cas 98977-36-7, 1-Boc-3-piperidone | Articles data

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Multi-chiral nitrogen-substituted piperidinol derivative and preparation method thereof
The invention belongs to the technical field of preparation of chiral piperidine alcohol compounds. The invention particularly relates to a multi-chiral nitrogen-substituted piperidinol derivative and a preparation method thereof. The 3 -hydroxypyridine serves as a starting raw material, and the corresponding substrate is obtained through catalytic hydrogenation reduction, amino protection, hydroxyl oxidation and Stork enamine - carbon alkylation to obtain the corresponding substrate. The process is simple, the reaction conditions are mild, and in particular, the ketone reducing liquid enzyme (KRED - 101) is selectively catalyzed, so that a chiral target product is obtained, and the yield is stable and the three wastes are few. The obtained piperidine heterocyclic derivative with the chiral center body has a plurality of drug activities and is suitable for industrial production.
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(2021/10/11)

Preparation method of N-tert-butyloxycarbonyl-3-piperidone and derivative thereof
The invention discloses a preparation method of N-tert-butyloxycarbonyl-3-piperidone, and the method comprises the following step: oxidizing N-tert-butyloxycarbonyl-3-hydroxypiperidine by virtue of aNaDCC-TEMPO system so as to generate N-tert-butyloxycarbonyl-3-piperidone. The invention also discloses a method for preparing (S)-N-tert-butyloxycarbonyl-3-hydroxypiperidine through an oxidation reaction and a reduction reaction by virtue of the NaDCC-TEMPO system. The method has the advantages of simple operation steps, high conversion rate and high product purity.
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(2020/07/21)

An investigation into the role of 2,6-lutidine as an additive for the RuCl3-NaIO4 mediated oxidative cleavage of olefins to ketones
2,6-Lutidine has been identified as a beneficial additive for the oxidative cleavage of olefins to ketones by NaIO4 in the presence of catalytic RuCl3, improving the yield and shortening the reaction times. In the absence of 2,6-lutidine reactions stalled at the diol intermediate with incomplete conversion to the desired ketones. The reaction protocol described herein also avoids the use of harmful solvents such as CCl4 and DCE and is tolerant of a range of functional groups.
Watson, David W.,Gill, Matthew,Kemmitt, Paul,Lamont, Scott G.,Popescu, Mihai V.,Simpson, Iain
supporting information
p. 4479 - 4482
(2018/11/23)

A N - Boc - 3 - piperidone preparation method (by machine translation)
The invention discloses a N - Boc - 3 - piperidone preparation method, which belongs to the technical field of organic synthesis. N - benzyl - 3 - hydroxy pyridine quaternary ammonium salt in the presence of a Lewis acid with potassium borohydride reduction reaction to obtain N - benzyl - 3 - piperidone; then after catalytic hydrogenation conditions with palladium of di-T-n-butyl reaction to obtain N - Boc - 3 - piperidone. Compared with the prior synthetic method, the invention one-step reaction will be N - benzyl - 3 - hydroxy pyridine quaternary ammonium salt selective reduction to obtain N - benzyl - 3 - piperidone, the reaction is fast, convenient separation of products, less side reaction, the advantages of synthetic route is simple. (by machine translation)
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Paragraph 0043; 0047; 0051; 0055; 0059; 0063

(2018/03/26)

A pharmaceutical intermediate N - BOC - 3 - piperidone preparation method (by machine translation)
The invention belongs to the field of organic synthetic technology, in particular to a pharmaceutical intermediate N - BOC - 3 - piperidone of the preparation method. To solve the problems of the prior N - BOC - 3 - piperidone in the preparation method of catalyst used is 2, 2, 6, 6 - tetramethyl piperidine nitrogen oxygen free radical or its derivatives catalytic abilities and the catalytic activity is low, the problem of catalyst is difficult to be recycled. The preparation method comprises: the 3 - hydroxy piperidine and sodium carbonate, di-T-n-butyl is the reaction in a solvent, to prepare the N - BOC - 3 - hydroxy piperidine; the N - BOC - 3 - hydroxy piperidine and potassium bromide, catalyst, sodium hypochlorite in weakly alkaline conditions arranged below the reaction in a solvent, to obtain N - BOC - 3 - piperidone. Preparation method of this invention the use of cross-linked polystyrene [...] in 9 - aza bicyclo [3, 3, 1] - nonyl - 9 - oxygen free radical as the catalyst, the use of sodium hypochlorite solution to carry out oxidation, in the method, the catalyst is easily recycled, can improve the preparation with the yield of the product, reducing N - BOC - 3 - piperidone the production cost of the, and can reduce the pollution of the environment. (by machine translation)
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Paragraph 0055; 0059-0061; 0076-0077

(2018/03/01)

Method for efficiently synthesizing 1-Boc-3-piperidone
The invention discloses a method for efficiently synthesizing 1-Boc-3-piperidone. The 1-Boc-3-piperidone is made of 1-benzyl-3-hydroxyl hydrochloride. The method includes carrying out reduction on the 1-benzyl-3-hydroxyl hydrochloride by the aid of sodium borohydride under the catalytic effects of platinum and carbon to obtain reduction products; adding activated carbon supported titanium tert-butoxide into the reduction products and carrying out reaction on the reduction products and di-tert-butyl dicarbonate to obtain 1-Boc-3-piperidinol; adding oxidizing agents into reaction liquid drop by drop under the effect of organic alkali and carrying out room-temperature reaction to obtain reaction products; purifying the reaction products after reaction is completely carried out so as to obtain the 1-Boc-3-piperidone. The activated carbon supported titanium tert-butoxide is used as a catalyst. The method has the advantages of short steps, mild synthesis conditions, inexpensive raw materials, high product yield, simplicity in purification and capability of reducing the production cost to a great extent.
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Paragraph 0021; 0025

(2018/02/04)

Metal-free, mild, nonepimerizing, chemo- and enantio- or diastereoselective N-alkylation of amines by alcohols via oxidation/imine-iminium formation/reductive amination: A pragmatic synthesis of octahydropyrazinopyridoindoles and higher ring analogues
A mild step and atom-economical nonepimerizing chemo- and enantioselective N-alkylating procedure has been developed via oxidation/imine-iminium formation/reduction cascade using TEMPO-BAIB-HEH-Bronsted acid catalysis in DMPU as solvent and a stoichiometric amount of amine. The optimized conditions were further extended for the nonenzymatic kinetic resolution of the chiral amine thus formed under nonenzymatic in situ hydrogen-transfer conditions using VAPOL-derived phosphoric acid (VAPOL-PA) as the Bronsted acid catalyst. The enantioselective cascade of the presented reaction was successfully utilized in the synthesis of octahydropyrazinopyridoindole and its higher ring analogues.
Khan, Imran A.,Saxena, Anil K.
p. 11656 - 11669
(2014/01/06)

SPIROCYCLIC MOLECULES AS PROTEIN KINASE INHIBITORS
The present invention relates to spirocyclic compounds of formula I, namely spirocyclic (1H-pyrazol-4-yl)-3-(1-(2,6-dichloro-3-fiuorophenyl) ethoxy)pyridin-2-amines having protein kinase inhibitory activity, and methods of synthesizing and using such compounds. Preferred compounds are c-Met and/or ALK inhibitors useful for the treatment of abnormal cell growth, such as cancers
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Paragraph 00250-00252

(2013/03/26)

Synthesis of 1,2,4-trisubstituted-1,2,5,6-tetrahydropyridines
A novel method for the synthesis of 1,2,4-trisubstituted- or 1,2,3,4-tetrasubstituted-1,2,5,6-tetrahydropyridine is presented. The process was carried out by the bromomethoxylation of 4-substituted-1,2,5,6- tetrahydropyridines 1 with N-bromosuccinimide (NBS) in methanol, dehydrobromination with 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU), and boron trifluoride etherate (BF3-OEt2)-catalyzed cross coupling of the corresponding enamine with trimethylsilyl-based nucleophiles. Homokainoid analogs were also synthesized via the protocol.
Chang, Meng-Yang,Lee, Ming-Fang,Lee, Nien-Chia,Huang, Yu-Ping,Lin, Chung-Han
p. 588 - 591
(2011/03/18)

PYRIMIDINE COMPOUNDS AS DELTA OPIOID RECEPTOR MODULATORS
Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows:wherein R1, R2, R3, and L, A, and Ra are defined herein.
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Page/Page column 36

(2011/05/08)

Gold (I) catalysis of X-H bond insertions
The utility of gold catalysis for carbene X-H bond insertion chemistry is described for the first time, taking advantage of the unique reactivity of sulfoxonium ylides as metal carbene precursors.
Mangion, Ian K.,Weisel, Mark
scheme or table
p. 5490 - 5492
(2010/10/20)

Conductometric method for the rapid characterization of the substrate specificity of amine-transaminases
Amine-transaminases (ATAs, ω-transaminases, ω-TA) are PLP-dependent enzymes that catalyze amino group transfer reactions. In contrast to the widespread and wellknown amino acid-transaminases, ATAs are able to convert substrates lacking an a-carboxylic functional group. They have gained increased attention because of their potential for the asymmetric synthesis of optically active amines, which are frequently used as building blocks for the preparation of numerous pharmaceuticals. Having already introduced a fast kinetic assay based on the conversion of the model substrate α-methylbenzylamine for the characterization of the amino acceptor specificity, we now report on a kinetic conductivity assay for investigating the amino donor specificity of a given ATA. The course of an ATA-catalyzed reaction can be followed conductometrically since the conducting substrates, a positively charged amine and a negatively charged keto acid, are converted to nonconducting products, a noncharged ketone and a zwitterionic amino acid. The decrease of conductivity for the investigated reaction systems were determined to be 33-52 μS mM-1. In contrast to other ATA-assays previously described, with this approach all transamination reactions between any amine and any keto add can be monitored without the need for an additional enzyme or staining solutions. The assay was used for the characterization of a ATA from Rhodobacter sphaeroides, and the data obtained were in excellent agreement with gas chromatography analysis.
Schaetzle, Sebastian,Hoehne, Matthias,Robins, Karen,Bornscheuer, Uwe T.
body text
p. 2082 - 2086
(2010/08/20)

Iridium-catalyzed X-H insertions of sulfoxonium ylides
Image Persented The unique reactivity of sulfoxonium ylides as a carbene source is described for a variety of X-H bond insertions, taking advantage of a simple, commercially available iridium catalyst. This method has applications in both intra- and intermolecular reactivity, including a practical ring-expansion strategy for lactams. The safety and stability of sulfoxonium ylides recommend them as preferable surrogates to traditional diazo ketones and esters.
Mangion, Ian K.,Nwamba, Ikenna K.,Shevlin, Michael,Huffman, Mark A.
supporting information; experimental part
p. 3566 - 3569
(2011/02/22)

DIPEPTIDYL PEPTIDASE-IV INHIBITING COMPOUNDS, METHODS OF PREPARING THE SAME, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AS ACTIVE AGENT
Disclosed herein are novel compounds of Formula (1) as defined in the specification having excellent inhibitory activity against dipeptidyl peptidase-IV (DPP-IV), methods of preparing the same and pharmaceutical compositions comprising the same as an active agent.
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Page/Page column 37

(2009/07/25)

Design and synthesis of Rho kinase inhibitors (II)
In a previous study, we identified several structurally unrelated scaffolds of the Rho kinase inhibitor using pharmacophore information obtained from the results of a high-throughput screening and structural information from a homology model of Rho kinase. 1H-Indazole is one of the candidate scaffolds on which a new series of potent Rho kinase inhibitors could be developed. In this study, the detailed structure-activity relationship of 1H-indazole analogues was studied. During this study, we found that the cell-free enzyme inhibitory potential of Rho kinase inhibitors having the 1H-indazole scaffold did not necessarily correlate with their inhibitory potential toward the chemotaxis of cultured cells. The choice of the linker substructure was shown to be an important factor for the 1H-indazole analogues to inhibit the chemotaxis of cells. Optimization of the 1H-indazole inhibitors with respect to the in vitro inhibition of monocyte chemotaxis induced by MCP-1 was carried out. The inhibitory potential was improved both in the cell-free enzyme assay and in the chemotaxis assay.
Iwakubo, Masayuki,Takami, Atsuya,Okada, Yuji,Kawata, Takehisa,Tagami, Yoshimichi,Ohashi, Hiroshi,Sato, Motoko,Sugiyama, Terumi,Fukushima, Kayoko,Iijima, Hiroshi
p. 350 - 364
(2008/02/04)

Design and synthesis of rho kinase inhibitors (III)
The structure-activity relationship of Rho kinase inhibitors bearing an isoquinoline scaffold was studied. N-(1-Benzyl-3-pyrrolidyl)-N-(5-isoquinolyl)amine analogues were optimized with respect to their inhibitory potencies for the enzyme and for chemotaxis. The potent analogues were further evaluated by an ex vivo test in which the selected compounds were orally administered to rats, and the Rho kinase inhibitory potency observed in the rat serum was evaluated 3 h after the administration. Compound 23g showed a high level of Rho kinase inhibitory activity in the rat serum and was stable in an in vitro metabolic test using a microsomal cytochrome preparation. The (R)-isomer of 23g displayed a higher level of inhibitory potency than the (S)-isomer in a cell-free kinase assay and in the cell migration assay (IC50ENZ = 25 nM and IC50MCP = 1 μ M). The (R)-isomer successfully inhibited the phosphorylation of MBS (myosin-binding subunit) in cells.
Iwakubo, Masayuki,Takami, Atsuya,Okada, Yuji,Kawata, Takehisa,Tagami, Yoshimichi,Sato, Motoko,Sugiyama, Terumi,Fukushima, Kayoko,Taya, Shinichiro,Amano, Mutsuki,Kaibuchi, Kozo,Iijima, Hiroshi
p. 1022 - 1033
(2007/10/03)

INHIBITORS OF PHOSPHODIESTERASE TYPE-IV
The present invention relates to isoxazoline derivatives, which can be used as selective inhibitors of phosphodiesterase (PDE) type IV. In particular, compounds disclosed herein can be useful in the treatment of AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease (COPD), psoriasis, allergic rhinitis, shock, atopic dermatitis, Crohn's disease, adult respiratory distress syndrome (ARDS), eosinophilic granuloma, allergic conjunctivitis, osteoarthritis, ulcerative colitis and other inflammatory diseases in a patient, particularly in humans. The present invention also relates to processes for the preparation of disclosed compounds, as well as pharmaceutical compositions thereof, and their use as phosphodiesterase (PDE) type IV inhibitors.
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Page/Page column 44

(2008/06/13)

ISOQUINOLINE DERIVATIVES HAVING KINASAE INHIBITORY ACTIVITY AND DRUGS CONTAINING THE SAME
An objective of the present invention is to provide compounds having Rho kinase inhibitory activity and useful for the treatment of diseases mediated by Rho kinase. The compounds according to the present invention are those represented by formula (I) or pharmaceutically acceptable salts or solvates thereof: wherein Q represents phenyl, pyridyl, pyrrolyl, thienyl, or furyl; these groups are optionally substituted by one or two halogens or alkyl, nitro, or amino groups; and p is 2 or 3.
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(2008/06/13)

Efficient preparation of (3S)-3-(4-fluorobenzyl)piperidinium mandelate
Methods for the preparation of (3S)-3-(4-fluorobenzyl)piperidine (2) and its mandelate salt (9) are described. The first generation synthesis started from 3-benzylpiperidone, and required Boc protection of the nitrogen for efficient separation of the enantiomers using chromatography on a chiral stationary phase. Subsequently, a resolution method using (R)-mandelic acid, produced high %ee salt 9 after recrystallization and eliminated the need for Boc protection. The third generation route, starting from pyridine-3- carboxaldehyde, led to a streamlined synthesis of racemate 2 and was optimized for producing multi-hundred gram quantities of the chiral salt.
Emmett, George C.,Cain, Gary A.,Estrella, Melissa J.,Holler, Edd R.,Piecara, James S.,Blum, Andrew M.,Mical, Alfred J.,Teleha, Christopher A.,Wacker, Dean A.
p. 92 - 96
(2007/10/03)

Discovery of CC chemokine receptor-3 (CCR3) antagonists with picomolar potency
Starting with our previously described20 class of CC chemokine receptor-3 (CCR3) antagonist, we improved the potency by replacing the phenyl linker of 1 with a cyclohexyl linker and by replacing the 4-benzylpiperidine with a 3-benzylpiperidine. The resulting compound, 32, is a potent and selective antagonist of CCR3. SAR studies showed that the 3-acetylphenyl urea of 32 could be replaced with heterocyclic ureas or heterocyclic-substituted phenyl ureas and still maintain the potency (inhibition of eotaxin-induced chemotaxis) of this class of compounds in the low-picomolar range (IC50 = 10-60 pM), representing some of the most potent CCR3 antagonists reported to date. The potency of 32 for mouse CCR3 (chemotaxis IC50 = 41 nM) and its oral bioavailability in mice (20% F) were adequate to assess the efficacy in animal models of allergic airway inflammation. Oral administration of 32 reduced eosinophil recruitment into the lungs in a dose-dependent manner in these animal models. On the basis of its overall potency, selectivity, efficacy, and safety profile, the benzenesulfonate salt of 32, designated DPC168, entered phase I clinical trials.
De Lucca, George V.,Ui, Tae Kim,Vargo, Brian J.,Duncia, John V.,Santella III, Joseph B.,Gardner, Daniel S.,Zheng, Changsheng,Liauw, Ann,Wang, Zhang,Emmett, George,Wacker, Dean A.,Welch, Patricia K.,Covington, Maryanne,Stowell, Nicole C.,Wadman, Eric A.,Das, Anuk M.,Davies, Paul,Yeleswaram, Swamy,Graden, Danielle M.,Solomon, Kimberly A.,Newton, Robert C.,Trainor, George L.,Decicco, Carl P.,Ko, Soo S.
p. 2194 - 2211
(2007/10/03)

Substituted fused bicyclic amines as modulators of chemokine receptor activity
The present application describes modulators of CCR3 of formula (Ia) and (Ib): or pharmaceutically acceptable salt forms thereof, wherein Z, R1, R2, R3, R4, R5, R5′, R6, a, b, c, d, and u are as defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using said modulators are disclosed.
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Page/Page column 23

(2010/02/13)

Design and synthesis of Rho kinase inhibitors (I)
Several structurally unrelated scaffolds of the Rho kinase inhibitor were designed using pharmacophore information obtained from the results of a high-throughput screening and structural information from a homology model of Rho kinase. A docking simulation using the ligand-binding pocket of the Rho kinase model helped to comprehensively understand and to predict the structure-activity relationship of the inhibitors. This understanding was useful for developing new Rho kinase inhibitors of higher potency and selectivity. We identified several potent platforms for developing the Rho kinase inhibitors, namely, pyridine, 1H-indazole, isoquinoline, and phthalimide.
Takami, Atsuya,Iwakubo, Masayuki,Okada, Yuji,Kawata, Takehisa,Odai, Hideharu,Takahashi, Nobuaki,Shindo, Kazutoshi,Kimura, Kaname,Tagami, Yoshimichi,Miyake, Mika,Fukushima, Kayoko,Inagaki, Masaki,Amano, Mutsuki,Kaibuchi, Kozo,Iijima, Hiroshi
p. 2115 - 2137
(2007/10/03)

Chemokine receptor binding heterocyclic compounds with enhanced efficacy
The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).
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(2008/06/13)

Acetamides and benzamides that are useful in treating sexual dysfunction
The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction.
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(2008/06/13)

Discovery of N-propylurea 3-benzylpiperidines as selective CC chemokine receptor-3 (CCR3) antagonists
The discovery of novel and selective small molecule antagonists of the CC Chemokine Receptor-3 (CCR3) is presented. Simple conversion from a 4- to 3-benzylpiperidine gave improved selectivity for CCR3 over the serotonin 5HT2A receptor. Chiral resolution and exploration of mono- and disubstitution of the N-propylurea resulted in several 3-benzylpiperidine N-propylureas with CCR3 binding IC50s under 5 nM. Data from in vitro calcium mobilization and chemotaxis assays for these compounds ranged from high picomolar to low nanomolar EC50s and correlated well with antagonist binding IC50s.
Varnes, Jeffrey G.,Gardner, Daniel S.,Santella III, Joseph B.,Duncia, John V.,Estrella, Melissa,Watson, Paul S.,Clark, Cheryl M.,Ko, Soo S.,Welch, Patricia,Covington, Maryanne,Stowell, Nicole,Wadman, Eric,Davies, Paul,Solomon, Kimberley,Newton, Robert C.,Trainor, George L.,Decicco, Carl P.,Wacker, Dean A.
p. 1645 - 1649
(2007/10/03)

N-ARYL-SUBSTITUTED CYCLIC AMINE DERIVATIVE AND MEDICINE CONTAINING THE SAME AS ACTIVE INGREDIENT
The present invention provides an excellent squalene synthase inhibitor. Specifically, it provides a compound (I) represented by the following formula, a salt thereof or a hydrate of them. Wherein R1 represents an optionally substituted vinyl group or an aromatic ring which may be substituted; ???n is an integer of 0 to 2; ???X, Y and Z are the same as or different from each other and each represents an optionally substituted carbon atom, or an optionally substituted nitrogen a tom, sulfuratomoroxygenatom, and Y optionally represents a single bond, and when Y represents the single bond, the ring to which X, Y and Z belong is a 5-membered ring; ???CyA represents a 5- to 14 membered non-aromatic cyclic amino groupornon-aromatic cyclic amidogroupwhichmaybe substituted, and the non-aromatic cyclic amino group or the non-aromatic cyclic amido group optionally having an oxygen atom or a sulfur atom; ???W represents a chain expressed by(1) optionally substituted -CH2-CH2-,(2) optionally substituted -CH=CH-,(3) -C≡C-,(4) an optionally substituted phenylene group,(5) a single bond,(6) -NH-CO-,(7) -CO-NH-,(8) -NH-CH2-,(9) -CH2-NH-,(10) -CH2-CO-,(11) -CO-CH2-,(12) -O-(CH2)m-,(13) -(CH2)m-O- (where m represents an integer of 0 to 5),(14) -O-CH2-CR2=,(15) -O-CH2-CHR2- (where R2 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom),(16) -NH-S(O)1-,(17) -S(O)1-NH-,(18) CH2-S(O)1-, or(19) -S(O)2-CH2- (where 1 represents 0, 1, or 2); and ???A represents a group having any of the following structural formulae: (wherein R3 and R4 represent independently a hydrogen atom or an optionally substituted C1-6 alkyl group, or combine through a carbon chain optionally containing a heteroatom to form a ring; ???R5 and R6 represent independently a hydrogen atom or an optionally substituted C1-6 alkyl group, or combine through a carbon chain optionally containing a heteroatom to form a ring; ???R7 represents a hydrogen atom, an optionally substituted C1-6 alkyl group, a hydroxyl group, an alkoxy group, a halogen atom or an optionally substituted amino group; ???R8 represents a hydrogen atom, a hydroxyl group, an alkoxy group, a halogen atom or an optionally substituted amino group; ???B1 represents an optionally substituted carbon atom, or an optionallysubstitutednitrogenatom, oxygen atom or sulfur atom; ???B2 represents an optionally substituted carbon atom or nitrogen atom; ???a and b represent an integer of 0 to 4, provided that a+b is an integer of 0 to 4; ???c represents 0 or 1; and----- represents a single bond or a double bond, provided that when c is 1 in which A is a quinuclidine having R8 represented by the case where R8 is a hydrogen atom or a hydroxyl group; Arl is an aromatic heterocycle; and W is one of (1) to (3), (6) to (11) and (16) to (19) are excluded).
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Page 42-43

(2010/02/05)

Acetamides and benzamides that are useful in treating sexual dysfunction
The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction.
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Page 123

(2008/06/13)

N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
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(2008/06/13)

N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
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(2008/06/13)

N-ureidoheterocycloalkyl-piperidines as modulators of chemokine receptor activity
The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
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(2008/06/13)

Sulfone derivatives, process for their production and use thereof
A compound represented by the formula: 1wherein R is a cyclic hydrocarbon group, or the like; W is a bond, or the like; X is a divalent hydrocarbon group, or the like; Y and Z are each independently —N(R6)— or the like; ring A is a nitrogen-containing heterocyclic ring, or the like; R5 and R6 are independently hydrogen atom, a hydrocarbon group, or the like; Z′ is imidoyl group, or the like; a is 0, 1 or 2; and b is 0 or 1, or a salt thereof.
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(2008/06/13)

Synthesis and pharmacological evaluation of 2-(3-piperidyl)-1,2,3,4-tetrahydroisoquinoline derivatives as specific bradycardic agents.
Novel 1,2,3,4-tetrahydroisoquinoline derivatives bearing directly a cyclic amine at the 2-position were prepared and examined for their bradycardic activities in isolated right atria and in anesthetized rats. The structure-activity relationships (SAR) study revealed that the 2-(3-piperidyl)-1,2,3,4-tetrahydroisoquinoline skeleton is essential for the appearance of potent in vitro activity, and that the presence of at least one methoxy group at the 6- or 7-position of the 1,2,3,4-tetrahydroisoquinoline ring is important to exert potent in vitro activity. In vivo tests of selected compounds demonstrated that 2-(1-benzyl-3-piperidyl)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline (6c) exhibited potent bradycardic activity with negligible influence on mean blood pressure in rats, although its potency is a half of that of Zatebradine.
Kakefuda, Akio,Watanabe, Toshihiro,Taguchi, Yasuko,Masuda, Noriyuki,Tanaka, Akihiro,Yanagisawa, Isao
p. 390 - 398
(2007/10/03)

Chemokine receptor binding heterocyclic compounds with enhanced efficacy
The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).
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Page/Page column 15-16

(2010/02/03)

(±)-2-(3-piperidyl)-1,2,3,4-tetrahydroisoquinolines as a new class of specific bradycardic agents
A series of (±)-2-(3-piperidyl)-1,2,3,4-tetrahydroisoquinolines were prepared and their bradycardic activities were examined in isolated guinea-pigs' right atria and in anesthetized rats. Modifications on the benzyl moiety of the parent compound, 1, led to the identification of compound 11e as a potent and specific bradycardic agent.
Kubota, Hideki,Kakefuda, Akio,Watanabe, Toshihiro,Taguchi, Yasuko,Ishii, Noe,Masuda, Noriyuki,Sakamoto, Shuichi,Tsukamoto, Shin-Ichi
p. 2155 - 2158
(2007/10/03)

CCR3 antagonists: a potential new therapy for the treatment of asthma. Discovery and structure-activity relationships.
CCR3 antagonist leads with IC(50) values in the microM range were converted into low nM binding compounds that displayed in vitro inhibition of human eosinophil chemotaxis induced by human eotaxin. In particular, 4-benzylpiperidin-1-yl-n-propylureas and erythro-3-(4-benzyl-2-(alpha-hydroxyalkyl)piperidin-1-yl)-n-propylureas (obtained via Beak reaction of N-BOC-4-benzylpiperidine) exhibited single digit nanomolar IC(50) values for CCR3.
Wacker, Dean A,Santella 3rd., Joseph B,Gardner, Daniel S,Varnes, Jeffrey G,Estrella, Melissa,DeLucca, George V,Ko, Soo S,Tanabe, Keiichi,Watson, Paul S,Welch, Patricia K,Covington, Maryanne,Stowell, Nicole C,Wadman, Eric A,Davies, Paul,Solomon, Kimberly A,Newton, Robert C,Trainor, George L,Friedman, Steven M,Decicco, Carl P,Duncia, John V
p. 1785 - 1789
(2007/10/03)

Beta-Amino-Acid derivatives as inhibitors of matrix metalloproteases and TNF-Alpha
The present application describes novel β-amino acid derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, X, Z, Ua, Xa, Ya, Za, R1, R2, R3, R4, and R4a are defined in the present specification, which are useful as metalloprotease and/or as TNF-α inhibitors.
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(2008/06/13)

Piperidine amides as modulators of chemo kine receptor activity
The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
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(2008/06/13)

N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
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(2008/06/13)

Thrombin receptor antagonists
A thrombin receptor antagonist having the formula or a pharmaceutically acceptable salt thereof, useful for inhibiting the aggregation of blood platelets. The compounds can be used in a method of acting upon a thrombin receptor which comprises administering a therapeutically effective but non-toxic amount of such compound to a mammal, preferably a human.
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(2008/06/13)

Discovery and initial structure-activity relationships of trisubstituted ureas as thrombin receptor (PAR-1) antagonists
Thrombin is the most potent agonist of platelet activation, and its effects are predominantly mediated by platelet thrombin receptors. Therefore, antagonists of the thrombin receptor have potential utility for the treatment of thrombotic disorders. Screening of combinatorial libraries revealed 2 to be a potent antagonist of the thrombin receptor. Modifications of this structure produced 11k, which inhibits thrombin receptor stimulated secretion and aggregation of platelets.
Barrow, James C,Nantermet, Philippe G,Selnick, Harold G,Glass, Kristen L,Ngo, Phung L,Young, Mary Beth,Pellicore, Janetta M,Breslin, Michael J,Hutchinson, John H,Freidinger, Roger M,Condra, Cindra,Karczewski, Jerzy,Bednar, Rodney A,Gaul, Stanley L,Stern, Andrew,Gould, Robert,Connolly, Thomas M
p. 2691 - 2696
(2007/10/03)

Assymetric synthesis of azepines
A novel process for the manufacture of compounds of the formula STR1 wherein R1 and R2 independently represent aroyl. The present invention also concerns novel intermediates used in the novel process for making compounds of formula I.
-
(2008/06/13)

Piperidinyl-3-phosphinic acids as novel uptake inhibitors of the neurotransmitter γ-aminobutyric acid (GABA)
Piperidinyl-3-phosphinic acid 2, piperidinyl-3-methylphosphinic acid 3 and N-(4,4-diphenyl-3-butenyl)-piperidinyl-3-phosphinic acid 4 have been synthesized as bioisosteres of the corresponding amino carboxylic acids, which are potent and specific GABA-uptake inhibitors. The novel amino phosphinic acids were tested for their GABA-uptake inhibitory activity and 2 and 4 were identified as the first phosphinic acid based GABA-uptake inhibitors. The methylphosphinic acid 3 was found to be inactive.
Kehler, Jan,Stensbol, Tine B.,Krogsgaard-Larsen, Povl
p. 811 - 814
(2007/10/03)

Preparation of 3-substituted piperidines which promote the release of human and animal growth hormone.
-
-
(2008/06/13)

Glycine Antagonists. Synthesis, Structure, and Biological Effects of Some Bicyclic 5-Isoxazolol Zwitterions
The bicyclic 5-isoxazolol zwitterions 4,5,6,7-tetrahydroisoxazolopyridin-3-ol (3, iso-THPO), 5,6,7,8-tetrahydro-4H-isoxazoloazepin-3-ol (12, iso-THAO), and 5,6,7,8-tetrahydro-4H-isoxazoloazepin-3-ol (13, iso-THIA), which are structurally related to the glycine antagonist 5,6,7,8-tetrahydro-4H-isoxazoloazepin-3-ol (iso-THAZ), have been synthesized and tested biologically.All of these compounds were glycine antagonists approximetely equipotent with iso-THAZ during microelectrophoretic ejection near cat spinal neurons.In contrast to iso-THAZ, which also interacts with 4-aminobutyric acid (GABA) receptors in rat brains, neither 12 or 13 show any significant affinities for GABA binding or uptake mechanisms in vitro.The glycine antagonist 3 was, however, shown also to be a moderately potent inhibitor of GABA uptake.The structure of 12 was established by an X-ray analysis.The bond lengths of the 5-isoxazolol anionic moiety of 12 are in agreement with a pronounced delocalization of the negative charge of this compound.
Brehm, Lotte,Krogsgaard-Larsen, Povl,Schaumburg, Kjeld,Johansen, Joergen S.,Falch, Erik,Curtis, David R.
p. 224 - 229
(2007/10/02)

Chemical Properties

Appearance/Colour :white to yellow low melting solid
Melting Point: 35-40 °C(lit.)
Boiling Point: 289.825 °C at 760 mmHg
Flash Point:129.082 °C
Density: 1.099 g/cm³
Storage Temp.:Store at?0-5°C
Vapor Pressure: 0.002mmHg at 25°C
Refractive Index: 1.481
PKA: -1.71±0.20(Predicted)
BRN: 5936353
PSA: 46.61000
LogP: 1.52430

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98977-36-7

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Chemical Properties

Appearance/Colour :white to yellow low melting solid

Melting Point: 35-40 °C(lit.)

Boiling Point: 289.825 °C at 760 mmHg

Flash Point:129.082 °C

Density: 1.099 g/cm³

Storage Temp.:Store at?0-5°C

Vapor Pressure: 0.002mmHg at 25°C

Refractive Index: 1.481

PKA: -1.71±0.20(Predicted)

BRN: 5936353

PSA: 46.61000

LogP: 1.52430

Global suppliers and manufacturers of 98977-36-7total 176 suppliers on LookChem

Article Database

98977-36-7

Articles about 98977-36-7Total 44 be found

More Articles about upstream products of 98977-36-7

More Articles about downstream products of 98977-36-7

Chemical Properties

Appearance/Colour :white to yellow low melting solid

Melting Point: 35-40 °C(lit.)

Boiling Point: 289.825 °C at 760 mmHg

Flash Point:129.082 °C

Density: 1.099 g/cm3

Storage Temp.:Store at?0-5°C

Vapor Pressure: 0.002mmHg at 25°C

Refractive Index: 1.481

PKA: -1.71±0.20(Predicted)

BRN: 5936353

PSA: 46.61000

LogP: 1.52430

Global suppliers and manufacturers of 98977-36-7total 176 suppliers on LookChem

Density: 1.099 g/cm³