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7517892 |
Ligands for monoamine receptors and transporters, and methods of use thereof
One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian...
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7511147 |
Process for manufacturing of chiral lobelin
The present invention relates to a shortened process for preparing L-lobeline by rhodium-catalysed asymmetric hydrogenation on an industrial scale.
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7385060 |
Method for producing salts of tolperisone
The invention relates to a method for producing an addition salt of 2,4′-dimethyl-3-piperidino-propiophenone (tolperisone) with a pharmaceutically acceptable acid, of formula (I). According to...
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7381734 |
Serine protease inhibitors
Compounds of formula (I)
where R 5 , R 6a , each X, L, Cy and Lp are as defined in the specification, are tryptase inhibitors useful as antiinflammatory agents.
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7365082 |
N-(substituted arylmethyl)-4-(disubstituted methyl)piperidines and piperazines
It has now been found that certain novel N-(substituted aryl)-4-(disubstituted methyl)piperidine and pyridine derivatives have provided unexpected insecticidal activity. These compounds are...
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7307091 |
Deuterated 3-piperidinopropiophenone and medicaments containing said compounds
The invention discloses deuterated 3-piperidinopropiophenones as well as their physiologically tolerated salts. Furthermore, the invention concerns the use of deuterated 3-piperidinopropiophenones...
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7294637 |
Method of treating addiction or dependence using a ligand for a monamine receptor or transporter
One aspect of the present invention relates to a method of treating of drug addiction or drug dependence in a mammal, comprising the step of administering to a mammal in need thereof a...
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7265226 |
1-alkyl-4-(3-substitutedphenyl)piperidines
8-Substituted-2,6-methano-3-benzazocines of general structure I in which A is —CH 2 —OH, —CH 2 NH 2 , —NHSO 2 CH 3 ,
and Y is O, S or
NOH are useful as analgesics, anti-diarrheal...
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7259157 |
N-substituted nonaryl-heterocyclo amidyl NMDA/NR2B Antagonists
Compounds represented by Formula (I):
or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.
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7247730 |
Process for the preparation of dexmethylphenidate hydrochloride
The present invention provides a new and efficient process for the preparation of the dexmethylphenidate hydrochloride with high optical purity, the process comprising:
(a) reacting a...
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RE39558 |
5-Substituted-6-cyclic-5,6,7,8-tetrahydronaphthalen 2-ol compounds which are useful for treating osteoporosis
Compounds of this formula
are useful for treating or preventing, obesity, breast cancer, osteoporosis, endometriosis, cardiovascular disease and prostatic disease.
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7115610 |
Substituted heterocyclic compounds
Disclosed are novel substituted heterocyclic derivatives having the structure of Formula I:
The compounds are useful for the treatment of various disease states, in particular cardiovascular...
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7109342 |
Piperidine derivatives and agent comprising the derivative as active ingredient
Piperidine derivatives represented by formula (I) or nontoxic salts thereof (wherein symbols are defined in the description):
Since the compound represented by formula (I) has a PDE4 inhibitory...
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7074934 |
Serine protease inhibitors
Compounds of formula (I) where R 2 , each X, L, Y, Cy, Lp, D and n are as defined in the specification, are serine protease inhibitors useful as antithrombotic agents.
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7067501 |
Aryloxyphenyl and arylsulfanylphenyl derivatives
The invention provides compounds of the formula
wherein the substituents are as defined in the application. The compounds are valuable glycine transport inhibitors.
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7041830 |
Process for preparing (RS) 3-methyl-1-(2-piperidinyl phenyl) butyl amine
The Present invention relates to a process for the preparation of (RS) 3-methyl-1-(2-piperidinyl phenyl) butyl amine of formula 1.
(RS) 3-Methyl-1-(2-piperidinyl phenyl butyl amine having...
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7030201 |
Bottom antireflective coatings
The present invention relates to bottom antireflective coating compositions and polymers useful in making such compositions.
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7002016 |
Process for the preparation of threo-methylphenidate hydrochloride
The present invention provides a process for the preparation of threo-methylphenidate hydrochloride. According to a preferred embodiment, the process comprises the following steps:
(a)...
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6992090 |
Substituted piperidine compounds and methods of their use
Novel 3,4-disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses...
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6962998 |
Processes for producing racemic piperidine derivative and for producing optically active piperidine derivative
Disclosed are a method for producing racemic piperidine derivatives by processing optically-active piperidine derivatives in a hydrogen atmosphere in the presence of a reducing catalyst; and a...
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6743790 |
Factor VIIa inhibitory (thio)urea derivatives, their preparation and their use
The present invention relates to compounds of the formula I, in which R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , A, X, m and n have the meanings indicated in the claims. The compounds of the formula I...
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6716986 |
Sulfuric acid mono-&lsqb 3-(&lcub 1-&lsqb 2-(4-fluoro-phenyl)-ethyl&rsqb -piperidin-4-YL&rcub -hydroxy-methyl)-2-methoxy-phenyl&rsqb ester
The present invention is directed to sulfuric acid mono-[3-({1-[2-(4-fluoro-phenyl)-ethyl]-piperidin-4-yl}-hydr
oxy-methyl)-2-methoxy-phenyl]ester, a metabolite of the 5HT 2A antagonist...
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6506778 |
Acylphenylurea derivatives, a process for their preparation and their use as pharmaceuticals
The invention is directed to acylphenylurea derivatives and their physiologically tolerated salts and physiologically functional derivatives. Compounds of the formula I in which the radicals have...
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6506764 |
Hydroxamic and carboxylic acid derivatives
Compounds of the formula B—X—(CH 2 ) m —CR 1 R 2 —(CH 2 ) n —CO—Y (I) have therapeutic utility as inhibitors of metalloproteinases etc.
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6498255 |
Heterocyclic-cyclic amine derivatives as cholinesterase inhibitors
Compounds of the formula wherein R 1 R 2 , R 7 , R 8 , X, Y, M and L are defined as below. The compounds of formula I are cholinesterase inhibitors and are useful in enhancing memory in...
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6472397 |
Nitrogen-containing heterocyclic compounds having antiplatelet aggregation effect and medicinal use thereof
The compounds represented by the formula (I), and pharmacologically acceptable salts and solvates thereof are disclosed. The compound is hydrolyzed in organisms into a compound represented by the...
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6451791 |
Amidoaromatic ring sulfonamide hydroxamic acid compounds
An amidoaromatic ring sulfonamide hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed, as are a treatment process that comprises administering a...
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6441178 |
Resolution of ritalinic acid salt
A process for preparing an enantiomerically-enriched form of threo-ritalinic acid, which comprises resolving a mixture of enantiomers of a salt of the acid, said salt being formed with an achiral...
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6441177 |
Tertiary amines
Tertiary amines of the formula wherein A 1 , A 2 , A 3 , A 4 , M, p, T and Q are as defined herein, and acid addition salts thereof, have antimycotic and cholesterol-lowering activity.
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6388022 |
Linker binding carriers for organic synthesis, their production and use
The present invention provides a linker binding carrier for organic synthesis represented by the formula: —Z—W—(SO 2 X)m wherein  is a carrier, X is a leaving group, Y is a bond or...
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6342509 |
Piperidine quaternary salts- CCR- 3 receptor antagonists
This invention relates to certain piperidine quatemrwy salts of Formula (I): that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods...
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6329399 |
Antifungal amine derivatives and processing for producing the same
Novel amine derivatives having an excellent antimycotic effect represented by general formula (1) below and salts thereof are provided. ##STR1## [in the formula (1, R 1 represents a C 1 -5 alkyl...
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6303637 |
Heterocyclic potassium channel inhibitors
The present invention relates to a class of heterocyclic compounds of Formula I that are useful as potassium channel inhibitors to treat autoimmune disorders, cardiac arrhythmias, and the like....
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6214996 |
Naphthalene derivates, process for the preparation thereof, and intermediates therefor
Naphthalene derivatives of the formula [I]: ##STR1## wherein R 1 and R 2 are the same or different and are each H, protected or unprotected OH, one of R 3 and R 4 is protected or unprotected...
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6191182 |
Phenyl alkyl ketone substituted by cyclic amine and a process for the preparation thereof
A novel process for the preparation of compounds of formula I ##STR1## by aminolysis of a p-halophenyl alkyl ketone of formula II ##STR2## with a cyclic amine of formula III ##STR3## in water at a...
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6147217 |
Synthesis of terfenadine and derivatives
Processes for preparing compounds having the general formula: ##STR1## wherein R 1a is protected carboxy, carboxy, hydroxymethyl, protected hydroxymethyl, or methyl are disclosed. Processes of the...
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6140321 |
Polymorphs of donepezil hydrochloride and process for production
Donepezil hydrochloride, 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride, is provided here in the form of four polymorphs which are stable against heat and humidity in the...
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6121293 |
Benzothiophene compounds, compositions, and methods
The invention provides benzothiophene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions...
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6107345 |
Benzocyclobutane compounds
A compound of formula (I): ##STR1## wherein: Z 1 , Z 2 , Z 3 , Z 4 , which may be identical or different, represent a group as defined in the description, X represents oxygen, S(O) p , --(CH 2 )...
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6090824 |
Therapeutic neurokinin receptor antagonist compounds
Compounds of formula I ##STR1## wherein Q 1 , Q 2 , Q 3 , and Q 4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide...
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6060488 |
Benzothiophenes for treating estrogen deficiency
This invention is related to novel benzothiophene compounds of formula I: ##STR1## where R, R 1 , R 2 , X and m are as defined in the specification, which are useful for the inhibition of the...
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6015899 |
Liquid antioxidants as stabilizers
Products are described which can be obtained by reacting components a), b) and c), where component a) is a compound of the formula I or a mixture of compounds of the formula I, component b) is a...
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6008220 |
Aromatic keto-acids and their derivatives as inhibitors of matrix metalloproteinases
Aromatic keto-acid compounds and derivatives are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix...
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5935585 |
Biaromatic amido compounds and pharmaceutical/cosmetic compositions comprised thereof
Novel pharmaceutically/cosmetically-active biaromatic amido compounds have the structural formula (I): ##STR1## in which Ar is a radical selected from among those of the following formulae (a)-(e):...
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5925653 |
Substituted pyridines and pyrimidines processes for their preparation and their use as pesticides and fungicides
Substituted pyridines and pyrimidines, processes for their preparation and their use as pesticides and fungicides. The invention relates to compounds of the formula ##STR1## in which A is N or CH,...
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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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5863903 |
Use of hydroxy alkyl piperidine and pyrrolidine compounds to treat diabetes
The present invention relates to hydroxy alkyl piperidine compounds and pharmaceutical compositions thereof which can be used to treat diabetes.
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5792870 |
2-amino-3-aroyl-benzo β!thiophenes and methods for preparing and using same to produce 6-hdyroxy-2-(4-hydroxyphenyl)-3- 4-(2-aminoethoxy)-benzoyl!benzo β! thiophenes
A group of 2-amino-3-aroyl-benzo β!thiophenes are prepared by treating an aldehyde with an anion of dimethylamino thioformamide, cyclizing the α-hydroxy thioamide, and subsequently acylating the...
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5733756 |
Lactams and processes for stereoselective enrichment of lactams, amides, and esters
Novel lactams and processes for the preparation of chiral compounds having utility as intermediates in the synthesis of compounds with Central Nervous System stimulant activity.
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5675009 |
Process for piperidine derivatives
The present invention is related to a novel process for preparing certain piperidine derivatives which are useful as antihistamines, antiallergy agents and bronchodilators.
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