- HETEROCYCLIC COMPOUNDS AS INHIBITORS OF HPK1
-
This disclosure relates to heterocyclics as inhibitors of HPK1, in particular relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising said compound that useful for treatment of HPK1 mediated diseases and conditions such as cancer. (I)
- -
-
Page/Page column 199
(2021/01/29)
-
- NEW MACROCYCLIC LRRK2 KINASE INHIBITORS
-
Compounds of formula (I): wherein R, X1, X2, X3, Z1, Z2, Z3, A and Ra are as defined in the description. Medicaments.
- -
-
Page/Page column 258-259
(2021/11/13)
-
- Synthesis of All-Carbon Quaternary Centers by Palladium-Catalyzed Olefin Dicarbofunctionalization
-
The redox-neutral dicarbofunctionalization of tri- and tetrasubstituted olefins to form a variety of (hetero)cyclic compounds under photoinduced palladium catalysis is described. This cascade reaction process was used to couple styrenes or acryl amides with a broad range of highly decorated olefins tethered to aryl or alkyl bromides (>50 examples). This procedure enables one or two contiguous all-carbon quaternary centers to be formed in a single step. The products could be readily diversified and applied in the synthesis of a bioactive oxindole analogue.
- Koy, Maximilian,Bellotti, Peter,Katzenburg, Felix,Daniliuc, Constantin G.,Glorius, Frank
-
supporting information
p. 2375 - 2379
(2020/01/24)
-
- Visible-Light-Promoted Intramolecular α-Allylation of Aldehydes in the Absence of Sacrificial Hydrogen Acceptors
-
We report herein an unprecedented protocol for radical cyclization of aldehydes with pendant alkenes via synergistic photoredox, cobaloxime, and amine catalysis. The transformation was achieved in the absence of external oxidants, providing a variety of 5-, 6-, and 7-membered ring products with alkene transposition in satisfactory yields. The reaction exhibits wide functional group compatibility and occurs under mild conditions with extrusion of H2.
- Liu, Feng,Liu, Jia-Li,tu, Jia-Lin
-
supporting information
p. 7369 - 7372
(2020/10/05)
-
- ROR-GAMMA INHIBITORS
-
The present invention relates to compounds of formula I and pharmaceutical compositions comprising compounds of formula I. Compounds of Formula I are useful in treatment of inflammatory, metabolic or autoimmune diseases which are mediated by RORy.
- -
-
Page/Page column 245
(2019/04/26)
-
- Providing a New Aniline Bioisostere through the Photochemical Production of 1-Aminonorbornanes
-
Recent years have witnessed an increasing focus on saturated substructures within drug development as a result of the pharmacokinetic and toxicological benefits correlated with higher saturation content. However, the synthetic challenges presented by densely functionalized saturated architectures generally prohibit their evaluation. The abundance of anilines within high-throughput screening libraries is demonstrative of these competing needs. Anilines are prone to adverse metabolic processing, commonly necessitating re-engineering of a given drug lead to ameliorate CYP450 inhibition and/or glutathione adduction issues, but the ease with which these systems are prepared outweighs the toxicity risks. This article contributes to the need for aniline bioisosteres through the development of a robust, photochemical methodology that supplies 1-aminonorbornanes, saturated bicyclic ring systems that offer similar spatial occupancy to anilines while improving metabolic stability. The chemistry provided herein details an efficient and flexible route toward architecturally distinctive 1-aminonorbornanes through the use of visible-light photoredox catalysis. The incorporation of readily diversifiable functional handles (e.g., -OH, -CO2Me, -NHBoc, -NHCbz) illustrates the potential utility of these 1-aminonorbornanes within drug-discovery programs. Additionally, these motifs offer improved metabolic stability relative to that of their aniline congeners (as demonstrated through microsomal stability assays and metabolite identification efforts), indicating applicability of 1-aminonorbornanes as aniline bioisosteres. This report describes the photochemical conversion of aminocyclopropanes into 1-aminonorbornanes via formal [3 + 2] cycloadditions initiated by homolytic fragmentation of amine radical cation intermediates. Aligning with the modern movement toward sp3-rich motifs in drug discovery, this strategy provides access to a diverse array of substitution patterns on this saturated carbocyclic framework while offering the robust functional-group tolerance (e.g., -OH, -NHBoc) necessary for further derivatization. Evaluating the metabolic stability of selected morpholine-based 1-aminonorbornanes demonstrated a low propensity for oxidative processing and no proclivity toward reactive metabolite formation, suggesting a potential bioisosteric role for 1-aminonorbornanes. Continuous-flow processing allowed for efficient operation on the gram scale, providing promise for translation to industrially relevant scales. This methodology only requires low loadings of a commercially available, visible-light-active photocatalyst and a simple salt; thus, it stays true to sustainability goals while readily delivering saturated building blocks that can reduce metabolic susceptibility within drug development programs.
- Staveness, Daryl,Sodano, Taylor M.,Li, Kangjun,Burnham, Elizabeth A.,Jackson, Klarissa D.,Stephenson, Corey R.J.
-
supporting information
p. 215 - 226
(2019/01/21)
-
- Macrocyclic MCL-1 inhibitors and methods of use
-
The present disclosure provides for compounds of Formula (I) wherein A2, A3, A4, A6, A7, A8, A15, RA, R5, R9, R10A, R10B, R11, R12, R13, R14, R16, W, X, and Y have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents for the treatment of diseases and conditions, including cancer. Also provided are pharmaceutical compositions comprising compounds of Formula (I).
- -
-
Paragraph 0977
(2019/02/28)
-
- Multicatalytic Stereoselective Synthesis of Highly Substituted Alkenes by Sequential Isomerization/Cross-Coupling Reactions
-
Starting from readily available alkenyl methyl ethers, the stereoselective preparation of highly substituted alkenes by two complementary multicatalytic sequential isomerization/cross-coupling sequences is described. Both elementary steps of these sequences are challenging processes when considered independently. A cationic iridium catalyst was identified for the stereoselective isomerization of allyl methyl ethers and was found to be compatible with a nickel catalyst for the subsequent cross-coupling of the in situ generated methyl vinyl ethers with various Grignard reagents. The method is compatible with sensitive functional groups and a multitude of olefinic substitution patterns to deliver products with high control of the newly generated C=C bond. A highly enantioselective variant of this [Ir/Ni] sequence has been established using a chiral iridium precatalyst. A complementary [Pd/Ni] catalytic sequence has been optimized for alkenyl methyl ethers with a remote C=C bond. The final alkenes were isolated with a lower level of stereocontrol. Upon proper choice of the Grignard reagent, we demonstrated that C(sp2) - C(sp2) and C(sp2) - C(sp3) bonds can be constructed with both systems delivering products that would be difficult to access by conventional methods.
- Romano, Ciro,Mazet, Clément
-
supporting information
p. 4743 - 4750
(2018/04/10)
-
- Copper-Catalyzed Enantio-, Diastereo-, and Regioselective [2,3]-Rearrangements of Iodonium Ylides
-
The first highly enantioselective, diastereoselective, and regioselective [2,3]-rearrangement of iodonium ylides has been developed as a general solution to catalytic onium ylide rearrangements. In the presence of a chiral copper catalyst, substituted allylic iodides couple with α-diazoesters to generate metal-coordinated iodonium ylides, which undergo [2,3]-rearrangements with high selectivities (up to >95:5 r.r., up to >95:5 d.r., and up to 97 % ee). The enantioenriched iodoester products can be converted stereospecifically into a variety of onium ylide rearrangement products, as well as compounds that are not accessible by classical onium ylide rearrangements.
- Xu, Bin,Tambar, Uttam K.
-
supporting information
p. 9868 - 9871
(2017/08/08)
-
- DIHYDROPYRROLOPYRIDINE INHIBITORS OF ROR-GAMMA
-
Provided are novel compounds of Formula (I): pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders mediated by RORy. Also provided are pharmaceutical compositions co
- -
-
Paragraph 00104
(2016/05/24)
-
- Dihydropyrrolopyridine inhibitors of ROR-gamma
-
Provided are novel compounds of Formula (I): pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders mediated by RORγ. Also provided are pharmaceutical compositions co
- -
-
Page/Page column 31; 32
(2016/11/21)
-
- The synthesis of α,α-disubstituted α-amino acids via ichikawa rearrangement
-
An approach to α,α-disubstituted α-amino acids is reported. The key step is allyl cyanate-to-isocyanate rearrangement. As demonstrated, the resultant allyl isocyanates can be directly trapped with various nucleophiles, for instance, alcohols, amines, and organometallic reagents, to provide a broad range of N-functionalized allylamines. The developed method has been successfully applied in the synthesis of two bioactive peptides: 2-aminoadamantane-2-carboxylic acid derived P2X7-evoked glutamate release inhibitor and 4-amino-tetrahydropyranyl-4-carboxylic acid derived dipeptide GSK-2793660, which is currently in clinical trials as cathepsin C inhibitor for the treatment of cystic fibrosis, noncystic fibrosis bronchiectasis, ANCA-associated vasculitis and bronchiectasis.
- Szczes?niak, Piotr,Pieczykolan, Micha?,Stecko, Sebastian
-
p. 1057 - 1074
(2016/02/19)
-
- ARGININE METHYLTRANSFERASE INHIBITORS AND USES THEREOF
-
Described herein are compounds of Formula (S-I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.
- -
-
Paragraph 00483
(2016/04/20)
-
- SUBSTITUTED PYRIMIDINE COMPOUNDS, COMPOSITIONS AND MEDICINAL APPLICATIONS THEREOF
-
The present disclosure relates to pyrimidine compounds of formula (I), their stereoisomers, tautomers, pharmaceutically acceptable salts, polymorphs, solvates, and hydrates thereof. The present disclosure also relates to process of preparation of these pyrimidine compounds, and to pharmaceutical compositions containing them. The compounds of the present disclosure are useful in the treatment, prevention or suppression of diseases and disorders mediated by epidermal growth factor receptor (EGFR) family kinases.
- -
-
Paragraph 000143
(2015/03/13)
-
- Hepatitis C Virus Inhibitors
-
The present disclosure is generally directed to antiviral compounds, and more specifically directed to combinations of compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such combinations, and methods for inhibiting the function of the NS5A protein.
- -
-
Paragraph 1903-1904
(2015/02/25)
-
- COMBINATIONS OF HEPATITIS C VIRUS INHIBITORS
-
The present disclosure is generally directed to antiviral compounds, and more specifically directed to combinations of compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such combinations, and methods for inhibiting the function of the NS5A protein.
- -
-
Page/Page column 624
(2015/02/02)
-
- USE OF CONDENSED BENZO[B]THIAZINE DERIVATIVES AS CYTOPROTECTANTS
-
The present invention relates to arylthiazine compounds, metabolites, N-oxides, amides, esters,pharmaceutically acceptable salts, hydrates and solvates thereof and their use as cytoprotectants in the treatment or prophylaxis of diseases or states, either acute or chronic, involving aberrant cellular lipid peroxidation in the central nervous system or in the periphery of the body. The present invention also relates to a method for their preparation and to pharmaceutical composition comprising as an active ingredient one or more of the aforementioned compounds.
- -
-
Page/Page column 57
(2014/12/12)
-
- NDM INHIBITOR
-
An objective of the present invention is to provide a novel NDM (New Delhi metallo-β-lactamase) inhibitor that functions as a drug for restoring the antibacterial activity of β-lactam antibiotics that have been inactivated as a result of decomposition by NDM. According to the present invention, there is provided an NDM inhibitor contains a compound represented by general formula (I):
- -
-
Paragraph 0114-0116
(2014/06/24)
-
- Novel spiroketal pyrrolidine GSK2336805 potently inhibits key hepatitis C virus genotype 1b mutants: From lead to clinical compound
-
Rapid clinical progress of hepatitis C virus (HCV) replication inhibitors, including these selecting for resistance in the NS5A region (NS5A inhibitors), promises to revolutionize HCV treatment. Herein, we describe our explorations of diverse spiropyrrolidine motifs in novel NS5A inhibitors and a proposed interaction model. We discovered that the 1,4-dioxa-7-azaspiro[4.4]nonane motif in inhibitor 41H (GSK2236805) supported high potency against genotypes 1a and 1b as well as in genotype 1b L31V and Y93H mutants. Consistent with this, 41H potently suppressed HCV RNA in the 20-day RNA reduction assay. Pharmacokinetic and safety data supported further progression of 41H to the clinic.
- Kazmierski, Wieslaw M.,Maynard, Andrew,Duan, Maosheng,Baskaran, Sam,Botyanszki, Janos,Crosby, Renae,Dickerson, Scott,Tallant, Matthew,Grimes, Rick,Hamatake, Robert,Leivers, Martin,Roberts, Christopher D.,Walker, Jill
-
p. 2058 - 2073
(2014/04/03)
-
- AMIDO SPIROCYCLIC AMIDE AND SULFONAMIDE DERIVATIVES
-
Provided are amido spirocyclic amide and sulfonamide compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
- -
-
Page/Page column 181
(2013/09/12)
-
- EP1 RECEPTOR LIGANDS
-
The present invention belongs to the field of EP1 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP1 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP1 receptor as well as to pharmaceutical compositions comprising them.
- -
-
Page/Page column 75
(2013/03/28)
-
- A newly-designed PE-supported arsine for efficient and practical catalytic Wittig olefination
-
A newly designed PE-supported arsine has been developed as an excellent catalyst for catalytic Wittig-type olefination. Simple ketones, in particular inactive ketones prove to be suitable substrates for the first time. This reaction provides an easy access to di-, tri-, and tetra-substituted olefins in high yield.
- Wang, Peng,Liu, Chun-Rong,Sun, Xiu-Li,Chen, Shuai-Shuai,Li, Jun-Fang,Xie, Zuowei,Tang, Yong
-
supporting information; experimental part
p. 290 - 292
(2012/01/06)
-
- IMIDAZOPYRIDIN-2-ONE DERIVATIVES
-
A compound represented by formula (I) having mTOR inhibitory activity or a pharmacologically acceptable salt thereof.
- -
-
Page/Page column 38
(2011/04/24)
-
- AZAINDOLE GLUCOKINASE ACTIVATORS
-
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.
- -
-
Page/Page column 54
(2011/06/26)
-
- INHIBITORS OF SERINE PROTEASES FOR THE TREATMENT OF HCV INFECTIONS
-
The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt thereof. These compounds inhibit serine protease, particularly the hepatitis C virus NS3-NS4A protease.
- -
-
Page/Page column 471
(2008/12/07)
-
- INHIBITORS OF SERINE PROTEASES
-
The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt or mixtures thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease.
- -
-
Page/Page column 301-302
(2010/11/26)
-
- 3-CYCLOALKYLCARBONYL INDOLES AS CANNABINOID RECEPTOR LIGANDS
-
The present invention provides novel compounds of Formula (I), which are CB2 selective ligands useful for the treatment of pain.
- -
-
Page/Page column 115
(2008/06/13)
-
- Synthesis of bicyclic tertiary α-amino acids
-
Novel bicyclic α-amino acids, exo and endo-1-azabicyclo-[2.2.1] heptane-2-carboxylic acid, 1-azabicyclo[2.2.1]heptane-7-carboxylic acid, and 1-azabicyclo[3.2.2]nonane-2-carboxylic acid have been readily synthesized for the generation of neuronal nicotinic receptor ligands. Alkylation of glycine-derived Schiff bases or nitroacetates with cyclic ether electrophiles, followed by acid-induced ring opening and cyclization in NH4OH, allowed for the preparation of substantial quantities of the three tertiary bicyclic α-amino acids.
- Strachan, Jon-Paul,Whitaker, Regina C.,Miller, Craig H.,Bhatti, Balwinder S.
-
p. 9909 - 9911
(2007/10/03)
-
- New high affinity H3 receptor agonists without a basic side chain
-
In this study, we replaced the basic amine function of the known histamine H3 receptor agonists imbutamine or immepip with non-basic alcohol or hydrocarbon moieties. All compounds in this study show a moderate to high affinity for the cloned human H3 receptor and, unexpectedly, almost all of them act as potent agonists. Moreover, in the alcohol series, we consistently observed an increased selectivity for the human H3 receptor over the human H4 receptor, but none of the compounds in this series possess increased affinity and functional activity compared to their alkylamine congeners. In this new series of compounds VUF5657, 5-(1H-imidazol-4-yl)-pentan-1-ol, is the most potent histamine H3 receptor agonist (pKi = 8.0 and pEC50 = 8.1) with a 320-fold selectivity at the human H3 receptor over the human H 4 receptor.
- Kitbunnadaj, Ruengwit,Hoffmann, Marcel,Fratantoni, Silvina A.,Bongers, Gerold,Bakker, Remko A.,Wieland, Kerstin,El Jilali, Ahmed,De Esch, Iwan J. P.,Menge, Wiro M. P. B.,Timmerman, Henk,Leurs, Rob
-
p. 6309 - 6323
(2007/10/03)
-
- Discovery and preclinical profile of saxagliptin (BMS-477118): A highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
-
Efforts to further elucidate structure-activity relationships (SAR) within our previously disclosed series of β-quaternary amino acid linked L-cis-4,5-methanoprolinenitrile dipeptidyl peptidase IV (DPP-IV) inhibitors led to the investigation of vinyl substitution at the β-position of α-cycloalkyl-substituted glycines. Despite poor systemic exposure, vinyl-substituted compounds showed extended duration of action in acute rat ex vivo plasma DPP-IV inhibition models. Oxygenated putative metabolites were prepared and were shown to exhibit the potency and extended duration of action of their precursors in efficacy models measuring glucose clearance in Zuckerfa/fa rats. Extension of this approach to adamantylglycine- derived inhibitors led to the discovery of highly potent inhibitors, including hydroxyadamantyl compound BMS-477118 (saxagliptin), a highly efficacious, stable, and long-acting DPP-IV inhibitor, which is currently undergoing clinical trials for treatment of type 2 diabetes.
- Augeri, David J.,Robl, Jeffrey A.,Betebenner, David A.,Magnin, David R.,Khanna, Ashish,Robertson, James G.,Wang, Aiying,Simpkins, Ligaya M.,Taunk, Prakash,Huang, Qi,Han, Song-Ping,Abboa-Offei, Benoni,Cap, Michael,Xin, Li,Tao, Li,Tozzo, Effie,Welzel, Gustav E.,Egan, Donald M.,Marcinkeviciene, Jovita,Chang, Shu Y.,Biller, Scott A.,Kirby, Mark S.,Parker, Rex A.,Hamann, Lawrence G.
-
p. 5025 - 5037
(2007/10/03)
-
- NOVEL 4-(2FUROYL)AMINOPIPERIDINES, INTERMEDIATES IN SYNTHESIZING THE SAME,PROCESS FOR PRODUCING THE SAME AND MEDICINAL USE OF THE SAME
-
There are provided novel 4-(2-furoyl)aminopiperidines represented by the general formula (I), their synthetic intermediates, processes for their preparation and medicaments containing them. In the above formula, X is CH or N, and Y is a group of the following general formula (II), formula (II-a) or formula (III): wherein a, b and c are each an integer of 0-6; Z is CH2 or NH; W is O or S; T is O or N-R15 wherein R15 is H, a C1-C6 alkyl group, a benzyl group or a phenethyl group; and R1 is H, a C1-C6 alkoxycarbonyl group, a benzyloxycarbonyl group, or the like.The 4-(2-furoyl) aminopiperidine derivatives according to this invention possess opioid μ antagonistic activity and are useful for the treatment or prevention of side effects which are caused by μ receptors agonist and which are selected from constipation, nausea/emesis or itch, or for the treatment or prevention of idiopathic constipation, postoperative ileus, paralytic ileus, irritable bowel syndrome or chronic pruritus.
- -
-
-
- BENZO(5,6)CYCLOHEPTA(1,2-B)PYRIDINE DERIVATIVES USEFUL FOR INHIBITION OF FARNESYL PROTEIN TRANSFERASE
-
Novel compounds of formula (1.0) are disclosed. In Formula (1.0) a represents N or NO, R and R are halo, R and R are independently H or halo provided that at least one is H, X is C, CH or N, and T represents a five or six membered heterocycloalkyl ring having one or two heteroatoms selected from S or O. Also disclosed are methods of inhibiting farnesyl protein transferase and methods for treating tumor cells.
- -
-
-
- Pharmaceutical compositions and methods for effecting dopamine release
-
Patients susceptible to or suffering from disorders, such as central nervous system disorders, which are characterized by an alteration in normal neurotransmitter release, such as dopamine release (e.g., Parkinsonism, Parkinson's Disease, Tourette's Syndrome, attention deficient disorder, or schizophrenia), are treated by administering a 1-aza-2-(3-pyridyl)bicyclo[2.2.1]heptane, a 1-aza-2-(3-pyridyl)bicyclo[2.2.2]octane, a 1-aza-2-(3-pyridyl)bicyclo[3.2.1]octane, a 1-aza-2-(3-pyridyl)bicyclo[3.2.2]nonane, a 1-aza-7-(3-pyridyl) bicyclo[2.2.1]heptane, a 1-aza-3-(3-pyridyl)bicyclo[3.2.2]nonane, or a 1-aza-7-(3-pyridyl)bicyclo[3.2.2]nonane. The compounds can exist as individual stereoisomers, racemic mixtures, diastereomers and the like.
- -
-
-
- Synthesis and structure-activity relationships of 4-alkynyloxy phenyl sulfanyl, sulfinyl, and sulfonyl alkyl hydroxamates as tumor necrosis factor-α converting enzyme and matrix metalloproteinase inhibitors
-
A series of 4-alkynyloxy phenyl sulfanyl, sulfinyl and sulfony alkyl and piperidine-4-carboxylic acid hydroxamides were synthesized. Their structure-activity relationships, against tumor necrosis factor-α (TACE) and matrix metalloproteinase (MMP) inhibito
- Venkatesan, Aranapakam M.,Davis, Jamie M.,Grosu, George T.,Baker, Jannie,Zask, Arie,Levin, Jeremy I.,Ellingboe, John,Skotnicki, Jerauld S.,DiJoseph, John F.,Sung, Amy,Jin, Guixian,Xu, Weixin,McCarthy, Diane Joseph,Barone, Dauphine
-
p. 6255 - 6269
(2007/10/03)
-
- BENZIMIDAZOLE DERIVATIVES
-
This invention relates to the compounds represented by a general formula [I]: ???[in which A1 and A2 represent optionally fluorine-substituted methine or the like; B represents halogen, cyano, lower alkyl or the like; D represents optionally substituted heterocyclic group or the like; and G represents C3-C20 aliphatic group such as alicyclic group]. These compounds inhibit nociceptin activities due to their high affinity to nociceptin receptor, and are useful as analgesic, antiobestic, corebral function improver, drugs for treatment of alzheimer's disease and dementia, remedies for schizophrenia and neurodegenerative diseases, antidepressant, remedies for diabetes insipidus, polyuria, hypotension and so on.
- -
-
-
- Alkynyl containing hydroxamic acid compounds as matrix metalloproteinase and tace inhibitors
-
Compounds of the formula are useful in treating disease conditions mediated by TNF-α, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.
- -
-
Page column 66
(2008/06/13)
-
- REVERSE HYDROXAMATE INHIBITORS OF MATRIX METALLOPROTEINASES
-
Compounds having the formula are matrix metalloproteinase inhibitors. Also disclosed are matrix metalloproteinase-inhibiting compositions and methods of inhibiting matrix metalloproteinase in a mammal.
- -
-
-
- Tetrahydropyran Esters as New Attractants for Cockroaches
-
Twenty four tetrahydropyran esters were synthesised and tested as attractants toward Blattella germanica and Supella longipalpa in the laboratory by using the choice-chamber method.In general, carboxylates were superior to propionates and acetates.Among the 2-, 3-, or 4-substituted esters, substitution at the 4-position was better than at the other two positions.These results are explained in terms of the receptor model proposed earlier by others.
- Pandey, Karuna Shanker,Shriprakash,Rao, Karumuru Mallikarjuna,Vaidyanathaswamy, Ramamoorthy
-
p. 647 - 651
(2007/10/02)
-
- Potent HIV Protease Inhibitors: The Development of Tetrahydrofuranylglycines as Novel P2 Ligands and Pyrazine Amides as P3-Ligands
-
A series of protease inhibitors bearing constrained unnaturel amino acids at the P2-position and novel heterocycles at the P3-position of compound 1 (Ro 31-8959) were synthesized, and their in vitro enzyme inhibitory and antiviral ac
- Ghosh, Arun K.,Thompson, Wayne J.,Holloway, M. Katharine,McKee, Sean P.,Duong, Tien T.,et al.
-
p. 2300 - 2310
(2007/10/02)
-