Chalcogens Bonded Directly At 2- And 5-positions Of The Oxazole Ring Patents (Class 548/227)
  • Publication number: 20030055079
    Abstract: This invention provides compounds of Formula I having the structure 1
    Type: Application
    Filed: August 23, 2002
    Publication date: March 20, 2003
    Applicant: Wyeth
    Inventors: Michael Sotirios Malamas, Elwood Eugene Largis, Iwan Gunawan, Zenan Li
  • Patent number: 6531604
    Abstract: 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: Grant
    Filed: January 11, 2002
    Date of Patent: March 11, 2003
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Tsuneo Yasuma, Haruhiko Makino, Akira Mori
  • Publication number: 20020173664
    Abstract: 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): 1
    Type: Application
    Filed: March 4, 2002
    Publication date: November 21, 2002
    Inventors: Hidetoshi Tsunoda, Michiru Sekiguchi, Hajime Iizuka, Kazuya Sakai
  • Patent number: 6479665
    Abstract: 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: Grant
    Filed: October 29, 2001
    Date of Patent: November 12, 2002
    Assignee: Isochem
    Inventors: Fabrice Cornille, Jean-Luc Copier, Jean-Pierre Senet, Yves Robin
  • Patent number: 6476231
    Abstract: 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: Grant
    Filed: May 11, 2001
    Date of Patent: November 5, 2002
    Assignee: DSM N.V.
    Inventors: Robert P Hof, Wilhelmus Zwaan
  • Publication number: 20020064736
    Abstract: 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: Application
    Filed: September 26, 2001
    Publication date: May 30, 2002
    Applicant: FUJI PHOTO FILM CO., LTD.
    Inventors: Shigeki Uehira, Jun Ogasawara, Kiyoshi Takeuchi, Yasuhiro Shimada, Yasuaki Deguchi
  • Publication number: 20020058819
    Abstract: 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: 1
    Type: Application
    Filed: September 19, 2001
    Publication date: May 16, 2002
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Keiko Nakamura, Takashi Kamikawa
  • Patent number: 6380191
    Abstract: 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: Grant
    Filed: June 16, 2000
    Date of Patent: April 30, 2002
    Assignee: Merck & Co. Inc.
    Inventors: Ranjit C. Desai, Soumya P. Sahoo, Jeffrey P. Bergman, Victoria K. Lombardo, Edward J. Metzger, Hiroo Koyama
  • Publication number: 20020042519
    Abstract: 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: Application
    Filed: November 8, 2001
    Publication date: April 11, 2002
    Applicant: SmithKline Beecham p.l.c.
    Inventors: Robert Gordon Giles, Norman John Lewis, Stephen Moore, Colin Ripley Pool, John Kirby Quick, Michael Urquhart
  • Publication number: 20020037911
    Abstract: 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: Application
    Filed: November 21, 2001
    Publication date: March 28, 2002
    Applicant: Merck & Co., Inc.
    Inventors: Ranjit C. Desai, Soumya P. Sahoo, Jeffrey P. Bergman, Victoria K. Lombardo, Edward J. Metzger, Hiroo Koyama
  • Patent number: 6355672
    Abstract: 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: Grant
    Filed: January 30, 2001
    Date of Patent: March 12, 2002
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Tsuneo Yasuma, Haruhiko Makino, Akira Mori
  • Publication number: 20020025975
    Abstract: 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: Application
    Filed: February 20, 2001
    Publication date: February 28, 2002
    Inventors: Bishwajit Nag, Debendranath Dey, Satyanarayana Medicherla, Partha Neogi
  • Patent number: 6331633
    Abstract: 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: Grant
    Filed: April 6, 1999
    Date of Patent: December 18, 2001
    Assignee: Calyx Therapeutics Inc.
    Inventors: Partha Neogi, Bishwajit Nag, Satyanarayana Medicherla, Debendranath Dey
  • Patent number: 6323225
    Abstract: 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: Grant
    Filed: July 18, 2000
    Date of Patent: November 27, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
  • Patent number: 6320055
    Abstract: 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: Grant
    Filed: April 27, 2000
    Date of Patent: November 20, 2001
    Assignee: BASF Aktiengesellschaft
    Inventors: Michael Slany, Michael Schulz, Martin Schäfer, Edgar Zeller, Klaus Ebel
  • Patent number: 6303640
    Abstract: 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: Grant
    Filed: June 29, 2000
    Date of Patent: October 16, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
  • Patent number: 6288090
    Abstract: 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: Grant
    Filed: July 6, 2000
    Date of Patent: September 11, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
  • Patent number: 6277869
    Abstract: 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: Grant
    Filed: November 28, 2000
    Date of Patent: August 21, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
  • Patent number: 6271243
    Abstract: 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: Grant
    Filed: November 28, 2000
    Date of Patent: August 7, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
  • Patent number: 6262274
    Abstract: 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: Grant
    Filed: October 13, 2000
    Date of Patent: July 17, 2001
    Assignee: Everlight USA, Inc.
    Inventors: Chong-Ming Chen, Yu-Liang Liu, Ya-Chieh Chao, Chien-Huang Wu
  • Patent number: 6251924
    Abstract: 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: Grant
    Filed: July 18, 2000
    Date of Patent: June 26, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
  • Patent number: 6239153
    Abstract: 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: Grant
    Filed: July 18, 2000
    Date of Patent: May 29, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
  • Patent number: 6232330
    Abstract: 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: Grant
    Filed: July 6, 2000
    Date of Patent: May 15, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
  • Patent number: 6218409
    Abstract: 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: Grant
    Filed: July 6, 2000
    Date of Patent: April 17, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
  • Patent number: 6214848
    Abstract: 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: Grant
    Filed: April 30, 1999
    Date of Patent: April 10, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
  • Patent number: 6211205
    Abstract: 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: Grant
    Filed: June 29, 2000
    Date of Patent: April 3, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
  • Patent number: 6211207
    Abstract: 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: Grant
    Filed: July 19, 2000
    Date of Patent: April 3, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
  • Patent number: 6211206
    Abstract: 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: Grant
    Filed: July 19, 2000
    Date of Patent: April 3, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
  • Patent number: 6200997
    Abstract: 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: Grant
    Filed: January 25, 1999
    Date of Patent: March 13, 2001
    Assignee: BASF Aktiengesellschaft
    Inventors: 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
  • Patent number: 6174904
    Abstract: 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: Grant
    Filed: May 27, 1999
    Date of Patent: January 16, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
  • Patent number: 6172089
    Abstract: 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: Grant
    Filed: April 30, 1999
    Date of Patent: January 9, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
  • Patent number: 6169099
    Abstract: 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: Grant
    Filed: April 30, 1999
    Date of Patent: January 2, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
  • Patent number: 6166042
    Abstract: 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: Grant
    Filed: April 30, 1999
    Date of Patent: December 26, 2000
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
  • Patent number: 6166043
    Abstract: 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: Grant
    Filed: April 30, 1999
    Date of Patent: December 26, 2000
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
  • Patent number: 6166217
    Abstract: 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: Grant
    Filed: June 18, 1999
    Date of Patent: December 26, 2000
    Assignee: AlliedSignal Inc.
    Inventors: Vincenzo Cannata, Valeriano Merli, Stefano Saguatti
  • Patent number: 6156773
    Abstract: 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: Grant
    Filed: April 30, 1999
    Date of Patent: December 5, 2000
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
  • Patent number: 6150383
    Abstract: 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: Grant
    Filed: March 30, 1999
    Date of Patent: November 21, 2000
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
  • Patent number: 6150384
    Abstract: 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: Grant
    Filed: April 30, 1999
    Date of Patent: November 21, 2000
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
  • Patent number: 6133293
    Abstract: 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: Grant
    Filed: April 30, 1999
    Date of Patent: October 17, 2000
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
  • Patent number: 6133295
    Abstract: 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: Grant
    Filed: May 27, 1999
    Date of Patent: October 17, 2000
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
  • Patent number: 6121295
    Abstract: 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: Grant
    Filed: April 30, 1999
    Date of Patent: September 19, 2000
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
  • Patent number: 6121294
    Abstract: 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: Grant
    Filed: May 27, 1999
    Date of Patent: September 19, 2000
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
  • Patent number: 6107251
    Abstract: 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: Grant
    Filed: February 12, 1999
    Date of Patent: August 22, 2000
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Akiyoshi Ueda, Yasuyuki Miyazawa, Yoshihiko Hara, Masami Koguchi, Akihiro Takahashi, Takashi Kawana
  • Patent number: 6103742
    Abstract: 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: Grant
    Filed: August 31, 1999
    Date of Patent: August 15, 2000
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
  • Patent number: 6093831
    Abstract: 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: Grant
    Filed: February 26, 1999
    Date of Patent: July 25, 2000
    Assignee: The Regents of the University of California
    Inventors: Henry Rapoport, Tae Bo Sim
  • Patent number: 6080765
    Abstract: 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: Grant
    Filed: May 27, 1999
    Date of Patent: June 27, 2000
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
  • Patent number: 6057351
    Abstract: 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: Grant
    Filed: April 5, 1999
    Date of Patent: May 2, 2000
    Assignee: Societe L'Oreal S.A.
    Inventors: Jean-Baptiste Galey, Lionel Breton, Odile Destree
  • Patent number: 6031112
    Abstract: 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: Grant
    Filed: January 25, 1999
    Date of Patent: February 29, 2000
    Assignee: P.F.C. Italiana S.r.l.
    Inventors: Vincenzo Cannata, Valeriano Merli, Stefano Saguatti
  • Patent number: 6025378
    Abstract: 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: Grant
    Filed: June 18, 1998
    Date of Patent: February 15, 2000
    Assignee: Bayer Aktiengesellschaft
    Inventors: Richard Connell, Siegfried Goldmann, Ulrich Muller, Stefan Lohmer, Hilmar Bischoff, Dirk Denzer, Rudi Grutzmann, Stefan Wohlfeil
  • Patent number: 6020496
    Abstract: 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: Grant
    Filed: May 12, 1999
    Date of Patent: February 1, 2000
    Assignee: Ube Industries, Ltd.
    Inventors: Hiroyuki Miyata, Kikuo Ataka, Nobuya Satake, Masahiko Hagihara