|8481743||Phenylpropionamide compounds and the use thereof|
The invention relates to phenylpropionamide compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein A, B, R1, R2, R3, R4 and R5 are defined as set forth in the sp...
Compounds of formula (I) as well as pharmaceutically acceptable salts thereof can be used in the form of pharmaceutical compositions, wherein A1, A2, R1, R2, R3 and R
|8350042||Antiviral compounds for the treatment of HCV infection|
Disclosed are compounds and methods of synthesis of Formula I for the development of antiviral drugs for the treatment of HCV infection. ...
|8236960||Synthesis of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy) phenylmethyl)carbamide and its tartrate salt and crystalline forms|
Disclosed herein are methods for synthesizing N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl) -N′-(4-(2-methylpropyloxy)-phenylmethyl)carbamide. Also disclosed herein is the hemi-tartrate salt of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2 -methylpropyl...
|7923564||Synthesis of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy) phenylmethyl)carbamide and its tartrate salt and crystalline forms|
Disclosed herein are methods for synthesizing N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)-phenylmethyl)carbamide. Also disclosed herein is the hemi-tartrate salt of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropylox...
|7732615||N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and crystalline forms|
Disclosed herein are methods for synthesizing N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)-phenylmethyl)carbamide. Also disclosed herein is the hemi-tartrate salt of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2 -methylpropylo...
|7381735||Ultrashort-acting opioids for transdermal application|
The subject invention concerns analogs of fentanyl opioids. The subject invention also concerns methods for synthesizing the compounds of the invention. The invention also concerns methods for treating pain in a patient by administering a compound of the invention t...
|7368443||2,6-disubstituted piperidines and piperazine compounds|
The present invention is directed to 2,6-disubstituted piperidine and piperazine analogs having the following general formula: which are used to treat diseases of the central nervous system, drug abuse, and withdrawal there...
|7351825||Cyclopropane compounds and pharmaceutical use thereof|
The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1):
|7335753||Bifunctional heterocyclic compounds and methods of making and using same|
The invention provides a family of bifunctional heterocyclic compounds useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. The invention also provides methods of making the bifunctional heterocyclic compounds, and methods of using...
|7317103||Imaging agents for diagnosis of Parkinson's disease|
Generally, the present invention is directed to central nervous system dopamine transporter-imaging agents and methods of use thereof. In certain embodiments, the present invention relates to radiolabeled piperidine derivatives for use as imaging agents in the diagn...
|7301023||Chiral salt resolution|
A method for resolving enantiomers of a compound containing the structure of the forula: wherein R4 or R5 may contan one or more asymmetric centers, by mixing a racemic mixture of enantiomers of a...
|7262211||Aromatic heterocyclic non-covalent inhibitors of urokinase and blood vessel formation|
Novel compounds having activity as non-covalent inhibitors of urokinase and having activity in reducing or inhibiting blood vessel formation are provided. These compounds have at a group having a guanidino moiety or derivative thereof. These compounds are useful in ...
|7208604||Methods for the synthesis of alfentanil, sufentanil, and remifentanil|
Synthetic pathways are disclosed for synthesizing derivatives or analogs of fentanyl. Specifically set out are pathways for synthesizing alfentanil, sufentanil and remifentanil. The disclosed methods require fewer steps and produce a greater yield of product than me...
A compound of the formula wherein R1, R2 and R3 are as defined above, useful as inhibitors of protein kinases, such as the enzyme Janus Kinase 3. ...
|7183277||Carboxylic acid amides|
Novel compounds of the formula I in which D, W, X, Y, T and R1 are as defined in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophyla...
|7176210||Cannabinoid receptor ligands and uses thereof|
Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein ...
The present invention relates to compounds of the general formula wherein X and Y are each independently selected from —CH2— or —O—, with the proviso that X and Y are not simultane...
|7169928||Non-imidazole alkylamines as histamine H-receptor ligands and their therapeutic applications|
Use of a compound of formula (A), wherein: W is a residue which imparts antagonistic and/or agonistic activity at histamine H3-receptors when attached to an imidazole ring in 4(5) position; R1
|7135483||Substituted heterocyclic compounds for treating multidrug resistance|
Substituted heterocyclinc compounds are disclosed. The compounds are useful for treating multidrug resistance. The compounds can be formulated in compositions with a carrier and, optionally, a therapeutic agent. One suitable substituted heterocyclic compound has the...
|7122675||Gamma secretase inhibitors|
Novel aryl and heteroaryl sulfonamides are disclosed. The sulfonamides, which are gamma secretase inhibitors, are represented by the formula: wherein Ar1 and Ar2 independently represent aryl or he...
|7091196||Bifunctional heterocyclic compounds and methods of making and using same|
The invention provides a family of compounds useful as anti-infective agents and/or anti-proliferative agents, for example, chemotherapeutic agents, anti-fungal agents, anti-bacterial agents, anti-parasitic agents, anti-viral agents, and/or anti-inflammatory agents,...
|7084144||Sulfonyl group containing compounds and their use for the treatment of erectile dysfunction|
A compound having the general formula (I): wherein: X is N or C; R0 is H, a lower alkyl group, a lower O-alkyl group, lower alkyl group, a benzyl ...
|7084140||Arylglycinamide derivatives, method of producing said derivatives and pharmaceutical compositions containing these compounds|
The invention relates to new arylglycinamide derivatives of general formula I and the pharmaceutically acceptable salts thereof, wherein R1 and R2 together with the N to which they are bound...
|7071220||N-substituted benzothiophenesulfonamide derivatives|
The present invention relates to an N-substituted benzothiophenesulfonamide derivative or a pharmaceutically acceptable salt thereof and applications thereof. Furthermore, it provides an agent for preventing or treating cardiac or circulatory disease and so on cause...
|7064137||4-(Phenyl-(piperidin-4-yl)-amino)-benzamide derivaties and their use for the treatment of pain, anxiety or gastrointestinal disorders|
Compounds of general formula (I): R1 is selected from any one of phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl and pyridine N-oxide; where each R1 phenyl ring and R1 heteroaromatic ring may optionall...
|7022716||Cyclic amine phenyl beta-3 adrenergic receptor agonists|
This invention provides compounds of Formula I having the structure wherein, R1, R2, R3, R4, R5, T, T1, T2,...
|7005524||Methods for the stereoselective synthesis of substituted piperidines|
One aspect of the present invention relates to methods of synthesizing substituted piperidines. A second aspect of the present invention relates to stereoselective methods of synthesizing substituted piperidines. The methods of the present invention will find use in...
|6995268||N- and O-substituted 4-[2-(diphenylmethoxy)-ethyl]-1- (phenyl) methyl) piperidine analogs and methods of treating CNS disorders therewith|
N- and O-substituted 4[2-diaromaticmethoxy and methylamino)alkyl]piperidines exhibit high CNS activity with respect to the dopamine transporter (DAT) and serotonin transporter (SERT). Preferred compounds exhibit highly differential behavior as between the DAT and SE...
|6974825||Compounds with analgesic effect|
Compounds of general formula (I) wherein m is 0 or 1, and n is 1 or 2; are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comp...
|6943177||Cis-2,6-disubstituted piperidines for the treatment of psychostimulant abuse and withdrawal, eating disorders, and central nervous system diseases and pathologies|
Cis-2,6-disubstituted piperdine analogs, or lobeline analogs, having the general formula: are used to treat diseases of the central nervous system, drug abuse and withdrawal therefrom as well as to treating eating diso...
The invention relates to heterocyclic derivatives of formula (I) A—B—X1—T1(R2)—L1—T2(R3)—X2—Q (I) or pharmaceutically-acceptable salts thereof, which ...
The invention provides compounds of general formula (I) wherein m, n, Q, Z1, Z2, R1, R2, R3, R4, R5, R6, R7 and R8
|6911544||Process for the preparation of (S,S)-cis-2-phenyl-3-aminopiperidine|
The present invention is directed to a process for preparing (S,S)-cis-2-phenyl-3-aminopiperidine and (S,S)-cis-2-phenyl-3-tertbutoxycarbonylaminopiperidine. ...
|6903085||Substituted piperidine compounds useful as modulators of chemokine receptor activity|
The invention provides compounds of formula (I) wherein R1, R2, R3, R6, Z, Q, m, n, X1, X2, X3, X4 and T are as defined in the specification, processes for their preparation, pha...
|6900228||Opiate compounds, methods of making and methods of use|
The present application relates to novel opioid receptor antagonists and agonists, methods of making these compounds, and methods of use thereof. ...
|6900329||MCH antagonists and their use in the treatment of obesity|
The present invention discloses compounds which, are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonist...
Compounds of formula (I): and their salts, solvates, prodrugs, etc., wherein the substituents have the values mentioned herein, are Procollagen C-Proteinase (PCP) inhibitors and have utility in conditions mediated by P...
|6878712||Amides as inhibitors for pyruvate dehydrogenase|
A compound of formula (I): wherein: Ring A is a nitrogen linked mono or bicyclic heterocyclic ring as defined within; R1 and R2 are independentl...
The present application is directed to compounds having the structure of Formula I: where R1 is phenyl, pyridinyl, thiophenyl, furanyl, imidazolyl or trazolyl, each optionally substituted by a straight or br...