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JP2005504086A |
Efficient chemical processes for preparing high yields, purities, and different polymorphic forms of 17-allyl amino geldanamycin (17-AAG) and other ansamycins are described and claimed.
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JP2005035983A |
To provide a piperazine derivative having MC4 (melanocortin 4) receptor antagonistic activity.This treating agent contains a piperazine derivative expressed by formula (1) [wherein, (n) is an integer of 1-8; R1 is H or a 1-10C alkyl; A i...
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JP2004339061A |
To obtain a new benzene derivative having a vanilloid receptor agonist activity and useful as a medicine such as a prophylactic/ therapeutic agent for pollakiuria/urinary incontinence or an analgesic agent.A compound is represented by fo...
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JP3593523B2 |
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JP2004532848A |
The present invention is directed to novel thalidomide derivative compounds that have activity as anti-angiogenic compounds. More particularly the compounds have the general structure: where R1 is selected from the group consisting of H,...
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JP2004524266A |
Compounds of formula I: wherein A, B, D, and R are as defined herein and their agriculturally acceptable salts are disclosed as effective insecticides. In addition, compositions comprising an insecticidally effective amount of a compound...
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JP2004520372A |
This invention provides the use of macrocyclic amines for inhibition of cellular invasion or angiogenesis. Compounds and pharmaceutical compositions of this invention are useful in the treatment of conditions characterized by cellular in...
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JP2004137165A |
To provide a method for producing a nitrogen-containing heterocyclic compound, by which the nitrogen-containing heterocyclic compound having a nitrogen atom and other different kind atoms and having various uses can easily be produced fr...
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JP3523887B2 |
PURPOSE: To provide a novel compound having excellent choline esterase- inhibiting activity and a monoamine reintrojection-inhibiting activity and useful as a medicine for treating and preventing senile dementia. CONSTITUTION: A compound...
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JP2004123694A |
To provide a method for producing an optically active sulfoxide derivative having a CCR5 antagonistic action or its intermediate without side-reaction, e.g., racemization, Pummerer rearrangement.The optically active compound (I) is produ...
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JP2004509947A |
The present invention relates to highly enantiomerically pure lactam-substituted propanoic acid derivatives and methods of making and using therefor. The invention involves a multi-step synthesis to produce the lactam compounds. In one s...
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JP2004509968A |
Disclosed are substantially enantiomerically pure bis-phosphine compounds comprising a substantially enantiomerically pure chiral backbone linking two phosphine residues wherein one of the phosphine residues has three phosphorus-carbon b...
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JP2004508373A |
Disclosed are cyclic and acyclic amidines, pharmaceutical compositions containing such amidines, and their use in treating or preventing progesterone receptor mediated diseases or conditions, such as osteopenia and osteoporosis.
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JP2004083554A |
To provide a production process of a lactum compound by which the compound is produced in a high yield under a mild reaction condition using an economically favorable solid catalyst in conducting Beckmann rearrangement reaction of a cycl...
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JP2004059553A |
To provide a method for producing an amide compound in high yield by the Beckmann rearrangement of an oxime compound in a liquid phase under a mild reaction condition.The method for the production of an amide compound comprises the rearr...
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JP2004505044A |
The present invention concerns methods for treating cell proliferative diseases, tumors associated with viral infections, and certain viral infections. The disclosed methods use compounds which inhibit heat shock protein 90 proteins. Suc...
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JP2004504356A |
The present invention features methods for inhibiting HCV replication and processing by targeting heat shock protein 90 (HSP90). HSP90 is a cellular chaperone protein that was found to be an essential factor in NS2/3 self-cleavage. HSP90...
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JP3487611B2 |
PURPOSE: To obtain new compds. useful as dual inhibitors having inhibitory activity against angiotensin converting enzyme and neutral endopeptidase in the treatment of hypertension, congestive heart failure, hepatocirrhosis, etc. CONSTIT...
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JP2003321443A |
To provide a method for the continuous production of ω-lauryl lactam under high temperature and pressure water condition in high efficiency.The ω-lauryl lactam can be synthesized in high efficiency by introducing cyclododecanone oxime ...
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JP3367670B2 |
Pharmaceutically useful nitrogen containing cyclic oxime and amine substituted compounds are disclosed which are azabicyclo[2.2.2]oximes, azabicyclo[2.2.2]-amines, azabicyclo[3.2.1]oximes and amine containing heterocyclic oximes wherein ...
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JP2002541255A |
Bifunctional molecules comprising two hsp-binding moieties which bind to hsp 90 in the pocket to which ansamycin antibiotics bind connected via a linker are effective for inducing the degradation and/or inhibition of HER-family tyrosine ...
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JP2002540197A |
Compounds of formula (I) are antibacterial agents wherein: R3 and R4, taken together with the carbon atoms to which they are respectively attached, form an optionally substituted saturated carbocyclic or heterocyclic ring of 5 to 16 atom...
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JP2002533452A |
The present invention provides compounds of formula (I) and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediat...
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JP2002241368A |
To provide an excellent neuropeptide Y(NPY) antagonist, i.e., an antifeeding agent, a therapeutic agent for myocardial infarction, a therapeutic agent for angina pectoris and an antihypertensive agent.A compound represented by the formul...
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JP2002526535A |
The present invention relates to biphenylene lactams of Formula II which are ligands at the prostaglandin receptors, as well as a method for treating prostaglandin mediated diseases comprising administration to a patient in need of such ...
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JP2002520369A |
the present invention provides water-soluble drugs, in particular, water-soluble analogues of geldanamycin, and compositions comprising the same. This invention also provides a method of rendering water-insoluble drugs soluble in water t...
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JP3291303B2 |
A hydrocarbon derivative is produced by the vapour phase reaction of a hydrocarbon with substantially pure oxygen in the presence of a suitable catalyst in a reactor 2. The product is removed in a scrubber 8, carbon monoxide, present in ...
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JP2002510672A |
The invention is directed to an anion-complexing compound with the formula Iwherein R1 is a six-membered ring, Y' is -NHC(X)NH-, and Y'' is selected from the group consisting of -NHC(X')-, -C(X')NH-, and -NHC(X') NH-; and wherein X and X...
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JP2002511068A |
Compounds of formula (1) or (2), enantiomers thereof, mixtures thereof, and pharmaceutically acceptable salts thereof:wherein: n is 0, or 1; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl; and R<1 >i...
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JP3257709B2 |
PURPOSE: To prepare new substituted N-biphenyl lactams that are angiotensin II receptor antagonists and effective for treating hypertension, congestive heart failure, elevated ocular pressure, cerebral stroke, angina, cardiac insufficien...
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JP2002504549A |
Disclosed are compounds of formula (I) or pharmaceutically acceptable addition salts thereof wherein: Y represents oxygen or sulfur; Z is nitrogen or CH; R1, R2 and R3 represents hydrogen, halogen, hydroxy, alkoxy, alkyl, trifluoromethyl...
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JP2002503228A |
The field of this invention is antitumor antibiotics. More particularly, the present invention relates to analogs of duocarmycin and CC-1065, which analogs have antitumor antibiotics activity.
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JP3242980B2 |
PURPOSE: To provide a new polycyclicamine compd. which has pharmaceutically floating properties like a neurokinin receptor antagonist and is useful for the treatment for substance P-dependent and neurokinin-dependent pathological conditi...
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JP2001526266A5 |
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JP2001526266A |
Selected novel azepine and larger medium ring compounds are effective for prophylaxis and treatment of inflammation, tissue degradation and related diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutical...
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JP2001322981A |
To provide a method for producing an N,N'-carbonylbislactam by reacting phosgene with at least 1 kind of lactam in the presence of a tertiary amine.This method for producing the N,N'-carbonylbislactam is provided by selecting the tertiar...
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JP2001316370A |
To provide a method of producing a cyclic compound that is useful in medicines, foods, cosmetics, chemicals and as an intermediate thereof through a shortened process that is safe and suitable for bulk production.A compound of formula (1...
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JP2001520215A |
The present invention relates to pharmaceutically acceptable compounds, including acylguanidine compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the inv...
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JP3223192B2 |
Pharmaceutically useful nitrogen containing cyclic oxime and amine substituted compounds of the formula which are azabicyclo[2.2.1]oximes, azabizyclo[2.2.2]oximes, azabicyclo[2.2.1]amines, azabicyclo[2.2.2]amines, azabicyclo[3.2.1]oximes...
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JP2001513565A |
Compounds of structural formula (I) where A is a lipophilic group including an aliphatic bridging group, B is a lipophilic group, D is a group having at least one amino or substituted amino group and R is hydrogen, alkyl or cycloalkyl, a...
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JP3202364B2 |
PURPOSE: To efficiently obtain the subject compd. and useful for polar solvent, extractant, etc., in a high yield hydrogenating the specific compd. at a high temp. and under a high pressure in the presence of a catalyst, a specific amine...
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JP2001509151A |
Macrocyclic compounds of formula (I) are potent inhibitors of matrix metalloproteinase and are useful in the treatment of diseases in which matrix metalloproteinase play a role. Also disclosed are matrix metalloproteinase inhibiting comp...
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JP2000256218A |
To produce a cyclic and/or polymerized compound by the metathesis of a starting substance containing at least two functional groups in the form of an alkene or alkyne unit which is substituted or not substituted. This method for a cyclic...
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JP2000239166A |
To obtain the subject new compound as a nitrogen-contg. cyclic oxime useful as an analgesic or a therapeutic agent for dysgnosia syndrome. This new compound is a compound of formula I [(n) is 1 or 2; R2 is H or a 1-4C alkyl; R3 is H, a 1...
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JP2000212163A |
To obtain a new compound useful as an analgesic, a medicine for treating recognition-declining syndrome. 1 A compound of formula I [(n) is 0, 1-4; R2 is H, a 1-4C alkyl; R3 is H, a 1-6C alkyl, hydroxy, a 1-4C alkoxy or the like; R is H, ...
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JP2000504730A |
The present invention relates to pharmaceutically acceptable compounds, including certain substituted indolinyl and derivatives thereof, 1,2,3,4-tetrahydroquinolinyl and derivatives thereof, 1,2,3,4-tetrahydroisoquinolinyl, benz[cd]indol...
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JP2000103781A |
To obtain the subject new compound useful as a raw material for liquid crystal materials, electronic materials, gas-permeable membrane, or the like.This new compound is represented by formula I (R1 and R2 are each H or a substituent; Q i...
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JP2000044539A |
To provide a new optically active cyclic amino acid ester derivative easily producible from a disubstituted aliphatic carboxylic acid and useful as an intermediate for an optically active cyclic amino acid which is useful as an intermedi...
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JP2971053B2 |
Compounds of formula (V) : wherein R2 represents a group R6-A- wherein A represents a divalent straight or branched, saturated or unsaturated hydrocarbon chain of up to 6 C atoms which may be interrupted by an O or S atom, and R6 represe...
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JP2969207B2 |
PURPOSE: To obtain an oxytocin antagonistic agent, comprising benzoheterocyclic compound as an active ingredient and having suppressing actions on matrical smooth muscles, milk release and synthesis and release of prostaglandins, vasodil...
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