cas 59184-90-6, 2-(PIPERIDIN-4-YL)-ACETIC ACID ETHYL ESTER

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Chemoselective catalytic hydrogenation of alkenes by Lindlar catalyst
Commercially available Lindlar catalyst (10% by weight) in methanol, selectively hydrogenates various alkenes in the presence of benzyl ether and benzyl amine functionalities.
Ghosh, Arun K.,Krishnan
p. 947 - 948
(1998)
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Therapeutic Uses
This invention relates to novel therapeutic uses for compounds which are inverse agonists of the H3 receptor. In particular this invention relates to therapeutic use of these compounds in the treatment of Multiple Sclerosis.
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(2015/03/28)

HETEROARYL COMPOUNDS AS 5-HT4 RECEPTOR LIGANDS
The present invention relates to novel compounds of formula (I), and their pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their pharmaceutically acceptable salts. The compounds of formula (I) are useful in the treatment of various disorders that are related to 5-HT4 receptors.
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(2014/07/08)

HETEROARYL COMPOUNDS AS 5-HT4 RECEPTOR LIGANDS
The present invention relates to novel compounds of formula (I), and their pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their pharmaceutically acceptable salts. The compounds of formula (I) are useful in the treatment of various disorders that are related to 5-HT4 receptors.
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(2013/04/10)

THERAPEUTIC USES
This invention relates to novel therapeutic uses for compounds which are inverse agonists of the H3 receptor. In particular this invention relates to therapeutic use of these compounds in the treatment of Multiple Sclerosis.
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(2013/07/31)

Discovery of Potent, Selective, and Orally Active Carboxylic Acid Based Inhibitors of Matrix Metalloproteinase-13
The matrix metalloproteinase enzyme MMP-13 plays a key role in the degradation of type II collagen in cartilage and bone in osteoarthritis (OA). An effective MMP-13 inhibitor would therefore be a novel disease modifying therapy for the treatment of arthritis. Our efforts have resulted in the discovery of a series of carboxylic acid inhibitors of MMP-13 that do not significantly inhibit the related MMP-1 (collagenase-1) or tumor necrosis factor-α (TNF-α) converting enzyme (TACE). It has previously been suggested (but not proven) that inhibition of the latter two enzymes could lead to side effects. A promising carboxylic acid lead 9 was identified and a convergent synthesis developed. This paper describes the optimization of 9 and the identification of a compound 24f for further development. Compound 24f is a subnanomolar inhibitor of MMP-13 (IC50 value 0.5 nM and Ki of 0.19 nM) having no activity against MMP-1 or TACE (IC50 of >10000 nM). Furthermore, in a rat model of MMP-13-induced cartilage degradation, 24f significantly reduced proteoglycan release following oral dosing at 30 mg/kg (75% inhibition, p 0.05) and at 10 mg/kg (40% inhibition, p 0.05).
Monovich, Lauren G.,Tommasi, Ruben A.,Fujimoto, Roger A.,Blancuzzi, Vincent,Clark, Kirk,Cornell, Wendy D.,Doti, Robert,Doughty, John,Fang, James,Farley, David,Fitt, John,Ganu, Vishwas,Goldberg, Ronald,Goldstein, Robert,Lavoie, Stacey,Kulathila, Raviraj,Macchia, William,Parker, David T.,Melton, Richard,O'Byrne, Elizabeth,Pastor, Gary,Pellas, Theodore,Quadros, Elizabeth,Reel, Noela,Roland, Dennis M.,Sakane, Yumi,Singh, Hem,Skiles, Jerry,Somers, Joseph,Toscano, Karen,Wigg, Andrew,Zhou, Siyuan,Zhu, Lijuan,Shieh, Wen-Chung,Xue, Song,McQuire, Leslie W.
experimental part
p. 3523 - 3538
(2010/03/30)

Microwave-assisted hydrogenation of pyridines
Using a commercially available device for controlled introduction of hydrogen in a vial for reactions under microwave dielectric heating, we developed a protocol for the transformation of substituted pyridines into the corresponding piperidines. Complete reduction occurred in 40 minutes, or even less, on substrates that require 24-48 hours to be reduced under standard conditions. Moreover, the reduction proved to be as stereoselective as the corresponding reaction carried out at room temperature. Georg Thieme Verlag Stuttgart.
Piras, Leonarda,Genesio, Eva,Ghiron, Chiara,Taddei, Maurizio
body text
p. 1125 - 1128
(2009/04/04)

COMPOSITIONS AND METHODS INCLUDING CELL DEATH INDUCERS AND PROCASPASE ACTIVATION
Compositions and methods are disclosed in embodiments relating to induction of cell death such as in cancer cells. Compounds and related methods for synthesis and use thereof, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells are disclosed. Compounds are disclosed in connection with modification of procaspases such as procaspase-3. In embodiments, compositions are capable of activation of procaspase-3.
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Page/Page column 76

(2008/12/08)

3-Mercaptopropionic acids as efficacious inhibitors of activated thrombin activatable fibrinolysis inhibitor (TAFIa)
A novel series of cyclic potent, selective, small molecule, thiol-based inhibitors of activated thrombin activatable fibrinolysis inhibitor (TAFIa) and the crystal structures of TAFIa inhibitors bound to porcine pancreatic carboxypeptidase B are described. Three series of cyclic arginine and lysine mimetic inhibitors vary significantly in their selectivity against other human basic carboxypeptidases, carboxypeptidase N and carboxypeptidase B. (-)2a displays TAFIa IC50 = 3 nM and 600-fold selectivity against CPN. Inhibition of TAFIa with (rac)2a resulted in dose dependent acceleration of human plasma clot lysis in vitro and was efficacious as an adjunct to tPA in an in vivo rabbit jugular vein thrombolysis model.
Islam, Imadul,Bryant, Judi,May, Karen,Mohan, Raju,Yuan, Shendong,Kent, Lorraine,Morser, John,Zhao, Lei,Vergona, Ron,White, Kathy,Adler, Marc,Whitlow, Marc,Buckman, Brad O.
p. 1349 - 1354
(2007/10/03)

NOVEL TRICYCLIC PIPERIDINYL COMPOUNDS USEFUL AS INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE
Novel tricyclic compounds of formula (1.0) or a pharmaceutically acceptable salt or solvate thereof, wherein: one of a, b, c, and d represents N or NR, wherein R is O-, -CH3 or -(CH2)nCO2H wherein n is 1 to 3, and the remaining a, b, c and d groups represent CR or CR; or each of a, b, c and d is independently selected from CR or CR; each R and each R is independently selected from H, halo, -CR3, -OR, -COR, -SR, -S(O)tR (wherein t is 0, 1 or 2), -SCN, -N(R)2, -NRR, -NO2, -OC(O)R, -CO2R, -OCO2R, -CN, -NHC(O)R, -NHSO2R, -CONHR, -CONHCH2CH2OH, -NRCOOR, -SRC(O)OR, -SRN(R); n is 0 (zero), 1, 2, 3, 4, 5 or 6; T is -CO-; -SO-; -SO2-; or -CRR-; Z represents alkyl, aryl, aralkyl, heteroalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl, heterocycloalkylalkyl, -OR, -SR, -CRR, -NRR, formulae (i), (ii), (iii), (iv), (v) and (vi). Pharmaceutical compositions are disclosed which are inhibitors of the enzyme, farnesyl protein transferase. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering the novel tricyclic compound to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human.
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Page/Page column 74

(2008/06/13)

Diarylacetylene piperidinyl amides as novel anxiolytics
N-Phenyl-2-[1-[3-(2-pyridinylethynyl)benzoyl]-4-piperidine]acetamide (9) and related piperidine acetamide derivatives have good oral activity in the elevated plus maze, an animal model predictive of clinical efficacy for the treatment of anxiety. Modest affinity was observed for the neurokinin NK-1 and 2 receptors, which are known to be involved in the regulation of mood and emotion.
Kordik, Cheryl P.,Luo, Chi,Gutherman, Maryann,Vaidya, Anil H.,Rosenthal, Daniel I.,Crooke, Jeffrey J.,McKenney, Sandra L.,Plata-Salaman, Carlos R.,Reitz, Allen B.
p. 3065 - 3067
(2007/10/03)

TRICYCLIC BENZAZEPINE DERIVATIVES AS SQUALENE SYNTHASE INHIBITORS USED FOR THE TREATMENT OF CARDIOVASCULAR DISEASES
The invention relates to novel tricyclic benzazepine derivatives of formula (I), methods for the production thereof, the use thereof for treating and/or preventing diseases, and the use thereof for producing medicaments used for the treatment and/or prophylaxis of diseases, preferably cardiovascular diseases, particularly dyslipidemia, arteriosclerosis, restenosis, and ischemia.
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Page/Page column 32

(2008/06/13)

TETRAHYDROBENZO[D]AZEPIN-2- ONE DERIVATIVES AND THE USE THEREOF FOR TREATING CARDIOVASCULAR DISEASES
The invention concerns novel tetrahydrobenzo[d]azepin-2-one derivatives, a method for the production thereof, their use for treating and/or preventing diseases, and their use for producing medicaments for treating and/or preventing diseases, preferably for treating and/or preventing cardiovascular diseases, particularly dyslipidemias, arteriosclerosis, restenosis and ischemias.
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Page/Page column 28

(2008/06/13)

NOVEL INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE
Novel compounds and pharmaceutical compositions are disclosed which are inhibitors of the enzyme, farnesyl-protein transferase. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering the novel aminooxyamide compound to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human.
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Page/Page column 85

(2010/02/12)

FUSED BENZENE DERIVATIVE AND USE
The present invention provides a compound represented by the general formula: [wherein Ring A represents an optionally substituted 5- to 8-membered ring, Ring B represents a further optionally substituted 4- to 10-membered ring, Ring C represents a further optionally substituted benzene ring, X1 represents carbon atom, X2 represents a carbon atom, an oxygen atom, etc., W represents a nitrogen atom, etc., Y11 represents a group represented by the formula CR2R3' (wherein R2 represents a hydrogen atom, a cyano group, a nitro group, etc., and R3' represents a hydrogen atom, a cyano group, a nitro group, etc., respectively), Y21 represents a group represented by the formula CR4R5' (wherein R4 represents a hydrogen atom, a cyano group, a nitro group, etc., and R5' represents a hydrogen atom, a cyano group, a nitro group, etc., respectively), etc., and R1 represents an electron-withdrawing group, respectively. The formula represents a single bond or a double bond] or a salt thereof, which is useful as an androgen receptor modulator.
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Page/Page column 85

(2010/02/12)

Novel farnesyl protein transferase inhibitors as antitumor agents
Disclosed are novel tricyclic compounds represented by the formula (1.0): and a pharmaceutically acceptable salt or solvate thereof. The compounds are useful for inhibiting farnesyl protein transferase. Also disclosed are pharmaceutical compositions comprising compounds of formula 1.0. Also disclosed are methods of treating cancer using the compounds of formula 1.0.
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Page 198

(2010/02/07)

VLA-4 INHIBITORS
The present invention relates to a compound represented by the following formula (I): (wherein, W represents WA-A1 -WB - (in which, WA is substituted or unsubstituted aryl, etc., A1 is -NR1-, single bond, -C(O)-, etc., and WB is substituted or unsubstituted arylene, etc.), R is single bond, -NH-, -OCH2-, alkenylene, etc., X is -C(O) -CH2-, etc., and M is, for example, the following formula: (in which, R11, R12 and R13 each independently represents hydrogen, hydroxyl, amino, halogen, etc., R14 is hydrogen or lower alkyl, Y represents -CH2-O-, etc., Z is substituted or unsubstituted arylene, etc., A2 is single bond, etc, and R10 is hydroxyl or lower alkoxy)), or salt thereof; and a medicament containing the same. This compound or salt thereof selectively inhibits binding of cell adhesion molecules to VAL-4 and exhibits high bioavailability so that it is useful as a preventive and/or remedy for inflammatory diseases, autoimmune diseases, metastasis, bronchial asthma, rhinostenosis, diabetes, and the like.
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(2008/06/13)

Pyridyl-containing spirocyclic compounds as inhibitors of fibrinogen-dependent platelet aggregation
Disclosed are certain substituted or unsubstituted pyridyl-containing spirocyclic compounds substituted with both basic and acidic functionality, which are useful in inhibiting platelet aggregation, inhibiting the binding of fibrinogen to blood platelets, and preventing or treating thrombosis
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(2008/06/13)

Synthesis of some new 4-substituted N-benzyl-piperidines
Via Knoevenagel condensation of N-benzyl-4-piperidone with malononitrile some new 4-substituted N-benzyl-piperidines have been prepared. By means of these transformations an economic and large-scale synthesis of biologically important intermediate N-benzyl-piperidine-4-ethanol has been elaborated.
Doernyei, Gabor,Incze, Maria,Moldvai, Istvan,Szantay, Csaba
p. 2329 - 2338
(2007/10/03)

Synthesis and in vivo evaluation of 3-[11C]methyl-(3-methoxy-naphthalen)-2-yl-(1-benzyl-piperidin)-4-yl-acetate (SB-235753), as a putative dopamine D4 receptors antagonist for PET
(3-Methoxy-naphthalen)-2-yl-(1-benzyl-piperidin)-4-yl-acetate (SB-235753) was labelled with 11C (t(1/2) = 20.4 min) as a putative radioligand for the non-invasive assessment of Dopamine D4 receptors in vivo with positron emission tomography (PET). The precursor for the radiosynthesis 3-hydroxynaphthyl-2-[(N-benzyl)-piperidyl]-acetate hydrochloride was prepared by a four-step synthesis starting from ethyl-4-pyridyl acetate. The radiolabelling consisted of methylation with [11C]methyltriflate in dimethylformamide in the presence of potassium hydroxide. [11C]SB-235753, was synthesised in 30 min with a radiochemical yield of 10 ± 5% (EOS, non-decay corrected) with 99% radiochemical purity and specific radioactivity of 10 ± 3 Ci/μmol. Biodistribution studies in rats with [11C]SB-235753 showed the uniform distribution of the tracer within different areas of the murine brain. At 30 min after injection 99% of the radioligand in plasma and 100% in cerebellum was metabolised. These findings suggest that [11C]SB-235753 can not be a suitable tracer for dopamine D4 receptor studies with PET.
Matarrese,Soloviev,Moresco,Todde,Simonelli,Colombo,Magni,Carpinelli,Fazio,Kienle, M. Galli
p. 359 - 374
(2007/10/03)

Benzylpiperazinyl and piperidinyl ethanone derivatives: dopamine receptor subtype specific ligands
Disclosed are compounds of the formula: or pharmaceutically acceptable addition salts thereof wherein: Y represents oxygen or sulfur; Z is nitrogen or CH; R1, R2 and R3 independently represent organic or inorganic substituents; R4 and R4' independently represent hydrogen, alkyl or form a ring with the atom to which they are attached; R5 represents hydrogen, alkyl, alkoxy, or alkylthio, and R6 represents hydrogen or alkyl; or R5 and R6 form a ring together with the atoms to which they are attached; and R7, R8, R9, R10 and R11 independently represent hydrogen or alkyl, which compounds are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents.
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(2008/06/13)

Pd/C(en)-catalyzed chemoselective hydrogenation with retention of the N-Cbz protective group and its scope and limitations
A chemoselective method for the hydrogenation of acetylene, olefin, azide, nitro and benzyl ester functionalities with retention of the aliphatic N-Cbz group was established. The chemoselectivity was accomplished by using a combination of 5% Pd/C-ethylenediamine [5% Pd/C(en)] and THF (or 1,4-dioxane) as a solvent, and the scope and limitations of this methodology were investigated. These results reinforce the utility of N-Cbz protective groups in synthetic chemistry, especially in peptide synthesis. (C) 2000 Elsevier Science Ltd.
Hattori, Kazuyuki,Sajiki, Hironao,Hirota, Kosaku
p. 8433 - 8441
(2007/10/03)

Aminoheterocyclic derivatives as antithrombotic or anticoagulant
The invention concerns compounds of formula (I), wherein each of G1, G2 and G6 is CH or n; m is 1 or 2; R1 includes hydrogen, halogeno and (1-4C)alkyl; M1 is a group of formula: NR2 -L1 -T1 R3, in which R2 and R3 together form a (1-4C)alkylene group, L1 includes (1-4C)alkylene, and T1 is CH or N; A may be a direct link; M2 is a group of the formula: (T2 R4)r -L2 T3 R5 in which R is 0 or 1, each of T2 and T3 is CH or N, each of R4 and R5 is hydrogen or (1-4C)alkyl, or R4 and R5 together form a (1-4C)alkylene group, and L2 includes (1-4C)alkylene; M3 may be a direct link to X; X includes sulphonyl; and Q includes naphthyl and a heterocycle moiety; or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use as antithrombotic or anticoagulant agents.
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(2008/06/13)

Tricyclic piperidinyl compounds useful as inhibitors of farnesyl-protein transferase
Novel tricyclic compounds and pharmaceutical compositions are disclosed which are inhibitors of the enzyme, farnesyl protein transferase. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering the novel tricyclic compound to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human.
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(2008/06/13)

Phenoxy- and phenoxyalkyl-piperidines as antiviral agents
Compounds of the formula STR1 wherein R1 is selected from STR2 Y is a bond or lower alkylene; R2 and R3 are independently hydrogen, lower-alkyl or halogen; R4 is STR3 R5 is hydrogen, lower-alkyl or halogen; R6 is hydrogen, lower-alkyl or halogen; R7 is hydrogen or lower-alkyl; R8 is hydrogen, lower-alkyl, or trifluoromethyl; R9 is lower-alkyl; R10 is lower-alkyl, trifluoromethyl or difluoromethyl; or pharmaceutically acceptable acid addition salts thereof are useful as antiviral agents.
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(2008/06/13)

TETRAZOLYL-(PHENOXY AND PHENOXYALKYL)-PIPERIDINYLPYRIDAZINES AS ANTIVIRAL AGENTS
Compounds of the formula wherein: Y is a bond, or C1-C6 alkylene; R1 is hydrogen or C1-C3 lower alkyl; R2 and R3 are each independently hydrogen, C1-C3 lower-qalkyl or halogen; R4 is hydrogen or C1-C3 lower-alkyl; or pharmaceutically acceptable acid addition salts thereof are useful as antiviral agents, particularly against picornaviruses
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(2008/06/13)

Syntheses and biological activities of 1,4-disubstituted piperidines
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Gupta,Saxena,Jain,Anand
p. 1010 - 1017
(2007/10/02)

1-PIPERIDINOPHTHALAZINES AS CARDIAC STIMULANTS
A series of 1-piperidinophthalazine derivatives as phosphodiesterase inhibitors and cardiac stimulants
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(2008/06/13)