Neuromed Pharmaceuticals Ltd.

Zalicus Pharmaceuticals, Ltd.

Neuromed Technologies, Inc.

Other

Merck Sharp + Dohme Corp.

Mark G. Degiacomo, Interim Trustee

Degiacomo, Interim Trustee, Mark G.

Hassan Pajouhesh

Hossein Pajouhesh

Yanbing Ding

Terrance P Snutch

Francesco Belardetti

Lingyun Zhang

Richard James Holland

Gerald Werner Zamponi

Ramesh Kaul

Jason Tan

Yuanxi Zhou

Nagasree Chakka

Yongbao Zhu

Brendan Whelan

Mike Grimwood

Jason Lamontagne

Prasun K Chakravarty

Michael Edward Grimwood

Joseph Leslie Duffy

Pengcheng Patrick Shao

Feng Ye

Sriram Tyagarajan

Navjot Chahal

The invention relates to compounds useful in treating conditions associated with voltage-gated ion channel function, particularly conditions associated with sodium channel activity. More specifically, the invention concerns compounds (e.g., compounds according to any of Formulas (I)-(XIII) and in particular Formula (X), and Compounds (1)-(236) of Table 1) that are useful in treatment of a variety of diseases and conditions. 

Benzimidazole inhibitors of the sodium channel

The invention relates to compounds useful in treating conditions associated with voltage-gated ion channel function, particularly conditions associated with sodium channel activity. More specifically, the invention concerns heterocyclic compounds (e.g., compounds according to any of Formulas (I)-(X) or Compounds (1)-(92) of Table 1) that are that are useful in treatment of conditions such as epilepsy, cancer, pain, migraine, Parkinson's Disease, mood disorders, schizophrenia, psychosis, tinnitus, amyotrophic lateral sclerosis, glaucoma, ischemia, spasticity disorders, obsessive compulsive disorder, restless leg syndrome and Tourette syndrome.

Heterocyclic inhibitors of the sodium channel

The invention relates to compounds useful in treating conditions associated with voltage-gated ion channel function, particularly conditions associated with sodium channel activity. More specifically, the invention concerns compounds (e.g., compounds according to any of Formulas (I)-(XIII) or Compounds (1)-(236) of Table 1) that are useful in treatment of a variety of diseases and conditions. 

Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing N-piperidinyl acetamide derivatives as shown in formula (1). 

N-piperidinyl acetamide derivatives as calcium channel blockers

Compounds of formula (I) which are useful in ameliorating conditions characterized by unwanted sodium and/or calcium channel actrvrh, particularly Na1, 7, Na1, 8, or Ca3, 2 channel activity are disclosed. More specifically, compounds for use in the treatment of conditions such as epilepsy, cancer, pain, migraine, Parkinson's disease, depression, schizophrenia, psychosis, and tinnitus are disclosed. 

Oxopiperazine derivatives for the treatment of pain and epilepsy

A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. 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, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.

Substituted aryl sulfone derivatives as calcium channel blockers

Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing thienopyrimidine or oxoquinazoline derivatives are disclosed of the general formula (1) or formula (2) where X is a linker and Y is an aromatic moiety or N(R5)(R6). 

Bicyclic pyrimidine derivatives as calcium channel blockers

Urea derivatives which comprise compounds of the formula  wherein A is H, B is piperidine and each Ar is phenyl are disclosed as useful in treating conditions such as pain, epilepsy, diabetes or prostate cancer.

Urea derivatives as calcium channel blockers

Urea derivatives which comprise piperidine or piperazine rings and further substitution are effective in ameliorating conditions characterized by unwanted calcium ion channel activity.

Aromatic derivatives of aliphatic diamines are effective in ameliorating conditions characterized by unwanted calcium ion channel activity, especially T-type and N-type channels. These conditions include, for example, stroke and pain.

Diamine calcium channel blockers

The invention relates to novel 3-amino pyrrolidine derivatives, as well as methods for modulating calcium channel activity and for treating conditions associated with calcium channel function. In particular, the compounds generally contain at least one benzhydril moiety, and are useful in treating conditions which benefit from blocking calcium ion channels.

N-type calcium channel blockers

Derivatives of urea that contain piperazine rings and additional substitution with aromatic groups are effective in ameliorating conditions associated with unwanted calcium ion channel activity.

Compounds that are derivatives of 3-aminomethyl-pyrrolidine generally containing at least one benzhydril moiety are useful in treating conditions which benefit from blocking calcium ion channels.

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Vancouver, Canada

Hassan Pajouhesh