Chalcogens Bonded Directly At 2- And 5-positions Of The Oxazole Ring Patents (Class 548/227)
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Publication number: 20030055079Abstract: This invention provides compounds of Formula I having the structure 1Type: ApplicationFiled: August 23, 2002Publication date: March 20, 2003Applicant: WyethInventors: Michael Sotirios Malamas, Elwood Eugene Largis, Iwan Gunawan, Zenan Li
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Patent number: 6531604Abstract: The invention provides compounds of the formula: wherein the ring A is an optionally substituted benzene ring; R1 is an optionally substituted non-aromatic heterocyclic group; R2 and R3 are independently hydrogen atom or an optionally substituted hydrocarbon group; n is an integer of 0-3; or salts thereof, which are useful as medicines having an osteogenesis promoting effect and chondrogensis promoting effect. The present invention relates to an amine compound having an excellent effect of inhibiting production and/or secretion of amyloid-b protein, a production and use thereof. Especially, it is effective for preventing and/or treating, for example, neurodegenerative diseases, amyloid angiopathy, neurological disorders caused by cerebrovascular disorders, and so forth.Type: GrantFiled: January 11, 2002Date of Patent: March 11, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Tsuneo Yasuma, Haruhiko Makino, Akira Mori
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Publication number: 20020173664Abstract: This invention provides amino acid N-carboxyanhydrides, each of which has an N-acyl substituent on its nitrogen atom, is represented by the following formula (1): 1Type: ApplicationFiled: March 4, 2002Publication date: November 21, 2002Inventors: Hidetoshi Tsunoda, Michiru Sekiguchi, Hajime Iizuka, Kazuya Sakai
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Patent number: 6479665Abstract: The invention relates to a process for the preparation of N-carboxyanhydrides by reaction of the corresponding amino acid with phosgene, diphosgene and/or triphosgene in a solvent medium, characterized in that the reaction is a least partially carried out in the presence of an unsaturated organic compound which has one or more ethylenic double bonds, one of the carbon of at least one ethylenic double bond of which is completely substituted by substituents other than halogen atoms. The N-carboxyanhydrides are thus obtained with better yields and an improved purity.Type: GrantFiled: October 29, 2001Date of Patent: November 12, 2002Assignee: IsochemInventors: Fabrice Cornille, Jean-Luc Copier, Jean-Pierre Senet, Yves Robin
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Patent number: 6476231Abstract: Process for the preparation of N-carboxy-t-leucine anhydride in which the corresponding N-carboxy-t-leucine is subjected to a cyclization with the aid of an acyl halogenide. Preferably, acetyl chloride is used as acyl halogenide. The N-carboxy-t-leucine anhydride obtained optionally is subsequently converted into a t-leucine-N-substituted amide with the aid of the corresponding amine. Preferably, methyl amine is chosen as the amine, and the reaction is carried out in a mixture of water and methanol as solvent.Type: GrantFiled: May 11, 2001Date of Patent: November 5, 2002Assignee: DSM N.V.Inventors: Robert P Hof, Wilhelmus Zwaan
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Publication number: 20020064736Abstract: A dye-forming coupler of the formula (I). A silver halide photographic light-sensitive material that contains at least one dye-forming coupler of the formula (I).Type: ApplicationFiled: September 26, 2001Publication date: May 30, 2002Applicant: FUJI PHOTO FILM CO., LTD.Inventors: Shigeki Uehira, Jun Ogasawara, Kiyoshi Takeuchi, Yasuhiro Shimada, Yasuaki Deguchi
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Publication number: 20020058819Abstract: A method of producing a metal salt of 2,4-oxazolidinedione of the general formula (III) wherein a 2-hydroxycarboxylate of the general formula (I), urea and a metal alkoxide of the formula (II) are reacted in an aromatic hydrocarbon; or a 2-hydroxycarboxylate of the general formula (I) and a metal alkoxide of the formula (II) are added to urea, and, then, they are reacted is provided: 1Type: ApplicationFiled: September 19, 2001Publication date: May 16, 2002Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Keiko Nakamura, Takashi Kamikawa
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Patent number: 6380191Abstract: Substituted 5-aryl-2,4-thiazolidinediones and oxazolidinediones are potent agonists of PPAR, and are therefore useful in the treatment, control or prevention of diabetes, hyperglycemia, hyperlipidemia (including hypercholesterolemia and hypertriglyceridemia), atherosclerosis, obesity, vascular restenosis, and other PPAR &agr; and/or &ggr; mediated diseases, disorders and conditions.Type: GrantFiled: June 16, 2000Date of Patent: April 30, 2002Assignee: Merck & Co. Inc.Inventors: Ranjit C. Desai, Soumya P. Sahoo, Jeffrey P. Bergman, Victoria K. Lombardo, Edward J. Metzger, Hiroo Koyama
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Publication number: 20020042519Abstract: A process for preparing a compound of formula (I, I) or a tautomeric form thereof or a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof, wherein: J represents O or S; T represents a substituted or unsubstituted aryl group and T1 is O or S; which process comprises reducing a compound of formula (II, II) or a tautomeric form thereof or a salt thereof or a solvate thereof, wherein T and T1 are as defined in relation to formula (I), with a complex hydride reducing agent or a source of a complex hydride reducing agent; and thereafter, as required, preparing a pharmaceutically acceptable salt or a pharmaceutically acceptable solvate of the compound of formula (I) or a tautomeric form thereof.Type: ApplicationFiled: November 8, 2001Publication date: April 11, 2002Applicant: SmithKline Beecham p.l.c.Inventors: Robert Gordon Giles, Norman John Lewis, Stephen Moore, Colin Ripley Pool, John Kirby Quick, Michael Urquhart
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Publication number: 20020037911Abstract: Substituted 5-aryl-2,4-thiazolidinediones and oxazolidinediones are potent agonists of PPAR, and are therefore useful in the treatment, control or prevention of diabetes, hyperglycemia, hyperlipidemia (including hypercholesterolemia and hypertriglyceridemia), atherosclerosis, obesity, vascular restenosis, and other PPAR &agr; and/or &ggr; mediated diseases, disorders and conditions.Type: ApplicationFiled: November 21, 2001Publication date: March 28, 2002Applicant: Merck & Co., Inc.Inventors: Ranjit C. Desai, Soumya P. Sahoo, Jeffrey P. Bergman, Victoria K. Lombardo, Edward J. Metzger, Hiroo Koyama
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Patent number: 6355672Abstract: The invention provides compounds of the formula: wherein the ring A is an optionally substituted benzene ring; R1 is an optionally substituted non-aromatic heterocyclic group; R2 and R3 are independently hydrogen atom or an optionally substituted hydrocarbon group; n is an integer of 0-3; or salts thereof, which are useful as medicines having an osteogenesis promoting effect and chondrogensis promoting effect. The present invention relates to an amine compound having an excellent effect of inhibiting production and/or secretion of amyloid-b protein, a production and use thereof. Especially, it is effective for preventing and/or treating, for example, neurodegenerative diseases, amyloid angiopathy, neurological disorders caused by cerebrovascular disorders, and so forth.Type: GrantFiled: January 30, 2001Date of Patent: March 12, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Tsuneo Yasuma, Haruhiko Makino, Akira Mori
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Publication number: 20020025975Abstract: Novel diphenylethylene compounds containing thiazolidinedione or oxazolidinedione moieties are provided which are effective in lowering blood glucose level, serum insulin, triglyceride and free fatty acid levels in animal models of Type II diabetes. In contrast to previously reported thiazolidinedione compounds, known to lower leptin levels, the present compounds increase leptin levels and have no known liver toxicity. The compounds are disclosed as useful for a variety of treatments including the treatment of inflammation, inflammatory and immunological diseases, insulin resistance, hyperlipidemia, coronary artery disease, cancer and multiple sclerosis.Type: ApplicationFiled: February 20, 2001Publication date: February 28, 2002Inventors: Bishwajit Nag, Debendranath Dey, Satyanarayana Medicherla, Partha Neogi
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Patent number: 6331633Abstract: Novel diphenylethylene compounds containing thiazolidinedione or oxazolidinedione moieties are provided which are effective in lowering blood glucose level, serum insulin, triglyceride and free fatty acid levels in animal models of Type II diabetes. In contrast to previously reported thiazolidine compounds, known to lower leptin levels, the present compound increase leptin levels and have no known liver toxicity.Type: GrantFiled: April 6, 1999Date of Patent: December 18, 2001Assignee: Calyx Therapeutics Inc.Inventors: Partha Neogi, Bishwajit Nag, Satyanarayana Medicherla, Debendranath Dey
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Patent number: 6323225Abstract: Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in the mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis and treatment of diabetes.Type: GrantFiled: July 18, 2000Date of Patent: November 27, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
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Patent number: 6320055Abstract: Process for preparing compounds of the formula I in which R is alkyl or aryl, in each case unsubstituted or substituted, R3 is hydrogen, alkyl or aryl, in each case unsubstituted or substituted, and X═O or NH, which comprises reacting an aldehyde R—CHO with CO and a compound of the formula II in which R2 is a group which reacts with a —CO2H group, which is formed during the reaction, with ring-closure to give compounds of the formula I, in the presence of a transition metal catalyst described.Type: GrantFiled: April 27, 2000Date of Patent: November 20, 2001Assignee: BASF AktiengesellschaftInventors: Michael Slany, Michael Schulz, Martin Schäfer, Edgar Zeller, Klaus Ebel
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Patent number: 6303640Abstract: Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in the mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis and treatment of diabetes.Type: GrantFiled: June 29, 2000Date of Patent: October 16, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
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Patent number: 6288090Abstract: Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in the mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis and treatment of diabetes.Type: GrantFiled: July 6, 2000Date of Patent: September 11, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
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Patent number: 6277869Abstract: Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in the mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis and treatment of diabetes.Type: GrantFiled: November 28, 2000Date of Patent: August 21, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
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Patent number: 6271243Abstract: Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in the mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis and treatment of diabetes.Type: GrantFiled: November 28, 2000Date of Patent: August 7, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
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Patent number: 6262274Abstract: A process for preparing N-[1-(S)-ethoxycarbonyl-3-phenylpropyl]-L-alanine N-carboxyanhydride of the following formula (I), is to react N-[1 -(S)-ethyoxy carbonyl-3-phenylpropyl]-L-alanine with XCOOR, wherein X is halogen atom, R is C1-C6 alkyl, to obtain a N-alkoxycarbonyl compound, then reacting with an acyl group activation reagent, finally contact with water. The compound of formula (I) is a key intermediate of ACE inhibitors.Type: GrantFiled: October 13, 2000Date of Patent: July 17, 2001Assignee: Everlight USA, Inc.Inventors: Chong-Ming Chen, Yu-Liang Liu, Ya-Chieh Chao, Chien-Huang Wu
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Patent number: 6251924Abstract: Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in he mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis and treatment of diabetes.Type: GrantFiled: July 18, 2000Date of Patent: June 26, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
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Patent number: 6239153Abstract: Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in the mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis and treatment of diabetes.Type: GrantFiled: July 18, 2000Date of Patent: May 29, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
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Patent number: 6232330Abstract: Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in the mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis and treatment of diabetes.Type: GrantFiled: July 6, 2000Date of Patent: May 15, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
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Patent number: 6218409Abstract: Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in the mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis and treatment of diabetes.Type: GrantFiled: July 6, 2000Date of Patent: April 17, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
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Patent number: 6214848Abstract: Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in the mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis and treatment of diabetes.Type: GrantFiled: April 30, 1999Date of Patent: April 10, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
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Patent number: 6211205Abstract: Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in the mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis and treatment of diabetes.Type: GrantFiled: June 29, 2000Date of Patent: April 3, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
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Patent number: 6211207Abstract: Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in the mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis and treatment of diabetes.Type: GrantFiled: July 19, 2000Date of Patent: April 3, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
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Patent number: 6211206Abstract: Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in the mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis and treatment of diabetes.Type: GrantFiled: July 19, 2000Date of Patent: April 3, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
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Patent number: 6200997Abstract: The present invention relates to heterocyclyl-substituted phenyl compounds of the formula I, where the substituents have the following meanings: Y is halogen, C1-C4-alkyl, C1-C4-haloalkyl or C1-C4-alkoxy; n is 0, 1 or 2, where the radicals Y may be different if n=2; E is a group A or B, where # denotes the bond to the phenyl ring, and G R&agr;, R&bgr;, Y, n, T and Z are each as defined in the description.Type: GrantFiled: January 25, 1999Date of Patent: March 13, 2001Assignee: BASF AktiengesellschaftInventors: Andreas Gypser, Hubert Sauter, Herbert Bayer, Markus Gewehr, Wassilios Grammenos, Thomas Grote, Roland Götz, Bernd Müller, Arne Ptock, Franz Röhl, Volker Harries, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann
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Patent number: 6174904Abstract: Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in the mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis and treatment of diabetes.Type: GrantFiled: May 27, 1999Date of Patent: January 16, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
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Patent number: 6172089Abstract: Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in the mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis and treatment of diabetes.Type: GrantFiled: April 30, 1999Date of Patent: January 9, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
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Patent number: 6169099Abstract: Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in the mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis and treatment of diabetes.Type: GrantFiled: April 30, 1999Date of Patent: January 2, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
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Patent number: 6166042Abstract: Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in the mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis and treatment of diabetes.Type: GrantFiled: April 30, 1999Date of Patent: December 26, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
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Patent number: 6166043Abstract: Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in the mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis and treatment of diabetes.Type: GrantFiled: April 30, 1999Date of Patent: December 26, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
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Patent number: 6166217Abstract: Process for the production of alkoxycarbonyldipeptides intermediates in the synthesis of the lisinopril which comprises protecting both amino functions of the L-lysine with an alkoxycarbonyl group, subsequently making the N-carboxyanhydride of the N6-[alkoxycarbonyl]-L-lysine by treatment with thionyl chloride and making the desired alkoxycarbonyldipeptide by reaction with L-proline in alkaline medium.Type: GrantFiled: June 18, 1999Date of Patent: December 26, 2000Assignee: AlliedSignal Inc.Inventors: Vincenzo Cannata, Valeriano Merli, Stefano Saguatti
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Patent number: 6156773Abstract: Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in the mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis and treatment of diabetes.Type: GrantFiled: April 30, 1999Date of Patent: December 5, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
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Patent number: 6150383Abstract: Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in the mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis and treatment of diabetes.Type: GrantFiled: March 30, 1999Date of Patent: November 21, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
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Patent number: 6150384Abstract: Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in the mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis and treatment of diabetes.Type: GrantFiled: April 30, 1999Date of Patent: November 21, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
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Patent number: 6133293Abstract: Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in the mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis and treatment of diabetes.Type: GrantFiled: April 30, 1999Date of Patent: October 17, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
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Patent number: 6133295Abstract: Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in the mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis and treatment of diabetes.Type: GrantFiled: May 27, 1999Date of Patent: October 17, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
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Patent number: 6121295Abstract: Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in the mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis and treatment of diabetes.Type: GrantFiled: April 30, 1999Date of Patent: September 19, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
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Patent number: 6121294Abstract: Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in the mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis and treatment of diabetes.Type: GrantFiled: May 27, 1999Date of Patent: September 19, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
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Patent number: 6107251Abstract: The present invention is directed to oxazole derivatives represented by the formula [I]; ##STR1## wherein A represents a nitrogen atom or a R.sub.3 -substituted carbon atom;B represents a nitrogen atom, or an unsubstituted or X-substituted carbon atom;Z represents an oxygen atom, sulfinyl or sulfonyl;R.sub.1 and R.sub.2 represent each independently hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 haloalkoxy, C.sub.1 -C.sub.6 haloalkyl or the like;R.sub.3 represents hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, nitro, formyl or acyl;X represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 alkynyl, C.sub.1 -C.sub.6 haloalkyl or the like;Y represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 alkynyl, C.sub.1 -C.sub.6 haloalkyl or the like;m represents an integer of 1 or 2, andn represents an integar of 1, 2, 3 or 4, and the salts thereof.Type: GrantFiled: February 12, 1999Date of Patent: August 22, 2000Assignee: Nippon Soda Co., Ltd.Inventors: Akiyoshi Ueda, Yasuyuki Miyazawa, Yoshihiko Hara, Masami Koguchi, Akihiro Takahashi, Takashi Kawana
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Patent number: 6103742Abstract: Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in the mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis and treatment of diabetes.Type: GrantFiled: August 31, 1999Date of Patent: August 15, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
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Patent number: 6093831Abstract: Amino acids are derivatized for use in peptide synthesis by conversion to N-carboxyanhydrides that are N-proected by either a trityl or a phenylfluorenyl group.Type: GrantFiled: February 26, 1999Date of Patent: July 25, 2000Assignee: The Regents of the University of CaliforniaInventors: Henry Rapoport, Tae Bo Sim
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Patent number: 6080765Abstract: Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in the mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis and treatment of diabetes.Type: GrantFiled: May 27, 1999Date of Patent: June 27, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
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Compounds of the 3-aryl 2,4 dioxo oxazolidine family and use thereof in cosmetic and pharmaceuticals
Patent number: 6057351Abstract: Novel compounds of the aryl 2,4 dioxo oxazolidine family, a method for synthesizing same, compositions containing said compounds, and the use of an effective amount of at least one of said compounds as an active principle in a physiologically acceptable medium in a cosmetic composition or for preparing a pharmaceutical composition, are disclosed. Said compound or said compositions are useful for inducing and/or stimulating hair growth and/or controlling hair loss and/or treating hyperseborrhea and/or acne.Type: GrantFiled: April 5, 1999Date of Patent: May 2, 2000Assignee: Societe L'Oreal S.A.Inventors: Jean-Baptiste Galey, Lionel Breton, Odile Destree -
Patent number: 6031112Abstract: Process for the production of alkoxycarbonyldipeptides intermediates in the synthesis of the lisinopril which comprises protecting both amino functions of the L-lysine with an alkoxycarbonyl group, subsequently making the N-carboxyanhydride of the N6-[alkoxycarbonyl]-L-lysine by treatment with thionyl chloride and making the desired alkoxycarbonyldipeptide by reaction with L-proline in alkaline medium.Type: GrantFiled: January 25, 1999Date of Patent: February 29, 2000Assignee: P.F.C. Italiana S.r.l.Inventors: Vincenzo Cannata, Valeriano Merli, Stefano Saguatti
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Patent number: 6025378Abstract: The bicyclic heterocyclic compounds are prepared by reaction of correspondingly substituted carboxylic acids with amines, in particular with phenylglycinolamine. The bicyclic heterocyclic compounds according to the invention are suitable as active compounds in medicaments, in particular in medicaments having an antiatherosclerotic action.Type: GrantFiled: June 18, 1998Date of Patent: February 15, 2000Assignee: Bayer AktiengesellschaftInventors: Richard Connell, Siegfried Goldmann, Ulrich Muller, Stefan Lohmer, Hilmar Bischoff, Dirk Denzer, Rudi Grutzmann, Stefan Wohlfeil
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Patent number: 6020496Abstract: 5-Alkoxy-2(3H)-oxazolone compounds represented by general formula (1); and a R.sup.1 process for the preparation thereof, wherein R.sup.1 is hydrogen, optionally substituted C.sub.1 -C.sub.10 alkyl, optionally substituted C.sub.3 -C.sub.10 cycloalkyl, optionally substituted C.sub.2 -C.sub.10 alkenyl or optionally substituted phenyl; R.sup.2 is hydrogen, optionally substituted C.sub.1 -C.sub.10 alkyl, optionally substituted phenyl or unsubstituted C.sub.2 -C.sub.10 alkenyl; R.sup.3 is optionally substituted C.sub.1 -C.sub.10 alkyl, optionally substituted C.sub.3 -C.sub.10 cycloalkyl, optionally substituted C.sub.2 -C.sub.10 alkenyl excluding 2-alkenyl, or optionally substituted phenyl.Type: GrantFiled: May 12, 1999Date of Patent: February 1, 2000Assignee: Ube Industries, Ltd.Inventors: Hiroyuki Miyata, Kikuo Ataka, Nobuya Satake, Masahiko Hagihara