- Preparation method of Wittig-Horner reagent
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A preparation method of a Wittig-Horner reagent is disclosed. According to the preparation method of the Wittig-Horner reagent provided by the invention, a compound with a structure as shown in a formula (I) and a glyoxylic acid aqueous solution with a sp
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Paragraph 0030-0034
(2021/07/31)
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- Total Synthesis and Structure-Activity Relationships Study of Odilorhabdins, a New Class of Peptides Showing Potent Antibacterial Activity
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The spread of antibiotic-resistant pathogens is a growing concern, and new families of antibacterials are desperately needed. Odilorhabdins are a new class of antibacterial compounds that bind to the bacterial ribosome and kill bacteria through inhibition
- Sarciaux, Matthieu,Pantel, Lucile,Midrier, Camille,Serri, Marine,Gerber, Cristelle,Marcia De Figueiredo, Renata,Campagne, Jean-Marc,Villain-Guillot, Philippe,Gualtieri, Maxime,Racine, Emilie
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p. 7814 - 7826
(2018/09/06)
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- NOVEL PEPTIDE DERIVATIVES AND USES THEREOF
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The invention provides for novel peptide derivatives and compositions comprising the same. The invention further provides methods of treatment comprising administering novel peptide derivatives and/or compositions comprising the same.
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Paragraph 00174
(2016/04/20)
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- NOVEL HETEROARYL AND HETEROCYCLE COMPOUNDS, COMPOSITIONS AND METHODS
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The invention relates to novel heteroaryl and heterocycle compounds of formula I and pharmaceutical compositions comprising them, uses and methods thereof for inhibiting the activity of PI3K and for treating inflammatory and autoimmune diseases and cancer.
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Paragraph 229
(2016/08/23)
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- NOVEL HETEROARYL AND HETEROCYCLE COMPOUNDS, COMPOSITIONS AND METHODS
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Provided are novel heteroaryl and heterocycle compounds of formula (I-1), (I-2) or (I-3) and pharmaceutical compositions comprising them, uses and methods thereof for inhibiting the activity of PI3K and for treating inflammatory and autoimmune disorders diseases and cancer.
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Page/Page column 137
(2014/02/16)
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- NOVEL HETEROARYL AND HETEROCYCLE COMPOUNDS, COMPOSITIONS AND METHODS
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The invention relates to novel heteroaryl and heterocycle compounds and pharmaceutical compositions comprising them, uses and methods thereof for inhibiting the activity of PI3k and for treating inflammatory and autoimmune disorders diseases and cancer.
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Page/Page column 109
(2014/02/16)
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- NOVEL HETEROARYL AND HETEROCYCLE COMPOUNDS, COMPOSITION AND METHODS THEREOF
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Disclosed are novel heteroaryl and heterocycle compounds of formula I-1, I-2 or I-3 and pharmaceutical compositions comprising them, uses and methods thereof for inhibiting the activity of PI3K and for treating inflammatory and autoimmune diseases and cancer.
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Page/Page column 136
(2014/02/16)
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- BARETTIN AND DERIVATIVES THEREOF FOR MEDICAL USE, IN PARTICULAR FOR THE TREATMENT OF DISEASES RELATED TO OXIDATIVE STRESS OR INFLAMMATION, AND FOR PRESERVING OR WASHING ORGANS
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The present invention relates to compounds of formula(I) herein, which includes barettin and derivatives thereof, or any pharmaceutically acceptable salt thereof for use as a medicament. Further the present invention relates to same compounds for use in t
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Page/Page column 22
(2014/10/18)
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- SUBSTITUTED HETEROCYCLIC ACETAMIDES AS KAPPA OPIOID RECEPTOR (KOR) AGONISTS
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The present invention relates to a series of substituted compounds having the general formula (I), including their ste reoisomers and/or their pharmaceutically acceptable salts, wherein R1, R2, R3. R4, R5, and R6 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (κ) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.
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Page/Page column 108; 109
(2013/09/26)
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- Synthesis, anticonvulsant activity, and neuropathic pain-attenuating activity of N-benzyl 2-amino-2-(hetero)aromatic acetamides
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N-Benzyl 2-acetamido-2-substituted acetamides, where the 2-substituent is a (hetero)aromatic moiety, are potent anticonvulsants. We report the synthesis and whole animal pharmacological evaluation of 16 analogues where the terminal 2-acetyl group was removed to give the corresponding primary amino acid derivatives (PAADs). Conversion to the PAAD structure led to a substantial drop in seizure protection in animal tests, demonstrating the importance of the N-acetyl moiety for anticonvulsant activity. However, several of the PAADs displayed notable pain-attenuating activities in a mouse model.
- Baruah, Pranjal K.,Dinsmore, Jason,King, Amber M.,Salomé, Christophe,De Ryck, Marc,Kaminski, Rafal,Provins, Laurent,Kohn, Harold
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supporting information; experimental part
p. 3551 - 3564
(2012/07/28)
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- Scalable synthesis of the desoxy-biphenomycin B core
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We describe the evolution of a kilogram-scale synthesis of the protected cyclic tripeptide desoxy-biphenomycin B, based on an early discovery route. The retrosynthetic concept included a macrolactamization strategy to build the core ring system of biphenomycin B in combination with a double catalytic asymmetric hydrogenation protocol for the construction of the ansa-tripeptide precursor. Eventually, the kilogram process comprised a 16-step sequence with an overall yield for the longest linear sequence of 19.5%.
- Berwe, Mathias,Joentgen, Winfried,Krueger, Jochen,Cancho-Grande, Yolanda,Lampe, Thomas,Michels, Martin,Paulsen, Holger,Raddatz, Siegfried,Weigand, Stefan
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experimental part
p. 1348 - 1357
(2012/01/12)
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- Merging the structural motifs of functionalized amino acids and α-Aminoamides: Compounds with Significant Anticonvulsant Activities
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Functional amino acids (FAAs) and α-aminoamides (AAAs) are two classes of antiepileptic drugs (AEDs) that exhibit pronounced anticonvulsant activities. We combined key structural pharmacophores present in FAAs and AAAs to generate a new series of compounds and document that select compounds exhibit activity superior to either the prototypical FAA (lacosamide) or the prototypical AAA (safinamide) in the maximal electroshock (MES) seizure model in rats. A representative compound, (R)-N-4′-((3′′-fluoro) benzyloxy)benzyl 2-acetamido-3-methoxypropionamide ((R)-10), was tested in the MES (mice, ip), MES (rat, po), psychomotor 6 Hz (32 mA) (mice, ip), and hippocampal kindled (rat, ip) seizure tests providing excellent protection with ED50 values of 13, 14, ~10 mg/kg, and 12 mg/kg, respectively. In the rat sciatic nerve ligation model (ip), (R)-10 (12 mg/kg) provided an 11.2-fold attenuation of mechanical allodynia. In the mouse biphasic formalin pain model (ip), (R)-10 (15 mg/kg) reduced pain responses in the acute and the chronic inflammatory phases.
- Salomé, Christophe,Salomé-Grosjean, Elise,Stables, James P.,Kohn, Harold
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supporting information; experimental part
p. 3756 - 3771
(2010/07/16)
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- Efficient total synthesis of (-)-kaitocephalin
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A highly dlastereoselectlve total synthesis of (-)-kaltocephalln, a novel antagonist of lonotroplc glutamate receptors, was accomplished In 12 steps starting from 5-substltuted proline ester via the aldol reaction with OBO-serlne aldehyde, (E)-selectlve α,β-dehydroamlno acid synthesis using a new HWE reagent, and catalytic hydrogenation.
- Hamada, Makoto,Shinada, Tetsuro,Ohfune, Yasufumi
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supporting information; experimental part
p. 4664 - 4667
(2009/12/24)
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- Stereocontrolled total synthesis of (-)-kaitocephalin
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(Chemical Equation Presented) This paper describes the successful implementation of a stereocontrolled strategy for the total chemical synthesis of the pyrrolidine-based alkaloid (-)-kaitocephalin. This scalable synthetic route profits from the strategic
- Vaswani, Rishi G.,Chamberlin, A. Richard
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p. 1661 - 1681
(2008/09/18)
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- A facile synthesis of α-amino-DOTA as a versatile molecular imaging probe
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An amino group has been introduced into one ligand of DOTA that can couple to peptidyl carboxylates by coupling α-brominated glycine to DO3A-tBu (1,4,7,10-tetraazacyclododecane-1,4,7-tris(acetic acid, tert-butylester)). α-Amino-DOTA was coupled
- Yoo, Byunghee,Pagel, Mark D.
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p. 7327 - 7330
(2007/10/03)
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- C-linked galactosyl serine AFGP analogues as potent recrystallization inhibitors
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(Chemical Equation Presented) A series of C-linked antifreeze glycoprotein analogues have been prepared to evaluate antifreeze activity as a function of distance between the carbohydrate moiety and polypeptide backbone. The building blocks for these analogues were prepared using either an olefin cross-metathesis or catalytic asymmetric hydrogenation. Analysis of antifreeze protein-specific activity revealed that only analogue 2a (n = 1) was a potent recrystallization inhibitor and thus has potential medical and industrial applications.
- Liu, Suhuai,Ben, Robert N.
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p. 2385 - 2388
(2007/10/03)
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- Identification of compounds that inhibit replication of human immunodeficiency virus
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The present invention relates to the discovery of a novel class of compounds that inhibit the replication of human immunodeficiency virus (HIV) and approaches to identify these compounds. More specifically, it has been found that enzymatically prepared al
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- COMPOUNDS HAVING BOTH α7 NICOTINIC AGONIST ACTIVITY AND 5HT3 ANTAGONIST ACTIVITY FOR TREATMENT OF CNS DISEASES
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The invention discloses compounds that are selective α7 nAChR agonists and 5-HT3 antagonists. The compounds are useful for treating many CNS diseases.
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- Quinuclidines-substituted-multi-cyclic-heteroaryls for the treatment of disease
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The invention provides compounds of Formula I: 1where in W is 2These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful to treat diseases or conditions in which α7 is known to be involved.
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- Substituted 7-aza[2.2.1]bicycloheptanes for the treatment of disease
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The invention provides compounds of Formula I: which may be in the form of pharmaceutical acceptable salts or compositions, are useful in treating diseases or conditions in which α7 nicotinic acetylcholine receptors (nAChRs) are known to be involved.
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- Interaction of VIVO, VVO2 and CuII with a peptide analogue SalGly-L-Ala
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The formation of complexes of a tripeptide analogue, salicylglycyl-L-alanine [HOC6H4C(O)NHCH2C(O)NHCH(CH3) -COOH, H2SalGly-L-Ala], was studied with CuII, VIVO and VVO2 in aqueous solution using pH-potentiometric and spectroscopic (UV/Vis, CD, EPR and 51V NMR) techniques. The results demonstrated the ambidentate character of the ligand. The metal ion-induced deprotonation and subsequent coordination of the two neighbouring amide groups was shown to occur in a cooperative way in the pH range 5-6. At pH ≈ 6.5 a complex with an (O-, 2 x CON-, COO-) binding set becomes predominant for both CuII, and VIVO. The affinity of the phenolate-O- for VIVO is high and the ligand is bound to this metal ion even at pH values greater than 10. Conversely, the affinity for VVO2 is significantly lower and no interaction between this metal oxo-ion and the ligand could be detected in the pH range 2-12. In contrast, with the dipeptide analogue H2SalGly, chelation involving the deprotonated amide-N-could be unambiguously detected. Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2003.
- Jakusch, Tamas,Doernyei, Agnes,Correia, Isabel,Rodrigues, Ligia M.,Toth, Gabor K.,Kiss, Tamas,Costa Pessoa, Joao,Marcao, Susana
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p. 2113 - 2122
(2007/10/03)
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- The synthesis and conformational aspects of a novel dioxopiperazine - A possible β-turn constraint
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The synthesis and conformational aspects of a dioxopiperazine was discussed. The cis configuration of the dioxopiperazine was rationalized using nuclear magnetic resonance (NMR) spectroscopy. Computational energy calculations were performed to explain the reluctance to cyclise of N-terminal partially protected dipeptides containing α, α-amino groups.
- Davies, John S.,Stelmach-Diddams, Malgosia,Fromentin, Regis,Howells, Alun,Cotton, Ron
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p. 239 - 243
(2007/10/03)
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- Peptidomimetic of helix-turn-helix or gamma-turn
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A peptidomimetic of the turn in the helix-turn-helix (HTH) motif of DNA-binding proteins was designed and synthesized. Conformational constraint was achieved by an unusual linking of two amino acids with a side-chain carbon--carbon bond. A phenyl ring pro
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- Phosphotyrosine peptidomimetics for inhibiting SH2 domain interactions
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The present invention makes available novel compounds represented by the general formula STR1 wherein Y represents a phosphate analog. Which compounds are useful for inhibiting an interaction between a protein containing an SH2 domain and a phophotyrosine
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- A convenient synthesis of 2-(diethoxyphosphonyl)glycine and its derivatives
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A simple and very efficient method for the preparation of 2-(diethoxyphosphonyl)glycine and its N-methyl analog as the free acids is described and their conversion to the corresponding t-butyl esters demonstrated.
- Shankar,Scott
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p. 231 - 234
(2007/10/02)
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- RENIN INHIBIOTRS
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Renin inhibiting compounds containing a single α-amino acid of the formula: STR1 and analogs thereof which inhibit the substrate-cleaving acting or renin, pharmaceutical compositions containing these compounds, processes for producing the compounds and methods of treating hypertension which employ the novel renin inhibitors.
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- General Synthesis of β,γ-Alkynylglycine Derivatives
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The coupling of α-haloglycinates 8 with alkynyltin reagents produces the fully protected β,γ-alkynylglycines 9.Subsequent deprotection of the amino or carboxyl groups generates differentially protected β,γ-alkynylglycine derivatives 10-14.The free amino a
- Williams, Robert M.,Aldous, David J.,Aldous, Suzanne C.
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p. 4657 - 4663
(2007/10/02)
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- N-phosphinyl di-and tripeptides as renin inhibitors.
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The invention concerns new renin inhibitor dipeptide and tripeptide derivatives of the formula:*(formula 01)* in which the meaning of all the symbols Rn and A is described in the text.
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