Category: 1198284-94-4

On October 10, 2013, Betschart, Claudia; Hintermann, Samuel; Behnke, Dirk; Cotesta, Simona; Fendt, Markus; Gee, Christine E.; Jacobson, Laura H.; Laue, Grit; Ofner, Silvio; Chaudhari, Vinod; Badiger, Sangamesh; Pandit, Chetan; Wagner, Juergen; Hoyer, Daniel published an article.SDS of cas: 1198284-94-4 The title of the article was Identification of a Novel Series of Orexin Receptor Antagonists with a Distinct Effect on Sleep Architecture for the Treatment of Insomnia. And the article contained the following:

Dual orexin receptor (OXR) antagonists (DORAs) such as almorexant, 1 (SB-649868), or suvorexant have shown promise for the treatment of insomnias and sleep disorders in several recent clin. trials in volunteers and primary insomnia patients. The relative contribution of antagonism of OX1R and OX2R for sleep induction is still a matter of debate. We therefore initiated a drug discovery project with the aim of creating both OX2R selective antagonists and DORAs. Here we report that the OX2R selective antagonist 26 induced sleep in mice primarily by increasing NREM sleep, whereas the DORA suvorexant induced sleep largely by increasing REM sleep. Thus, OX2R selective antagonists may also be beneficial for the treatment of insomnia. The experimental process involved the reaction of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate(cas: 1198284-94-4).SDS of cas: 1198284-94-4

The Article related to preparation orexin receptor antagonist sleep insomnia, Pharmacology: Structure-Activity and other aspects.SDS of cas: 1198284-94-4

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

On August 8, 2019, Khan, M. Amin published a patent.SDS of cas: 1198284-94-4 The title of the patent was Preparation of spiro-lactam NMDA receptor modulators and uses thereof. And the patent contained the following:

The title compounds I [R1 = (independently) H, alkyl, C(O)alkyl, etc.; q = 0-3; R3 = H, alkyl, C(O)R31, C(O)OR32; R6, if present, = (independently) H, (un)substituted alkyl, OH, halo; m = 0-4; R31 and R32 = (independently) H, (un)substituted alkyl, cycloalkyl] or pharmaceutically acceptable salts and/or stereoisomers thereof, having potency in the modulation of NMDA receptor activity, and therefore useful in the treatment of conditions such as depression and related disorders as well as other disorders, were prepared and/or claimed. E.g., a multi-step synthesis of II, starting from piperidine-4-carboxylic acid, was described. Exemplified compounds I were evaluated in the NMDA receptor agonist assays (data given). Representative compounds I were also tested in the pharmacokinetics assays (data given). Pharmaceutical composition comprising compound I was disclosed. The experimental process involved the reaction of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate(cas: 1198284-94-4).SDS of cas: 1198284-94-4

The Article related to spiro lactam pren nmda receptor modulator antidepressant pharmacokinetic, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.SDS of cas: 1198284-94-4

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

On March 24, 2016, Semeraro, Teresa; Tarsi, Luca; Micheli, Fabrizio; Luker, Tim; Cremonesi, Susanna published a patent.Category: esters-buliding-blocks The title of the patent was Preparation of 2-[bis(4-fluorophenyl)methyl]-2,7-diazaspiro[4.5]decan-10-one derivatives useful as inhibitors of human dopamine active transporter (DAT) protein. And the patent contained the following:

The invention relates to compounds of formula I, and in particular 2-[bis(4-fluorophenyl)methyl]-2,7-diazaspiro[4.5]decan-10-one derivatives and related compounds, method for their preparation and their use as inhibitors of human dopamine active transporter (DAT) protein for the treatment of sexual dysfunction, affective disorders, anxiety, depression, attention deficit hyperactivity disorder (ADHD), obesity, etc. Compounds of formula I, wherein Q is C=NOH, NH, Ncycloalkyl, etc.; X is CO, NH, Nalkyl, etc.; Y is O, SO0-2, Nalkyl, etc.; Z is O, S and CR11R12; A is (CHR5R6)0-2; B is (CR1R2)0-2; M is (R9R10)0-2; R1 and R2 are independently H, OH, F, alkyl, etc., or R1R2 together form =O; R3, R4, R7 and R8 are independently H, OH, alkoxy and alkyl, or R3 and R4, R7 and R8 may both be O, wherein said O atoms are linked by an alkylene group to form a straight chain or branched alkylenedioxy group; R5 and R6 are independently H and alkyl, or R5 and R6 from =O; R13 is substituted phenyl; R14 is (un)substituted phenyl; R9, R10, R11 and R12 are independently H and alkyl, are claimed. Example compound II was prepared by a multistep procedure (procedure given). All the invention compounds were evaluated for their affinity to the human transporters DAT, NET, SERT and hERG. From the assay, it was determined that example compound II exhibited pIC50 value of 6.89, 5.42, 4.65 and 5.7 towards human transporters DAT, NET, SERT and hERG resp. 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 bisfluorophenylmethyldiazaspirodecanone preparation human dopamine active transporter inhibitor, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Category: esters-buliding-blocks

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

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 June 3, 2021, Gray, Nathanael S.; Hatcher, John M.; Sreevatsan, Prasanna published a patent.Related Products of 1198284-94-4 The title of the patent was Potent and selective azaindole inhibitors of CDK8 and CDK19 for disease treatment. And the patent contained the following:

Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with CDK8 and/or CDK19. 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 cdk8 cdk19 inhibitor azaindole, Pharmacology: Other (All Agents and Effects Not Otherwise Assignable) and other aspects.Related Products of 1198284-94-4

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

On June 11, 2020, Hu, Yonghan; Wu, Dongdong; Peng, Wei; Lu, Liang; Li, Xin; Zhang, Xiuchun; Wang, Ruzhi; Zhu, Sheng; Huang, Bin; Liu, Tao; Zhu, Jinlian; Wu, Yuchuan published a patent.Recommanded Product: 1198284-94-4 The title of the patent was Heterocyclic compound, application and pharmaceutical composition and application. And the patent contained the following:

The invention disclosed a kind of heterocyclic compound, its preparation method and application. The claimed compound is shown in structure I (R1 = H, F, difluoromethyl, OMe, cyclopropyl, etc.; Y1 = N or CH; Y2 = N, CH, C(F), etc.; R9 = H, Me, or difluoromethyl; X1 = N, CH, C(OH), etc.; s,t = 0 or 1; X3 = N; X2 = CH2, or C(O); X4 = hetero atom containing fragment forming heterocycle; X6 = C(O), or CH2. CHR; R = C1-4 alkyl; X5 = N or CH; R6 = H, halo, cyclopropyl, etc.; R7 = H or halo; R8 = (un)substituted C1-4 alkyl, halo, cyclopropyl, oe H). The claimed compound is prepared via multiple steps (procedure given). The prepared compound can be used as RET kinase inhibitor for treating and preventing diseases mediated by abnormal expression of RET such as cancers (papillary thyroid carcinoma, medullary thyroid carcinoma, pheochromocytoma, pancreatic ductal adenocarcinoma, multiple endocrine tumors (also for example MEN2A or MEN2B), breast cancer (also for example metastatic breast cancer), testicular cancer, small cell lung cancer, Non-small cell lung cancer, chronic bone marrow mononuclear leukemia, colon cancer, rectal cancer, ovarian cancer, or salivary adenocarcinoma). 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: 1198284-94-4

The Article related to heterocyclic compound preparation ret kinase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Recommanded Product: 1198284-94-4

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

On April 26, 2012, Badiger, Sangamesh; Behnke, Dirk; Betschart, Claudia; Cotesta, Simona; Hintermann, Samuel; Ofner, Silvio; Pandit, Chetan; Roy, Bernard Lucien published a patent.Synthetic Route of 1198284-94-4 The title of the patent was Preparation of diazaspiro[5.5]undecanes as orexin receptor inhibitors. And the patent contained the following:

The title compounds I [A = (un)substituted 5-6 membered aromatic ring which contain 1-4 heteroatoms selected from N, O and S; m, n = 0-6; R1, R2 = halo alkyl, cycloalkyl, etc.; X1 = C(O) and X2 = N(LB); or X1 = N(LB) and X2 = C(O); L = C(R6)2; R6 = H, alkyl, cycloalkyl, etc.; or two R6 together with the carbon atom to which they are bound form cycloalkyl; B = (un)substituted 5-6 membered monocyclic or 8-10 membered fused bicyclic aromatic ring which may contain 1-4 heteroatoms selected from N, O and S], useful as orexin receptor inhibitors, were prepared E.g., a multi-step synthesis of II, starting from 2,9-diazaspiro[5.5]undecan-1-one trifluoroacetate and 2-chloro-4,6-dimethylpyrimidine, was described. Exemplified compounds I were tested for inhibiting human orexin 1 and human orexin 2 receptors (data given). Pharmaceutical composition comprising the compound I was disclosed. 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 diazaspiroundecane preparation orexin receptor inhibitor, 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 25, 2011, Brain, Christopher Thomas; Cho, Young Shin; Giraldes, John William; Lagu, Bharat; Levell, Julian; Luzzio, Michael; Perez, Lawrence Blas; Wang, Yaping; Yang, Fan published a patent.Recommanded Product: 1198284-94-4 The title of the patent was Preparation of pyrrolopyrimidine derivatives for use as CDK4/6 inhibitors. And the patent contained the following:

Title compounds I [A = CH or N; L = bond, C(O), or S(O)2; R1 = alkyl, (un)substituted cycloalkyl, PH, piperidinyl, or tetrahydropyranyl; R2 = (un)substituted diazabycycloheptanyl, diazaspirononanyl, diazabicyclooctanyl, etc.; R4 = H, D, CH3, etc.; R8, R9, R10, and R11 independently = H or D], and their pharmaceutically acceptable salts, are prepared and disclosed as cyclin-dependent kinases 4 and 6 (CDK4/6) inhibitors. Thus, e.g., II was prepared by a multistep procedure (preparation given). Select I were evaluated in CDK4/cyclin D1 enzymic activity assays, e.g., II demonstrated an IC50 value of 0.008 to 0.016 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: 1198284-94-4

The Article related to pyrimidine pyrrolo derivative preparation cdk4 cdk6 inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Recommanded Product: 1198284-94-4

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

On August 23, 2018, Zhou, Guo Qiang published a patent.SDS of cas: 1198284-94-4 The title of the patent was Preparation of diazaspirodecanyl pyrimidines useful as SSAO inhibitors. And the patent contained the following:

The invention provides compound of formula I and pharmaceutically acceptable salts of the compounds, methods of treating patients for liver disease, and processes for preparing the compounds Example compound (E)-I�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. From the assay, it was determined that compound I(E)-I�HCl exhibited IC50 value of less than 60 nM. The experimental process involved the reaction of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate(cas: 1198284-94-4).SDS of cas: 1198284-94-4

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

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

On October 8, 2020, Fu, Zhifei; Luo, Miaorong; Zhang, Yang; Cai, Yalei; Zhu, Wu; Li, Jian; Chen, Shuhui published a patent.Safety of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate The title of the patent was Nitrogen-containing spiro derivative as RET inhibitor. And the patent contained the following:

The invention disclosed a kind of nitrogen-containing spiro derivative as RET inhibitor. The claimed compound is shown in structure I (T = CN or N; R1,R2,R3 = H, halo, C1-6 alkyl, etc.; R4 = H, amino, hydroxy, etc.; D1,D2 = (un)substituted -CH2CH2-; D3 = methylene, carbonyl, etc.; D4 = ethylene, propylene, -OCH2CH2-, etc.). The claimed compound is prepared via multiple steps (procedure given). The prepared compound can be used as RET inhibitor for treating RET mediated disease. 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 nitrogen containing spiro derivative preparation ret inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines 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