- COMPOSITIONS AND METHODS OF MAKING EXPANDED HEMATOPOIETIC STEM CELLS USING DERIVATIVES OF CARBAZOLE
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This invention is directed to, inter alia, compounds, methods, systems, and compositions for the maintenance, enhancement, and expansion of hematopoietic stem cells derived from one or more sources of CD34+ cells. Sources of CDS 4+ cells include bone marrow, cord blood, mobilized peripheral blood, and non-mobilized peripheral blood. Also provided herein are compounds of Formula I which are useful in maintaining, enhancing, and expanding of hematopoietic stem cells.
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Paragraph 0168
(2020/11/12)
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- Direct conversion of phenols into primary anilines with hydrazine catalyzed by palladium
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Primary anilines are essential building blocks to synthesize various pharmaceuticals, agrochemicals, pigments, electronic materials, and others. To date, the syntheses of primary anilines mostly rely on the reduction of nitroarenes or the transition-metal-catalyzed Ullmann, Buchwald-Hartwig and Chan-Lam cross-coupling reactions with ammonia, in which non-renewable petroleum-based chemicals are typically used as feedstocks via multiple step syntheses. A long-standing scientific challenge is to synthesize various primary anilines directly from renewable sources. Herein, we report a general method to directly convert a broad range of phenols into the corresponding primary anilines with the cheap and widely available hydrazine as both amine and hydride sources with simple Pd/C as the catalyst.
- Qiu, Zihang,Lv, Leiyang,Li, Jianbin,Li, Chen-Chen,Li, Chao-Jun
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p. 4775 - 4781
(2019/05/16)
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- Deacetylative Amination of Acetyl Arenes and Alkanes with C-C Bond Cleavage
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The Br?nsted acid-catalyzed synthesis of primary amines from acetyl arenes and alkanes with C-C bond cleavage is described. Although the conversion from an acetyl group to amine has traditionally required multiple steps, the method described herein, which uses an oxime reagent as an amino group source, achieves the transformation directly via domino transoximation/Beckmann rearrangement/Pinner reaction. The method was also applied to the synthesis of γ-aminobutyric acids, such as baclophen and rolipram.
- Hyodo, Kengo,Hasegawa, Genna,Maki, Hiroya,Uchida, Kingo
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supporting information
p. 2818 - 2822
(2019/04/25)
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- Copper(II) catalyzed aromatization of tetrahydrocarbazole: An unprecedented protocol and its utility towards the synthesis of carbazole alkaloids
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An efficient protocol for the aromatization of tetrahydrocarbazole is described by using catalytic copper(II) chloride dihydrate in DMSO. This newly established methodology has utilized towards the synthesis of naturally occurring carbazole alkaloids, namely 3-methylcarbazole, 3-formyl carbazole, glycozoline, glycozolicine and clauszoline-K. In addition, the protocol is generalized for the aromatization of N-substituted tetrahydrocarbazole, 1,2,3,4-tetrahydroquinoline, 1,2,3,4-tetrahydroisoquinoline and 1,2,3,4-tetrahydro β-carboline to give the corresponding heteroaromatic compounds from very good to excellent yield. Moreover, this method has been proven to be tolerant to a broad range of functional groups with excellent yields.
- Dalvi, Bhakti A.,Lokhande, Pradeep D.
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supporting information
p. 2145 - 2149
(2018/05/08)
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- Design, synthesis, and evaluation of potent Wnt signaling inhibitors featuring a fused 3-ring system
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The Wnt signaling pathway is a critical developmental pathway which operates through control of cellular functions such as proliferation and differentiation. Aberrant Wnt signaling has been linked to the formation and metastasis of tumors. Porcupine, a member of the membrane-bound O-acyltransferase family of proteins, is an important component of the Wnt pathway. Porcupine catalyzes the palmitoylation of Wnt proteins, a process needed for their secretion and activity. Here we report a novel series of compounds obtained by a scaffold hybridization strategy from a known porcupine inhibitor class. The leading compound 59 demonstrated subnanomolar inhibition of Wnt signaling in a paracrine cellular assay. Compound 59 also showed excellent chemical, plasma and liver microsomal stabilities. Furthermore, compound 59 exhibited good pharmacokinetic profiles with 30% oral bioavailability in rat. Collectively, these results strongly support further optimization of this novel scaffold to develop better Wnt pathway inhibitors.
- Xu, Zhixiang,Li, Jiajun,Wu, Yiyuan,Sun, Zhijian,Luo, Lusong,Hu, Zhilin,He, Sudan,Zheng, Jiyue,Zhang, Hongjian,Zhang, Xiaohu
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p. 154 - 165
(2015/12/04)
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- Recyclable copper catalyzed nitrogenation of biphenyl halides: A direct approach to carbazoles
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A novel A21-CuI catalyzed direct nitrogenation of biphenyl halides for the direct synthesis of carbazoles via a direct C-H amination process has been developed. A recyclable and inexpensive Cu-catalyst was successfully employed in N-heterocyclic compound synthesis via tandem azidation and C-H amination, which makes this protocol very practical and easy to handle.
- Ou, Yang,Jiao, Ning
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supporting information
p. 3473 - 3475
(2013/05/22)
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- Integrin receptor inhibitors
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Provided are compounds of formula (I) wherein A, Q, W, X, Y, Z, R1 to R4, m and n are as defined herein. Compounds of the invention bind to α4 integrin receptors and thereby inhibit binding of ligands for α4 int
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- Composition of matter having bioactive properties
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Particles of coordinated complex comprising a basic, hydrous polymer and a capacitance adding compound, as well as methods for their production, are described. These complexes exhibit a high degree of bioactivity making them suitable for a broad range of applications through their incorporation into conventional vehicles benefiting from antimicrobial and similar properties.
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- STEROID RECEPTOR MODULATOR COMPOUNDS AND METHODS
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Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
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- STEROID RECEPTOR MODULATOR COMPOUNDS AND METHODS
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Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
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- STEROID RECEPTOR MODULATOR COMPOUNDS AND METHODS
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Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
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- Steroid receptor modulator compounds and methods
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Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
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- STEROID RECEPTOR MODULATOR COMPOUNDS AND METHODS
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Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
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- Steroid receptor modulator compounds and methods
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Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiting steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
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- Tricyclic steroid receptor modulator compounds and methods
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Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
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- Pyrrolo[1',2':1,2]pyrazino[6,5-b]carbazoles
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The synthesis of the new heterocycles pyrrolo[1',2':1,2]pyrazino[6,5-b]carbazoles was achieved by the intramolecular cyclisation of 2-(1-pyrrolyl)carbazole derivatives. These latter compounds were obtained by the Clauson-Kaas reaction starting from the corresponding 2-aminocarbazoles, obtained by reduction of 2-nitrocarbazoles. A study of this reduction has shown that the introduction of acetyl grouping in position 9 makes this reaction easier and gives better results than previous methods. 1H-NMR spectra are studied.
- Lancelot,Gazengel,Rault,Robba
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- 2-Hydrocarbyloxy-pyridine compounds
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Compounds of the formula SPC1 Wherein X is aliphatic, cycloaliphatic, aromatic, aralkyl, hetaryl, hetarylalkyl or hydrogen; Y is aliphatic, aromatic, aralkyl, --COOR1, --COR2, EQU1 --SO2 R2, EQU2 --CN, --NH2, --NO, --NO2 or hydrogen with the proviso that when Y is hydrogen, X is other than hydrogen; Z1 is cyano, EQU3 --NH--OR10, EQU4 --OR12, --SR12 or --SO2 R12 and Z2 is chlorine, bromine, cyano, hydroxy, mercapto, --OR12, --SR12, --SO2 R12, EQU5 --NH--OR10 or EQU6 R1 is aliphatic; R2 is aliphatic, cycloaliphatic, aromatic, aralkyl or heterocyclic; R3 and R4 when taken separately are hydrogen, aliphatic, cycloaliphatic, aromatic or aralkyl; R3 and R4 when taken together with the nitrogen atom to which they are attached form a heterocyclic moiety; R5 and R6 when taken separately are aliphatic, aromatic, aralkyl, heterocyclic or hydrogen; R5 and R6 when taken together with the nitrogen atom to which they are attached are heterocyclic; R7 is hydrogen, aliphatic or aromatic; R8 and R9 are aliphatic or aromatic, R10 is hydrogen, aliphatic or aralkyl, R11 is aliphatic and R12 is aliphatic, aromatic or aralkyl; R10 and R11 when taken together with the nitrogen atom to which they are attached are heterocyclic.
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