Category: 1198284-94-4

On August 23, 2018, Fan, Mengyang; Qin, Luoheng; Wei, Yi; Zhou, Guoqiang; Zhou, Jingye published a patent.Synthetic Route of 1198284-94-4 The title of the patent was Preparation of aminopyrimidine compounds as SSAO inhibitors. And the patent contained the following:

The invention provides compounds of the formula I (wherein R1 is substituted piperidinyl, substituted 2,8-diazaspiro[4.5]decan-1-one, substituted piperazinyl, etc.) and pharmaceutically acceptable salts of the compounds, methods of treating patients for liver disease, and processes for preparing the compounds Example compound II�HCl was prepared by BOC-deprotection of tert-Bu N-[(E)-3-fluoro-2-[[2-(2-methyl-1-oxo-2,8-diazaspiro[4.5]decan-8-yl)pyrimidin-5-yl]oxymethyl]allyl]carbamate. The invention compounds were evaluated for their SSAO inhibitory activities (some data given). The experimental process involved the reaction of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate(cas: 1198284-94-4).Synthetic Route of 1198284-94-4

The Article related to aminopyrimidine preparation ssao inhibitor nonalcoholic steatohepatitis, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Synthetic Route of 1198284-94-4

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

On August 23, 2018, Fan, Mengyang; Qin, Luoheng; Wei, Yi; Zhou, Guoqiang; Zhou, Jingye published a patent.Product Details of 1198284-94-4 The title of the patent was Preparation of aminopyrimidine compounds useful as semicarbazide-sensitive amino oxidase (SSAO) inhibitors. And the patent contained the following:

The invention provides compounds of the formula I (wherein R1 is substituted piperidinyl, substituted 2,8-diazaspiro[4.5]decan-1-one, substituted piperazinyl, etc.) and pharmaceutically acceptable salts of the compounds, methods of treating patients for liver disease, and processes for preparing the compounds Example compound II�HCl was prepared by BOC-deprotection of tert-Bu N-[(E)-3-fluoro-2-[[2-(2-methyl-1-oxo-2,8-diazaspiro[4.5]decan-8-yl)pyrimidin-5-yl]oxymethyl]allyl]carbamate. The invention compounds were evaluated for their SSAO inhibitory activities (some data given). The experimental process involved the reaction of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate(cas: 1198284-94-4).Product Details of 1198284-94-4

The Article related to aminopyrimidine semicarbazide sensitive amino oxidase inhibitor liver disease, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Product Details of 1198284-94-4

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

On September 1, 2021, Luo, Zhibo; Wang, Lingli; Fu, Zhifei; Shuai, Bin; Luo, Miaorong; Hu, Guoping; Chen, Jian; Sun, Jikui; Wang, Jiansong; Li, Jian; Chen, Shuhui; Zhang, Yang published an article.Application In Synthesis of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate The title of the article was Discovery and optimization of selective RET inhibitors via scaffold hopping. And the article contained the following:

Aberrant alterations of rearranged during transfection (RET) have been identified as actionable drivers of multiple cancers, including thyroid carcinoma and lung cancer. Currently, several approved multikinase inhibitors such as vandetanib and cabozantinib demonstrate clin. activity in patients with RET-rearranged or RET-mutant cancers. However, the observed response rates are only modest and the ‘off-target’ toxicities resulted from the inhibition of other kinases is also a concern. Herein, we designed and synthesized a series of RET inhibitors based on the structure of selective RET inhibitor BLU-667 and investigated their biol. activities. We identified compound I as a novel potent and selective RET inhibitor with improved drug-like properties. Compound I exhibits a selective inhibitory profile with an inhibitory concentration 50 (IC50) of 1.29 nM for RET and 1.97 (RET V804M) or 0.99 (RET M918T) for mutant RETs. The proliferation of Ba/F3 cells transformed with NSCLC related KIF5B-RET fusion was effectively suppressed by compound I (IC50 = 19 nM). Addnl., compound 9 displayed less ‘off-target’ effects than BLU-667. In mouse xenograft models, compound I repressed tumor growth driven by KIF5B-RET-Ba/F3 cells in a dose-dependent manner. Based on its exceptional kinase selectivity, good potency and high exposure in tumor tissues, compound 9 represents a promising lead for the discovery of RET directed therapeutic agents and the study of RET-driven tumor biol. The experimental process involved the reaction of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate(cas: 1198284-94-4).Application In Synthesis of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate

The Article related to pyrimidine derivative synthesis ret inhibitor antitumor agent, lung cancer, papillary thyroid cancer, ret inhibitor, tyrosine kinase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application In Synthesis of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate

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

On December 7, 2011, Lu, Shoufu; Yu, Xinmin published a patent.HPLC of Formula: 1198284-94-4 The title of the patent was Method for preparing diazaspirocyclic compounds. And the patent contained the following:

The invention relates to a process for the preparation of diazaspirocyclic compounds (e.g., I). For instance, substitution of compound II with 1-bromo-3-chloro-propane followed by azidation, heterocyclization, and reduction gave compound I as a white solid. The experimental process involved the reaction of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate(cas: 1198284-94-4).HPLC of Formula: 1198284-94-4

The Article related to diazaspirocyclic compound preparation, Heterocyclic Compounds (One Hetero Atom): Spiro Compounds With One Hetero Atom In Each Ring and other aspects.HPLC of Formula: 1198284-94-4

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

On May 6, 2016, Pasternak, Alexander; Dong, Shuzhi; Gu, Xin; Jiang, Jinlong; Shi, Zhi-Cai; Walsh, Shawn P.; Wu, Zhicai; Yu, Yang; Ferguson, Ronald, II; Guo, Zhiqiang; Frie, Jessica; Suzuki, Takao; Blizzard, Timothy A.; Fu, Qinghong; Vangelder, Kelsey F. published a patent.Related Products of 1198284-94-4 The title of the patent was Spiro[piperidine-azacycle] derivatives as inhibitors of the renal outer medullary potassium channel and their preparation. And the patent contained the following:

The invention provides compounds of formula I and pharmaceutically acceptable salts thereof, which are inhibitor of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention. Compounds of formula I wherein A is CH2, CH2CH2 and CH2CH2CH2; B is CH2 and CH2; X is (un)substituted 4-(tetrazol-1-yl)phenyl, (un)substituted oxoisobenzofuranyl, (un)substituted (tetrazol-1-yl)pyridinyl, etc.; Y is O, NH and a bond; Z is (un)substituted Ph, (un)substituted pyridinyl, (un)substituted pyrimidinyl, etc.; n is 0, 1 and 2; R1 is H, D and OH; R2 is H and D; R3 is H, D and alkyl; R4 is H and D; each R5 is independently oxo and (un)substituted alkyl; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by arylation of 5-[(1R)-2-(2,8-diazaspiro[4.5]dec-8-yl)-1-hydroxyethyl]-4-methyl-2-benzofuran-1(3H)-one with 5-chloro-3-methyl-1,2,4-thiadiazole. The invention compounds were evaluated for their ROMK channel inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value of 0.2508 μM. The experimental process involved the reaction of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate(cas: 1198284-94-4).Related Products of 1198284-94-4

The Article related to spiropiperidine azacycle preparation romk channel inhibitor, Heterocyclic Compounds (One Hetero Atom): Spiro Compounds With One Hetero Atom In Each Ring and other aspects.Related Products of 1198284-94-4

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

On May 6, 2016, Pasternak, Alexander; Dong, Shuzhi; Gu, Xin; Jiang, Jinlong; Shi, Zhi-Cai; Walsh, Shawn P.; Wu, Zhicai; Yu, Yang; Ferguson, Ronald, II; Guo, Zhiqiang; Frie, Jessica; Suzuki, Takao; Blizzard, Timothy A.; Fu, Qinghong; Vangelder, Kelsey F. published a patent.Recommanded Product: tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate The title of the patent was Spiro[piperidine-azacycle] derivatives as inhibitors of the renal outer medullary potassium channel and their preparation. And the patent contained the following:

The invention provides compounds of formula I and pharmaceutically acceptable salts thereof, which are inhibitor of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention. Compounds of formula I wherein A is CH2, CH2CH2 and CH2CH2CH2; B is CH2 and CH2; X is (un)substituted 4-(tetrazol-1-yl)phenyl, (un)substituted oxoisobenzofuranyl, (un)substituted (tetrazol-1-yl)pyridinyl, etc.; Y is O, NH and a bond; Z is (un)substituted Ph, (un)substituted pyridinyl, (un)substituted pyrimidinyl, etc.; n is 0, 1 and 2; R1 is H, D and OH; R2 is H and D; R3 is H, D and alkyl; R4 is H and D; each R5 is independently oxo and (un)substituted alkyl; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by arylation of 5-[(1R)-2-(2,8-diazaspiro[4.5]dec-8-yl)-1-hydroxyethyl]-4-methyl-2-benzofuran-1(3H)-one with 5-chloro-3-methyl-1,2,4-thiadiazole. The invention compounds were evaluated for their ROMK channel inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value of 0.2508 μM. The experimental process involved the reaction of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate(cas: 1198284-94-4).Recommanded Product: tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate

The Article related to spiropiperidine azacycle preparation romk channel inhibitor, Heterocyclic Compounds (One Hetero Atom): Spiro Compounds With One Hetero Atom In Each Ring and other aspects.Recommanded Product: tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate

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

On November 29, 2018, Bellenie, Benjamin Richard; Cheung, Kwai Ming Jack; Davis, Owen Alexander; Hoelder, Swen; Huckvale, Rosemary; Lloyd, Matthew Garth published a patent.Safety of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate The title of the patent was Preparation of 4,6-diamino-quinolin-2(1H)-one derived inhibitors of Bcl6 for treatment of cancer. And the patent contained the following:

The invention relates to compounds of formula I that function as inhibitors of Bcl6 (B-cell lymphoma 6) useful for treatment of disorders involving Bcl6 activity such as proliferative disorders including cancers. Addnl., the invention comprises synthetic processes for the preparation of I and pharmaceutical compositions containing I. Compounds of formula I [wherein X1 = N, CH, C-alkyl, C-halo, etc.; X2 and X3 independently = N, CH, CF, CCl, etc.; R1 = H, CH3, 2-(methoxyethoxy)ethyl, etc.; R2 = 2,3-dichloro-pyridin-4-yl, 2-chloro-4-cyano-pyridin-4-yl, 2-chloro-5-methoxy-pyrimidin-4-yl, etc.; R3 = H, C1-2 alkyl, cyano, etc.; R4 = cyano, C1-4 alkyl, C1-4 haloalkyl, etc.; R5 = H, C1-4 alkyl, cyano, nitro, acetylenyl, Ph, etc.; with provisos] and pharmaceutically acceptable salts or solvates thereof, are claimed and exemplified. Example compound II was prepared from the reaction of 6-amino-1-methyl-4-[(1-methyl-1-pyrimidin-2-ylethyl)amino]quinolin-2-one and 2,4-dichloropyridine-3-carbonitrile under microwave heating for 1 h at 160°C. Pharmacol. activity of I was evaluated using a HTRF assay and Trx-6xHis-Bcl6 derived from the human Bcl6 BRB domain from which II demonstrated a pIC50 value of 7.38 μM. The experimental process involved the reaction of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate(cas: 1198284-94-4).Safety of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate

The Article related to quinolinone diamino derivative preparation inhibitor bcl6 inhibitor cancer, Heterocyclic Compounds (More Than One Hetero Atom): Other 6-Membered Rings, Two Hetero Atoms and other aspects.Safety of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate

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

On December 1, 2011, Noguchi, Toshiya; Ushiyama, Fumihito; Horikiri, Hiromasa; Yamamoto, Keiko; Ono, Naoya; Takayama, Tetsuo; Kamiyama, Tomoko published a patent.Product Details of 1198284-94-4 The title of the patent was Preparation of heterocyclic compounds or salts thereof for use as antibacterial agents. And the patent contained the following:

Disclosed is a medicament having a strong antibacterial activity against Gram-pos. bacteria, Gram-neg. bacteria, and resistant bacteria. A compound represented by formula I [a bond containing dotted line and connecting X2 to Y1 represents single bond or double bond; Z1-6 = N, CR; R = H, (halo)alkoxy, OH, halogen, (halo)alkyl, cycloalkyl, CN, NO2, etc.; X1 = (oxo-containing) C1-4 alkylene; X2 = bonding hand, CH; Y1 = spirocyclic group; X3 = C1-4 alkylene, NR'(CH2)m, SOn, bonding hand; R’ = H, C1-6 alkyl; m, n = 0, 1, 2; R1 = C3-6 cycloalkyl, C3-6 cycloalkenyl, aryl, heterocyclic group] or a salt thereof is useful as an antibacterial agent. Thus, compound II was synthesized through a multistep process and showed antibacterial activity against Staphylococcus aureus (MIC 0.03). The experimental process involved the reaction of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate(cas: 1198284-94-4).Product Details of 1198284-94-4

The Article related to heterocyclic antibacterial agent preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Product Details of 1198284-94-4

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

On June 30, 2011, Badiger, Sangamesh; Behnke, Dirk; Betschart, Claudia; Chaudhari, Vinod; Cotesta, Simona; Hinrichs, Juergen Hans-Hermann; Ofner, Silvio; Pandit, Chetan published a patent.Quality Control of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate The title of the patent was Preparation of diaza-spiro[5.5]undecanes as orexin receptor antagonists. And the patent contained the following:

The title compounds I [A = (un)substituted 8-10 membered fused bicyclic aromatic ring system which may contain from 1-4 heteroatoms selected from N, O and S, wherein the ring system may contain not more than 2 O atoms and not more than 2 S atoms; or A = (un)substituted 5-6 membered monocyclic aromatic ring system which may contain 1-4 heteroatoms selected from N, O and S, wherein the ring system may contain not more than 2 O atoms and not more than 2 S atoms; m = 0-6; n = 0-6; R1, R2 = halo, alkyl, haloalkyl, etc.; X1 = C(O) and X2 = N(LB); or X1 = N(LB) and X2 = C(O); L = C(R7)2; R7 = H, alkyl, haloalkyl, etc.; B = (un)substituted 5-10 membered monocyclic or fused polycyclic aromatic ring system which may contain from 1-4 heteroatoms selected from N, O and S, wherein the ring system may contain not more than 2 O atoms and not more than 2 S atoms], were prepared E.g., a multi-step synthesis of II, starting from indole-3-carboxaldehyde, was described. Exemplified compounds I were tested for inhibition of orexin-1 and orexin-2 receptors binding (data provided). Pharmaceutical compositions comprising the compound I, alone or in combination with other therapeutic agent, were also disclosed. The experimental process involved the reaction of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate(cas: 1198284-94-4).Quality Control of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate

The Article related to diazaspiroundecane preparation orexin receptor antagonist, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Quality Control of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate

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

On January 30, 2014, Ding, Fa-Xiang; Dong, Shuzhi; Frie, Jessica; Gu, Xin; Jiang, Jinlong; Pasternak, Alexander; Tang, Haifeng; Wu, Zhicai; Yu, Yang; Suzuki, Takao published a patent.Category: esters-buliding-blocks The title of the patent was Preparation of 2,8-diazaspiro[4.5]decan-1-one derivatives as inhibitors of the renal outer medullary potassium channel. And the patent contained the following:

The present invention provides compounds of Formula I [ R1 = H, halo, OH or C1-3 alkoxy; m = 0 or 1; n = 1 or 2; R2 = H, oxo, OH, etc.; R3a = H, oxo, C3-4 cycloalkyl, etc.; R3b = H, or C1-3 alkyl; R4 = H or oxo; R5 = H, halo, (un)substituted C1-3 alkyl, etc.; R6 = H or C1-3 alkyl; R7 = H, or (un)substituted C1-3 alkyl; R7b = H or C1-3 alkyl; R8 = H, halo or C1-3 alkyl; R9 = H, F, OH, etc.; R10 = H, halo, CN, etc.; R11 and R12 = H, CH2OH, CH2OCH3 or C1-3 alkyl optionally substituted with 1- 3 of F; R13 = H, SO2Me, (un)substituted C1-3 alkyl, etc.] and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. Compound II was prepared in a multi-step synthesis and had IC50 of 0.01μM in Thallium Flux assay. Compounds I may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention. The experimental process involved the reaction of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate(cas: 1198284-94-4).Category: esters-buliding-blocks

The Article related to diazaspirodecanone preparation romk inhibitor cardiovascular disease treatment, 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.Category: esters-buliding-blocks

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