RS60002B1 - Inhibitori bromodomena - Google Patents

Inhibitori bromodomena

Info

Publication number
RS60002B1
RS60002B1 RS20200242A RSP20200242A RS60002B1 RS 60002 B1 RS60002 B1 RS 60002B1 RS 20200242 A RS20200242 A RS 20200242A RS P20200242 A RSP20200242 A RS P20200242A RS 60002 B1 RS60002 B1 RS 60002B1
Authority
RS
Serbia
Prior art keywords
shirt
acupuncture
magnetic
bronchitis
asthma
Prior art date
Application number
RS20200242A
Other languages
English (en)
Inventor
Michael John Bennett
Juan Manuel Betancort
Amogh Boloor
Stephen W Kaldor
Jeffrey Alan Stafford
James Marvin Veal
Original Assignee
Celgene Quanticel Research 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 Celgene Quanticel Research Inc filed Critical Celgene Quanticel Research Inc
Publication of RS60002B1 publication Critical patent/RS60002B1/sr

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    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/92—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with a hetero atom directly attached to the ring nitrogen atom
    • C07D211/94—Oxygen atom, e.g. piperidine N-oxide
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/64—One oxygen atom attached in position 2 or 6
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72—Nitrogen atoms
    • C07D213/73—Unsubstituted amino or imino radicals
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
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    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
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    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having 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
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    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
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    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
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    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/56—One oxygen atom and one sulfur atom
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    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
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    • 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
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    • 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
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    • C07D401/14—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 three or more hetero rings
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  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
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Description

BlOdAG-i^i'iVI oTIMUliAi'OK-ilAJIOA fl'AiWJiSi< OoJJ3Ai>flA bA
JiiiUNOHIi'IbOM IAbi'iMOM
U- b- uAoi' X'.^ xiiM IlVTj X' JA ilJJ UOi^ ^ JI- IaJLjA^ AA jjriUol
Pronalazak pripala©blasti medicine- f izioterapšijtskih aparata
za lskaciju ili stimulaciju refleksnih aesta na telu tj. akupunkturnih tačaka- aparat za. vršenje pritiska na povenutim isestijaa.
1'?nmCKI?KUBL??
Pronalazak rešava pr©blem da. se bi©Biagnetnim stimulatsreja naae-njenim©s©baaa sa br©nchitis©Ei i asthra©ia ostvari k©mbia©vani efekat siagnetneg p©lja i akupresure, tj. stimulacije- akupunkturnih tačaka, bez angaževanja lekara akupunkturologa, ci'ae se pevečava terapijski efekat lečenja kod©soba sa br«achitis©9 i" asthmeci.
?i'?J? T?HNIRE.
Trajni :sagneti keriste se u akupunkturi na,,taj način:- što se p©-stavljaju na akupunkturnu tačku i fiksiraju.- flasteres. Peznat©je da se k®d nas i u svetu k©riste magnetna pomagala ka©ss© sulaa-gnetns jastuče, raagnetna kolenica, magnetna nalaktica, magnetna majica,, magnetna prestirka. Magneti su pestavljeni na odredjensm
rastejanju i naizaeničnim rasp©red©m p©l©va H-S-N—S—A' taks da je
• dsbijen* prscienljive^pslje na većoj pevršini.Postavljanjem Magneta na "švaj način Ima se pezitivan uticaj magnetnog p©lja, ali ne p©-stejiedredjena ciljana stizaulacija akupunkturnih- tačaka.Ako se pestave magneti na©dredjena aesta na©devnom predmetu,tj. aajici k©ja su podudarna sa aestiina akupunkturnih tačaka na telu, debija se koiabinevani uticaj sagneta i akupunkture, Čime se povećava efikasnest lečenja u©seba sa broncmitisoa i asthiaGEi i nije neo-phodne prisustvo lekara akupunktureloga u postavljanju magneta na akupunkturnu tačku.
IZLAGANJ??iJ?jJII? F?UNAL?bKA
Pronalazak bieraagneni stiaulater -majica namenjen©s®bama sa br©nchitis@m i asthm©m predstavlja priraenu znanja iz©blasti magnet©terapije i akupunkture na p@seban edevni predaet majicu. Pri t©ae se ugradftuju stalni magneti na©dredjena aesta na ma-jici k©ja su podudarna sa mestiaia akupunkturnih tačaka na telu, tak© da magneti prilik©ra n©"enja majice vrše akupresuru t j. stimulaciju akupunkturnih tačaka. Prednosti©v@g pr©nalaska su uglavnera sadržane u činjenici da se na©vaj način k©mbinuje efekat akupresure i p©zitivan uticaj magnetnog p©lja te predstavlja udru-žen terapijski efekat. Pri tame nije petrebn©prisustv©lekara za©dredjivanje akupunkturnih tačaka, niti fiksiranje magneta flaster®® na akupunkturn©j tački. Majica se ia©že k©ristiti sa-aestaln© ili uz medikaraent©znu terapiju.
■ itARATAif OPIS^ LIKtiNACRTA
Pronalazak je detaljn®©pisan na primeru izv®djenja prikazanom
na nacrt u kerae :
Slika 1- predstavlja prikaz majice sa prednje strane
Slika 2- predstavlja prikaz majice sa zadnje strane
DETALJAN UPIS PROMALASKA
Slika prikazuje©devni prediaet - majicu u čiji je uležak uštep©van®8 stalnih magneta na mestima 1,2,3,4,5, i6. Tip magneta je 06x 4-±tsindukcije 800 Gausa(80 mT). Mest©br 1 nalazi se na prednj©j strani majice na g©rnj©j horizontalnoj liniji majice-©k©vratnika ,na mesti početka središnje vertikalne linije sajice. Mest©br 2 nalazi se na prednj©j strani,©bsstran©na b©čniia vertikalnim lini-jama raaeneg dela majice na 9-11 era ispad gernje h©riz@ntalne linije ramenog dela.Mefet©br 3 nalazi se na prednjoj strani majice na središnj©j vertikalnoj liniji na 13 - 25 era©d gornje horizontalne ivice majice. Mest©br.4 nalazi se na zadnj©j strani majice,na gernjoj h©riz©ntaln©j liniji na pečetku središnje vertikalne linije.Mest© br. 5 nalazi se na zadnjej strani,©bestran©10-12 cm isp©d gornje horizontalne linije i 2-3 cm lateraln®©d središnje vertikalne linije majice. Mest© br. 6 nalazi se na za-dnj©j strani majice, na dsnjej h©riz©ntaln©j liniji, na denjeia kraju središnje vertikalne linije, u visini pupka.Mest© 7 predstavlja središnju vertikalnu liniju.Mest©br 8 predstavlja g©rnju g®rnju horiz©ntalnu liniju majice, mest®br. 9 d@nju h@riz©ntalnu liniju na prednj©j strani majice, šest© br 10 predstavlja b©čne vertikalne linije majice, mest©11 predstavlja središnju vertikalnu liniju na zadnj©j strani majice, mest© br 12 predstavlja d©nju h©riz©ntalnu ivicu na zadnjej strani aajice.
Magneti su pestavljeni tak© da severnira pelera N, tj. zaobljenim stransasiagneta, naležu direktn© na©dredjeni de© tela tj. akupunkturnu tačku. Keriščenjem magnetn@g p©lja jedneg aagneta stiaulišu se pojedinačn©tačke u©v©s slučaju akupunkturne tačke REN 22, LI, REN 17, Tu 14, UB 13, Tu 4.
Bioaagnetni stisulat©r raajica naaenjen osebaaa sa bronchitisoa i asthmora je izradjen©d prir©dn©g materijala pasiuka. N©šenje raaji-ce ne©graničava pokrete i pruža prijatan osečaj koraetnesti, omogućava k©ži da nesmetan©diše. M@že se priaenjivati saiaostaln© ili uz taedika&enteznu terapiju. Nije neophedn©prisustvo lekara za pestavljenje akupunkturnih magneta. Nisu zabeleženi negativni efekti duže priraene stimulacije akupunkturnih tačaka trajnim magnetima. -

Claims (1)

  1. Bi©aagnetni stiaulatsr majica naaienjen©sobama sa bronchitis©®i asthmen©buhvata©davni predmet sajicu na k©joj su uštepsvani trajni akupunkturni magneti na tačkama 1,2,3,4,5,6 i k©ji na taj način vrše stimulaciju akupunkturnih tačaka, p®večavaju efikas-n@st lečenja u es©ba sa brsnchitisea i asthaom i čija primena isključuje akupunkturolega u p©stavljanju magneta, či0e se po-jednsstavljuje pestupak lečenja i eaegučava šira primena©v©g patenta.
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