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 CA002673435A CA2673435A CA2673435A1 CA 2673435 A1 CA2673435 A1 CA 2673435A1 CA 002673435 A CA002673435 A CA 002673435A 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
delusional
depressive
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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
CA002673435A
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French (fr)
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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
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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
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.
Publication of CA2673435C publication Critical patent/CA2673435C/en
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Expired - Fee Related legal-status Critical Current
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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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32Alcohol-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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.
CA2673435A 2006-12-21 2007-12-03 Succinate salt of 2-((4-(1-methyl-4-(pyridin-4-yl)-1h-pyrazol-3-yl) phenoxy)methyl)quinoline Expired - Fee Related 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
CA2673435A Expired - Fee Related 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 (25)

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)
PL (1) PL2125786T3 (en)
PT (1) PT2125786E (en)
RU (1) RU2430918C2 (en)
SI (1) SI2125786T1 (en)
TW (1) TWI359660B (en)
WO (1) WO2008084299A1 (en)
ZA (1) ZA200904230B (en)

Families Citing this family (6)

* 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
WO2015006689A1 (en) 2013-07-12 2015-01-15 University Of South Alabama Treatment and diagnosis of cancer and precancerous conditions using pde10a inhibitors and methods to measure pde10a expression
KR102233916B1 (en) * 2019-05-28 2021-03-30 주식회사 엘지생활건강 Composition for Skin Moisturizing, Improving Skin Wrinkle and Elasticity comprising PQ1 Succinic Acid

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
EA011451B1 (en) * 2001-02-12 2009-04-28 Уайт Novel succinate salt of o-desmethyl-venlafaxine
MXPA04003192A (en) * 2001-11-29 2004-07-27 Pfizer Prod Inc Succinic acid salts of 5, 8, 14-triazatetracyclo '10.3.1.0 <2,11>.0<4,9> -hexadeca -2(11), 3, 5, 7, 9-pentaene and pharmaceutical compositions thereof.
CA2469889A1 (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
NZ575575A (en) * 2003-08-18 2010-04-30 Lundbeck & Co As H Succinate and malonate salt of trans-4-((1R,3S)-6-chloro-3-phenylindan-1-yl)-1,2,2-trimethylpiperazine and the use as a medicament
ME01142B (en) * 2005-01-07 2013-03-20 Pfizer Prod Inc Heteroaromatic quinoline compounds and their use as pde10 inhibitors
US20060165910A1 (en) 2005-01-21 2006-07-27 Cabot Corporation Processes for forming nanoparticles
AR058361A1 (en) * 2005-12-16 2008-01-30 Wyeth Corp Lyolyzed Compositions of a Triazolopyrimidine Compound

Also Published As

Publication number Publication date
RU2430918C2 (en) 2011-10-10
CN101611029B (en) 2014-09-10
AU2007343135B2 (en) 2013-03-21
DE602007013294D1 (en) 2011-04-28
CY1111919T1 (en) 2015-11-04
RU2009123347A (en) 2011-01-27
IL199389A (en) 2014-01-30
KR20090092338A (en) 2009-08-31
PT2125786E (en) 2011-04-21
DK2125786T3 (en) 2011-05-09
WO2008084299A1 (en) 2008-07-17
KR20120043775A (en) 2012-05-04
JP5254602B2 (en) 2013-08-07
US20100063089A1 (en) 2010-03-11
PL2125786T3 (en) 2011-07-29
NZ577716A (en) 2012-10-26
TWI359660B (en) 2012-03-11
CN101611029A (en) 2009-12-23
EP2125786B1 (en) 2011-03-16
ZA200904230B (en) 2010-04-28
AU2007343135A1 (en) 2008-07-17
CA2673435C (en) 2012-10-09
US8283471B2 (en) 2012-10-09
AT502028T (en) 2011-04-15
SI2125786T1 (en) 2011-05-31
BRPI0720936A2 (en) 2014-03-11
TW200833337A (en) 2008-08-16
JP2008208114A (en) 2008-09-11
EP2125786A1 (en) 2009-12-02
MX2009006528A (en) 2009-06-26
HK1134670A1 (en) 2010-05-07
AR064417A1 (en) 2009-04-01
ES2360014T3 (en) 2011-05-31

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