Tag: 200-300

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

Shalygina, E. E.; Kobylinskii, D. V.; Ivanovskii, S. A.; Balakin, K. V.; Dorogov, M. V.; Toporova, T. A. published an article in 2004, the title of the article was Synthesis and properties of 1-acylindolinesulfonamides.COA of Formula: C12H12ClNO3S And the article contains the following content:

Title compounds I and II were prepared by N-acylation of indoline, bromination and chlorosulfonylation (or just chlorosulfonylation), and amidation. Several properties indicative of potential pharmacol. activities were determined The experimental process involved the reaction of 1-(Cyclopropanecarbonyl)indoline-5-sulfonyl chloride(cas: 879562-21-7).COA of Formula: C12H12ClNO3S

The Article related to combinatorial library acylindolinesulfonamide preparation pharmacol potential, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.COA of Formula: C12H12ClNO3S

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

Shalygina, E. E.; Kobylinskii, D. V.; Ivanovskii, S. A.; Balakin, K. V.; Dorogov, M. V.; Toporova, T. A. published an article in 2004, the title of the article was Synthesis and properties of 1-acylindolinesulfonamides.COA of Formula: C12H12ClNO3S And the article contains the following content:

Title compounds I and II were prepared by N-acylation of indoline, bromination and chlorosulfonylation (or just chlorosulfonylation), and amidation. Several properties indicative of potential pharmacol. activities were determined The experimental process involved the reaction of 1-(Cyclopropanecarbonyl)indoline-5-sulfonyl chloride(cas: 879562-21-7).COA of Formula: C12H12ClNO3S

The Article related to combinatorial library acylindolinesulfonamide preparation pharmacol potential, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.COA of Formula: C12H12ClNO3S

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 May 31, 2007, Kerns, Jeffrey K.; Busch-Petersen, Jakob; Li, Huijie; Boehm, Jeffrey Charles; Nie, Hong; Taggart, John J. published a patent.Application of 860624-88-0 The title of the patent was Preparation of indolecarboxamide derivatives as inhibitors of kinase activity. And the patent contained the following:

The title compounds with general formula I [wherein X = O, S, S(O), S(O)2, etc,; R1 = H, (un)substituted alkyl, haloalkyl, heterocycloalkyl, etc.; R2 = (un)substituted alkyl, aryl, cycloalkyl, etc.; R3 = independently OH, oxo, alkyl, or haloalkyl; m = 1-3] or pharmaceutically acceptable salts thereof were prepared for the treatment of disorders associated with inappropriate IKK2 activities. In particular, I can be used for the treatment and prevention of inflammatory and tissue repair disorders, including rheumatoid arthritis, asthma, and COPD. For example, compound II was prepared in a multi-step synthesis. II exhibited IKK2 inhibitory activity with pIC50 value of 4.6 in IKK2 assay. The experimental process involved the reaction of Methyl 5-bromoindoline-7-carboxylate(cas: 860624-88-0).Application of 860624-88-0

The Article related to preparation indolecarboxamide inhibitor kinase activity, treatment inflammatory tissue repair disorder human, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Application of 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 October 2, 2008, Boehm, Jeffrey Charles; Busch-Petersen, Jakob; Fu, Wei; Jin, Qi; Kerns, Jeffrey K.; Li, Huijie; Lin, Guoliang; Lin, Xichen; Neipp, Christopher E. published a patent.COA of Formula: C10H10BrNO2 The title of the patent was Preparation of indolecarboxamide derivatives for use as IKK2 inhibitors. And the patent contained the following:

Title compounds I [R1 = YZ; R2 = bicyclo group or (un)substituted heterocycloalkyl containing S, S(O), or SO2; R3 and R4 independently = H or F; Y = bond, alkylene, alkenylene, or alkynylene; Z = (un)substituted aryl or heteroaryl; m = 0 or 1; with provisions], and their pharmaceutically acceptable salts, are prepared and disclosed as IKK2 inhibitors. Thus, e.g., II was prepared by bromination of 1-(1,1-dimethylethyl) 7-Me 2,3-dihydro-1H-1,7-dicarboxylate (preparation given) followed by deprotection, oxidation, condensation with tetrahydro-4H-thiopyran-4-one, protection, oxidation, deprotection/hydrolysis, amidation with ammonia, and coupling with phenylboronic acid. Select I were evaluated in IKK2 assays and demonstrated a pIC50 of about 5.0 to about 8.5. I were disclosed as therapeutic agents for the inhibition of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKKβ) activity, such as rheumatoid arthritis, asthma, rhinitis, and chronic obstructive pulmonary disease. The experimental process involved the reaction of Methyl 5-bromoindoline-7-carboxylate(cas: 860624-88-0).COA of Formula: C10H10BrNO2

The Article related to indolecarboxamide derivative preparation ikk2 inhibitor rheumatoid arthritis asthma rhinitis, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.COA of Formula: C10H10BrNO2

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 28, 2005, Baldwin, Ian Robert; Bamborough, Paul; Christopher, John Andrew; Kerns, Jeffrey K.; Longstaff, Timothy; Miller, David Drysdale published a patent.Name: Methyl 5-bromoindoline-7-carboxylate The title of the patent was Preparation of 7-indolecarboxamides as IKK2 kinase inhibitors for the treatment of such as inflammatory and tissue repair disorders. And the patent contained the following:

Title compounds I [wherein R1, R2 = H, halo, alkylene, alkenylene, (hetero)aryl, etc., and salts, solvates, or physiol. functional derivatives thereof] were prepared as IKK2 kinase inhibitors. For instance, Pd-catalyzed coupling of Boc-protected bromide II (preparation given) with phenylboronic acid followed by deprotection with HCl gave 7-indolecarboxamide III. Most invented compounds were found to have activity >4.8 in the IKK2 assay, in which the degree of phosphorylation of GST-IκBα was measured as a ratio of specific 665 nm energy transfer signal to reference europium 620 nm signal. Therefore, I and their pharmaceutical compositions are useful in the treatment and prevention of disease states mediated by IKK2 mechanisms, including inflammatory and tissue repair disorders. The experimental process involved the reaction of Methyl 5-bromoindoline-7-carboxylate(cas: 860624-88-0).Name: Methyl 5-bromoindoline-7-carboxylate

The Article related to indolecarboxamide preparation ikk2 kinase inhibitor, treatment inflammatory tissue repair disorder indolecarboxamide preparation, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Name: Methyl 5-bromoindoline-7-carboxylate

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 24, 2014, Buckman, Brad Owen; Nicholas, John Beamond; Emayan, Kumaraswamy; Seiwert, Scott D.; Yuan, Shendong published a patent.Reference of Methyl 2-(6-bromo-1H-indol-3-yl)acetate The title of the patent was N-Heteroaryl carbamates as lysophosphatidic acid receptor antagonists and their preparation. And the patent contained the following:

Compounds of formula I, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided. Compounds of formula I wherein one of and B is acetylene and the other is (un)substituted 6- to 11-membered aryl, (un)substituted 5- to 11- membered heteroaryl, (un)substituted 4- to 11-membered heterocyclyl and (un)substituted 4- to 11-membered carbocyclyl; G is (un)substituted 6- to 11-membered aryl, (un)substituted 5- to 11- membered heteroaryl, (un)substituted 5- to 11-membered heterocyclyl and (un)substituted 5- to 11-membered carbocyclyl; D is OH, CO2H and derivatives, CONH2 and derivatives, azolyl, etc.; E is (un)substituted 6- to 10-membered arylene, (un)substituted 3- to 11-membered carbocyclyl, (un)substituted 3- to 11-membered heterocyclyl and (un)substituted 5- to 10-membered heteroarylene; J is (CR4R5)0-3; K is (CR2’R3′)n; M is (CR2R3)m; n and m are independently 0 – 3, provided that the sum of m + n is equal or greater than 1; L1 and L2 are independently a bond, CH2, CC, etc.; L3 is azolyl, thienyl, aminosulfonyl, etc.; L5 is single bond, CH=CH, CC, etc.; dashed bonds are single and double bonds; each Y is independently absent CR9, C(R9)2, N and NH, provided that only one of Y can be absent; R2, R2′, R3 and R3′ are independently H, halo, alkyl, haloalkyl, etc.; R4, R5 and R9 are independently H and (un)substituted alkyl; R4R5 or two adjacent R9 can be taken together to form (un)substituted cycloalkyl; 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 LPA antagonistic activity. From the assay, it was determined that compound II exhibited EC50 value in the range of greater than or equal to 50 nM and less than or equal to 500 nM. The experimental process involved the reaction of Methyl 2-(6-bromo-1H-indol-3-yl)acetate(cas: 152213-63-3).Reference of Methyl 2-(6-bromo-1H-indol-3-yl)acetate

The Article related to heteroaryl carbamate preparation lysophosphatidic acid receptor antagonist, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Reference of Methyl 2-(6-bromo-1H-indol-3-yl)acetate

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 24, 2014, Buckman, Brad Owen; Nicholas, John Beamond; Emayan, Kumaraswamy; Seiwert, Scott D.; Yuan, Shendong published a patent.Reference of Methyl 2-(6-bromo-1H-indol-3-yl)acetate The title of the patent was N-Heteroaryl carbamates as lysophosphatidic acid receptor antagonists and their preparation. And the patent contained the following:

Compounds of formula I, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided. Compounds of formula I wherein one of and B is acetylene and the other is (un)substituted 6- to 11-membered aryl, (un)substituted 5- to 11- membered heteroaryl, (un)substituted 4- to 11-membered heterocyclyl and (un)substituted 4- to 11-membered carbocyclyl; G is (un)substituted 6- to 11-membered aryl, (un)substituted 5- to 11- membered heteroaryl, (un)substituted 5- to 11-membered heterocyclyl and (un)substituted 5- to 11-membered carbocyclyl; D is OH, CO2H and derivatives, CONH2 and derivatives, azolyl, etc.; E is (un)substituted 6- to 10-membered arylene, (un)substituted 3- to 11-membered carbocyclyl, (un)substituted 3- to 11-membered heterocyclyl and (un)substituted 5- to 10-membered heteroarylene; J is (CR4R5)0-3; K is (CR2’R3′)n; M is (CR2R3)m; n and m are independently 0 – 3, provided that the sum of m + n is equal or greater than 1; L1 and L2 are independently a bond, CH2, CC, etc.; L3 is azolyl, thienyl, aminosulfonyl, etc.; L5 is single bond, CH=CH, CC, etc.; dashed bonds are single and double bonds; each Y is independently absent CR9, C(R9)2, N and NH, provided that only one of Y can be absent; R2, R2′, R3 and R3′ are independently H, halo, alkyl, haloalkyl, etc.; R4, R5 and R9 are independently H and (un)substituted alkyl; R4R5 or two adjacent R9 can be taken together to form (un)substituted cycloalkyl; 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 LPA antagonistic activity. From the assay, it was determined that compound II exhibited EC50 value in the range of greater than or equal to 50 nM and less than or equal to 500 nM. The experimental process involved the reaction of Methyl 2-(6-bromo-1H-indol-3-yl)acetate(cas: 152213-63-3).Reference of Methyl 2-(6-bromo-1H-indol-3-yl)acetate

The Article related to heteroaryl carbamate preparation lysophosphatidic acid receptor antagonist, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Reference of Methyl 2-(6-bromo-1H-indol-3-yl)acetate

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; Brockunier, Linda L.; Nargund, Ravi; Marcantonio, Karen; Zorn, Nicolas; Xiao, Dong; Peng, Xuanjia; Li, Peng; Guo, Tao published a patent.Related Products 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 and aromatic ring system; ring B is benzofuran, pyridinofuran pyrazolopyridine, etc.; E is absent and CR5R9; F is (CH)0-2 and (CH2)0-2; Z is N and CRa; Z1, Z2 and Z3 are independently CH and H, wherein 1 or 2 of Z1 – Z2 are N; 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, OH, halo, etc.; R9 is H; R5R9 taken together to form C3-6 cycloalkyl; R6 is H, OH, C1-6 alkyl, C1-6 haloalkyl, etc.; R7 is H and C1-6 alkyl; R6R7 taken together to form oxo; R8 is H, halo and OH and derivatives; R10 is H and C1-6 alkyl; Ra is H, halo and CN; 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 3.784 nM to 4.674 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).Related Products of 1256359-96-2

The Article related to tetracyclic heterocycle preparation antiviral treatment hepatitis c, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Related Products 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; Brockunier, Linda L.; Nargund, Ravi; Marcantonio, Karen; Zorn, Nicolas; Xiao, Dong; Peng, Xuanjia; Li, Peng; Guo, Tao published a patent.Recommanded Product: 4-Fluoro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole 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 and aromatic ring system; ring B is benzofuran, pyridinofuran pyrazolopyridine, etc.; E is absent and CR5R9; F is (CH)0-2 and (CH2)0-2; Z is N and CRa; Z1, Z2 and Z3 are independently CH and H, wherein 1 or 2 of Z1 – Z2 are N; 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, OH, halo, etc.; R9 is H; R5R9 taken together to form C3-6 cycloalkyl; R6 is H, OH, C1-6 alkyl, C1-6 haloalkyl, etc.; R7 is H and C1-6 alkyl; R6R7 taken together to form oxo; R8 is H, halo and OH and derivatives; R10 is H and C1-6 alkyl; Ra is H, halo and CN; 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 3.784 nM to 4.674 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).Recommanded Product: 4-Fluoro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole

The Article related to tetracyclic heterocycle preparation antiviral treatment hepatitis c, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Recommanded Product: 4-Fluoro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-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