[go: up one dir, main page]

WO2010039913A1 - Composé calcilytique - Google Patents

Composé calcilytique Download PDF

Info

Publication number
WO2010039913A1
WO2010039913A1 PCT/US2009/059159 US2009059159W WO2010039913A1 WO 2010039913 A1 WO2010039913 A1 WO 2010039913A1 US 2009059159 W US2009059159 W US 2009059159W WO 2010039913 A1 WO2010039913 A1 WO 2010039913A1
Authority
WO
WIPO (PCT)
Prior art keywords
alkyl
methyl
heteroaryl
heterocycloalkyl
compound
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.)
Ceased
Application number
PCT/US2009/059159
Other languages
English (en)
Inventor
Michael P. Demartino
Jae U. Jeong
Robert W. Marquis, Jr.
Joshi M. Ramanjulu
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.)
GlaxoSmithKline LLC
Original Assignee
GlaxoSmithKline LLC
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 GlaxoSmithKline LLC filed Critical GlaxoSmithKline LLC
Publication of WO2010039913A1 publication Critical patent/WO2010039913A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • 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
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4535—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/662—Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
    • A61K31/663—Compounds having two or more phosphorus acid groups or esters thereof, e.g. clodronic acid, pamidronic acid
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Definitions

  • the composition is in unit dosage form.
  • a tablet, or capsule may be administered, for nasal application, a metered aerosol dose may be administered, for transdermal application, a topical formulation or patch may be administered and for transmucosal delivery, a buccal patch may be administered.
  • dosing is such that the patient may administer a single dose.
  • treatment includes, but is not limited to prevention, retardation, and prophylaxis of the disease.
  • the compound administered to a patient causes an increase in serum PTH for a period of more than about twenty- four hours provided that it is co-administered with an anti resorptive agent.
  • compositions for inhalation are in the form of a solution, suspension or emulsion that may be administered as a dry powder or in the form of an aerosol using a conventional propellant such as dichlorodifluoromethane or trichlorofluoromethane.
  • the medium was decanted and the cell monolayer was washed twice with phosphate-buffered saline (PBS) kept at 37 0 C. After the second wash, 6 mL of 0.02% EDTA in PBS was added and incubated for 4 minutes at 37 0 C. Following the incubation, cells were dispersed by gentle agitation.
  • PBS phosphate-buffered saline
  • FTIR FTIR spectroscopy
  • FTIR spectra were recorded on a Nicolet 510 infrared spectrometer. FTIR spectra were recorded in transmission mode, and band positions are reported in inverse wavenumbers (cm'l). Mass spectra were taken on either a SCIEX5 or Micromass instruments, using electrospray (ES) ionization techniques. Elemental analyses were obtained using a Perkin- Elmer 240C elemental analyzer. Melting points were taken on a Thomas-Hoover melting point apparatus and are uncorrected. All temperatures are reported in degrees Celsius. Analtech Silica Gel GF and E. Merck Silica Gel 60 F-254 thin layer plates were used for thin layer chromatography. Both flash and gravity chromatography were carried out on E.

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention porte sur de nouveaux composés calcilytiques, sur des compositions pharmaceutiques, sur des procédés de synthèse et sur des procédés d'utilisation associés.
PCT/US2009/059159 2008-10-01 2009-10-01 Composé calcilytique Ceased WO2010039913A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US10187908P 2008-10-01 2008-10-01
US61/101,879 2008-10-01

Publications (1)

Publication Number Publication Date
WO2010039913A1 true WO2010039913A1 (fr) 2010-04-08

Family

ID=42073875

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2009/059159 Ceased WO2010039913A1 (fr) 2008-10-01 2009-10-01 Composé calcilytique

Country Status (1)

Country Link
WO (1) WO2010039913A1 (fr)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2025015268A1 (fr) * 2023-07-13 2025-01-16 Aconcagua Bio, Inc. Modulateurs de l'activité du récepteur de la calcitonine et/ou du récepteur de l'amyline
US12486269B2 (en) 2024-02-08 2025-12-02 Aconcagua Bio, Inc. Compounds and compositions for treating conditions associated with calcitonin receptor and/or amylin receptor activity

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007062370A2 (fr) * 2005-11-22 2007-05-31 Smithkline Beecham Corporation Composes calcilytiques
US20070232628A1 (en) * 2004-05-06 2007-10-04 Luengo Juan I Calcilytic Compounds

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070232628A1 (en) * 2004-05-06 2007-10-04 Luengo Juan I Calcilytic Compounds
WO2007062370A2 (fr) * 2005-11-22 2007-05-31 Smithkline Beecham Corporation Composes calcilytiques

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2025015268A1 (fr) * 2023-07-13 2025-01-16 Aconcagua Bio, Inc. Modulateurs de l'activité du récepteur de la calcitonine et/ou du récepteur de l'amyline
US12486269B2 (en) 2024-02-08 2025-12-02 Aconcagua Bio, Inc. Compounds and compositions for treating conditions associated with calcitonin receptor and/or amylin receptor activity

Similar Documents

Publication Publication Date Title
JP7256300B2 (ja) グルカゴン様ペプチド１受容体アゴニスト
TWI767410B (zh) 作為lpa受體拮抗劑之三唑胺基甲酸酯吡啶基磺醯胺及其用途
CN108602776B (zh) 用作irak抑制剂的杂芳基化合物及其用途
KR100813384B1 (ko) ＺＡＰ-70 및(또는) Ｓｙｋ 억제제로서의 2,4디(헤테로)-아릴아미노-피리미딘 유도체
CA3149963A1 (fr) Inhibiteurs heterocycliques de la kinase rip1
CA2971640A1 (fr) Modulateurs de cot et procedes d'utilisation associes
KR20200100713A (ko) Lpa 길항제로서의 시클로헥실 산 트리아졸 아졸
WO2014079150A1 (fr) Composés hétérocycliques et leurs procédés d'utilisation
TW200911245A (en) Pyridone derivatives
JP6559699B2 (ja) 置換含窒素複素環誘導体、それを含む医薬組成物及びその抗腫瘍性の適用
WO2019101086A1 (fr) Inhibiteur de ssao/vap-1 halo-allylamine et son utilisation
CN102112450A (zh) 5-炔基-嘧啶
JP7629442B2 (ja) 肝臓再生を促進または肝細胞死を縮減もしくは防止するためのヘテロアリール置換ピラゾロ－ピリジンタンパク質キナーゼ阻害剤
JP5508257B2 (ja) アリールアミドピリミドン化合物
HK1219482A1 (zh) 基於喹唑啉的呼吸道合胞病毒抑制剂
JP6883045B2 (ja) オレキシン受容体調節因子としてのハロ置換ピペリジン
WO2018113085A1 (fr) Inhibiteurs de la tyrosine kinase de bruton
CN112020494A (zh) 用作tlr2信号转导调节剂的化合物
CN112189012A (zh) 作为pi3激酶和自噬途径的调节剂的三取代芳基和杂芳基衍生物
AU2017393297A1 (en) Integrin antagonists
KR20100016528A (ko) 신경퇴행성 질환의 치료를 위한 아릴아미드 피리미돈 유도체
AU2023315120A1 (en) Novel 7-substituted indole sulfonamide derivatives
JP2025540714A (ja) Ｌｐａ受容体活性と関連する状態を処置するための化合物および組成物
JP2025523939A (ja) 新規のナフチルおよびイソキノリンスルホンアミド誘導体
JPWO2016098793A1 (ja) 環状グアニジル基を有するチアゾール誘導体

Legal Events

Date Code Title Description
121 Ep: the epo has been informed by wipo that ep was designated in this application

Ref document number: 09818487

Country of ref document: EP

Kind code of ref document: A1

NENP Non-entry into the national phase

Ref country code: DE

WWE Wipo information: entry into national phase

Ref document number: 2009818487

Country of ref document: EP

122 Ep: pct application non-entry in european phase

Ref document number: 09818487

Country of ref document: EP

Kind code of ref document: A1