- C-glycosylation of cyclic N-acyliminium ions with trimethylsilyloxyfuran
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C-glycosylation of 2-methoxy-5-alkoxycarbonyl pyrrolidines with trimethylsilyloxyfuran allows us to obtain the corresponding pyrrolidines contigus to a α,β-unsaturated butyrolactone.
- Pichon, Marianne,Figadere, Bruno,Cave, Andre
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Read Online
- Stereoselective construction of a key hydroindole precursor of epidithiodiketopiperazine (ETP) natural products
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An asymmetric synthetic strategy for constructing the divergent-synthesis monomer of epidithiodiketopiperazine (ETP) natural products has been successfully developed. The functionalized 2,3,3a,4,7,7a-hexahydroindole scaffold was constructed by a diastereoselective inverse electron-demand Diels-Alder (IEDDA) reaction. This journal is the Partner Organisations 2014.
- Feng, Minghao,Jiang, Xuefeng
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Read Online
- INHIBITORS OF NOROVIRUS AND CORONAVIRUS REPLICATION
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Compounds of Formula (I) and methods of inhibiting the replication of viruses in a biological sample or patient, of reducing the amount of viruses in a biological sample or patient, and of treating a virus infection in a patient, comprising administering to said biological sample or patient an effective amount of a compound represented by Formula (I), a compound of Table A or B or a pharmaceutically acceptable salt thereof.
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Paragraph 00370-00372
(2021/10/15)
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- Preparation method of (s)-1-(t-butyloxycarboryl)-5-oxopyrrolidine-2-carboxylic acid ethyl ester
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The invention discloses a preparation method of (s)-1-(t-butyloxycarboryl)-5-oxopyrrolidine-2-carboxylic acid ethyl ester and aims at mainly solving the technical problems of complexity, long period,high cost, low yield and the like in the original technology. In the technical scheme of the invention, the preparation method comprises the following steps of step 1, preparation of boc-glu-oet: mixing h-glu-oet with a protective agent of boc- groups to prepare the boc-glu-oet, or mixing boc-glu-oh with ethyl acetate, performing reaction on a mixture under the action of diazoalkane, and performing treatment to obtain the boc-glu-oet; step 2, preparation of carboxyl active ester of the boc-glu-oet: mixing the boc-glu-oet with a carboxyl activating reagent, and performing low-temperature reaction on a mixture under the action of condensing agent to prepare a carboxyl activator of the boc-glu-oet; and sep 3, preparation of boc-pyr-oet: performing intramolecular cyclization on the carboxyl activator of the boc-glu-oet to prepare a crude product, and then performing extraction, purification and crystallization to obtain a target product. The preparation method provided by the invention greatly simplifies the process route, lowers the cost and is suitable for mass production.
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Paragraph 0013-0015
(2018/12/13)
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- Green preparation method of N-substituted-L-pyroglutamate
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The invention provides a green preparation method of N-substituted-L-pyroglutamate. The method comprises the steps as follows: L-glutamic acid diester hydrochloride (III) is prepared from L-glutamic acid (II) as a starting material in the presence of an acidic reagent by an esterification reaction; then, L-glutamic acid diester hydrochloride (III) is subjected to N-substituted protective reactionwith an N-substituent protective reagent with a one-pot method in the presence of a base and a solvent, an N-substituted protective group is introduced, heating is performed for dealcoholization cyclization in molecules, and N-substituted-L-pyroglutamate as shown in the formula (I) is obtained. The method has the advantages of cheap and easily available raw materials, classic reaction types, shortprocess route, simple and convenient operation, small waste water amount, green and environment-friendly production process, high reaction yield and low product cost. 5R-benzyloxyaminopiperidine-2S-carboxylate, 5R-benzyloxyaminopiperidine-2S-formate ethanedioate and avibactam can be prepared from N-substituted-L-pyroglutamate as shown in the formula (I).
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Paragraph 0060; 0061
(2018/03/28)
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- POLYMYXIN ANALOGS USEFUL AS ANTIBIOTIC POTENTIATORS
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The disclosure provides compounds of the formula (I) or a tautomer thereof, or a pharmaceutically acceptable salt of either of the foregoing. The variables A, R1, and R2 are defined in the disclosure. The disclosure further includes pharmaceutical compositions comprising a compound of formula I together with at least one pharmaceutically acceptable carrier. The disclosure also includes a method of sensitizing bacteria to an antibacterial agent, comprising administering to a patient infected with the bacteria, simultaneously or sequentially, a therapeutically effective amount of the antibacterial agent and a compound of formula (I).
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Paragraph 0171
(2017/12/09)
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- PROCESS FOR PREPARING DIPEPTIDYL PEPTIDASE IV INHIBITORS AND INTERMEDIATES THEREFOR
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A process for preparing an amine of the structure which comprises a. treating an aqueous solution of a keto acid of the structure with ammonium formate, nicotinamide adenine dinucleotide, dithiothreitol and partially purified phenylalanine dehydrogenase and/or formate dehydrogenase enzyme (PDH/FDH); and b. adjusting pH of the reaction mixture with sodium hydroxide to form the desired amine which is substantially free of undesirable excess ammonium ions.
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Paragraph 0041; 0111
(2016/07/27)
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- Proline compounds as Granzyme B inhibitors
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Proline compounds as Granzyme B inhibitors, compositions that include the compounds, and methods for using the compounds. Methods for treating cutaneous scleroderma, epidermolysis bullosa, radiation dermatitis, alopecia areata, and discoid lupus erythematosus are provided.
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Page/Page column 67
(2016/10/27)
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- Protected amino hydroxy adamantane carboxylic acid and process for its preparation
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Dipeptidyl peptidase IV (DP 4) inhibiting compounds are provided. The provided compounds can be used for treating diabetes and related diseases, especially Type II diabetes, and other diseases as set out herein, employing such DP 4 inhibitor or a combination of such DP 4 inhibitor and one or more of another antidiabetic agent such as metformin, glyburide, troglitazone, pioglitazone, rosiglitazone and/or insulin and/or one or more of a hypolipidemic agent and/or anti-obesity agent and/or other therapeutic agent.
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Paragraph 0138; 0139
(2015/11/24)
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- SPIRO COMPOUNDS AS HEPATITIS C VIRUS INHIBITORS
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Disclosed are spiro compounds of formula (I), or stereomers, geometric isomers, tautomers, nitrogen oxides, hydrates, solvates, metabolites, pharmaceutically acceptable salts or prodrugs thereof. The compounds can be used to treat hepatitis C virus (HCV) infection or hepatitis C disease. Furthermore disclosed are pharmaceutical compositions containing the compounds and the method of using the compounds or pharmaceutical compositions in the treatment of HCV infection or hepatitis C disease.
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Paragraph 0450
(2015/11/09)
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- Structural Properties and Stereochemically Distinct Folding Preferences of 4,5-cis and trans-Methano- L -Proline Oligomers: The Shortest Crystalline PPII-Type Helical Proline-Derived Tetramer
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The synthesis, structural properties, and folding patterns of a series of L-proline methanologues represented by cis- and trans-4,5-methano-L-proline amides and their oligomers are reported as revealed by X-ray crystallography, circular dichroism measurements, and DFT calculations. We disclose the first example of a crystalline tetrameric proline congener to exhibit a polyproline II helical conformation. Experimental evidence of PPII-type helical arrangement (both in solution and in the solid state) of cis-4,5-methano-L-proline oligomers is supported by theoretical calculations reflecting the extent of n→π? stabilization of the trans-amide conformation.
- Berger, Gilles,Vilchis-Reyes, Miguel,Hanessian, Stephen
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supporting information
p. 13268 - 13272
(2015/11/09)
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- CYCLIC AMINE DERIVATIVES AS EP4 RECEPTOR ANTAGONISTS
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There is described a novel group of cyclic amine derivative compounds, having an EP4 receptor antagonistic activity and specifically pharmaceutical compounds which are useful for the treatment or alleviation of Prostaglandin E mediated diseases. The present invention therefore relates to novel compounds which are selective antagonists of the EP4 subtype of PGE2 receptors with analgesic and antinflammatory activity, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments, inter alia for the treatment or alleviation of Prostaglandin E mediated diseases such as acute and chronic pain, osteoarthritis, inflammation-associated disorder as arthritis, rheumatoid arthritis, cancer, migraine and endometriosis.
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- Synthesis and biological evaluation of all eight stereoisomers of DPP-IV inhibitor saxagliptin
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All eight stereoisomers of saxagliptin have been synthesized and evaluated for their inhibitory activity against DPP-IV. It was unambiguously confirmed that the configuration of saxagliptin was critical to potent inhibition of DPP-IV. Docking study was performed to elucidate the configuration-activity relationship of saxagliptin stereoisomers. Tyr662 and Tyr470 have been suggested as the key residues of DPP-IV interacting with the inhibitors. This work provides valuable information for further inhibitor design against DPP-IV.
- Dong, Jizhe,Gong, Yanchun,Liu, Jun,Chen, Xiangfeng,Wen, Xiaoan,Sun, Hongbin
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p. 1383 - 1393
(2014/03/21)
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- CYCLIC AMINE DERIVATIVES AS EP4 RECEPTOR ANTAGONISTS
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There is described a novel group of cyclic amine derivative compounds, having an EP4 receptor antagonistic activity and specifically pharmaceutical compounds which are useful for the treatment or alleviation of Prostaglandin E mediated diseases. The present invention therefore relates to novel compounds which are selective antagonists of the EP 4 sub type of PGE2 receptors with analgesic and antinflammatory activity, processes for their preparation, pharmaceutical compositions containing them and theiruse as medicaments, inter alia for the treatment or alleviation of Prostaglandin E mediated diseases such as acute and chronic pain, osteoarthritis, inflammation-associated disorder as arthritis, rheumatoid arthritis, cancer, migraine and endometriosis.
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- Discovery of a novel class of potent and orally bioavailable sphingosine 1-phosphate receptor 1 antagonists
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A series of subtype selective sphingosine 1-phosphate receptor 1 (S1P 1) antagonists are disclosed. Our high-throughput screening campaign revealed hit 1 for which an increase in potency and mouse oral exposure was achieved with minor modifications to the chemical scaffold. In vivo efficacy revealed that at high doses compounds 12 and 15 inhibited tumor growth. Further optimization of our lead series led to the discovery of proline derivatives 37 (XL541) and 38 which had similar efficacy as our first generation analogues at significantly lower doses. Analogue 37 displayed excellent pharmacokinetics and oral exposure in multiple species.
- Ibrahim, Mohamed A.,Johnson, Henry W. B.,Jeong, Joon Won,Lewis, Gary L.,Shi, Xian,Noguchi, Robin T.,Williams, Matthew,Leahy, James W.,Nuss, John M.,Woolfrey, John,Banica, Monica,Bentzien, Frauke,Chou, Yu-Chien,Gibson, Anna,Heald, Nathan,Lamb, Peter,Mattheakis, Larry,Matthews, David,Shipway, Aaron,Wu, Xiang,Zhang, Wentao,Zhou, Sihong,Shankar, Geetha
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experimental part
p. 1368 - 1381
(2012/04/04)
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- STRUCTURAL MIMETICS OF PROLINE-RICH PEPTIDES AND THE PHARMACEUTICAL USE THEREOF
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The invention relates to compounds of general formula (I), which can be used particularly as structural mimetics of proline-rich peptides and are therefore capable of binding PRM binding domains (proline-rich motif binding domains) of proteins. The invention also relates to the use of said compounds as pharmaceutical active agents and the use of these pharmaceutical active agents for treating bacterial diseases, neurodegenerative diseases and tumours.
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Page/Page column 25-26
(2011/02/26)
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- Spirocyclic systems derived from pyroglutamic acid
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The synthesis and likely conformational structure of rigid spirocyclic bislactams and lactam-lactones derived from pyroglutamic acid, and their suitability as lead structures for applications in drug development programmes using cheminformatic analysis, has been investgated.
- Cowley, Andrew R.,Hill, Thomas J.,Kocis, Petr,Moloney, Mark G.,Stevenson, Robert D.,Thompson, Amber L.
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experimental part
p. 7042 - 7056
(2011/11/14)
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- PTERIDINONES AS INHIBITORS OF POLO - LIKE KINASE
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The present invention provides compounds having a structure according to Formula (I) or a salt or solvate thereof, wherein ring A, X, R1, R2, R3, R4, R5 and R6, are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.
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- Heterocyclic Compound
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The present invention provides a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof. The compound of the present invention shows a strong IAP antagonistic activity.
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Page/Page column 124
(2011/02/26)
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- Chemical reactivity of 6-diazo-5-oxo-l-norleucine (DON) catalyzed by metalloporphyrins (Fe,Ru)
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The transfer of the metallocarbene derived from N- and O-protected 6-diazo-5-oxo-l-norleucine (DON) catalyzed by metalloporphyrins undergoes dimerization, cyclopropanation, N-H and S-H insertion reactions, respectively. An efficient and direct synthesis of 5-oxo-l-pipecolic acid from DON is described from unprotected 6-diazo-5-oxo-l-norleucine.
- Le Maux, Paul,Nicolas, Irène,Chevance, Soizic,Simonneaux, Gérard
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experimental part
p. 4462 - 4468
(2010/07/06)
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- SPHINGOSINE-1-PHOSPHATE RECEPTOR ANTAGONISTS
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This disclosure relates to sphingosine-1 -phosphate (SlP) receptor antagonists, compositions comprising the SlP receptor antagonists and methods for using and processes for making the SlP receptor antagonists. In particularly, this disclosure relates to sphingosine-1 -phosphate 1 (SlPl) receptor antagonists, compositions comprising the SlPl receptor antagonist and methods for using the SlPl receptor antagonist, such as in the treatment of cancer, and processes for making the SlPl receptor antagonists.
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Page/Page column 87-88
(2010/04/30)
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- Prodrug of cinnamide compound
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The present invention provides a most suitable prodrug of a cinnamide compound. The prodrug is represented by Formula (I) wherein Ra and Rb each denote a C1-6 alkyl group or the like; Xa denotes a methoxy group or a fluorine atom; Y denotes a phosphono group or the like; and A denotes a cyclic lactam derivative.
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Page/Page column 70-71
(2009/03/07)
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- PYRROLOTRIAZINE KINASE INHIBITORS
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The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's Disease.
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Page/Page column 70-71
(2011/04/19)
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- 2-AZA-BICYCLO[3.1.0]HEXANE DERIVATIVES
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The invention relates to novel 2-aza-bicyclo[3.1.0]hexane derivatives of Formula (I) wherein A, B, n and R1 are as described in the description, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists.
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Page/Page column 84
(2008/12/07)
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- Pyrrolidinyl pyridone and pyrazinone analogues as potent inhibitors of prolyl oligopeptidase (POP)
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We report the synthesis and in vitro activity of a series of novel pyrrolidinyl pyridones and pyrazinones as potent inhibitors of prolyl oligopeptidase (POP). Within this series, compound 39 was co-crystallized within the catalytic site of a human chimeric POP protein which provided a more detailed understanding of how these inhibitors interacted with the key residues within the catalytic pocket.
- Haffner, Curt D.,Diaz, Caroline J.,Miller, Aaron B.,Reid, Robert A.,Madauss, Kevin P.,Hassell, Annie,Hanlon, Mary H.,Porter, David J.T.,Becherer, J. David,Carter, Luke H.
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scheme or table
p. 4360 - 4363
(2009/04/06)
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- (d)-2-tert-Butoxycarbonylamino-5,5-difluoro-5-phenyl-pentanoic acid: Synthesis and incorporation into the growth hormone secretagogues
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The first enantioselective synthesis of (d)-2-tert-butoxycarbonylamino-5,5-difluoro-5-phenyl-pentanoic acid 3 was achieved. The incorporation of the titled compound into growth hormone secretagogue (GHS) compounds resulted in new analogs 10 and 16, both o
- Li, Jun,Chen, Stephanie Y.,Murphy, Brian J.,Flynn, Neil,Seethala, Ramakrishna,Slusarchyk, Dorothy,Yan, Mujing,Sleph, Paul,Zhang, Hongjian,Humphreys, William G.,Ewing, William R.,Robl, Jeffrey A.,Gordon, David,Tino, Joseph A.
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scheme or table
p. 4072 - 4074
(2009/04/16)
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- TWO CYCLIC OXOMORPHORIN DERIVATIVES
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The present invention relates to a compound represented by formula (I): wherein R1 represents a C1-3 alkyl group, R2 represents a hydrogen atom or a C1-3 alkyl group, Ar represents a phenyl group or the like which may be substituted with 1 to 3 substituents, X represents an oxygen atom or the like, n and m are the same or different and integers of 0 to 2, or a pharmacologically acceptable salt, and use thereof as a medicament.
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Page/Page column 25
(2008/12/08)
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- THIOPHENE DERIVATIVES AS PPAR AGONISTS I
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The invention discloses compounds of formula (I); wherein: R is a carboxylic acid or a derivative thereof; R1 is alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, alkylthio, halo or trihalomethyl; R2 is aryl, heteroaryl, arylalkyl or heteroarylalkyl; R3 is H or F; and L is a linking group comprising a chain of from 2 to 8 atoms linking R and the carbonyl group (A); and pharmaceutically acceptable derivatives thereof, useful for treating disorders mediated by peroxisome-proliferator-activated receptor (PPAR) subtype δ (PPARδ). The compounds of the invention are therefore useful in the treatment of metabolic syndrome, obesity, type-II diabetes, dyslipidemia, wound healing, inflammation, neurodegenerative disorders and multiple sclerosis.
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Page/Page column 120
(2010/11/26)
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- Synthesis and uses of pyroglutamic acid derivatives
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Novel pyroglutamic acid derivatives (I), wherein R1 is -OH, -ORa, wherein Ra is alkyl, cycloalkyl, alkenyl, cycloalkenyl, aryl, aralkyl or heterocyclyl; R2, R3 and R4 are independently H, a nitrogen protecting group which hydrolyzes under acidic conditions or phtalamide; X is a pharmaceutically acceptable anion; and Y is a N-containing group; either in the form of their isolated optically active stereoisomers or in the form of mixtures thereof, are useful compounds for enhancing an immuneresponse in a subject and/or for treating tumours, bacterial, fungal or viral infections, or autoimmune diseases.
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Page/Page column 28
(2008/06/13)
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- PROLINAMIDE DERIVATIVES AS SODIUM CHANNEL MODULATORS
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The invention provides a compound of formula (I), a solvate, a salt or prodrug thereof, useful in the treatment of diseases and conditions mediated by modulation of use-dependent voltage-gated sodium channels.
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Page/Page column 35
(2008/06/13)
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- QUATERNARY ALPHA-AMINOCARBOXAMIDE DERIVATIVE AS MODULATORS OF VOLTAGE-GATED SODIUM CHANNELS
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The invention relates to quaternary E-aminocarboxyamide derivatives of formula (I), wherein R1, R2, R3, R4, R5, R6, X, q and n are as defined in claim 1, for treating diseases and conditions mediated by modulation of voltage-gated sodium channels.
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Page/Page column 69
(2010/11/27)
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- Trans-2,5-Disubstituted pyrrolidines: Rapid stereocontrolled access from sulfones
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A direct method for the reliable synthesis of trans-2,5-distributed pyrrolidines from pyroglutamic acid that was conducted at scale and without chromatographic purification of key intermediates was investigated. An analogous reaction involving the partial reduction of succinimides and displacement of the resulting lactol with benzenesulfinic acid yields sulfonyl pyrrolidinones. It was found that a highly diastereoselective and general approach to 2,5-difunctionalized pyrrolidines could be achieved by applying this strategy to the pyroglutamate system. The four step synthesis required no chromatographic purification of intermediates, where the product sulfone was readily purified by recrystallization and the sequence proceeded in 52% overall yield. The results show that such an approach would be of great importance for the preparation of substituted pyrrolidines in natural product systems.
- Moloney, Mark G.,Panchal, Terry,Pike, Richard
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p. 3894 - 3897
(2008/09/18)
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- DIPEPTIDYL PEPTIDASE-IV INHIBITORS
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The present invention relates generally to pyrrolidine and thiazolidine DPP-IV inhibitor compounds. The present invention also provides synthetic methods for preparation of such compounds, methods of inhibiting DPP-IV using such compounds and pharmaceutical formulations containing them for treatment of DPP-IV mediated diseases, in particular, Type-2 diabetes.
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Page/Page column 114
(2008/06/13)
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- Discovery, structure - Activity relationship, and pharmacological evaluation of (5-substituted-pyrrolidinyl-2-carbonyl)-2-cyanopyrrolidines as potent dipeptidyl peptidase IV inhibitors
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A series of (5-substituted pyrrolidinyl-2-carbonyl)-2-cyanopyrrolidine (C5-Pro-Pro) analogues was discovered as dipeptidyl peptidase IV (DPPIV) inhibitors as a potential treatment of diabetes and obesity. X-ray crystallography data show that these inhibitors bind to the catalytic site of DPPIV with the cyano group forming a covalent bond with the serine residue of DPPIV. The C5-substituents make various interactions with the enzyme and affect potency, chemical stability, selectivity, and PK properties of the inhibitors. Optimized analogues are extremely potent with subnanomolar Ki's, are chemically stable, show very little potency decrease in the presence of plasma, and exhibit more than 1,000-fold selectivity against related peptidases. The best compounds also possess good PK and are efficacious in lowering blood glucose in an oral glucose tolerance test in ZDF rats.
- Pei, Zhonghua,Li, Xiaofeng,Longenecker, Kenton,Von Geldern, Thomas W.,Wiedeman, Paul E.,Lubben, Thomas H.,Zinker, Bradley A.,Stewart, Kent,Ballaron, Stephen J.,Stashko, Michael A.,Mika, Amanda K.,Beno, David W. A.,Long, Michelle,Wells, Heidi,Kempf-Grote, Anita J.,Madar, David J.,McDermott, Todd S.,Bhagavatula, Lakshmi,Fickes, Michael G.,Pireh, Daisy,Solomon, Larry R.,Lake, Marc R.,Edalji, Rohinton,Fry, Elizabeth H.,Sham, Hing L.,Trevillyan, James M.
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p. 3520 - 3535
(2007/10/03)
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- Synthesis of macrocyclic analogues of the neuroprotective agent glycyl-l-prolyl-l-glutamic acid (GPE)
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The syntheses of seven macrocyclic analogues of the neuroprotective tripeptide glycyl-l-prolyl-l-glutamic acid (GPE) 1 are described. Macrocycles 6 and 7 mimic the cis conformer of GPE whereas macrocycles 2-5, 8, and 9 mimic the trans conformer of GPE. The macrocyclic peptides of well-defined geometry were prepared via Grubbs ring closing metathesis of an appropriate diene precursor. In turn each of the diene precursors were prepared from the readily available allyl-substituted amino acid building blocks 12, 13, 14, 27, 36 and 51. The Royal Society of Chemistry 2006.
- Harris, Paul W. R.,Brimble, Margaret A.
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p. 2696 - 2709
(2008/02/08)
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- PHARMACEUTICAL COMPOSITIONS AS INHIBITORS OF DIPEPTIDYL PEPTIDASE-IV (DPP-IV)
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The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.
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- A concise synthesis of (2S,4R)- and (2S,4S)-4-methylglutamic acid
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A concise, multi-gram scale method for producing the bioactive and enantiomerically pure epimers, (2S,4R)- and (2S,4S)-glutamic acids, in a single synthetic scheme is described.
- Gu, Zi-Qiang,Li, Min
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p. 3203 - 3205
(2007/10/03)
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- Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method
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Dipeptidyl peptidase IV (DP 4) inhibiting compounds are provided having the formula where x is 0 or 1 and y is 0 or 1 (provided that x=1 when y=0 and x=0 when y=1); n is 0 or 1; X is H or CN; and wherein R1, R2, R3 and R4 are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, and other diseases as set out herein, employing such DP 4 inhibitor or a combination of such DP 4 inhibitor and one or more of another antidiabetic agent such as metformin, glyburide, troglitazone, pioglitazone, rosiglitazone and/or insulin and/or one or more of a hypolipidemic agent and/or anti-obesity agent and/or other therapeutic agent.
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- 2,4-substituted pyrrolidine derivatives-CCR-3 receptor antagonists
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This invention relates to certain 2,4-substituted pyrrolidine derivatives that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.
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- Potent bicyclic lactam inhibitors of thrombin: Part I: P3 modifications
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Peptidomimetic inhibitors of general structure 1 have been prepared. Optimization of the binding affinities of these compounds through variation of the P3 hydrophobic residue is described. Selected substituted bicylic lactams displayed interesting pharmacological profiles both in vitro and in vivo.
- St-Denis, Yves,Augelli-Szafran, Corinne E.,Bachand, Benoit,Berryman, Kent A.,DiMaio, John,Doherty, Annette M.,Edmunds, Jeremy J.,Leblond, Lorraine,Levesque, Sophie,Narasimhan, Lakshmi S.,Penvose-Yi, Jan R.,Rubin, J. Ronald,Tarazi, Micheline,Winocour, Peter D.,Siddiqui, M. Arshad
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p. 3193 - 3198
(2007/10/03)
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