Category: 944559-46-0

On June 25, 2020, Han, Amy; Kelly, Marcus; Olson, William published a patent.Category: thiazole The title of the patent was Tubulysins and protein-tubulysin conjugates. And the patent contained the following:

Provided herein are compounds, compositions, and methods for the treatment of diseases and disorders associated with cancer, including tubulysins and protein (e.g., antibody) drug conjugates thereof. The experimental process involved the reaction of Ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate(cas: 944559-46-0).Category: thiazole

The Article related to tubulysin protein conjugate antibody cancer, Pharmaceuticals: Formulation and Compounding and other aspects.Category: thiazole

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On November 24, 2017, Liu, Denggui; Yang, Kunyu; Zhou, Wei; Chen, Hao; Zeng, Qingdong published a patent.Quality Control of Ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate The title of the patent was Preparation of 2-(4-methyl-1-oxo-2-penten-1-yl)-4-thiazolecarboxylic acid ethyl ester. And the patent contained the following:

The invention discloses a preparation method of anti-cancer medicament intermediate, using glyceraldehyde acetonide and L-cysteine hydrochloride as raw materials, through steps such as cyclization, oxidation, de-propylidene, reoxidizing, and halohydrin to obtain an intermediate compound, which was further reacted with isobutyric aldehyde through Wittig, and compound 2-(4-methyl-1-oxo-2-penten-1-yl)-4-thiazolecarboxylic acid Et ester is obtained. The experimental process involved the reaction of Ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate(cas: 944559-46-0).Quality Control of Ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate

The Article related to thiazolecarboxylic acid ethyl ester preparation, Amino Acids, Peptides, and Proteins: Amino Acids and other aspects.Quality Control of Ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On January 22, 2011, Zanda, Matteo; Sani, Monica; Lazzari, Paolo published a patent.Recommanded Product: Ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate The title of the patent was Pharmaceutical compositions comprising tubulysin compounds. And the patent contained the following:

The present invention relates to synthetic tubulysin compounds having a high cytotoxicity, with antimitotic and/or antiangiogenic properties, the corresponding solvates and pharmaceutically acceptable salts thereof, their use for the treatment of tumors and/or diseases associated to angiogenesis, and a process for their preparation with high yield. Pharmaceutical compositions comprising tubulysin compounds or their conjugates with polymers or biomols., e.g., proteins, hormones, aptamers, polysaccharides, antibodies and fragments thereof, peptides, vitamins, etc., are disclosed. Thus, (2S,4R)-4-[2-[(1R,3R)-1-acetoxy-3-[(2S,3R)-N-benzyl-3-methyl-2-(1-methylpiperidine-2-carboxamido)pentanamido]-4-methylpentyl]thiazole-4-carboxamido]-2-methyl-5-phenylpentanoic acids was prepared and formulated into nanoparticles of polylactate-polyglycolate copolymer. The high cytotoxicity of the compound against 3 tumor cell lines (HL60, HT29 and A2780) was demonstrated. The experimental process involved the reaction of Ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate(cas: 944559-46-0).Recommanded Product: Ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate

The Article related to tubulysin compound preparation antitumor antimitotic angiogenesis inhibitor pharmaceutical, Pharmaceuticals: Formulation and Compounding and other aspects.Recommanded Product: Ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On December 12, 2017, Liu, Denggui; Yang, Kunyu; Zhou, Wei; Chen, Hao; Zeng, Qingdong published a patent.Application In Synthesis of Ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate The title of the patent was Method for preparing anticancer drug intermediate. And the patent contained the following:

The title anticancer drug intermediate is a compound shown in formula IIIa or IIIb. The title method comprises the steps of: conducting halogenation on 2-acetyl-4-formate thiazole compound, and reacting with tri-Ph phosphine, tri-Me phosphite, or tri-Et phosphite. The inventive compound can be applied in preparing a compound shown in formula I via conducting Wittig or Wittig-Horner reaction with isobutyraldehyde. The preparing process has the advantages of low raw material costs, mild reaction conditions, little pollution, and easy industrialization. The experimental process involved the reaction of Ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate(cas: 944559-46-0).Application In Synthesis of Ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate

The Article related to thiazole containing phosponate preparation anticancer drug intermediate, Organometallic and Organometalloidal Compounds: Phosphorus Compounds and other aspects.Application In Synthesis of Ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On November 20, 2008, Richter, Wolfgang published a patent.COA of Formula: C12H15NO3S The title of the patent was Preparation of tubulysine derivatives for treatment of cancer. And the patent contained the following:

The invention relates to novel cytotoxic peptides R1R2NCR3R4CONHCR5R6CONR7CR8R9-X-CHR10-A-CONHR11 [A is an optionally-substituted 5- or 6-membered heteroaryl ring; X is O, S, NR12, CR13R14, or CH2CR13R14; R1-R6, R8-R10, R12-R14 are independently H, optionally substituted alk(en)(yn)yl, aryl, heteroaryl, cycloalkyl, etc.; or two R groups form (hetero)cycloalkyl; R7 is alkyl, oxaalkyl, alkanoyl, CH2OCOPh, alkylaminoalkyl, hydroxyalkyl, etc.; R11 is -CH(CH2R15)(CH2)0-3CHR16R17, where R15 is optionally substituted aryl, heteroaryl, heterocycloalkyl,heteroalkylcycloalkyl, or heteroaralkyl;R16 is H, optionally alkyl, aryl, or heteroaryl;R17 is CO2H or ester, CONHNH2, OH, NH2, SH, or optionally substituted alkyl, cycloalkyl, heteroalkyl, orheterocycloalkyl] and their use for the treatment of cancer and other diseases. Thus, peptide I was prepared by a multistep procedure involving peptide coupling in solution Compounds of the invention show an activity against several cancer cell lines between 0.03 to 60 nM. The experimental process involved the reaction of Ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate(cas: 944559-46-0).COA of Formula: C12H15NO3S

The Article related to peptide tubulysine derivative preparation treatment cancer, Amino Acids, Peptides, and Proteins: Poly(Amino Acids) and Peptides and other aspects.COA of Formula: C12H15NO3S

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On May 31, 2007, Sani, Monica; Fossati, Giacomo; Huguenot, Florent; Zanda, Matteo published an article.Reference of Ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate The title of the article was Total synthesis of tubulysins U and V. And the article contained the following:

A reliable and modular reaction sequence has been developed for the synthesis of the challenging tubulysin U and V (I, R = OAc, OH). This route allowed preparation of hundreds of milligrams of the stereochem. pure tetra-peptides, which are produced in small amounts by two different species of myxobacteria. This strategy made the full biol. evaluation of the tubulysins and their analogs possible. The experimental process involved the reaction of Ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate(cas: 944559-46-0).Reference of Ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate

The Article related to tubulysin asym preparation, Amino Acids, Peptides, and Proteins: Poly(Amino Acids) and Peptides and other aspects.Reference of Ethyl 2-(4-methylpent-2-enoyl)thiazole-4-carboxylate

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica