Lighthouse Pharmaceuticals, Inc.

United States of America

Back to Profile

1-10 of 10 for Lighthouse Pharmaceuticals, Inc. Sort by
Query
Aggregations
Date
2025 August 1
2025 (YTD) 1
2023 1
2021 2
2020 1
See more
IPC Class
C07C 233/62 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups 8
C07C 233/78 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom 8
C07C 247/16 - Compounds containing azido groups with azido groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton 8
C07C 247/18 - Compounds containing azido groups with azido groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by carboxyl groups 6
A61P 31/04 - Antibacterial agents 5
See more
Status
Pending 1
Registered / In Force 9
Found results for  patents

1.

KETONE INHIBITORS OF LYSINE GINGIPAIN

      
Application Number 18905445
Status Pending
Filing Date 2024-10-03
First Publication Date 2025-08-28
Owner Lighthouse Pharmaceuticals, Inc. (USA)
Inventor
  • Konradi, Andrei W.
  • Galemmo, Jr., Robert A.
  • Dominy, Stephen S.
  • Lynch, Casey C.
  • Holsinger, Leslie J.

Abstract

The present invention provides compounds according to Formula I as described herein, and their use for inhibiting the lysine gingipain protease (Kgp) from the bacterium Porphyromonas gingivalis. Also described are gingipain activity probe compounds and methods for assaying gingipain activity are also described, as well as methods for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease.

IPC Classes  ?

  • C07C 233/62 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
  • A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
  • A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
  • A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
  • A61K 31/42 - Oxazoles
  • A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
  • A61K 31/4402 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
  • A61K 31/4406 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 3, e.g. zimeldine
  • A61K 31/4409 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
  • A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
  • A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
  • A61K 31/655 - Azo (—N=N—), diazo (=N2), azoxy (N—O—N or N(=O)—N), azido (—N3) or diazoamino (—N=N—N) compounds
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61P 25/00 - Drugs for disorders of the nervous system
  • A61P 31/04 - Antibacterial agents
  • C07B 59/00 - Introduction of isotopes of elements into organic compounds
  • C07C 233/78 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
  • C07C 235/10 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms not being part of nitro or nitroso groups
  • C07C 235/50 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms not being part of nitro or nitroso groups
  • C07C 237/42 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
  • C07C 245/08 - Azo compounds, i.e. compounds having the free valencies of —N=N— groups attached to different atoms, e.g. diazohydroxides with nitrogen atoms of azo groups bound to carbon atoms of six-membered aromatic rings with the two nitrogen atoms of azo groups bound to carbon atoms of six-membered aromatic rings, e.g. azobenzene
  • C07C 247/16 - Compounds containing azido groups with azido groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
  • C07C 247/18 - Compounds containing azido groups with azido groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by carboxyl groups
  • C07C 317/28 - SulfonesSulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
  • C07C 323/40 - Y being a hydrogen or a carbon atom
  • C07C 323/42 - Y being a carbon atom of a six-membered aromatic ring
  • C07C 381/00 - Compounds containing carbon and sulfur and having functional groups not covered by groups
  • C07D 213/65 - One oxygen atom attached in position 3 or 5
  • C07D 213/68 - One oxygen atom attached in position 4
  • C07D 213/70 - Sulfur atoms
  • C07D 213/81 - AmidesImides
  • C07D 213/82 - AmidesImides in position 3
  • C07D 239/34 - One oxygen atom
  • C07D 239/36 - One oxygen atom as doubly bound oxygen atom or as unsubstituted hydroxy radical
  • C07D 239/38 - One sulfur atom
  • C07D 257/04 - Five-membered rings
  • C07D 261/12 - Oxygen atoms
  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07F 5/02 - Boron compounds

2.

Ketone inhibitors of lysine gingipain

      
Application Number 17740260
Grant Number 12110263
Status In Force
Filing Date 2022-05-09
First Publication Date 2023-05-11
Grant Date 2024-10-08
Owner Lighthouse Pharmaceuticals, Inc. (USA)
Inventor
  • Konradi, Andrei W.
  • Galemmo, Jr., Robert A.
  • Dominy, Stephen S.
  • Lynch, Casey C.
  • Holsinger, Leslie J.

Abstract

P. gingivalis infection, including brain disorders such as Alzheimer's disease.

IPC Classes  ?

  • C07C 233/62 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
  • A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
  • A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
  • A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
  • A61K 31/42 - Oxazoles
  • A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
  • A61K 31/4402 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
  • A61K 31/4406 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 3, e.g. zimeldine
  • A61K 31/4409 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
  • A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
  • A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
  • A61K 31/655 - Azo (—N=N—), diazo (=N2), azoxy (N—O—N or N(=O)—N), azido (—N3) or diazoamino (—N=N—N) compounds
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • A61P 25/00 - Drugs for disorders of the nervous system
  • A61P 31/04 - Antibacterial agents
  • C07B 59/00 - Introduction of isotopes of elements into organic compounds
  • C07C 233/78 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
  • C07C 235/10 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms not being part of nitro or nitroso groups
  • C07C 235/50 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms not being part of nitro or nitroso groups
  • C07C 237/42 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
  • C07C 245/08 - Azo compounds, i.e. compounds having the free valencies of —N=N— groups attached to different atoms, e.g. diazohydroxides with nitrogen atoms of azo groups bound to carbon atoms of six-membered aromatic rings with the two nitrogen atoms of azo groups bound to carbon atoms of six-membered aromatic rings, e.g. azobenzene
  • C07C 247/16 - Compounds containing azido groups with azido groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
  • C07C 247/18 - Compounds containing azido groups with azido groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by carboxyl groups
  • C07C 317/28 - SulfonesSulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
  • C07C 323/40 - Y being a hydrogen or a carbon atom
  • C07C 323/42 - Y being a carbon atom of a six-membered aromatic ring
  • C07C 381/00 - Compounds containing carbon and sulfur and having functional groups not covered by groups
  • C07D 213/65 - One oxygen atom attached in position 3 or 5
  • C07D 213/68 - One oxygen atom attached in position 4
  • C07D 213/70 - Sulfur atoms
  • C07D 213/81 - AmidesImides
  • C07D 213/82 - AmidesImides in position 3
  • C07D 239/34 - One oxygen atom
  • C07D 239/36 - One oxygen atom as doubly bound oxygen atom or as unsubstituted hydroxy radical
  • C07D 239/38 - One sulfur atom
  • C07D 257/04 - Five-membered rings
  • C07D 261/12 - Oxygen atoms
  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07F 5/02 - Boron compounds

3.

Ketone inhibitors of lysine gingipain

      
Application Number 16899376
Grant Number 11325884
Status In Force
Filing Date 2020-06-11
First Publication Date 2021-02-25
Grant Date 2022-05-10
Owner LIGHTHOUSE PHARMACEUTICALS, INC. (USA)
Inventor
  • Konradi, Andrei W.
  • Galemmo, Jr., Robert A.
  • Dominy, Stephen S.
  • Lynch, Casey C.
  • Holsinger, Leslie J.

Abstract

P. gingivalis infection, including brain disorders such as Alzheimer's disease.

IPC Classes  ?

  • C07C 233/62 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
  • C07D 213/82 - AmidesImides in position 3
  • C07D 239/34 - One oxygen atom
  • C07D 239/36 - One oxygen atom as doubly bound oxygen atom or as unsubstituted hydroxy radical
  • C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 257/04 - Five-membered rings
  • C07D 261/12 - Oxygen atoms
  • C07D 213/70 - Sulfur atoms
  • C07C 317/28 - SulfonesSulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
  • C07C 233/78 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
  • C07C 235/10 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms not being part of nitro or nitroso groups
  • C07C 235/50 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms not being part of nitro or nitroso groups
  • C07B 59/00 - Introduction of isotopes of elements into organic compounds
  • C07C 237/42 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07C 381/00 - Compounds containing carbon and sulfur and having functional groups not covered by groups
  • C07C 323/42 - Y being a carbon atom of a six-membered aromatic ring
  • C07D 213/65 - One oxygen atom attached in position 3 or 5
  • C07D 213/68 - One oxygen atom attached in position 4
  • C07D 239/38 - One sulfur atom
  • C07C 247/18 - Compounds containing azido groups with azido groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by carboxyl groups
  • C07F 5/02 - Boron compounds
  • A61P 31/04 - Antibacterial agents
  • A61P 25/00 - Drugs for disorders of the nervous system
  • A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
  • A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
  • A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
  • A61K 31/42 - Oxazoles
  • A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
  • A61K 31/4402 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
  • A61K 31/4406 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 3, e.g. zimeldine
  • A61K 31/4409 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
  • A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
  • A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
  • A61K 31/655 - Azo (—N=N—), diazo (=N2), azoxy (N—O—N or N(=O)—N), azido (—N3) or diazoamino (—N=N—N) compounds
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • C07C 245/08 - Azo compounds, i.e. compounds having the free valencies of —N=N— groups attached to different atoms, e.g. diazohydroxides with nitrogen atoms of azo groups bound to carbon atoms of six-membered aromatic rings with the two nitrogen atoms of azo groups bound to carbon atoms of six-membered aromatic rings, e.g. azobenzene
  • C07C 247/16 - Compounds containing azido groups with azido groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
  • C07C 323/40 - Y being a hydrogen or a carbon atom
  • C07D 213/81 - AmidesImides

4.

Inhibitors of lysine gingipain

      
Application Number 16866022
Grant Number 11332464
Status In Force
Filing Date 2020-05-04
First Publication Date 2021-01-21
Grant Date 2022-05-17
Owner LIGHTHOUSE PHARMACEUTICALS, INC. (USA)
Inventor
  • Konradi, Andrei W.
  • Dominy, Stephen S.
  • Lynch, Casey Crawford
  • Coburn, Craig
  • Vacca, Joseph

Abstract

P. gingivalis infection, including brain disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula I, as described herein, and pharmaceutically acceptable salts thereof.

IPC Classes  ?

  • C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 277/28 - Radicals substituted by nitrogen atoms
  • C07D 277/24 - Radicals substituted by oxygen atoms
  • C07C 233/78 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
  • C07D 277/64 - Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
  • C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 213/50 - Ketonic radicals
  • C07C 247/16 - Compounds containing azido groups with azido groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
  • C07C 233/62 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
  • C07C 247/18 - Compounds containing azido groups with azido groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by carboxyl groups
  • C07D 213/53 - Nitrogen atoms

5.

Aminopyridine compounds and methods for the preparation and use thereof

      
Application Number 16678700
Grant Number 11059786
Status In Force
Filing Date 2019-11-08
First Publication Date 2020-05-14
Grant Date 2021-07-13
Owner LIGHTHOUSE PHARMACEUTICALS, INC. (USA)
Inventor
  • Konradi, Andrei W.
  • Galemmo, Jr., Robert A.
  • Lynch, Casey C.

Abstract

P. gingivalis infection, including brain disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula I and Formula III, as described herein, and pharmaceutically acceptable salts thereof.

IPC Classes  ?

  • C07D 213/73 - Unsubstituted amino or imino radicals
  • C07D 217/22 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
  • C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
  • C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
  • A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

6.

Ketone inhibitors of lysine gingipain

      
Application Number 16353786
Grant Number 10730826
Status In Force
Filing Date 2019-03-14
First Publication Date 2019-07-11
Grant Date 2020-08-04
Owner LIGHTHOUSE PHARMACEUTICALS, INC. (USA)
Inventor
  • Konradi, Andrei W.
  • Galemmo, Jr., Robert A.
  • Dominy, Stephen S.
  • Lynch, Casey C.
  • Holsinger, Leslie J.

Abstract

P. gingivalis infection, including brain disorders such as Alzheimer's disease.

IPC Classes  ?

  • C07C 233/62 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
  • C07D 213/82 - AmidesImides in position 3
  • C07D 239/34 - One oxygen atom
  • C07D 239/36 - One oxygen atom as doubly bound oxygen atom or as unsubstituted hydroxy radical
  • C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 257/04 - Five-membered rings
  • C07D 261/12 - Oxygen atoms
  • C07D 213/70 - Sulfur atoms
  • C07C 317/28 - SulfonesSulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
  • C07C 233/78 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
  • C07C 235/10 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms not being part of nitro or nitroso groups
  • C07C 235/50 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms not being part of nitro or nitroso groups
  • C07B 59/00 - Introduction of isotopes of elements into organic compounds
  • C07C 237/42 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
  • C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07C 381/00 - Compounds containing carbon and sulfur and having functional groups not covered by groups
  • C07C 323/42 - Y being a carbon atom of a six-membered aromatic ring
  • C07D 213/65 - One oxygen atom attached in position 3 or 5
  • C07D 213/68 - One oxygen atom attached in position 4
  • C07D 239/38 - One sulfur atom
  • C07C 247/18 - Compounds containing azido groups with azido groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by carboxyl groups
  • C07F 5/02 - Boron compounds
  • A61P 31/04 - Antibacterial agents
  • A61P 25/00 - Drugs for disorders of the nervous system
  • A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
  • A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
  • A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
  • A61K 31/42 - Oxazoles
  • A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
  • A61K 31/4402 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
  • A61K 31/4406 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 3, e.g. zimeldine
  • A61K 31/4409 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
  • A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
  • A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
  • A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
  • A61K 31/655 - Azo (—N=N—), diazo (=N2), azoxy (N—O—N or N(=O)—N), azido (—N3) or diazoamino (—N=N—N) compounds
  • A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
  • C07C 245/08 - Azo compounds, i.e. compounds having the free valencies of —N=N— groups attached to different atoms, e.g. diazohydroxides with nitrogen atoms of azo groups bound to carbon atoms of six-membered aromatic rings with the two nitrogen atoms of azo groups bound to carbon atoms of six-membered aromatic rings, e.g. azobenzene
  • C07C 247/16 - Compounds containing azido groups with azido groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
  • C07C 323/40 - Y being a hydrogen or a carbon atom
  • C07D 213/81 - AmidesImides

7.

Inhibitors of lysine gingipain

      
Application Number 15996660
Grant Number 10301301
Status In Force
Filing Date 2018-06-04
First Publication Date 2018-12-06
Grant Date 2019-05-28
Owner LIGHTHOUSE PHARMACEUTICALS, INC. (USA)
Inventor
  • Konradi, Andrei
  • Dominy, Stephen S.
  • Lynch, Casey Crawford
  • Coburn, Craig
  • Vacca, Joseph

Abstract

P. gingivalis infection, including brain disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula I, as described herein, and pharmaceutically acceptable salts thereof.

IPC Classes  ?

  • C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 213/53 - Nitrogen atoms
  • C07D 277/28 - Radicals substituted by nitrogen atoms
  • C07D 277/64 - Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
  • C07C 233/62 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
  • C07C 233/78 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
  • C07C 247/16 - Compounds containing azido groups with azido groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
  • C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 213/50 - Ketonic radicals
  • C07C 247/18 - Compounds containing azido groups with azido groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by carboxyl groups
  • C07D 277/24 - Radicals substituted by oxygen atoms

8.

Inhibitors of arginine gingipain

      
Application Number 15975490
Grant Number 10906881
Status In Force
Filing Date 2018-05-09
First Publication Date 2018-11-22
Grant Date 2021-02-02
Owner LIGHTHOUSE PHARMACEUTICALS, INC. (USA)
Inventor
  • Konradi, Andrei
  • Dominy, Stephen S.
  • Lynch, Casey C.
  • Coburn, Craig
  • Vacca, Joseph

Abstract

P. gingivalis infection, including brain disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula I, as described herein, and pharmaceutically acceptable salts thereof.

IPC Classes  ?

  • C07C 279/12 - Derivatives of guanidine, i.e. compounds containing the group the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton being further substituted by nitrogen atoms not being part of nitro or nitroso groups
  • A61P 31/04 - Antibacterial agents
  • C07D 277/64 - Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
  • C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links

9.

Inhibitors of lysine gingipain

      
Application Number 15683348
Grant Number 09988375
Status In Force
Filing Date 2017-08-22
First Publication Date 2017-12-07
Grant Date 2018-06-05
Owner LIGHTHOUSE PHARMACEUTICALS, INC. (USA)
Inventor
  • Konradi, Andrei
  • Dominy, Stephen S.
  • Lynch, Casey Crawford
  • Coburn, Craig
  • Vacca, Joseph

Abstract

P. gingivalis infection, including brain disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula I, as described herein, and pharmaceutically acceptable salts thereof.

IPC Classes  ?

  • C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 277/28 - Radicals substituted by nitrogen atoms
  • C07D 213/53 - Nitrogen atoms
  • C07D 277/64 - Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
  • C07C 233/62 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
  • C07C 247/16 - Compounds containing azido groups with azido groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
  • C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 213/50 - Ketonic radicals
  • C07C 233/78 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom

10.

Inhibitors of lysine gingipain

      
Application Number 14875416
Grant Number 09758473
Status In Force
Filing Date 2015-10-05
First Publication Date 2016-04-07
Grant Date 2017-09-12
Owner LIGHTHOUSE PHARMACEUTICALS, INC. (USA)
Inventor
  • Konradi, Andrei
  • Dominy, Stephen S.
  • Crawford Lynch, Casey
  • Coburn, Craig
  • Vacca, Joseph

Abstract

P. gingivalis infection, including brain disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula I, as described herein, and pharmaceutically acceptable salts thereof.

IPC Classes  ?

  • C07C 247/16 - Compounds containing azido groups with azido groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
  • C07C 233/62 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
  • C07C 233/78 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
  • C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 277/64 - Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
  • C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
  • C07D 213/50 - Ketonic radicals