Category: iodides-buliding-blocks

On June 7, 2007, Naidu, B. Narasimhulu; Banville, Jacques; Beaulieu, Francis; Connolly, Timothy P.; Krystal, Mark R.; Matiskella, John D.; Ouellet, Carl; Plamondon, Serge; Remillard, Roger; Sorenson, Margaret E.; Ueda, Yasutsugu; Walker, Michael A. published a patent.Computed Properties of 70931-59-8 The title of the patent was Bicyclic heterocycles, particularly 4-oxopyrimido[2,1-c][1,4]oxazine-2-carboxamide and 4-oxopyrimido[2,1-c][1,4]oxazepine-2-carboxamide derivatives, as HIV integrase inhibitors, their preparation, pharmaceutical compositions, and use in therapy. And the patent contained the following:

The invention is related to bicyclic pyrimidinone compounds, e.g. pyrimidooxazine I, which inhibit HIV integrase and prevent viral integration into human DNA. The invention is also related to the preparation of pharmaceutical compositions comprising a therapeutically effective amount of bicyclic pyrimidinones and a pharmaceutically acceptable carrier, optionally including a therapeutically effective amount of at least one other agent used for treatment of AIDS or HIV infection, as well as to the use of the compositions for the treatment of those infected with HIV. Thus, hydrogenolysis of dibenzyl compound II gave phosphonic acid I. I was tested for HIV integrase inhibition and for inhibition of HIV replication. The experimental process involved the reaction of 1-(Bromomethyl)-4-fluoro-2-iodobenzene(cas: 70931-59-8).Computed Properties of 70931-59-8

The Article related to pyrimidinone bicyclic preparation hiv integrase inhibitor, oxopyrimidooxazine oxopyrimidooxazepine carboxamide preparation hiv integrase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Computed Properties of 70931-59-8

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

On February 4, 2021, Schenkel, Laurie B.; Vasbinder, Melissa Marie; Kuntz, Kevin Wayne; Perl, Nicholas Robert; Downing, Jennifer published a patent.Product Details of 1096481-48-9 The title of the patent was Preparation of pyrazolopyrimidine carboxamides and related heterobicyclic amides as inhibitors of CD38 useful in the treatment of cancer. And the patent contained the following:

The invention relates to preparation of pyrazolopyrimidine carboxamides and related heterobicyclic amides(I) which are inhibitors of CD38 and are useful in the treatment of cancer. Compounds I wherein V is N or CRv; Rv is H, halo, or C1-4 alkyl; W is N or CRw; Rw is H, halo, or C1-4 alkyl;; Ring A is a 5-membered heteroaryl group having 1, 2 or 3 ring-forming heteroatoms selected from N, O, and S; L is a C1-4 alkylene linker; n is 0 or 1; Q is H, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, etc.; etc…, are claimed. The example compound II was prepared via 3-steps synthesis using imidazole as starting material (procedure given). Compounds I were evaluated for their biol. activity (data given). Compounds I can be useful in treatment of cancers. The experimental process involved the reaction of Methyl 2-amino-5-iodo-3-methylbenzoate(cas: 1096481-48-9).Product Details of 1096481-48-9

The Article related to pyrazolopyrimidine carboxamide preparation cd38 inhibitor antitumor cancer, heterobicyclic amide preparation cd38 inhibitor antitumor cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Product Details of 1096481-48-9

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

On February 1, 2016, Beaudegnies, Renaud; Quaranta, Laura; Murphy Kessabi, Fiona; Lamberth, Clemens; Knauf-Beiter, Gertrud; Fraser, Torquil published an article.Category: iodides-buliding-blocks The title of the article was Synthesis and anti-oomycete activity of novel quinazolin- and benzothiazol-6-yloxyacetamides: Potent aza-analogs and five-ring analogs of quinoline fungicides. And the article contained the following:

Synthesis and anti-oomycete activity of quinazolines, e.g., I and benzothiazol-6-yloxyacetamide II was described. The synthesized compounds showed excellent in vivo activity against the three economically most important oomycete pathogens Phytophthora infestans, Plasmopara viticola and Pythium ultimum. These were polar analogs of known quinolin-6-yloxyacetamides, which were not active against the soil-borne damping-off disease caused by Pythium ultimum. The Bogert quinazoline synthesis, proved to be highly useful for the concise construction of required quinazolin-6-ol building blocks. The experimental process involved the reaction of Methyl 2-amino-5-iodo-3-methylbenzoate(cas: 1096481-48-9).Category: iodides-buliding-blocks

The Article related to preparation quinazoline benzothiazolyloxyacetamide anti oomycete sar, benzothiazole, crop protection, fungicide, heterocycle, quinazoline, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Category: iodides-buliding-blocks

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

On February 17, 2009, Naidu, B. Narasimhulu; Sorenson, Margaret E.; Digiugno, Dawn published a patent.Formula: C7H5BrFI The title of the patent was Preparation of bicyclic heterocycles, particularly pyrimido[2,1-c][1,4]oxazine-2-carboxamides, as HIV integrase inhibitors. And the patent contained the following:

The invention is related to the preparation of title compounds I [R1 = C1-6(Ar1)alkyl, C1-6(Ar1)oxyalkyl, C1-6(Ar1)hydroxyalkyl, etc.; R2 = H, alkyl, OH, alkyloxy; Ar1 = (un)substituted Ph, naphthyl, benzothiophenyl, etc.; X-Y-Z = C(R3)2OC(R3)2, C(R3)2OC(R3)2C(R3)2, C(R3)2C(R3)2C(R3)2C(R3)2; R3 = H, alkyl], and their pharmaceutically acceptable salts or solvates which inhibit HIV integrase and prevent viral integration into human DNA. The invention is also related to the pharmaceutical compositions comprising pyrimidinones I, and methods of using them for treating HIV infection and AIDS. Thus, reacting ester II (preparation given) with 4-fluorobenzylamine in DMF/ethanol in the presence of TEA at 90掳 gave amide III in 82% yield. Selected I displayed IC50 values in the range of 0.002-0.1 渭M for the inhibition of HIV integrase activity. III demonstrated synergistic or additive-synergistic HIV antiviral activity when used in combination with other antiviral agents, e.g., zidovudine, indinavir, T-20, etc. Crystalline forms of III were prepared (crystal data were given). The experimental process involved the reaction of 1-(Bromomethyl)-4-fluoro-2-iodobenzene(cas: 70931-59-8).Formula: C7H5BrFI

The Article related to bicyclic heterocycle hiv integrase inhibitor preparation, pyrimidooxazine carboxamide preparation hiv integrase inhibitor aids treatment, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Formula: C7H5BrFI

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

On September 7, 2006, Naidu, B. Narasimhulu; Banville, Jacques; Beaulieu, Francis; Connolly, Timothy P.; Krystal, Mark R.; Matiskella, John D.; Ouellet, Carl; Plamondon, Serge; Remillard, Roger; Sorenson, Margaret E.; Ueda, Yasutsugu; Walker, Michael A. published a patent.Reference of 1-(Bromomethyl)-4-fluoro-2-iodobenzene The title of the patent was Preparation of bicyclic heterocycles, particularly pyrimido[2,1-c][1,4]oxazine-2-carboxamides, as HIV integrase inhibitors. And the patent contained the following:

The invention is related to the preparation of title compounds I [R1 = C1-6(Ar1)alkyl, C1-6(Ar1)oxyalkyl, C1-6(Ar1)hydroxyalkyl, etc.; R2 = H, alkyl, OH, alkyloxy; Ar1 = (un)substituted Ph, naphthyl, benzothiophenyl, etc.; X-Y-Z = C(R3)2OC(R3)2, C(R3)2OC(R3)2C(R3)2, C(R3)2C(R3)2C(R3)2C(R3)2; R3 = H, alkyl], and their pharmaceutically acceptable salts or solvates which inhibit HIV integrase and prevent viral integration into human DNA. The invention is also related to the pharmaceutical compositions comprising pyrimidinones I, and methods of using them for treating HIV infection and AIDS. Thus, reacting ester II (preparation given) with 4-fluorobenzylamine in DMF/ethanol in the presence of TEA at 90掳 gave amide III in 82% yield. Selected I displayed IC50 values in the range of 0.002-0.1 渭M for the inhibition of HIV integrase activity. III demonstrated synergistic or additive-synergistic HIV antiviral activity when used in combination with other antiviral agents, e.g., zidovudine, indinavir, T-20, etc. The experimental process involved the reaction of 1-(Bromomethyl)-4-fluoro-2-iodobenzene(cas: 70931-59-8).Reference of 1-(Bromomethyl)-4-fluoro-2-iodobenzene

The Article related to bicyclic heterocycle hiv integrase inhibitor preparation, pyrimidooxazine carboxamide preparation hiv integrase inhibitor aids treatment, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Reference of 1-(Bromomethyl)-4-fluoro-2-iodobenzene

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

On March 20, 2008, Flynn, Daniel L.; Kaufman, Michael D.; Patt, William C.; Petillo, Peter A. published a patent.Safety of Ethyl 5-chloro-2-iodobenzoate The title of the patent was Preparation of heterocyclic ureas as kinase inhibitors useful for the treatment of proliferative and inflammatory diseases. And the patent contained the following:

The present invention relates to novel kinase inhibitors and modulators of general formula I (wherein E1 is cyclopropyl, furyl, Ph, etc.; A is Ph, naphthyl, indanyl, etc.; Z6 is H, C1-C6alkyl, branched C3-C7alkyl, etc.; R3 and R16 are H, C1-C6 alkyl, branched C3-C7alkyl, etc.; R4 is H, C1-C6alkyl, hydroxyC1-C6alkyl, etc.; X2 is a direct bond or (un)branched C1-C6 alkyl; t is 1-3) useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds Preferably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration. Example compound II was prepared by reacting 2-amino-6-(3-amino-4-fluorophenyl)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one (preparation given) and 3-tert-butyl-1-phenyl-1H-pyrazol-5-amine (preparation given). In general, the I tested exhibited >50 % inhibition activity at 0.2-2 渭M concentration in V600E B-Raf kinase and C-Raf kinase assays. In general, the I tested exhibited >50 % inhibition of proliferation at 1-10uM concentration against A375 cells. The experimental process involved the reaction of Ethyl 5-chloro-2-iodobenzoate(cas: 1012882-90-4).Safety of Ethyl 5-chloro-2-iodobenzoate

The Article related to heterocyclic urea kinase inhibitor preparation proliferative inflammatory disease treatment, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Safety of Ethyl 5-chloro-2-iodobenzoate

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

On October 15, 2015, Loso, Michael R.; Gustafson, Gary D.; Kubota, Asako; Yap, Maurice C.; Buchan, Zachary A.; Steward, Kimberly M.; Sullenberger, Michael T.; Hoekstra, William J.; Yates, Christopher M. published a patent.COA of Formula: C7H3BrF3I The title of the patent was Preparation of metalloenzyme inhibitor compounds as fungicides for pharmaceutical and agricultural use. And the patent contained the following:

The invention describes compounds of formula I having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes as well the use of I to protect and/or cure plants against damage caused by agriculturally relevant fungi. I [wherein Z is (un)substituted pyrimidinyl, thiazolyl, oxazolyl, etc.; R1 is alkyl, haloalkyl, (hetero)aryl, etc.; R2 is aryl or heteroaryl; R3 is H, alkyl, (hetero)aryl, etc.; R4, R5, R6, and R7 are independently H, alkyl, alkoxy, etc.] are claimed and exemplified. Coupling of 1-(4-bromophenyl)-2,2-dimethyl-1-(pyrimidin-5-yl)propan-1-ol with (4-(trifluoromethoxy)phenyl)boronic acid provided II in 93% yield. Candidate compounds of I were evaluated for fungicidal activity against Leaf Blotch of Wheat (Mycosphaerella graminicola; Anamorph; Septoria tritica; Bayer Code SEPTTR)(data given). The experimental process involved the reaction of 5-Bromo-2-iodobenzotrifluoride(cas: 364-12-5).COA of Formula: C7H3BrF3I

The Article related to metalloenzyme inhibitor preparation pharmaceutical agricultural fungicide, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.COA of Formula: C7H3BrF3I

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

On October 12, 2017, Patil, Rakesh Ishwar; Gunjal, Amol Pandurang; Verma, Jeevan; Kumar, Puneet; Rai, Santosh Kumar; Rai, Himanshu; Kumar, Anil published a patent.Synthetic Route of 364-12-5 The title of the patent was Preparation of heterocyclic compounds as GPR119 agonist for treatment of metabolic disorders. And the patent contained the following:

The invention relates to novel compounds of formula I as GPR119 agonist, compositions containing such compounds and method of their preparation which are useful for the prevention or treatment of metabolic disorders including diabetes mellitus type I and type II. I [wherein X1, X2, X3, X4, and X5 independently = N, O, S, or CH; R1 and R2 independently = H, O, C1-6alkyl, amino, etc.; A = tetrazol-1-ylphenyl-, 4-dimethylaminocarbonyl-Ph, 1-benzyl-piperazin-4-yl, etc.; B = morpholin-4-ylcarbonyl-Ph, -CH2OH, 4-cyano-Ph, etc.; n = 0, 1, 2, or 3] or a pharmaceutically acceptable salt, hydrate, or stereoisomer thereof, are claimed and exemplified. Example compound II was prepared from the oxidation of the corresponding sulfanyl intermediate in 37.62% yield. Exemplified I were evaluated for antidiabetic activity using an oral glucose tolerance test in mice and Sprague-Dawley rats from which II demonstrated dose-dependent reduction of glucose at 3mpk and 10mpk. The experimental process involved the reaction of 5-Bromo-2-iodobenzotrifluoride(cas: 364-12-5).Synthetic Route of 364-12-5

The Article related to heterocyclic compound preparation gpr119 metabolic disease diabetes, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Synthetic Route of 364-12-5

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

On December 3, 2020, Hopper, Allen Taylor; Mischke, Steven; La, Daniel published a patent.HPLC of Formula: 1012882-90-4 The title of the patent was Cyanopiperiddine compounds as CYP46A1 inhibitors and their preparation, pharmaceutical compositions and use in the treatment of diseases. And the patent contained the following:

Described herein are cyanopiperidine compounds I that act as CYP46A1 inhibitors, compositions comprising these compounds, and methods of their use into treating neurodegenerative diseases and the like, or a pharmaceutically active salts thereof. Specifically, the invention relates to compounds of formula I wherein R1 is (un)substituted C6-10 aryl, (un)substituted C3-7 cycloalkyl, (un)substituted 3- to 7-membered heterocyclic ring, etc.; X is (CH2)0-2; Y is (CRaRb)0-4; Ra and Rb are independently H, halo, CN, OH, NO2, NH2 and derivatives, C1-6 alkyl, etc.; R7-R10 are independently H, C1-6 (halo)alkyl, C1-6 (halo)alkoxy, etc.; each of the R2 and R3 are independently halo, CN OH, NO2, NH2 and derivatives, C1-6 alkyl, C3-7 cycloalkyl, etc.; ring A is 5- to 6-membered N-containing heteroaryl; ring B is C6-10 aryl, 5- to 6-membered heteroaryl; and their pharmaceutically acceptable salts as CYP46A1 inhibitors in the treatment of diseases thereof, are claimed. Example compound II was prepared by using olefination, heterocyclization, and amidation as the key steps. All the invention compounds were evaluated for their CYP46A1 inhibitory activity. The experimental process involved the reaction of Ethyl 5-chloro-2-iodobenzoate(cas: 1012882-90-4).HPLC of Formula: 1012882-90-4

The Article related to cyano piperiddine preparation cyp46a1 inhibitor treatment disease, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.HPLC of Formula: 1012882-90-4

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

On June 7, 2007, Naidu, Narasimhulu B.; Ueda, Yasutsugu; Connolly, Timothy P. published a patent.Name: 1-(Bromomethyl)-4-fluoro-2-iodobenzene The title of the patent was Preparation of pyrimidine derivatives as HIV integrase inhibitors. And the patent contained the following:

Title compounds I, wherein R1 is arylalkyl, arylamide, arylester, arylhydroxyalkyl or aryloxyalkyl; R2 is H, alkyl, hydroxy or alkoxy; R3 is (un)substituted methyl; R4 is alkyl are prepared as HIV integrase inhibitors. Thus, II was prepared and displayed and HIV-integrase inhibition between 0.002 to 0.10 渭M and an inhibition of HIV replication between 0.003 to 0.10 渭M. Further, I can successfully be employed as prodrugs for treatment of AIDS or HIV infection selected from the group consisting of nucleoside HIV reverse transcriptase inhibitors, non-nucleoside HIV reverse transcriptase inhibitors, HIV protease inhibitors, HIV fusion inhibitors, HIV attachment inhibitors, CCR5 inhibitors, CXCR inhibitors, HIV budding or maturation inhibitors, and HIV integrase inhibitors. The experimental process involved the reaction of 1-(Bromomethyl)-4-fluoro-2-iodobenzene(cas: 70931-59-8).Name: 1-(Bromomethyl)-4-fluoro-2-iodobenzene

The Article related to pyrimidine preparation hiv integrase inhibition human prodrug, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Name: 1-(Bromomethyl)-4-fluoro-2-iodobenzene

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com