Target and Its Patented Drug(s)

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Target General Information
Patent(s) and the Corresponding Patented Drug(s)
References
Target General Information  Top
Target ID T08123 Target Info
Target Name Leucine-rich repeat kinase 2 (LRRK2)
Synonyms PARK8; Leucine-rich repeat serine/threonine-protein kinase 2; Dardarin
Target Type Clinical trial Target
Gene Name LRRK2
Biochemical Class Kinase
UniProt ID
LRRK2_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2015150612
Title Substituted Isatins and The Therapeutic Applications Thereof for The Treatment of Neurodegenerative Diseases.
Abstract The invention relates to a family of differently substituted isatins that exhibit activity inhibiting the protein kinase with leucine-rich repeats (LRRK2), such that they are useful in the treatment of diseases mediated by said enzyme, such as inflammatory diseases, autoimmune diseases and neurodegenerative diseases, especially Parkinson's disease.
Applicant(s) Consejo Superior Investigacion
Representative Drug(s) D08WVK Drug Info IC50 = 11 nM Click to Show More [1]
2 D0QK7K Drug Info IC50 = 23 nM [1]
3 D07SEG Drug Info N.A. [1]
Patent ID WO2016042089
Title Macrocyclic Lrrk2 Kinase Inhibitors.
Abstract The present invention relates to novel macrocyclic compounds of formula (I) and compositions containing said compounds acting as kinase inhibitors, in particular as inhibitors of LRRK2 (Leucine-Rich Repeat Kinase 2). Moreover, the present invention provides processes for the preparation of the disclosed compounds, as well as methods of using them, for instance as a medicine or diagnostic agent, in particular for the treatment and/or diagnosis of diseases characterized by LRRK2 kinase activity such as neurological disorders including Parkinson's disease and Alzheimer's disease.
Applicant(s) Onocodesign S.A
Representative Drug(s) D0M5BR Drug Info N.A. [1]
Patent ID WO2014170248
Title Arylpyrrolopyridine Derived Compounds As Lrrk2 Inhibitors.
Abstract The present invention is directed to arylpyrrolopyridine derivatives of formula (A) (A). The compounds are considered useful for the treatment of diseases associated with LRRK2 such as Lewy body dementia, Parkinson's disease cancer.
Applicant(s) H. Lundbeck A / S
Representative Drug(s) D00FKF Drug Info IC50 = 1 nM Click to Show More [1]
2 D03GDC Drug Info N.A. [1]
Patent ID WO2014140235
Title Macrocyclic Lrrk2 Kinase Inhibitors.
Abstract The present invention relates to macrocyclic compounds and compositions containing said compounds acting as kinase inhibitors, in particular as inhibitors of LRRK2 kinase, for use in the diagnosis, prevention and/or treatment of LRRK2 -kinase associated diseases. Moreover, the present invention provides methods of using said compounds, for instance as a medicine or diagnostic agent. Finally, the present invention also relates to new macrocyclic compounds.
Applicant(s) Ipsen Pharma Sas Oncodesign Sa
Representative Drug(s) D01YHY Drug Info N.A. [1]
Patent ID WO2014106612
Title Aminopyridine Derived Compounds As Lrrk2 Inhibitors.
Abstract The present invention is directed to aminopyridine derived compounds of formula (A). The compounds are considered useful for the treatment of diseases associated with LRRK2 such a Lewy body dementia, Parkinson's disease or cancer.
Applicant(s) H. Lundbeck A/S
Representative Drug(s) D0D6DN Drug Info IC50 = 91 nM Click to Show More [1]
2 D0X8LX Drug Info N.A. [1]
Patent ID WO2014060113
Title Novel Kinase Inhibitors.
Abstract The present invention relates to novel compounds of formula (I) that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases. These diseases include autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, alzheimer's disease, parkinson's disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases.
Applicant(s) Origenis Gmbh
Representative Drug(s) D07FFA Drug Info LRRK2 enzyme potency < 10 nM Click to Show More [1]
2 D08VBG Drug Info N.A. [1]
Patent ID WO2014060112
Title Pyrazolo[4,3-D]Pyrimidines As Kinase Inhibitors.
Abstract The present invention relates to novel compounds of formula (I) that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases. These diseases include autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, alzheimer's disease, parkinson's disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases.
Applicant(s) Origenis Gmbh
Representative Drug(s) D0V8XG Drug Info LRRK2 enzyme potency < 10 nM Click to Show More [1]
2 D0O8AP Drug Info N.A. [1]
Patent ID WO2015113452
Title Compounds.
Abstract The present invention relates to novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, to compositions containing them and to their use in the treatment of or prevention of diseases characterized by LRRK2 kinase activity, for example Parkinson's disease, Alzheimer's disease and amyotrophic lateral sclerosis (ALS).
Applicant(s) Glaxosmithkline Intellectual Property Development Limited
Representative Drug(s) D02YTB Drug Info N.A. Click to Show More [1]
2 D0XY1J Drug Info N.A. [1]
Patent ID WO2015113451
Title Compounds.
Abstract Provided are novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, compositions containing them and their use in the treatment of or prevention of diseases characterized by LRRK2 kinase activity, for example Parkinson's disease, Alzheimer's disease and amyotrophic lateral sclerosis (ALS).
Applicant(s) Glaxosmithkline Intellectual Property Development Limited
Representative Drug(s) D01EIT Drug Info N.A. Click to Show More [1]
2 D0C5HR Drug Info N.A. [1]
Patent ID WO2014200682
Title Bidentate-Binding Modulators of Lrrk2 and Jnk Kinases.
Abstract Both JNK and LRRK2 are associated with Parkinson's disease (PD), myocardial infarction (Ml), and other medical disorders. Here we report a reasonably selective and potent kinase inhibitors (e.g., compounds 6 and 10) that bound to both JNK and LRRK2 (a dual inhibitor). A bidentate-binding strategy that simultaneously utilized the ATP hinge binding and a unique protein surface site outside of the ATP pocket was applied to the design and identification of this kind of inhibitor. Compound 6 was a potent JNK3 and modest LRRK2 dual inhibitor with an enzyme IC50 value of 12 nM and 99 nM (LRRK2-G2019S), respectively. 6 also exhibited good cell potency, inhibited LRRK2:G2019S induced mitochondrial dysfunction in SHSY5Y cells, and was demonstrated to be reasonably selective against a panel of 116 kinases from representative kinase families.
Applicant(s) The Scripps Research Institute
Representative Drug(s) D00GWE Drug Info N.A. Click to Show More [1]
2 D0SV0D Drug Info N.A. [1]
Patent ID WO2014150981
Title Inhibitors of Lrrk2 Kinase Activity.
Abstract The present invention provides compounds having a structure according to Formula I. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.
Applicant(s) Elan Pharmaceuticals, lnc
Representative Drug(s) D03HNU Drug Info N.A. Click to Show More [1]
2 D0HY0H Drug Info N.A. [1]
3 D0PY1G Drug Info N.A. [1]
Patent ID WO2014137728
Title Compounds Inhibiting Leucine-Rich Repeat Kinase Enzyme Activity.
Abstract The present invention is directed to indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0FS9X Drug Info IC50 = 0.76 nM [1]
Patent ID WO2014137725
Title Compounds Inhibiting Leucine-Rich Repeat Kinase Enzyme Activity.
Abstract The present invention is directed to indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK2 kinase is involved.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0FS9X Drug Info IC50 = 0.76 nM [1]
Patent ID WO2014137723
Title Compounds Inhibiting Leucine-Rich Repeat Kinase Enzyme Activity.
Abstract The present invention is directed to indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0FS9X Drug Info IC50 = 0.76 nM [1]
Patent ID WO2014137719
Title Compounds Inhibiting Leucine-Rich Repeat Kinase Enzyme Activity.
Abstract The present invention is directed to indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0FS9X Drug Info IC50 = 0.76 nM [1]
Patent ID WO2014134776
Title Compounds Inhibiting Leucine-Rich Repeat Kinase Enzyme Activity.
Abstract The present invention is directed to indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK2 kinase is involved.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0FS9X Drug Info IC50 = 0.76 nM [1]
Patent ID WO2014134774
Title Compounds Inhibiting Leucine-Rich Repeat Kinase Enzyme Activity.
Abstract Disclosed are indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which LRRK2 kinase is involved. Also disclosed are pharmaceutical compositions in the prevention or treatment of such diseases in which LRRK2 kinase is involved.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0FS9X Drug Info IC50 = 0.76 nM [1]
Patent ID WO2015092592
Title Novel 3,4-Disubstituted-1H-Pyrrolo[2,3-B]Pyridines and 4,5-Disubstituted-7H-Pyrrolo[2,3-C]Pyridazines As Lrrk2 Inhibitors.
Abstract The present invention provides novel 3,4-disubstituted-1 H-pyrrolo[2,3-b]pyridine derivatives and 4,5-disubstituted-7H-pyrrolo[2,3-c]pyridazine derivatives of Formula (I), and the pharmaceutically acceptable salts thereof (I) wherein R1, R2, R3, R4 and X are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of formula (I) and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.
Applicant(s) Pfizer Inc
Representative Drug(s) D0Q6VL Drug Info N.A. [1]
Patent ID WO2016036586
Title Compounds Inhibiting Leucine-Rich Repeat Kinase Enzyme Activity.
Abstract The present invention is directed to substituted certain reversed indazole compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R9, and A are as defined herein, which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.
Applicant(s) Merck Sharp & Dohme Corp
Patent ID WO2015073344
Title Compounds Inhibiting Leucine-Rich Repeat Kinase Enzyme Activity.
Abstract The present invention is directed to substituted indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.
Applicant(s) Merck Sharp & Dohme Corp
Patent ID WO2015026683
Title Compounds Inhibiting Leucine-Rich Repeat Kinase Enzyme Activity.
Abstract The present invention is directed to azaindazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.
Applicant(s) Merck Sharp & Dohme Corp
Patent ID WO2012143144
Title Pyrazolo [4, 3-D] Pyrimidines Useful As Kinase Inhibitors.
Abstract The present invention relates to novel compounds of formula (I) that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases. These diseases include autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, alzheimer's disease, parkinson's disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases.
Applicant(s) Origenis Gmbh
Patent ID WO2012143143
Title Heterocyclic Compounds As Kinase Inhibitors.
Abstract The present invention relates to novel compounds of formula (I) that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases. These diseases include autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, alzheimer's disease, parkinson's disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases.
Applicant(s) Origenis Gmbh
Patent ID WO2012118679
Title Compounds Inhibiting Leucine-Rich Repeat Kinase Enzyme Activity.
Abstract Disclosed are compounds of Formula I: and the pharmaceutically acceptable salts thereof, wherein &quot;A&quot; is S-; -SO-, -SO2-, -O- or NRa-, and Ra, and R1 through R5 are defined herein. Also disclosed are pharmaceutical formulations comprising a compound of Formula I and methods of treating, managing, or ameliorating diseases amenable to treatment, management, or amelioration by inhibition of LRRK2 kinase activity, for example, Parkinson's disease.
Applicant(s) Merck Sharp & Dohme Corp
Patent ID WO2012058193
Title Leucine-Rich Repeat Kinase Enzyme Activity.
Abstract Disclosed are compounds of Formula (I): and the pharmaceutically acceptable salts thereof, wherein &quot;A&quot; is S-; -SO-, -SO2-, -O- or NRac-, wherein Rac is H, or C1-20 alkyl and R1 through R5 are defined herein. Also disclosed are pharmaceutical formulations comprising a compound of Formula I and methods of treating, managing, or ameliorating diseases amenable to treatment, management, or amelioration by inhibition of LRRK2 kinase activity, for example, Parkinson's disease.
Applicant(s) Merck Sharp & Dohme Corp
United States Patent and Trademark Office (USPTO)
Patent ID US20140288043
Title Preparation of Pyrazolopyridine Compounds As Lrrk2 Inhibitors.
Applicant(s) Genentech, Inc
Representative Drug(s) D0DP6U Drug Info Ki = 0.5 nM Click to Show More [1]
2 D0ZW5B Drug Info Ki = 0.5 nM [1]
3 D06FIH Drug Info N.A. [1]
4 D0NO4O Drug Info N.A. [1]
Patent ID US20140005183
Title Preparation of Novel 4-(Substituted Amino)-7H-Pyrrolo[2,3-D]Pyrimidines As Lrrk2 Inhibitors Patent.
Applicant(s) Pfizer Inc
Representative Drug(s) D0GJ4G Drug Info N.A. [1]
Korean Intellectual Property Office (KIPO)
Patent ID KR2016035411
Title Pyridopyrimidine Derivatives As Protein Kinase Lrrk2 Inhibitors.
Applicant(s) Oscotec, Inc., S. Korea. Assignee
Representative Drug(s) D01PFZ Drug Info IC50 = 1.1 nM Click to Show More [1]
2 D0S4IB Drug Info IC50 = 2.5 nM [1]
3 D04WND Drug Info N.A. [1]
References  Top
REF 1 Leucine-rich repeat kinase 2 inhibitors: a patent review (2014-2016).Expert Opin Ther Pat. 2017 Jun;27(6):667-676.

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