CA2673435A1 - Succinate salt of 2-((4-(1-methyl-4-(pyridin-4-yl)-1h-pyrazol-3-yl) phenoxy)methyl)quinoline - Google Patents

Succinate salt of 2-((4-(1-methyl-4-(pyridin-4-yl)-1h-pyrazol-3-yl) phenoxy)methyl)quinoline Download PDF

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Publication number
CA2673435A1
CA2673435A1 CA 2673435 CA2673435A CA2673435A1 CA 2673435 A1 CA2673435 A1 CA 2673435A1 CA 2673435 CA2673435 CA 2673435 CA 2673435 A CA2673435 A CA 2673435A CA 2673435 A1 CA2673435 A1 CA 2673435A1
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CA
Canada
Prior art keywords
disorder
salt
dementia
succinate salt
delusional
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
CA 2673435
Other languages
French (fr)
Other versions
CA2673435C (en
Inventor
Patrick Robert Vorhoest
Caroline Proulx
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Pfizer Products Inc
Original Assignee
Pfizer Products Inc.
Patrick Robert Vorhoest
Caroline Proulx
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
Priority to US87126006P priority Critical
Priority to US60/871,260 priority
Application filed by Pfizer Products Inc., Patrick Robert Vorhoest, Caroline Proulx filed Critical Pfizer Products Inc.
Priority to PCT/IB2007/003819 priority patent/WO2008084299A1/en
Publication of CA2673435A1 publication Critical patent/CA2673435A1/en
Application granted granted Critical
Publication of CA2673435C publication Critical patent/CA2673435C/en
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=39321475&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CA2673435(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application status is Active legal-status Critical
Anticipated expiration legal-status Critical

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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 three or more hetero rings

Abstract

The present invention relates to a succinate salt of 2-((4-(1-methyl-4- (pyridin-4-yl)-1 H-pyrazol-3-yl)phenoxy)methyl)quinoline, and to a method for treating disorders of the Central Nervous System (CNS) and other disorders in a mammal, including a human, by administering to the mammal the succinate salt. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier and the succinate salt.

Claims (14)

1. A succinate salt of Formula I:
2. The salt according to claim 1, wherein the salt has characteristic X-ray powder diffraction peaks as measured with copper radiation of 2-Theta ~
0.1 °
of 15.8, 21.0 and 26.6.
3. The salt according to claim 1, wherein the salt has characteristic X-ray powder diffraction peaks as measured with copper radiation of 2-Theta ~
0.1 °
of 15.8, 16.7, 21.0, 24.2 and 26.6.
4. The salt according to claim 1, wherein the salt has the characteristic X-ray powder diffraction pattern of FIG. 1.
5. The salt according to claim 1, 2, 3 or 4, wherein the salt has a melting onset temperature of 184 ~ 3°C.
6. The salt according to claim 1, 2, 3, 4 or 5, wherein the salt increases in weight by less than 0.5% at 90 ~ 2% relative humidity in an isothermal (25.1 ~ 0.1 °C) moisture sorption test conducted from approximately 1%
to 90%
(~2%) humidity.
7. The salt according to claim 1, 2, 3, 4, 5 or 6, wherein the salt is anhydrous.
8. A pharmaceutical composition comprising a succinate salt as defined in claim 1, 2, 3, 4, 5, 6 or 7, and a pharmaceutically acceptable carrier.
9. The pharmaceutical composition according to claim 8 wherein the succinate salt is crystalline.
10. A pharmaceutical composition for use in the treatment of a psychotic disorder, delusional disorder or drug induced psychosis; anxiety disorder, movement disorder, mood disorder, neurodegenerative disorder or drug addiction, comprising an amount of a succinate salt as defined in claim 1, 2, 3, 4, 5, 6 or 7 effective in treating said disorder or condition, and a pharmaceutically acceptable carrier.
11. Use of an effective amount of a succinate salt as defined in claim 1, 2, 3, 4, 5, 6 or 7 for the treatment of a psychotic disorder, delusional disorder or drug induced psychosis; anxiety disorder, movement disorder, mood disorder, or neurodegenerative disorder.
12. Use of an effective amount of a succinate salt as defined in claim 1, 2, 3, 4, 5, 6 or 7 for the treatment of dementia, Alzheimer's disease, multi-infarct dementia, alcoholic dementia or other drug-related dementia, dementia associated with intracranial tumors or cerebral trauma, dementia associated with Huntington's disease or Parkinson's disease, or AIDS-related dementia; delirium; amnestic disorder; post-traumatic stress disorder; mental retardation; a learning disorder, reading disorder, mathematics disorder, or a disorder of written expression;
attention-deficit/hyperactivity disorder; age-related cognitive decline, major depressive episode of the mild, moderate or severe type; a manic or mixed mood episode; a hypomanic mood episode; a depressive episode with atypical features;
a depressive episode with melancholic features; a depressive episode with catatonic features; a mood episode with postpartum onset; post-stroke depression; major depressive disorder; dysthymic disorder; minor depressive disorder; premenstrual dysphoric disorder; post-psychotic depressive disorder of schizophrenia; a major depressive disorder superimposed on a psychotic disorder comprising a delusional disorder or schizophrenia; a bipolar disorder comprising bipolar I disorder, bipolar II disorder, cyclothymic disorder, Parkinson's disease;
Huntington's disease; dementia, Alzheimer's disease, multi-infarct dementia, AIDS-related dementia, Fronto temperal Dementia; neurodegeneration associated with cerebral trauma; neurodegeneration associated with stroke;
neurodegeneration associated with cerebral infarct; hypoglycemia-induced neurodegeneration; neurodegeneration associated with epileptic seizure;
neurodegeneration associated with neurotoxin poisoning; multi-system atrophy, paranoid, disorganized, catatonic, undifferentiated or residual type;
schizophreniform disorder; schizoaffective disorder of the delusional type or the depressive type; delusional disorder; substance-induced psychotic disorder, psychosis induced by alcohol, amphetamine, cannabis, cocaine, hallucinogens, inhalants, opioids, or phencyclidine; personality disorder of the paranoid type; or personality disorder of the schizoid type.
13. Use of an amount of the succinate salt as defined in claim 1, 2, 3, 4, 5, 6 or 7 effective in inhibiting PDE10 for the treatment of a psychotic disorder, delusional disorder or drug induced psychosis; anxiety disorder, movement disorder, mood disorder, neurodegenerative disorder or drug addiction.
14. Use of a succinate salt as defined in claim 1, 2, 3, 4, 5, 6 or 7 in the manufacture of a medicament for the treatment of a psychotic disorder, delusional disorder or drug induced psychosis; anxiety disorder, movement disorder, mood disorder, neurodegenerative disorder or drug addiction.
CA 2673435 2006-12-21 2007-12-03 Succinate salt of 2-((4-(1-methyl-4-(pyridin-4-yl)-1h-pyrazol-3-yl) phenoxy)methyl)quinoline Active CA2673435C (en)

Priority Applications (3)

Application Number Priority Date Filing Date Title
US87126006P true 2006-12-21 2006-12-21
US60/871,260 2006-12-21
PCT/IB2007/003819 WO2008084299A1 (en) 2006-12-21 2007-12-03 Succinate salt of 2-((4-(1-methyl-4-(pyridin-4-yl)-1h-pyrazol-3-yl) phenoxy)methyl)quinoline

Publications (2)

Publication Number Publication Date
CA2673435A1 true CA2673435A1 (en) 2008-07-17
CA2673435C CA2673435C (en) 2012-10-09

Family

ID=39321475

Family Applications (1)

Application Number Title Priority Date Filing Date
CA 2673435 Active CA2673435C (en) 2006-12-21 2007-12-03 Succinate salt of 2-((4-(1-methyl-4-(pyridin-4-yl)-1h-pyrazol-3-yl) phenoxy)methyl)quinoline

Country Status (23)

Country Link
US (1) US8283471B2 (en)
EP (1) EP2125786B1 (en)
JP (1) JP5254602B2 (en)
KR (2) KR20090092338A (en)
CN (1) CN101611029B (en)
AR (1) AR064417A1 (en)
AT (1) AT502028T (en)
AU (1) AU2007343135B2 (en)
BR (1) BRPI0720936A2 (en)
CA (1) CA2673435C (en)
CY (1) CY1111919T1 (en)
DE (1) DE602007013294D1 (en)
DK (1) DK2125786T3 (en)
ES (1) ES2360014T3 (en)
HK (1) HK1134670A1 (en)
IL (1) IL199389A (en)
MX (1) MX2009006528A (en)
NZ (1) NZ577716A (en)
PT (1) PT2125786E (en)
RU (1) RU2430918C2 (en)
TW (1) TWI359660B (en)
WO (1) WO2008084299A1 (en)
ZA (1) ZA200904230B (en)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010033045A1 (en) * 2008-09-16 2010-03-25 Igor Anatolievich Pomytkin Compositions and methods for prevention or treatment of beta amyloid deposition
TWI396689B (en) * 2008-11-14 2013-05-21 Amgen Inc Pyrazine derivatives as phosphodiesterase 10 inhibitors
US20120214842A1 (en) * 2011-02-18 2012-08-23 Exonhit Therapeutics Sa Methods for treating diseases of the retina
US9464076B2 (en) 2013-03-15 2016-10-11 Daiichi Sankyo Company, Limited Benzothiophene derivative
US10039764B2 (en) 2013-07-12 2018-08-07 University Of South Alabama Treatment and diagnosis of cancer and precancerous conditions using PDE10A inhibitors and methods to measure PDE10A expression

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5795909A (en) * 1996-05-22 1998-08-18 Neuromedica, Inc. DHA-pharmaceutical agent conjugates of taxanes
WO2002064543A2 (en) * 2001-02-12 2002-08-22 Wyeth Novel succinate salt of o-desmethyl-venlafaxine
ES2258652T3 (en) * 2001-11-29 2006-09-01 Pfizer Products Inc. Succinate salts of 5,8,14-triazatetracyclo (10.3.1.02,11.04,9) -hexadeca-2 (11), 3,5,7,9-pentaene and pharmaceutical compositions thereof.
WO2003050108A1 (en) * 2001-12-12 2003-06-19 Pfizer Products Inc. Salt forms of e-2-methoxy-n-(3-(4-(3-methyl-pyridin-3-yloxy)-phenylamino)-quinazolin-6-yl)-allyl)-acetamide, its preparation and its use against cancer
BRPI0413555A (en) * 2003-08-18 2006-10-17 Lundbeck & Co As H compound or salt thereof, pharmaceutical composition, use of a compound or salt and method for treating a disease, for the manufacture of a compound and for the preparation of compound
UA86283C2 (en) * 2005-01-07 2009-04-10 Пфайзер Продактс Инк. Heteroaromatic quinoline compounds and use thereof as pde10 inhibitors
WO2006078828A2 (en) 2005-01-21 2006-07-27 Cabot Corporation Method of making nanoparticulates and use of the nanoparticulates to make products using a flame reactor
US20070149552A1 (en) * 2005-12-16 2007-06-28 Wyeth Lyophilized compositions of a triazolopyrimidine compound

Also Published As

Publication number Publication date
EP2125786B1 (en) 2011-03-16
EP2125786A1 (en) 2009-12-02
JP5254602B2 (en) 2013-08-07
CN101611029A (en) 2009-12-23
TW200833337A (en) 2008-08-16
AU2007343135B2 (en) 2013-03-21
CY1111919T1 (en) 2015-11-04
BRPI0720936A2 (en) 2014-03-11
US8283471B2 (en) 2012-10-09
ES2360014T3 (en) 2011-05-31
AR064417A1 (en) 2009-04-01
IL199389A (en) 2014-01-30
CA2673435C (en) 2012-10-09
CN101611029B (en) 2014-09-10
PT2125786E (en) 2011-04-21
SI2125786T1 (en) 2011-05-31
TWI359660B (en) 2012-03-11
MX2009006528A (en) 2009-06-26
WO2008084299A1 (en) 2008-07-17
NZ577716A (en) 2012-10-26
RU2430918C2 (en) 2011-10-10
KR20090092338A (en) 2009-08-31
AU2007343135A1 (en) 2008-07-17
DE602007013294D1 (en) 2011-04-28
JP2008208114A (en) 2008-09-11
HK1134670A1 (en) 2015-06-19
DK2125786T3 (en) 2011-05-09
RU2009123347A (en) 2011-01-27
US20100063089A1 (en) 2010-03-11
KR20120043775A (en) 2012-05-04
ZA200904230B (en) 2010-04-28
AT502028T (en) 2011-04-15

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