Abstract: The invention is directed to substituted piperidine derivatives. Specifically, the invention is directed to compounds according to Formula IIII: wherein A, B, X, Y, L1, L2, L3, R1, R2, R3, R4, R5, R6, R9, z2, z4, z5, and z6 are as defined herein, and salts thereof.

Abstract: The invention relates to compounds of Formula (I), salts thereof, combinations, pharmaceutical compositions thereof, as well as therapeutic methods of treatment and prevention.

Abstract: Disclosed are compounds having the formula: wherein R1, R2, and R3 are as defined herein, and methods of making and using the same.

Abstract: The present disclosure relates to compositions for treating CD96 mediated diseases, and related methods.

Abstract: This invention relates to novel compounds according to Formula (I) which are inhibitors of furin, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of fibrotic diseases, including pulmonary fibrosis, renal fibrosis, liver fibrosis, skin fibrosis, ocular fibrosis, cardiac fibrosis, and other miscellaneous fibrotic conditions. The disclosed compounds may also be useful for treating other furin-mediated conditions, including but not limited to, hypertension, cancer, infectious diseases, and genetic disorders (e.g., cystic fibrosis (CF)), and neurodegenerative disorders.

Abstract: The present invention relates to novel compounds or pharmaceutically acceptable salts thereof, corresponding compositions, and methods and/or uses in therapy, for example in the treatment of parasitic infections such as malaria, in particular infection by Plasmodium falciparum.

Abstract: A modular production system including a plurality of production modules connected in a linear series to form a production tunnel, and collectively defining a production channel, and wherein at least one fluid inlet port defined along the production tunnel, said inlet port is in fluid communication with a pressurized fluid source, whereby influx of fluid from said fluid source through said fluid inlet port acts to maintain the fluid pressure within the production channel at a higher pressure than the atmospheric pressure outside of the production tunnel; and wherein one of said production modules positioned between said proximal-most and distal-most production modules comprises a depyrogenator and/or sterilization module, comprising a transparent tubular body, and an irradiation source positioned external to said transparent tubular body, said irradiation source capable of heating the internal environment of the depyrogenation and/or sterilization module to a temperature sufficient to depyrogenate or sterilize

Abstract: This invention relates to novel compounds according to Formula (I) which are inhibitors of ghrelin O-acyltransferase (GOAT), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of metabolic disorders (e.g. Prader-Willi syndrome, metabolic syndrome, insulin resistance, impaired glucose tolerance, prediabetes, diabetes mellitus (e.g., type II diabetes mellitus), dysglycemia (e.g., hyperglycemia), obesity (e.g., obesity caused by Prader-Willi syndrome), increased adiposity, poor glycemic control, hyperphagia, impaired satiety, dyslipidemia (e.g., atherogenic dyslipidemia), hepatic steatosis (e.g., non-alcoholic fatty liver disease (e.g., non-alcoholic steatohepatitis))), psychiatric disorders (e.g., eating disorders (e.g., bulimia nervosa, binge eating disorder, night-time eating syndrome), substance related disorders (e.g., addiction disorders (e.g.

Abstract: Disclosed are compounds having the formula: (I) wherein q, r, s, A, B, C, RA1, RA2, RB1, RB2, RC1, RC2, R3, R4, R5, R6, R14, R15, R16, R17, Rx, and Ry are as defined herein, or a tautomer thereof, or a salt, particularly a pharmaceutically acceptable salt, thereof.

Abstract: Methods are provided for determining prognosis of multiple myeloma in a patient by measuring expression of BCMA in a sample. Also provided are methods for treating multiple myeloma by measuring expression of BCMA in a sample and administering an effective amount of an antigen binding protein that binds BCMA. Also provided are kits for measuring BCMA expression in a sample.

Abstract: This invention relates to novel compounds according to Formula (I) which are inhibitors of ghrelin O-acyltransferase (GOAT), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of metabolic disorders (e.g. Prader-Willi syndrome, metabolic syndrome, insulin resistance, impaired glucose tolerance, prediabetes, diabetes mellitus (e.g., type II diabetes mellitus), dysglycemia (e.g., hyperglycemia), obesity (e.g., obesity caused by Prader-Willi syndrome), increased adiposity, poor glycemic control, hyperphagia, impaired satiety, dyslipidemia (e.g., atherogenic dyslipidemia), hepatic steatosis (e.g., non-alcoholic fatty liver disease (e.g., non-alcoholic steatohepatitis))), psychiatric disorders (e.g., eating disorders (e.g., bulimia nervosa, binge eating disorder, night-time eating syndrome), substance related disorders (e.g., addiction disorders (e.g.

Abstract: The invention relates to compounds of Formula (I), (Ia), (Ib), (II) or (III), salts thereof, pharmaceutical compositions thereof, as well as therapeutic methods of treatment and prevention.

Abstract: The present invention provides a combination of a Type I protein arginine methyltransferase (Type I PRMT) inhibitor and a Type II protein arginine methyltransferase (Type II PRMT) inhibitor. The present invention also provides methods for treating cancer in a human in need thereof, the methods comprising administering to the human a combination of a Type I PRMT inhibitor and a Type II PRMT inhibitor, together with at least one of: a pharmaceutically acceptable carrier and a pharmaceutically acceptable diluent, thereby treating the cancer in the human. The present invention further provide a pharmaceutical composition comprising a therapeutically effective amount of a Type I PRMT inhibitor and a second pharmaceutical composition comprising a therapeutically effective amount of a Type II PRMT inhibitor.

Abstract: The present invention relates to an ICOS binding protein or antigen binding portion thereof that is an agonist to human ICOS and does not induce complement, ADCC, or CDC when placed in contact with a T cell in vivo and methods of treating cancer, infectious disease and/or sepsis with said ICOS binding protein or antigen binding portion thereof. Further the ICOS binding proteins or antigen binding portions thereof of the present invention are capable of activating a T cell when placed in contact with said T cell; stimulating T cell proliferation when placed in contact with said T cell and/or inducing cytokine production when placed in contact with said T cell. The present invention relates to ICOS binding proteins or antigen binding portions thereof comprising one or more of: SEQ ID NO: 1; SEQ ID NO:2; SEQ ID NO:3; SEQ ID NO:4; SEQ ID NO:5; and/or SEQ ID NO:6.

Abstract: An electronic device including a continuity sensor and electrical circuitry configured to detect and report the continuity state of an article, container or product packaging is disclosed. The continuity sensor includes a first substrate with first and second coils thereon, and a second substrate with a third coil thereon. The first coil has an integrated circuit electrically connected thereto. The first substrate is part of, or is attached or secured to a part of the article, container or packaging. The second substrate is another part of, or is attached or secured to another part of the article, container or packaging. One of the article, container or packaging parts is (re)movable with respect to the other part. The first and second coils have one coupling when the article, container or packaging is closed or sealed, and a different coupling when the article, container or packaging is open or unsealed.

Abstract: Disclosed herein are new C-mannoside compounds and compositions and their application as pharmaceuticals for the treatment of human disease. Methods of inhibition of FimH activity in a human subject are also provided for the treatment diseases such as urinary tract infection.

Abstract: Compounds of formula (I) and salts thereof: wherein R1, R2, R3, R4 are defined herein. Compounds of formula (I) and salts thereof have been found to inhibit the binding of the BET family of bromodomain proteins to, for example, acetylated lysine residues and thus may have use in therapy, for example in the treatment of autoimmune and inflammatory diseases, such as rheumatoid arthritis; and cancers.

Abstract: A compound of formula (I) wherein R, R1, R2, R3, Y, Y1, a, X, and Z are as defined herein. The compounds of the present invention are inhibitors of hematopoietic prostaglandin D synthase (H-PGDS) and can be useful in the treatment of Duchenne Muscular Dystrophy. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting H-PGDS activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

Abstract: Disclosed are compounds having the formula: wherein q, r, s, A, B, C, RA1, RA2, RB1, RB2, RC1, RC2, R3, R4, R5, R6, R14, R15, R16, and R17, are as defined herein, or a tautomer thereof, or a salt, particularly a pharmaceutically acceptable salt, thereof.

Abstract: The invention is directed to substituted pyridine derivatives. Specifically, the invention is directed to compounds according to Formula (Iar): wherein Yar, X1ar, X2ar, R1ar, R2ar, R3ar, R4ar and R5ar are as defined herein; or a pharmaceutically acceptable salt or prodrug thereof. The compounds of the invention are selective inhibitors of DNMT1 and can be useful in the treatment of cancer, pre-cancerous syndromes, beta hemoglobinopathy disorders, sickle cell disease, sickle cell anemia, and beta thalassemia, and diseases associated with DNMT1 inhibition. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting DNMT1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.