Abstract: The present invention relates to a pyridine derivative of formula (1) wherein R1 is optionally-substituted C1-6 alkyl, optionally-substituted C3-10 cycloalkyl, or optionally-substituted 5- to 10-membered saturated or partially-unsaturated heterocyclyl; R2 is halogen atom, cyano, C1-6 alkyl which may be optionally substituted with 1 to 3 the same or different halogen atoms, C1-6 alkoxy which may be optionally substituted with 1 to 3 the same or different halogen atoms, or amino which may be optionally substituted with 1 to 2 the same or different C1-6 alkyl; and the bind with broken line is single or double bond, or a pharmaceutically acceptable salt thereof, which is useful as a medicament for treating symptoms in anxiety-related disorder.

Abstract: Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.

Abstract: A method is described for production of a high purity compound of the formula (I) in crystalline form of the modification A. In this, starting from high purity gadobutrol, the gadolinium is removed by decomplexation with oxalic acid, and then with a calcium salt the calcium complex is produced in high purity. During the crystallization, a water equivalent of 9-11 weight % is set. The crystalline form of the modification A of the compound of the formula (I) is used in the production of Gadovist.

Abstract: Compounds of formula (I) are provided which are useful in the treatment of diseases or conditions modulated at least in part by CCR6:

Abstract: The invention provides (1) processes for making substantially-pure (?) huperzine A and substantially-pure (?) huperzine A derivatives; (2) compositions useful in making substantially-pure (?) huperzine A and substantially-pure (?) huperzine A derivatives; and (3) methods of treating or preventing neurological disorders using substantially-pure (?) huperzine A and substantially-pure (?) huperzine A derivatives.

Abstract: The present invention relates to a process for phospholipidation of imidazoquinolines and oxoadenines. More particularly, the present invention relates to a high-yielding and scalable procedure for the phospholipidation of imidazoquinolines and oxoadenines which obviates the need to isolate unstable phosphoramidite intermediates. This process may be used for the phospholipidation of toll-like receptor 7 (TLR7)—active and toll-like receptor (TLR8)—active imidazoquinolines and oxoadenines.

Abstract: The invention provides compounds of Formula XXIII: wherein R1 is hydrogen, alkyl, acyl, or silyl, R2 is hydrogen, alkyl, benzyl, acyl, or ester, and R3 is hydrogen, alkyl, an aromatic group, azacyclic, carbocycle, aryl, cycloalkyl, heterocycloalkyl, heterocycle, heteroaryl, heteroalkyl, acyl, or ester, as well as derivatives and stereoisomers, pharmaceutically acceptable salts and derivatives thereof; and methods of making and using such compounds. The invention includes pharmaceutical compositions containing such compounds, and the use of such compounds in methods of treating conditions, diseases, or disorders.

Abstract: The present invention provides a compound of formula (I) in free form or in pharmaceutically acceptable salt form, a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract: The present invention relates to N-acylimino compound of formula (I): wherein X is O or S, in particular O; m is an integer selected from 0, 1, 2, 3, 4, 5 or 6; Het is a 5 or 6 membered carbon-bound or nitrogen-bound heterocyclic ring, W1-W2-W3-W4 represents a carbon chain group connected to N and C?N, and thus forming a saturated, unsaturated, or partially unsaturated 5 or 6 membered nitrogen containing heterocycle, wherein W1, W2, W3 and W4 each individually represent CRvRw, R1, R2 may be hydrogen, halogen, etc. R3 may be hydrogen, halogen, CN, C1-C6-alkyl, etc. R4a, R4b if present, may be hydrogen, halogen, C1-C6-alkyl, etc. R5 may be hydrogen, halogen, C1-C6-alkyl, C1-C6-alkenyl, C1-C6-alkinyl, C3-C8-cycloalkyl, S(O)nNR9aR9b, NR9aR9b, C(?O)OR8, C(?O)NR9aR9b, C(?S)NR9aR9b, C(?O)R7a, C(?S)R7a, NR9a—C(?O)R7a, NR9a—C(?S)R7a, NR9a—S(O)nR8a, a moitey Q-phenyl, where the phenyl ring is optionally substituted with one or more, e.g.

Abstract: The present invention provides compounds useful as inhibitors of Ca2+/calmodulin-dependent protein kinase (CaMKII), compositions thereof, and methods of using the same.

Abstract: The present invention relates to piperidine derivatives of formula (I) wherein Ar1, Ar2, RAr1, R1, R2 and R3 are as described in the description, their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as CXCR7 receptor modulators.

Abstract: The present invention relates to novel compounds of formula (I) that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases. These diseases include autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, alzheimer's disease, parkinson's disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases.

Abstract: The invention provides compounds of formula I: wherein R1-R3, Ra, and Rb have any of the values defined herein, and salts thereof. The compounds have immunomodulatory properties.

Abstract: A water-soluble peptide fluorescence material having a structure of formula (I): In formula (I), n is an integer greater than or equal to 1, R1 is independently selected from hydrogen or a nitrogen-containing functional group, R2 is independently selected from hydrogen or alkyl, and A1 is polymerized by at least one amino acid monomer and having a structure of formula (II): In formula (II), m is an integer greater than or equal to 1, and R3 in each of the amino acid monomers of A1 is independently selected from hydrogen, alkyl, aralkyl, alkylthioaalkyl, hydroxyaralky, heteroaralkyl, carboxylalkyl, or guanidinylalkyl. A2 is —OR5 or —N(R4)2, and R4 is independently selected from hydrogen, alkyl, aralkyl, alkylthioaalkyl, hydroxyaralky, heteroaralkyl, carboxylalkyl, guanidinylalkyl, monoglycosyl, biglycosyl, or oligosaccharyl, and R5 is hydrogen, alkyl, aralkyl, alkylthioaalkyl, hydroxyaralky, heteroaralkyl, carboxylalkyl, or guanidinylalkyl.

Abstract: The invention relates to a process for the preparation of lifitegrast (I) comprising a) reacting benzofuran-6-carboxylic acid (II) with a non-chlorinated carboxyl activating agent; and b) reacting the activated compound obtained in step a) with compound (III) or a salt thereof to give lifitegrast. It also relates to a process for the purification of lifitegrast (I) by i) reacting lifitegrast with dicyclohexylamine to give the dicyclohexylamine salt of lifitegrast (Ia); ii) isolating the salt from the reaction medium; iii) converting the isolated salt into lifitegrast by treatment with an acid; and iv) isolating lifitegrast from the reaction medium. It also relates to the dicyclohexylamine salt of lifitegrast (Ia) and to a process for its preparation.

Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating MAGL-mediated diseases and disorders including, e.g., pain, an inflammatory disorder, traumatic brain injury, depression, anxiety, Alzheimer's disease, a metabolic disorder, stroke, or cancer.

Abstract: The present invention relates to a compound for treating a degenerative disease of central nervous system or a brain tumor, a composition and a use thereof, wherein the compound has the structure of Formula I. These compounds can be used as SGK1 and JNK dual inhibitors with antioxidant effect, which can be formulated into suitable formulations for treating a degenerative disease of central nervous system or a brain tumor.

Abstract: This document relates to an abiraterone derivative, 2-(((3S,8R,9S,10R,13S,14S)-10,13-dimethyl-17-(pyridin-3-yl)-2,3,4,7,8,9,10,11,12,13,14,15-dodecahydro-1H-cyclopenta[a]phenanthren-3-yl)oxy)-2-oxoacetic acid (ABOA). This document also relates to compositions comprising a non-covalently bound complex comprising ABOA and human serum albumin, wherein the ABOA and the human serum albumin in the composition have a ratio of weight from about 1:1 to about 1:2000. This document also relates to compositions comprising ABOA and human serum albumin, wherein the ABOA and the human serum albumin in the composition have a ratio of weight from about 1:1 to about 1:2000. This document also relates to compositions consisting essentially of ABOA and human serum albumin, wherein the ABOA and the human serum albumin in the composition have a ratio of weight from about 1:1 to about 1:2000.

Abstract: Compounds having a structure according to formula (I) where R1, R2, and R3 are as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.

Abstract: Substituted-3H-imidazo[4,5-c]pyridine and 1H-pyrrolo[2,3-c]pyridine series of novel Ectonucleotide Pyrophosphatase/Phosphodiesterase-1 (ENPP1) and related compounds, which are useful as inhibitors of ENPP1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the ENPP1.