AR058545A1 - Sintesis en un solo recipiente de derivados tetrazolicos de rapamicina(sirolimus) y composiciones farmaceuticas que los contienen. - Google Patents

Sintesis en un solo recipiente de derivados tetrazolicos de rapamicina(sirolimus) y composiciones farmaceuticas que los contienen.

Info

Publication number
AR058545A1
AR058545A1 ARP060105535A ARP060105535A AR058545A1 AR 058545 A1 AR058545 A1 AR 058545A1 AR P060105535 A ARP060105535 A AR P060105535A AR P060105535 A ARP060105535 A AR P060105535A AR 058545 A1 AR058545 A1 AR 058545A1
Authority
AR
Argentina
Prior art keywords
cycloalkyl
group
formula
molecule
alkyl
Prior art date
Application number
ARP060105535A
Other languages
English (en)
Inventor
Madhup Dhaon
Chu-Nung Hsiao
Subhash Patel
Young Chen
Sanjay Chemburkar
Peter Bonk
Original Assignee
Abbott Lab
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
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=38371962&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR058545(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Abbott Lab filed Critical Abbott Lab
Publication of AR058545A1 publication Critical patent/AR058545A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18—Bridged systems
    • 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
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • C07D413/02—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
    • C07D413/08—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 alicyclic rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicinal Preparation (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Reivindicacion 1: Un método para preparar una molécula de formula (1) caracterizado porque comprende (a) hacer reaccionar una molécula de formula (2) con anhídrido tríflico, para producir una molécula de formula (3) y (b) hacer reaccionar la molécula de formula (3) con una molécula de formula (4) donde R1 se selecciona del grupo que consiste en =O(H, H) y (H, OH); R2 y R5 se seleccionan independientemente del grupo que consiste en H, -C(=O)R6, -C(=O)OR6, -C(=O)NHR6 y -C(=S)OR6; R3 se selecciona del grupo que consiste en =O y OR5; o R2 y R3 pueden tomarse juntos para formar una porcion de formula A-C(R7)(R8)-O-B, donde A es un enlace a un O unido al C 28 y B está unido al C 28, como se definio con anterioridad; R4 se selecciona del grupo que consiste en H y alquilo C1-4; R6 se selecciona del grupo que consiste en alquilo C1-10, cicloalquilo C3-6, grupos arilo y grupos heterocíclicos; R7 y R8 se seleccionan independientemente del grupo que consiste en H, alquilo C1-6, o R7 y R8 tomados juntos son =O; R9 y R10 se seleccionan independientemente del grupo que consiste en H, alquenilo, alquenilcicloalquenilo, alquenilcicloalquilo, alquilo, alquilcicloalquenilo, alquilcicloalquilo, alquinilo, aralquilo, arilo, cicloalquenilo, cicloalquilo, cicloalquilalquilo, cicloalquilcicloalquilo, cicloalquenilalquilo, heterociclilo, aza, amida, amonio, oxa, tia, sulfonilo, sulfinilo, sulfonamida, fosforilo, fosfinilo, fosfino, fosfonio, ceto, éster, alcohol, carbamato, urea, tiocarbonilo, boratos, boranos, boraza, sililo, siloxilo, silaza, y combinaciones de estos. Reivindicacion 2: El método de la reivindicacion 1, caracterizado porque se realiza en un solo recipiente.
ARP060105535A 2005-12-14 2006-12-14 Sintesis en un solo recipiente de derivados tetrazolicos de rapamicina(sirolimus) y composiciones farmaceuticas que los contienen. AR058545A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US11/300,671 US7700614B2 (en) 2005-12-14 2005-12-14 One pot synthesis of tetrazole derivatives of rapamycin

Publications (1)

Publication Number Publication Date
AR058545A1 true AR058545A1 (es) 2008-02-13

Family

ID=38371962

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP060105535A AR058545A1 (es) 2005-12-14 2006-12-14 Sintesis en un solo recipiente de derivados tetrazolicos de rapamicina(sirolimus) y composiciones farmaceuticas que los contienen.

Country Status (16)

Country Link
US (2) US7700614B2 (es)
EP (4) EP2712867A1 (es)
JP (3) JP5457678B2 (es)
KR (7) KR20130121991A (es)
CN (2) CN101331138B (es)
AR (1) AR058545A1 (es)
AU (1) AU2006338175B2 (es)
BR (1) BRPI0619844A2 (es)
CA (3) CA2936497C (es)
ES (1) ES2642054T3 (es)
IL (2) IL191693A (es)
MX (1) MX349034B (es)
NZ (1) NZ568304A (es)
TW (1) TWI386413B (es)
WO (1) WO2007094886A2 (es)
ZA (1) ZA200804209B (es)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7700614B2 (en) * 2005-12-14 2010-04-20 Abbott Laboratories One pot synthesis of tetrazole derivatives of rapamycin
CN102234288B (zh) * 2010-05-06 2014-07-02 上海医药工业研究院 唑他莫司的制备方法
JP5985474B2 (ja) 2010-08-04 2016-09-06 メリル ライフ サイエンシズ ピーブィティ．エルティディ 抗増殖特性を有する新規４２−ｏ−（ヘテロアルコキシアルキル）ラパマイシン化合物の調製プロセス
CN102731527A (zh) * 2012-07-12 2012-10-17 浙江医药股份有限公司新昌制药厂 一种西罗莫司42－醚衍生物的合成方法
SG11201507406YA (en) * 2013-03-15 2015-10-29 Biosensors Int Group Ltd Purification of rapamycin derivatives
CN108948046B (zh) * 2017-05-20 2020-11-10 鲁南制药集团股份有限公司 一种替西罗莫司的中间体及其制备方法

Family Cites Families (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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US3993749A (en) 1974-04-12 1976-11-23 Ayerst Mckenna And Harrison Ltd. Rapamycin and process of preparation
US4885171A (en) 1978-11-03 1989-12-05 American Home Products Corporation Use of rapamycin in treatment of certain tumors
US4401653A (en) 1981-03-09 1983-08-30 Ayerst, Mckenna & Harrison Inc. Combination of rapamycin and picibanil for the treatment of tumors
JPH04230389A (ja) 1990-07-16 1992-08-19 American Home Prod Corp ラパマイシン誘導体
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PT98990A (pt) 1990-09-19 1992-08-31 American Home Prod Processo para a preparacao de esteres de acidos carboxilicos de rapamicina
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US5120727A (en) 1991-05-29 1992-06-09 American Home Products Corporation Rapamycin dimers
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FR2736550B1 (fr) 1995-07-14 1998-07-24 Sandoz Sa Composition pharmaceutique sous la forme d'une dispersion solide comprenant un macrolide et un vehicule
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Also Published As

Publication number Publication date
MX349034B (es) 2017-07-07
WO2007094886A2 (en) 2007-08-23
JP5457678B2 (ja) 2014-04-02
NZ568304A (en) 2011-07-29
KR101580896B1 (ko) 2016-01-06
CN101331138B (zh) 2013-05-15
BRPI0619844A2 (pt) 2011-10-18
US7700614B2 (en) 2010-04-20
ZA200804209B (en) 2010-08-25
CN102746321A (zh) 2012-10-24
CA2631971C (en) 2016-10-04
WO2007094886A3 (en) 2007-11-29
EP2862863B1 (en) 2017-09-06
KR20130121991A (ko) 2013-11-06
KR20080080185A (ko) 2008-09-02
AU2006338175A1 (en) 2007-08-23
US20100204466A1 (en) 2010-08-12
IL218681A (en) 2013-10-31
JP2009519963A (ja) 2009-05-21
IL218681A0 (en) 2012-05-31
TW200745134A (en) 2007-12-16
EP2712867A1 (en) 2014-04-02
KR20170010115A (ko) 2017-01-25
JP2013032368A (ja) 2013-02-14
JP2013032367A (ja) 2013-02-14
US8129521B2 (en) 2012-03-06
CA2936497C (en) 2018-04-17
AU2006338175B2 (en) 2013-10-03
KR20160003333A (ko) 2016-01-08
KR101773527B1 (ko) 2017-08-31
IL191693A0 (en) 2009-02-11
KR101840627B1 (ko) 2018-03-21
ES2642054T3 (es) 2017-11-15
EP1973919A2 (en) 2008-10-01
EP2862863A1 (en) 2015-04-22
EP1973919A4 (en) 2010-11-10
KR20170101323A (ko) 2017-09-05
KR20150056880A (ko) 2015-05-27
EP3287464A1 (en) 2018-02-28
CA2936497A1 (en) 2007-08-23
CN102746321B (zh) 2017-07-21
IL191693A (en) 2012-04-30
CA2997700A1 (en) 2007-08-23
KR101358695B1 (ko) 2014-02-07
KR20150002862A (ko) 2015-01-07
TWI386413B (zh) 2013-02-21
EP1973919B1 (en) 2014-09-03
US20080167335A1 (en) 2008-07-10
CA2631971A1 (en) 2007-08-23
AU2006338175A2 (en) 2009-03-12
CN101331138A (zh) 2008-12-24

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