608142-93-4

Upstream product

• 115812-96-9 4-fluoro-3-nitropyridine 
• 57260-71-6 1-t-Butoxycarbonylpiperazine 
• 13091-23-1 4-chloro-3-nitropyridine 

Downstream Products

• 170017-74-0 1-[1,1-dimethylethoxycarbonyl]-4-(2-aminophenyl)piperazine 
• 1405126-16-0 2-(2,6-difluorophenyl)-N-(4-(1-piperazinyl)-3-pyridinyl)imidazo[1,5-b]pyridazin-7-amine 
• 1405128-82-6 tert-butyl 4-(3-((2-(2,6-difluorophenyl)imidazo[1,5-b]pyridazin-7-yl)amino)-4-pyridinyl)-1-piperazinecarboxylate 
• 1023298-54-5 4-(3-amino-pyridin-4-yl)-piperazine-1-carboxylic acid tert-butyl ester 
• 608142-96-7 4-(3-benzenesulfonyl-1H-pyrrolo[3,2-b]pyridin-7-yl)-piperazine-1-carboxylic acid tert-butyl ester 
• 608142-95-6 4-(3-phenylsulfanyl-1H-pyrrolo[3,2-b]pyridin-7-yl)-piperazine-1-carboxylic acid tert-butyl ester 

Relevant academic research and scientific papers

Structure guided optimization, in vitro activity, and in vivo activity of pan-PIM kinase inhibitors

Proviral insertion of Moloney virus (PIM) 1, 2, and 3 kinases are serine/threonine kinases that normally function in survival and proliferation of hematopoietic cells. As high expression of PIM1, 2, and 3 is frequently observed in many human malignancies, including multiple myeloma, non-Hodgkins lymphoma, and myeloid leukemias, there is interest in determining whether selective PIM inhibition can improve outcomes of these human cancers. Herein, we describe our efforts toward this goal. The structure guided optimization of a singleton high throughput screening hit in which the potency against all three PIM isoforms was increased >10,000-fold to yield compounds with pan PIM Kis 10 pM, nanomolar cellular potency, and in vivo activity in an acute myeloid leukemia Pim-dependent tumor model is described.

COMPOSITIONS AND METHODS FOR TREATING CANCER

The instant invention provides a method of treating a cancer, selected from the group consisting of breast cancer, melanoma, colorectal cancer, non-small cell lung cancer and ovarian cancer, by administering a combination of a WEE1 inhibitor and a CHK1 inhibitor, wherein the WEE1 inhibitor is MK-1775 or a pharmaceutically acceptable salt thereof, or MK-3652 or a pharmaceutically acceptable salt thereof, and the CHK1 inhibitor is MK-8776 or a pharmaceutically acceptable salt thereof, or SCH900444 or a pharmaceutically acceptable salt thereof.

BICYCLIC PYRIDAZINE COMPOUNDS AS PIM INHIBITORS

The invention relates to bicyclic compounds of formulas I and I', and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.

DIAMIDO THIAZOLE DERIVATIVES AS PROTEIN KINASE INHIBITORS

The present invention relates to novel Diamido Thiazole Derivatives of structure I, compositions comprising the Diamido Thiazole Derivatives, and methods for using the Diamido Thiazole Derivatives for treating or preventing a proliferative disorder, an anti -proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral infection, a fungal infection, or a disorder related to the activity of a protein kinase. Formula (I) wherein: M is -C(O)-, -C(S)-. -S(O)-. -S(O)2-. -NHS(O)2-. -OC(O)- or -NHC(O)-; Q is:formula (II).

HETEROCYCLIC AMIDE COMPOUNDS AS PROTEIN KINASE INHIBITORS

The present invention related to novel heterocyclic amide compounds of Formula 1: as disclosed herein or a pharmaceutically accept able salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosedare compositions comprising said compounds, and methods for using said compounds for treating or preventing a proliferative disease, an anti-proliferative disorder, inflammation, arthritis, a neurological or neurodenerative disease, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease or a fungal disease

ANILINOPIPERAZINE DERIVATIVES AND METHODS OF USE THEREOF

The present invention relates to novel Anilinopiperazine Derivatives of Formula (I), compositions comprising the Anilinopiperazine Derivatives, and methods for using the Anilinopiperazine Derivatives for treating or preventing a proliferative disorder, cancer, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease, a fungal infection, or a disorder related to the activity of a protein kinase.

2-AMINOTHIAZOLE-4-CARBOXYLIC AMIDES AS PROTEIN KINASE INHIBITORS

The present invention relates to novel Anilinopiperazine Derivatives of formula (I), compositions comprising the Anilinopiperazine Derivatives, and methods for using the Anilinopiperazine Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease, a fungal infection, or a disorder related to the activity of a protein kinase.

Bicyclic heteroarylpiperazines as selective brain penetrant 5-HT 6 receptor antagonists

Starting from the potent and selective but poorly brain penetrant 5-HT 6 receptor antagonist SB-271046, a successful strategy for improving brain penetration was adopted involving conformational constraint with concomitant reduction in hydrogen bond count. This provided a series of bicyclic heteroarylpiperazines with high 5-HT6 receptor affinity. 5-Chloroindole 699929 combined high 5-HT6 receptor affinity with excellent brain penetration and also had good oral bioavailability in both rat and dog.