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Class 562/450 - Amide


Subclass of Class 562 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the acid contains the carbonyl residue
No. of applications: 278
Last issue date: 05/03/2012


1              
Application No.Application TitleIssue Date
20120108632PRENYLTRANSFERASE INHIBITORS FOR OCULAR HYPERTENSION CONTROL AND THE TREATMENT OF GLAUCOMA
The invention concerns in one embodiment a method of treating glaucoma or elevated intraocular pressure comprising administering a pharmaceutically effective amount of a composition comprising at least one prenyltransferase inhibitor. In another embodiment, the inventio...
05/03/2012
20120053243PARAKERATOSIS INHIBITOR AND SKIN PREPARATION FOR EXTERNAL USE
To provide a parakeratosis inhibitor, pore reducing agent and skin roughness preventing/ameliorating agent that exhibit capabilities of parakeratosis inhibition, pore reduction, skin roughness prevention/amelioration, etc., and further provide a skin preparation for ext...
03/01/2012
20120016151PROCESS FOR MANUFACTURE AND RESOLUTION OF 2-ACYLAMINO-3-DIPHENYLPROPANOIC ACID
The invention relates to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, in particular neutral endopeptidase (NEP) inhibitors....
01/19/2012
20110288239POLYMERIC POLYAMINES AND METHOD FOR PRODUCING THE SAME
The present invention discloses a polymeric polyamine which can be produced by polymerizing polyoxyalkylene-amine and a linker. The linker can be anhydride, carboxylic acid, epoxy, isocyanate or poly(styrene-co-maleic anhydride) copolymers (SMA). The present invention a...
11/24/2011
20110251418CASR AGONISTS
By searching various kinds of compounds having CaSR agonistic activity, the present invention provides CaSR agonistic agents, pharmaceutical compositions, preventive or therapeutic agents for diarrhea and kokumi-imparting agents each of which comprise the compound. More...
10/13/2011
20110229940METHOD FOR PRODUCING L-AMINO ACID
The present invention relates to a method for producing an L-amino acid by reacting an enantiomeric mixture of an N-succinyl amino acid with L-succinylase in the presence of N-acylamino acid racemase to specifically hydrolyze the L-form. In particular, the present inven...
09/22/2011
20110213157TRICYCLIC AMIDE COMPOUND
A compound represented by the following general formula (I):

[wherein R1 represents hydrogen atom or a C1-6 alkyl group, A and B represent —(CH2)2—, —(CH...

09/01/2011
20110130587PROCESS FOR PREPARING R-BETA-AMINO PHENYLBUTYRIC ACID DERIVATIVES
Disclosed is a process for preparing single enantiomers of beta-amino phenylbutyric acid derivatives and pharmaceutically acceptable salts thereof, which affords the desired compounds having special optical configuration. The process comprises a step of chemical synthes...
06/02/2011
20110118482BIDENTATE CHIRAL LIGANDS FOR USE IN CATALYTIC ASYMMETRIC ADDITION REACTIONS
Compounds of the formula (I), in the form of mixtures comprising predominantly one diastereomer or in the form of pure diastereomers, Z1-Q-P*R0R1 (I) in which Z1 is a C-bonded, secondary phosphine group —P(R)2; in...
05/19/2011
20110092733NATEGLINIDE CRYSTALS
Nateglinide M-type crystals (main peaks in powder X-ray diffraction: 6.0°, 14.2°, 15.2°, 18.8° (2θ)) can be produced by dissolving nateglinide in a solvent in which nateglinide is highly soluble and then adding a solvent in which nateglinide is difficultly soluble....
04/21/2011
20110064673New L-Glutamic acid and L-Glutamine derivative (III), use thereof and method for obtaining them
The present invention relates to fluorinated glutamic acid (glutamate) and glutamine derivatives wherein the fluorine atom is 19F. The glutamic acid (glutamate) and glutamine derivatives are compound(s) of general Formula I, which encompasses all possible diastereoisome...
03/17/2011
20110065681AMIDE COMPOUNDS, COMPOSITIONS AND USES THEREOF
Compounds are provided according to formula 1:

where A, B, W, X′, L, R1, R3, R4b, and m′ are as defined herein. Provided compounds and pharmaceutical compositions thereof ...

03/17/2011
20110046397NEW PROCESSES
The invention relates to a new process for producing NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a γ-amino-δ-biphenyl-α-methylalkanoic acid, or acid ester, backbone. In detail, the new processes, according to the present invention, are...
02/24/2011
20110039933S1P-1 RECEPTOR AGONISTS
The invention provides compounds formula (I), their preparation, and their use as pharmaceutically active immuno-suppressive agents for the treatment of autoimmune disorders, organ transplant rejection, disorders associated with an activated immune system, as well as ot...
02/17/2011
20100331552ACID SALT OF TOLTERODINE HAVING EFFECTIVE STABILITY FOR TRANSDERMAL DRUG DELIVERY SYSTEM
The present invention relates to an acid salt of tolterodine with superior stabililty and useful as a transdermal drug delivery system. More specifically, the present invention relates to a novel acid salt of tolterodine with superior stabililty to the conventional acid...
12/30/2010
20100324140GLUCAGON RECEPTOR ANTAGONISTS, PREPARATION AND THERAPEUTIC USES
The present invention discloses novel compounds of Formula I, or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention disclos...
12/23/2010
20100305131Substituted Aminopropionic Derivatives as Neprilysin inhibitors
The present invention provides a compound of formula I′;

or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, B1, X and n are defined...

12/02/2010
20100286427RETINOID PRODRUG COMPOUND
A compound represented by the following general formula (I):

[R1 to R5 represent hydrogen atom, an alkyl group, or a trialkylsilyl group, X represents —NH—CO—, —CO—NH—, —N(...

11/11/2010
20100273725Novel compounds useful in therapeutic and cosmetic methods
The present invention relates to photosensitizer compounds for use in cosmetic and therapeutic applications of photodynamic therapy. The compounds of the present invention are designed for topical application and are characterized by a low permeability to the stratum co...
10/28/2010
20100256414PROCESS FOR THE PREPARATION OF CHIRALLY PURE NATEGLINIDE
The invention relates to N-(trans-4-isopropylcyclohexylcarbonyl)-D-phenylalanine (nateglinide) in the novel crystalline form “G” and a process for the preparation thereof. A process for the preparation of chirally pure nateglinide by treating a lower alkyl ester the...
10/07/2010
20100234307PREPARATION AND USE OF BIPHENYL AMINO ACID DERIVATIVES FOR THE TREATMENT OF OBESITY
This invention relates to certain biphenyl amino acid compounds, compositions, and methods for treating or preventing obesity and related diseases....
09/16/2010
20100216886POLYMORPHS OF N2-(1,1'-BIPHENYL-4-YLCARBONYL)-N1-[2-(4-FLUOROPHENYL)-1,1-DIMETHYLETHYL]-L-ALPHA-GLUTAMINE
Disclosed are novel polymorphic forms of N2-(1,1′-biphenyl-4-ylcarbonyl)-N1-[2-(4-fluorophenyl)-1,1-dimethylethyl]-L-α-glutamine, methods of preparing the polymorphic forms, compositions containing the polymorphic forms, and methods of treatment...
08/26/2010
20100172844ALBUMIN BINDING MOLECULES AND USES THEREOF
The invention relates to portable albumin binders, which are useful for improving the pharmacokinetic properties of diagnostic or therapeutic agents, in particular increasing the blood circulations time and/or the tissue penetration capacity of such agents....
07/08/2010
20100168079Biaryl Benzylamine Derivatives
The present invention relates to biaryl-benzylamine compounds, to processes for their production, to their use as pharmaceuticals and to pharmaceutical compositions comprising them....
07/01/2010
20100152460PROCESS FOR THE PREPARATION OF OPIOID MODULATORS
The present invention is directed to novel processes for the preparation of opioid modulators (agonists and antagonists) and intermediates in their synthesis. The opioid modulators are useful for the treatment and prevention of as pain and gastrointestinal disorders....
06/17/2010
20100145090PROCESS FOR THE PREPARATION OF PROTECTED L ALANINE DERIVATIVES
The present invention is directed to a novel process for the preparation of protected L-alanine derivatives, useful as intermediates in the synthesis of compounds useful as mu/delta opioid modulators....
06/10/2010
20100129311PHENYLALANINE AMIDE INHIBITORS OF ATP-SENSITIVE POTASSIUM CHANNELS
The present invention relates to new phenylalanine amide inhibitors of ATP-sensitive potassium channels, pharmaceutical compositions thereof, and methods of use thereof.

...

05/27/2010
20100093536CONTROL OF GRASSY WEEDS WITH VINYLGLYCINES AND VINYLGLYCINE-PRODUCING ORGANISMS
The present disclosure concerns specific herbicide molecules, herbicidal compositions comprising the molecules and the bacterial strains that produce certain of these molecules, and methods of using these molecules and bacterial strains to control grassy weeds and other...
04/15/2010
20090324540COMPOUNDS AND COMPOSITIONS FOR DELIVERING ACTIVE AGENTS
Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well....
12/31/2009
20090305891CYCLOALKYLPHENYL SUBSTITUTED CYCLIC KETOENOLS
The disclosure relates to novel cycloalkylphenyl-substituted cyclic ketoenols of the formula (I)

in which

  • J, X, Y, m and CKE are as defin...
12/10/2009
20090291978Enzyme Inhibitors
Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers, wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxyest...
11/26/2009
20090281160Angiotensin 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 the p...
11/12/2009
20090253933NATEGLINIDE CRYSTALS
Nateglinide M-type crystals (main peaks in powder X-ray diffraction: 6.0°, 14.2°, 15.2°, 18.8° (2θ)) can be produced by dissolving nateglinide in a solvent in which nateglinide is highly soluble and then adding a solvent in which nateglinide is difficultly soluble....
10/08/2009
20090252676N-ALKOXYAMIDE CONJUGATES AS IMAGING AGENTS
The present disclosure is directed to compounds, diagnostic agents, and related methods. In some cases, methods for treating patients are provided. More specifically, the disclosure provides compounds, diagnostic agents, and kits for detecting and/or imaging and/or moni...
10/08/2009
20090143469SALTS OF NATEGLINIDE
The present invention relates to salts of organic acid, in particular salt of nateglinide, combined preparations comprising one or more salts of nateglinide and, optionally, one or more additional ingredients and the use thereof in pharmaceutical compositions for preven...
06/04/2009
20090131384COMPOUNDS AND METHODS FOR TREATMENT OF DISORDERS ASSOCIATED WITH ER STRESS
The invention provides novel compounds, methods for treating or preventing a condition related to ER-stress, e.g. hypercholesterolemia, atherosclerosis and related conditions, and pharmaceutical compositions related thereto....
05/21/2009
20090131441Metabolites Of 2-Arylpropionic Acid Derivatives And Pharmaceutical Compositions Containing Them
Metabolites of 2-(R)-4-isobutylarylpropionamides and pharmaceutical compositions containing such compounds are useful in inhibiting the chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membran...
05/21/2009
20090124669Structural Analogues of Avenanthramides, Their Use in Compositions Useful in the Treatment of Dermatological Disorders
Novel compounds for the prevention and treatment of dermatological disorders with an immunoallergic, hyperproliferative and inflammatory component, and a method of producing such compounds. The compounds are bioisosteres of substances with avenanthramide structures....
05/14/2009
20090111874Phenyl-containing n-acyl amine and aminoacid derivatives, methods for the production thereof, a pharmaceutical composition and the use thereof
The present invention relates to novel phenyl-N-acyl derivatives of biogenic amines and amino acids of general formula (I) as cyclooxynease inhibitors, possessing analgetic and anti-inflammatory properties and devoid of side effects in particular ulcerogeneity and pro-s...
04/30/2009
20090076301METHODS FOR PRODUCING NATEGLINIDE CRYSTALS
There is provided methods for producing nateglinide crystals, which comprises the steps of adding an acid(s) to a reaction mixture containing nateglinide to make it acidic, the reaction mixture being obtained by reacting trans-4-isopropylcyclohexylcarbonyl chloride with...
03/19/2009
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