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Patent No. 5523741

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Class 514/419 - C=X bonded directly or indirectly by an acyclic carbon or carbon chain to ring carbon of the five-membered hetero ring (e.g., tryptophan, etc.) (X is chalcogen)


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein a C=X group (X is Chalcogen)
No. of patents: 958
Last issue date: 03/20/2012


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NumberTitleIssue Date
8138221Pharmaceutically acceptable salts of thymodepressin and processes for their manufacture
The present invention relates to pharmaceutically acceptable crystalline and amorphous salts of D-isoglutamyl-D-tryptophan as well as processes for their manufacture, pharmaceutical compositions comprising them, and their uses in the preparation of pharmaceutical co...
03/20/2012
8124585Composition for relieving discomfort
The invention relates to a method of controlling feelings of pain in infants or diseased or elderly persons using a complete nutrition or a nutritional supplement. The method comprises administering increased levels of folic acid, vitamin B6 and vitamin B12 or their...
02/28/2012
8101649N-acylhydrazone derivatives useful as modulators of nicotinic acetylcholine receptors
This invention relates to N-acylhydrazone derivatives, which are found to be useful as modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders a...
01/24/2012
8063094Anti-cytokine heterocyclic compounds
Heterocyclic compounds which are inhibitors of Mitrogen-Activated Protein Kinase-Activated Protein Kinase-2 (MAPKAP-K2) as described, in addition to their use in the treatment of cytokine mediated diseases. ...
11/22/2011
8044091Phospho-indoles as HIV inhibitors
3-phosphoindole compounds for the treatment of retroviral infections, and particularly for HIV, are described. Also included are compositions comprising the 3-phosphoindole derivatives alone or in combination with one or more other anti-retroviral agents, processes ...
10/25/2011
8017645Melatonin daily dosage units
The present invention relates to a disposable container for a medicament or cosmetic agent for topical application, containing a single dose of melatonin or of a melatonin derivative which corresponds to a locally effective dose but which does not cause any systemic...
09/13/2011
8003682Indole compounds, a process for their preparation and pharmaceutical compositions containing them
Compounds of formula (I): wherein: R1 represents an alkyl, cycloalkyl or cycloalkylalkyl group, R2 represents a linear or branched (C1-C
08/23/2011
7989487Estrogen receptor modulators and uses thereof
A method for preventing, diagnosing, or treating a condition mediated by an estrogen receptor by administering to a patient in need thereof an effective amount of a compound of formula I, II, or a combination thereof: wherein R1, R3, R4, and R5 are independently sel...
08/02/2011
7985764Amide derivative or salt thereof
It was found that a compound according to the following formula: or a pharmaceutically acceptable salt thereof, has a strong antagonism for both the 5-HT2B and 5-HT7 receptors. In addition, the compoun...
07/26/2011
7973070Monatin hydrate crystals
New (2R,4R) monatin monosodium salt hydrate crystals characterized by having specific characteristic X-ray diffraction peaks provide general-purpose, stable, and safe monatin sodium salt crystals incorporating no organic solvent. These crystal may be prepared by a m...
07/05/2011
7964629Inhibitors of isoprenylcysteine carboxyl methyltransferase
The present invention relates, in general, to isoprenylcysteine carboxyl methyltransferase (Icmt) and, in particular, to inhibitors of Icmt and to methods of disease treatment using same. ...
06/21/2011
79604275-hydroxyindole-3-carboxylate derivatives and uses thereof
The present invention relates to 5-hydroxy-indole-3-carboxylate derivatives of formula I, or racemic mixture or optical isomers or pharmaceutically acceptable salts and/or hydrates thereof, wherein: substituents R1
06/14/2011
7960428Enantiomerically pure phosphoindoles as HIV inhibitors
3-phosphoindole compounds substantially in the form of a single enantiomer useful for the treatment of Flaviviridae virus infections, and particularly for HIV infections are provided. Also provided are pharmaceutical compositions comprising the 3-phosphoindole compo...
06/14/2011
7951835Crystals of non-natural-type stereoisomer salt of monatin and use thereof
The present invention provides salt crystals of non-natural stereoisomer forms of monatin and to the use thereof. ...
05/31/2011
7951834Angiotensin I-converting enzyme (ACE) inhibitors
This invention relates to a process for the synthesis of ketomethylene derivatives of the tripeptide Phe-Gly-Pro (“keto-ACE”, compound 5a) and analogues thereof. The synthesis process proceeds via an α,β-unsaturated keto intermediate. A key feature of t...
05/31/2011
7943658Indole indane amide compounds useful as CB2 agonists and method
Indole indane amides which are CB2 agonists are provided which have the structure wherein R1, R2, R3, R4 and R5 are as defined herein, which compounds are useful in tre...
05/17/2011
7939558Compounds having activity in increasing ion transport by mutant-CFTR and uses thereof
The invention provides compositions, pharmaceutical preparations and methods for increasing activity (e.g., ion transport) of the mutant cystic fibrosis transmembrane conductance regulator protein (mutant-CFTR), e.g., ΔF508 CFTR, G551D-CFTR, G1349D-CFTR, or D1152H-...
05/10/2011
7928137Meta-benzamidine derivatives as serine protease inhibitors
Compounds of formula I in which R1, R2, R3, each X, L, Y, Cy, Lp, D and n have the meanings as set out in the specification, and corresponding compounds in which the unsubstituted or substit...
04/19/2011
7919519S1P receptor modulating compounds and use thereof
The present invention relates to compounds of the general formula (I) that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulat...
04/05/2011
7902250Compositions based on aminoacids, suitable for the treatment of heart failure
Compositions based on amino acids are described, in particular for oral or parenteral use, suitable for treating heart insufficiency. The compositions according to the invention comprise up to 75% of the branched chain amino acids leucine, isoleucine and vali...
03/08/2011
7902251Method for treating pain
The present invention provides pharmaceutical compositions useful in a method for treating neuropathic pain, said method comprising administration of a pain-ameliorating effective amount of the compound according to formula I
03/08/2011
7888384Heterocyclic derivatives for modulation of calcium channels
Heterocyclic derivatives act as Ca channel antagonists. The compositions are useful for treating or relieving Ca channel mediated conditions. ...
02/15/2011
7888383Organic compounds
There are provided according to the invention compounds of formula (I) in free or salt form, wherein R1, R2, R4, R5, R6, D, X, W, m and n are as described in ...
02/15/2011
785522517βHSD type 5 inhibitor
To provide a novel and excellent method for treating and/or preventing prostatic cancer, benign prostatic hyperplasia, acne, seborrhea, hirsutism, baldness, alopecia, precocious puberty, adrenal hypertrophy, polycystic ovary syndrome, breast cancer, lung cancer, end...
12/21/2010
7838548Compounds and methods for treating toll-like receptor 2-related diseases and conditions
The present invention relates to compounds and methods useful in the prevention or treatment of diseases or conditions associated with Toll-like receptor 2 activation. ...
11/23/2010
7816394Methods of transdermally administering an indole serotonin receptor agonist and transdermal compositions for use in the same
Methods of transdermally delivering a therapeutic amount of an indole serotonin receptor agonist to an individual in need thereof, e.g., to provide a therapeutic level of an indole serotonin receptor agonist to an individual in need thereof, are provided. Also provi...
10/19/2010
7803835Substituted acetic acid derivatives
The present invention relates generally to substituted acetic acid derivatives and methods of using them. ...
09/28/2010
7795296Crystals of non-natural-type stereoisomer salt of monatin and use thereof
The present invention provides salt crystals of non-natural stereoisomer forms of monatin and to the use thereof. ...
09/14/2010
7795297Indole compounds, method of preparing them and uses thereof
Indole compounds corresponding to the formula (I): as defined in the claims, pharmaceutically acceptable addition salts of such compounds, pharmaceutical compositions containing such compounds, the process for their prepara...
09/14/2010
7781481N-arylsulfonyl-2,3-dihydro-1H-indoles and the use thereof as CCR9 inhibitors
N-(benzenesulphonyl)-2,3-dihydro-1H-indols, wherein the indol is substituted by cyano, carboxy or alkylcarbonyloxy and their use as therapeutical agents. ...
08/24/2010
7750039Indoles are cannabinoid receptor ligands
The present invention provides novel compounds of Formula (I) which are CB2 selective ligands useful for the treatment of pain. ...
07/06/2010
77454791,5-substituted indol-2-yl amide derivatives
The present invention relates to compounds of formula I wherein R1 to R4 and G are as defined in the description and claims and pharmaceutically acceptable salts thereof. The compounds are useful for t...
06/29/2010
77413633-Acylindole derivatives, preparation and therapeutic use thereof
The invention relates to compounds of formula (I), wherein X, R1, R2, R3, R4 and R5 are as described herein. The invention also includes preparative methods for the pre...
06/22/2010
7737173Indole-3-carboxylic acid amide, ester, thioamide and thiol ester compounds bearing aryl or heteroaryl groups having sphingosine-1-phosphate (S1P) receptor antagonist biological activity
The invention provides compounds represented by the formula I, each of which compounds may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity: and wherein the variables Y, R4, n, ...
06/15/2010
7709521Substituted indole derivatives for pharmaceutical compositions for treating respiratory diseases
The present invention relates to substituted indoles of formula (I) useful as pharmaceutical compounds for treating respiratory disorders. ...
05/04/2010
7696240Fused pyrrole derivatives
The invention is concerned with novel fused pyrrole derivatives of formula (I) wherein A, Ar, R1, R2, R2′ and R2″ and n are as defined in the description and in the claims, as...
04/13/2010
7683092Crystalline forms of antidiabetic compounds
Novel crystalline forms of two indole compounds connected to phenoxyalkylcarboxylic acid groups are selective PPAR gamma partial agonists that are useful in the treatment of type 2 diabetes, hyperglycemia, obesity, dyslipidemia, and the metabolic syndrome. The novel...
03/23/2010
7674818Aryl, aryloxy, alkyloxy substituted 1-indol-3-yl glyoxylic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
Compounds of formula I are provided: wherein: R1, R2, and R3, are as defined herein, as well as pharmaceutical composition and methods using the compounds as inhibitors of plasminogen activator inhibitor (PAI-1) and...
03/09/2010
7662848Process for the preparation of Fluvastatin Sodium salt
The present invention is directed to a process for preparing Fluvastatin Sodium salt by basic hydrolysis of its alkyl ester. The reaction is performed in conditions suitable to allow a selective hydrolysis of the desired syn isomer, while the unwanted anti isomer is...
02/16/2010
7659304Tryptophan derivative and application thereof
A compound represented by the following formula (I) or a salt thereof is provided: wherein X represents a halogen atom; R1 represents a hydrogen atom, substituted or unsubstituted C1-6 alkyl group, subst...
02/09/2010
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