207405-68-3

Usage

Uses

Used in Pharmaceutical Industry:
N-Boc-endo-3-aminotropane is used as a reagent for the synthesis of tropane-derived CCR5 receptor antagonists. These antagonists are essential in the development of medications targeting various diseases, including HIV and certain types of cancer. The compound's role in this process is vital for creating effective treatments and therapies.

Upstream product

• 28957-72-4 N-benzylnortropinone 
• 24424-99-5 di-tert-butyl dicarbonate 
• 542-05-2 acetonedicarboxylic acid 
• 944123-76-6 1,1-Dimethylethyl 3-[(phenylmethyl)amino]-8-azabicyclo[3.2.1]octane-8-carboxylate 
• 185099-67-6 Boc-tropinone 
• 185099-67-6 N-Boc-nortropinone 
• 207405-67-2 1,1-dimethylethyl endo-3-[(phenylmethyl)amino]-8-azabicyclo[3.2.1]octane-8-carboxylate 

Downstream Products

• 716358-99-5 endo-tert-butyl (1R,5S)-3-{[4-(methylsulfonyl)-2-nitrophenyl]amino}-8-azabicyclo[3.2.1]octane-8-carboxylate 
• 280762-06-3 endo-tert-butyl 3-[(2-nitrophenyl)amino]-8-azabicyclo[3.2.1]octane-8-carboxylate 
• 1397287-30-7 (rac)-(3-endo)-3-[4-(4-Chloro-benzyl)-6-(1-hydroxy-1-methyl-ethyl)-pyrimidin-2-ylamino]-8-aza-bicyclo[3.2.1]octane-8-carboxylic acid tert-butyl ester 
• 1424328-50-6 C₂₃H₃₀N₆O₆S 
• 1424328-52-8 endo-tert-butyl 3-(6-(2-fluoro-4-(methylsulfonyl)phenylamino)-5-nitropyrimidin-4-ylamino)-8-azabicyclo[3.2.1]octane-8-carboxylate 
• 866933-46-2 Velusetrag 

Relevant academic research and scientific papers

1-(3-AMINOPROPYL) SUBSTITUTED CYCLIC AMINE COMPOUNDS, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITIONS AND USES THEREOF

Provided are 1-(3-aminopropyl) substituted cyclic amine compounds as represented by formula (I), pharmaceutically acceptable salts, enantiomers, diastereoisomers, racemates and mixtures thereof, and a method of synthesizing said 1-(3-aminopropyl) substituted cyclic amine compounds by using aromatic heterocyclic formaldehyde as raw material. Said compounds can be used as CCR 5 antagonist for the treatment of HIV infection.

ANTIMICROBIAL COMPOSITIONS, METHODS OF USE, AND METHODS OF TREATMENT OF INFECTIONS

The present disclosure provides compositions including a compound (e.g., compounds A-D), pharmaceutical compositions including the compound, methods of treatment of a condition (e.g., an infection) or disease, methods of treatment using compositions or pharmaceutical compositions, and the like.

INHIBITORS OF CYCLIN-DEPENDENT KINASE 7 (CDK7)

The present invention provides novel compounds of Formula (I) and Formula (II), and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g.,leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g., cyclin-dependent kinase 7 (CDK7)), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject. (I)

CEPHEM COMPOUND HAVING CATECHOL GROUP

A compound of the formula: wherein X is -N=, -CH=, or the like; W is -CH2- or the like; U is -S- or the like; R1 and R2 are each independently hydrogen, halogen, optionally substituted lower alkyl, or the like; R3/su

BRIDGED PIPERIDINE DERIVATIVES

The present invention relates to compounds of formula (l); hetaryl I is a five or six membered heteroaryl group, containing 1 to 3 heteroatoms, selected from S or N; hetaryl II is a six membered heteroaryl group, containing 1 to 3 heteroatoms, selected from S or N, or is a two membered ring system containing 1 to 4 heteroatoms selected from S, or N, wherein at least one ring is aromatic in nature; R1 is lower alkyl, lower alkoxy, lower alkyl substituted by halogen or halogen; R2 is lower alkyl, lower alkyl substituted by halogen, halogen, lower alkoxy, cycloalkyl substituted by lower alkyl or lower alkyl substituted by halogen, or is lower alkyl substituted by hydroxy, or is furyl, or is O-benzyl, (CH2)p-phenyl, optionally substituted by halogen, lower alkoxy, lower alkyl substituted by halogen, lower alkyl or by cyano; R3 is hydrogen or lower alkyl; Y is (CH2)n-, -CH2OCH2-, -CH2O-, CH2S-, -CH2SCH2- and is bonded to two of the ring carbon atoms, bonding being to either the ring carbon atoms a and b or the ring carbon atoms c and d; p is 0 or 1; m is 0, 1 or 2; if m is 2 then R1 may be the same or different; -75- n is 2 or 3; o is 0, 1 or 2, if o is 2, then R2 may be the same or different; or to pharmaceutically active acid addition salts thereof. The present compounds of formula I are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of β-amyloid in the brain, in particular Alzheimers disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.

Novel 4,4-disubstituted piperidine-based C-C chemokine receptor-5 inhibitors with high potency against human immunodeficiency virus-1 and an improved human ether-a-go-go related gene (hERG) profile

We recently described (J. Med. Chem. 2008, 51, 6538-6546) a novel class of CCR5 antagonists with strong anti-HIV potency. Herein, we detail SAR converting leads 1 and 2 to druglike molecules. The pivotal structural motif enabling this transition was the secondary sulfonamide substituent. Further finetuning of the substituent pattern in the sulfonamide paved the way to enhancing potency and bioavailability and minimizing hERG inhibition, resulting in discovery of clinical compound 122 (GSK163929).

Prokinetic agent for bowel preparation

The invention provides methods of bowel preparation before a diagnostic, surgical or therapeutic procedure, in particular, bowel preparation before a colonoscopy procedure, using a 5-HT4 receptor agonist as a prokinetic agent.

Discovery of bioavailable 4,4-disubstituted piperidines as potent ligands of the chemokine receptor 5 and inhibitors of the human immunodeficiency virus-1

We describe robust chemical approaches toward putative CCR5 scaffolds designed in our laboratories. Evaluation of analogues in the 125I-[MIP-1β] binding and Ba-L-HOS antiviral assays resulted in the discovery of 64 and 68 in the 4,4-disubstitited piperidine class H, both potent CCR5 ligands (pIC50 = 8.30 and 9.00, respectively) and HIV-1 inhibitors (pIC50 = 7.80 and 7.84, respectively, in Ba-L-HOS assay). In addition, 64 and 68 were bioavailable in rodents, establishing them as lead molecules for further optimization toward CCR5 clinical candidates.

CARBAMATE COMPOUNDS AS 5-HT4 RECEPTOR AGONISTS

The invention provides novel benzoimidazolone-carboxamide-derived carbamate 5-HT4 receptor agonist compounds of formula (I): wherein R1, R2, R3, R4, a, and b are defined in the disclosure. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.

Quinolinone compounds as 5-HT4 receptor agonists

The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.