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CY1108508T1 - ΠΑΡΑΓΩΓΑ 3-ΦΑΙΝΥΛ-ΠΥΡΑΖΟΛΙΟΥ ΩΣ ΡΥΘΜΙΣΤΕΣ ΤΟΥ ΥΠΟΔΟΧΕΑ 5-HT-2a ΣΕΡΟΤΟΝΙΝΗΣ ΧΡΗΣΙΜΑ ΓΙΑ ΤΗ ΘΕΡΑΠΕΙΑ ΔΙΑΤΑΡΑΧΩΝ ΠΟΥ ΣΧΕΤΙΖΟΝΤΑΙ ΜΕ ΑΥΤΟΝ - Google Patents

ΠΑΡΑΓΩΓΑ 3-ΦΑΙΝΥΛ-ΠΥΡΑΖΟΛΙΟΥ ΩΣ ΡΥΘΜΙΣΤΕΣ ΤΟΥ ΥΠΟΔΟΧΕΑ 5-HT-2a ΣΕΡΟΤΟΝΙΝΗΣ ΧΡΗΣΙΜΑ ΓΙΑ ΤΗ ΘΕΡΑΠΕΙΑ ΔΙΑΤΑΡΑΧΩΝ ΠΟΥ ΣΧΕΤΙΖΟΝΤΑΙ ΜΕ ΑΥΤΟΝ

Info

Publication number
CY1108508T1
CY1108508T1 CY20081101299T CY081101299T CY1108508T1 CY 1108508 T1 CY1108508 T1 CY 1108508T1 CY 20081101299 T CY20081101299 T CY 20081101299T CY 081101299 T CY081101299 T CY 081101299T CY 1108508 T1 CY1108508 T1 CY 1108508T1
Authority
CY
Cyprus
Prior art keywords
psychosis
schizophrenia
disorders
pharmaceutical compositions
atrial fibrillation
Prior art date
Application number
CY20081101299T
Other languages
English (en)
Inventor
Bradley Teegarden
Yifeng Xiong
Sonja Strah-Pleynet
Honnappa Jayakumar
Peter I Dosa
Konrad Feichtinger
Martin Casper
Juerg Lehmann
Robert M Jones
David J Unett
Jin Sun Karoline Choi
Original Assignee
Arena Pharmaceuticals, Inc.
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
Application filed by Arena Pharmaceuticals, Inc. filed Critical Arena Pharmaceuticals, Inc.
Publication of CY1108508T1 publication Critical patent/CY1108508T1/el

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—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 being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms
    • C07D231/16—Halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/02—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
    • C07D401/12—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—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
    • C07D409/12—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
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—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
    • C07D413/10—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 carbon chain containing aromatic rings
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—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
    • C07D413/12—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
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    • C07D417/02—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 C07D415/00 containing two hetero rings
    • C07D417/12—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 C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
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  • Chemical & Material Sciences (AREA)
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  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Η παρούσα εφεύρεση αφορά ορισμένα παράγωγα 3-φαινυλ-πυραζολίου του τύπου (1a) και φαρμακευτικές συνθέσεις αυτών που ρυθμίζουν τη δραστικότητα του 5-ΗΤ2Α υποδοχέα σεροτονίνης. Ενώσεις και φαρμακευτικές συνθέσεις αυτών κατευθύνονται σε μεθόδους χρήσιμες στη θεραπεία συσσωμάτωσης αιμοπεταλίου, ασθένειας στεφανιαίας αρτηρίας, μυοκαρδιακής απόφραξης, πρόσκαιρης ισχαιμικής προσβολής, στηθάγχης, εμβολής, κολπικής μαρμαρυγής, μείωσης του κινδύνου σχηματισμού θρόμβου αίματος, άσθματος ή συμπτωμάτων αυτού, ανησυχίας ή συμπτώματος, συμπεριφορικών διαταραχών, προκαλούμενης από φάρμακο ψύχωσης, διεγερτικής ψύχωσης, συνδρόμου Gilles de la Tourette, μανιακής διαταραχής, οργανικής ή NOS ψύχωσης, ψυχωτικής διαταραχής, ψύχωσης, οξείας σχιζοφρένειας, χρόνιας σχιζοφρένειας, NOS σχιζοφρένειας και σχετικών διαταραχών και διαταραχών ύπνου, διαταραχών ύπνου, διαβητικών-σχετικών διαταραχών, προοδευτικής πολυεστιακής λευκοεγκεφαλοπάθειας και των παρομοίων. Η παρούσα εφεύρεση επίσης αφορά μεθόδους για τη θεραπεία διαταραχών που προκαλούνται από υποδοχέα 5-ΗΤ2Α σεροτονίνης σε συνδυασμό με άλλους φαρμακευτικούς παράγοντες που χορηγούνται ξεχωριστά ή μαζί.
CY20081101299T 2004-11-19 2008-11-13 ΠΑΡΑΓΩΓΑ 3-ΦΑΙΝΥΛ-ΠΥΡΑΖΟΛΙΟΥ ΩΣ ΡΥΘΜΙΣΤΕΣ ΤΟΥ ΥΠΟΔΟΧΕΑ 5-HT-2a ΣΕΡΟΤΟΝΙΝΗΣ ΧΡΗΣΙΜΑ ΓΙΑ ΤΗ ΘΕΡΑΠΕΙΑ ΔΙΑΤΑΡΑΧΩΝ ΠΟΥ ΣΧΕΤΙΖΟΝΤΑΙ ΜΕ ΑΥΤΟΝ CY1108508T1 (el)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US62977404P 2004-11-19 2004-11-19
US64763905P 2005-01-26 2005-01-26
US65838405P 2005-03-02 2005-03-02
US71338405P 2005-09-01 2005-09-01
US73316505P 2005-11-04 2005-11-04
EP05849546A EP1833799B1 (en) 2004-11-19 2005-11-17 3-PHENYL-PYRAZOLE DERIVATIVES AS MODULATORS OF THE 5-HT-2a SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO

Publications (1)

Publication Number Publication Date
CY1108508T1 true CY1108508T1 (el) 2014-04-09

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CY20081101299T CY1108508T1 (el) 2004-11-19 2008-11-13 ΠΑΡΑΓΩΓΑ 3-ΦΑΙΝΥΛ-ΠΥΡΑΖΟΛΙΟΥ ΩΣ ΡΥΘΜΙΣΤΕΣ ΤΟΥ ΥΠΟΔΟΧΕΑ 5-HT-2a ΣΕΡΟΤΟΝΙΝΗΣ ΧΡΗΣΙΜΑ ΓΙΑ ΤΗ ΘΕΡΑΠΕΙΑ ΔΙΑΤΑΡΑΧΩΝ ΠΟΥ ΣΧΕΤΙΖΟΝΤΑΙ ΜΕ ΑΥΤΟΝ

Country Status (36)

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US (6) US20070244086A1 (el)
EP (2) EP1978019A1 (el)
JP (1) JP5016494B2 (el)
KR (2) KR20130027039A (el)
CN (3) CN101084195B (el)
AR (1) AR051675A1 (el)
AT (1) ATE407927T1 (el)
AU (1) AU2005307744C1 (el)
BR (1) BRPI0518446A2 (el)
CA (1) CA2588513C (el)
CR (1) CR9098A (el)
CY (1) CY1108508T1 (el)
DE (1) DE602005009748D1 (el)
DK (1) DK1833799T3 (el)
EA (1) EA011935B1 (el)
ES (1) ES2314750T3 (el)
GT (1) GT200500336A (el)
HN (1) HN2005032627A (el)
HR (1) HRP20080592T3 (el)
IL (1) IL182945A (el)
MA (1) MA29081B1 (el)
MX (1) MX2007005959A (el)
MY (1) MY147684A (el)
NI (1) NI200700127A (el)
NO (1) NO340656B1 (el)
NZ (1) NZ554817A (el)
PE (1) PE20061130A1 (el)
PL (1) PL1833799T3 (el)
PT (1) PT1833799E (el)
RS (1) RS50698B (el)
SA (1) SA05260357B1 (el)
SI (1) SI1833799T1 (el)
SV (1) SV2008002307A (el)
TN (1) TNSN07188A1 (el)
TW (2) TWI409062B (el)
WO (1) WO2006055734A2 (el)

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BRPI0412263B1 (pt) 2003-07-22 2019-10-15 Arena Pharmaceuticals, Inc. Derivados de diaril e aril heteroaril uréia, uso e composição farmacêutica contendo os mesmos, bem como processo para preparação da dita composição
WO2005103011A1 (en) 2004-03-23 2005-11-03 Arena Pharmaceuticals, Inc. Processes for preparing substituted n-aryl-n’-[3-(1h-pyrazol-5-yl) phenyl] ureas and intermediates thereof
SA05260357B1 (ar) * 2004-11-19 2008-09-08 ارينا فارماسيتو تيكالز ، أنك مشتقات 3_فينيل_بيرازول كمعدلات لمستقبل سيروتينين 5_ht2a مفيدة في علاج الاضطرابات المتعلقه به
EP2018371B1 (en) 2006-05-18 2015-03-04 Arena Pharmaceuticals, Inc. Primary amines and derivatives thereof as modulators of the 5-ht2a serotonin receptor useful for the treatment of disorders related thereto
EP2027119A2 (en) 2006-05-18 2009-02-25 Arena Pharmaceuticals, Inc. Ethers, secondary amines and derivatives thereof as modulators of the 5-ht2a serotonin receptor useful for the treatment of disorders related thereto
CN102827081A (zh) 2006-05-18 2012-12-19 艾尼纳制药公司 用作5-ht2a 血清素受体调节剂的苯基-吡唑的晶型和其制备方法
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