1363380-59-9

Upstream product

• 3174-74-1 dihydropyran 
• 25637-16-5 4-bromotetrahydro-2H-pyran 
• 1351450-56-0 3-benzyloxytetrahydropyran-4-one 
• 1351450-55-9 3-benzyloxy-4,4-dimethoxytetrahydropyran 
• 29943-42-8 Tetrahydro-4H-pyran-4-one 
• 104681-92-7 4,4-dimethoxytetrahydro-2H-pyran-3-ol 
• 286-22-6 3,4-epoxytetrahydropyran 
• 134419-59-3 4-oxanyl methanesulfonate 
• 2081-44-9 Tetrahydro-pyran-4-ol 
• 1363380-59-9 trans-4-aminotetrahydro-2H-pyran-3-ol 
• 1268515-66-7 (3R,4S)-3-(benzyloxy)tetrahydro-2H-pyran-4-amine 
• 1268515-65-6 (3S)-3-(benzyloxy)-tetrahydro-4H-pyran-4-one 
• 1268515-64-5 (3S)-3-(benzylyoxy)-4,4-dimethoxytetrahydro-2H-pyran 
• 1034144-67-6 (3S)-4,4-dimethoxytetrahydro-2H-pyran-3-ol 

Downstream Products

• 1096770-58-9 (3R,4S)-4-aminotetrahydro-2H-pyran-3-ol 

Relevant academic research and scientific papers

MUSCARINIC M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS

The present invention relates to compounds of formula (I), or their isotopic forms, stereoisomers, tautomers or pharmaceutically acceptable salt (s) thereof as muscarinic M1 receptor positive allosteric modulators (M1 PAMs). The present invention describes the preparation, pharmaceutical composition and the use of compound formula (I).

BENZOISOQUINOLINONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS

The present invention is directed to substituted benzoisoquinolinone compounds, their salts, pharmaceutical compositions comprising them and their use in therapy. In particular, the invention is directed substituted benzoisoquinolinone compounds which are muscarinic M1 receptor positive allosteric modulators. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M1 receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M1 receptors are involved.

Synthesis and Pharmacological Evaluation of Heterocyclic Carboxamides: Positive Allosteric Modulators of the M1 Muscarinic Acetylcholine Receptor with Weak Agonist Activity and Diverse Modulatory Profiles

Targeting allosteric sites at M1 muscarinic acetylcholine receptors is a promising strategy for the treatment of Alzheimer's disease. Positive allosteric modulators not only may potentiate binding and/or signaling of the endogenous agonist acetylcholine (ACh) but also may possess direct agonist activity (thus referred to as PAM-agonists). Recent studies suggest that PAM-agonists with robust intrinsic efficacy are more likely to produce adverse effects in vivo. Herein we present the synthesis and pharmacological evaluation of a series of pyrrole-3-carboxamides with a diverse range of allosteric profiles. We proposed structural modifications at top, core, or pendant moieties of a prototypical molecule. Although generally there was a correlation between the degree of agonist activity and the modulatory potency of the PAMs, some derivatives displayed weak intrinsic efficacy yet maintained strong allosteric modulation. We also identified molecules with the ability to potentiate mainly the affinity or both affinity and efficacy of ACh.

QUINAZOLINE COMPOUNDS USEFUL AS M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS

The present invention is directed to compounds of Formula (I): (Formula (I)) and pharmaceutically acceptable salts thereof, wherein X, Y, Z, R1, R7, R8, R9, R11, n and p are defined herein. The compounds of Formula (I) are M1 receptor positive allosteric modulators that are useful in the treatment of diseases in which the M1 receptor is involved, including Alzheimer's disease, schizophrenia, pain and sleep disorders. The invention also relates to pharmaceutical compositions comprising a compound of Formula (I) and a pharmaceutically acceptable carrier, and to methods of using the compounds of Formula (I) in the treatment of diseases mediated by the M1 receptor.

FLOURO-NAPHTHYL DERIVATIVES

The present invention relates to compounds of formula wherein R1 is C4-6-cycloalkyl or C4-6-heterocycloalkyl, which are optionally substituted by one or two substituents, selected from hydroxy or lower alkyl; A is phenyl, pyridinyl or piperidinyl; R2 is hydrogen, halogen, lower alkyl, cyano, C4-6-cycloalkyl, lower alkoxy, lower alkoxy substituted by halogen, or is a five- or six-membered heteroaryl, optionally substituted by lower alkyl; n is 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof. The compounds may be used for the treatment or prophylaxis of Alzheimer's disease, cognitive impairment, schizophrenia, pain or sleep disorders.

N-methyl tetrahydroquinoline M1 receptor positive allosteric modulators

The present invention is directed to N-methyl tetrahydroquinoline compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.

PYRIDINE DERIVATIVES AS MUSCARINIC M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS

The present invention provides, in part, compounds of Formula I: (I) N-oxides thereof, and pharmaceutically acceptable salts of the compounds or N-oxides; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds,N-oxides, or salts, and their uses for treating M1-mediated (or M1-associated) disorders including, e.g., Alzheimer's disease, schizophrenia (e.g., its cognitive and negative symptoms), pain, addiction, and a sleep disorder.

INDOL AND INDAZOL DERIVATIVES

The present invention relates to indole and indazole derivatives of the following formula (I) wherein A is (AA) and the remaining variables are as defined in the specification. The compounds may be used for the treatment or prophylaxis of Alzheimer's disease, cognitive impairment, schizophrenia, pain or sleep disorders.

FLUORO-NAPHTHYL DERIVATIVES

The present invention relates to compounds of formula wherein R1 is C4-6-cycloalkyl or C4-6-heterocycloalkyl, which are optionally substituted by one or two substituents, selected from hydroxy or lower alkyl; A is phenyl, pyridinyl or piperidinyl; R2 is hydrogen, halogen, lower alkyl, cyano, C4-6-cycloalkyl, lower alkoxy, lower alkoxy substituted by halogen, or is a five-or six-membered heteroaryl, optionally substituted by lower alkyl; n is 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof. The compounds may be used for the treatment or prophylaxis of Alzheimer's disease, cognitive impairment, schizophrenia, pain or sleep disorders.

SELECTIVE ANDROGEN RECEPTOR MODULATORS

The present invention provides novel selective androgen receptor modulators and their salts and pharmaceutical compositions thereof.