cas 16694-18-1, 2-Thiophenecarboxylicacid, 4-bromo-

Articles about 16694-18-1Total 21 be found

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COMPOSITIONS AND METHODS OF TARGETING MUTANT K-RAS
Compounds and compositions are presented that inhibit K-Ras, and especially mutant K-Ras. Certain compounds preferentially or even selectively inhibit specific forms of mutant K-Ras, and particularly the G12D mutant form.
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Paragraph 0397; 0398

(2018/08/03)

SUBSTITUTED (THIOPHENYL-CARBONYL)IMIDAZOLIDINONES, AND USE THEREOF
The present invention relates to novel substituted (thiophenyl-carbonyl)imidazolidinones, methods for their production, their use for the treatment and/or prevention of diseases, as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, especially retroviral diseases, in humans and/or animals.
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Page/Page column 12-13

(2012/02/03)

Direct bromination of ethyl 5-alkylthiophene-2-carboxylates
Approaches to brominated thiophene-2-carboxylic acids by electrophilic bromination of the corresponding acids and esters were compared and investigated. A synthetic route was developed involving direct bromination of ethyl 5-alkylthiophene-2-carboxylates followed by saponification of the resulting ethyl 5-alkyl-4-bromothiophene-2-carboxylates. The key bromination step is selective in dichloromethane solution at 0-5 °C and furnishes the corresponding ethyl 5-alkyl-4-bromothiophene-2-carboxylates in excellent yields. No migration or isomerization of the alkyl substituents was observed. Georg Thieme Verlag Stuttgart New York.
Taydakov, Ilya V.,Krasnoselskiy, Sergey S.
body text
p. 2965 - 2968
(2010/10/19)

AZAINDOLES USEFUL AS INHIBITORS OF ROCK AND OTHER PROTEIN KINASES
The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
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Page/Page column 183

(2008/06/13)

Structure-based design and synthesis of novel non-zinc chelating MMP-12 inhibitors
A new class of MMP-12 inhibitors was discovered and optimized using structure-based drug design methods. Modeling studies using a known MMP-12 crystal structure identified a new interaction mode for these new MMP-12 inhibitors. Further optimization resulted in the discovery of a compound displaying nanomolar activity against MMP-12 and which was co-crystallized with MMP-12.
Dublanchet, Anne-Claude,Ducrot, Pierre,Andrianjara, Charles,O'Gara, Margaret,Morales, Renaud,Compere, Delphine,Denis, Alexis,Blais, Stephane,Cluzeau, Philippe,Courte, Karine,Hamon, Jacques,Moreau, Francois,Prunet, Marie-Laure,Tertre, Anita
p. 3787 - 3790
(2007/10/03)

BIARYL LINKED HYDROXAMATES: PREPARATION AND PHARMACEUTICAL APPLICATIONS
The present invention relates to hydroxamate compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to biaryl containing compounds and methods for their preparation. These compounds may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with enzymes having histone deacetylase activities. Formula (I), where Z is a single bond or C1-C4 hydrocarbon, A is an aromatic ring, B is an aromatic ring.
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Page/Page column 77-78

(2010/02/11)

Novel thiophene amidines, compositions thereof, and methods of treating complement-mediated diseases and conditions
Disclosed is a method for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade, comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of Formula I or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R1, R2, R3, R4 and R7 are defined in the specification, Z is SO or SO2, and Ar is an aromatic or heteroaromatic group as defined herein.
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(2008/06/13)

Novel thiophene derivatives, their process of preparation and the pharmaceutical compositions which comprise them
A compound of formula (I) selected from: wherein: X represents oxygen or sulphur, Y represents oxygen, —NH— or —N(C1-C6)alkyl-, Ra represents hydrogen, halogen, (C1-C3)alkyl, hydroxyl or (C1-C3)alkoxy, Rb represents hydrogen, halogen or (C1-C3)alkyl, A represents phenyl, pyridyl, (C5-C6)cycloalkyl or (C5-C6)cycloalkenyl, R1 and R2 each represent a group selected from hydrogen, halogen, cyano, nitro, haloalkyl, haloalkoxy, alkyl, alkenyl, alkynyl, —OR4, —NR4R5, —S(O)nR4, —C(O)R4, —CO2R4, —O—C(O)R4, —C(O)NR4R5, —NR5—C(O)R4, —NR5—SO2R4, -T-CN, -T-OR4, -T-OCF3, -T- NR4R5, -T-S(O)nR4, -T-C(O)R4, -T-CO2R4, -T-O—C(O)R4, -T-C(O)NR4R5, -T-NR4—C(O)R5, -T-NR4—SO2R5, —R6 and -T-R6 in which n, T, R4, R5 and R6 are as defined in the description, R3 represents an —R7 or —U—R11 group in which R7 represents hydrogen, alkyl, aryl, cycloalkyl or heterocycle, U represents a linear or branched alkylene chain and R11 is defined in the description, their optical isomers or their addition salts with a pharmaceutically acceptable acid or base, and their use as inhibitor of metalloproteinase and more specifically of metalloproteinase-12.
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Page/Page column 15

(2010/11/30)

ISOQUINOLINONE DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS
This invention is directed to isoquinolinone derivatives and their use in modulating the activity of orphan nuclear receptors, pharmaceutical compositions containing such derivatives, and methods of using such derivatives in treating disease-states associ
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Page 82

(2010/02/07)

NOVEL THIOPHENE AMIDINES, COMPOSITIONS THEREOF, AND METHODS OF TREATING COMPLEMENT-MEDIATED DISEASES AND CONDITIONS
Disclosed is a method for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade, comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of Formula (I) or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R1, R2, R3, R4 and R7 are defined in the specification, Z is SO or SO2, and Ar is an aromatic or heteroaromatic group as defined herein.
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Page 150-151

(2010/02/05)

Compounds
Compounds of formula I: wherein A, D, Ar1, E and Ar2 are as defined in the specification, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, especially in the treatment or prophylaxis of psychotic and intellectual impairment disorders.
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(2008/06/13)

Compounds and compositons for treating C1s-mediated diseases and conditions
Disclosed is a method for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade, comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of Formula I or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R1, R2, R3, R4, X, Y and Z are defined in the specification.
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(2008/06/13)

Design and Synthesis of 4,5-disubstituted-thiophene-2-amidines as potent urokinase inhibitors
A study of the S1 binding of lead 5-methylthiothiophene amidine 3, an inhibitor of urokinase-type plasminogen activator, was undertaken by the introduction of a variety of substituents at the thiophene 5-position. The 5-alkyl substituted and unsubstituted thiophenes were prepared using organolithium chemistry. Heteroatom substituents were introduced at the 5-position using a novel displacement reaction of 5-methylsulfonylthiophenes and the corresponding oxygen or sulfur anions. Small alkyl group substitution at the 5-position provided inhibitors equipotent with 3 but possessing improved solubility.
Rudolph,Illig, Carl R.,Subasinghe, Nalin L.,Wilson, Kenneth J.,Hoffman, James B.,Randle, Troy,Green, David,Molloy, Chris J.,Soll, Richard M.,Lewandowski, Frank,Zhang, Marie,Bone, Roger,Spurlino, John C.,Deckman, Ingrid C.,Manthey, Carl,Sharp, Celia,Maguire, Diane,Grasberger, Bruce L.,DesJarlais, Renee L.,Zhou, Zhao
p. 491 - 495
(2007/10/03)

Heteroaryl amidines, methylamidines and guanidines, preparation thereof, and use thereof as protease inhibitors
The present invention is directed to compounds of Formula I: wherein X is O, S or NR7and R1-R7, Y and Z are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, plasmin and urokinase. Certain of the compounds exhibit direct, selective inhibition of urokinase, or are intermediates useful for forming compounds having such activity.
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(2008/06/13)

Synthesis and antitumour activity of new derivatives of flavone-8- acetic acid (FAA). Part 31): 2-Heteroaryl derivatives
A range of 14 derivatives of flavone-8-acetic acid (FAA) with a heterocyclic substituent in place of the 2-phenyl group have been prepared and their anti-tumour activity evaluated in vitro against a panel of human and murine tumour cell lines and in vivo against MAC 15A. Some of the compounds, notably 2c,d and s, showed significant in vivo activity and these require further studies in order to evaluate their potential for development.
Aitken, R. Alan,Bibby, Michael C.,Bielefeldt, Florian,Double, John A.,Laws, Andrea L.,Mathieu, Anne-Laure,Ritchie, Robert B.,Wilson, David W. J.
p. 405 - 411
(2007/10/03)

Phosphorylamides, their preparation and use
A phosphorylamide derivative represented by the general formula (I): STR1 wherein R represents an amino group that may be substituted, or a salt thereof, possesses potent antibacterial activity against Helicobacter bacterium, especially Helicobacter pylori, and is useful for prevention or treatment of digestive diseases caused by Helicobacter bacterium, solely or in combination with an antacid or an acid secretion inhibitor.
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(2008/06/13)

PHOTOSYNTHESIS OF HETEROPOLYCYCLIC QUINOLONES
Four new anilidoquinolones; 9-anilidobenzothienoquinolin-6(5H)-one (6), 9-N'-methylanilidobenzothieno-5-N-methylquinolin-6-one (7), 9-anilidothienothienylquinolin-6(5H)-one (16), and 9-N'-methylanilidothienothienyl-5-N-methylquinolin-6-one (17) were prepared by photochemical dehydrohalogenation from the dianilides (4,5,14 and 15).Photochemical dehydrogenation of the anilides to produce multicondensed diquinolones did not occur.
Dogan, Jasna,Karminski-Zamola, Grace M.,Boykin, David W.
p. 1659 - 1666
(2007/10/03)

H-D Exchange Reaction of 2-Thiophenecarboxylic Acids and Convenient Synthesis of Valeric Acid with Ni-Al Alloy in Alkaline Deuterium Oxide
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Tsuzuki, Hirohisa,Mukumoto, Mamoru,Mataka, Shuntaro,Yonemitsu, Tadashi,Tashiro, Masashi
p. 1046 - 1058
(2007/10/02)

Synthesis and Biological Activity of Acyclic Analogues of 5,10-Dideaza-5,6,7,8-tetrahydrofolic Acid
The synthesis and biological evaluation of a number of analogues of N-benzoyl>-L-glutamic acid (2) (7-DM-DDATHF), an acyclic modification of the novel folate antimetabolite 5,10-dideazatetrahydrofolic acid (DDATHF), are described.The synthetic procedure utilized previously for the synthesis of 2, 15, and 16 was extended to the preparation of analogues modified in the benzoyl region with thiophene and methylene groups replacing the benzene ring (compounds 27a-c) and in the glutamate region with aspartic acid and phenylalanine replacing L-glutamic acid (compounds 36, 37).The 2-amino-4,6-dioxo derivative 33 was obtained from intermediate 30 via a palladium-catalyzed carbon-carbon coupling reaction with diethyl (4-iodobenzoyl)-L-glutamate, followed by reduction and removal of protecting groups with base.Cell culture cytotoxicity studies of all of the above acyclic analogues of DDATHF against CCRF-CEM human lymphoblastic leukemic cells gave IC50s ranging from 0.042 to >48 μM.Inhibition and cell culture reversal studies against isolated enzymes suggest the mode of action of these compounds.Compound 2 was only 3-fold less inhibitory toward glycinamide ribonucleotide formyltransferase (GARFT, isolated from L1210 leukemic cells) than DDATHF itself.These acyclic analogues were less efficient substrates for the enzyme folylpolyglutamate synthetase (FPGS) compared with their bicyclic counterparts.Moderate antitumor activity was observed for compound 2 against 6C3HED lyphosarcoma and C3H mammary adenocarcinoma in vivo.
Shih, Chuan,Gossett, Lynn S.,Worzalla, John F.,Rinzel, Sharon M.,Grindey, Gerald B.,et al.
p. 1109 - 1116
(2007/10/02)

Synthesis and Tubulin Binding of 4'-(1-Azi-2,2,2-trifluoroethyl)oncodazole, a Photolabile Analogue of Oncodazole
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Ladd, David L.,Harrsch, Peter B.,Kruse, Lawrence I.
p. 417 - 420
(2007/10/02)

(N-1)-t-Butoxycarbonyl-geschuetzte 2-Thienylhydrazine; III. Der Einfluss der Methoxygruppe auf die Fischer-Reaktion
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Binder, Dieter,Prager, Bernhard C.,Noe, Christian R.
p. 1801 - 1824
(2007/10/02)

Chemical Properties

Appearance/Colour :white to light yellow crystal powder
Melting Point: 121 °C
Boiling Point: 323.742 °C at 760 mmHg
Flash Point:149.594 °C
Density: 1.924 g/cm³
Storage Temp.:under inert gas (nitrogen or Argon) at 2–8 °C
PKA: 3.50±0.10(Predicted)
PSA: 65.54000
LogP: 2.20880

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16694-18-1

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Chemical Properties

Appearance/Colour :white to light yellow crystal powder

Melting Point: 121 °C

Boiling Point: 323.742 °C at 760 mmHg

Flash Point:149.594 °C

Density: 1.924 g/cm³

Storage Temp.:under inert gas (nitrogen or Argon) at 2–8 °C

PKA: 3.50±0.10(Predicted)

PSA: 65.54000

LogP: 2.20880

Global suppliers and manufacturers of 16694-18-1total 71 suppliers on LookChem

Article Database

16694-18-1

Articles about 16694-18-1Total 21 be found

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Chemical Properties

Appearance/Colour :white to light yellow crystal powder

Melting Point: 121 °C

Boiling Point: 323.742 °C at 760 mmHg

Flash Point:149.594 °C

Density: 1.924 g/cm3

Storage Temp.:under inert gas (nitrogen or Argon) at 2–8 °C

PKA: 3.50±0.10(Predicted)

PSA: 65.54000

LogP: 2.20880

Global suppliers and manufacturers of 16694-18-1total 71 suppliers on LookChem

Density: 1.924 g/cm³