Polycyclo Ring System Having At Least Three Cyclos And Having The Hetero Ring As One Of The Cyclos Patents (Class 549/12)
  • Publication number: 20030065021
    Abstract: The present invention offers a tracheal smooth muscle relaxant containing the compound represented by the following formula (1) or pharmacologically acceptable salt thereof as an effective ingredient.
    Type: Application
    Filed: October 1, 2002
    Publication date: April 3, 2003
    Inventors: Shinya Yamashita, Jiro Takeo, Shuji Jinno, Yasuyo Kogure, Hiroyuki Onuki, Takaaki Okita, Junichiro Hata, Yasuhiro Fukuda, Naomi Ohtsuka
  • Patent number: 6525086
    Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, A, X, T, Q, Z, U, Y, Ar, p and n are as defined in the specification. These compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).
    Type: Grant
    Filed: March 14, 2001
    Date of Patent: February 25, 2003
    Assignee: Novo Nordisk A/S
    Inventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
  • Patent number: 6521769
    Abstract: Chiral ligands and transition metal complexes based on such chiral ligands useful in asymmetric catalysis are disclosed. The chiral ligands include chiral C1-C6 TunaPhos ligands. The ruthenium TunaPhos complex reduces ketones to the corresponding alcohols with 95-99.6% enantioselectivity. The transition metal complexes of the chiral ligands are useful in asymmetric reactions such as asymmetric hydrogenation, hydride transfer, hydrosilylation, hydroboration, hydrovinylation, hydroformylation, hydrocarboxylation, isomerization, allylic alkylation, cyclopropanation, Diels-Alder reaction, Heck reaction, isomerization, Aldol reaction, Michael addition and epoxidation reactions.
    Type: Grant
    Filed: September 19, 2000
    Date of Patent: February 18, 2003
    Assignee: The Penn State Research Foundation
    Inventor: Xumu Zhang
  • Publication number: 20020188119
    Abstract: A process for preparing enantiomerically enriched tetrahydrobenzothipeine oxides comprises cyclizing an enantiomerically enriched aryl-3-propanalsulfoxide wherein the sulfur atom of the aryl-3-propanalsulfoxide is a chiral center.
    Type: Application
    Filed: February 11, 2002
    Publication date: December 12, 2002
    Inventors: Jinglin Li, Ching-Cheng Wang, David B. Reitz, Victor Snieckus, Horng-Chih Huang, Andrew J. Carpenter
  • Patent number: 6489481
    Abstract: Treatment or the prevention of neurological disorders in a warm-blooded mammal, by use of a compound of formula VIII wherein A, B, R2, R3, R4, R5, R8, R9 and n are as defined in the specification, or pharmaceutically-acceptable salts, prodrugs or solvates thereof. Processes for the preparation of compounds of Formula VIII are described, as are pharmaceutical compositions containing them.
    Type: Grant
    Filed: June 25, 2001
    Date of Patent: December 3, 2002
    Assignee: AstraZeneca AB
    Inventors: Richard Alan Keith, Timothy Martin Piser, Michael Thaddeus Klimas
  • Publication number: 20020128308
    Abstract: The invention provides compounds of the formula: 1
    Type: Application
    Filed: January 11, 2002
    Publication date: September 12, 2002
    Inventors: Tsuneo Yasuma, Haruhiko Makino, Akira Mori
  • Patent number: 6433187
    Abstract: Derivatives of known tubulin-binding compounds are provided in which a (poly)fluorobenzene, a fluoropyridine, or a fluoronitrobenzene moiety is incorporated or added to the structure. These derivatives can be used as antimitotic agents and can be considered covalent modifiers of tubulin. The strategy developed for each of the compounds is to i) append a fluorinated electrophile (e.g., pentafluorophenylsulfonamido, 2-fluoropyridyl, or 3,5-dinitro-4-fluorophenyl) to an existing functional group in a natural product, ii) replace an aromatic ring in a natural product with a fluorinated electrophile, or iii) attach a fluorinated electrophile to an open valence in a portion of the molecule that will not interfere with recognition and binding to the tubulin site. Derivatives are provided based on colchicine, steganacin, podophyllotoxin, nocodazole, combretastatin, curacin A, vinblastine, vincristine, dolastatin, 2-methoxyestradiol, dihydroxy-pentamethoxyflavanone and others.
    Type: Grant
    Filed: December 15, 1999
    Date of Patent: August 13, 2002
    Assignee: Tularik Inc.
    Inventors: David Clark, Walter Frankmoelle, Jonathan Houze, Juan C. Jaen, Julio C. Medina
  • Patent number: 6420417
    Abstract: Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals. Also provided are compositions and methods for combination therapy employing ileal bile acid transport inhibitors and HMG Co-A reductase inhibitors for the treatment of hyperlipidemic conditions.
    Type: Grant
    Filed: September 29, 2000
    Date of Patent: July 16, 2002
    Assignee: G. D. Searle & Co.
    Inventors: Bradley T. Keller, Kevin C. Glenn, Robert E. Manning
  • Publication number: 20020055499
    Abstract: Compounds of the formula (I) are disclosed which are dual fibrinogen receptor and vitronectin receptor antagonists and are useful in the treatment of atherosclerosis, in the prevention of restenosis and in the prevention of tumor metastasis and tumor growth: 1
    Type: Application
    Filed: December 12, 2001
    Publication date: May 9, 2002
    Inventors: Dirk Heerding, James Martin Samanen
  • Publication number: 20020035104
    Abstract: Provided are compounds of formula (I) 1
    Type: Application
    Filed: August 16, 2001
    Publication date: March 21, 2002
    Applicant: GENENTECH, INC.
    Inventors: Dean R. Artis, David Y. Jackson, Thomas E. Rawson, Mark E. Reynolds, Daniel P. Sutherlin, Mark S. Stanley
  • Publication number: 20020032329
    Abstract: Among its several embodiments, the present invention provides an improved process for the preparation of tetrahydrobenzothiepine-1,1-dioxide compounds; the provision of a process for preparing a diastereomeric mixture of tetrahydrobenzothiepine-1,1-dioxide compounds from a single diastereomer of such compounds; the provision of a process for the preparation of 3-bromo-2-substituted propionaldehyde compounds; and the provision of a process for the preparation of 3-thio-2-substituted propionaldehyde compounds.
    Type: Application
    Filed: March 8, 2001
    Publication date: March 14, 2002
    Inventors: Kevin A. Babiak, Andrew Carpenter, Shine Chou, Pierre-Jean Colson, Payman Farid, Robert Hett, Christian H. Huber, Kevin J. Koeller, Jon P. Lawson, James Li, Eduardo K. Mar, Lawrence M. Miller, Vladislav Orlovski, James C. Peterson, Mark J. Pozzo, Claire A. Przybyla, Samuel J. Tremont, Jay S. Trivedi, Grace M. Wagner, Gerald A. Weisenburger, Benxin Zhi
  • Publication number: 20020013476
    Abstract: Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals.
    Type: Application
    Filed: April 9, 2001
    Publication date: January 31, 2002
    Applicant: G.D. Searle & Co.
    Inventors: Len F. Lee, Shyamal C. Banerjee, Horng-Chih Huang, Jinglin J. Li, Raymond E. Miller, David B. Reitz, Samuel J. Tremont
  • Publication number: 20020004522
    Abstract: Method and compositions for treating a patient having a neurological disease or disorder, such as stroke, head trauma, spinal cord injury, spinal cord ischemia, ischemia- or hypoxia-induced nerve cell damage, epilepsy, anxiety, neuropsychiatric or cognitive deficits due to ischemia or hypoxia such as those that frequently occur as a consequence of cardiac surgery under cardiopulmonary bypass, or neurodegenerative diseases such as Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, or amyotrophic lateral sclerosis (ALS).
    Type: Application
    Filed: April 2, 2001
    Publication date: January 10, 2002
    Applicant: NPS Pharmaceuticals, Inc.
    Inventors: Alan L. Mueller, Scott T. Moe
  • Patent number: 6315928
    Abstract: The present invention relates to specific photochromic 3H-naphtho[2,1-b]pyran derivatives and to their use in plastics of all types, especially for ophthalmic purposes. In particular, the present invention relates to spiro compounds derived from naphthopyrans and having a fluorene structure, referred to as spirofluorenopyrans, in which an annelated ring system is joined by a spiro bond to the central carbon atom of the fluorene structure.
    Type: Grant
    Filed: March 2, 2001
    Date of Patent: November 13, 2001
    Assignee: Optische Werke G. Rodenstock
    Inventors: Claudia Mann, Manfred Melzig, Udo Weigand
  • Patent number: 6297260
    Abstract: The present invention describes novel nitrosated and/or nitrosylated nonsteroidal antiinflammatory compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated nonsteroidal antiinflammatory compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase. The present invention also provides methods for treating, preventing and/or reducing inflammation, pain, and fever; decreasing or reversing the gastrointestinal, renal and other toxicities resulting from the use of nonsteroidal antiinflammatory drugs; treating and/or preventing gastrointestinal disorders; treating inflammatory disease states and disorders; and treating and/or preventing ophthalmic diseases or disorders.
    Type: Grant
    Filed: October 29, 1999
    Date of Patent: October 2, 2001
    Assignee: NitroMed, Inc.
    Inventors: Upul K. Bandarage, Qing Dong, Xinqin Fang, David S. Garvey, Gregory J. Mercer, Stewart K. Richardson, Joseph D. Schroeder, Tiansheng Wang
  • Patent number: 6268392
    Abstract: Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals. Also provided are compositions and methods for combination therapy employing ileal bile acid transport inhibitors and EG Co-A reductase inhibitors for the treatment of hyperlipidemic conditions.
    Type: Grant
    Filed: March 9, 1998
    Date of Patent: July 31, 2001
    Assignee: G. D. Searle & Co.
    Inventors: Bradley T. Keller, Kevin C. Glenn, Robert E. Manning
  • Patent number: 6211227
    Abstract: The present invention provides tricyclic compounds which are useful for the treatment of pollakiuria and urinary incontinence and which are represented by general formula (I): (wherein R1 represents hydrogen, substituted or unsubstituted lower alkyl, etc.; X1—X2—X3 represents CR5═CR6—CR7═CR8 (wherein R5, R6, R7 and R8, which may be the same or different, each represents hydrogen, substituted or unsubstituted lower alkyl, hydroxy, substituted or unsubstituted lower alkoxy, etc.), N(O)m═CR5—CR6═CR7 (wherein R5, R6 and R7 have the same significances as defined above, and m represents 0 or 1), S—CR7═CR8 (wherein R7 and R8 have the same significances as defined above), etc.
    Type: Grant
    Filed: October 14, 1999
    Date of Patent: April 3, 2001
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Makoto Yoshida, Takashi Seishi, Shigeru Aono, Tsuyoshi Yamagata, Kaoru Atsuki, Toshiaki Kumazawa, Haruki Takai, Koji Suzuki, Akira Karasawa
  • Patent number: 6207837
    Abstract: Efficient synthesis of diaryl sulfide derivatives useful as intermediates for pharmaceutical compounds. Provision of a convenient process for producing large quantities of dibenzo[b,f]thiepine derivatives using such intermediates.
    Type: Grant
    Filed: January 18, 2000
    Date of Patent: March 27, 2001
    Assignee: Nippon Suisan Kaisha, Ltd.
    Inventors: Naomi Ohtsuka, Shuji Jinno, Takaaki Okita
  • Patent number: 6180659
    Abstract: The present invention offers a tracheal smooth muscle relaxant containing the compound represented by the following formula (1) or pharmacologically acceptable salt thereof as an effective ingredient.
    Type: Grant
    Filed: August 31, 1998
    Date of Patent: January 30, 2001
    Assignee: Nippon Suisan Kaisha, Ltd.
    Inventors: Shinya Yamashita, Jiro Takeo, Shuji Jinno, Yasuyo Kogure, Hiroyuki Onuki, Takaaki Okita, Junichiro Hata, Yasuhiro Fukuda, Naomi Ohtsuka
  • Patent number: 6111115
    Abstract: A process for preparation of 2-(10,11-dihydro-10-oxodibenzo[b,f]thiepin-2-yl)propionic acid (i.e., Zaltoprofen) is performed by subjecting 2-(4-amino-3-carboxy-methylphenyl)propionic acid or its salt to diazotization and subsequent reaction with thiophenol to produce 2-(3-carboxymethyl-4-phenylthiophenyl)propionic acid or its salt, and subjecting the product to cyclization reaction. Other related processes and related compounds are also disclosed.
    Type: Grant
    Filed: February 17, 1999
    Date of Patent: August 29, 2000
    Assignees: Nippon Chemiphar Co., Ltd., Ube Industries, Ltd.
    Inventors: Masao Yamamoto, Kunio Kobayashi, Katsumasa Harada, Shigeyoshi Nishino, Hiroshi Sasaki
  • Patent number: 6096780
    Abstract: This invention is to provide a compound for antagonizing CCR5, said compound being represented by the formula: ##STR1## wherein R.sup.1 is an optionally substituted phenyl or an optionally substituted thienyl; Y is --CH.sub.2 --, --S-- or --O--; and R.sup.2, R.sup.3 and R.sup.4 are independently an optionally substituted aliphatic hydrocarbon group or an optionally substituted alicyclic heterocyclic ring group, and being effective for the prevention and treatment of infectious disease of HIV.
    Type: Grant
    Filed: August 19, 1999
    Date of Patent: August 1, 2000
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Mitsuru Shiraishi, Masanori Baba, Yoshio Aramaki, Osamu Nishimura, Naoyuki Kanzaki
  • Patent number: 6060468
    Abstract: The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula ##STR1## wherein X, Y, Z, R.sup.1, R.sup.1a, R.sup.2, R.sup.2a, p, r and s are as defined in the detailed part of the present description or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for treatment of indications caused by or related to secretion and circulation of insulin antagonising peptides.
    Type: Grant
    Filed: October 3, 1997
    Date of Patent: May 9, 2000
    Assignee: Novo Nordisk A/S
    Inventors: Tine Krogh J.o slashed.rgensen, Erik Fischer, Rolf Hohlweg, Knud Erik Andersen, Uffe Bang Olsen, Zdenek Polivka, Vladimir Valenta, Karel Sindelar
  • Patent number: 6057441
    Abstract: This invention concerns the compounds of formula (I), ##STR1## the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is zero to 6; p and q are zero to 4; r is zero to 5; R.sup.1 and R.sup.2 each independently are hydrogen; optionally substituted C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; halomethylcarbonyl; or R.sup.1 and R.sup.2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; each R.sup.3 and R.sup.4 independently are halo, cyano, hydroxy, halomethyl, halomethoxy, carboxyl, nitro, amino, mono- or di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkylcarbonylamino, aminosulfonyl, mono- or di(C.sub.1-6 alkyl)aminosulfonyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkyloxycarbonyl; each R.sup.5 independently is C.sub.1-6 alkyl, cyano or halomethyl; X is CR.sup.6 R.sup.7, NR.sup.8, O, S, S(.dbd.O) or S(.dbd.O).sub.
    Type: Grant
    Filed: October 6, 1998
    Date of Patent: May 2, 2000
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Pilar Gil-Lopetegui, Francisco Javier Fernandez-Gadea, Theo Frans Meert
  • Patent number: 6054474
    Abstract: Polycyclic alkaloids of formula (I), ##STR1## wherein R.sub.1 is H, C.sub.1-6 alkyl, or C.sub.6-12 aryl optionally substituted with polar groups; R.sub.2 and R.sub.3 are independently H, OH, C.sub.1-6 alkyl, --C(NH)--NH.sub.2, a positively charged group, or C.sub.7-13 aralkyl optionally substituted with NH.sub.2, OH, C.sub.1-6 alkyl, or halogen; or R.sub.2 and R.sub.3 together form a 5 to 6 member ring optionally incorporating a heteroatom; R.sub.4 is H, C.sub.1-6 alkyl, OR.sub.6, SR.sub.6 or N(R.sub.6).sub.2, wherein each R.sub.6 is independently H, C.sub.1-3 alkyl; X is O, S, SO, SO.sub.2, N--R.sub.5, or C--(R.sub.5).sub.2, wherein each R.sub.5 is independently H, C.sub.1-6 alkyl, or C.sub.7-13 aralkyl optionally interrupted with one or more heteroatom; n is an integer from 0 to 2; m is an integer from 0 to 3; with the proviso that when X is CH.sub.2 then R1 is not CH.sub.3, R.sub.2 and R.sub.3 are not both H, R.sub.4 is not OH, m is not 3 and n is not 0.
    Type: Grant
    Filed: March 25, 1998
    Date of Patent: April 25, 2000
    Assignee: Biochem Pharma, Inc.
    Inventors: John Dimaio, Dilip M. Dixit
  • Patent number: 5990104
    Abstract: Polycyclic alkaloids of formula (I), wherein R.sub.1 is H, C.sub.1-6 alkyl, or C.sub.6-12 aryl optionally substituted with polar groups; R.sub.2 and R.sub.3 are independently H, OH, C.sub.1-6 alkyl, --C(NH)--NH.sub.2, a positively charged group, or C.sub.7-13 aralkyl optionally substituted with NH.sub.2, OH, C.sub.1-6 alkyl, or halogen; or R.sub.2 and R.sub.3 together form a 5 to 6 member ring optionally incorporating a heteroatom; R.sub.4 is H, C.sub.1-6 alkyl, OR.sub.6, SR.sub.6, or N(R.sub.6).sub.2, wherein each R.sub.6 is independently H, C.sub.1-3 alkyl; X ix O, S, SO, SO.sub.2, or N--R.sub.5, wherein each R.sub.5 is independently H, C.sub.1-6 alkyl, or C.sub.7-13 aralkyl optionally interrupted with one or more heteroatom; n is an integer from 0 to 2; and m is an integer from 0 to 3. These compounds act as antagonists at the ionotropic NMDA (N-methyl-(D)-aspartic acid) receptor.
    Type: Grant
    Filed: March 25, 1998
    Date of Patent: November 23, 1999
    Assignee: Biochem Pharma, Inc.
    Inventors: John Dimaio, Dilip M. Dixit
  • Patent number: 5952512
    Abstract: A method of producing an amine salt of an optically active benzothiepin derivative, which is characterized by allowing a benzothiepin derivative represented by the formula (I) ##STR1## wherein R stands for a lower alkyl group, to react with an optically active amine.
    Type: Grant
    Filed: September 11, 1996
    Date of Patent: September 14, 1999
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Yoshiharu Maeda, Motoki Ikeuchi, Shigeo Yabuno
  • Patent number: 5939452
    Abstract: The invention relates to novel benzopyran and other benzo-fused leukotriene B.sub.4 (LTB.sub.4) antagonists of formula I and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing such compounds, and to a method of using such compounds as LBT.sub.4 antagonists. The compounds of the invention inhibit the action of LTB.sub.4 and are therefore useful in the treatment of LTB.sub.4 induced illnesses such as inflammatory disorders including rheumatoid arthritis, osteoarthritis, inflammatory bowel disease, psoriasis and other skin disorders such as eczema, erythema, pruitus and acne, stroke and other forms of reperfusion injury, graft rejection, autoimmune diseases, asthma and other conditions where marked neutrophil infiltration occurs.
    Type: Grant
    Filed: April 9, 1997
    Date of Patent: August 17, 1999
    Assignee: Pfizer Inc
    Inventors: Mark Anthony Dombroski, Kevin Koch, Anthony Daniel Piscopio
  • Patent number: 5902516
    Abstract: A five-coordinate phosphorous compound which is useful as an stabilizer for organic materials and represented by the formula (I): ##STR1## wherein R.sup.1, R.sup.2, R.sup.4 and R.sup.5 independently represent hydrogen atom, an alkyl group, a cycloalkyl group, an alkylcycloalkyl group, an aralkyl group or a phenyl group; R.sup.3 represents hydrogen atom or an alkyl group; X represents a direct bond, a sulfur atom or a group represented by --CHR.sup.6 -- wherein R.sup.6 represents hydrogen atom, an alkyl group or a cycloalkyl group, and a process for producing the compound (I) are provided.
    Type: Grant
    Filed: August 7, 1997
    Date of Patent: May 11, 1999
    Assignee: Sumitomo Chemical Co., Ltd
    Inventors: Naoki Inui, Taketoshi Kikuchi, Kanako Fukuda, Takashi Sanada
  • Patent number: 5734067
    Abstract: Providing a novel tricyclic, condensed heterocyclic compound having an anti-oxidative action and being promising for use in pharmaceutical agents, cosmetics, chemical products and the like. By chemical synthesis, a novel anti-oxidative, tricyclic, condensed heterocyclic compound represented by the following formula: ##STR1## (wherein X--Y represents CH.sub.2 --C.dbd.O, CH.sub.2 --CH.sub.2 or CH.dbd.CH; Z represents O, S, or S.dbd.O; R.sub.1 to R.sub.8 represent independently those selected from the group consisting of hydrogen atom, a hydroxyl group, a halogen group, a lower alkyl group, a lower alkoxyl group, a lower alkyl ketone group and CF.sub.3 ; and at least two of R.sub.1 to R.sub.4 are hydroxyl groups); and the salts thereof are provided. The compound has an anti-oxidative activity at the same degree as or higher than the activity of .alpha.
    Type: Grant
    Filed: March 4, 1997
    Date of Patent: March 31, 1998
    Assignee: Nippon Suisan Kaisha, Ltd.
    Inventors: Shuji Jinno, Yasuyo Kogure, Hiroyuki Onuki, Takaaki Okita
  • Patent number: 5726325
    Abstract: The present invention relates to tricyclic compounds represented by general formula (I) which are useful as therapeutic agents for urinary incontinence: ##STR1## wherein R.sup.1 represents hydrogen and the like; --X.sup.1 --X.sup.2 --X.sup.3 -- represents --CR.sup.2 .dbd.CR.sup.3 --CR.sup.4 .dbd.CR.sup.5 -- (wherein R.sup.2, R.sup.3, R.sup.4, and R.sup.5 represent hydrogen and the like) and the like; and Y represents --CH.sub.2 O-- and the like.
    Type: Grant
    Filed: June 6, 1997
    Date of Patent: March 10, 1998
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Makoto Yoshida, Shin-ichi Sasaki, Shigeru Aono, Shigeki Fujiwara, Haruki Takai, Tsuyoshi Yamagata, Ken Nagashima, Akira Karasawa
  • Patent number: 5684041
    Abstract: A compound having the structure: ##STR1## wherein (a) n is from 1 to about 3;(b) X is selected from the group consisiting of O, S, SO, or SO.sub.2 ;(c) Y is independently hydrogen or straight, branched or cyclic alkyl having from 1 to about 4 carbon atoms, or the Y's are bonded together to form an alkanyl ring having from 3 to about 7 atoms;(d) Z is hydrogen or straight, branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen;(e) W is O or S; and(f) R.sub.1, R.sub.2 and R.sub.3 are independently hydrogen, straight, branched or cyclic alkyl having from 1 to 10 carbon atoms, aryl, heterocyclyl, heteroaryl, hydroxy, or alkoxy; or R1, R2 or R3 may be bonded to form one or more rings each ring having from 3 to about 7 atoms wherein from 1 to 3 atoms may be heteroatoms.pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.
    Type: Grant
    Filed: February 1, 1996
    Date of Patent: November 4, 1997
    Assignee: The Procter & Gamble Company
    Inventor: Michael Wiard Scherz
  • Patent number: 5684031
    Abstract: A compound having the structure: ##STR1## wherein (a) n is from 1 to about 3;(b) X is selected from the group consisting of O, S, SO, or SO.sub.2 ; (c) Y is independently hydrogen or straight, branched or cyclic alkyl having from 1 to about 4 carbon atoms, or the Y's are bonded together to form an alkanyl ring having from about 3 to about 7 atoms;(d) Z is hydrogen or straight, branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen;(e) R.sub.1 is hydrogen or straight, branched or cyclic alkyl, aryl or C(.dbd.NH)--NHR.sub.4 ; and(f) R.sub.2, R.sub.3, and R.sub.4, are independently hydrogen, straight, branched or cyclic alkyl having from one to 10 carbon atoms, or aryl; R.sub.2 and R.sub.3 can be bonded together to form a ring having 5 or 6 atoms.pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.
    Type: Grant
    Filed: February 1, 1996
    Date of Patent: November 4, 1997
    Assignee: The Procter & Gamble Company
    Inventors: John Michael Janusz, James Madison Ridgeway, II
  • Patent number: 5679703
    Abstract: Disclosed is a tricyclic compound represented by formula (I): ##STR1## where X.sup.1 -X.sup.2 represents CH.dbd.CH--CH.dbd.CH, CH.dbd.CH--CH.dbd.N or S--CH.dbd.CH;Y--Z represents CH.sub.2 --O or CH.sub.2 --S; thenL--M represents C.dbd.CR.sup.9 (in which R.sup.9 represents hydrogen or lower alkyl) or CH--CR.sup.10 R.sup.11 (in which each of R.sup.10 and R.sup.11 independently represents hydrogen or lower alkyl);W represents NR.sup.4 (in which R.sup.4 represents hydrogen or lower alkyl) or O;each of R.sup.1, R.sup.2 and R.sup.3 independently represents hydrogen, lower alkyl, lower alkoxy, halogen, nitro, amino or mono or di-lower alkyl-substituted amino;R.sup.5 represents hydrogen or lower alkyl;each of R.sup.6, R.sup.7 and R.sup.8 independently represents hydrogen, halogen, lower alkyl or lower alkoxy;provided that when Y--Z represents CH.dbd.CH or CH.sub.2 CH.sub.2, then L--M represents C.dbd.CR.sup.9 (in which R.sup.9 has the same meaning as defined above),or CH--CR.sup.10a R.sup.11a (in which each of R.sup.
    Type: Grant
    Filed: September 7, 1995
    Date of Patent: October 21, 1997
    Assignee: Kyowa Hakko Kogyo, Co., Ltd.
    Inventors: Masashi Yanase, Toshiaki Kumazawa, Shiro Shirakura, Eiko Oishi, Koji Yamada
  • Patent number: 5672620
    Abstract: A compound having the structure: ##STR1## wherein (a) n is from 1 to about 3;(b) X is selected from the group consisting of O, S, SO, or SO.sub.2 ;(c) Y is independently hydrogen or straight, branched or cyclic alkyl having from 1 to about 4 carbon atoms, or the Y's are bonded together to form an alkanyl ring having from 3 to about 7 atoms;(d) Z is hydrogen or straight, branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen;(e) W is hydrogen or straight, branched or cyclic alkyl, aryl, hydroxy or alkoxy; and(f) R.sub.1 and R.sub.2 are independently hydrogen or straight, branched or cyclic alkyl having from one to 10 carbon atoms, aryl, heterocyclyl, heteroaryl, hydroxy, or alkoxy; or R.sub.1 and R.sub.2 are bonded together to form a ring having from from 3 to about 7 atoms wherein one to three atoms may be heteroatoms.pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.
    Type: Grant
    Filed: February 1, 1996
    Date of Patent: September 30, 1997
    Assignee: The Procter & Gamble Company
    Inventors: Michael Wiard Scherz, Laurence Ichih Wu
  • Patent number: 5631210
    Abstract: Compounds of Formula I and their agriculturally suitable salts are disclosed which are useful for controlling undesired vegetation ##STR1## wherein Q is ##STR2## and R.sup.1 through R.sup.7, m, n, p and q 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 amount of a compound of Formula I.
    Type: Grant
    Filed: June 14, 1996
    Date of Patent: May 20, 1997
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Chi-Ping Tseng
  • Patent number: 5527801
    Abstract: The present invention is to provide an ameliorant for blood lipid metabolism which comprises as an active ingredient N-(6,11-dihydrodibenzo[b,e]thiepin-11-yl)-4-(4-fluorophenyl)-1-piperazineb utanamide or a pharmaceutically acceptable salt thereof, more particularly, to provide a hyperlipidemia inhibitor and an atherosclerosis inhibitor.
    Type: Grant
    Filed: March 14, 1994
    Date of Patent: June 18, 1996
    Assignee: Dainippon Pharmaceutical Co., Ltd.
    Inventors: Yoshinobu Masuda, Hisao Minato, Akihisa Ikeno, Kunihiko Takeyama, Kanoo Hosoki
  • Patent number: 5525736
    Abstract: A process for the production of a 5-7 membered ring cyclic sulfonium salt compound, including a 5-7 membered ring cyclic sulfonium salt compound having a non-nucleophilic anion, is described. Members of the latter group are potentially useful as initiators for cationic polymerizations. The process comprises reacting a 1.4-, 1.5-, or 1.6-diol compound or a 5-7 membered ring cyclic ether compound with a mercapto compound and a strong protonic acid yielding the cyclic sulfonium salt compound. Some compounds described are also novel compounds per se.
    Type: Grant
    Filed: February 23, 1995
    Date of Patent: June 11, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: Jan-Erik Nystrom, Per Engelhardt, Katarina Beierlein, Mikael Sellen, Bjorn Elman, Jan Vagberg, Martin Nylof
  • Patent number: 5519147
    Abstract: Novel polythiophene derivatives are provided along with sensing devices comprising such derivatives in a layer disposed upon a substrate. In preferred embodiments, the polythiophene derivatives bear crown ether moieties covalently bound to 3 positions of adjacent thiophene units.
    Type: Grant
    Filed: February 23, 1995
    Date of Patent: May 21, 1996
    Assignee: Trustees of the University of Pennsylvania
    Inventors: Timothy M. Swager, Michael J. Marsella
  • Patent number: 5420299
    Type: Grant
    Filed: January 24, 1994
    Date of Patent: May 30, 1995
    Assignee: The University of Sydney
    Inventors: Richard K. Haynes, Simone C. Vonwiller
  • Patent number: 5340807
    Abstract: Disclosed is a tricyclic compound represented by the formula (I): ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represents hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, amino, C1-6 alkylamino, halogenated C1-6 alkyl, halogenated C1-6 alkoxy, halogen, nitro, cyano, carboxy, C1-6 alkoxycarbonyl, hydroxymethyl, CR.sup.9 R.sup.10 CO.sub.2 R.sup.11 (wherein each of R.sup.9, R.sup.10 and R.sup.11 independently represents hydrogen or C1-6 alkyl) or CONR.sup.12 R.sup.13 (wherein each of R.sup.12 and R.sup.13 independently represents hydrogen or C1-6 alkyl); R.sup.5 represents hydrogen or C1-6 alkyl; each of R.sup.6, R.sup.7 and R.sup.8 independently represents hydrogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkanoyloxy, C1-6 alkylthio, thiocyanato or halogen; X represents CH or N; Y.sup.1 -Y.sup.2 represents CH.sub.2 --O, CH.sub.2 --(O).sub.n, (wherein n represents 0, 1, or 2), CH.sub.2 CH.sub.2, CH.dbd.CH or CON(R.sup.14) (wherein R.sup.
    Type: Grant
    Filed: December 11, 1992
    Date of Patent: August 23, 1994
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Toshiaki Kumazawa, Masashi Yanase, Hiroyuki Harakawa, Hiroyuki Obase, Shoji Oda, Shiro Shirakura, Koji Yamada, Kazuhiro Kubo
  • Patent number: 5332857
    Abstract: Variously substituted 3,5-dihydroxy-6,8-nonadienoic acids and esters, are blood cholesterol lowering agents and so are useful in the prevention and treatment of cardiovascular diseases such as atherosclerosis.
    Type: Grant
    Filed: July 6, 1992
    Date of Patent: July 26, 1994
    Assignee: Pfizer Inc.
    Inventors: Peter A. McCarthy, Frederick J. Walker
  • Patent number: 5302595
    Abstract: Compounds of the formula I ##STR1## wherein X, Y and v are as defined below, novel intermediates used in their synthesis, and the pharmaceutically acceptable salts of such compounds and intermediates. The compounds of formula I and the novel intermediates used in their synthesis are muscarinic receptor antagonists that are selected for smooth muscle muscarinic sites and are useful in the prevention and treatment of diseases associated with altered motility or tone of smooth muscle, such as irritable bowel syndrome, diverticular disease, urinary incontinence, aesophageal achalasia, and chronic obstructive airways disease.
    Type: Grant
    Filed: January 6, 1993
    Date of Patent: April 12, 1994
    Assignee: Pfizer Inc.
    Inventors: Peter E. Cross, Alexander R. MacKenzie
  • Patent number: 5276053
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: October 6, 1992
    Date of Patent: January 4, 1994
    Assignee: Warner-Lambert Company
    Inventor: Graham Johnson
  • Patent number: 5264538
    Abstract: Cyclic poly(aryl ether) oligomers and mixtures thereof, and methods for the preparation thereof in a highly dilute reaction medium under reaction conditions favorable for ring closure at low degrees of polymerization. These oligomers are represented by the general formula ##STR1## where each Y is divalent oxygen or divalent sulfur, each Ar is an aromatic diradical which comprises one or more C.sub.6 to C.sub.20 arylene groups and has at least one electron withdrawing group attached to an aromatic ring, and n is an integer from 1 to about 20 with the proviso that for integer values of n equal to 1 or 2 all linkages between independent aromatic rings comprise at least one atom.
    Type: Grant
    Filed: June 27, 1990
    Date of Patent: November 23, 1993
    Assignee: The Dow Chemical Company
    Inventors: Michael J. Mullins, Edmund P. Woo, Kimberly E. Balon, Daniel J. Murray, Cheng-Cheng C. Chen
  • Patent number: 5242931
    Abstract: Novel Tricyclic compound represented by formula ##STR1## possess a TXA.sub.2 biosynthesis inhibiting act and/or a TXA.sub.2 receptor antagonizing activity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.
    Type: Grant
    Filed: March 23, 1992
    Date of Patent: September 7, 1993
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii
  • Patent number: 5216178
    Abstract: Novel aminoalkylthiodibenzoxepins, physiologically tolerable acid addition salts thereof, a method of preparing same, pharmaceutical and veterinary preparations including same and methods of treating by administering same are disclosed. These compounds are useful as analgesic, antidepressant and anticonvulsant agents. A process for selectively reducing olefins by alkaline earth metals in loweralkanols is also disclosed.
    Type: Grant
    Filed: August 15, 1991
    Date of Patent: June 1, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Helen H. Ong, Vernon B. Anderson, James A. Profitt
  • Patent number: 5192765
    Abstract: Amines of the following formula: ##STR1## where the variables are defined in the specification are useful in the treatment of diseases associated with altered motility and/or tone of smooth muscle.
    Type: Grant
    Filed: June 6, 1991
    Date of Patent: March 9, 1993
    Assignee: Pfizer Inc.
    Inventors: David Alker, Robert J. Bass, Peter E. Cross
  • Patent number: 5180736
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: May 17, 1991
    Date of Patent: January 19, 1993
    Assignee: Warner-Lambert Company
    Inventor: Graham Johnson
  • Patent number: 5158943
    Abstract: A sulfur-containing hetrocyclic compound of the formula (I) ##STR1## wherein the ring A is an optionally substituted benzene ring, R is a hydrogen atom or an optionally substituted hydrocarbon residue, B is a carboxyl group which may be esterified or amidated, X is --CH(OH)-- or --CO--, and n is an integer of 0, 1 or 2, or its salt, which is useful in the prevention or treatment of osteoporosis.
    Type: Grant
    Filed: May 23, 1991
    Date of Patent: October 27, 1992
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takashi Sohda, Iwao Yamazaki
  • Patent number: 5142054
    Abstract: Disclosed are new 1,3-dioxenones having the formulae ##STR1## in an optically pure state, a process for preparing same and the use thereof.
    Type: Grant
    Filed: February 12, 1991
    Date of Patent: August 25, 1992
    Assignee: Studiengesellschaft Kohle mbH
    Inventors: Kurt Schaffner, Martin Demuth