HRP20100035T1 - Kristalni oblici bifenilnog spoja - Google Patents

Kristalni oblici bifenilnog spoja Download PDF

Info

Publication number
HRP20100035T1
HRP20100035T1 HR20100035T HRP20100035T HRP20100035T1 HR P20100035 T1 HRP20100035 T1 HR P20100035T1 HR 20100035 T HR20100035 T HR 20100035T HR P20100035 T HRP20100035 T HR P20100035T HR P20100035 T1 HRP20100035 T1 HR P20100035T1
Authority
HR
Croatia
Prior art keywords
ester
ethyl
compound according
biphenyl
carbamoylpiperidin
Prior art date
Application number
HR20100035T
Other languages
English (en)
Inventor
Axt Sabine
J. Church Timothy
Malathong Viengkham
Original Assignee
Theravance
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=36540140&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20100035(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Theravance filed Critical Theravance
Publication of HRP20100035T1 publication Critical patent/HRP20100035T1/hr

Links

Classifications

    • 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
    • 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
    • A61K31/13—Amines
    • 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
    • A61K31/45—Non condensed piperidines, e.g. piperocaine having oxo groups directly attached to the heterocyclic ring, e.g. cycloheximide
    • 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
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/42—Phosphorus; Compounds thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/007—Pulmonary tract; Aromatherapy
    • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
    • A61M15/00—Inhalators
    • 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
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • 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
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D211/40—Oxygen atoms
    • C07D211/44—Oxygen atoms attached in position 4
    • C07D211/46—Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
    • A61M2202/00—Special media to be introduced, removed or treated
    • A61M2202/06—Solids
    • A61M2202/064—Powder
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Otolaryngology (AREA)
  • Biomedical Technology (AREA)
  • Anesthesiology (AREA)
  • Hematology (AREA)
  • Inorganic Chemistry (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Kristalna farmaceutski prihvatljiva sol ili slobodna baza bifenil-2-ilkabamiska kiselina 1-(2-{[4-(4-karbamoilpiperidin-1-ilmetil)benzoil]metilamino}ethyl)piperidin-4-il estera, koji ima formulu I: ili njihov farmaceutski prihvatljiv solvat. Patent sadrži još 29 patentnih zahtjeva.

Claims (30)

1. Kristalna farmaceutski prihvatljiva sol ili slobodna baza bifenil-2-ilkabamiska kiselina 1-(2-{[4-(4-karbamoilpiperidin-1-ilmetil)benzoil]metilamino}ethyl)piperidin-4-il estera, koji ima formulu I: [image] ili njihov farmaceutski prihvatljiv solvat.
2. Spoj prema zahtjevu 1, gdje je kristalna sol ili slobodna baza formule I difosfatna sol koja je karakterizirana barem jednim od (i) uzorkom rendgenske difrakcije na prahu koji ima dva ili više difrakcijskih vrhova na 20 vrijednosti odabranih od 6.4+0.2, 7.6+0.2, 8.6+0.2, 13.7+0.2, 15.0+0.2, 19.4+0.2, 21.6+0.2, 22.1+0.2, 22.9+0.2, i 23.7+0.2; i (ii) tragom diferencijalne skenirajuće kalorimetrije koji pokazuje maksimalni endotermički protok topline od oko 154.5 °C.
3. Spoj prema zahtjevu 1, gdje je kristalna sol ili slobodna baza formule I monosulfatna sol koja je karakterizirana barem jednim od (i) uzorkom rendgenske difrakcije na prahu koji ima dva ili više difrakcijskih vrhova na 20 vrijednosti odabranih od 7.7+0.2, 8.4+0.2, 8.8+0.2, 12.6+0.2, 13.7+0.2, 14.1+0.2, 15.3+0.2, 16.0+0.2, 19.7+0.2, 20.6+0.2, 23.0+0.2, i 24.4+0.2; i (ii) tragom diferencijalne skenirajuće kalorimetrije koji pokazuje maksimalni endotermički protok topline od oko 76.5 °C.
4. Spoj prema zahtjevu 1, gdje je kristalna sol ili slobodna baza formule I dioksalatna sol koja je karakterizirana barem jednim od (i) uzorkom rendgenske difrakcije na prahu koji ima dva ili više difrakcijskih vrhova na 20 vrijednosti odabranih od 7.7+0.2, 8.7+0.2, 13.5+0.2. 14.0+0.2, 14.8+0.2, 15.4+0.2, 15.8+0.2, 19.4+0.2, 22.9+0.2, 23.3+0.2, i 24.6+0.2; i (ii) tragom diferencijalne skenirajuće kalorimetrije koji pokazuje maksimalni endotermički protok topline od oko 73.7 °C.
5. Spoj prema zahtjevu 1, gdje je kristalna sol ili slobodna baza formule I slobodna baza koja je karakterizirana barem jednim od (i) uzorkom rendgenske difrakcije na prahu koji ima dva ili više difrakcijskih vrhova na 20 vrijednosti odabranih od 4.7+0.2, 9.6+0.2, 12.7+0.2, 13.7+0.2, 16.7+0.2, 17.4+0.2, 18.5+0.2, 19.4+0.2, 20.8+0.2, 21.4+0.2, 24.2+0.2, i 25.6+0.2; i (ii) tragom diferencijalne skenirajuće kalorimetrije koji pokazuje maksimalni endotermički protok topline od oko 102.7 °C.
6. Spoj prema zahtjevu 1, gdje je kristalna sol ili slobodna baza formule I slobodna baza, koja je karakterizirana barem jednim od (i) uzorkom rendgenske difrakcije na prahu koji ima dva ili više difrakcijskih vrhova na 20 vrijednosti odabranih od 4.6+0.2, 9.3+0.2, 12.9+0.2, 13.6+0.2, 14.0+0.2, 14.6+0.2, 16.5+0.2, 18.64+0.2, 19.1+0.2, 20.9+0.2, 22.1+0.2, 22.7+0.2, i 25.7+0.2 i (ii) tragom diferencijalne skenirajuće kalorimetrije koji pokazuje maksimalni endotermički protok topline od oko 98.6 °C .
7. Farmaceutski sastav koji sadrži farmaceutski prihvatljivi nosač i spoj prema bilo kojem zahtjevu od 1 do 6.
8. Sastav prema zahtjevu 7, koji nadalje sadrži terapeutski učinkovitu količinu agensa odabranog od agonista beta2-adrenergičkih receptora, steroidnih protuupalnih agensa, inhibitora fosfodiesteraze-4, i njihovih kombinacija; gdje su spoj i agens formulirani zajedno ili odvojeno.
9. Sastav prema zahtjevu 8, koji sadrži terapeutski učinkovitu količinu agonista beta2-adrenergičkih receptora i steroidnog protuupalnog agensa.
10. Sastav prema zahtjevu 8, gdje je agonist beta2-adrenergičkih receptora monohidrokloridna sol N-{2-[4-((R)-2-hidroksi-2-feniletilamino)fenil]etil}-(R)-2-hidroksi-2-(3-formamido-4-hidroksifenil)etilamina.
11. Sastav prema zahtjevu 8, gdje je steroidni protuupalni agens 6α,9α-difluoro-17α-[(2-furanilkarbonil)oksi]-11β-hidroksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karbotionska kiselina S’-fluorometil ester.
12. Sastav prema zahtjevu 7, naznačen time da je sastav formuliran za primjenu putem inhalacije.
13. Sastav prema zahtjevu 7, naznačen time da je nosač vodena izotonična slana otopina koja ima pH u rasponu od oko 4 do oko 6.
14. Sastav prema zahtjevu 13, koji sadrži citratni pufer.
15. Uređaj za davanje lijeka koji sadrži inalator sa suhim prahom koji sadrži sastav prema zahtjevu 7.
16. Kristalni oblik spoja prema bilo kojem zahtjevu od 1 do 6, u mikroniziranom obliku.
17. Farmaceutski sastav koji sadrži farmaceutski prihvatljiv nosač i spoj prema zahtjevu 16.
18. Sastav prema zahtjevu 17, naznačen time da je nosač laktoza.
19. Postupak priprave spoja prema zahtjevu 2, koji sadrži dovođenje u vezu bifenil-2-ilkarbaminska kiselina 1-(2-{[4-(4-karbamoilpiperidin-1-ilmeti])benzoil] metilamino}etil)piperidin-4-il estera s fosfornom kiselinom.
20. Postupak priprave spoja prema zahtjevu 3, koji sadrži dovođenje u vezu bifenil-2-ilkarbaminska kiselina 1-(2-{[4-(4-karbamoilpiperidin-1-ilmetil)benzoil]metilamino}etil)piperidin-i4-il estera sa sumpornom kiselinom.
21. Postupak priprave spoja prema zahtjevu 4, koji sadrži: formiranje jezgri kristalizacije kristalne dioksalatne soli bifenil-2-ilkarbaminska kiselina 1-(2-{[4-(4-karbamoilpiperidin-1-ilmetil)benzoil]metilamino}etil)piperidin-4-il estera dovođenjem u vezu bifenil-2-ilkarbaminska kiselina 1-(2-{[4-(4-karbamoilpiperidin-1-ilmetil)benzoil]metilamino}etil)piperidin-4-il estera s oksalnom kiselinom; formiranje dioksalatne soli bifenil-2-ilkarbaminska kiselina 1-(2-{[4-(4-karbamoilpiperidin-1-ilmetil)benzoil]metilamino}etil)piperidin-4-il estera dovođenjem u vezu bifenil-2-ilkarbaminska kiselina 1-(2-{[4-(4-karbamoilpiperidin-1-ilmetil)benzoil]metilamino}etil)piperidin-4-il estera s oksalnom kiselinom, i otapanjem soli u inertnom razrjeđivaču kako bi se formirala otopina, i dodavanje jezgre kristalizacije u otopinu.
22. Postupak priprave spoja prema zahtjevima 5 ili 6, koji sadrži: formiranje jezgri kristalizacije kristalne slobodne baze dovođenjem u vezu bifenil-2-ilkarbaminska kiselina 1-(2-{[4-(4-karbamoilpiperidin-1-ilmetil)benzoil]metilamino}etil)piperidin-4-il estera s inertnim razrjeđivačem; formiranje slobodne baze dovođenjem u vezu bifenil-2-ilkarbaminska kiselina 1-(2-{[4-(4-karbamoilpiperidin-1-ilmetil)benzoil]metilamino}etil)piperidin-4-il estera s inertnim razrjeđivačem, i otapanjem rezultirajućeg kristalnog estera kako bi se dobila otopina; i dodavanje jezgre kristalizacije u otopinu.
23. Upotreba spoja prema bilo kojem zahtjevu od 1 do 6 u postupku pročišćavanja bifenil-2-ilkarbaminska kiselina 1-(2-{[4-(4-karbamoilpiperidin-1-ilmetil)benzoil]metilamino}etil)piperidin-4-il estera, koja sadrži formiranje kristalne soli ili kristalne slobodne baze bifenil-2-ilkarbaminska kiselina 1-(2-{[4-(4-karbamoilpiperidin-1-ilmetil)benzoil]metilamino}etil)piperidin-4-il estera.
24. Spoj prema bilo kojem zahtjevu od 1 do 6, naznačen time da je za upotrebu u liječenju ili kao lijek.
25. Upotreba spoja prema bilo kojem zahtjevu od 1 do 6, naznačena time da je za proizvodnju lijeka.
26. Upotreba prema zahtjevu 25, naznačena time da je lijek za liječenje plućnog poremećaja.
27. Upotreba prema zahtjevu 25, naznačena time da je lijek za izazivanje bronhodilacije.
28. Upotreba prema zahtjevu 25, naznačena time da je lijek za liječenje kronične opstruktivne bolesti pluća ili astme.
29. Difosfatna, monosulfatna ili diokslatna sol bifenil-2-ilkarbaminska kiselina 1-(2-{[4-(4-karbamoilpiperidin-1-ilmetil)benzoil]metilamino}etil)piperidin-4-il estera.
30. Spoj prema zahtjevu 29, koji je difosfatna sol bifenil-2-ilkarbaminska kiselina 1-(2-{[4-(4-karbamoilpiperidin-1-ilmetil)benzoil]metilamino}etil)piperidin-4-il estera.
HR20100035T 2005-03-10 2010-01-20 Kristalni oblici bifenilnog spoja HRP20100035T1 (hr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US66020805P 2005-03-10 2005-03-10
PCT/US2006/008644 WO2006099165A1 (en) 2005-03-10 2006-03-09 Crystalline forms of a biphenyl compound

Publications (1)

Publication Number Publication Date
HRP20100035T1 true HRP20100035T1 (hr) 2010-02-28

Family

ID=36540140

Family Applications (1)

Application Number Title Priority Date Filing Date
HR20100035T HRP20100035T1 (hr) 2005-03-10 2010-01-20 Kristalni oblici bifenilnog spoja

Country Status (24)

Country Link
US (12) US20070112027A1 (hr)
EP (1) EP1856050B1 (hr)
JP (2) JP5009894B2 (hr)
KR (1) KR101270183B1 (hr)
CN (1) CN101163677B (hr)
AR (2) AR053336A1 (hr)
AT (1) ATE449762T1 (hr)
AU (1) AU2006223325B2 (hr)
CA (1) CA2599236C (hr)
CY (1) CY1109775T1 (hr)
DE (1) DE602006010668D1 (hr)
DK (1) DK1856050T3 (hr)
ES (1) ES2337604T3 (hr)
HK (1) HK1114608A1 (hr)
HR (1) HRP20100035T1 (hr)
IL (1) IL185471A (hr)
MX (1) MX2007011083A (hr)
MY (1) MY147792A (hr)
PE (1) PE20061347A1 (hr)
PL (1) PL1856050T3 (hr)
PT (1) PT1856050E (hr)
SI (1) SI1856050T1 (hr)
TW (1) TWI372749B (hr)
WO (1) WO2006099165A1 (hr)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI341836B (en) * 2004-03-11 2011-05-11 Theravance Inc Biphenyl compounds useful as muscarinic receptor antagonists
US7416328B2 (en) * 2004-12-28 2008-08-26 Waters Investments Limited System and method for a thermogravimetric analyzer having improved dynamic weight baseline
TWI372749B (en) 2005-03-10 2012-09-21 Theravance Inc Crystalline forms of a biphenyl compound
US7973055B2 (en) 2006-03-09 2011-07-05 Theravance, Inc. Crystalline forms of a biphenyl compound
EP2230934B8 (en) 2007-12-14 2012-10-24 AeroDesigns, Inc Delivering aerosolizable food products
EP2103939A1 (en) * 2008-03-20 2009-09-23 sanofi-aventis Fluorescence based assay to detect sodium/calcium exchanger (NCX) "reverse mode" modulating compounds
EP2103944A1 (en) * 2008-03-20 2009-09-23 sanofi-aventis Fluorescence based assay to detect sodium/calcium exchanger "forward mode" modulating compounds
US8030957B2 (en) 2009-03-25 2011-10-04 Aehr Test Systems System for testing an integrated circuit of a device and its method of use
CA2765621C (en) 2009-07-15 2018-02-13 Theravance, Inc. Crystalline freebase forms of a biphenyl compound
WO2011083387A1 (en) * 2010-01-07 2011-07-14 Pfizer Limited Hydrochloride salt of biphenyl-2-yl-carbamic acid 1-{9-[(3-fluoro-4-hydroxy-benzoyl)-methyl-amino]-nonyl}-piperidin-4-yl ester
SG186708A1 (en) * 2010-07-13 2013-02-28 Theravance Inc Process for preparing a biphenyl-2-ylcarbamic acid
US8900635B2 (en) 2010-11-15 2014-12-02 Humanetics Corporation Nanoparticle isoflavone compositions and methods of making and using the same
US9084726B2 (en) 2013-11-26 2015-07-21 Humanetics Corporation Suspension compositions of physiologically active phenolic compounds and methods of making and using the same
WO2017054702A1 (zh) * 2015-09-28 2017-04-06 四川海思科制药有限公司 一种联苯衍生物及其制备方法和在医药上的用途
CN112694434B (zh) * 2020-12-29 2023-06-16 浙江和泽医药科技股份有限公司 一种雷芬那辛新中间体及其活性亲电砌块和雷芬那辛的新制备方法
WO2023002502A1 (en) * 2021-07-17 2023-01-26 Msn Laboratories Private Ltd, R&D Center Novel process for the preparation of 1-(2-{4-[(4-carbamoylpiperidin-1-yl)methyl]- n-methylbenzamido}ethyl)piperidin-4-yl n-({1,1'-biphenyl}-2-yl)carbamate
WO2023104920A1 (en) 2021-12-09 2023-06-15 Medichem, S.A. Crystalline acetone solvate of revefenacin
CN114276290B (zh) * 2021-12-24 2024-05-28 浙江和泽医药科技股份有限公司 一种雷芬那辛无水晶型及其制备方法
CN117180235A (zh) * 2023-09-19 2023-12-08 山东京卫制药有限公司 一种无定型雷芬那辛吸入制剂
CN117263848A (zh) * 2023-09-19 2023-12-22 山东京卫制药有限公司 一种雷芬那辛的吸入喷雾剂
CN117263849A (zh) * 2023-09-19 2023-12-22 山东京卫制药有限公司 一种雷芬那辛三水合物晶型及其制备方法

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2425983C3 (de) * 1973-06-12 1978-09-14 Toyama Chemical Co. Ltd., Tokio Sulfonsäuresalze von Acylcholinen, Verfahren zu ihrer Herstellung und diese enthaltende pharmazeutische Zusammensetzung
EP0747355A4 (en) 1994-02-10 1997-04-09 Yamanouchi Pharma Co Ltd NEW CARBAMATES AND MEDICINAL PRODUCTS CONTAINING THEM
HU221033B1 (hu) * 1996-02-21 2002-07-29 Schering Corp. Poradagoló készülék
US6006747A (en) * 1997-03-20 1999-12-28 Dura Pharmaceuticals, Inc. Dry powder inhaler
US6693202B1 (en) * 1999-02-16 2004-02-17 Theravance, Inc. Muscarinic receptor antagonists
UA73543C2 (uk) * 1999-12-07 2005-08-15 Тераванс, Інк. Похідні сечовини, фармацевтична композиція та застосування похідного при приготуванні лікарського засобу для лікування захворювання, яке опосередковується мускариновим рецептором
WO2001042212A1 (en) * 1999-12-07 2001-06-14 Theravance, Inc. Carbamate derivatives having muscarinic receptor antagonist activity
US20030018019A1 (en) * 2001-06-23 2003-01-23 Boehringer Ingelheim Pharma Kg Pharmaceutical compositions based on anticholinergics, corticosteroids and betamimetics
US20050113113A1 (en) * 2001-11-15 2005-05-26 Reed Mark J. Enhanced wireless phone
TW200526547A (en) * 2003-09-22 2005-08-16 Theravance Inc Amino-substituted ethylamino β2 adrenergic receptor agonists
PE20050973A1 (es) * 2003-10-29 2005-11-19 Theravance Inc Sales de acido naftalen-1,5-disulfonico de un compuesto de 4-amino-1-(piridilmetil)piperidina como antagonistas de receptores muscarinicos
TWI341836B (en) * 2004-03-11 2011-05-11 Theravance Inc Biphenyl compounds useful as muscarinic receptor antagonists
TW200540154A (en) * 2004-06-10 2005-12-16 Theravance Inc Crystalline form of a substituted pyrrolidine compound
TWI372749B (en) 2005-03-10 2012-09-21 Theravance Inc Crystalline forms of a biphenyl compound
US20060205949A1 (en) * 2005-03-10 2006-09-14 Theravance, Inc. Crystalline forms of a biphenyl compound
US8037880B2 (en) * 2006-04-07 2011-10-18 The University Of Western Ontario Dry powder inhaler
US8377956B2 (en) * 2010-03-01 2013-02-19 Xenoport, Inc. Use of (3R)-4-{[(1S)-2-methyl-1-(2-methylpropanoyloxy)propoxy]carbonylamino}-3-(4-chlorophenyl) butanoic acid for treating urinary incontinence

Also Published As

Publication number Publication date
US10577347B2 (en) 2020-03-03
US20200317641A1 (en) 2020-10-08
AR053336A1 (es) 2007-05-02
US20070112027A1 (en) 2007-05-17
PT1856050E (pt) 2010-02-17
US20100048622A1 (en) 2010-02-25
EP1856050A1 (en) 2007-11-21
US20100021395A1 (en) 2010-01-28
US8716313B2 (en) 2014-05-06
MX2007011083A (es) 2008-02-19
BRPI0608446A2 (pt) 2009-12-29
ES2337604T3 (es) 2010-04-27
TWI372749B (en) 2012-09-21
US20130125887A1 (en) 2013-05-23
US8921395B2 (en) 2014-12-30
CN101163677A (zh) 2008-04-16
CA2599236A1 (en) 2006-09-21
US9656993B2 (en) 2017-05-23
IL185471A (en) 2012-02-29
US11390603B2 (en) 2022-07-19
ATE449762T1 (de) 2009-12-15
WO2006099165A1 (en) 2006-09-21
JP5009894B2 (ja) 2012-08-22
KR101270183B1 (ko) 2013-05-31
JP2012107066A (ja) 2012-06-07
PE20061347A1 (es) 2007-02-03
US20150152054A1 (en) 2015-06-04
US20140288033A1 (en) 2014-09-25
US7700777B2 (en) 2010-04-20
IL185471A0 (en) 2008-01-06
US8242137B2 (en) 2012-08-14
AU2006223325A1 (en) 2006-09-21
US8377965B2 (en) 2013-02-19
DE602006010668D1 (de) 2010-01-07
US20180051004A1 (en) 2018-02-22
AR106744A2 (es) 2018-02-14
US20070298112A1 (en) 2007-12-27
AU2006223325B2 (en) 2011-12-22
US20220388981A1 (en) 2022-12-08
KR20070113283A (ko) 2007-11-28
CN101163677B (zh) 2012-01-04
CY1109775T1 (el) 2014-09-10
HK1114608A1 (en) 2008-11-07
PL1856050T3 (pl) 2010-05-31
MY147792A (en) 2013-01-31
TW200714586A (en) 2007-04-16
JP2008533036A (ja) 2008-08-21
US20100256185A1 (en) 2010-10-07
US9249099B2 (en) 2016-02-02
EP1856050B1 (en) 2009-11-25
CA2599236C (en) 2013-06-25
DK1856050T3 (da) 2010-02-01
SI1856050T1 (sl) 2010-04-30
US20160168120A1 (en) 2016-06-16

Similar Documents

Publication Publication Date Title
HRP20100035T1 (hr) Kristalni oblici bifenilnog spoja
ES2292988T3 (es) Derivados de nicotinamida utiles como inhibidores de pde4.
JP5611844B2 (ja) 多環芳香族ナトリウムチャネル遮断薬
JP5286251B2 (ja) インフルエンザ治療剤
HRP20130192T1 (hr) Kristalni oblik bifenilnog spoja
RU2007146669A (ru) Пролекарства антагонистов a2b рецептора аденозина
JP2009535340A5 (hr)
JP6602902B2 (ja) 脾臓チロシンキナーゼｉ（ｓｙｋ）阻害剤としての２−（２−アミノシクロヘキシル）アミノピリミジン−５−カルボキサミド類
CN101379057B (zh) 联苯-2-基氨基甲酸1-[2-(2-氯-4-{[(r)-2-羟基-2-(8-羟基-2-氧代-1,2-二氢喹啉-5-基)乙基氨基]甲基}-5-甲氧基苯基氨甲酰基)乙基]哌啶-4-基酯的琥珀酸盐及其治疗肺疾病的用途
HRP20191257T1 (hr) Farmaceutske formulacije koje sadrže 4-{(1r)-2-[(6-{2-[(2,6-diklorbenzil)oksi]etoksi}heksil)amino]-1-hidroksietil}-2-(hidroksimetil)fenol
HRP20171614T1 (hr) Heterociklički spojevi, lijekovi koji sadrže te spojeve, njihova primjena i postupci za njihovu proizvodnju
JP2005533860A5 (hr)
HRP20151344T1 (hr) Kristalni oblik slobodne baze bifenilnog spoja
JP2007518738A5 (hr)
JP2008543860A5 (hr)
JP2008509156A5 (hr)
CN104854105A (zh) 具有毒蕈碱受体拮抗剂和β2肾上腺素能受体激动剂活性的化合物
JP2012533550A5 (hr)
JP2013538857A5 (hr)
TW200845998A (en) Heterocyclic compounds useful in treating diseases and conditions
JP2016534088A5 (hr)
TW200307545A (en) Nicotinamide derivatives and a tiotropium salt in combination for the treatment of diseases
JP2015536997A (ja) カンナビノイド受容体媒介性化合物
JP2012532191A5 (hr)
RU2014100744A (ru) Лечение респираторных нарушений с помощью trpa1 антагонистов