158984-76-0

Upstream product

• 586-95-8 pyridine-4-methanol 
• 100-39-0 benzyl bromide 
• 100-44-7 benzyl chloride 
• 219975-80-1 1-benzyl-4-(hydroxymethyl)pyridin-1-ium chloride 
• 503545-00-4 1-benzyl-2,6-dioxo-1,2,3,6-tetrahydropyridine-4-carboxylic acid ethyl ester 

Downstream Products

• 909035-04-7 1-benzyl-4-[(2-bromo-4,5-difluorophenoxy)methyl]-1,2,3,6-tetrahydropyridine 
• 189745-22-0 1-benzyl-4-benzyloxymethyl-1,2,3,6-tetrahydropyridine 
• 878167-10-3 1-benzyl-4-(4-chloro-2-iodo-phenoxymethyl)-1,2,3,6-tetrahydro-pyridine 
• 1013333-17-9 1-(phenylmethyl)-4-[(tert-butyldimethylsilanyloxy)methyl]-1,2,3,6-tetrahydropyridine 
• 67686-01-5 1-benzyl-4-piperidinemethanol 
• 39478-61-0 trans-1-(phenylmethyl)-4-(hydroxymethyl)piperidin-3-ol 
• 1150315-94-8 4-{[(2-bromo-4-chlorophenyl)oxy]methyl}-1-(phenylmethyl)-1,2,3,6-tetrahydropyridine 
• 1441357-42-1 C₁₉H₂₁NO 
• 219975-81-2 rel-tert-Butyl (3R,4R)-3-hydroxy-4-(hydroxymethyl)piperidine-1-carboxylate 
• 195628-18-3 rel-(3R,4R)-4-(hydroxymethyl)piperidin-3-ol 
• 1355084-90-0 3-{6-[(2,6-dichlorophenyl)methoxy]-2H-spiro[1-benzofuran-3,4'-piperidine]-1'-yl}-2-methylpropanoic acid hydrochloride 
• 1355092-75-9 4-{6-[(2,6-dichlorophenyl)methoxy]-2H-spiro[1-benzofuran-3,4'-piperidine]-1'-yl}butanoic acid 
• 1355085-09-4 2-{6-[(2,6-dichlorophenyl)methoxy]-2H-spiro[1-benzofuran-3,4'-piperidine]-1'-yl}acetic acid hydrochloride 
• 1355087-58-9 1'-benzyl-6-methoxy-2H-spiro(benzofuran-3,4'-piperidine) hydrochloride 

Relevant academic research and scientific papers

OXALAMIDES AS MODULATORS OF INDOLEAMINE 2,3-DIOXYGENASE

The present invention relates to novel compounds which act as modulators of indoleamine 2,3-dioxygenase (IDOl) and to the use of said compounds in the prophylaxis and/or treatment of diseases or conditions mediated by indoleamine 2,3-dioxygenase. The inve

Spiro-1-benzofuranpiperidinylalkanoic acids as a novel and selective sphingosine S1P5 receptor agonist chemotype

The synthesis and SAR of a novel class of spirobenzofuranpiperidinyl-derived alkanoic acids 6–34 as sphingosine S1P5 receptor agonists are described. The target compounds generally elicit high S1P5 receptor agonistic potencies and in general are selective against both S1P1 and S1P3 receptor subtypes. The key compound 32 shows a high bioavailability of 73% and a CNS/plasma ratio of 0.8 after oral administration in rats.

PYRAZOLO[1,5-A]PYRIMIDINE-5,7-DIAMINE COMPOUNDS AS CDK INHIBITORS AND THEIR THERAPEUTIC USE

The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain pyrazolo[1,5-a]pyrimidine-5,7- diamine compounds (referred to herein as "PPDA compounds") that, inter alia, inhibit (e.g., selectively inhibit) CDK (e.g., CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8, CDK9, CDK10, CDK11, CDK12, CDK13, etc.). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CDK; and to treat disorders including: disorders that are associated with CDK; disorders that result from an inappropriate activity of a cyclin-dependent kinase (CDK); disorders that are associated with CDK mutation; disorders that are associated with CDK overexpression; disorders that are associated with upstream pathway activation of CDK; disorders that are ameliorated by the inhibition of CDK; proliferative disorders; cancer; viral infections (including HIV); neurodegenerative disorders (including Alzheimer's disease and Parkinson's disease); ischaemia; renal diseases; and cardiovascular disorders (including atherosclerosis). Optionally, the treatment further comprises treatment (e.g., simultaneous or sequential treatment) with a further active agent which is, e.g., an aromatase inhibitor, an anti-estrogen, a Her2 blocker, a cytotoxic chemotherapeutic agent, etc.

SUBSTITUTED PYRIDINE DERIVATIVES AS FABI INHIBITORS

The present invention provides substituted pyridine derivatives of formula (I), which may be therapeutically useful as as anti-bacterial agents, more particulalrly FabI inhibitors. Formula(I) in which R1 to R5 and L have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage anti-bacterial agents, more particularly FabI inhibitors. The present invention also provides methods for synthesizing and administering the FabI inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.

SPIRO-CYCLIC AMINE DERIVATIVES AS S1P MODULATORS

The present invention relates spiro- cyclic amine derivatives of the formula (I) wherein R1; R2; R3; Q; -W-T-; R5; Z; and A have the definitions provided in the claims; or a pharmaceutically acceptable salt, a solvate or hydrate thereof or one or more N-oxides thereof. The compounds of the invention have affinity to S1P receptors and may be used in the treatment, alleviation or prevention of diseases and conditions in which (a) SIP receptor (s) is (are) involved

Synthesis of novel piperidyl spirofused benzofurans/benzopyrans by radical cyclization

Several new piperidyl spirofused benzofurans and piperidyl spirofused benzopyrans were synthesized via an intramolecular radical cyclization as the key step. It was found that the yield of the formation of five-member ring was much higher than that of six

Development of two diastereoselective routes towards trans-4-aminomethyl-piperidin-3-ol building blocks

Two diastereoselective, scaleable routes towards trans-3,4-disubstituted piperidines with a 4-hydroxymethyl-3-hydroxy or 4-aminomethyl-3-hydroxy substitution pattern are being described. In the first route, the 3,4-trans configuration was introduced regio- and diastereoselectively via a hydroboration/oxidation sequence starting from 4-hydroxymethylpyridine. In the second route, regioselective epoxide ring opening of N-benzyl-3,4-epoxy-piperidine was achieved with LiCN, in situ generated from acetocyanohydrin and LiNH2. The regioselectivity of both the hydroboration and the epoxide ring opening was positively influenced by the presence of the basic piperidine nitrogen. Both routes have been optimized to be performed at large scale.

SPIROPIPERIDINE DERIVATIVES

The invention provides compounds of formula (I): wherein the dotted line represents an optional covalent bond between X and Y, and X, Y, Z, m, R2, R3, R4, R5, R6, R7, R8, R9, a and b have the meanings given in the specification, and pharmaceutically acceptable salts and solvates thereof. The compounds are delta opioid receptor agonists and have a number of therapeutic applications, particularly in the treatment of pain.

Synthesis of piperidine derivatives by reduction of pyridinium salts

Piperidine derivatives 1a-e and 2a-f have been prepared by the reduction of 3-and 4-substituted pyridinium salts with NaBH4 in moderate to excellent yields. The reactions regioselectively give 1,2,5,6-tetrahydropyridines, and the yields depend greatly upon the nature of substituents on the phenyl ring and on the nitrogen atom, the nature and the position of the substituents on the pyridyl ring, and the chain length between the aryloxy and the pyridyl groups. Copyright Taylor & Francis Group, LLC.

4-(aminomethyl)-piperidine benzamides for treating gastrointestinal disorders

The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, —R1—R2— is a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C1-6alkyl or hydroxy; R3is hydrogen or halo; R4is hydrogen or C1-6alkyl; R5is hydrogen or C1-6alkyl; L is C3-6cycloalkyl, oxoC5-6cycloalkyl, C2-6alkenyl, or L is a radical of formula —Alk—R6—, Alk—X—R7, —Alk—Y—C(═O)—R9, or —Alk—Y—C(═O)—NR11R12wherein each Alk is C1-12alkanediyl; and R6is hydrogen, amino, cyano, C1-6alkylsulfonylamino, C3-6cycloalkyl, oxoC5-6cycloalkyl, aryl or a heterocyclic ringsystem; R7is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, aryl or a heterocyclic ringsystem; X is O, S, SO2or NR8; said R8being hydrogen or C1-6alkyl; R9is hydrogen, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxy, hydroxy or aryl; Y is a direct bond or NR10; said R10being hydrogen, or C1-6alkyl; R11and R12each independently are hydrogen, C1-6alkyl, C3-6cycloalkyl, or R11and R12combined with the nitrogen atom may form an optionally substituted pyrrolidinyl, piperidinyl, piperazinyl or 4-morpholinyl ring. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating or preventing gastrointestinal disorders.