Sanwa Kagaku Kenkyusho Co., Ltd.

Other

Telik, Inc.

Nippon Paper Industries Co., Ltd.

Takahito Jomori

Yoshiro Ishiwata

Yukiharu Matsumoto

Takuji Kakigami

Shoji Yokochi

Kouji Matsushima

Hugo O Villar

Edgardo Laborde

Louise Robinson

Brian T Peterson

Fanying Meng

Steven E Anuskiewicz

Hideaki Inagaki

Takahiko Mitani

Kiichi Sawai

Yuji Hayashi

Akira Tashita

Masayasu Kurono

Ryoichi Unno

Koichi Sugita

Hiroyasu Ebinuma

Noriaki Kato

Saori Kasahara

Hisashi Michishita

Kaori Taniko

Hiroshi Nagano

Yasuo Suzuki

Akira Hasegawa

Yasuaki Kondo

Toshinao Usui

Fumio Takaiwa

Hiromoto Kimura

Hiroshi Ozawa

Toshiyuki Kouzaki

Motohiro Takeda

Mitsuhiro Makino

Yukari Kobara

Hidetsugu Saito

Yoshiro Ishiwatari

Hitoshi Hamashima

Takao Igami

Masahiko Koketsu

Humio Takaiwa

Hiroshi Yasuda

A prophylactic or therapeutic agent for diabetic maculopathy, which can be administered for a long time and exhibits efficacy in a mechanism different from that of existing medicines. The invention relates to a prophylactic or therapeutic agent for diabetic maculopathy, comprising, as an active ingredient, a compound represented by the general formula: wherein X represents a halogen or a hydrogen atom, Rand Rconcurrently or differently represent a hydrogen atom or an optionally substituted C1 to C6 alkyl group, or Rand R, together with a nitrogen atom bound thereto and optionally another nitrogen atom or an oxygen atom, are combined to form a 5- to 6-membered heterocycle. Preferably, the compound is (2S,4S)-6-fluoro -2',5&#x2032;-dioxospiro chroman-4,4&#x2032;-imidazolidine]-2-carboxamide. The invention also provides a model animal with diabetic maculopathy produced by subjecting a diabetic animal to intraocular ischemia/reperfusion to express edema in a retinal visual cell layer or in a macula lutea.

Prophylactic or therapeutic agent for diabetic maculopathy

The present invention is regarding plants and plant storage organs thereof in which GLP-1 derivatives are accumulated, and methods of producing them. The transgenic plants and plant storage organs thereof accumulate tandem repeated GLP-1 derivatives cleavable with intestinal digestive enzyme to monomeric molecules and are produced by methods comprising: integrating into vectors linked DNAs which comprise tandem repeated DNAs encoding the GLP-1 derivative with trypsin resistance in which the amino acid in the 26th position is Gln, the amino acid in the 34th position is Asn or Asp, and C-terminal consists of Arg or Lys to produce monomeric molecules; introducing the vectors into plant cells; and redifferentiating the obtained transformants. The edible transgenic plants and plant storage organs are useful for treating diabetes and can be ingested by diabetic patients.

Plant and plant storage organ having GLP-1 derivative accumulated therein and method of producing the same

A prophylactic or therapeutic agent for diabetic maculopathy, which can be administered for a long time and exhibits efficacy in a mechanism different from that of existing medicines. The invention relates to a prophylactic or therapeutic agent for diabetic maculopathy, comprising, as an active ingredient, a compound represented by the general formula: wherein X represents a halogen or a hydrogen atom, Rand Rconcurrently or differently represent a hydrogen atom or an optionally substituted C1 to C6 alkyl group, or Rand R, together with a nitrogen atom bound thereto and optionally another nitrogen atom or an oxygen atom, are combined to form a 5- to 6-membered heterocycle. Preferably, the compound is (2S,4S)-6-fluoro-2',5&#x2032;-dioxospiro[chroman-4,4&#x2032;-imidazolidine]-2-carboxamide. The invention also provides a model animal with diabetic maculopathy produced by subjecting a diabetic animal to intraocular ischemia/reperfusion to express edema in a retinal visual cell layer or in a macula lutea.

The present invention provides a method for highly producing a recombinant protein in a plant storage organ and a GLP-1 derivative. The plant storage organ in which the recombinant protein is highly produced is obtained by transformation with the use of a vector which comprises a recombinant protein gene, a cytokinin-related gene, a drug-resistant gene and a removable DNA element, in which the cytokinin-related gene and the drug-resistant gene exist in the positions so that they can behave together with the DNA element, while the recombinant protein to be expressed in the plant storage organ exists in the position so that it would not behave together with the DNA element. The GLP-1 is produced by using the method, and a derivative having been stabilized against enzymatic digestion is further provided.

GLP-1 derivative

Compounds which are antagonists of MCP-1 function and are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephrtitis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection; pharmaceutical compositions comprising these compounds; and the use of these compounds and compositions in the prevention or treatment of such diseases.

Antagonists of MCP-1 function and methods of use thereof

A GLP-1 derivative is provided including an amino acid sequence of GLP-1 (7-35) having deletion, substitution and/or addition of one or more amino acids and having Waa-(Xaa)n-Yaa (in which Waa is Arg or Lys, Xaa is Arg or Lys, n is an integer of 0 to 14, and Yaa is Arg, Arg-NH, Lys, Lys-NHor Hse) added to the C-terminus of the peptide having a GLP-1 activity. These derivatives are highly absorbable via a mucous membrane. The GLP-1 derivative can be conferred with resistance to dipeptidyl peptidase IV by substituting amino acid 8 in its GLP-1 amino acid sequence with Ser, or with resistance to trypsin by substituting amino acids 26 and 34 with Gln and Asn, respectively. The absorption efficiency of the GLP-1 derivatives via mucous membranes can be further improved by preparing a composition using a charge-regulated fat emulsion regulated to be negatively charged thereon.

GLP-1 derivative and preparation thereof absorbable via mucous membrane

Chemical compounds which are antagonists of Monocyte Chemoattractant Protein-1 (MCP-1) function, pharmaceutical compositions comprising these compounds, methods of treatment employing these compounds and compositions, and processes for preparing these compounds. The compounds are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection.

The present invention relates to chemical compounds, pharmaceutical compositions comprising said compounds, uses of said compounds and compositions, methods of treatment employing said compounds and compositions, and processes for preparing said compounds. Specifically, this invention relates to novel compounds which are antagonists of MCP-1 function and are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection. More specifically, the invention is related to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases.

Compounds which are antagonists of MCP-1 function and are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection; pharmaceutical compositions comprising these compounds; and the use of these compounds and compositions in the prevention or treatment of such diseases.

There are described sulfated and phosphated saccharide erivatives of the Formula ##STR1## wherein R.sub.1 is hydrogen atom or a residue of sulfate, phosphate or L-fucose; R.sub.2, R.sub.3 and R.sub.4 are hydrogen atom or a residue of sulfate or phosphate, respectively; 1 is an integer of 0 or 1;

Sulfated and phosphated saccharide derivatives, process for the

A potentiator for interferon and an antiviral activity-potentiating composition containing interferon and its potentiator are provided. The potentiator is a mixture of flavin adenine dinucleotide (FAD) and porcine liver extract.

Potentiator for interferon and an antiviral activity-potentiating

A removable rating plug for a circuit breaker provides an active variable impedance in series with a reference resistor between the sensing terminals of the circuit breaker trip circuit to adjust the sensing voltage produced in response to the input current received from current monitors in the protected circuit. The active variable impedance, which is energized by the input current, includes a high gain transistor amplifier, preferably a Darlington transistor, controlled by an operational amplifier. A control circuit includes a pair of reference diodes which match the forward drop across the Darlington transistor when full on, in series with a reference voltage selection circuit which applies a reference voltage to the non-inverting input of the operational amplifier. The voltage at the connection between the Darlington transistor and the reference resistor is fed back to the inverting input of the operational amplifier so that the gain of the amplifier, and therefore the variable impedance in series with the reference resistor, varies with the reference voltage.

Organo-platinum complex and use thereof as anti-tumor agent

An organo-silicone compound of the formula ##STR1## wherein X is a methylene or carbonyl radical, Y is an NH or O, n is an integer, R.sub.1 is a hydrogen atom, halogen atom or alkyl group, R.sub.2, R.sub.3 and R.sub.4 are an alkyl group, alkoxy group, phenyl radical or substituted phenyl radical, respectively, and R.sub.5 is a hydrogen atom or a group of ##STR2## in which X, Y, n, R.sub.2, R.sub.3 and R.sub.4 have the meanings as referred to, and used as an anti-tumor agent or for use in anti-tumor compositions.

Uracil derivatives for use as anti-tumor agents having silicon

Growing community of inventors

Nagoya, Japan

Takahito Jomori