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6028084 |
Pyrazole derivatives, method for preparing same, and pharmaceutical compositions containing said derivatives
Compounds of formula (I), wherein R 1 is fluorine, hydroxy, (C 1 -5) alkoxy, (C 1 -5) alkylthio, hydroxy(C 1 -5)alkoxy, a -NR 10 R 11 , group, cyano, (C 1 -5) alkyl-sulphonyl or (C 1 -5)...
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6025353 |
Method of using cyclooxygenase-2 inhibitors as anti-angiogenic agents
This invention relates to the use of cyclooxygenase-2 inhibitors or derivatives thereof in preventing and treating angiogenic disorders.
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6020356 |
Pharmaceutical composition for the treatment of autoimmune diseases
A pharmaceutical composition comprising an anti-inflammatory drug capable of suppressing the production of cytokines (CSAID) an immunosuppressant and a pharmaceutically acceptable excipient.
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6017932 |
Pharmaceutical compositions containing at least one NSAID having increased bioavailability
A novel composition for increasing the bioavailability of Non-steroidal Anti-inflammatory Drugs (NSAIDs), particularly those belonging to the category which exhibits its activity by selectively...
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6015829 |
1-phenylpyrazole compounds and medicinal application thereof
1-Phenylpyrazole compounds of the formula (1): ##STR1## which is exemplified by 5-amino-1-(3-cyano-4-isobutoxyphenyl)pyrazole-4-carboxylic acid, an optical isomer thereof and a pharmaceutically...
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6013666 |
Oxirane carboxylic acid derivative and its manufacturing method
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6013644 |
Spiro-substituted azacycles as modulators of chemokine receptor activity
The present invention is directed spiro-substituted azacycles of formula I: (wherein R 1 , R 2 , R 3 , R 4 , R 5 , k, l and m are defined herein) which are useful as modulators of chemokine...
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6010710 |
Direct pour-on skin solution for antiparasitic use in cattle and sheep
The direct pour-on skin solution intended to eliminate parasites, in particular Boophilus microplus, from cattle and sheep comprises from 0.05 to 25%, preferably from 0.05 to 10%, and in particular...
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6001807 |
Use of CRF-antagonists for treating emesis
CRF-antagonists are useful in the treatment of emesis.
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5994359 |
Imino oxyphenyl acetic acid derivatives, methods and intermediates for their preparation and use thereof
2-Iminooxyphenylacetic acid derivatives ##STR1## where the substituents and the index have the following meanings: R 1 is C(CO 2 CH 3 )NOCH 3 (Ia), C(CONHCH 3 )NOCH 3 (Ib), C(CONH 2...
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5981554 |
Method of treatment of sugar plant to improve the sugar content
A method for improving and/or increasing the sugar content and/or preventing reduction of the sugar content of sugar plants, preferably sugar cane, which comprises treating said plants with an...
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5977154 |
Selective β3 adrenergic agonist
The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective β3 adrenergic...
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5972982 |
Heteroaryl-substituted deoxy glycerols and antibacterial and antiviral compositions containing the same
Heteroaryl-substituted deoxy glycerols represented by the general Formulas Ia, Ib and Ic: ##STR1## wherein: X is oxygen (--O--) or sulfur (--S--); R is substituted or unsubstituted straight or...
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5965565 |
Piperidines promote release of growth hormone
The present invention is directed to certain piperidines, pyrrolidines, and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein B is selected from: ##STR2## and R 1 , R 1a , R...
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5965491 |
Pesticidal 1-aryl-3-iminopyrazoles
1-Aryl-3-iminopyrazoles of the formula: ##STR1## wherein R 31 , R 32 , R 33 , R 4 , R 5 , R 12 , R 13 , R 14 , R 15 and Z are as defined in the specification, are useful as pesticides or as...
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5962489 |
Heteroaromatic compounds and crop protection agents containing them
Heteroaromatic compounds of the formulae IA and IB ##STR1## where the dashed line is a double bond between the carbon atom and a Z atom, and the index and the substituents have the following...
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5962492 |
2 cyclo(alkyl and alkenyl) phenyl-alkenylyl heteroaryl compounds and pharmaceutical compositions containing same
Compounds of general formula (1) ##STR1## are described wherein Y is a halogen atom or a group --OR 1 , wherein R 1 is an optionally substituted alkyl group; X is --O--, --S--, or --N(R 6 ),...
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5958948 |
Substituted pyrazoles as CRF antagonists
The compounds of the formula wherein A, R 1 , R 3 , X 1 , Y and Z are as defined herein, have corticotropin-releasing factor (CRF) antagonist activity. They are useful in the treatment of illnesses...
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5955491 |
Method for treating osteoporosis
The present invention provides a cathepsin L inhibitor containing a compound of the formula: ##STR1## wherein R 1 is a hydrogen atom or an arylalkyl, heterocyclic-alkyl or lower alkyl group which...
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5948779 |
Substituted condensation products of n-benzyl-3-indenyl acetamides with heterocyclic aldehydes
Substituted condensation products of N-benzyl-3-indenylacetamides with heterocyclic aldehydes are useful for inducing or promoting apotosis and for arresting uncontrolled neoplastic cell...
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5945382 |
Fungicidal arylpyrazoles
The present invention relates to new derivatives of the family of 3-arylpyrazoles of formula (I), their methods of preparation, the compositions containing them and their utilization for the...
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5935973 |
Heterocyclcarboxamide derivatives and their use as therapeutic agents
Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which A is methylene or O; B is methylene or O; g is 0,1,2,3 or 4; R 1 is an optional substituent; U is an alkylene...
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5932598 |
Prodrugs of benzenesulfonamide-containing COX-2 inhibitors
Prodrugs of COX-2 inhibitors are described as being useful in treating inflammation and inflammation-related disorders.
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5925631 |
Alkylated styrenes as prodrugs to COX-2 inhibitors
The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions...
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5922744 |
Ethane-1-2-diamine derivatives and tachykinin antagonists
The present invention provides a compound of formula: ##STR1## wherein R, R 1 , R 2 , R 3 , R 4 , R 5 , R 6a and R 6b are defined herein or a pharmaceutically acceptable salt thereof, a process...
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5922751 |
Aryl pyrazole compound for inhibiting phosphodiesterase IV and methods of using same
Novel compounds which are effective PDE IV inhibitors are disclosed The compounds possess similar or improved PDE IV inhibition as compared to rolipram, with improved selectivity with regard to,...
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5916908 |
Pharmaceutical pyrazole compositions useful as inhibitors of protein kinases
A method for selectively inhibiting a kinase is disclosed, which comprises contacting a composition containing a kinase with a compound of the formula: ##STR1## wherein: R 1 is lower alkyl, lower...
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5914344 |
Substituted carboxanilide derivative and plant disease control agent comprising same as active ingredient
A substituted carboxanilide derivative represented by the formula (1): ##STR1## wherein A is a hydrogen atom or methyl, B is a methyl or ethyl, and Het is 1-methyl-3-substituted-4-pyrazolyl or...
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5914351 |
Anti-viral aromatic hydrazones
Compounds of the formula ##STR1## wherein Q is a hydrazone derivative; R 1 is hydrogen, halogen, alkyl or alkoxy; R 2 is hydrogen, halogen, alkyl, alkoxy, alkenoxy, alkynyloxy, halomethyl,...
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5914335 |
Pesticidal 1-arylpyrazole-5-sulfinilimine derivatives
Compounds of formula (I): ##STR1## compositions containing them and methods of use to control pests.
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5908852 |
1,3,5 trisubstituted pyrazole compounds for treatment of inflammation
A class of 1,3,5-substituted pyrazoles is described for the treatment of inflammation, including treatment of pain and disorders such as arthritis. Compounds of particular interest are of Formula I...
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5906983 |
High fructose containing insecticide compositions and methods of using the same
A composition effective for the control of insects is disclosed, wherein the composition contains a phenyl pyrazole compound or a halopyridyl compound, and a food attractant containing at least one...
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5891909 |
Amidinohydrazones as protease inhibitors
Amidino and benzamidino compounds, including compounds of the formula: ##STR1## wherein R 1 -R 4 , R 6 -R 9 , Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or...
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5889058 |
Peptidyl derivatives
Methods of use for compounds of formula (I) are described wherein R represent a --CONHOH, carboxyl (--CO 2 H) or esterified carboxyl group; R 1 represents a hydrogen atom or an optionally...
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5872117 |
1,2-ethanediol derivative and salt thereof, process for producing the same, and cerebral function-improving agent comprising the same
This invention relates to a 1,2-ethanediol derivative and a salt thereof, a process for producing the same, and a cerebral function-improving agent comprising the same. The cerebral...
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5859040 |
Synergistic antimicrobial compositions containing 1-hydroxymethylpyrazole and a preservative
Compositions comprising a compound of formula I ##STR1## where R and R' are independently selected from hydrogen and alkyl of 1 to 4 carbon atoms, R" is a moiety selected from the group consisting...
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5858387 |
N-phenylpyrazole-based antiparasitic external device for cattle, in particular ear-rings
The external device such as a ring, in particular an ear-ring, intended to eliminate cattle parasites, in particular Haematobia irritans, formed of a matrix including from 0.1 to 40%, preferably...
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5854232 |
Acyclic anc cyclic amides as neurotransmitter release enhancers
This invention relates to compounds of formula (IA), (IB), (IC) or (ID), wherein m, X, Z, R 2 , R 3 , R 4 , R 5 , R 6 , R 14 and the dotted lines are as defined below, their pharmaceutically...
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5849732 |
Phenol compound having antioxidative activity and the process for preparing the same
Disclosed are a phenol compound represented by the formula (1): ##STR1## wherein R 0 represents H, alkyl or alkyloxy; R 1 represents alkyl; R 2 represents alkyl or alkyloxy; OR 3 represents OH;...
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5837706 |
Drug for neuroprotection
A drug containing a calmodulin inhibitor as an active ingredient is disclosed. This drug is useful in the suppression of neuronal cell death, in particular brain neuronal cell death, due to, for...
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5827863 |
Pyrazole derivatives as angiotensin II antagonists
Compounds of general formula I and their salts and solvates are angiotensin II receptor antagonists and as such are useful in the treatment of hypertension, congestive heart failure and elevated...
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5824674 |
Brefeldin A derivatives and their utility in the treatment of cancer
Provided are brefeldin A derivatives of the formula: ##STR1## wherein one of R 1 and R 2 is H and the other of R 1 and R 2 is a substituent group having 1 to 12 carbon atoms containing a basic...
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5801189 |
Method for combating insects
Use of 1-phenyl pyrazole derivatives for surface treatment to control cockroaches or ants.
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5792783 |
3-heteroaryl-2-indolinone compounds for the treatment of disease
The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
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5780506 |
***WITHDRAWN PATENT AS PER THE LATEST USPTO WITHDRAWN LIST***
Phenylacetic acid derivatives, and use as fungicides
The present invention relates to phenylacetic acid derivatives of the formula I ##STR1## and their salts. The invention additionally relates to processes and intermediates for preparing these...
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5776983 |
Catecholamine surrogates useful as β.sub.3 agonists
Compounds of the formula ##STR1## or pharmaceutically acceptable salts thereof wherein: A is a bond, --(CH 2 ) n -- or --CH(B)--, where n is an integer of 1 to 3 and B is --CN, --CON(R 9 )R 9 ' or...
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5767151 |
3,3-(disubstituted) cyclohexan-1-ylidine acetate dimers and related compounds
The present invention relates to novel 3,3-(disubstituted)-cyclohexan-1-ylidene acetate dimers of Formula (I): ##STR1## and related compounds, pharmaceutical compositions containing these...
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5763461 |
Therapeutic phenoxyalkylheterocycles
Compounds of the formula ##STR1## wherein Pyr is chosen from the group consisting of pyridyl, pyrazyl, pyrimidyl, quinolyl, indolyl and 7-azaindolyl or any of these substituted with one or two...
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5763470 |
Benzopyran compounds and methods for their use
The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
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5760029 |
Spirocycle integrin inhibitors
This invention relates to novel heterocycles, including (S)-2-phenylsulfonylamino-3- 8-(2-pyridinylaminomethyl)-!-1-oxa-2-azaspi ro- 4,5!-dec-2-en-3-yl!carbonylamino! propionic acid, which are...
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