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AERIE PHARMACEUTICALS INC (AERI)
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Aerie Pharmaceuticals : Patent Issued for 6-Aminoisoquinoline Compounds (USPTO 9890123)

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02/23/2018 | 11:09pm CEST

By a News Reporter-Staff News Editor at Diabetes Week -- According to news reporting originating from Alexandria, Virginia, by NewsRx journalists, a patent by the inventors deLong, Mitchell A. (Chapel Hill, NC); Royalty, Susan M. (Davis, CA); Sturdivant, Jill Marie (Chapel Hill, NC); Heintzelman, Geoffrey Richard (Durham, NC), filed on June 9, 2016, was published online on February 13, 2018 (see also Aerie Pharmaceuticals Inc.).

The assignee for this patent, patent number 9890123, is Aerie Pharmaceuticals Inc. (Irvine, CA).

Reporters obtained the following quote from the background information supplied by the inventors: "A variety of hormones, neurotransmitters and biologically active substances control, regulate or adjust the functions of living bodies via specific receptors located in cell membranes. Many of these receptors mediate the transmission of intracellular signals by activating guanine nucleotide-binding proteins (G proteins) to which the receptor is coupled. Such receptors are generically referred to as G-protein coupled receptors (GPCRs) and include, among others, .alpha.-adrenergic receptors, .beta.-adrenergic receptors, opioid receptors, cannabinoid receptors and prostaglandin receptors. The effect of these receptors is not direct but mediated by a host of intracellular proteins. The importance of these secondary, or 'downstream' proteins is only now being recognized and investigated as potential intervention points in disease states. One of the most important classes of these downstream proteins is the 'kinase' class.

"The various kinases play an important role in the regulation of various physiological functions. By way of example, kinases have been implicated in a number of disease states, including, but not limited to: cardiac indications such as angina pectoris, essential hypertension, myocardial infarction, supraventricular and ventricular arrhythmias, congestive heart failure, atherosclerosis, renal failure, diabetes, respiratory indications such as asthma, chronic bronchitis, bronchospasm, emphysema, airway obstruction, upper respiratory indications such as rhinitis, seasonal allergies, inflammatory disease, inflammation in response to injury, rheumatoid arthritis. The importance of p38 MAPK inhibitors as new drugs for rheumatoid arthritis is reflected by the large number of compounds that has been developed over the last years (J. Westra and P. C. Limburg Mini-Reviews in Medicinal Chemistry Volume 6, Number 8, August 2006) Other conditions include chronic inflammatory bowel disease, glaucoma, hypergastrinemia, gastrointestinal indications such as acid/peptic disorder, erosive esophagitis, gastrointestinal hypersecretion, mastocytosis, gastrointestinal reflux, peptic ulcer, Zollinger-Ellison syndrome, pain, obesity, bulimia nervosa, depression, obsessive-compulsive disorder, organ malformations (for example, cardiac malformations), neurodegenerative diseases such as Parkinson's Disease and Alzheimer's Disease, multiple sclerosis, Epstein-Barr infection and cancer (Nature Reviews Drug Discovery 1, 493-502 2002). In other disease states, the role of kinases is only now becoming clear. The retina is a complex tissue composed of multiple interconnected cell layers, highly specialized for transforming light and color into electrical signals perceived by the brain. Damage or death of the primary light-sensing cells, the photoreceptors, results in devastating effects on vision. Despite the identification of numerous mutations that cause inherited retinal degenerations, the cellular and molecular mechanisms leading from the primary mutations to photoreceptor apoptosis are not well understood, but may involve the wnt pathway (AS Hackam The Wnt Signaling Pathway in Retinal Degeneration IUBMB Life Volume 57, Number 6/June 2005).

"The success of the tyrosine-kinase inhibitor STI571 (Gleevec) in the treatment of chronic myelogenous leukaemia (Nature Reviews Drug Discovery 2, 296-313 2003) has spurred considerable efforts to develop other kinase inhibitors for the treatment of a wide range of other cancers (Nature Reviews Cancer 3, 650-665 2003). The balance between the initiation and the inactivation of the intracellular signals regulates the intensity and duration of the response of the receptors to stimuli such as agonists. When desensitization occurs, the mediation or regulation of the physiological function mediated or regulated by the G proteins to which the receptors are coupled is reduced or prevented. For example, when agonists are administered to treat a disease or condition by activation of certain receptors, the receptors become desensitized from the action of the GRKs such that agonist administration may no longer result in therapeutic activation of the appropriate receptors. At that point, administration of the agonist no longer enables sufficient or effective control of or influence on the disease or condition intended to be treated.

"In view of the role of kinases in many disease states, there is an urgent and continuing need for ligands which inhibit or modulate the activity of kinases. Without wishing to be bound by theory, it is thought that modulation of the activity of kinases by the compounds of the present invention is responsible for their beneficial effects."

In addition to obtaining background information on this patent, NewsRx editors also obtained the inventors' summary information for this patent: "In a first aspect of the invention, a compound is provided according to Formula (I):

"##STR00001##

"wherein A is --CH.sub.2NH--,

"##STR00002## --SCH.sub.2--, --CH.sub.2S(O)--, --CH.sub.2S(O)(O)--, --S(O)CH.sub.2--, --S(O)(O)CH.sub.2--, --CH.sub.2CH.sub.2--, --CH(R.sub.10)CH.sub.2--, --CH.sub.2CH(R.sub.10), --CH.dbd.CH--,

"##STR00003## wherein R.sub.10 is hydrogen, unsubstituted C.sub.1-C.sub.4 alkyl, C.sub.1-C.sub.4 alkenyl, C.sub.1-C.sub.4 alkynyl, or amino;

"wherein R.sub.1, and R.sub.2 are, independently, hydrogen, hydroxyl, halogen, C.sub.1-C.sub.4 alkyl, C.sub.2-C.sub.4 alkenyl, C.sub.2-C.sub.4 alkynyl, amino, nitro, cyano, C.sub.1-C.sub.4 carbonyl, C.sub.1-C.sub.4 carbonylamino, C.sub.1-C.sub.4 alkoxy, C.sub.1-C.sub.4 sulfonyl, C.sub.1-C.sub.4 sulfonylamino, C.sub.1-C.sub.4 thioalkyl or C.sub.1-C.sub.4 carboxyl; and

"wherein R.sub.3 is hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxy, amino, cyano, cycloalkyl, heterocycloalkyl, aryl, C.sub.1-C.sub.4 alkyl aryl, heteroaryl, C.sub.1-C.sub.4 alkyl heteroaryl, carbonyl, carbonylamino, thioalkyl, sulfonyl, sulfonylamino, acyl, or carboxyl.

"In a second aspect, a compound is provided according to Formula II:

"##STR00004##

"wherein R.sub.1 and R.sub.2 are, independently, hydrogen, hydroxyl, halogen, C.sub.1-C.sub.4 alkyl, C.sub.2-C.sub.4 alkenyl, C.sub.2-C.sub.4 alkynyl, amino, nitro, cyano, C.sub.1-C.sub.4 carbonyl, C.sub.1-C.sub.4 carbonylamino, C.sub.1-C.sub.4 alkoxy, C.sub.1-C.sub.4 sulfonyl, C.sub.1-C.sub.4 sulfonylamino, C.sub.1-C.sub.4 thioalkyl or C.sub.1-C.sub.4 carboxyl;

"wherein R.sub.4 is hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxy, amino, cyano, cycloalkyl, heterocycloalkyl, aryl, C.sub.1-C.sub.4 alkyl aryl, heteroaryl, C.sub.1-C.sub.4 alkyl heteroaryl, carbonyl, carbonylamino, thioalkyl, sulfonyl, sulfonylamino, acyl, or carboxyl; and

"wherein B is a chain containing from 0 to 3 member atoms, X represents n independently chosen member atoms which together form a ring structure and n is an integer from about 0 to about 5.

"In another aspect, a compound is provided according to Formula III:

"##STR00005##

"wherein one of X.sub.1, X.sub.2 and X.sub.3 is independently selected from CH.sub.2, O, S, S(O), S(O)(O),

"##STR00006## and the other two of X.sub.1, X.sub.2 and X.sub.3 are independently selected from CH.sub.2, O, S, S(O), S(O)(O),

"##STR00007## and bond;

"wherein R.sub.1, and R.sub.2 are, independently, hydrogen, hydroxyl, halogen, C.sub.1-C.sub.4 alkyl, C.sub.2-C.sub.4 alkenyl, C.sub.2-C.sub.4 alkynyl, amino, nitro, cyano, C.sub.1-C.sub.4 carbonyl, C.sub.1-C.sub.4 carbonylamino, C.sub.1-C.sub.4 alkoxy, C.sub.1-C.sub.4 sulfonyl, C.sub.1-C.sub.4 sulfonylamino, C.sub.1-C.sub.4 thioalkyl and C.sub.1-C.sub.4 carboxyl; and

"wherein R.sub.5 and R.sub.10 are independently hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxy, amino, cyano, cycloalkyl, heterocycloalkyl, aryl, C.sub.1-C.sub.4 alkyl aryl, heteroaryl, C.sub.1-C.sub.4 alkyl heteroaryl, carbonyl, carbonylamino, thioalkyl, sulfonyl, sulfonylamino, acyl, or carboxyl.

"In a further aspect of the invention, a compound is provided according to Formula IV

"##STR00008##

"wherein A is a substituted or unsubstituted linker consisting of at least one member atom and at most 4 member atoms wherein the linker may be mono- or disubstituted with halogen, cyano, nitro or C.sub.1-C.sub.4 alkyl, or the substituted atoms may attach back to the main chain to form a ring;

"wherein R.sub.1, and R.sub.2 are, independently, hydrogen, hydroxyl, halogen, C.sub.1-C.sub.4 alkyl, C.sub.2-C.sub.4 alkenyl, C.sub.2-C.sub.4 alkynyl, amino, nitro, cyano, C.sub.1-C.sub.4 carbonyl, C.sub.1-C.sub.4 carbonylamino, C.sub.1-C.sub.4 alkoxy, C.sub.1-C.sub.4 sulfonyl, C.sub.1-C.sub.4 sulfonylamino, C.sub.1-C.sub.4 thioalkyl or C.sub.1-C.sub.4 carboxyl; and

"wherein R.sub.3 is hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxy, amino, cyano, cycloalkyl, heterocycloalkyl, aryl, C.sub.1-C.sub.4 alkyl aryl, heteroaryl, C.sub.1-C.sub.4 alkyl heteroaryl, carbonyl, carbonylamino, thioalkyl, sulfonyl, sulfonylamino, acyl, or carboxyl.

"In yet a further aspect, a method is provided for influencing the action of a kinase in a cell, a tissue, or a living mammal comprising administering to or contacting with the cell, tissue, or mammal at least one compound according to claim 1, 6, 12 or 16, or increasing the effectiveness of another therapeutic agent in a cell, tissue or living mammal comprising administering to or contacting with the cell, tissue or mammal a therapeutically effective amount of at least one compound according to claim 1, 6, 12 or 16.

"In yet another aspect of the invention, a pharmaceutical composition is provided, comprising:

"a) a 6-aminoisoquinoline derivative having the structure

"##STR00009##

"wherein R.sub.1, and R.sub.2 are, independently, hydrogen, hydroxyl, halogen, C.sub.1-C.sub.4 alkyl, C.sub.2-C.sub.4 alkenyl, C.sub.2-C.sub.4 alkynyl, amino, nitro, cyano; C.sub.1-C.sub.4 carbonyl, C.sub.1-C.sub.4 carbonylamino, C.sub.1-C.sub.4 alkoxy, C.sub.1-C.sub.4 sulfonyl, C.sub.1-C.sub.4 sulfonylamino, C.sub.1-C.sub.4 thioalkyl or C.sub.1-C.sub.4 carboxyl; and

"wherein R.sub.4 is hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxy, amino, cyano, cycloalkyl, heterocycloalkyl, aryl, C.sub.1-C.sub.4 alkyl aryl, heteroaryl, C.sub.1-C.sub.4 alkyl heteroaryl, carbonyl, carbonylamino, thioalkyl, sulfonyl, sulfonylamino, acyl, or carboxyl; and b) a carrier.

"In yet a further aspect is provided a method of treating a condition comprising administering to a subject in need of treatment a safe and effective amount of a 6-aminoisoquinoline derivative, wherein the condition is selected from the group consisting of eye disease, bone disorder, obesity, heart disease, hepatic disease, renal disease, pancreatitis, cancer, myocardial infarct, gastric disturbance, hypertension, fertility control, nasal congestion, neurogenic bladder disorder, gastrointestinal disorder, and dermatological disorder."

For more information, see this patent: deLong, Mitchell A.; Royalty, Susan M.; Sturdivant, Jill Marie; Heintzelman, Geoffrey Richard. 6-Aminoisoquinoline Compounds. U.S. Patent Number 9890123, filed June 9, 2016, and published online on February 13, 2018. Patent URL: http://patft.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PALL&p=1&u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&r=1&f=G&l=50&s1=9890123.PN.&OS=PN/9890123RS=PN/9890123

Keywords for this news article include: Aerie Pharmaceuticals Inc., Pharmaceutical Companies, Gases, Cancer, Kinase, Business, Elements, Hydrogen, Oncology, Gastroenterology, Health and Medicine, Inorganic Chemicals, Obesity and Diabetes, Enzymes and Coenzymes, Nutritional and Metabolic Diseases and Conditions.

Our reports deliver fact-based news of research and discoveries from around the world. Copyright 2018, NewsRx LLC

(c) 2018 NewsRx LLC, source Health Newsletters

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Financials ($)
Sales 2018 23,1 M
EBIT 2018 -152 M
Net income 2018 -200 M
Finance 2018 386 B
Yield 2018 -
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P/E ratio 2019
Capi. / Sales 2018 -16 622x
Capi. / Sales 2019 21,4x
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