Tag: 200-300

On March 24, 2016, Cremonesi, Susanna; Luker, Tim; Semeraro, Teresa; Micheli, Fabrizio published a patent.Name: tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate The title of the patent was Preparation of spirocyclic derivatives for the treatment and prevention of dopamine transporter-mediated diseases. And the patent contained the following:

The invention relates to preparation of spirocyclic derivs of formula I wherein R1, R2, R3, R4, R5, R6, R9, R10, Q, X, Y, Z, A, L, B, m, n and p are as defined in the disclosure, pharmaceutical compositions comprising such compounds; their use in therapy (for example in the treatment or prevention of a disease, disorder or condition ameliorated by inhibition of a dopamine transporter). The experimental process involved the reaction of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate(cas: 1198284-94-4).Name: tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate

The Article related to spirocyclic derivative preparation dopamine transporter disease therapy prophylaxis, Heterocyclic Compounds (More Than One Hetero Atom): General and other aspects.Name: tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On January 15, 2009, Degnan, Andrew P.; Tora, George O.; Denhart, Derek J.; Vrudhula, Vivekananda M.; Macor, John E.; Bronson, Joanne J. published a patent.Synthetic Route of 141940-37-6 The title of the patent was Preparation of substituted heterocyclic ethers as inhibitors of NK-1 and SERT and their use in treating CNS disorders. And the patent contained the following:

The invention encompasses compounds of Formula I (wherein R1 is H or alkyl; R2 is H, alkyl, cyanoalkyl, haloalkyl, etc.; R3 is H or alkyl; Ar1 is substituted Ph or pyridinyl; Ar2 is substituted indolyl, indazolyl, benzimidazolyl, or benzotriazolyl), including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders. The compounds of Formula I demonstrate inhibition of neurokinin-1 or serotonin reuptake or both and can be used therefore to treat conditions associated with aberrant levels of tachykinins or serotonin or both. Such conditions are anxiety, depression, obsessive compulsive disorder, bulimia, panic disorder, posttraumatic stress disorder, alc. dependence, or urinary incontinence. Synthetic procedures for preparing I are exemplified. Example compound II, prepared by removing the protecting groups from the corresponding intermediate, had an NK-1 and SERT IC50 values of 0.01-100 nM in binding assays. The experimental process involved the reaction of tert-Butyl (4-(trifluoromethyl)phenyl)carbamate(cas: 141940-37-6).Synthetic Route of 141940-37-6

The Article related to preparation heterocyclic ether nk1 sert inhibitor cns disorder treatment, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Synthetic Route of 141940-37-6

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On January 15, 2009, Degnan, Andrew P.; Tora, George O.; Denhart, Derek J.; Vrudhula, Vivekananda M.; Macor, John E.; Bronson, Joanne J. published a patent.Formula: C12H14F3NO2 The title of the patent was Preparation of substituted heterocyclic ethers as inhibitors of NK-1 and SERT and their use in treating CNS disorders. And the patent contained the following:

The invention encompasses compounds of Formula I (wherein R1 is H or alkyl; R2 is H, alkyl, cyanoalkyl, haloalkyl, etc.; R3 is H or alkyl; Ar1 is substituted Ph or pyridinyl; Ar2 is substituted indolyl, indazolyl, benzimidazolyl, or benzotriazolyl), including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders. The compounds of Formula I demonstrate inhibition of neurokinin-1 or serotonin reuptake or both and can be used therefore to treat conditions associated with aberrant levels of tachykinins or serotonin or both. Such conditions are anxiety, depression, obsessive compulsive disorder, bulimia, panic disorder, posttraumatic stress disorder, alc. dependence, or urinary incontinence. Synthetic procedures for preparing I are exemplified. Example compound II, prepared by removing the protecting groups from the corresponding intermediate, had an NK-1 and SERT IC50 values of 0.01-100 nM in binding assays. The experimental process involved the reaction of tert-Butyl (4-(trifluoromethyl)phenyl)carbamate(cas: 141940-37-6).Formula: C12H14F3NO2

The Article related to preparation heterocyclic ether nk1 sert inhibitor cns disorder treatment, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Formula: C12H14F3NO2

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On October 1, 2015, Patane, Michael published a patent.Quality Control of tert-Butyl (4-(trifluoromethyl)phenyl)carbamate The title of the patent was Compositions and methods for treating or preventing diseases or disorders associated with misregulated eif4e. And the patent contained the following:

Disclosed herein are compounds, compositions, formulations, kits and methods of treatment useful for treating or preventing one or more hyperproliferative disorders, e.g., cancer or a neurol. disease or disorder. The experimental process involved the reaction of tert-Butyl (4-(trifluoromethyl)phenyl)carbamate(cas: 141940-37-6).Quality Control of tert-Butyl (4-(trifluoromethyl)phenyl)carbamate

The Article related to thiazolylpyrazole preparation hyperproliferative cancer neurol eif4e, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Quality Control of tert-Butyl (4-(trifluoromethyl)phenyl)carbamate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On May 1, 2014, Patane, Michael published a patent.Product Details of 141940-37-6 The title of the patent was Compositions and methods for treating or preventing diseases or disorders associated with misregulated eIF-4E. And the patent contained the following:

Disclosed herein are compounds, compositions, formulations, kits and methods of treatment useful for treating or preventing one or more hyperproliferative disorders, e.g., cancer or a neurol. disease or disorder. Compounds of formula I wherein each R1 is independently (halo)alkyl, Cl, etc.; R2 is OH, NH2, aryl, etc.; R3 is H, alkyl, halo, etc; R4 is (un)substituted aryl, etc.; are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their anti-proliferative activity (some data given). The experimental process involved the reaction of tert-Butyl (4-(trifluoromethyl)phenyl)carbamate(cas: 141940-37-6).Product Details of 141940-37-6

The Article related to thiazolylpyrazole preparation hyperproliferative cancer neurol eif4e, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Product Details of 141940-37-6

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On December 1, 2008, Stiff, Cory; Graber, David R.; Thorarensen, Atli; Wakefield, Brian D.; Marotti, Keith R.; Melchior, Earline P.; Sweeney, Michael T.; Han, Fusen; Rohrer, Douglas C.; Zurenko, Gary E.; Romero, Donna L. published an article.Synthetic Route of 141940-37-6 The title of the article was Bacterial translation inhibitors, 1-acylindazol-3-ols as anthranilic acid mimics. And the article contained the following:

The discovery and initial optimization of a novel anthranilic acid derived class of antibacterial agents has been described in a recent series of papers. This paper describes the discovery of 1-acylindazol-3-ols as a novel bioisostere of an anthranilic acid. The synthesis and structure-activity relationships of the indazol bioisosteres are described herein. The experimental process involved the reaction of tert-Butyl (4-(trifluoromethyl)phenyl)carbamate(cas: 141940-37-6).Synthetic Route of 141940-37-6

The Article related to acylindazolol preparation bacterial translation inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Synthetic Route of 141940-37-6

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On May 11, 2021, Riechert, Eva; Kmietczyk, Vivien; Stein, Frank; Schwarzl, Thomas; Sekaran, Thileepan; Juergensen, Lonny; Kamuf-Schenk, Verena; Varma, Eshita; Hofmann, Christoph; Rettel, Mandy; Guer, Kira; Oelschlaeger, Julie; Kuehl, Friederike; Martin, Judit; Ramirez-Pedraza, Marta; Fernandez, Mercedes; Doroudgar, Shirin; Mendez, Raul; Katus, Hugo A.; Hentze, Matthias W.; Voelkers, Mirko published an article.Related Products of 2358-84-1 The title of the article was Identification of dynamic RNA-binding proteins uncovers a Cpeb4-controlled regulatory cascade during pathological cell growth of cardiomyocytes. And the article contained the following:

RNA-binding proteins (RBPs) control critical aspects of cardiomyocyte function, but the repertoire of active RBPs in cardiomyocytes during the growth response is largely unknown. We define RBPs in healthy and diseased cardiomyocytes at a system-wide level by RNA interactome capture. This identifies 67 cardiomyocyte-specific RBPs, including several contractile proteins. Furthermore, we identify the cytoplasmic polyadenylation element-binding protein 4 (Cpeb4) as a dynamic RBP, regulating cardiac growth both in vitro and in vivo. We identify mRNAs bound to and regulated by Cpeb4 in cardiomyocytes. Cpeb4 regulates cardiac remodeling by differential expression of transcription factors. Among Cpeb4 target mRNAs, two zinc finger transcription factors (Zeb1 and Zbtb20) are discovered. We show that Cpeb4 regulates the expression of these mRNAs and that Cpeb4 depletion increases their expression. Thus, Cpeb4 emerges as a critical regulator of cardiomyocyte function by differential binding to specific mRNAs in response to pathol. growth stimulation. The experimental process involved the reaction of Oxybis(ethane-2,1-diyl) bis(2-methylacrylate)(cas: 2358-84-1).Related Products of 2358-84-1

The Article related to cpeb rna binding protein cardiomyocyte cell growth, cpeb4, rbps, zeb1, cardiomycoytes, pathological hypertrophy, Mammalian Pathological Biochemistry: Cardiovascular Diseases and other aspects.Related Products of 2358-84-1

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On May 31, 2022, Wang, Shengxuan; Liu, Tingjun; Sun, Lili; Du, Hongxia; Xu, Zhongjin; Li, Ranran; Yu, Ying; Mao, Yongjiang; Shi, Kerong published an article.Application of 2358-84-1 The title of the article was Menin regulates lipid deposition in mouse hepatocytes via interacting with transcription factor FoxO1. And the article contained the following:

Non-alc. fatty liver disease (NAFLD) is rapidly being recognized as the leading cause of chronic liver disease worldwide. Men1, encoding protein of menin, is a key causative gene of multiple endocrine neoplasia type 1 syndrome including pancreatic tumor. It is known that insulin that secretes by endocrine tissue pancreatic islets plays a critical role in hepatic metabolism Mouse model of hemizygous deletion of Men1 was shown to have severe hepatic metabolism disorders. However, the mol. function of menin on lipid deposition in hepatocytes needs to be further studied. Transcriptome sequencing does show that expression suppression of Men1 in mouse hepatocytes widely affect signaling pathways involved in hepatic metabolism, such as fatty acid metabolism, insulin response, glucose metabolism and inflammation. Further mol. studies indicates that menin overexpression inhibits expressions of the fat synthesis genes Srebp-1c, Fas, and Acc1, the fat differentiation genes Pparγ1 and Pparγ2, and the fat transport gene Cd36, thereby inhibiting the fat accumulation in hepatocytes. The biol. process of menin regulating hepatic lipid metabolism was accomplished by interacting with the transcription factor FoxO1, which is also found to be critical for lipid metabolism Moreover, menin responds to insulin in hepatocytes and mediates its regulatory effect on hepatic metabolism Our findings suggest that menin is a crucial mediation factor in regulating the hepatic fat deposition, suggesting it could be a potential important therapeutic target for NAFLD. The experimental process involved the reaction of Oxybis(ethane-2,1-diyl) bis(2-methylacrylate)(cas: 2358-84-1).Application of 2358-84-1

The Article related to menin lipid deposition hepatocyte transcription factor, foxo1, hepatocyte, lipid metabolism, menin, non-alcoholic fatty liver disease (nafld), Mammalian Pathological Biochemistry: Digestive Tract Diseases and other aspects.Application of 2358-84-1

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On July 2, 2009, Nazare, Marc; Zech, Gernot; Goerlitzer, Jochen; Just, Melitta; Weiss, Tilo; Hessler, Gerhard; Czechtizky, Werngard; Ruf, Sven published a patent.Synthetic Route of 53838-27-0 The title of the patent was Preparation of pyrazole-carboxamide derivatives as P2Y12 antagonists for treating cardiovascular disorders. And the patent contained the following:

The present invention relates to compounds of the formula I (wherein D is 3-15-membered heterocyclyl, (C6-C14)-aryl, etc.; Q and Z are -(C0-C4)-alkylene-O-(C0-C4)-alkylene-; -(C0-C4)-alkylene-SO2-(C0-C4)-alkylene-, etc.; J is H, (C1-C6)-alkyl, etc.; A is a covalent bond, (C1-C8)-alkylene, etc.; B is a covalent bond, (C2-C10)alkenyl, etc.; V is (un)substituted monocyclic or bicyclic 3-15-membered heterocyclyl; G is a covalent bond, (C2-C10)-alkenyl, etc.; M is H, (C1-C8)-alkyl, etc.; R1 is H or (C1-C4)alkyl; R2 is H, (C1-C6)alkyl, etc.). The compounds of the formula I are valuable pharmacol. active compounds They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable e.g. for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them. Example compound II was prepared in a multistep synthesis that culminated in the conversion of the 5-(1-ethoxycarbonyl-cyclobutoxy) intermediate to II. In a human P2Y12 recombinant cell membrane binding assay, II had an IC50 of 0.601 μM. The experimental process involved the reaction of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate(cas: 53838-27-0).Synthetic Route of 53838-27-0

The Article related to pyrazole carboxamide derivative preparation p2y12 antagonist treatment cardiovascular disorder, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Synthetic Route of 53838-27-0

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On March 2, 2006, Andrzej, Roman Batt; Baxter, Andrew John; Heeney, Celine; Stockley, Martin Lee; Bryan Roe, Michael; Hudson, Peter; Handy, Rachel published a patent.Electric Literature of 53838-27-0 The title of the patent was Preparation of tetraaza-benzo[f]azulenes as vasopressin V1a antagonists. And the patent contained the following:

The title compounds I [G = NR5R6, II-V; A1 = CH2, CH(OH), NH, N(alkyl), O and S; A2 = CH2, CH(OH), C(O), NH; A3, A12 = S, NH, N(alkyl), etc.; A4, A13 = CR9, N; A5, A14 = CR10, N; A6 = CH2, NH, N(alkyl), O; A7, A11 = C, N; A8, A9 = CH, N, NH, S, etc.; A10 = CH:CH, CH, N, NH, etc.; the ring constituted by A7-A11 is aromatic; R1-R3 = H, alkyl, O(alkyl), NO2, F, Cl, Br; R4 = H, alkyl, aryl, heteroaryl, etc.; R5, R6 = alkyl, aryl, (CH2)f-aryl, (CH2)f-heteroaryl; R9, R10 = H, alkyl, alkoxy, etc.; W = O, NH; X = (CH2)m, C(O), SOj; Y = O, S, NH, N(alkyl); a, f, j = 1-2; m = 0-2; with provisos] which are vasopressin V1a receptor antagonists, were prepared and formulated. E.g., a multi-step synthesis of 4-(3,3-dimethylbutyl)piperazine-1-carboxylic acid 4-(3,6-dimethyl-4,10-dihydro-3H-2,3,4,9-tetraaza-benzo[f]azulene-9-carbonyl)-2-fluorobenzylamide, starting from 4-(tert-butoxycarbonylamino-methyl)-3-fluorobenzoic acid and 3,6-dimethyl-3,4,9,10-tetrahydro-2,3,4,9-tetraazabenzo[f]azulene (preparations of the reactants was provided), was given. Compounds I were assayed to determine their ability to inhibit the cellular consequences of AVP stimulation on intact cells. In the assay, compounds I cause significant inhibition of cellular activation at concentrations of 30 μM or less. Preferred compounds I cause significant inhibition at concentrations of 300 nM. Pharmaceutical compositions of the compounds I are useful as treatment of dysmenorrhea. The experimental process involved the reaction of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate(cas: 53838-27-0).Electric Literature of 53838-27-0

The Article related to benzoazulene tetraaza triaza preparation vasopressin v1a antagonist dysmenorrhea treatment, Heterocyclic Compounds (More Than One Hetero Atom): Diazepines and other aspects.Electric Literature of 53838-27-0

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics