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SE8504619D0 - carbacyclin analogues - Google Patents

carbacyclin analogues

Info

Publication number
SE8504619D0
SE8504619D0 SE8504619A SE8504619A SE8504619D0 SE 8504619 D0 SE8504619 D0 SE 8504619D0 SE 8504619 A SE8504619 A SE 8504619A SE 8504619 A SE8504619 A SE 8504619A SE 8504619 D0 SE8504619 D0 SE 8504619D0
Authority
SE
Sweden
Prior art keywords
alkyl
substd
opt
beta
alpha
Prior art date
Application number
SE8504619A
Other languages
Swedish (sv)
Other versions
SE8504619L (en
Inventor
P A Aristoff
R C Kelly
N A Nelson
Original Assignee
Upjohn Co
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
Priority claimed from US06/125,608 external-priority patent/US4338457A/en
Application filed by Upjohn Co filed Critical Upjohn Co
Publication of SE8504619D0 publication Critical patent/SE8504619D0/en
Publication of SE8504619L publication Critical patent/SE8504619L/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no 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
    • C07D309/10—Oxygen atoms
    • C07D309/12—Oxygen atoms only hydrogen atoms and one oxygen atom directly attached to ring carbon atoms, e.g. tetrahydropyranyl ethers
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C405/00—Compounds containing a five-membered ring having two side-chains in ortho position to each other, and having oxygen atoms directly attached to the ring in ortho position to one of the side-chains, one side-chain containing, not directly attached to the ring, a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, and the other side-chain having oxygen atoms attached in gamma-position to the ring, e.g. prostaglandins ; Analogues or derivatives thereof
    • C07C405/005—Analogues or derivatives having the five membered ring replaced by other rings
    • C07C405/0075—Analogues or derivatives having the five membered ring replaced by other rings having the side-chains or their analogues or derivatives attached to a condensed ring system
    • C07C405/0083—Analogues or derivatives having the five membered ring replaced by other rings having the side-chains or their analogues or derivatives attached to a condensed ring system which is only ortho or peri condensed, e.g. carbacyclins
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyrane Compounds (AREA)
  • Indole Compounds (AREA)

Abstract

(A) Carbacycline derivs. of formulae (X) and (X1) are new. n is 1 or 2. L1 is alpha-R3, beta-R4; beta-R3 or a mixt. of both; R3 and R4 being each H, methyl or fluoro, M1 is alpha-hydroxy, beta-R5 or alpha-R5, beta-hydroxy; R5 being H or methyl. R7 is CmH2m. CH3 (m is 1-5); phenoxy opt. substd. by 1-3 of chloro, fluoro, trifluoromethyl, 1-3C alkyl or alkoxy phenyl, benzyl, phenethyl or phenylpropyl, all opt. ring-substd. as phenoxy; cis-CH=CH.CH2.CH3; (CH2)2. CH(OH).CH3 or (CH2)3.CH=C(CH3)2. R8 is H, hydroxymethyl or hydroxy. R15 is H or fluoro R16 is hydrogen or together with R17 is methylene. R17 is H or 1-4C alkyl. R20, R21, R22, R23 or R4 can all be H (2 R22 alpha or beta); or R20 is H, R21 and R33 form a second C-C bond, and R23 and R24 form a second bond or are both H; or R22, R23 and R24 are all H (R22 alpha or beta) and R21 and R20 are together oxo, or R20 is H and R21 alpha or beta hydroxy. X1 is COOR1, hydroxymethyl, COL4, or CH2NL2L3 or R1 is a cation. L4 is NR51R52; pyrrolidino, piperidino, morpholino, piperazino, hexamethyl eneimino, pyrrolino or 3,4-didehhydropiperidinyl (opt. substd). N(R53).COR51 or N(R53).SO2.R51 R51 and R52 are H, 1-12C alkyl, 3-10C cycloalkyl, 7-12C aralkyl, phenyl (opt. substd. by 1-3 chloro, 1-3C alkyl, hydroxy, carboxy, 2-5C alkoxycarbonyl or nitro), 2-5C (carboxy-, carbamoyl- or cyano) alkyl, 3-6C acetyl alkyl, 7-11C benzo(sic)alkyl (opt.substd) pyridyl (opt. substd). 6-9C pyridylalkyl (opt. substd.) or is 1-4C mono- di- or tri-hydroxyalkyl; at most one of R51 and R52 is H or alkyl. R53 is H or 1-4C alkyl, and is N(R3). COR51, R51 cannot be H. L2 and L3 are H or 1-4C alkyl. Y is cis or trans vinylene, ethylene or CC Z1 is CH2.(CH2)f. C(R2)2; trans-CH2. CH=CH, or -Ph-(CH2)g R2 is H or fluoro f is 0-3, Ph is 1,2-,1,3- or 1,4-phenylene. g is 0-3. (X) and (X1) are useful in human and veterinary medicine as antithromotics, antiulcer agents (reducing acid secretion and counteracting effects of non-steroidal antiinflam
SE8504619A 1980-02-28 1985-10-04 carbacyclin analogues SE8504619L (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US06/125,608 US4338457A (en) 1980-02-28 1980-02-28 Composition and process
US13505580A 1980-03-28 1980-03-28
US14054680A 1980-04-15 1980-04-15
US14295380A 1980-04-23 1980-04-23

Publications (2)

Publication Number Publication Date
SE8504619D0 true SE8504619D0 (en) 1985-10-04
SE8504619L SE8504619L (en) 1985-10-04

Family

ID=27494588

Family Applications (6)

Application Number Title Priority Date Filing Date
SE8100564A SE453594B (en) 1980-02-28 1981-01-28 carbacyclin analogues
SE8504615A SE8504615L (en) 1980-02-28 1985-10-04 carbacyclin analogues
SE8504618A SE8504618L (en) 1980-02-28 1985-10-04 carbacyclin analogues
SE8504617A SE8504617D0 (en) 1980-02-28 1985-10-04 carbacyclin analogues
SE8504619A SE8504619L (en) 1980-02-28 1985-10-04 carbacyclin analogues
SE8504616A SE8504616D0 (en) 1980-02-28 1985-10-04 carbacyclin analogues

Family Applications Before (4)

Application Number Title Priority Date Filing Date
SE8100564A SE453594B (en) 1980-02-28 1981-01-28 carbacyclin analogues
SE8504615A SE8504615L (en) 1980-02-28 1985-10-04 carbacyclin analogues
SE8504618A SE8504618L (en) 1980-02-28 1985-10-04 carbacyclin analogues
SE8504617A SE8504617D0 (en) 1980-02-28 1985-10-04 carbacyclin analogues

Family Applications After (1)

Application Number Title Priority Date Filing Date
SE8504616A SE8504616D0 (en) 1980-02-28 1985-10-04 carbacyclin analogues

Country Status (12)

Country Link
JP (2) JPH02167248A (en)
AU (2) AU542861B2 (en)
CA (1) CA1201712A (en)
CH (2) CH648017A5 (en)
DE (4) DE3105588A1 (en)
FR (1) FR2484413B1 (en)
GB (1) GB2070596B (en)
HK (1) HK6989A (en)
IL (1) IL61936A (en)
IT (1) IT1144901B (en)
NL (1) NL8100959A (en)
SE (6) SE453594B (en)

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3237200A1 (en) * 1982-10-05 1984-04-05 Schering AG, 1000 Berlin und 4709 Bergkamen 5-FLUORCARBACYCLINE, METHOD FOR THE PRODUCTION THEREOF AND THEIR USE AS MEDICINAL PRODUCTS
CA1201712A (en) * 1980-02-28 1986-03-11 Paul A. Aristoff Carbacyclin analogs
DE3048906A1 (en) * 1980-12-19 1982-07-15 Schering Ag, 1000 Berlin Und 4619 Bergkamen NEW CARBACYCLINE, METHOD FOR THE PRODUCTION THEREOF AND THEIR USE AS MEDICINAL PRODUCTS
DE3142733A1 (en) * 1981-10-23 1983-05-05 Schering Ag, 1000 Berlin Und 4619 Bergkamen METHOD FOR PRODUCING CARBACYCLIN INTERMEDIATE PRODUCTS
DE3146278C2 (en) * 1981-11-21 1984-10-31 Grünenthal GmbH, 5190 Stolberg cis-bicyclo [3.3.0] octane derivatives, medicaments containing them and processes for the preparation of these compounds
IL67332A (en) * 1981-12-01 1985-12-31 Chinoin Gyogyszer Es Vegyeszet Inter-m-phenylene-prostacyclin analogues,process for the preparation thereof and pharmaceutical compositions containing them
DE3204443A1 (en) * 1982-02-08 1983-08-18 Schering Ag, 1000 Berlin Und 4619 Bergkamen NEW CARBACYCLINE, METHOD FOR THE PRODUCTION THEREOF AND THEIR USE AS MEDICINAL PRODUCTS
US4533749A (en) * 1982-02-16 1985-08-06 The Upjohn Company 9-Substituted carbacyclin analogs
US4487961A (en) * 1982-02-16 1984-12-11 The Upjohn Company 9-Substituted carbacyclin analogs
US4486598A (en) * 1982-02-22 1984-12-04 The Upjohn Company Carbacyclin analogs
US4490555A (en) * 1982-03-19 1984-12-25 The Upjohn Company 9-Substituted carbacyclin analogs
US4487960A (en) * 1982-04-19 1984-12-11 The Upjohn Company 9-Substituted carbacyclin analogs
HU190007B (en) * 1982-05-06 1986-08-28 Chinoin Gyogyszer Es Vegyeszeti Termekek Gyara Rt,Hu Process for producing new aromatic prostacylin analogues
DE3225287A1 (en) * 1982-07-02 1984-01-05 Schering AG, 1000 Berlin und 4709 Bergkamen NEW CARBACYCLINAMIDES, METHOD FOR THE PRODUCTION THEREOF AND THEIR USE AS MEDICINAL PRODUCTS
DE3225288A1 (en) * 1982-07-02 1984-01-19 Schering AG, 1000 Berlin und 4709 Bergkamen NEW CARBACYCLINE, METHOD FOR THE PRODUCTION THEREOF AND THEIR USE AS MEDICINAL PRODUCTS
US4668814A (en) * 1984-03-08 1987-05-26 The Upjohn Company Interphenylene carbacyclin derivatives
US4683330A (en) * 1984-03-08 1987-07-28 The Upjohn Company Interphenylene carbacyclin derivatives
DE3408699A1 (en) * 1984-03-08 1985-09-12 Schering AG, 1000 Berlin und 4709 Bergkamen NEW CARBACYCLINE, METHOD FOR THE PRODUCTION THEREOF AND THEIR USE AS MEDICINAL PRODUCTS
DE3568977D1 (en) * 1984-07-18 1989-04-27 Upjohn Co An interphenylene-carbacyclin compound
DE3428266A1 (en) * 1984-07-27 1986-01-30 Schering AG, 1000 Berlin und 4709 Bergkamen NEW CARBACYCLINE, METHOD FOR THE PRODUCTION THEREOF AND THEIR USE AS MEDICINAL PRODUCTS
DE19722849A1 (en) * 1997-05-23 1998-11-26 Schering Ag Leukotriene B¶4¶ antagonists, especially 3-oxa-tetra-hydronaphthalene LTB¶4¶ antagonists
US6700025B2 (en) * 2001-01-05 2004-03-02 United Therapeutics Corporation Process for stereoselective synthesis of prostacyclin derivatives
CN101265226B (en) 2003-05-22 2013-04-24 联合治疗公司 Compounds and methods for delivery of prostacyclin analogs
US20090124697A1 (en) 2003-12-16 2009-05-14 United Therapeutics Corporation Inhalation formulations of treprostinil
KR101161889B1 (en) * 2003-12-16 2012-07-02 유나이티드 쎄러퓨틱스 코포레이션 Use of treprostinil to treat and prevent ischemic lesions
CA2710725C (en) 2010-07-22 2017-08-01 Alphora Research Inc. Protected aldehydes for use as intermediates in chemical syntheses, and processes for their preparation
CA2726599C (en) 2010-12-30 2017-07-25 Alphora Research Inc. Process for treprostinil salt preparation
CA3212313A1 (en) 2013-03-14 2014-10-02 United Therapeutics Corporation Solid forms of treprostinil
KR101830693B1 (en) * 2016-04-28 2018-02-21 연성정밀화학(주) Process for Preparing Treprostinil and Intermediate Therefor
HU231212B1 (en) 2018-04-16 2021-11-29 CHINOIN Gyógyszer és Vegyészeti Termékek Gyára Zrt. Process for production of iloprost

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5495552A (en) * 1978-01-06 1979-07-28 Sankyo Co Ltd Prostacyline derivative and its preparation
JPS54119441A (en) * 1978-03-09 1979-09-17 Sumitomo Chem Co Ltd Novel bicyclooctane derivative
GB2017699B (en) * 1978-03-31 1983-01-12 Ono Pharmaceutical Co 6,9-methano-pgi2 analogues
US4180657A (en) * 1978-08-14 1979-12-25 The Upjohn Company Acyl-substituted phenyl esters of prostacyclin-type compounds
US4192891A (en) * 1979-04-25 1980-03-11 E. R. Squibb & Sons, Inc. Prostacyclin analogs and their use in inhibition of arachidonic acid-induced platelet aggregation and bronchoconstriction
CA1201712A (en) * 1980-02-28 1986-03-11 Paul A. Aristoff Carbacyclin analogs
US4338457A (en) * 1980-02-28 1982-07-06 The Upjohn Company Composition and process
DE3121155A1 (en) * 1981-05-22 1982-12-09 Schering Ag, 1000 Berlin Und 4619 Bergkamen NEW CARBACYCLINE, METHOD FOR THE PRODUCTION THEREOF AND THEIR USE AS MEDICINAL PRODUCTS

Also Published As

Publication number Publication date
SE8504617L (en) 1985-10-04
DE3153460C2 (en) 1990-08-16
DE3153474C2 (en) 1990-05-31
SE8100564L (en) 1981-08-29
JPH048427B2 (en) 1992-02-17
AU542861B2 (en) 1985-03-21
CH648017A5 (en) 1985-02-28
AU567392B2 (en) 1987-11-19
CA1201712A (en) 1986-03-11
AU3820885A (en) 1985-06-20
SE8504616L (en) 1985-10-04
IL61936A0 (en) 1981-02-27
DE3105588A1 (en) 1981-12-10
HK6989A (en) 1989-01-27
NL8100959A (en) 1981-10-01
GB2070596B (en) 1984-02-08
SE8504618D0 (en) 1985-10-04
SE453594B (en) 1988-02-15
GB2070596A (en) 1981-09-09
SE8504619L (en) 1985-10-04
SE8504616D0 (en) 1985-10-04
JPH02167248A (en) 1990-06-27
CH655308A5 (en) 1986-04-15
JPH06145085A (en) 1994-05-24
SE8504615D0 (en) 1985-10-04
SE8504618L (en) 1985-10-04
IT8120019A0 (en) 1981-02-26
SE8504617D0 (en) 1985-10-04
FR2484413A1 (en) 1981-12-18
SE8504615L (en) 1985-10-04
AU6660681A (en) 1981-09-03
DE3153460A1 (en) 1988-08-11
IT1144901B (en) 1986-10-29
DE3105588C2 (en) 1989-04-13
DE3153390C2 (en) 1989-09-14
IL61936A (en) 1986-08-31
FR2484413B1 (en) 1986-05-23

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