| Patent(s) and the Corresponding Patented Drug(s) |
Top |
| World Intellectual Property Organization (WIPO) |
| Patent ID |
WO2013161312 |
| Title |
Pyrrolopyridinone Derivatives As Ttx-S Blockers. |
| Abstract |
The present invention relates to pyrrolopyridinone derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved. |
| Applicant(s) |
Raqualia Pharma Inc |
| Representative Drug(s) |
D06VYB |
Drug Info
|
IC50 = 910 nM |
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[1] |
|
2
|
D09YJV
|
Drug Info
|
IC50 < 1000 nM
|
[1] |
| Patent ID |
WO2013064984 |
| Title |
Biaryl Ether Sulfonamides and Their Use As Therapeutic Agents. |
| Abstract |
This invention is directed to biaryl ether sulfonamides, or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. |
| Applicant(s) |
Xenon Pharmaceuticals Inc |
| Patent ID |
WO2013064983 |
| Title |
Benzenesulfonamide Compounds and Their Use As Therapeutic Agents. |
| Abstract |
This invention is directed to benzensulfonamide compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment of sodium channel-mediated diseases or conditions, such as pain. |
| Applicant(s) |
Xenon Pharmaceuticals Inc |
| Representative Drug(s) |
D0TA8W |
Drug Info
|
IC50 > 0.8 nM; IC50 < 10000 nM |
[1] |
| Patent ID |
WO2012047703 |
| Title |
Cyclopropyl-Spiro-Piperidines Useful As Sodium Channel Blockers. |
| Abstract |
Pharmaceutical compositions comprise cyclopropyl-spiro-piperidine compounds. The compounds are blockers of voltage-gated sodium channels. Methods of treating conditions associated with, or caused by, voltage-gated sodium channel activity, including, pain, epilepsy conditions, irritable bowel syndrome, depression, anxiety, bipolar disorder, neurodegenerative disorders; psychiatric disorders, myotonia, arrhythmia, movement disorders, neuroendocrine disorders, ataxia, multiple sclerosis, irritable bowel syndrome, incontinence, neuropathy and tinnitus, comprise administering the instant cyclopropyl-spiro-piperidine compounds. A method of administering local anesthesia comprises administering an effective amount of a cyclopropyl-spiro-piperidine compound. |
| Applicant(s) |
Merck Sharp & Dohme Corp |
| Representative Drug(s) |
D01RJL |
Drug Info
|
IC50 < 1000000 nM |
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[1] |
|
2
|
D02GCY
|
Drug Info
|
IC50 < 1000000 nM
|
[1] |
|
3
|
D0D8NX
|
Drug Info
|
IC50 < 1000000 nM
|
[1] |
|
4
|
D0OX5S
|
Drug Info
|
IC50 < 1000000 nM
|
[1] |
| Patent ID |
WO2010137351 |
| Title |
Aryl Substituted Carboxamide Derivatives As Calcium or Sodium Channel Blockers. |
| Abstract |
The present invention relates to aryl substituted carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, which have blocking activities of T-type calcium channels or voltage gated sodium channels as the tetrodotoxin-sensitive (TTX-S) blockers such as NaV1.3 and NaV1.7, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels or voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels or voltage gated sodium channels are involved. |
| Applicant(s) |
Raqualia Pharma Inc |
| Representative Drug(s) |
D0M8WO |
Drug Info
|
N.A. |
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[1] |
|
2
|
D0OP5F
|
Drug Info
|
N.A.
|
[1] |
| Patent ID |
WO2012020567 |
| Title |
Acyl Piperazine Derivatives As Ttx-S Blockers. |
| Abstract |
The present invention relates to acyl piperazine derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved. |
| Applicant(s) |
Raqualia Pharma Inc |
| Representative Drug(s) |
D03GPV |
Drug Info
|
IC50 < 5000 nM |
[1] |
| Patent ID |
WO2011103196 |
| Title |
Aryl Carboxamide Derivatives As Sodium Channel Inhibitors for Treatment of Pain. |
| Abstract |
The present invention provides compounds that are inhibitors of voltage-gated sodium channels (Nav), in particular Nav 1.7, and are therefore useful for the treatment of diseases treatable by inhibition of these channels, in particular, chronic pain disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds. |
| Applicant(s) |
Amgen, Inc |
| Representative Drug(s) |
D0I0MT |
Drug Info
|
IC50 > 80000 nM |
[1] |
| Patent ID |
WO2010151597 |
| Title |
Methods for Using Pyrrolo-Benzo-1,4-Diazines As Sodium Channel Blockers. |
| Abstract |
Pyrrolo-benzo-1,4-diazine compounds represented by Formula I or II, or pharmaceutically acceptable salts thereof, are blockers of voltage-gated sodium channels. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, voltage-gated sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, epilepsy or epilepsy conditions, irritable bowel syndrome, depression, anxiety, bipolar disorder, neurodegenerative disorders, psychiatric disorders, myotonia, arrhythmia, movement disorders, neuroendocrine disorders, ataxia, multiple sclerosis, irritable bowel syndrome, incontinence, neuropathy and tinnitus, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. |
| Applicant(s) |
Schering Corp |
| Patent ID |
WO2010022055 |
| Title |
Inhibitors of Voltage-Gated Sodium Channels. |
| Applicant(s) |
Amgen, Inc |
| Representative Drug(s) |
D0E9ZW |
Drug Info
|
IC50 > 5000 nM |
[1] |
| Patent ID |
WO2014066490 |
| Title |
Benzoxazolinone Compounds with Selective Activity In Voltage-Gated Sodium Channels. |
| Abstract |
Disclosed are compounds of Formula A: Formula A, or a salt thereof, wherein "Het", Ra, and Rb are defined herein, which have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating neuropathic pain disorders using the same. |
| Applicant(s) |
Merck Sharp & Dohme Corp |
| Patent ID |
WO2014061970 |
| Title |
Sodium Channel Blockers, Preparation Method Thereof and Use Thereof. |
| Abstract |
The present invention relates to a compound having a blocking effect against sodium ion channels, particularly Nav1.7, a preparation method thereof and the use thereof. A compound represented by formula 1 according to the invention, or a pharmaceutically acceptable salt, hydrate, solvate or isomer thereof may be effectively used for the prevention or treatment of pain, for example, acute pain, chronic pain, neuropathic pain, post-surgery pain, migraine, arthralgia, neuropathy, nerve injury, diabetic neuropathy, neuropathic disease, epilepsy, arrhythmia, myotonia, ataxia, multiple sclerosis, irritable bowel syndrome, urinary incontinence, visceral pain, depression, erythromelalgia, or paroxysmal extreme pain disorder (PEPD). |
| Applicant(s) |
Daewoong Pharmaceutical Co., Ltd |
| Patent ID |
WO2013122897 |
| Title |
Dihydrobenzoxazine and Tetrahydroquinoxaline Sodium Channel Inhibitors. |
| Abstract |
The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention. |
| Applicant(s) |
Amgen Inc |
| Patent ID |
WO2013088315 |
| Title |
Sulfonamide Derivatives. |
| Abstract |
The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav 1.7 inhibitors of Formula (I): or a pharmaceutically acceptable salt thereof, wherein X, Z, R1a, R1b, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain. |
| Applicant(s) |
Pfizer Limited |
| Representative Drug(s) |
D07NQG |
Drug Info
|
N.A. |
[1] |
| Patent ID |
WO2013063459 |
| Title |
Benzoxazolinone Compounds with Selective Activity In Voltage-Gated Sodium Channels. |
| Abstract |
Disclosed are compounds of Formula (A) or a salt thereof, wherein "Het", Ra, and Rb are defined herein, which have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula (A) or their salts, and methods of treating neuropathic pain disorders using the same. |
| Applicant(s) |
Merck Sharp & Dohme Corp |
| Patent ID |
WO2012007877 |
| Title |
N- Sulfonylbenzamides As Inhibitors of Voltage - Gated Sodium Channels. |
| Abstract |
The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula 10 (I): (I) or a pharmaceutically acceptable salt thereof, wherein Z, R 1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain. |
| Applicant(s) |
Pfizer Limited |
| Patent ID |
WO2012004714 |
| Title |
Benzene Sulfonamides As Inhibitors of Voltage-Gated Sodium Channels. |
| Abstract |
The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new sulfonamide Nav1.7 inhibitors of formula (I) or pharmaceutically acceptable salts thereof, wherein X, Y1, Y2, Z, R1, R2 and R3 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain. |
| Applicant(s) |
Pfizer Limited |
| Patent ID |
WO2012004706 |
| Title |
Chemical Compounds. |
| Abstract |
The invention relates to new sulfonamide Nav1.7 inhibitors and pharmaceutically acceptable salts thereof, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain. |
| Applicant(s) |
Pfizer Limited |
| Representative Drug(s) |
D06QWY |
Drug Info
|
N.A. |
[1] |
