Day: November 3, 2022

On December 10, 2002, Munchhof, Michael John; Sobolov-Jaynes, Susan Beth; Marx, Matthew Arnold published a patent.Related Products of 52537-00-5 The title of the patent was Preparation of thienopyrimidines and thienopyridines as anticancer agents. And the patent contained the following:

The title compounds [I and II; X1 = CH; R1 = H, alkyl, C(O)alkyl; R2 = aryl, heterocyclic; R11 = H, alkyl, C(O)NR6R9, etc.; R6 = H, alkyl, etc.; R9 = H, alkyl, etc.] and analogs useful for treating hyperproliferative disorders, were prepared E.g., a multi-step synthesis of I [X1 = N; R1 = indol-5-yl; R2 = H; R11 = Br], was given. Compounds I are effective at 0.2-2.5 g/day for a 70 kg human. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Related Products of 52537-00-5

The Article related to anticancer agent thienopyrimidine thienopyridine preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Related Products of 52537-00-5

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On January 3, 2013, Suzuki, Masaki; Kondo, Kazumi; Kurimura, Muneaki; Valluru, Krishna Reddy; Takahashi, Akira; Kuroda, Takeshi; Takahashi, Haruka; Fukushima, Tae; Miyamura, Shin; Ghosh, Indranath; Dogra, Abhishek; Harriman, Geraldine; Elder, Amy; Shimizu, Satoshi; Hodgetts, Kevin J.; Newcom, Jason S. published a patent.Recommanded Product: 6-Chloro-2,3-dihydro-1H-indole The title of the patent was Quinazolines as STEP inhibitors and their preparation and use in the treatment of central nervous system agents. And the patent contained the following:

Methods of treating disorders using quinazoline compounds of formula I that modulate STriatal-enriched tyrosine phosphatase (STEP) are described herein. Compounds of formula I wherein m is 0 and 1; L is a bond and NH and derivatives; R1 is H, C1-8 alkyl, halo, C1-8 haloalkyl, etc.; R2 is C1-8 alkoxy, benzodioxolyl, piperazinyl, halo, etc.; R3 is pyridinyl, pyrimidinyl, pyrazinyl, etc.; R4 is H, C1-8 alkyl, C1-8 alkoxy, etc.; and salts thereof, are claimed. Example compound II•3HCl was prepared by amination of 4-bromo-6-methoxy-2-(pyridin-3-yl)quinazoline with 3-aminopyridine-2-carboxamide. All the invention compounds were evaluated for their STEP inhibitory activity (some data given). The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Recommanded Product: 6-Chloro-2,3-dihydro-1H-indole

The Article related to quinazoline preparation step inhibitor treatment cns disorder, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Recommanded Product: 6-Chloro-2,3-dihydro-1H-indole

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On August 14, 2014, Dai, Xing; Liu, Hong; Palani, Anandan; He, Shuwen; Lai, Zhong; Nargund, Ravi; Marcantonio, Karen; Xiao, Dong; Brockunier, Linda L.; Zorn, Nicolas; Dang, Qun; Peng, Xuanjia; Li, Peng published a patent.Electric Literature of 1256359-96-2 The title of the patent was Preparation of tetracyclic heterocycle compounds and methods of use thereof for the treatment of hepatitis C. And the patent contained the following:

The invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system. Compounds of formula I wherein A is C3-6 cycloalkyl, azetidin-1-ylcarbonyl and 5- to 6-membered aromatic ring system optionally containing heteroatoms; ring B is benzofuran, pyridinofuran pyrazolopyridine, etc.; Z1, Z2 and Z3 are independently CH and H, with the proviso that no more than one of Z1 – Z3 is N; Z4 is N, Z5 is CH and dashed bond to Z5 is double bond; Z4 is C, Z5 is NH and dashed bond is to Z5 is single bond; R2 is H, C1-6 alkyl, and C1-6 alkoxy; R3 is H and C1-6 alkyl; R4 is C1-6 alkyl and C1-6 alkoxy; R5 is H, C1-6 alkyl, CH2CO2H and derivatives, and SO2Me; R6 is H, C1-6 alkyl, C1-6 haloalkyl, etc.; R7 is H and C1-6 alkyl; R6R7 taken together to form C3-4 cycloalkyl; R8 is H, halo and CN; R9 and R10 are independently H and halo; dashed bond is single and double bond; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their anti-HCV activity. From the assay, it was determined that compound II exhibited IC50 values in the range of 4.006 nM to 6.558 nM. The experimental process involved the reaction of 4-Fluoro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole(cas: 1256359-96-2).Electric Literature of 1256359-96-2

The Article related to tetracyclic heterocycle preparation antiviral treatment hepatitis c, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Electric Literature of 1256359-96-2

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On August 14, 2014, Dai, Xing; Liu, Hong; Palani, Anandan; He, Shuwen; Lai, Zhong; Nargund, Ravi; Marcantonio, Karen; Xiao, Dong; Brockunier, Linda L.; Zorn, Nicolas; Dang, Qun; Peng, Xuanjia; Li, Peng published a patent.Application of 1256359-96-2 The title of the patent was Preparation of tetracyclic heterocycle compounds and methods of use thereof for the treatment of hepatitis C. And the patent contained the following:

The invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system. Compounds of formula I wherein A is C3-6 cycloalkyl, azetidin-1-ylcarbonyl and 5- to 6-membered aromatic ring system optionally containing heteroatoms; ring B is benzofuran, pyridinofuran pyrazolopyridine, etc.; Z1, Z2 and Z3 are independently CH and H, with the proviso that no more than one of Z1 – Z3 is N; Z4 is N, Z5 is CH and dashed bond to Z5 is double bond; Z4 is C, Z5 is NH and dashed bond is to Z5 is single bond; R2 is H, C1-6 alkyl, and C1-6 alkoxy; R3 is H and C1-6 alkyl; R4 is C1-6 alkyl and C1-6 alkoxy; R5 is H, C1-6 alkyl, CH2CO2H and derivatives, and SO2Me; R6 is H, C1-6 alkyl, C1-6 haloalkyl, etc.; R7 is H and C1-6 alkyl; R6R7 taken together to form C3-4 cycloalkyl; R8 is H, halo and CN; R9 and R10 are independently H and halo; dashed bond is single and double bond; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their anti-HCV activity. From the assay, it was determined that compound II exhibited IC50 values in the range of 4.006 nM to 6.558 nM. The experimental process involved the reaction of 4-Fluoro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole(cas: 1256359-96-2).Application of 1256359-96-2

The Article related to tetracyclic heterocycle preparation antiviral treatment hepatitis c, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application of 1256359-96-2

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On March 7, 2013, Courtney, Stephen Martin; Prime, Michael; Mitchell, William; Brown, Christopher John; De Aguiar Pena, Paula C.; Johnson, Peter; Dominguez, Celia; Toledo-Sherman, Leticia M.; Munoz, Ignacio published a patent.Computed Properties of 52537-00-5 The title of the patent was Preparation of phenylpyrimidine derivatives and analogs for use as kynurenine-3-monooxygenase inhibitors. And the patent contained the following:

Title compounds I [L = C(O), C(O)O, C(O)NR4, NR4S(O)2, etc.; X and Y independently = N or CH, provided at least one is N; R1 = (un)substituted aryl or heteroaryl; R2 = H or alkyl; R3 = H, OH, halo, alkyl, etc.; R4 and R5 taken together with the N atom to which they are attached to form an (un)substituted heterocycloalkyl, aryl, heteroaryl, etc.; with provisions], and their pharmaceutically acceptable salts, are prepared and disclosed as kynurenine-3-monooxygenase inhibitors. Thus, e.g., II was prepared by a multistep procedure (preparation given). Select I were evaluated as kynurenine-3-monooxygenase inhibitors (data given). The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Computed Properties of 52537-00-5

The Article related to pyrimidine derivative preparation kynurenine monooxygenase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Computed Properties of 52537-00-5

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On July 13, 2017, Song, Yuntao; Brdiges, Alexander James published a patent.SDS of cas: 860624-88-0 The title of the patent was Preparation of 2-anilino-4-heteroaryl pyrimidine compounds as selective EGFR tyrosine kinase inhibitors for treatment of cancer. And the patent contained the following:

The present invention provides compounds of formula I or a subgeneric structure or species thereof, or a pharmaceutically acceptable salt, ester, solvate, and/or prodrug thereof, and methods and compositions for treating or ameliorating abnormal cell proliferative disorders, such as cancer,. Compounds of formula I [wherein A is (un)substituted indol-1-yl, (un)substituted indol-3-yl, (un)substituted indazol-3-yl, etc.; R1 = H, F, Cl, OH, etc.; R2 = -OCF3, cyclopropyl, methoxy, etc.; R3 = C2-6 alkenyl-R7, C2-6alkynyl-R7, R7, etc; R7 = OH, C1-6alkoxy, oxetanyl, pyrrolidinyl, etc.; R10 = H, -CD3, C1-6alkyl, etc.; E1 and E2 independently = C-R1 or N with the proviso that E1 and E2 are not both N; E3 and Z are independently CH or N; Y = -C(O)-CHCH-aryl, -C(O)-CHCH-heteroaryl, -S(O)2-CHCH-aryl, etc.] or a stereoisomer or a pharmaceutically acceptable salt, solvate, ester, or prodrug thereof, are claimed and exemplified. Example compound II was prepared from a multistep procedure (preparation given). Candidate compounds of I were evaluated for inhibition of proliferation of PC-9 cells from which II demonstrated an IC50 value of 6.8 nM. The experimental process involved the reaction of Methyl 5-bromoindoline-7-carboxylate(cas: 860624-88-0).SDS of cas: 860624-88-0

The Article related to anilino heteroaryl pyrimidine compound preparation egfr kinase inhibitor cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.SDS of cas: 860624-88-0

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On November 10, 2016, Lan, Jiong; Zhou, Fusheng; Zhao, Jinzhu; Xu, Feng; Shi, Xia; Xie, Jing; Xu, Hui; Wang, Lixiao published a patent.Application In Synthesis of 6-Chloro-2,3-dihydro-1H-indole The title of the patent was Bicyclic substituted benzene sulfonamide derivatives as voltage-gated sodium channel inhibitors and their preparation, pharmaceutical compositions and use in the treatment of diseases. And the patent contained the following:

The invention relates to bicyclic substituted benzene sulfonamide derivatives of formula I, and the preparation method and pharmaceutical use as voltage-gated sodium channel inhibitors in the treatment of diseases thereof. In particular, disclosed in the present invention are the compounds of formula I or their pharmaceutically acceptable salts, stereoisomers, solvates or prodrugs thereof, and the preparation method and use thereof. Compounds of formula I wherein R1-R4 are independently H, OH, CN, NO2, halo, NH2 and derivatives, C1-20 alkyl, C3-20 cycloalkly, etc.; R5 is 5- to 6-membered heteroaryl, -CO-C1-20 alkyl, C3-20 cycloalkyl; L1 and L2 are independently a bond, -(CH2)1-3, etc.; dotted double bond is either a single bond or a double bond; X is a bond, NH and derivatives, O, S; Z1 is (un)substituted CH2, O, -CO-, (un)substituted -CH=, -N=, etc.; Z2 is -CO-, (un)substituted CH2, -NH- and derivatives, =N-, (un)substituted =CH-, O, etc.; Z3 is NH and derivatives, CH2, (un)substituted -CH=, etc.; Z4 is a bond, NH and derivatives, CH2, (un)substituted =CH-, =N-, etc.; ring A is (un)substituted 5- to 6-membered (hetero)aryl, etc.; and their pharmaceutically acceptable salts, stereoisomers, solvates or prodrugs as voltage-gated sodium channel inhibitors useful in the treatment of diseases thereof, are claimed. Compounds of formula I were prepared by using condensation as the key step. All the invention compounds were evaluated for their voltage-gated sodium channel inhibitory activity. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Application In Synthesis of 6-Chloro-2,3-dihydro-1H-indole

The Article related to benzenesulfonamide preparation voltage gated sodium channel inhibitor treatment disease, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application In Synthesis of 6-Chloro-2,3-dihydro-1H-indole

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On February 6, 2003, Toda, Narihiro; Ori, Mayuko; Takami, Kazuko; Tago, Keiko; Kogen, Hiroshi published an article.SDS of cas: 79815-20-6 The title of the article was Total Synthesis of (+)-Benzastatin E via Diastereoselective Grignard Addition to 2-Acylindoline. And the article contained the following:

A stereoselective total synthesis of (+)-benzastatin E is described. The synthesis involves a diastereoselective Grignard addition to 2-acylindoline I, which is derived from com. available (S)-2-indolinecarboxylic acid. The unknown absolute configuration of (+)-1 is determined as (9S,10R). The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).SDS of cas: 79815-20-6

The Article related to benzastatin e asym synthesis, grignard addition diastereoselective benzastatin e preparation, Biomolecules and Their Synthetic Analogs: Other Bacterial and Fungal Metabolites and other aspects.SDS of cas: 79815-20-6

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Wang, Pei-Long; Li, Yan; Ma, Lan; Luo, Chen-Guang; Wang, Zhen-Yu; Lan, Quan; Wang, Xi-Sheng published an article in 2016, the title of the article was Palladium-Catalyzed C-7 Selective C-H Carbonylation of Indolines for Expedient Synthesis of Pyrroloquinazolinediones.Application of 52537-00-5 And the article contains the following content:

A novel palladium-catalyzed C-7 selective C-H carbonylation of indolines with carbon monoxide for an expedient synthesis of pyrroloquinazolinediones, a structural motif with great potential in biol. active compounds, has been developed. Oxidation of the pyrroloquinazolinedione with 2,3-dichloro-5,6-dicyano-p-benzoquinone (DDQ) could easily afford the corresponding indole-based derivative in excellent yield. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Application of 52537-00-5

The Article related to pyrroloquinazolinedione preparation, carbon monoxide carbonylation indoline palladium catalyst, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application of 52537-00-5

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On January 7, 2021, Zhong, Wenge; Zhu, Xiaotian; Feng, Song; Wu, Lei; Huang, Wei; Liu, Hao; Liu, Rongqiang; Wen, Kate Xin; Zhou, Hua published a patent.Safety of 6-Chloro-2,3-dihydro-1H-indole The title of the patent was Preparation of substituted tetrahydroisoquinolinylaminopyridines and pyrrolopyridinylphenyldialkyl phosphine and their analogs as HPK1 inhibitors for treating cancers. And the patent contained the following:

The invention is related to the preparation of compounds I [X = CR2R3, NR3; A = CR2, N; R = 8-10 membered bicyclic N-containing heteroaryl or 8-10 membered bicyclic N-containing heterocyclyl optionally substituted with oxo, wherein the heteroaryl or heterocyclyl represented by R has 1 to 3 heteroatoms selected from N, O, and S, and is further optionally substituted, and wherein R is either connected with the pyrimidine ring via a nitrogen ring atom or R = (un)substituted quinolin-4-yl, indol-1-yl, isoquinolin-1-yl, etc.; R1 = H, D, halo,, OH, CN, NH2, NO2, etc.; or R and R1 together with the carbon atoms to which they are attached, form a ring selected from II, III, IV, etc.; Rb = independently at each occurrence H, D, COOH, etc.; Rc = independently Ph, 5-6 membered monocyclic heterocyclyl having 1-3 heteroatoms selected from N and O; 5-6 membered monocyclic heteroaryl having 1-3 heteroatoms selected from N and O; wherein the Ph, heterocyclyl, or heteroaryl represented by R is optionally substituted with one to three substituents independently selected from the group consisting of halogen, OH, CN, etc.; m = 0-3; Y = (CH2)p; p = 1-3; Z = (CH2)q; q = 1-3 and p+q ≤4], their pharmaceutically acceptable salts and stereoisomers as hematopoietic progenitor kinase 1 (HPK1)inhibitors for treating cancers. The invention is also related to the preparation of compounds V [A1 = CR’, N; X = P(O)R3R4; R’ = H, D, halo, CN, NO2, etc.; R1′ = independently at each occurrence H, D, OH, (un)substituted alk(en/yn)yl, etc.; R2′ = independently at each occurrence H, NO2, alkoxycarbonyl, etc.; m, n = independently 0-2] as HPK1 inhibitors for treating cancers. Thus, reaction of (1H-indol-3-yl)dimethylphosphine oxide (preparation given) with [1-(2,5-dichloropyrimidin-4-yl)-1H-indol-3-yl]dimethylphosphine oxide and treatment of the resulting [1-[5-chloro-2-[(6-methoxy-2-methyl-1,2,3,4-tetrahydroisoquinolin-7-yl)amino]pyrimidin-4-yl]-1H-indol-3-yl]dimethylphosphine oxide with 6-methoxy-2-methyl-1,2,3,4-tetrahydroisoquinolin-7-amine gave VI. VI inhibited HPK1 and JAK3 kinases with IC50 of ≤100μ=nM and > 1μM, resepctively. Certain HPK1 inhibitors I and V are selective against one or more kinases selected from: Lck, ZAP70, JAK3, PKC-theta, TBK1, and MAP4K3. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Safety of 6-Chloro-2,3-dihydro-1H-indole

The Article related to tetrahydroisoquinolinylaminopyrimidine pyrrolopyridinylphenyldialkyl phosphine preparation hpk1 inhibitor antitumor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Safety of 6-Chloro-2,3-dihydro-1H-indole

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles