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7538114 |
Glycine transporter-1 inhibitors
The present invention provides compounds that are glycine transporter 1 (hereinafter referred to as GlyT-1) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition...
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7449466 |
Cyclic aminophenyl sulfamate derivative
This invention provides cyclicamino-phenyl sulfamate derivatives represented by a formula
wherein each of R 1 and R 2 stands for hydrogen or lower alkyl; each of R 3 and R 4 stands for...
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7435851 |
Puleganic amides
The present invention provides substituted puleganic amides and compositions thereof, which are both useful as a topical treatment for skin, such as a repellant for insects and arthropods.
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7396834 |
4(Phenyl-piperazinyl-methyl) benzamide derivatives and their use for the treatment of pain or gastrointestinal disorders
Compounds of general formula: wherein R 1 and R 2 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared....
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7381821 |
Piperazine derivatives and their use as synthesis intermediates
The present invention relates to new enantiomerically pure piperazine derivatives of formula (I) wherein Y represents hydroxy or a leaving group and n is 1, 2, 3, 4 or 5, and to their use as...
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7375106 |
Synergistic combination of an opioid analgesic and a NSAID
The invention relates to a combined pharmaceutical preparation comprising an opioid diarylmethyl piperazine compounds and a NSAID. Such a preparation in which the compounds are either given...
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7199241 |
Process for preparing (S) and (R)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide
The present invention relates to a process for preparing (S)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide
and (R)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide
by...
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7141573 |
Polypharmacophoric agents
One aspect of the present invention relates to polypharmacophoric compounds. In certain embodiments, the polyphamacophore compounds comprise individual pharmacophore units selected from the group...
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7122539 |
Nitric esters and nitrate salts of specific drugs
Nitric acid salts with medicines active in the respiratory system pathology treatment.
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6977301 |
Process for preparing (S) and (R)—2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide
The present invention relates to a process for preparing (S)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide
and (R)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide
by...
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6908999 |
Process for the preparation of {2-[4-α-phenyl-p-chlorobenzyl)piperazin-1-yl]ethoxy} acetic acid and novel intermediates therefor
The invention refers to a novel process for the preparation of {2-[-(α-phenyl-p-chlorobenzyl)piperazin-1-yl]ethoxy}acetic acid, which comprises hydrolyzing an N,N-disubstituted...
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6897305 |
Calcium channel drugs and uses
Novel multibinding compounds are disclosed. The compounds of this invention comprise 2-10 ligands covalently connected, each of the ligands being capable of binding to a ligand binding site in a Ca...
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6821965 |
Amidobenzamide derivatives which are useful as cytokine inhibitors
The invention concerns amide derivatives of the Formula (I) wherein R 3 is (1-6C)alkyl or halogeno; Q is aryl or heteroaryl which optionally bears 1, 2, 3 or 4 substituents such as hydroxy,...
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6803465 |
Optically active 4-(tert-butoxycarbonyl)piperazine compound, and method for producing the same
A method for producing 1-[(substituted phenyl)phenylmethyl]piperazines useful as intermediates for pharmaceuticals and the like, more particularly, for example, to an intermediate for the...
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6787543 |
Benzhydryl derivatives
A compound of the formula (I): in which Z, R 1 , R 2 , R 8 , R 10 , R 11 , R 12 , R 13 and R 14 are each as defined in the description, or a salt thereof. The object compound of the present...
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6686353 |
Diarylalkyl cyclic diamine derivatives as chemokine receptor antagonists
Cyclic diamines of formula (I) or their pharmacologically acceptable acid addition salts, and their medical applications are described. These compounds inhibit the action of chemokines such as...
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6680321 |
Compounds with analgesic effect
Compounds of the formula (I) as well as their pharmaceutically acceptable salts, and pharmaceutical compositions comprising the novel compounds. The novel compounds of the formula (I) are useful...
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6436942 |
Enantiomers of 1&lsqb (4-chloro-phenyl) phenylmethyl&rsqb -4-&lsqb (4-methylphenyl) sulfony&rsqb piperazine
Levorotatory and dextrorotatory enantiomers of 1-[(4-chlorophenyl)phenylmethyl]-4-[(4-methylphenyl)sulfonyl
]piperazine of the formula their preparation and use for the preparation of...
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6335331 |
Pseudopolymorphic forms of 2-&lsqb 2-&lsqb 4-&lsqb Bis (4-fluorophenyl) methyl&rsqb -1-piperazinyl&rsqb ethoxy&rsqb acetic acid dihydrochloride
The present invention relates to new pseudopolymorphic forms of 2-[2-[4-[bis (4-fluorophenyl)methyl]-1-piperazinyl]ethoxy]acetic acid dihydrochloride, namely, anhydrous...
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6265579 |
Process for preparing piperazine-substituted aliphatic carboxylates
A process is disclosed for the preparation of a piperazine-substituted aliphatic carboxylate having the formula ##STR1## where m and n are individually an integer of from 1 to 6, R and R' are...
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6262057 |
Pseudopolymorphic forms of 2-[2-[4-[Bis(4-fluorophenyl)methyl]-1-piperazinyl]ethoxy]acetic acid dihydrochloride
The present invention relates to new pseudopolymorphic forms of 2-[2-[4-[bis(4-fluorophenyl)methyl]-1-piperazinyl]ethoxy]ace
tic acid dihydrochloride, namely, anhydrous...
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6255487 |
Process of preparing [2-(1-piperazinyl)ethoxy]methyl compounds
The present invention relates to novel substituted [2-(1-piperazinyl)-ethoxy]methyl compounds of formula ##STR1## in which R 1 represents a --CONH 2 , --CN, --COOH, --COOM or --COOR 3 group, M...
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6239277 |
Process for preparing piperazine-substituted aliphatic carboxylates
A process is disclosed for the preparation of a piperazine-substituted aliphatic carboxylate having the formula ##STR1## where m and n are individually an integer of from 1 to 6, R and R' are the...
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6177427 |
Treatment of glaucoma and ocular hypertension
Compositions of non-steroidal glucocorticoid antagonists for treating glaucoma or ocular hypertension and methods for their use are disclosed.
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6100400 |
Process for the preparation of esters of [2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]-ethoxy]acetic acid
The invention provides a process for the preparation of esters [2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]ac
etic acid, of the formula (I) ##STR1## wherein X represents a halogen...
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6046332 |
Methods for the manufacture of cetirizine
The present invention relates to a process for the preparation of a [2-[4-[4-(chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]ac
etic acid derivative of formula I: and, in particular, for the...
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5910499 |
Antiallergic agent having an anti-oxidant action
An antiallergic agent having leucotriene production inhibiting action and antihistaminic action, which can be orally administered is provided; the antiallergic agent comprises a hydroquinone...
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5854249 |
Opioid diarylmethylpiperazines and piperidines
A method for the treatment or prophylaxis of one or more conditions or disorders selected from the group consisting of physiological pain, diarrhea, urinary incontinence, mental illness, drug and...
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5747494 |
Pharmaceutical compositions for the treatment of depressive disorders
A method for treating a depressive disorder which comprises administering to a patient in need thereof a therapeutically effective amount of a combination of (i) hydroxyzine, an individual...
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5717094 |
Process and intermediates for preparing compounds having a disubstituted acetylene moiety and retinoic acid-like biological activity
A process is disclosed for the preparation of disubstituted acetylene derivatives having retinoic acid like biological activity, wherein 6-ethynyl-chroman, 6-ethynyl-thio chroman and...
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5716950 |
Diazacycloalkanealkylsulfonamide derivatives
A diazacycloalkanealkylsulfonamide derivative having the following formula I!: ##STR1## and pharmacologically acceptable salts thereof. The compounds have antiallergic activity with low...
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5703082 |
Enantiomers of 1- (4-chlorophenyl)phenylmethyl!- (4-methylphenyl)sulfonyl!p i
Levorotatory and dextrorotatory enantiomers of 1- (4-chlorophenyl)phenylmethyl!-4- (4-methylphenyl)sulfonyl!piperazine of the formula ##STR1## their preparation and use for the preparation of...
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5703071 |
Tropolone derivatives and pharmaceutical composition thereof for preventing and treating ischemic diseases
The present invention provides novel tropolone derivatives of the formula I ##STR1## wherein R 10 is a substituted or unsubstituted piperazinyl or benzothiazolidinyl group, and pharamaceutical...
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5681830 |
Opioid compounds
Diarylmethyl piperazine compounds having utility as exogenous receptor combinant species for binding with receptors such as delta, mu, sigma, and/or kappa receptors are disclosed. Compounds of the...
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5658908 |
Opioid diarylmethylpiperazines and piperdines
Diarylmethylpiperazine compounds having utility as receptor-binding species, e.g., for mediating analgesia, and for combatting drug addiction, alcohol addiction, and drug overdose. The compounds...
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5574159 |
Opioid compounds and methods for making therefor
Diarylmethyl piperazine compounds having utility as exogenous receptor combinant species for binding with receptors such as delta, mu, sigma, and/or kappa receptors are disclosed. Compounds of the...
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5565611 |
Process for preparing acid addition salt of Z-isomer of triphenylethylene compound
The present invention provides a process for preparing an acid addition salt of the Z-isomer of a compound of the formula ##STR1## wherein R 1 and R 2 represent a lower alkyl group, or taken...
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5525633 |
Triaryl-ethylene derivatives
The present invention relates to novel triaryl-ethylene derivatives that are useful as anti-neoplastic agents, antiatherosclerotic agents, and hypocholesterolemic agents.
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5413997 |
Triphenylmethane derivatives
A triphenylmethane derivative represented by the following general formula: ##STR1## exhibits bone absorption inhibiting effects and is useful as a medicament for treating osteoporosis.
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5391552 |
Diphenylpiperazine derivative and drug for circulatory organ containing the same
A diphenylpiperazine derivative represented by general formula (1), salt thereof, and drug for the circulatory organs containing the same as the active ingredient: ##STR1## wherein R 1 and R 2 ...
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5382687 |
Enamine derivatives
An enamine derivative containing a fluoroalkyl group, a fluoroaryl group or a fluoroaralkyl group is effective as a charge transport material in an electrophotographic member excellent in...
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5342839 |
2-hydroxy-3-phenoxy-propyl-substituted piperazines, their preparation and use
2-Hydroxy-3-phenoxy-propyl-substituted piperazines of the formula I ##STR1## in which R 1 -R 5 , Y, m and n have the meaning indicated in the description, and the preparation thereof are...
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5326762 |
Inhibitors of acyl-coenzyme A: cholesterol acyl transferase
Amides of the formula ##STR1## wherein R 1 and R 2 are independently heteroaryl, X-substituted heteroaryl, X-substituted phenyl, N-substituted triazinyl or N-substituted imidazolyl; and in...
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5324728 |
Naphthoic acid derivative
A naphthoic acid derivative represented by the following general formula or a salt thereof: ##STR1## wherein R 1 , R 2 and R 3 are each independently a hydrogen atom, a halogen atom, a hydroxyl...
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5308840 |
Substituted or unsubstituted benzhydryl heteroalkyl-substituted aminophenol compounds and pharmaceutical compositions thereof
Aminophenol derivatives of the following formula (I) ##STR1## wherein X is hydrogen atom, lower alkyl or a protecting group for phenolic hydroxy, Y is hydrogen atom or lower alkyl, Z is hydrogen...
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5215987 |
Substituted benzhydryl 2-hydroxypropyl piperazine derivatives
Substituted benzhydryl 2-hydroxypropyl piperazine derivatives and methods of synthesis of the derivatives are described. The substituted benzhydryl 2-hydroxypropyl piperazine derivatives are useful...
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5190946 |
Methods and compounds
Compounds of formula ##STR1## wherein R and R 3 , which may be the same or different, each is hydrogen, an alkyl group containing 1 to 5 carbon atoms, or an optionally substituted aryl or aralkyl...
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5166205 |
Derivatives of 1-diphenylmethyl piperazine and their use as antihistamines
The present invention relates to novel derivatives of 1-diphenylmethyl piperazinyl, characterized in that they correspond to the general formula I, and their therapeutically acceptable salts,...
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5142052 |
Cationic effect-driven carbinol/amine reaction
Aryl- and heterocyclic-methanamines are prepared by reacting a hydroxy-aryl carbinol or a heterocyclic carbinol with a primary or a secondary amine in the presence of a cationic effect reagent.
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5141937 |
7-diphenylmethylenebicycloheptane or 7-diphenylmethylenebicylcoheptene derivatives
Pharmaceutical products containing a 7-diphenylmethylenebicycloheptane or 7-diphenylmethylenebicycloheptene derivative of the formula I ##STR1## in which A, B, R 1 , R 2 , R 3 and R 4 have the...
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