Category: 68638-67-5

On October 13, 2009, Dorsey, Bruce D.; Milkiewicz, Karen L.; Pippin, Douglas A.; Theroff, Jay P.; Underiner, Ted; Weinberg, Linda; Zificsak, Craig A. published a patent.Name: 3-((6-Bromopyridin-2-yl)amino)propanoic acid The title of the patent was Preparation of pyridopyrazine derivatives as ALK and c-Met inhibitors. And the patent contained the following:

Title compounds I [ A = N or CH; X = -L2G1L3G2L4R7 or R8, wherein G1 and G2 independently = bond, (un)substituted (hetero)aryl or heterocycloalkyl; R7 = (un)substituted alkyl, alkenyl, alkynyl, (hetero)aryl or (hetero)cycloalkyl; R8 = H, halo, CN or CO2H; L1-4 independently = bond, alkyl-C(O)-alkyl, alkyl-C(O)O-alkyl, alkyl-O-alkyl, alkyl, alkenyl, alkynyl, etc.; R1 = (un)substituted (hetero)cycloalkyl or (hetero)aryl; R2 and R3 independently = H, OH or alkyl; R2 and R3 together may form a carbonyl group; R4, R5 and R6 independently = H or alkyl; R4 and R5 together may form a carbonyl group, or one of R4 and R5 forms a double bond with R6], and their pharmaceutically acceptable salts, are prepared and disclosed as Anaplastic Lymphoma Kinase (ALK) and c-Met inhibitors. Thus, e.g., II was prepared by acylation of 7-iodo-1,2,3,4-tetrahydropyrido[2,3-b]pyrazine (preparation given) with benzoyl chloride followed by Suzuki coupling reaction with (4-ethoxycarbonylphenyl)boronic acid to generate intermediate 4-(1-benzyl-1,2,3,4-tetrahydropyrido[2,3-b]pyrazin-7-yl)benzoic acid Et ester followed by hydrolysis and amidation with (S)-(+)-1-[(2-pyrrolidinyl)methyl]pyrrolidine to provide II as trifluoroacetate salt. All exemplar compounds were tested for their ability to inhibit the kinase activity for ALK and c-Met. For instance, II exhibited IC50 values ranging from 0.1 to 1 μM for ALK and c-Met kinase inhibition, resp. As inhibitors of ALK and/or c-Met, I may be used to treat ALK- or c-Met-mediated disorders or conditions. The experimental process involved the reaction of 3-((6-Bromopyridin-2-yl)amino)propanoic acid(cas: 68638-67-5).Name: 3-((6-Bromopyridin-2-yl)amino)propanoic acid

The Article related to pyridopyrazine preparation anaplastic lymphoma kinase alk cmet inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Name: 3-((6-Bromopyridin-2-yl)amino)propanoic acid

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On November 15, 2007, Dorsey, Bruce D.; Milkiewicz, Karen L.; Pippin, Douglas A.; Theroff, Jay P.; Underiner, Theodore L.; Weinberg, Linda; Zificsak, Craig A. published a patent.Formula: C8H9BrN2O2 The title of the patent was Preparation of pyridopyrazine derivatives as ALK and c-Met inhibitors. And the patent contained the following:

Title compounds I [ A = N or CH; X = -L2G1L3G2L4R7 or R8, wherein G1 and G2 independently = bond, (un)substituted (hetero)aryl or heterocycloalkyl; R7 = (un)substituted alkyl, alkenyl, alkynyl, (hetero)aryl or (hetero)cycloalkyl; R8 = H, halo, CN or CO2H; L1-4 independently = bond, alkyl-C(O)-alkyl, alkyl-C(O)O-alkyl, alkyl-O-alkyl, alkyl, alkenyl, alkynyl, etc.; R1 = (un)substituted (hetero)cycloalkyl or (hetero)aryl; R2 and R3 independently = H, OH or alkyl; R2 and R3 together may form a carbonyl group; R4, R5 and R6 independently = H or alkyl; R4 and R5 together may form a carbonyl group, or one of R4 and R5 forms a double bond with R6], and their pharmaceutically acceptable salts, are prepared and disclosed as Anaplastic Lymphoma Kinase (ALK) and c-Met inhibitors. Thus, e.g., II was prepared by acylation of 7-iodo-1,2,3,4-tetrahydropyrido[2,3-b]pyrazine (preparation given) with benzoyl chloride followed by Suzuki coupling reaction with (4-ethoxycarbonylphenyl)boronic acid to generate intermediate 4-(1-benzyl-1,2,3,4-tetrahydropyrido[2,3-b]pyrazin-7-yl)benzoic acid Et ester followed by hydrolysis and amidation with (S)-(+)-1-[(2-pyrrolidinyl)methyl]pyrrolidine to provide II as trifluoroacetate salt. All exemplar compounds were tested for their ability to inhibit the kinase activity for ALK and c-Met. For instance, II exhibited IC50 values ranging from 0.1 to 1 μM for ALK and c-Met kinase inhibition, resp. As inhibitors of ALK and/or c-Met, I may be used to treat ALK- or c-Met-mediated disorders or conditions. The experimental process involved the reaction of 3-((6-Bromopyridin-2-yl)amino)propanoic acid(cas: 68638-67-5).Formula: C8H9BrN2O2

The Article related to pyridopyrazine preparation anaplastic lymphoma kinase alk cmet inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Formula: C8H9BrN2O2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On October 13, 2009, Dorsey, Bruce D.; Milkiewicz, Karen L.; Pippin, Douglas A.; Theroff, Jay P.; Underiner, Ted; Weinberg, Linda; Zificsak, Craig A. published a patent.Name: 3-((6-Bromopyridin-2-yl)amino)propanoic acid The title of the patent was Preparation of pyridopyrazine derivatives as ALK and c-Met inhibitors. And the patent contained the following:

Title compounds I [ A = N or CH; X = -L2G1L3G2L4R7 or R8, wherein G1 and G2 independently = bond, (un)substituted (hetero)aryl or heterocycloalkyl; R7 = (un)substituted alkyl, alkenyl, alkynyl, (hetero)aryl or (hetero)cycloalkyl; R8 = H, halo, CN or CO2H; L1-4 independently = bond, alkyl-C(O)-alkyl, alkyl-C(O)O-alkyl, alkyl-O-alkyl, alkyl, alkenyl, alkynyl, etc.; R1 = (un)substituted (hetero)cycloalkyl or (hetero)aryl; R2 and R3 independently = H, OH or alkyl; R2 and R3 together may form a carbonyl group; R4, R5 and R6 independently = H or alkyl; R4 and R5 together may form a carbonyl group, or one of R4 and R5 forms a double bond with R6], and their pharmaceutically acceptable salts, are prepared and disclosed as Anaplastic Lymphoma Kinase (ALK) and c-Met inhibitors. Thus, e.g., II was prepared by acylation of 7-iodo-1,2,3,4-tetrahydropyrido[2,3-b]pyrazine (preparation given) with benzoyl chloride followed by Suzuki coupling reaction with (4-ethoxycarbonylphenyl)boronic acid to generate intermediate 4-(1-benzyl-1,2,3,4-tetrahydropyrido[2,3-b]pyrazin-7-yl)benzoic acid Et ester followed by hydrolysis and amidation with (S)-(+)-1-[(2-pyrrolidinyl)methyl]pyrrolidine to provide II as trifluoroacetate salt. All exemplar compounds were tested for their ability to inhibit the kinase activity for ALK and c-Met. For instance, II exhibited IC50 values ranging from 0.1 to 1 μM for ALK and c-Met kinase inhibition, resp. As inhibitors of ALK and/or c-Met, I may be used to treat ALK- or c-Met-mediated disorders or conditions. The experimental process involved the reaction of 3-((6-Bromopyridin-2-yl)amino)propanoic acid(cas: 68638-67-5).Name: 3-((6-Bromopyridin-2-yl)amino)propanoic acid

The Article related to pyridopyrazine preparation anaplastic lymphoma kinase alk cmet inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Name: 3-((6-Bromopyridin-2-yl)amino)propanoic acid

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On November 15, 2007, Dorsey, Bruce D.; Milkiewicz, Karen L.; Pippin, Douglas A.; Theroff, Jay P.; Underiner, Theodore L.; Weinberg, Linda; Zificsak, Craig A. published a patent.Formula: C8H9BrN2O2 The title of the patent was Preparation of pyridopyrazine derivatives as ALK and c-Met inhibitors. And the patent contained the following:

Title compounds I [ A = N or CH; X = -L2G1L3G2L4R7 or R8, wherein G1 and G2 independently = bond, (un)substituted (hetero)aryl or heterocycloalkyl; R7 = (un)substituted alkyl, alkenyl, alkynyl, (hetero)aryl or (hetero)cycloalkyl; R8 = H, halo, CN or CO2H; L1-4 independently = bond, alkyl-C(O)-alkyl, alkyl-C(O)O-alkyl, alkyl-O-alkyl, alkyl, alkenyl, alkynyl, etc.; R1 = (un)substituted (hetero)cycloalkyl or (hetero)aryl; R2 and R3 independently = H, OH or alkyl; R2 and R3 together may form a carbonyl group; R4, R5 and R6 independently = H or alkyl; R4 and R5 together may form a carbonyl group, or one of R4 and R5 forms a double bond with R6], and their pharmaceutically acceptable salts, are prepared and disclosed as Anaplastic Lymphoma Kinase (ALK) and c-Met inhibitors. Thus, e.g., II was prepared by acylation of 7-iodo-1,2,3,4-tetrahydropyrido[2,3-b]pyrazine (preparation given) with benzoyl chloride followed by Suzuki coupling reaction with (4-ethoxycarbonylphenyl)boronic acid to generate intermediate 4-(1-benzyl-1,2,3,4-tetrahydropyrido[2,3-b]pyrazin-7-yl)benzoic acid Et ester followed by hydrolysis and amidation with (S)-(+)-1-[(2-pyrrolidinyl)methyl]pyrrolidine to provide II as trifluoroacetate salt. All exemplar compounds were tested for their ability to inhibit the kinase activity for ALK and c-Met. For instance, II exhibited IC50 values ranging from 0.1 to 1 μM for ALK and c-Met kinase inhibition, resp. As inhibitors of ALK and/or c-Met, I may be used to treat ALK- or c-Met-mediated disorders or conditions. The experimental process involved the reaction of 3-((6-Bromopyridin-2-yl)amino)propanoic acid(cas: 68638-67-5).Formula: C8H9BrN2O2

The Article related to pyridopyrazine preparation anaplastic lymphoma kinase alk cmet inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Formula: C8H9BrN2O2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On July 15, 2004, Boys, Mark L.; Schretzman, Lori A.; Tollefson, Michael B.; Chandrakumar, Nizal S.; Khanna, Ish K.; Nguyen, Maria; Downs, Victoria; Mohler, Scott B.; Gesicki, Glen J.; Penning, Thomas D.; Chen, Barbara B.; Wang, Yaping; Khilevich, Albert; Desai, Bipinchandra N.; Yu, Yi; Wendt, John A.; Stenmark, Heather; Wu, Lisa; Huff, Renee M.; Nagarajan, Srinivasan R.; Devadas, Balekudru; Lu, Hwang-fun; Russell, Mark; Spangler, Dale P.; Parikh, Mihir D.; Clare, Michael published a patent.COA of Formula: C8H9BrN2O2 The title of the patent was Heteroarylalkanoic acids as integrin receptor antagonists. And the patent contained the following:

The present invention relates to pharmaceutical compositions comprising compounds I [A = (un)saturated and/or (un)substituted 4-8 membered monocyclic or 7-12 membered bicyclic ring, containing 1 to 5 heteroatoms selected from the group consisting of O, N or S; ring A may further contain a carboxamide, sulfone, sulfonamide, or an acyl group; A1 = (un)saturated and/or (un)substituted 5-9 membered monocyclic or 8-14 membered polycyclic heterocycle containing at least one N; or A1 = substituted urea, iminourea or thiourea alicyclic or cyclic analog; Z1 = CH2, CH2O, O, NH, CO, S, SO, CHOH, SO2; Z2 = (un)substituted 1-5 carbon linker optionally containing one or more heteroatoms; alternatively Z1-Z2 may contain a carboxamide, sulfone, sulfonamide, alkenyl, acyl group, or aryl or heteroaryl ring; X = CO, SO2, S, O, substituted amine, substituted CH; Y = CO, SO2, substituted amine, etc.; Y5 = C or N; Y3 and Y4 independently = H, halo, (un)substituted-alkyl, -aryl, -alkene, etc.; or Y3 and Y4 together form a (un)saturated and/or (un)substituted 3-8 membered monocyclic or a 7-11 membered bicyclic ring optionally containing heteroatoms; or X and Y3 form a 3-7 membered monocyclic ring optionally containing heteroatoms; Rb = OH, alkoxy, arylamine, etc.], or a pharmaceutically acceptable salt thereof, methods of selectively inhibiting or antagonizing the ανβ3 and/or the ανβ5 integrin without significantly inhibiting the ανβ6 integrin, and methods to prepare I. Thus, e.g., II was prepared in four steps with oxadiazole ring forming via cyclization reaction of amide oxime III with cyclic anhydride IV (preparation given). I antagonize αvβ3 integrin with an IC50 values ranging from 0.1 nM to 100 μM in the 293-cell assay. Similarly, I also antagonized αvβ5 integrin with an IC50 values of < 50 μM in the cell adhesion assay. The experimental process involved the reaction of 3-((6-Bromopyridin-2-yl)amino)propanoic acid(cas: 68638-67-5).COA of Formula: C8H9BrN2O2

The Article related to butanoic acid heteroaryl derivative preparation integrin receptor antagonist, alkanoic acid heteroaryl derivative preparation integrin receptor antagonist, Aliphatic Compounds: Carboxylic Acids and Peroxycarboxylic Acids and Their Sulfur-Containing Analogs and Salts and other aspects.COA of Formula: C8H9BrN2O2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On October 31, 1978, Da Settimo, A.; Biagi, G.; Primofiore, G.; Ferrarini, P. L.; Livi, O. published an article.Related Products of 68638-67-5 The title of the article was Synthesis of some 11H-indolo[3,2-c][1,8]naphthyridines. And the article contained the following:

Twelve 11H-indolo[3,2-c][1,8]naphthyridines I (R = OEt, OH, SH, H; R1 = H, F, Br, Me, MeO, OH; R2 = H, MeO, OH) were prepared in 11.9-93.6% yield by 2 methods, e.g., by the Fischer indole synthesis. The UV of I were discussed. Several I were prepared from II, which was prepared in 70.9% yield from 7-bromo-2,3-dihydro-1,8-naphthyridin-4(1H)-one. II displayed a passive cutaneous anaphylaxis inhibition when administered i.p. in the rat at a dose of 25 mg/kg, but it exhibited no oral activity. The experimental process involved the reaction of 3-((6-Bromopyridin-2-yl)amino)propanoic acid(cas: 68638-67-5).Related Products of 68638-67-5

The Article related to anaphylaxis ethoxydihydronaphthyridinone, indolonaphthyridine uv nmr preparation, fischer indole synthesis indolonaphthyridine, 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 68638-67-5

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem