115652-52-3

Upstream product

• 107017-73-2 tert-butyl (1-(hydroxymethyl)cyclopropyl)carbamate 
• 308266-11-7 1-(benzyloxymethyl)-1-(dibenzylamino)cyclopropane 

Downstream Products

• 861648-82-0 [1-(3,5-dichlorophenylamino)cyclopropyl]methanol 
• 218594-09-3 1-(N-benzylamino)-1-cyclopropanemethanol 
• 107017-73-2 tert-butyl (1-(hydroxymethyl)cyclopropyl)carbamate 
• 1337527-08-8 benzyl (R)-3-((R)-2,3-didodecanamidopropylthio)-1-(1-(hydroxymethyl)cyclopropylamino)-1-oxopropan-2-ylcarbamate 

Relevant academic research and scientific papers

SMALL MOLECULE CORRECTORS OF MAMMALIAN SLC6A8 FUNCTION

Disclosed are compounds, compositions, and methods useful for treating or preventing a disease or disorder associated with mutation in a protein.

Heterocyclic compound serving as SOS1 inhibitor

The invention provides a compound serving as an SOS1 inhibitor, and particularly provides a compound with a structure as shown in a formula (I), or an optical isomer, a pharmaceutically acceptable salt, a prodrug, a deuterated derivative, a hydrate and a solvate of the compound. The compound can be used for treating or preventing diseases or symptoms related to the activity or expression quantity of SOS1.

COMBINATIONS OF MEDICAMENTS, CONTAINING PDE4-INHIBITORS AND EP4-RECEPTOR-ANTAGONISTS

The present invention relates to new medicament combinations which contain in addition to one or more PDE4-inhibitors (1) at least one EP4 receptor antagonist (2), as well as the use thereof for the treatment of preferably respiratory complaints such as particularly COPD, chronic sinusitis and asthma. The invention relates in particular to those medicament combinations which contain at least one EP4 receptor antagonist (2), in addition to one or more, preferably one, PDE4 inhibitor of general formula 1 wherein X is SO or SO2, but preferably SO, and wherein R3 denotes an optionally substituted, mono- or bicyclic, unsaturated, partly saturated or saturated heterocyclic group or an optionally substituted, mono- or bicyclic heteroaryland wherein R1 and R2 have the meanings given in claim 1, the preparation thereof and the use thereof for the treatment of respiratory complaints.

SUBSTITUTED PIPERAZINO-DIHYDROTHIENOPYRIMIDINES

The invention relates to new piperidino-dihydrothienopyrimidines of formula 1, as well as pharmacologically acceptable salts thereof, wherein X is SO or SO2, but preferably SO, and wherein R1, R2, R3 and R4 may have the meanings given in claim 1, as well as pharmaceutical compositions which contain these compounds. These new piperidino-dihydrothienopyrimidines are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system or cancers.

NOVEL PHENYL-SUBSTITUTED PIPERAZINO-DIHYDROTHIENOPYRIMIDINES

The invention relates to novel dihydrothienopyrimidines of the formula 1, and to pharmacologically acceptable salts thereof, formula (1) in which X is SO or SO2, but preferably SO, and either R3 is a monosubstituted phenyl ring in the ortho position or in the meta position, or R3 is a phenyl ring bisubstituted in any positions, and pharmaceutical compositions which comprise these compounds. These novel dihydrothienopyrimidines are suitable for the treatment of respiratory or gastrointestinal symptoms or disorders, inflammatory disorders of the joints, of the skin or of the eyes, disorders of the peripheral or central nervous system or cancers.

NOVEL PIPERAZINO-DIHYDROTHIENO-PYRIMIDINE DERIVATIVES

The invention relates to the novel dihydrothienopyrimidine sulfoxides of formula (I) and to the pharmacologically acceptable salts thereof, wherein X represents SO or SO2 , preferably however SO, and wherein R3, R4, R4', R5, R6 and R7 are defined as in claim 1. The invention also relates to pharmaceutical compositions containing said compounds. The novel dihydrothienopyrimidine sulfoxides are suitable for use in the treatment of respiratory or gastrointestinal disorders or diseases, inflammatory diseases of the joints, the skin or the eyes, diseases of the peripheral or central nervous system or cancers

HETEROCYCLE-SUBSTITUTED PIPERAZINO-DIHYDROTHIENOPYRIMIDINES

The invention relates to new dihydrothienopyrimidinesulphoxides of formula 1, as well as pharmacologically acceptable salts thereof, wherein X is SO or SO2, but preferably SO, and wherein R3 denotes an optionally substituted, mono- or bicyclic, unsaturated, partially saturated or saturated heterocycle or an optionally substituted, mono- or bicyclic heteroaryl and wherein R1 and R2 have the meanings stated in claim 1, as well as pharmaceutical compositions which contain these compounds. These new dihydrothienopyrimidinesulphoxides are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system or cancers.

Synthesis of spirocyclopropanated analogues of iprodione

Methyl 1-(tert-butoxycarbonylamino)cyclopropanecarboxylate (9) was converted into the spirocyclopropanated five-membered ring analogue 7a of Iprodione (1) in five steps with an overall yield of 28%. The spirocyclopropanated five-membered ring analogue 8a was prepared from tert-butyl N-[1-(hydroxymethyl)cyclopropyl]carbamate (10) in five steps with an overall yield of 19%. En route to the spirocyclopropanated six-membered ring analogues of Iprodione (1), the oxalic acid diamides 5b and 6b could be obtained starting from 9 or 10 in 33 or 19% yield, respectively. Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2005.

Cyclopropyl building blocks for organic synthesis, 58(+): A new short access to amino acids incorporating an aminocyclopropyl moiety from N,N-dibenzylcarboxamides

Our recently reported titanium-mediated transformation of N,N-dialkylcarboxamides to cyclopropylamines has been applied to N,N-dibenzyl-2-benzyloxyacetamide using a variety of alkylmagnesium bromides to yield 1-(benzyloxymethyl)-1-(dibenzylamino)cyclopropane (15a, 48percent) and 2-substituted analogs 15b-f (33-48percent). These have been transformed in just a few steps into N-Boc-protected methyl esters of 1-aminocyclopropanecarboxylic acid (1, 29percent overall), coronamic acid (2, 35percent) and norcoronamic acid (21percent), 2,3-methanoglutamic acid (21g, 19percent) and 2,3-methanoornithine (211, 12percent). Similarly, the corresponding derivatives of 3,4-methano-γ-aminobutyric acid (26, 23percent) and 4-spirocyclopropane-γ-butyrolactam (32, 44percent) have been synthesized.

New "Ofloxacin" Type Antibacterial Agents. Incorporation of the Spiro Cyclopropyl Group at N-1

The first example incorporating a spiro cyclopropyl group into an "ofloxacin" type of quinolone antibacterial agent has been prepared by potassium fluoride mediated ring closure of the hydroxymethyl cyclopropyl intermediate to give 9'-fluoro-7'-oxo-10'-(1-piperazinyl)spiropyridobenzoxazine>-6'-carboxylic acid.Analogues were made by substitution at C-7 by various complex amines.Evaluation of these compounds for antibacterial activity was carried out.All examples prepared and examined showed in vitro minimum inhibitory values and in vivo mouse protection results to be diminished as compared to the parent, ofloxacin.