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AZABENZIMIDAZOLE DERIVATIVES AS PI3K BETA INHIBITORS

The present invention relates to azabenzimidazole derivatives of Formula (I) (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as pI3Kbeta inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active 10 ingredient as well as the use of said compounds as a medicament.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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Heterocyclic Compounds and Methods of Use

This disclosure provides compounds and methods of using those compounds to treat metabolic disorders and hyperproliferative disorders, including administration of the compounds in conjunction with hormone receptor antagonists.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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Pyridazine -3- formamide compound, preparation method and application thereof in medicine and pharmacy (by machine translation)

The invention relates to a method for the treatment and Janus or prevention of (JAK), kinase 2(TYK2), in particular tyrosine kinase, of a compound or a pharmaceutically acceptable salt. thereof, in particular, or a pharmaceutically acceptable salt thereof, to a pharmaceutical composition (I) containing said compound or a pharmaceutically acceptable salt thereof, and a process for the preparation of said compound or a pharmaceutically acceptable salt of said compound or a pharmaceutically acceptable salt of said compound or a pharmaceutically acceptable salt of, said compound or a pharmaceutically acceptable salt of said compound or a solvate thereof, and a. pharmaceutically acceptable salt of said compound, The. compound of formula Janus or a pharmaceutically acceptable salt thereof, according (I) to claim. (by machine translation)

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Reference£º
Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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Piperadinyl-substituted pyridylalkane, alkene and alkine carboxamides

The invention relates to new piperidinyl-substituted pyridyl carboxamides of the general formula (I), wherein the structure element E has meanings (E1) or (E2) and whereby the heterocyclic ring can optionally have a double bond. These substances have especially high cytostatic activities and pronounced immunosuppressive properties which make them suitable for therapeutic treatment in broad tumor spectrum.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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3-(Carboxymethyl)-8-Amino-2-Oxo-1,3-Diaza-Spiro-[4.5]-Decane Derivatives

The invention relates to 3-(carboxymethyl)-8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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QUINOXALINE DERIVATIVES AS INHIBITORS OF THE TYROSINE KINASE ACTIVITY OF JANUS KINASES

The present invention relates to quinoxaline compound of the formula (I): wherein R1 is carbocyclyl or heterocyclyl, either of which is optionally substituted with 1, 2, 3, 4 or 5 R7; R2 is carbocyclyl or heterocyclyl, either of which is optionally substituted with 1, 2, 3, 4 or 5 R8; R3, R4, R5 and R6 are each independently hydrogen or R9; and R7, R8 and R9 are each independently selected from organic and inorganic substituents, their use in therapy of diseases, in particular diseases mediated by the tyrosine kinase activity of Janus kinases, including JAK-2 and JAK-3 kinases

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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Hi-JAK-ing the ubiquitin system: The design and physicochemical optimisation of JAK PROTACs

PROTACs have recently emerged as a novel paradigm in drug discovery. They can hijack existing biological machinery to selectively degrade proteins of interest, in a catalytic fashion. Here we describe the design, optimisation and biological activity of a set of novel PROTACs targeting the Janus kinase family (JAK1, JAK2, JAK3 and TYK2) of proximal membrane-bound proteins. The JAK family proteins display membrane localisation by virtue of their association with cytoplasmic tails of cytokine receptors, and there are no reports of a successful PROTAC strategy being deployed against this class of proteins. JAK PROTACs from two distinct JAK chemotypes were designed, optimising the physicochemical properties for each template to enhance cell permeation. These PROTACs are capable of inducing JAK1 and JAK2 degradation, demonstrating an extension of the PROTAC methodology to an unprecedented class of protein targets. A number of known ligase binders were explored, and it was found that PROTACs bearing an inhibitor of apoptosis protein (IAP) ligand induced significantly more JAK degradation over Von Hippel?Lindau (VHL) and Cereblon (CRBN) PROTACs. In addition, the mechanism of action of the JAK PROTACs was elucidated, and it was confirmed that JAK degradation was both IAP- and proteasome-dependent.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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PYRAZOLE COMPOUNDS

Compounds of formula (I): wherein R1, R2, R3, R4, R5, and X are defined herein. Also disclosed are pharmaceutical compositions and methods related to use of these compounds.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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NEW TETRACYCLIC COMPOUNDS

This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic [4,3- b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem

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SULFUR-CONTAINING BICYCLIC COMPOUND

A sulfur-containing bicyclic compound having a PAM action of GABAB, and it use for preventing and/or treating schizophrenia, CIAS, cognitive impairment, fragile X syndrome, autism spectrum disorder, spasticity, anxiety disorder, substance addiction, pain, fibromyalgia, or Charcot-Marie-Tooth disease. A pharmaceutical composition for preventing and/or treating schizophrenia, cognitive impairment associated with schizophrenia (CIAS), cognitive impairment, fragile X syndrome, autism spectrum disorder, spasticity, anxiety disorder, substance addiction, pain, fibromyalgia, Charcot-Marie-Tooth disease, or the like, which has a positive allosteric modulator (PAM action) of GABAB.

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Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem