"Without question, the greatest invention in the history of mankind is beer. Oh, I grant you that the wheel was also a fine invention, but the wheel does not go nearly as well with pizza."
|Application No.||Application Title||Issue Date|
|20130102677||NOVEL SOLID FORMS OF TACEDINALINE|
Novel solid forms of tacedinaline (4-(acetylamino)-N-(2-aminophenyl)benzamide), including crystalline tacedinaline Forms A, B, and D, a novel crystalline tacedinaline TFA salt, and amorphous tacedinaline, are disclosed. Pharmaceutical compositions comprising crystalline...
|20130071899||Process for Producing Aliskiren|
A new route of synthesis of the compound Aliskiren of formula (I), used in the treatment of hypertension, is described.
|20130053412||Cyclopentanecarboxamide derivatives, medicaments containing such compounds and their use|
The invention relates to cyclopentanecarboxamide derivatives of formula 1, to their use as Fatty Acid Synthase inhibitors, to methods for their therapeutic use and to pharmaceutical compositions containing them, wherein R1, R2, R3, LO, W...
|20130035328||ANTIVIRAL COMPOUNDS AND METHODS|
The invention relates to compounds having antiviral activity and methods utilizing the compounds to treat viral infections....
|20130030359||DIPEPTIDE-BASED PRODRUG LINKERS FOR AROMATIC AMINE-CONTAINING DRUGS|
The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof, comprising a drug linker conjugate D-L, wherein D being a biologically active moiety containing an aromatic amine group is conjugated to one or more polymeric carriers via dipeptid...
The present invention relates to compounds of Formula (I)
and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as opioid agon...
|20120321560||Method for Obtaining Novel Derivatives of Naphthalene for the In Vivo Diagnosis of Alzheimer's Disease|
This invention relates to a chemistry branch, particularly to the field of compounds' organic synthesis that belongs to the aromatic bicyclic or naphthalene category, used in the detection of amyloid sheets. These new naphthalene derivatives have a general formula: Wher...
|20120272990||COLORING AGENTS AND METHODS OF USE THEREOF|
Dyes, compositions comprising dyes and methods for using the same are provided....
|20120272462||DYES FOR POLYMER COLORATION, THEIR PREPARATION AND THEIR USE|
The present invention relates to a compound of formula (I), where X, Y, T and Z are each as defined in claim 1, to its preparation and to its use.
|20120258960||NOVEL MULTIFUNCTIONAL PEPTIDASE INHIBITORS, ESPECIALLY FOR MEDICAL USE|
The invention relates to compounds of the general formula (1) or the acid addition salts thereof with organic and/or inorganic acids; as well as to the use of the compounds of the general formula (1) in medicine.
|20120238676||USE OF OLIGOMERIC CARBODIIMIDES AS STABILIZERS|
Oligomeric carbodiimides comprising at least one heterocyclic end group are used as stabilizers for polymers. The oligomeric carbodiimides may be compounds of the general formula (I),
where A1, A
|20120238763||PROCESS FOR PRODUCING 3-ALKOXY-2-AMINO-6-FLUOROBICYCLO [3.1.0] HEXANE-2,6-DICARBOXYLIC ACID DERIVATIVE AND INTERMEDIATE THEREOF|
A process for producing a 3-alkoxy-2-amino-6-fluoro bicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivative represented by the formula (I) or a salt thereof, which includes converting a compound represented by the formula (VI) or a salt thereof to the compound represented...
|20120225891||AMIDE DERIVATIVES, PROCESS FOR PREPARATION THEREOF AND USE THEREOF AS INSECTICIDE|
A compound represented by Formula (1):
|20120220663||SOLID FORMS OF ALISKIREN HEMIFUMARATE AND PROCESSES FOR PREPARATION THEREOF|
The present invention provides polymorphic forms of aliskiren hemifumarate, and processes for preparation thereof and for the preparation of the amorphous form of aliskiren hemifumarate. The present invention also provides pharmaceutical compositions comprising the alis...
|20120196916||BETA- AND GAMMA-AMINO-ISOQUINOLINE AMIDE COMPOUNDS AND SUBSTITUTED BENZAMIDE COMPOUNDS|
Disclosed are beta and gamma-amino isoquinoline amide compounds and substituted benzamide compounds. In particular, the invention provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The c...
|20120196865||Acyl Guanidine Derivatives Modulating The Hedgehog Protein Signaling Pathway|
The present invention relates to acyl guanidine derivatives modulating the hedgehog protein signaling pathway to be used as drugs, in particular for treating diseases involving a tissue dysfunction associated with a deregulation of the hedgehog protein signaling pathway...
The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases.
|20120178666||PRODRUGS OF GUANFACINE|
Prodrugs of guanfacine with amino acids or short peptides, pharmaceutical compositions containing such prodrugs and a method for providing therapeutic benefit in the treatment of ADHD/ODD (attention deficient hyperactivity disorder and oppositional defiance disorder) wi...
|20120165555||RING OPENING OF LACTONES AND LACTAMS|
The present invention provides a novel process for opening a lactone and/or a lactam ring. More particularly, the present invention provides a process that employs a novel catalyst in the opening of a lactone ring and/or a lactam ring. Additionally, the present inventio...
|20120165276||QUATERNARY ALKYL AMMONIUM BACTERIAL EFFLUX PUMP INHIBITORS AND THERAPEUTIC USES THEREOF|
Disclosed are compounds having at least one quaternary alkyl ammonium functionality. The compounds inhibit bacterial efflux pump inhibitors and are used in combination with an anti-bacterial agent to treat or prevent bacterial infections. These combinations can be effec...
|20120142781||Antagonists of the Magnesium Binding Defect as Therapeutic Agents and Methods for Treatment of Abnormal Physiological States|
This invention provides a class of therapeutic compounds and methods for the treatment of mammals with physiological disorders, such as for example a frequently occurring type of essential hypertension, which are critically associated with the decreased binding of magne...
|20120142668||CATHEPSIN C INHIBITORS|
Disclosed are 4-amino-2-butenamides of Formula (I) having pharmacological activity, pharmaceutical compositions containing them, and methods for the treatment of diseases mediated by the cathepsin C enzyme such as chronic obstructive pulmonary disease.
|20120142646||Novel Compounds 621|
The present invention provides compounds of formula (I)
wherein k, Ar, R2, R3, R4, R5, R4′, R5′, R6, R7, A, D, m and...
|20120135984||DUAL-ACTION INHBITORS AND METHODS OF USING SAME|
Provided are compounds, compositions, and methods for treating diseases and conditions wherein an inhibitor of a kinase, such as rho kinase (ROCK), and an inhibitor of one or more of the monoamine transporters, such as NET or SERT, act in concert to improve the conditio...
|20120115841||BRIDGED SPIRO [2.4] HEPTANE DERIVATIVES AS ALX RECEPTOR AND/OR FPRL2 AGONISTS|
The present invention relates to bridged spiro[2.4]heptane derivatives of formula (I), wherein W, Y, Z, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds as ALX receptor and/or FPRL2 a...
|20120108562||THERAPEUTIC COMPOSITIONS AND METHODS|
PAD4 inhibitory compositions and methods for their use in treatment of cancer and autoimmune disease are provided according to embodiments of the present invention....
|20120094971||Compositions Including 6-Aminohexanoic Acid Derivatives As HDAC Inhibitors|
This invention relates to compounds of Formula (I) wherein Cy1, L1, Y, R1, L2, and Ar2 are defined herein, for the treatment of cancers, inflammatory disorders, and neurological conditions.
|20120095264||SOLID STATES OF ALISKIREN FREE BASE|
The present invention describes a solid state of aliskiren free base, and process for the preparation thereof....
|20120088770||ALPHA HELIX MIMETICS AND METHODS RELATING THERETO|
Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a chemical library relating thereto, and methods relating thereto, are disclosed. Applications ...
|20120083440||METHODS AND COMPOUNDS FOR THE TARGETED DELIVERY OF AGENTS TO BONE FOR INTERACTION THEREWITH|
Bone targeted compounds and methods are provided. Compounds can include a Bone Targeting Portion (RT), having an affinity for bone; a Bone Active Portion (RA) for interacting with and affecting bone; and a Linking Portion (RL) connecting...
|20120059190||NOVEL NITRATION OF TETRACYCLINES|
The invention in one embodiment is directed to a method of preparing a compound of formula 1,
or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are each independently chos...
|20120046272||Novel Therapeutic Compounds|
The present invention describes a series of therapeutically active compounds of formula I,
that are useful for treating a disorder in a mammal. In the f...
|20120028995||NOVEL COMPOUNDS FOR MEDICAL USE AS PEPTIDASE EFFECTORS|
The invention relates to compounds of general formula (I) as set forth in the claims as well as to the use of the compounds of the general formula (1) in the medical field, specifically for use in the suppression of DNA synthesis and inflammatory cytokine production as ...
|20120029083||POLYMORPHIC FORMS OF ALISKIREN HEMIFUMARATE AND PROCESS FOR PREPARATION THEREOF|
Provided are amorphous and polymorphic forms of aliskiren hemifumarate, pharmaceutical compositions thereof, and processes for their preparation....
|20120029188||Substituted Aniline Derivatives|
The present invention relates to novel aniline derivatives and their use in therapy, in particular their use in the treatment of fungal infections....
Nanostructures are formed from alkylated derivatives of aromatic acids of the formula:
wherein at least one of R1 to R6 represents a carboxylic acid group, a primary amide group, an este...
|20110294741||USE OF COMPOUNDS IN THE TREATMENT OF TAU-INDUCED CYTOTOXICITIES|
The present invention relates to derivatives of L-Tyrosyl-L-Arginine and the use of said derivatives in the prevention and/or treatment of a tau-induced cytotoxicity....
|20110294171||PREPARATION OF A SATURATED ALDEHYDE|
The invention relates to a compound according to Formula (IX)
and salts thereof,
|20110275783||Nitro compound, amine compound and polyamide derived therefrom|
A polyamide represented by formula (6) is provided. The polyamide is fabricated by performing a polycondensation reaction with amine compound shown in formula (4) and an acid or derivative thereof shown in formula (5) as monomers. In formulas (5) and (6), X represents a...
|20110275674||Small Molecules Modulator of Epigenetic Regulation and Their Therapeutic Applications|
Disclosed are methods and compositions for modulating the function of transcription factors, especially transcription factors that recruit epigenetic regulators (histone modifying enzymes) to specific DNA promoters. The targeted transcription factors include but are not...