Chalcogen Bonded Directly At The 2-position Of The Oxazole Ring Patents (Class 548/221)
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Patent number: 6624186Abstract: The present invention relates to ion channel modulating agents. More particularly, the present invention relates to a particular class of chemical compounds that has proven useful as modulators of SKCa, IKCa and BKCa channels. In further aspects, the present invention relates to the use of these SK/IK/BK channel modulating agents for the manufacture of medicaments, and pharmaceutical compositions comprising the SK/IK/BK channel modulating agents. The SK/IK/BK channel modulating agents of the invention are useful for the treatment or alleviation of diseases and conditions associated with the SK/IK/BK channels.Type: GrantFiled: May 15, 2001Date of Patent: September 23, 2003Assignee: Neurosearch A/SInventors: Lene Teuber, Palle Christophersen, Dorte Strobaek, Bo Skaaning Jensen
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Publication number: 20030153559Abstract: The invention refers to novel propenecarboxylic acid amidoxime derivatives furthermore N-oxides and/or geometrical isomers and/or optical isomers and/or pharmaceutically suitable acid addition salts and/or quaternary derivatives thereof. The novel compounds are suitable for the treatment of a state connected with oxygen deficit and/or energy deficit, or a disease based on PARP inhibition, especially an autoimmune or neurodegenerative disease, and/or a viral disease, and/or a disease caused by a toxic effect.Type: ApplicationFiled: November 20, 2002Publication date: August 14, 2003Inventors: Peter Literati Nagy, Balazs Sumegi, Kalman Takacs
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Publication number: 20030144263Abstract: Compounds of the formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, 1Type: ApplicationFiled: January 9, 2003Publication date: July 31, 2003Applicant: Syngenta LimitedInventor: Michael Barry Gravestock
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Patent number: 6600048Abstract: The present invention relates to novel herbicidal phenoxypropionic acid N-alkyl-N-2-fluorophenyl amide compounds represented in the following formula (1), a method for preparing thereof, their use to control barnyard grass produced from rice and composition as suitable herbicides. wherein, R is methyl or ethyl group; X is hydrogen, halogen, cyano, C1˜C6 alkyl, C1˜C6 alkoxy, C1˜C3 haloalkyl substituted with 1 to 3 of halogen atom(s), C1˜C3 haloalkoxy substituted with 1 to 3 of halogen atom(s), C2˜C4 alkoxyalkoxy, phenox,benzyloxy, C2˜C6 alkenyl, C2˜C6 alkinyl, C2˜C6 alkenyloxy, C2˜C6 alkinyloxy, or phenyl group; Y is hydrogen or fluoro; n is an integer of 1 or 2 and when n is 2, X can be in a combination of other substituents.Type: GrantFiled: July 30, 2002Date of Patent: July 29, 2003Assignee: Dongbu Hannong Chemical Co., Ltd.Inventors: Dae Whang Kim, Hae Sung Chang, Young Kwan Ko, Jae Wook Ryu, Jae Chun Woo, Dong Wan Koo, Jin Seog Kim
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Patent number: 6593489Abstract: 3,4-Disubstituted-1-cyclopentene compounds, in substantially enantiopure form, have the relative stereochemistry according to formula (1A) or (1B) including the opposite enantiomers thereof, wherein R1 is either COOX, wherein X is selected from the group consisting of alkyl, H, and a salt-forming cation, or CH2OH, whererin the hydroxy group is optionally protected; R2 is H or a protecting group; R3 is H or alkyl, and R4 is selected from the group consisting of H, alkoxy, alkyl, aryl, and aralkyl; or, in the case of formula (1A), R2 and R4 are linked to form an oxazolidonone ring. These compounds can be used to prepare a series of complementary stereochemcially varied cyclopentane scaffolds.Type: GrantFiled: September 11, 2000Date of Patent: July 15, 2003Assignee: ChirotechTechnology LimitedInventors: Mark Edward Brennan Smith, Nadine Derrien
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Patent number: 6586452Abstract: The present invention relates to novel nodulosporic acid derivatives, which are acaricidal, antiparasitic, insecticidal and anthelmintic agents.Type: GrantFiled: July 9, 2001Date of Patent: July 1, 2003Assignee: Merck & Co., Inc.Inventors: Thomas Shih, Steven L. Colletti, Michael H. Fisher, Peter T. Meinke, Howard C. H. Kuo, Prasun K. Chakravarty, Matthew J. Wyvratt, Sriram Tyagarajan, Richard Berger
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Patent number: 6548667Abstract: The present invention provides a novel sulfonamide derivative of general formula (I) useful as an inhibitor of matrix metalloproteinase (MMP), its isomers, pharmaceutically acceptable salts thereof and a process for preparing the same. Since the sulfonamide derivatives of the present invention selectively inhibit MMP activity in vitro, the MMP inhibitors comprising the sulfonamide derivatives as an effective ingredient can be practically applied for the prevention and treatment of all sorts of diseases caused by overexpression and overactivation of MMP.Type: GrantFiled: December 6, 2001Date of Patent: April 15, 2003Assignee: Samsung Electronics Co. Ltd.Inventors: Young-Jun Park, Hae-Young Bae, Ji-Uk Yoo, Myeong-Yun Chae, Sang-Hyun Paek, Hye-Kyung Min, Hyun-Gyu Park, Choon-Ho Ryu, Kyung-Chul Kim, Jeoung-Wook Lee
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Patent number: 6544931Abstract: The invention relates to novel substituted heteroaryloxyacetanilides of the general formula (I), in which n, R, X, and Z are to intermediates for their preparation and to their use as herbicides.Type: GrantFiled: January 16, 2002Date of Patent: April 8, 2003Assignee: Bayer AktiengesellschaftInventors: Klaus-Helmut Müller, Lothar Rohe, Joachim Kluth, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen
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Patent number: 6500847Abstract: Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented. The compounds of the invention have the generalized formulas: wherein r is 0-2, T is selected from and R40 is a mono- or bi-heterocyclic structure. These compounds are useful for inhibiting matrix metalloproteases and, therefore, combating conditions to which MMP's contribute, such as osteoarthritis, rheumatoid arthritis, septic arthritis, periodontal disease, corneal ulceration, proteinuria, aneurysmal aortic disease, dystrophobic epidermolysis, bullosa, conditions leading to inflammatory responses, osteopenias mediated by MMP activity, tempero mandibular joint disease, demyelating diseases of the nervous system, tumor metastasis or degenerative cartilage loss following traumatic joint injury, and coronary thrombosis from athrosclerotic plaque rupture.Type: GrantFiled: April 30, 2001Date of Patent: December 31, 2002Assignee: Bayer CorporationInventors: Michael C. VanZandt, David R. Brittelli, Brian R. Dixon
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Publication number: 20020188131Abstract: Sulphonylbenzazolones of the formula 1Type: ApplicationFiled: April 1, 2002Publication date: December 12, 2002Inventors: Lutz Assmann, Hans-Ludwig Elbe, Robert Markert, Ralf Tiemann, Klaus Stenzel
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Patent number: 6489268Abstract: The present invention relates to high selective herbicidal phenoxypropionic acid alkoxycarbonyl anilid compounds represented in formula 1, method of preparing thereof, their use to control barnyard grass produced from rice, and a composition as suitable herbicides, wherein R is a hydrogen atom, methyl or ethyl group; R1 is a hydrogen atom, C1-C6 alkyl, C1-C6 alkyl substituted with 1 to 3 of the group consisting of hydroxy, carboxyl, and a halogen atom, C3-C6 cycloalkyl, C3-C4 alkenyl, C3-C4 alkinyl, or C2-C4 alkoxyalkyl group; n is an integer of 1 or 2 and when n is 2, R1 can be a combination of other substituents.Type: GrantFiled: January 29, 2002Date of Patent: December 3, 2002Assignee: Dongbu Hannong Chemical Co., Ltd.Inventors: Dae Whang Kim, Hae Sung Chang, Young Kwan Ko, Jae Wook Ryu, Jae Chun Woo, Dong Wan Koo, Tae-Joon Kim
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Patent number: 6486098Abstract: The present invention relates to novel herbicidal phenoxypropionic acid N-alkyl-N-2-fluorophenyl amides represented in formula (1), a method for preparing thereof, their use to control barnyard grass produced from rice and composition as suitable herbicides. In said formula, R is methyl or ethyl group; X is hydrogen, halogen, cyano, C1˜C6 alkyl, C1˜C6 alkoxy, C1˜C3 haloalkyl substituted with 1 to 3 of halogen atom(s), C1˜C3 haloalkoxy substituted with 1 to 3 of halogen atom(s), C2˜C4 alkoxyalkoxy, phenoxy, benzyloxy, C2˜C6 alkenyl, C2˜C6 alkinyl, C2˜C6 alkkenyloxy, C2˜C6 alkinyloxy, or phenyl group; Y is hydrogen or fluoro; n is an integer of 1 or 2 and when n is 2, X can be in a combination of other substituents.Type: GrantFiled: February 20, 2001Date of Patent: November 26, 2002Assignee: Dongbu Hannong Chemical Co. Ltd.Inventors: Dae Whang Kim, Hae Sung Chang, Young Kwan Ko, Jae Wook Ryu, Jae Chun Woo, Dong Wan Koo, Jin Seog Kim
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Patent number: 6472414Abstract: Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure including pharmaceutically acceptable salts thereof or prodrug esters thereof, wherein q is 0, 1 or 2; Rx is H, alkyl, aryl or halogen; A is (1) a bond; (2) —O—; or (3) B is: and wherein L2, L1, R1, R2, R3, R3′, R3a, R3b, R4, R4′, R5, X, are as defined herein.Type: GrantFiled: May 18, 1999Date of Patent: October 29, 2002Assignee: Bristol-Myers Squibb CompanyInventors: Scott A. Biller, John K. Dickson, R. Michael Lawrence, David R. Magnin, Michael A. Poss, Jeffrey A. Robl, William A. Slusarchyk, Richard B. Sulsky, Joseph A. Tino
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Publication number: 20020151721Abstract: Novel optically active or racemic azethidine carboxylic acid derivatives (azethidine-2-carboxylic acid N-carboxyamino acid anhydrides) which are useful as drug intermediates and an industrially advantageous process for producing the same are provided. Namely, a process for obtaining azethidine-2-carboxylic acid N-carboxyamino acid anhydrides starting with azethidine-2-carboxylic acids is provided. Via the azethidine-2-carboxylic acid N-carboxyamino acid anhydrides according to the invention, azethidine derivatives having peptide bond, which are useful as drugs, can be obtained by an industrial and economic process without resorting deblocking reaction.Type: ApplicationFiled: May 9, 2002Publication date: October 17, 2002Inventors: Kazuhiko Matsuo, Kentaro Tsukuya
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Patent number: 6465499Abstract: Sulphonylbenzazolones of the formula in which R1, R2, R3, R4, R5 and Q are each as defined in the description, a process for preparing these compounds and their use as microbicides in crop protection and in the protection of materials.Type: GrantFiled: November 21, 2000Date of Patent: October 15, 2002Assignee: Bayer AktiengesellschaftInventors: Lutz Assmann, Hans-Ludwig Elbe, Robert Markert, Ralf Tiemann, Klaus Stenzel
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Patent number: 6444615Abstract: This invention relates to 1-substituted-phenyl-3-substituted-2-thioxo-4,5-imidazolidinediones and 2,4,5-imidazolidinetriones which have activity as herbicides, to compositions which contain these compounds and to methods of use of these compounds. In particular, the present invention pertains to 2-thioxo-4,5-imidazolidinediones or 2,4,5-imidazolidinetriones wherein a 2,4,5,6-tetrasubstituted phenyl ring is linked to the heterocyclic ring.Type: GrantFiled: April 18, 2000Date of Patent: September 3, 2002Assignee: Dow AgroSciences LLCInventors: Bin Li, Ying Man, Zongjian Zhang, Adam Chi-Tung Hsu
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Publication number: 20020103377Abstract: Piperidinyloxy, pyrrolidinyloxyl and azetidinyloxy compounds of the formula: 1Type: ApplicationFiled: December 5, 2000Publication date: August 1, 2002Inventors: Michele A. Weidner-Wells, Christine Boggs, Dennis Hlasta, Erin Nelson
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Publication number: 20020099074Abstract: The invention relates to a novel anilide compound and a pharmaceutical composition comprising the same.Type: ApplicationFiled: December 19, 2001Publication date: July 25, 2002Applicant: Kowa Company, Ltd.,JapanInventors: Kimiyuki Shibuya, Katsumi Kawamine, Yukihiro Sato, Toshiyuki Edano, Mitsuteru Hirata, Chiyoka Ozaki
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Patent number: 6417213Abstract: A compound of the formula wherein R1 is H or a substituent; m is 1-3; Ar is an aromatic group which may be substituted; X is a bond or a divalent straight-chain group having 1-6 atoms which may be substituted; Y is —S—, —O—, or —N(R2)— (R2 is H or a substituent group), Z is —N═ or —C(R3)═ (R3 is H or a hydrocarbon group), ring A is a benzene ring; ring B is a 5- to 7-membered ring which may be substituted, or a salt thereof is useful for eliciting a prostaglandin I2 receptor agonistic effect.Type: GrantFiled: March 7, 2001Date of Patent: July 9, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Shigenori Ohkawa, Masaki Setoh, Zen-ichi Terashita
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Publication number: 20020055505Abstract: The present invention provides a compound of formula I 1Type: ApplicationFiled: November 1, 2001Publication date: May 9, 2002Inventors: David John Anderson, Jackson B. Hester
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Patent number: 6384281Abstract: A pharmaceutical compound of formula (I) in which R1 and R2 are each hydrogen or C1-4 alkyl, or R1 and R2 together with the nitrogen atom to which they are attached form an azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, or morpholino group, said group being optionally substituted with 1 to 3 C1-4alkyl substituents, R3 is a naphythyl, indolyl, benzothienyl, benzofuranyl, benzothiazolyl, quinolinyl or isoquinolinyl group, said group being optionally substituted, and n is 1 or 2; or a salt or ester thereof.Type: GrantFiled: October 3, 2001Date of Patent: May 7, 2002Assignee: Eli Lilly and CompanyInventors: Martine Keenan, Sandra Ginette Milutinovic, David Edward Tupper
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Publication number: 20020037910Abstract: The invention provides novel anilide compounds and pharmaceutical compositions comprising them.Type: ApplicationFiled: February 21, 2001Publication date: March 28, 2002Inventors: Kimiyuki Shibuya, Katsumi Kawamine, Yukihiro Sato, Toshiyuki Edano, Souhei Tanabe, Masami Shiratsuchi
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Patent number: 6362208Abstract: The invention relates to a novel anilide compound and a pharmaceutical composition comprising the same. The invention relates to a compound represented by the following general formula: represents a divalent residue of benzene with a substituent(s), heterocycle-condensed benzene which may or may not have a substituent, pyridine which may or may not have a substituent, cyclohexane or naphthalene or Ar represents an aryl group which may or may not have a substituent; X represents —NH—, oxygen atom or sulfur atom; Y represents —NR4—, oxygen atom, sulfur atom, sulfoxide or sulfone; Z represents single bond or —NR5—; R4 represents hydrogen atom, a lower alkyl group, an aryl group or a silylated lower alkyl group which may or may not have a substituent; R5 represents hydrogen atom, a lower alkyl group, an aryl group or a silylated lower alkyl group which may or may not have a substituent; and n represents an integer of 0 to 15.Type: GrantFiled: December 6, 1999Date of Patent: March 26, 2002Assignee: Kowa Company, Ltd.Inventors: Kimiyuki Shibuya, Katsumi Kawamine, Yukihiro Sato, Toshiyuki Edano, Mitsuteru Hirata, Chiyoka Ozaki
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Patent number: 6362183Abstract: An aromatic sulfonyl alpha-hydroxy hydroxamic acid compound that, inter alia, inhibits matrix metalloprotease activity is disclosed, as is a treatment process that comprises administering a contemplated aromatic sulfonyl alpha-hydroxy hydroxamic acid compound in an MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: GrantFiled: June 4, 1999Date of Patent: March 26, 2002Assignee: G. D. Searle & CompanyInventors: John N. Freskos, Terri L. Boehm, Brent V. Mischke, Robert M. Heintz, Joseph J. McDonald, Gary A. DeCrescenzo, Susan C. Howard
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Patent number: 6358885Abstract: This invention relates to certain phenylheterocyclic compounds, herbicidal compositions thereof and a method for their use as general and selective preemergent or postemergent herbicides or plant growth regulants.Type: GrantFiled: April 15, 1999Date of Patent: March 19, 2002Assignees: Mississippi State University, Research Technology Corporation Mississippi StateInventors: Thomas P. Selby, Thomas M. Stevenson
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Patent number: 6358983Abstract: The present invention relates to carboxylic acid derivatives of the formula I the substituents having the meanings explained in the description, preparation and use as endothelin receptor antagonists.Type: GrantFiled: April 27, 2000Date of Patent: March 19, 2002Assignee: Abbott LaboratoriesInventors: Wilhelm Amberg, Rolf Jansen, Heinz Hillen, Stefan Hergenröder, Manfred Raschack, Liliane Unger
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Patent number: 6352958Abstract: Novel herbicidal compounds, compositions containing them, and methods for their use in controlling weeds are disclosed. The novel herbicidal compounds are represented by formula I: where J is a 1-substituted-6-trifluoromethyl-2,4-pyrimidinedione-3-yl, a 1-substituted-6-trifluoromethyl-1,3,5-triazine-2,4-dion-1-yl, a 3,4,5,6-tetrahydrophthalimid-1-yl, a 4-difluoromethyl-4,5-dihydro-3-methyl-1,2,4-triazol-5(1H)-on-1-yl, a 5,6,7,8-tetrahydro-1H,3H-[1,3,4]thiadiazolo[3,5-a]pyridazineimin-1-yl, or a 1,6,8-triazabicyclo[4.3.0]-nonane-7,9-dion-8-yl ring attached at the 7 position of a benzofuran, benzoxazole, indole, 2,3-dihydrobenzimidazole or benzimidazole, and X is selected from hydrogen, halogen, cyano, nitro, and amino. Preferred R groups are optionally substituted alkyl groups.Type: GrantFiled: April 12, 2000Date of Patent: March 5, 2002Assignee: FMC CorporationInventors: Scott D. Crawford, Lester L. Maravetz, George Theodoridis, Benjamin Dugan
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Publication number: 20020016460Abstract: Disclosed are novel compounds of formula (I): 1Type: ApplicationFiled: August 2, 2001Publication date: February 7, 2002Inventors: Roger John Snow, Mario Cardozo, Daniel Goldberg, Abdelhakim Hammach, Tina Morwick, Neil Moss, Usha R. Patel, Anthony S. Prokopowicz, Hidenori Takahashi, Matt Aaron Tschantz, Xiao-Jun Wang
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Patent number: 6340751Abstract: Disclosed is a process for the preparation of a 4-substituted azetidinone derivative, which comprises reacting an azetidinone derivative and an amide compound in the presence of a magnesium compound such as those represented by the following formulas (II): and (IV): represented by the following formula (III): MgR5R6 (III) wherein R5 represents a C1-12 alkyl group, a C2-5 alkenyl group, a 5- to 8-membered alicyclic group which may be substituted by a lower C1-4 alkyl group, a phenyl group which may be substituted by a lower C1-4 alkyl group, a lower C1-4 alkoxy group or a halogen atom or a benzyl group which may be substituted by a lower C1-4 alkyl group, a lower C1-4 alkoxy group or a halogen atom, and R6 represents a halogen atom, a methanesulfonyloxy group, a benzenesulfonyloxy group, a p-toluenesulfonyloxy group, a trifluoromethanesulfonyloxy group, an acetoxy group which may be substituted by a halogen atom or a cyano group or an OR7 group (R7 representingType: GrantFiled: July 19, 1999Date of Patent: January 22, 2002Assignee: Takasago International CorporationInventors: Takao Saito, Toshiyuki Murayama, Takaji Matsumoto, Takashi Miura
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Patent number: 6339042Abstract: The novel compounds of formula I: wherein Het represents an optionally substituted, optionally benzofused nitrogen containing 5- or 6-membered heteroaromatic group; R1 represents an alkyl, alkoxyalkyl or cycloalkyl group; R2 each independently represent an alkyl or alkenyl group, and m is 0 or an integer from 1 to 6, and herbicidal compositions containing such compounds as active ingredients can be utilized in various agricultural methods.Type: GrantFiled: November 29, 1999Date of Patent: January 15, 2002Assignee: American Cyanamid Co.Inventors: Trevor Newton, Helmut Siegfried Baltruschat
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Publication number: 20010053789Abstract: Phenolic compounds with a phenolic molecule to which are covalently linked an oxygen-containing group, a nitrogen- or another oxygen containing group, and a C1-C4 alkoxy group, obtainable from monocotyledonous plants, animals that eat such plants, or chemical synthesis, have been found to act as an antidepressant or otherwise a treatment for bettering mood, a therapy for improving sexual desire or performance, an adjunctive therapy for achieving weight loss, and an adjunctive therapy for substance abuse and addiction. These compounds, at concentrations suitable for human therapeutic use, may be obtained from plants such as corn in their early growth stages and from parts of animals such as the velvet antler tips of deer and elk.Type: ApplicationFiled: April 13, 2001Publication date: December 20, 2001Inventors: Mark J. Rosenfeld, Patricia J. Berger, Norman C. Negus
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Patent number: 6288063Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula (T)xA—B—D—E—G wherein A is an aryl or heteroaryl rings; B is an aryl or heteroaryl ring or a bond; each T is a substituent group; x is 0, 1, or 2; the group D represents the group E represents a two or three carbon chain bearing one to three substituent groups which are independent or are involved in ring formation, possible structures being shown in the text and claims; and the group G represents and with the proviso that when G is each of the substituents on E is an independent substituent; and include pharmaceutically acceptable salts thereof.Type: GrantFiled: May 27, 1998Date of Patent: September 11, 2001Assignee: Bayer CorporationInventors: Harold Clinton Eugene Kluender, David Ross Brittelli, William Riley Schoen, Sookhee Nicole Ha
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Patent number: 6271248Abstract: Compounds of the formula wherein X, Y, R1, R2, R3, R4 and R5 are as described herein, inhibit the activity of endothelin.Type: GrantFiled: January 20, 2000Date of Patent: August 7, 2001Assignee: Bristol-Myers Squibb CompanyInventors: Natesan Murugesan, Joel C. Barrish, John Lloyd
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Patent number: 6268313Abstract: The dihalopropene compounds of the general formula [I] have excellent insecticidal/acaricidal activity, so that they are satisfactorily effective for the control of noxious insects, mites and ticks.Type: GrantFiled: March 7, 2000Date of Patent: July 31, 2001Assignee: Sumitomo Chemical Company, LimitedInventors: Noriyasu Sakamoto, Sanshiro Matsuo, Masaya Suzuki, Taro Hirose, Kazunori Tsushima, Kimitoshi Umeda
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Patent number: 6204278Abstract: The invention provides novel anilide compounds and pharmaceutical compositions comprising them. The invention relates to compounds of a formula: where Ar is an optionally-substituted aryl group; R4 and R5 are the same or different, and each is a hydrogen atom, a lower alkyl group, or a lower alkoxy group; and R4 and R5 may together form a lower alkylene group of which one or more methylene moieties may optionally be substituted by oxygen and/or sulfur atoms; X is —NH—, or oxygen or sulfur atom; Y is —NH—, an oxygen or sulfur atom, or a sulfoxide or sulfone group; Z is a single bond, or —NH6—; R6 represents a hydrogen atom or a lower alkylene group; and n is an integer of from 0 to 15; and their salts and solvates. The compounds of the invention are useful as pharmaceutical compositions, especially as acyl coenzyme A cholesterol acyltransferase (ACAT) inhibitors.Type: GrantFiled: May 19, 1997Date of Patent: March 20, 2001Assignee: Kowa Company, Ltd.Inventors: Kimiyuki Shibuya, Katsumi Kawamine, Yukihiro Sato, Toshiyuki Edano, Souhei Tanabe, Masami Shiratsuchi
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Patent number: 6204380Abstract: Carboxylic acid ester derivatives of formula (1): wherein R is C1-C6 alkyl, R2 and R3 are independently hydrogen or C1-C3 alkyl, and Q is optionally substituted phenyl, can be easily converted by ring closing into pyridazin-3-one derivatives of formula (7): The carboxylic acids of formula (1) can be produced by reacting hydrazone compounds of formula (5): wherein R3 and Q are as defined above, with malonic acid monoester derivatives of formula (6): wherein R and R2 are as defined above, in the presence of a base.Type: GrantFiled: April 21, 1999Date of Patent: March 20, 2001Assignee: Sumitomo Chemical Company, LimitedInventor: Takashi Furukawa
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Patent number: 6187944Abstract: Acrylonitrile compounds having pesticidal activity of formula (I) and salts thereof. wherein Q is Y is ═C(R4)— or ═N—, R1 is alkyl, haloalkyl, etc., each of R2 and R3 is halogen, alkyl which may be substituted, alkenyl which may be substituted, etc., R4 is hydrogen, halogen, alkyl or haloalkyl, 1 is from 1 to 4, m is from 0 to 5, n is from 0 to 3, q is from 0 to 4, when 1 is 2 or more, a plurality of R2 may be the same or different, when each of m, n and q is 2 or more, a plurality of R3 may be the same or different.Type: GrantFiled: August 16, 1999Date of Patent: February 13, 2001Assignee: Ishihara Sangyo Kaisha Ltd.Inventors: Toru Koyanagi, Yuji Nakamura, Masayuki Morita, Koji Sugimoto, Tsuyoshi Ikeda, Munekazu Ogawa
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Patent number: 6180655Abstract: Sulphonylbenzazolones of the formula in which R1, R2, R3, R4, R5 and Q are each as defined in the description. a process for preparing these compounds and their use as microbicides in crop protection and in the protection of materials.Type: GrantFiled: April 9, 1999Date of Patent: January 30, 2001Assignee: Bayer AktiengesellschaftInventors: Lutz Assmann, Hans-Ludwig Elbe, Robert Markert, Ralf Tiemann, Klaus Stenzel
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Patent number: 6174887Abstract: An amide compound of the formula (I): wherein R is amino and the like, A is alkylene and the like, X is O, S and the like, M is arylene and the like, R1, R2, R3 and R4 are H, hydroxy and the like, R5 is H, alkyl and the like, m is an integer of 0-6, R6 is an optionally substituted aryl and the like, and R7 is H, an optionally substituted alkyl and the like, a pharmaceutically acceptable acid addition salt thereof and a pharmaceutical containing same as an active ingredient. The amide compounds exhibit superior suppressive effects on cytokines directly or indirectly involved in inflammations, such as IL-8, IL-1, IL-6, TNF-&agr;, GM-CSF and the like, and are useful for the prophylaxis and treatment of rheumatic diseases, arthritis due to gout and the like.Type: GrantFiled: February 20, 1998Date of Patent: January 16, 2001Assignee: Japan Tobacco Inc.Inventors: Junichi Haruta, Kazuhiko Sakuma, Yoshihiro Watanabe
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Patent number: 6174907Abstract: Benzimidazole compounds represented by the formula set out below and analogs thereof, wherein Y represents a single bond or sulfur atom; Z represents oxygen atom, sulfur atom, or N—R4; R1 and R2 independently represent hydrogen, a halogen atom, alkyl group or other; R3 and R4 independently represent hydrogen, alkyl group, acyl group or other; n and m independently represent an integer of 1, 2, or 3; and L represents a linking group such as C2-12 alkylene group or an alkylene group containing one or more phenylene groups or ether groups. The compounds are useful as an active ingredient of a medicament such as a preventive and therapeutic medicament for hyperlipemia or arterial sclerosis.Type: GrantFiled: September 30, 1999Date of Patent: January 16, 2001Assignee: Fuji Photo Film Co., Ltd.Inventors: Kozo Aoki, Kazuhiro Aikawa
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Patent number: 6172057Abstract: Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflammatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states. The present invention provides low molecular weight, non-peptide inhibitors of matrix metalloproteinases (MMPs) and TNF-&agr; converting enzyme (TACE) for the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.Type: GrantFiled: February 19, 1998Date of Patent: January 9, 2001Assignee: American Cyanamid CompanyInventors: Aranapakam Mudumbai Venkatesan, George Theodore Grosu, Jamie Marie Davis, Baihua Hu, Derek Cecil Cole, Jannie Lea Baker, Marcy Pamela Jacobson, Matthew Robin O'Dell
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Patent number: 6156772Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.Type: GrantFiled: May 14, 1999Date of Patent: December 5, 2000Assignee: Merck & Co., Inc.Inventors: Mark Goulet, Thomas F. Walsh, Feroze Ujjainwalla, Matthew J. Wyvratt, Jr.
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Patent number: 6150416Abstract: The present invention provides non-peptide cathepsin D binding compounds and methods for using such compounds in the detection, labelling and inhibition of cathepsin D.Type: GrantFiled: February 3, 1998Date of Patent: November 21, 2000Assignee: The Regents of the University of CaliforniaInventors: Ellen K. Kick, Jonathan A. Ellman, Irwin D. Kuntz, Christina E. Lee, Guangcheng Liu, Diana C. Roe, A. Geoffrey Skillman
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Patent number: 6140506Abstract: The present invention produces novel cis-oxazolidinone compound which is racemic form or optically active form, of a formula (1) ##STR1## wherein R represents C.sub.1 -C.sub.6 alkyl group, C.sub.2 -C.sub.6 alkenyl group, C.sub.1 -C.sub.6 alkoxyl group, C.sub.1 -C.sub.6 alkylamino group, aryl group or halogen atom, and oxazolidinone ring is at cis-configuration, comprising reacting cis-1,2-indene epoxide of a formula (3) ##STR2## form, with sulfonyl isocyanate compound of a formula (4) ##STR3## in the presence of metal halide catalyst. Further, cis-1-amino-2-indanol is produced by hydrolyzing the oxazolidinone compound. The latter compound is useful as an intermediate of HIV-drug.Type: GrantFiled: December 30, 1998Date of Patent: October 31, 2000Assignee: Nissan Chemical Industries, Ltd.Inventors: Akio Baba, Kenji Suzuki, Yoshinobu Yanagawa, Yoko Ohkuni, Takashi Oda, Masao Shimada, Masami Kozawa
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Patent number: 6110952Abstract: This invention relateds to compounds of formula I, (2-imidazolinylamino)benzoxazoles. The compounds have been found to be alpha-2 adrenocepto agonists and are useful for treatment of disorders modulated by alpha-2 adrenoceptors.Type: GrantFiled: August 9, 1999Date of Patent: August 29, 2000Assignee: The Procter & Gamble CompanyInventors: Raymond Todd Henry, Russell James Sheldon, William Lee Seibel
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Patent number: 6069160Abstract: The invention relates to heteroatom-containing benzocyclopentaneoxazolidinones, to processes for their preparation and their use as medicaments, especially as antibacterial medicaments.Type: GrantFiled: April 12, 1996Date of Patent: May 30, 2000Assignee: Bayer AktiengesellschaftInventors: Andreas Stolle, Dieter Habich, Stephan Bartel, Bernd Riedl, Martin Ruppelt, Hanno Wild, Rainer Endermann, Klaus-Dieter Bremm, Hein-Peter Kroll, Harald Labischinski, Klaus Schaller, Hans-Otto Werling
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Patent number: 6060492Abstract: The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective .beta.3 adrenergic receptor agonists useful in the treatment of Type II diabetes and obesity. The invention provides compounds and method of treating type II diabetes, comprising administering to a mammal in need thereof compounds of the Formula II: ##STR1## The variables in Formula II are defined herein.Type: GrantFiled: June 25, 1997Date of Patent: May 9, 2000Assignee: Eli Lilly and CompanyInventors: Michael Gregory Bell, Thomas Alan Crowell, Donald Paul Matthews, John Hampton McDonald, III, David Andrew Neel, Anthony John Shuker, Mark Alan Winter
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Patent number: 6025374Abstract: A class of substituted azetidine, pyrrolidine and piperidine derivatives are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.Type: GrantFiled: May 28, 1997Date of Patent: February 15, 2000Assignee: Merck Sharp & Dohme, Ltd.Inventors: Jose Luis Castro Pineiro, Caroline Henry, Victor Giulio Matassa, Austin John Reeve, Francine Sternfeld, Leslie Joseph Street
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Patent number: 5998456Abstract: Benzimidazole compounds represented by the formula set out below and analogs thereof, wherein Y represents a single bond or sulfur atom; Z represents oxygen atom, sulfur atom, or N--R.sup.4 ; R.sup.1 and R.sup.2 independently represent hydrogen, a halogen atom, alkyl group or other; R.sup.1 and R.sup.4 independently represent hydrogen, alkyl group, acyl group or other; n and m independently represent an integer of 1, 2, or 3; and L represents a linking group such as C.sub.2-12 alkylene group or an alkylene group containing one or more phenylene groups or ether groups. The compounds are useful as an active ingredient of a medicament such as a preventive and therapeutic medicament for hyperlipemia or arterial sclerosis.Type: GrantFiled: January 16, 1998Date of Patent: December 7, 1999Assignee: Fuji Photo Film Co., Ltd.Inventors: Kozo Aoki, Kazuhiro Aikawa
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Patent number: RE37029Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: November 5, 1998Date of Patent: January 23, 2001Assignee: Aventis Pharmaceuticals Inc.Inventors: Joseph T. Strupczewski, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegler