cas 697739-03-0, 5-FLUORO-2-METHYL-3-NITRO-BENZOIC ACID METHYL ESTER

Articles about 697739-03-0Total 17 be found

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ANTI-CANCER NUCLEAR HORMONE RECEPTOR-TARGETING COMPOUNDS
The disclosure relates to anti-cancer compounds derived from nuclear steroid receptor binders, to products containing the same, as well as to methods of their use and preparation.
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Page/Page column 136

(2020/11/30)

Isoindoline compound, and preparation method, pharmaceutical composition and application thereof
The invention relates to a polysubstituted isoindoline compound represented by a general formula (I), and a preparation method, a pharmaceutical composition and an application thereof. Specifically, as a CRL4CRBNE3 ubiquitin ligase regulator with a novel structure, the polysubstituted isoindoline compound provided by the invention has stronger anti-tumor activity and an anti-tumor spectrum, and can be used for preparing medicines for treating diseases related to CRL4CRBNE3 ubiquitin ligase.
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Paragraph 0475; 1148-1150

(2020/04/17)

ETHER COMPOUNDS AND USES THEREOF
The present invention provides compounds that modulate protein function, to restore protein homeostasis and/or cell-cell adhesion. The invention provides methods of modulating protein-mediated diseases, such as cytokine-mediated diseases, disorders, conditions, or responses. Compositions of these compounds are also provided. Methods of treatment, amelioration, or prevention of protein-mediated diseases, disorders, and conditions are also provided.
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(2019/03/12)

METHOD FOR PREPARATION OF 5-FLUORO-2-METHYL-3-NITROBENZOIC ACID AND ITS METHYL ESTER
The invention discloses a method for preparation of 5-fluoro-2-methyl-3-nitrobenzoic acid and its methyl ester by conversion of 5-fluoro-2-methylbenzoic acid with fuming nitric acid and oleum and subsequent conversion with methanol.
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Page/Page column 9; 10

(2019/02/06)

Preparation method for 2-methyl-5-fluorobenzoic acid
The invention discloses a preparation method for 2-methyl-5-fluorobenzoic acid. The method comprises the steps of reacting 2-X-4-fluorotoluene with magnesium chips to form a Grignard reagent, and converting the obtained Grignard reagent to obtain the 2-methyl-5-fluorobenzoic acid, wherein X is selected from chloro, bromo or iodo.
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(2019/01/04)

Preparation method of ovarian cancer resistance medicine Rucaparib key intermediate
The invention discloses a preparation method of an ovarian cancer resistance medicine Rucaparib key intermediate, and relates to preparation of medical intermediates. A compound 1 takes methyl alcoholand cyclohexane as solvents, toluenesulfonic acid serve
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(2018/09/11)

Isoindoline derivative and intermediate, preparation method, pharmaceutical composition and application thereof
The invention discloses an isoindoline derivative, and an intermediate, a preparation method, a pharmaceutical composition and application thereof. The isoindoline derivative of the invention and the pharmaceutical composition thereof can adjust productio
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(2016/10/08)

Identification of novel PARP-1 inhibitors: Drug design, synthesis and biological evaluation
A series of AG014699 derivatives containing a novel scaffold of 2,3-dihydro-1H-[1,2]diazepino[4,5,6-cd]indole-1,4(6H)-dione were synthesized and evaluated for their inhibitory activities toward PARP-1 enzyme and two cell lines, MCF-7 cells and the BRCA1-deficient MDA-MB-436 cells. Our results demonstrated that of all AG014699 derivatives synthesized in this work, compounds 6 and 7 showed strong PARP-1 inhibitory activity (IC50 = 3.5 nM and 2.4 nM, respectively), only four and three times less potent than AG014699. Compound 6 also had significantly cell inhibitory activity against both MCF-7 cells (CC50 = 25.8 μM) and the BRCA1-deficient MDA-MB-436 cells (CC50 = 5.4 μM), nearly as good as AG014699, indicating that it can be a promising compound for further evaluation.
Xie, Zhouling,Zhou, Youli,Zhao, Wei,Jiao, He,Chen, Yu,Yang, Yong,Li, Zhiyu
supporting information
p. 4557 - 4561
(2015/10/12)

Multkilogram scale-up of a reductive alkylation route to a novel PARP inhibitor
Novel PARP inhibitor 1 is a promising new candidate for treatment of breast and ovarian cancer. A modified synthetic route to 1 has been developed and demonstrated on 7 kg scale. In order to scale up the synthesis to multikilogram scale, several synthetic challenges needed to be overcome. The key issues included significant thermal hazards present in a Leimgruber-Batcho indole synthesis, a low-yielding side-chain installation, a nonrobust Suzuki coupling and hydrogen cyanide generation during a reductive amination. In addition to these issues, changing from intravenous to oral delivery required a new salt form and therefore a new crystallization procedure. This contribution describes development work to solve these issues and scaling up of the new process in the pilot plant.
Gillmore, Adam T.,Badland, Matthew,Crook, Clare L.,Castro, Nieves M.,Critcher, Douglas J.,Fussell, Steven J.,Jones, Katherine J.,Jones, Matthew C.,Kougoulos, Eleftherios,Mathew, Jinu S.,McMillan, Lynne,Pearce, John E.,Rawlinson, Fiona L.,Sherlock, Alexandra E.,Walton, Robert
p. 1897 - 1904
(2013/03/13)

METHODS OF USING DIHYDROPYRIDOPHTHALAZINONE INHIBITORS OF POLY (ADP-RIBOSE)POLYMERASE (PARP)
Provided herein are methods of treating cancer comprising administering a topoisomerase inhibitor, temozolomide, or a platin in combination with a Compound of Formula (I) or Formula (II), where the substituents Y, Z, A, B, R1, R2, R3, R4 and R5 are as defined herein.
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Page/Page column 122

(2011/11/01)

DIHYDROPYRIDOPHTHALAZINONE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP)
A compound having the structure set forth in Formula (I) and Formula (II): wherein the substituents Y, Z, A, B, R1, R2, R3, R4 and R5 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.
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Page/Page column 65

(2010/03/02)

TRICYCLIC COMPOUND AND PHARMACEUTICAL USE THEREOF
The present invention provides a compound represented by the formula wherein R1 is a hydrocarbon group optionally having substituent(s), amino optionally having substituent(s), hydroxy optionally having a substituent or a heterocyclic group opt
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Page/Page column 61-62

(2009/09/26)

REARRANGED PENTANOLS, A METHOD FOR THE PRODUCTION THEREOF, AND THEIR USE AS ANTIPHLOGISTICS
The invention relates to compounds of formula (I), to a method for the production thereof, and to their use as antiphlogistics.
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Page/Page column 19

(2008/06/13)

1-AMINO-2-OXY-SUBSTITUTED TETRAHYDRONAPHTALENE DERIVATIVES, METHODS FOR THE PRODUCTION THEREOF, AND THEIR USE AS ANTIPHLOGISTICS
The invention relates to polysubstituted tetrahydronaphtalene derivatives of formula (I), to methods for the production thereof, and to their use as antiphlogistics. The substituents are defined in Claim 1.
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Page/Page column 65

(2010/02/11)

Rearranged pentanols, a process for their production and their use as anti-inflammatory agents
The invention relates to the compounds of formula I, a process for their production and their use as anti-inflammatory agents.
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Page/Page column 7

(2010/02/12)

HETEROAROMATIC UREAS WHICH MODULATE THE FUNCTION OF THE VANILLOID-1 RECEPTOR (VR1)
Compounds of formula (I): are useful as therapeutic compounds, particularly in the treatment of pain and other conditions ameliorated by the modulation of the function of the vanilloid-1 receptor (VR1).
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Page/Page column 29-30

(2010/02/11)

AMINO-HETEROCYCLES AS VR-1 ANTAGONISTS FOR TREATING PAIN
the present invention provides a compound of formula (I): wherein V represents NR5, O, S, SO or S(O)2; W and X each independently represent CH or N; Y represents N, CH or C-Ar2, with the proviso that at least one, but no more than two, of W, X and Y are N; Z represents CH or C-Ar2, with the proviso that when Y is N or CH then Z is C-Ar2, and with the further proviso that when Y is C-Ar2 then Z is CH; Ar1 represents a fused 9 or 10 membered heterobicyclic ring system containing one, two, three or four heteroatoms selected from nitrogen, oxygen and sulfur, wherein at least one of the rings in said ring system is aromatic; Ar2 represents an aromatic ring selected from phenyl, pyridyl, pyrimidinyl and pyridazinyl which is optionally fused and substituted; R1 represents halogen, hydroxy, oxo, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, haloC1-6alkyl, hydroxyC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy, hydroxyC1-6alkoxy, C3-7cycloalkyl, C3-7cycloalkoxy, C3-5cycloalkylC1-4alkyl, cyano, nitro, SR6, SOR6, SO2R6, COR6, NR3COR6, CONR3R4, NR3SO2R6, SO2NR3R4, -(CH2)mcarboxy, esterified -(CH2)mcarboxy or -(CH2)mNR3R4; R2 represents hydrogen, halogen, hydroxy, C1-6alkyl, haloC1-6alkyl, C3-7cycloalkyl, C1-6alkoxy, haloC1-6alkoxy, unsubstituted phenyl or phenyl substituted with one or two groups selected from halogen, C1-6alkyl, haloC1-6alkyl, C3-7cycloalkyl, C1-6alkoxy or haloC1-6alkoxy; R3 and R4 are each independently hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl or fluoroC1-6alkyl; or R3 and R4 and the nitrogen atom to which they are attached together form a heteroaliphatic ring of 4 to 7 ring atoms, optionally substituted by one or two groups selected from hydroxy or C1-4alkoxy, which ring may optionally contain as one of the said ring atoms an oxygen or a sulfur atom, S(O), S(O)2, or NR5; R5 represents hydrogen, C1-4alkyl, hydroxyC1-4alkyl or C1-4alkoxyC1-4alkyl; R6 represents hydrogen, C1-6alkyl, fluoroC1-6alkyl, C3-7cycloalkyl, unsubstituted phenyl, or phenyl substituted with one or two groups selected from halogen, C1-6alkyl, haloC1-6alkyl, C3-7cycloalkyl, C1-6alkoxy or haloC1-6alkoxy; m is either zero or an integer from 1 to 4; n is either zero or an integer from 1 to 3; or a pharmaceutically acceptable salt, N-oxide or a prodrug thereof; a pharmaceutical composition comprising it; its use in methods of treatment; use of it for the manufacture of a medicament for treating VR-1 related conditions such as those in which pain and/or inflammation predominate; and methods of treatment using it.
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Page 29

(2010/02/07)

Chemical Properties

Boiling Point: 297.7±40.0 °C(Predicted)
Density: 1.335±0.06 g/cm3(Predicted)
Solubility:Slightly soluble in water. Soluble in dimethyl sulfoxide and acetone.
Storage Temp.:Sealed in dry,Room Temperature
PSA: 72.12000
LogP: 2.35210

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Chemical Properties

Boiling Point: 297.7±40.0 °C(Predicted)

Density: 1.335±0.06 g/cm3(Predicted)

Solubility:Slightly soluble in water. Soluble in dimethyl sulfoxide and acetone.

Storage Temp.:Sealed in dry,Room Temperature

PSA: 72.12000

LogP: 2.35210

Global suppliers and manufacturers of 697739-03-0total 72 suppliers on LookChem