao Minamida, Tetsuo Okauchi
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Patent number: 5461053Abstract: 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: GrantFiled: October 22, 1992Date of Patent: October 24, 1995Assignee: SanofiInventors: Robert Boigegrain, Roger Brodin, Jean P. Kan, Dominique Olliero, Camille G. Wermuth, Jean-Jacques Bourguignon, Paul Worms
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Patent number: 5418233Abstract: 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: GrantFiled: October 14, 1992Date of Patent: May 23, 1995Assignee: Karl Thomae GmbHInventors: Guenter Linz, Helmut Pieper, Frank Himmelsbach, Austel: Volkhard, Thomas Mueller, Johannes Weisenberger, Elke Seewaldt-Becker