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JP3145533B2 |
PURPOSE: To obtain a new compound useful as an antirheumatic agent. CONSTITUTION: The compound of formula I [A is CH2CH2 or CH=CH; R1 is H or 1-4C alkyl (with the proviso that when A is CH2CH2, R1 is 1-4C alkyl); R2 is H or 1-4C alkyl; n...
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JP3137333B2 |
PURPOSE:To efficiently obtain the subject compound in one pot by reacting guanosine triphosphate (GTP) with GTP cyclohydrase-pyruvoyltetrahydropterin synthase and sepiapterin reductase. CONSTITUTION:Guanosine 5'-triphosphate (GTP) is rea...
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JP2001501596A |
The present invention relates to bioconjugates and the delivery of bioactive agents which are preferably targeted for site-specific release in cells, tissues or organs. More particularly, this invention relates to bioconjugates which com...
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JP3124592B2 |
PURPOSE: To provide the subject compound useful as an antirheumatic agent because of its strong antirheumatic activity and low toxicity. CONSTITUTION: A compound of formula I [R1 is CH2, CH2CH2, CH2S, etc.; R2, is 1-4C alkyl, benzyl; R3 ...
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JP3117137B2 |
Compounds of the formula I or salts thereof I where R1 is H or an aliphatic radical; R2 and R3 are H, alkyl or phenyl; W is O, S, NR4 or NOR4 ; X is CHR2, O or NR4; L is a (substituted) phenyl, naphthyl or monocyclic heteroaryl radical, ...
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JP2000516241A |
This invention is directed to bicyclic pyrimidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compoun...
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JP2000319250A |
To obtain a new compound which has a strong matrix metalloproteinase-13 (collagenase-3)-inhibiting activity and a strong aggrecanase- inhibiting activity. A compound of formula I [R1 is OH or hydroxyamino; R2 is H, a 3 to 7C cycloalkyl o...
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JP2000514447A |
The invention concerns compounds of formula (1) and their use in the preparation of medicines for treating thrombosis.
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JP3100469B2 |
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JP2000511183A |
Corticotropin releasing factor (CRF) antagonists of formula I:and their use in treating anxiety, depression, and other psychiatric and neurological disorders.
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JP3071448B2 |
Sulphonylureas of the formula where A is a bond or a C1-C10-hydrocarbon radical, R<1> is a saturated or unsaturated hydrocarbon radical which is optionally substituted by halogen, saturated or unsaturated alkoxy, alkylthio, alkylsulp...
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JP2000136135A |
To obtain a pharmaceutical composition useful for treating colorectal cancer by separating a mixture of equal amounts of diasteromers of formyl- tetrahydrofolate calcium with a polar solvent. A chiral auxiliary group is applied to any of...
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JP2000109482A |
To obtain a new compound with a glutamate group on the terminal of the homoglutamic acid moiety of a methotrexate derivative, useful as a therapeutic agent for rheumatism.This new compound is shown by the formula (A is CH2, CH2O or the l...
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JP3027613B2 |
A process for the preparation of optically pure diastereoisomers of tetrahydrofolate compounds is described, comprising the conversion, for example, of only the 5,6S,7,8-tetrahydrofolic acid component of a racemic mixture of 5,6,7,8-tetr...
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JP2000086663A |
To obtain the subject new compound exhibiting high affinity for Corticotropin Releasing Factor(CRF) receptor and useful as a therapeutic agent of a preventing agent for diseases such as depression, anxiety, hypertension, inflammation, to...
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JP3023586B2 |
PURPOSE: To provide novel compounds useful as excellent stabilizers for organic materials susceptible to oxidative, thermal or light-induced degradation such as lubricants, hydraulic liquids and natural or (semi)synthetic polymers. CONST...
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JP2000502722A |
This invention relates to compounds of formula (I), wherein A, B, D, E, K, G, R<3> and R<5> are defined as in the specification, and to the pharmaceutically acceptable salts of such compounds. Compounds (I) are corticotropin releasing fa...
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JP2995448B2 |
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JP2970698B2 |
This invention relates to intermediates for the preparation of certain conjugates of folates and antifolates with difluoroglutamic acid which are useful in the treatment of patients suffering from certain neoplastic diseases including le...
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JP2958902B2 |
Three new non-polyglutamatable glutamic acid derivatives in the antifolate series are provided as well as procedures for their preparation. These compounds are: 4-amino-4-deoxy-10-deazapteroyl- tau -methyleneglutamic acid (1); 4-amino-4-...
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JPH11246408A |
To obtain the subject therapeutic agent useful for hepatic function disorders, such as acute/chronic hepatitis, cirrhosis and fatty liver, by including leucovorin as an active ingredient. This therapeutic agent not only has yellow-decrea...
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JPH11509409A |
PCT No. PCT/EP96/03009 Sec. 371 Date May 1, 1998 Sec. 102(e) Date May 1, 1998 PCT Filed Jul. 10, 1996 PCT Pub. No. WO97/03208 PCT Pub. Date Jan. 30, 1997The disclosure concerns a process for the microbial preparation of riboflavin by cul...
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JPH11509193A |
Method for inducing cell damage by administering a restraining agent (RA) to a target cell population at a concentration and under conditions sufficient to retard but not arrest the progress of the target cells through the cell cycle, an...
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JPH11222434A |
To obtain an expression inhibitor of an inducible nitrogen monoxide syntheses having inhibiting actions on the expression of the inducible nitrogen monoxide syntheses and useful for the prophylaxis or therapy of diseases caused by nitrog...
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JPH11193235A |
To obtain the subject preparation capable of reducing the side effects of a methotrexate analogue and improving the compliance of a patient and having a systemic therapeutic effect for the treatment of a chronic inflammatory disease by i...
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JPH11171773A |
To provide the inhibitor capable of exhibiting a high inhibiting action against a dihydrofolic acid reductase which is originated from cycloguanyl- resistant falciparum malaria parasite and has a structure where the 16-alanine and the 10...
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JP2897180B2 |
Riboflavin, vitamin B2, is produced in spherulitic forms by dissolving riboflavin with a primary solvent and adding to the resulting solution a secondary solvent, in which riboflavin is generally not soluble but which is miscible with th...
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JP2894576B2 |
This invention relates to certain conjugates of folates and antifolates with difluoroglutamic acid which are useful in the treatment of patients suffering from certain neoplastic diseases including leukemia, melanomas, carcinomas, sarcom...
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JPH11116482A |
To provide a method for using a tetrahydrofolate of a natural stereoisomeric form in an agent suitable for exerting an influence on the homocysteine- level, especially suitable for assisting the remethylation of the homocysteine. 5-Formy...
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JP2886570B2 |
NEW MATERIAL:The compound of formula I {A<1> and A<2> are C or N provided that at least one is N; R<1> is H, OH, lower alkoxy, etc.; R<2> and R<3> are H, lower alkyl, aryl or arylalkyl; W is group of formula II (R<6> is H or lower alkyl)...
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JPH11106342A |
To obtain a pharmaceutical composition obtained by combining a substantially pure diastereomer of a tetrahydrophorate derivative with a pharmaceutically acceptable carrier. This therapeutic preparation composition obtained by separating ...
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JP2875630B2 |
PCT No. PCT/EP94/00643 Sec. 371 Date Jan. 11, 1996 Sec. 102(e) Date Jan. 11, 1996 PCT Filed Mar. 4, 1994 PCT Pub. No. WO94/21613 PCT Pub. Date Sep. 29, 1994Condensed nitrogen heterocycles, process for their preparation, and their use as ...
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JPH1180131A |
To obtain the subject new compound having strong thyroxine kinase blocking activities and cancer cell growth inhibiting activities, and useful as a carcinostatic agent, an immunosuppressant, a platelet aggregation inhibitor, a therapeuti...
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JPH11502509A |
A therapeutic compound of the chlorambucil family conjugated to two or three acyl groups derived from fatty acids. The compound has the following formula.in which X is chlorambucil, Y is an optional spacer group, AA is an amino acid, B i...
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JPH11502193A |
Novel, heterocyclic compounds having at least one ring nitrogen, disclosed side chains and, in some embodiments, an oxygen ortho to the ring nitrogen inhibit inflammatory responses associated with TNF- alpha and fibroblast proliferation ...
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JP2856760B2 |
Process for the purification of salts of riboflavin 5'-phosphate obtained by phosphorylation of riboflavin and reaction of the riboflavin 5'-phosphate (5'-FMN) contaminated with unreacted riboflavin and isomeric riboflavin monophosphates...
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JPH11501616A |
The present invention relates to a compound of the formula and the pharmaceutically acceptable salts thereof wherein W is a bicyclic heterocyclic ring system. The compounds are alpha -1 adrenergic antagonists and are useful in the treatm...
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JP2847065B2 |
Methods for encapsulating ionizable antineoplastic agents in liposomes using transmembrane potentials. Trapping efficiencies approaching 100% and rapid loading are readily achieved. Dehydration protocols which allow liposomes to be conve...
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JP2844532B2 |
The present invention relates to the preparation of substantially pure diastereoisomers of derivatives of tetrahydrofolate and the use of such diastereoisomers. More particularly the present invention provides a process for the preparati...
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JP2843592B2 |
A process of preparing l -biopterin is disclosed which comprises the steps of: Subjecting to selective Grignard reaction D-ribose having the hydroxyl groups in the 2- and 3-positions protected by an acetal group to give 6-deoxy-3,4-O-alk...
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JPH10330265A |
To obtain a therapeutic agent for liver diseases having promoting action of bilirubin excretion and bile acid excretion and capable of relieving jaundice symptom by including folic acid or its salt as an active ingredient. This medicine ...
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JPH10512850A |
Methods and devices for preventing an adverse reaction of the skin to the presence of a skin-sensitizing agent by administering an effective amount of a potassium-sparing diuretic.
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JP2818799B2 |
Sulphonyl ureas substituted by heterocycles, of the formula in which A denotes a C1-C10-hydrocarbon radical, R<1> denotes saturated or unsaturated alkyl or cycloalkyl which can be substituted by halogen or radicals from the group compris...
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JP2815617B2 |
Compounds of the formula (1) : or pharmaceutically acceptable salts thereof as described, wherein is a pyridine, pyrazine or triazine ring; R<1> is C1-6alkyl, C2-6alkenyl, C3-5cycloalkylC1-6alkyl, or C1-6alkyl substituted by 1 to 6 fluor...
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JPH10510517A |
The use of a compound of formula I in which R1 and R2 are N, X1 and X2 which may be the same or different are hydrogen, hydroxy, or an optionally substituted alkyl, and Z1 and Z2 which may be the same or different are hydrogen, hydroxy, ...
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JP2807577B2 |
The cyclic amide derivative is defined by the formula (I) or a salt thereof: R1-(CH2)n-Z in which R1 is a group derived from a cyclic amide compound, substituted or unsubstituted, n is zero or an integer of 1 to 10 and Z is R2 being an a...
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JP2787587B2 |
Compounds of the formula I, their stereoisomers or their salts (I) wherein A denotes >C(R4)2 or >C=C(R5)2; R1 denotes H, an optionally substituted aliphatic or cycloaliphatic radical, forfuryl, tetrahydrofurfuryl or (substituted) phenyl;...
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JP2787590B2 |
Compounds of the formula I or their salts in which R<1> denotes (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl, where these radicals are substituted by halogen, saturated and unsaturated (C1-C6)alkoxy, (C1-C6)alkylthio, -sulphinyl or -sulp...
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JP2761104B2 |
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JPH1087492A |
To obtain the subject medicinal agent containing a hetrocyclic compound having a specific structure as active ingredient, capable of preventing or treating septicemia, rheumatic inflammation. Crohn's disease, etc., through inhibiting nit...
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