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7638548 |
Spiroindolinone derivatives
There are provided compounds of the general formulas
wherein X, Y, R 1 , R 2 , R 3 and R 4 are as described herein. The compounds exhibit anticancer activity.
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7638547 |
Cis-alkoxy-substituted spirocyclic 1H-pyrrolidine-2,4-dione derivatives serving as pesticides
The invention relates to novel cis-alkoxy-substituted spirocyclic 1H-pyrrolidine-2,4-dione derivatives of the formula (I)
in which A, G, X and Y are as defined in the disclosure, to a...
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7632953 |
Process for the preparation of gabalactam
The present invention provides an improved process for the preparation of gabalactam of formula 1
that includes preparing an aqueous solution of an alkali or alkaline earth metal hydroxide,...
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7550499 |
Urea antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions
The present invention provides novel ureas containing N-aryl or N-heteroaryl substituted heterocycles and analogues thereof, which are selective inhibitors of the human P2Y 1 receptor. The...
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7538135 |
Benzenesulfonylamino compounds and pharmaceutical compositions containing these compounds
Compounds of the formula
provide pharmacological agents which bind to Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the instant invention are useful for the...
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7528156 |
Compounds
The invention provides compounds of general formula (D wherein m, n, Q, Z1, Z2, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined in the specification, processes for their preparation,...
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7524856 |
Tricyclic spiroderivatives as modulators of chemokine receptor activity
The invention provides compounds of formula (I) wherein m, R 1 , n, R 2 , q, p, X, Y, R 3 , R 4 , t and, R 5 are as defined in the specification, processes for their preparation, pharmaceutical...
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7514466 |
Purification of progesterone receptor modulators
Methods for purifying a compound of formula I are provided, wherein A, B X, Q, and R 1 are defined herein.
The methods include mixing the compound of formula I and a solvent; adding a base to...
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7498338 |
Compounds
The invention provides compounds of formula (I) wherein m, R 1 , n, R 2 , q, X, Y, Z, t, R 3 , R 4 , R 5 , R 6 , R 7 and R 8 are as defined in the specification, processes for their preparation,...
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7476688 |
Cyclic amidine derivatives
A cyclic amidine derivative represented by the formula:
[wherein R 1 , R 2 and R 3 represent hydrogen, C 1-6 alkyl, aryl-C 1-6 alkyl, etc.; R 4 , R 5 and R 7 represent hydrogen, C 1-6 ...
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7449475 |
Tricyclic spiropiperidines or spiropyrrolidines
The invention provides compounds of formula (I)
wherein m R 1 , n, R 2 , q, X, Y, Z, R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , t, and R 9 are as defined in the specification, processes for their...
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7439263 |
Pyrrolidine and thiazolidine compounds
Compounds of formula (I):
wherein:
X 1 represents an atom or group selected from CR 4a R 4b , O, S(O) q1 and NR 5 , wherein R 4a , R 4b , q 1 and R 5 are as defined in the...
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7410978 |
Once daily dosage forms of trospium
A pharmaceutical composition of a pharmaceutically acceptable trospium salt, with upon administration to a human patient generates an average steady state blood levels of trospium with a minimum (C...
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7396846 |
Growth hormone secretagogues
This invention relates to novel compounds which are useful in the modulation of endogenous growth hormone levels in a mammal. The invention further relates to novel intermediates for use in the...
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7393858 |
Tetrahydropyran compounds as tachykinin antagonists
The present invention relates to compounds of formula (Ia)
wherein A, B, n, m, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 and R 11 are defined herein, and pharmaceutically...
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7390798 |
Carboxamide spirolactam CGRP receptor antagonists
The present invention is directed to compounds of Formula I: I (where variables A 1 , A 2 , B, J, K, m, n, R 4 , R 5a , R 5b and R 5c are as defined herein) useful as antagonists of CGRP...
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7304081 |
Amido compounds and their use as pharmaceuticals
The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The...
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7288560 |
Spirocyclic cyclohexane derivatives
The present invention relates to spirocyclic cyclohexane compounds, to methods for their production, to pharmaceutical compositions containing these compounds, to methods of treatment using such...
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7250438 |
Anti-bacterial and anti-cancer spiro beta-lactone/gamma-lactams
Disclosed herein are novel spiro beta-lactone/gamma lactams for use in treating bacterial infections and cancer. The compounds are characterized by a terminal electron-withdrawing group such as a...
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7238703 |
Azabicyclic, azatricyclic and azaspirocyclic derivatives of aminocyclohexane NMDA, 5HT3, and neuronal nicotinic receptor antagonists
Azabicyclic, azatricyclic and azaspirocyclic derivatives of aminocyclohexanes which are systemically-active as NMDA, 5HT 3 , and nicotinic receptor antagonists, pharmaceutical compositions...
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7214701 |
Active substance combinations having insecticidal and acaricdal properties
The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising
(a) compounds of the formula (I)
in which W, X, Y, Z, A, B, D and G...
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7205328 |
Oxindoles with anti-HIV activity
The present invention relates to inhibition of viruses, e.g., HIV using oxindoles and compounds related to oxindoles. The invention further relates to methods for identifying and using agents,...
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7115575 |
Glucopyranosyloxypyrazole derivatives, medicinal compositions containing the same and intermediates in the production thereof
The present invention relates to glucopyranosyloxypyrazole derivatives represented by the general formula:
wherein R 1 represents a hydrogen atom or a lower alkyl group; one of Q 1 and T 1 ...
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7087635 |
3-substituted oxindole β3 agonists
The present invention relates to a β3 adrenergic receptor agonist of formula I:
or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and,...
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7084138 |
Active ingredient combinations with insecticidal and acaricidal properties
The invention relates to novel active compound combinations having very good insecticidal and acaricidal properties and containing
(a) cyclic ketoenols having the formula
in which the groups...
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7022693 |
Treatment of lipodystrophy
An inhibitor of the renin-angiotensin system is useful for the treatment or prevention of the lipodystrophy syndrome, e.g. in AIDS patients also receiving anti-retroviral therapy.
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6994866 |
Combinations of active ingredients, which exhibit insecticidal and acaricidal properties
The invention relates to novel active compound combinations having very good insecticidal and acaricidal properties and containing
(a) cyclic ketoenols having the formula
in which the...
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6984659 |
2-pyrrolidinone derivatives substituted at position 4 for reducing the extracellular glutamate level
2-pyrrolidinone derivatives which have in position 4 at least one substituent are described herein. Methods of treating polygltamine disorders such as Huntington's disease, dentorubropallidoluysian...
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6962938 |
Spiro-cyclic β-amino acid derivatives as inhibitors of matrix metalloproteases and TNF-α converting enzyme (TACE)
The present application describes novel spiro-cyclic β-amino acid derivatives of formula I:
or pharmaceutically acceptable salt forms thereof, wherein ring B is a 3-13 membered carbocycle or...
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6939888 |
1-H-3-arylpirrolidine-2,4-dione derivatives
The invention concerns 1-H-3-arylpyrrolidine-2,4-dione derivatives of formula (I),
in which A, B, G, X, Y and Z are as defined in the description, methods of preparing them and intermediates...
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6924291 |
Process for making spiro isobenzofuranone compounds
This invention relates to a process for making spiro isobenzofuranone compounds by coupling of an aminopyrazine fragment with a spirolactone piece.
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6911463 |
3-substituted oxindole β-3 agonists
The present invention relates to a β3 adrenergic receptor agonist of formula (I); or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and,...
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6908926 |
Substituted imidazoles, their preparation and use
Disclosed is a novel class of substituted imidazole compounds, pharmaceutical compositions containing them and uses of these compounds in the treatment and/or prevention of diseases and disorders...
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6900234 |
Synergistic therapeutic compositions and methods
Compositions and methods for achieving a therapeutic effect such as lowering blood pressure and treating congestive heart failure in a mammal. More specifically, synergistic compositions comprising...
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6890938 |
Indole-type inhibitors of p38 kinase
Compound with an indole linked through an aliphatic ring system to an aromatic moiety are useful in treating conditions associated with enhanced P38α kinase activity.
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6887869 |
Mikanolide derivatives, their preparation and therapeutic uses
The invention concerns novel mikanolide derivatives, their preparation method and their therapeutic uses, in particular as anti-cancer and anti-viral agents. The compounds correspond to general...
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6861391 |
Trifluoromethyl-substituted spirocyclic ketoenols
Trifluoromethyl-substituted spirocyclic ketoenols of the formula (I) are provided
wherein
Het represents one of the groups
and G, V, W, X, Y, and Z are as defined in the specification....
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6835744 |
3,3-substituted indoline derivatives
This invention provides compounds of the formula I: wherein: R 1 and R 2 are independently H, OH, OAc, alkylaryl, alkylheteroaryl, 1-propynyl, 3-propynyl, and substituted alkyl, O(alkyl),...
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6825220 |
3-Substituted oxindole β 3 agonists
The present invention relates to a β;3 adrenergic receptor agonist of formula I: (1); or a pharmaceutical salt thereof; which is useful for treating Type II diabetes and/or obesity.
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6818664 |
Angiogenesis inhibitor
A compound represented by the following formula (I) or a salt thereof and a medicament such as an angiogenesis inhibitor and an antitumor agent which comprises said compound or a physiologically...
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6806283 |
Selective serotonin receptor antagonists and therapeutic applications thereof
Spiro[9,10-dihydroanthracene]-9,3′-pyrrolidine (SPAN) and derivatives thereof are provided as selective serotonin receptor antagonists. The compounds are selective, high affinity antagonists of...
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6627649 |
Pharmaceutical compositions containing in combination two antagonists selective of arginine-vassopressin V receptors, even of V1 a and V2 receptors
The invention relates to pharmaceutical compositions containing...
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6589976 |
Utilizing spirocyclic phenyl keto-enols as pesticides and herbicides
The invention relates to novel spirocyclic phenylketoenols of the formula in which Het represents one of the groups in which Q represents and X, Y, Z, m, n, R 6 , R 9 , R 10 and R 11 are...
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6555567 |
Substituted spiroheterocyclic 1H-3-aryl-pyrrolidine-2,4-dione derivatives, processes for their preparation, and their use as pesticides
The invention concerns substituted spiro heterocyclic 1H-3-arylpyrrolidine-2,4-dione derivatives depicted by the formula: X is alkyl, halogen or alkoxy; Y is hydrogen, alkyl, halogen, alkoxy or...
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6544970 |
Cyclic regimens utilizing indoline derivatives
This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general...
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6503939 |
Combination regimens using 3,3-substituted indoline derivatives
This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds that are antagonists of the progesterone receptor having the structure: ...
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6495591 |
Fungal efflux pump inhibitors
The use of compounds of the milbemycin class as inhibitors of efflux pumps in microbes or other cells is described, along with pharmaceutical compositions incorporating a milbemycin. Also described...
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6489352 |
Conformationally constrained compounds as pharmaceutical agents
Novel substituted amino acids of formula are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders,...
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6489354 |
3-alkyl substituted pyrrolidine modulators of chemokine receptor activity
The present invention is directed to pyrrolidine compounds of the formula I: (wherein R 1 , R 2 , R 3 , R 4c , R 4d , and R 4f are defined herein) which are useful as modulators of chemokine...
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6468971 |
Maintaining kidney function during surgery or trauma
Kappa-opioid agonists prevent the impairment of renal function otherwise caused by the combination of gaseous anesthesia and surgery or severe trauma. Not only do these agents preserve renal...
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