Abstract: 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 agonists for the treatment of inflammatory and obstructive airways diseases.

Abstract: PAD4 inhibitory compositions and methods for their use in treatment of cancer and autoimmune disease are provided according to embodiments of the present invention.

Abstract: The present invention describes a solid state of aliskiren free base, and process for the preparation thereof.

Abstract: 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.

Abstract: 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 of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed.

Abstract: 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 the Bone Targeting Portion and the Bone Active Portion.

Abstract: The invention relates to solid states of pharmaceutically acceptable compounds of aliskiren, and processes for preparation thereof. The invention further provides pharmaceutical formulations comprising the amorphous or crystalline forms of pharmaceutically acceptable compounds of aliskiren and processes thereof; and a method of inhibiting renin for treating hypertension.

Abstract: The present invention relates to compounds of formula I, The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are inhibitors of the blood clotting enzymes, especially factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

Abstract: 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 chosen from hydrogen, (C1-C6)alkyl, and cycloalkyl, R is —NR3R4, where R3 and R4 are each independently chosen from hydrogen, and (C1-C4)alkyl; and n ranges from 1-4, comprising: (a) reacting a C1-C12 alkyl nitrate with a compound of formula 2, or a salt thereof, in the presence of an acid at a concentration greater than 70% weight of acid/weight of solution, the acid being selected from the group consisting of sulfuric acid, and R5—SO3H wherein R5 is C1-C4 alkyl optionally substituted with one or more halogen, or R5 is C6-C10 aryl optionally substituted with one or more C1-C4 alkyl or halogen, to produce a reaction mixture containing a compound of formula 3 or a salt thereof; (b) reducing the compound of formula 3 or a salt thereof to form a compound of formula 4 or a salt thereof (c) acylating the compound of for

Abstract: The present invention describes a series of therapeutically active compounds of formula I, X—Y—Z??(I) that are useful for treating a disorder in a mammal. In the formula I, X and Z, which may be same or different, are independently selected from substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted heterocyclic group or substituted or unsubstituted heterocyclylalkyl; and Y is a linker selected from —O—, —S—, —NH—, —(CH2)n—, —CO—, —CONRa—, —NRaCO—, —NRaCOO—, —COO—, —CONRaCO—, —CONRaCOO— and —COOCOO—.

Abstract: Provided are amorphous and polymorphic forms of aliskiren hemifumarate, pharmaceutical compositions thereof, and processes for their preparation.

Abstract: The present invention relates to novel aniline derivatives and their use in therapy, in particular their use in the treatment of fungal infections.

Abstract: 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 well as in the stimulation of anti-inflammatory cytokine production in vitro and in vivo. This abstract is neither intended to define the invention disclosed in this specification nor intended to limit the scope of the invention in any way.

Abstract: 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 ester group, an amidine group, or a salt thereof, at least one other of R1 to R6 is X—Rc, and the remaining of R1 to R6 independently represent H or substituted or unsubstituted organic groups; X represents a linking group; and Rc represents a substituted or unsubstituted alkyl group.

Abstract: 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 the Bone Targeting Portion and the Bone Active Portion.

Abstract: 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.

Abstract: The invention relates to a compound according to Formula (IX) and salts thereof, wherein R1, R2 and R5 are each independently selected from H and hydrocarbon moieties, which hydrocarbon moieties optionally comprise one or more heteroatoms, and which hydrocarbons optionally comprise substituents, or when the compound according to formula (IX) is a salt, R1 and/or R2 may be a cation, R3, and R4 each independently selected from hydrocarbon moieties, which hydrocarbon moieties optionally comprise one or more heteroatoms, and which hydrocarbons optionally comprise substituents, and wherein any two of R1, R2, R3, R4 and R5 are optionally linked together to form a ring structure. The invention further relates to the preparation of such a compound and to the use of such a compound for preparing a pharmaceutical compound, an agrochemical compound, an intermediate for a pharmaceutical compound or an intermediate for an agrochemical compound.

Abstract: 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 aromatic groups or aliphatic groups. In formula (5), R represents OH group or halogen.

Abstract: 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 limited to the myocyte enhancing factor (MEF2), the forkhead/winged helix transcription factor FOXP3 and the transcription factor GATA3. Also disclosed are small molecule modulators of MEF2 and its associated factors that include but not limited to histone deacetylases (HDACs), p300/CBP and Cabin1 and the therapeutic applications thereof.

Abstract: There is provided a novel pest control agent (pesticide), particulally insecticide or miticide. A substituted isoxazoline compound or a substituted enone oxime compound represented by Formula (1) or (2), and apest control agent containing them: wherein A1, A2, A3 and A4 are C or N, G1 is a benzene ring, etc., G2 is 1-trazolyl, etc., X and Y are halogen atom, etc., R3 is haloalkyl, etc., R3a is halogen atom, etc., R3b and R3c are H, etc., is haloalkyl, etc., m is 0-5, n is 0-4.

Abstract: The present disclosure is generally directed to compounds which can modulate G-protein coupled receptor 88, compositions comprising such compounds, and methods for modulating G-protein coupled receptor 88.

Abstract: The invention relates to a process for the preparation of compounds that are important building blocks in convergent synthesis routes to 2(S),4(S),5(S),7(S)-2,7-dialkyl-4-hydroxy-5-amino-8-aryl-octanoyl amides or pharmaceutically acceptable salts thereof, such as the compound Aliskiren, and to a process for the preparation of these octanoyl amides, comprising reacting said building block.

Abstract: The present invention relates to substituted amido phenoxybenzamide compounds of general formula (I): in which A, R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined in the claims, to pharmaceutical compositions and combinations containing said compounds, to methods of preparing said compounds, and to the use of said compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.

Abstract: A method of combating infectious agents, such as Pneumocystis pneumonia, and a method of treating a subject in need of such treatment is disclosed. The method comprises administering to the subject a bis-benzamidoxime of formula I wherein the linker is a di-substituted cyclic moiety of any ring size and may contain at least one heteroatom; the aromatic group is 1,2-; 1,3-; or 1,4-disubstituted; R is selected from the group consisting of a hydrogen, a linear or branched alkyl group, containing from 1 to 20 carbon atoms; R? is selected from the group consisting of a hydrogen, a linear or branched alkyl group containing from one to twenty carbon atoms, an aromatic ring, a cycloalkyl group containing three to eight carbon atoms, or a hydroxyl group; alternatively, R and R? may form a cyclic structure that can be fused to another cyclic system; or a pharmaceutically acceptable salt thereof. Pharmaceutical formulations and active compounds useful in the practice of the present invention are also disclosed.

Abstract: The invention relates to methods and compositions for promoting cognitive function and/or treating cognitive function disorders and impairments. In particular the methods are accomplished by administering to a subject CI-994 or dinaline or a pharmaceutically acceptable salt, ester, prodrug or metabolite thereof.

Abstract: The present invention relates to photo-labile pro-fragrance conjugates comprising: a) a photo-labile unit which upon exposure to electromagnetic radiation is capable of releasing a pro-fragrance unit; and b) a pro-fragrance unit, which when so released is either i) a pro-fragrance compound capable of releasing a fragrance raw material; or ii) a fragrance raw material. The present invention relates to systems for delivering fragrances to a situs, and to laundry detergent compositions, fine fragrances, personal care and hair care compositions comprising said systems.

Abstract: The invention relates to pharmaceutical compositions which contain the active agent Aliskiren and are suitable for the production of tablets by dry pressing, so that prior wet granulation can be obviated. The invention also relates to tablets which can be obtained by dry pressing of these pharmaceutical compositions and to a method for producing these tablets. The invention furthermore relates to the use of the novel pharmaceutical compositions and tablets for treating hypertension and illnesses associated therewith.

Abstract: Dyes, compositions comprising dyes and methods for using the same are provided.

Abstract: Provided are the expression method of influenza virus polymerase PAc-PB1N complex, the co-crystallization method of the complex and the three-dimendional structure of the crystal of PAc-PB1N complex. Also provided are the compounds binding to the influenza virus polymerase PAc and the expression method of influenza virus polymerase PAN. The three-dimensional structure of the crystal of PAc-PB1N complex can be used for screening and designing the drug for the treatment of influenza.

Abstract: Provided herein are compositions including diastereomers in substantially diastereomerically pure form and enantiomers in substantially enantiomerically pure form, and processes for preparing them and converting them to metyrosine.

Abstract: The invention describes a novel technical process and novel intermediates useful for the manufacture of enantiomerically pure 8-aryloctanoic acids of the formula I which are pharmaceutically active compounds as rennin inhibitors.

Abstract: Amidine analogs that can inhibit the activity of sphingosine kinase 1 and sphingosine kinase 2 (SphK1 & SphK2) are provided. The compounds can prevent angiogenesis in tumor cells.

Abstract: The present invention relates to a novel manufacturing process and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially rennin inhibitors such as Aliskiren. The invention describes a preparation of enantiomerically pure 8-aryloctanoic acids of general formula I from readily available key intermediate, a novel bicyclic compound of formula IV.

Abstract: The present invention relates to a compound of formula (I) wherein X is hydrogen, R1, R1C(O), R1CO2, or a COX2 inhibitor, wherein R1 is C1-20 alkyl, aryl, arylalkyl, alkyloxy or arylalkyloxy; wherein Y is OR2, NHR3N(R3)2, or a COX inhibitor; wherein R2 is hydrogen or C1-20 alkyl and each R3 is independently hydrogen or a C1-4 alkyl; wherein T is OR4, NHR5N(R5)2, or a COX inhibitor wherein R4 is hydrogen or C1-20 alkyl and each R5 is independently hydrogen or a C1-4 alkyl; wherein Z is hydrogen, R6, R6C(O), R6CO2, or a COX2 inhibitor; wherein R6 is C1-20 alkyl, aryl, arylalkyl, alkyloxy or arylalkyloxy; with the proviso wherein when X and Z are hydrogen and T is OH, Y is not OH; for use in the prevention and/or treatment of pain wherein said compound is provided for systemic administration.

Abstract: This invention relates to new radiohalogenated benzamide derivatives and their use in tumor diagnosis and tumor therapy. The radiohalogenated benzamide derivatives according to the invention exhibit novel and especially advantageous properties, in particular with respect to tumor concentration and retardation, liver concentration and blood accumulation. The radiation-therapy doses to be achieved in the tumor, compared to healthy body tissue, are advantageous for the compounds according to the invention.

Abstract: The present invention concerns prodrugs of mexiletine (and mexiletine's active metabolite) with amino acids or peptides and pharmaceutical compositions containing such prodrugs. Methods for providing pain relief, treating arrhythmia, decreasing the adverse GI side effects associated with mexiletine, increasing the bioavailability of mexiletine, and improving the pharmacokinetic reproducibility of mexiletine with the aforementioned prodrugs are also provided. Oligopeptides incorporating lysine or arginine residues attached directly or indirectly through a glycine residue are also described herein.

Abstract: This invention relates to new radiohalogenated benzamide derivatives and their use in tumor diagnosis and tumor therapy. The radiohalogenated benzamide derivatives according to the invention exhibit novel and especially advantageous properties, in particular with respect to tumor concentration and retardation, liver concentration and blood accumulation. The radiation-therapy doses to be achieved in the tumor, compared to healthy body tissue, are advantageous for the compounds according to the invention.

Abstract: The present invention relates to photo-labile pro-fragrance conjugates comprising: a) a photo-labile unit which upon exposure to electromagnetic radiation is capable of releasing a pro-fragrance unit; and b) a pro-fragrance unit, which when so released is either i) a pro-fragrance compound capable of releasing a fragrance raw material; or ii) a fragrance raw material. The present invention relates to systems for delivering fragrances to a situs, and to laundry detergent compositions, fine fragrances, personal care and hair care compositions comprising said systems.

Abstract: A first aspect of the invention is a compound (sometimes also referred to herein as an “active agent” or “active compound”) of Formula I or Ia: or a pharmaceutically acceptable salt or prodrug thereof. Compositions thereof and methods of using the same (e.g. for the treatment of a neurological disease) are also described.

Abstract: A photosensitive composition comprising: (A) a compound capable of generating a compound having a specific structure upon irradiation with actinic rays or radiation, a pattern forming method using the photosensitive composition, and a compound capable of generating a compound having a specific structure upon irradiation with actinic rays or radiation.

Abstract: The invention relates to a new salt of aliskiren, the respective production and usage, and pharmaceutical preparations containing such a salt.

Abstract: Peripheral Benzodiazepine Receptor (PBR) is an attractive target for tumor imaging and treatment due to its up-regulation in numerous cancer cell types. DAA1 106 is a selective PBR ligand with high binding affinity. Aspects of the present invention are series of functionalized DAA1 106 analogs, which can be conjugated to a variety of signaling and treatment moieties, and are widely applicable in PBR targeted molecular imaging and drug delivery.

Abstract: The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.

Abstract: The present invention provides methods for the prevention of, delay of progression to or the treatment of diseases modulated by an increase in tissue bradykinin levels by administering to a warm-blooded animal a therapeutically effective amount of a renin inhibitor, or a pharmaceutically acceptable salt thereof, alone or in combination with (i)) an ACE inhibitor or a pharmaceutically acceptable salt thereof, (II) an angiotensin II receptor blocker, or a pharmaceutically acceptable salt of either.

Abstract: The present invention relates to compounds of formula I, The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are inhibitors of the blood clotting enzymes, especially factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

Abstract: A diamine includes a structure of formula (I), wherein X and Y are independently a divalence group selected from the group consisting of: —O—, —(C?O)—O—, —O—(C?O)—, —(C?O)—NH—, and —NH—(C?O)—; and R has a structure of formula (II): wherein R1, R2, R3, R4, R5, m, and n are as defined in Claim 1. A polyamic acid is prepared by reacting a diamine reactant including the aforesaid diamine of formula (I) with a tetracarboxylic dianhydride reactant. A liquid crystal orienting film contains a polyimide converted from the aforesaid polyamic acid.

Abstract: Provided herein are novel, stilbene like compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, metabolites, prodrugs, solvates, pharmaceutically acceptable salts and compositions thereof. These compounds can inhibit HDACs and are useful as a therapeutic or ameliorating agent for diseases that are involved in cellular growth such as WO 2009/047615 A2 malignant tumors, autoimmune diseases, skin diseases, infections, inflammation, etc.

Abstract: The invention relates to solid states of pharmaceutically acceptable compounds of aliskiren, and processes for preparation thereof. The invention further provides pharmaceutical formulations comprising the amorphous or crystalline forms of pharmaceutically acceptable compounds of aliskiren and processes thereof; and a method of inhibiting renin for treating hypertension.

Abstract: The present invention relates to a synthetic process for the preparation of a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor.

Abstract: The present invention is directed to aspartic protease inhibitors. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.