HRP20171692T1 - Derivati karbamat/uree - Google Patents

Derivati karbamat/uree Download PDF

Info

Publication number
HRP20171692T1
HRP20171692T1 HRP20171692TT HRP20171692T HRP20171692T1 HR P20171692 T1 HRP20171692 T1 HR P20171692T1 HR P20171692T T HRP20171692T T HR P20171692TT HR P20171692 T HRP20171692 T HR P20171692T HR P20171692 T1 HRP20171692 T1 HR P20171692T1
Authority
HR
Croatia
Prior art keywords
compound
salt
6alkyl
piperidin
carboxylate
Prior art date
Application number
HRP20171692TT
Other languages
English (en)
Inventor
Yves Auberson
Mark Gary Bock
Dario Braga
Marco Curzi
Stephanie Kay Dodd
Stefano Luca Giaffreda
Haiyang Jiang
Piotr Karpinski
Thomas J. Troxler
Tielin Wang
Xiaoyang Wang
Xuechun Zhang
Original Assignee
Novartis Ag
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=49263333&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20171692(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of HRP20171692T1 publication Critical patent/HRP20171692T1/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
    • C07D401/04—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
    • 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
    • C07D401/14—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
    • 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
    • A61K31/33—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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P37/04—Immunostimulants
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13—Dicarboxylic acids
    • C07C57/15—Fumaric acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/235—Saturated compounds containing more than one carboxyl group
    • C07C59/245—Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
    • C07C59/265—Citric acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • 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

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Hydrogenated Pyridines (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Claims (22)

1. Spoj, naznačen time, da je to spoj formule I: [image] (I), ili njegova sol, u kojoj R1 je C1-6alkil, C2-6alkenil, C2-6alkinil, C3-6cikloalkil, C5-6cikloalkenil ili C3-6cikloalkil-C1-4alkil; gdje navedeni C1-6alkil, C2-6alkenil, C2-6alkinil ili C3-6cikloalkil-C1-4alkil, može biti supstituiran jednom ili više puta s halogenom; i gdje navedeni C3-6cikloalkil ili C5-6cikloalkenil, može biti supstituiran jednom ili više puta s halogenom, C1-4alkilom ili C1-4halogenalkilom; m je 1 ili 2; n je 0, 1, 2, 3 ili 4; svaki R2 neovisno je halogen, hidroksi, amino, cijano, nitro, C1-6alkil, C1-6halogenalkil, C1-6hidroksialkil, C1-4alkoksi-C1-6alkil, amino-C1-6alkil, C1-4alkil-amino-C1-6alkil, di(C1-4alkil)-amino-C1-6alkil, C1-6alkoksi, C1-6halogenalkoksi, C1-6alkilamino, di(C1-6alkil)amino, C2-6alkenil, C2-6halogenalkenil, C2-6alkinil ili C2-6halogenalkinil; ili C3-6cikloalkil, pri čemu jedan ugljikov atom može biti zamijenjen s kisikovim atomom, gdje C3-6cikloalkil može biti izravno priključen na metilen ili preko C1-2alkilena, i gdje C3-6cikloalkil može biti supstituiran jednom ili više puta s halogenom; ili dva R2 na istom ugljikovom atomu, zajedno s navedenim ugljikovim atomom, tvore C3-6cikloalkil; X1 je kisik ili -N(R4)-; R4 je vodik, C1-6alkil, C3-6cikloalkil ili C3-6cikloalkil-C1-2alkil; p je1 i q je 1; p je 0 i q je1; ili p je 0 i q je 0; r je 0, 1, 2, 3 ili 4; svaki R3 neovisno je halogen, hidroksi, amino, cijano, nitro, C1-6alkil, C1-6halogenalkil, C1-6hidroksialkil, C1-4alkoksi-C1-6alkil, amino-C1-6alkil, C1-4alkil-amino-C1-6alkil, di(C1-4alkil)-amino-C1-6alkil, C1-6alkoksi, C1-6halogenalkoksi, C1-6alkilamino, di(C1-6alkil)amino, C2-6alkenil, C2-6halogenalkenil, C2-6alkinil ili C2-6halogenalkinil; ili C3-6cikloalkil, pri čemu jedan ugljikov atom može biti zamijenjen s kisikovim atomom, gdje C3-6cikloalkil može biti izravno priključen na metilen ili preko C1-2alkilena, i gdje C3-6cikloalkil može biti supstituiran jednom ili više puta s halogenom; ili dva R3 na istom ugljikovom atomu, zajedno s navedenim ugljikovim atomom, tvore C3-6cikloalkil; A je [image] gdje je veza koja je označena sa zvjezdicom, priključena na dušikov atom; R5 je vodik, C1-6alkil, C2-6alkenil, C2-6alkinil, C3-6cikloalkil, C5-6cikloalkenil ili C3-6cikloalkil-C1-4alkil; gdje navedeni C1-6alkil, C2-6alkenil, C2-6alkinil ili C3-6cikloalkil-C1-4alkil, može biti supstituiran jednom ili više puta s halogenom, hidroksilom ili C1-6alkoksi; i gdje navedeni C3-6cikloalkil ili C5-6cikloalkenil, može biti supstituiran jednom ili više puta s halogenom, C1-4alkilom ili C1-4halogenalkilom; X2 je dušik ili ugljik; s je 0, 1, 2 ili 3; svaki R6 neovisno je halogen, hidroksi, amino, cijano, nitro, C1-6alkil, C1-6halogenalkil, C1-6hidroksialkil, C1-4alkoksi-C1-6alkil, amino-C1-6alkil, C1-4alkil-amino-C1-6alkil, di(C1-4alkil)-amino-C1-6alkil, C1-6alkoksi, C1-6halogenalkoksi, C1-6alkilamino, di(C1-6alkil)amino, C2-6alkenil, C2-6halogenalkenil, C2-6alkinil ili C2-6halogenalkinil; ili C3-6cikloalkil, pri čemu jedan ugljikov atom može biti zamijenjen s kisikovim atomom, gdje C3-6cikloalkil može biti izravno priključen na metilen ili preko C1-2alkilena, i gdje C3-6cikloalkil može biti supstituiran jednom ili više puta s halogenom.
2. Spoj formule I prema zahtjevu 1, naznačen time, da X1 je kisik; ili njegova sol.
3. Spoj formule I prema bilo kojem od zahtjeva 1 ili 2, naznačen time, da p je1 i q je 1; ili njegova sol.
4. Spoj formule I prema bilo kojem od zahtjeva 1 do 3, naznačen time, da R1 je izopropil, ciklopropil, ciklobutil ili ciklopentil i m je 1; ili njegova sol.
5. Spoj formule I prema bilo kojem od zahtjeva 1 do 4, naznačen time, da A je odabran od A3 i A4: [image] (A3); [image] (A4); gdje je veza koja je označena sa zvjezdicom, priključena na dušikov atom; ili njegova sol.
6. Spoj formule I prema zahtjevu 1, naznačen time, da R1 je izopropil ili ciklobutil; m je 1; n je 0, 1 ili 2; svaki R2 neovisno je halogen, C1-4alkil, C1-4halogenalkil, C1-4alkoksi, C1-4halogenalkoksi ili C3-4cikloalkil; ili dva R2 na istom ugljikovom atomu, zajedno s navedenim ugljikovim atomom, tvore C3-4cikloalkil; X1 je kisik; p je 1 i q je 1; r je 0, 1 ili 2; gdje svaki R3 neovisno je halogen, C1-4alkil, C1-4halogenalkil, C1-4alkoksi, C1-4halogenalkoksi ili C3-4cikloalkil; ili dva R3 na istom ugljikovom atomu, zajedno s navedenim ugljikovim atomom, tvore C3-4cikloalkil; A je odabran od A3 i A4: [image] (A3); [image] (A4); gdje je veza koja je označena sa zvjezdicom, priključena na dušikov atom; R5 je vodik ili metil; s je 0, 1 ili 2; i svaki R6 neovisno je halogen, C1-4alkil, C1-4halogenalkil, C1-4alkoksi, C1-4halogenalkoksi ili C3-4cikloalkil; ili njegova sol.
7. Spoj formule I prema zahtjevu 1, naznačen time, da je navedeni spoj odabran iz skupine koju čine: 4-ciklobutilpiperazin-1-karboksilat 1-(6-okso-1,6-dihidropiridazin-3-il)piperidin-4-ila; 4-izopropilpiperazin-1-karboksilat 1-(1-metil-6-okso-1,6-dihidropiridazin-3-il)piperidin-4-ila; 4-izopropilpiperazin-1-karboksilat 1-(6-okso-1,6-dihidropiridazin-3-il)piperidin-4-ila; 4-ciklopropilpiperazin-1-karboksilat 1-(6-okso-1,6-dihidropiridazin-3-il)piperidin-4-ila; 4-ciklobutilpiperazin-1-karboksilat 1-(1-metil-6-okso-1,6-dihidropiridazin-3-il)piperidin-4-ila; 4-izopropilpiperazin-1-karboksilat 1-(1-etil-6-okso-1,6-dihidropiridazin-3-il)piperidin-4-ila; 4-izopropilpiperazin-1-karboksilat 1-(1-metil-2-okso-1,2-dihidropiridin-4-il)piperidin-4-ila; 4-ciklobutilpiperazin-1-karboksilat 1-(2-okso-1,2-dihidropiridin-4-il)piperidin-4-ila; 4-izopropilpiperazin-1-karboksilat 1-(2-okso-1,2-dihidropiridin-4-il)piperidin-4-ila; i 4-izopropilpiperazin-1-karboksilat 1-(6-okso-1,6-dihidropiridin-3-il)piperidin-4-ila; ili soli tih spojeva.
8. Spoj formule I prema zahtjevu 1, naznačen time, da navedeni spoj je 4-ciklobutilpiperazin-1-karboksilat 1-(6-okso-1,6-dihidropiridazin-3-il)piperidin-4-ila, koji ima sljedeću formulu: [image] ili njegova sol.
9. Spoj formule I prema zahtjevu 1, naznačen time, da navedeni spoj je 4-izopropilpiperazin-1-karboksilat 1-(1-metil-6-okso-1,6-dihidropiridazin-3-il)piperidin-4-ila, koji ima sljedeću formulu: [image] ili njegova sol.
10. Spoj formule I prema zahtjevu 1, naznačen time, da navedeni spoj je 4-izopropilpiperazin-1-karboksilat 1-(6-okso-1,6-dihidropiridazin-3-il)piperidin-4-ila, koji ima sljedeću formulu: [image] ili njegova sol.
11. Spoj formule I prema zahtjevu 1, naznačen time, da navedeni spoj je 4-ciklobutilpiperazin-1-karboksilat 1-(1-metil-6-okso-1,6-dihidropiridazin-3-il)piperidin-4-ila, koji ima sljedeću formulu: [image] ili njegova sol.
12. Spoj formule I prema zahtjevu 1, naznačen time, da navedeni spoj je slobodan oblik od 4-ciklobutilpiperazin-1-karboksilat 1-(1-metil-6-okso-1,6-dihidropiridazin-3-il)piperidin-4-ila u čvrstom obliku; ili je to sol od 4-ciklobutilpiperazin-1-karboksilat 1-(1-metil-6-okso-1,6-dihidropiridazin-3-il)piperidin-4-ila u čvrstom obliku, pri čemu spomenuta sol je citrat, hidroklorid, fumarat, adipat, maleat ili sebakat od 4-ciklobutilpiperazin-1-karboksilat 1-(1-metil-6-okso-1,6-dihidropiridazin-3-il)piperidin-4-ila.
13. Farmaceutski sastav, naznačen time, da obuhvaća terapeutski djelotvornu količinu spoja prema bilo kojem od zahtjeva 1 do 12, ili njegove soli, te jedan ili više farmaceutski prikladnih nosača.
14. Spoj prema bilo kojem od zahtjeva 1 do 12, ili njegova sol, naznačen/a time, da se upotrebljava kao lijek.
15. Spoj prema bilo kojem od zahtjeva 1 do 12, ili njegova sol, naznačen/a time, da se upotrebljava u liječenju poremećaja ili bolesti kod pojedinca, koji/koja je posredovan/a putem H3-receptora.
16. Spoj prema bilo kojem od zahtjeva 1 do 12, ili njegova sol, za uporabu prema zahtjevu 15, naznačen/a time, da je poremećaj ili bolest odabran/a od sljedećih: pretilost, epilepsija, poremećaji spavanja i budnosti s povećanom pospanošću tijekom dana, poremećaji povezani s povećanim umorom ili prekomjernom pospanošću, ili poremećaji s pogoršanim kognitivnim funkcijama.
17. Spoj prema bilo kojem od zahtjeva 1 do 12, ili njegova sol, za uporabu prema zahtjevu 15, naznačen/a time, da poremećaj je narkolepsija.
18. Kombinacija, naznačena time, da obuhvaća terapeutski djelotvornu količinu spoja prema bilo kojem od zahtjeva 1 do 12, ili njegove soli, te jednu ili više terapeutski djelotvornih tvari.
19. Spoj prema bilo kojem od zahtjeva 1 do 12, ili njegova sol, u kombinaciji s drugim djelotvornim tvarima, naznačen/a time, da se upotrebljava u liječenju poremećaja koji su posredovani putem H3-receptora.
20. Spoj prema bilo kojem od zahtjeva 1 do 12, ili njegova sol, u kombinaciji s drugim djelotvornim tvarima, za uporabu prema zahtjevu 19, naznačen/a time, da je poremećaj odabran od sljedećih: pretilost, epilepsija, poremećaji spavanja i budnosti s povećanom pospanošću tijekom dana, poremećaji povezani s povećanim umorom ili prekomjernom pospanošću, ili poremećaji s pogoršanim kognitivnim funkcijama.
21. Spoj prema bilo kojem od zahtjeva 1 do 12, ili njegova sol, u kombinaciji s drugim djelotvornim tvarima, za uporabu prema zahtjevu 19, naznačen/a time, da poremećaj je narkolepsija.
22. Spoj, naznačen time, da je to spoj formule II-1: [image] (II-1); ili njegova sol; u kojoj p, q, r, R3 i A su isti kao što su definirani za formulu I; i Ra je izlazna skupina.
HRP20171692TT 2012-07-20 2017-11-06 Derivati karbamat/uree HRP20171692T1 (hr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
CN2012078933 2012-07-20
CN2013078309 2013-06-28
EP13770709.7A EP2875016B1 (en) 2012-07-20 2013-07-18 Carbamate/urea derivatives
PCT/IB2013/055916 WO2014013469A1 (en) 2012-07-20 2013-07-18 Carbamate/urea derivatives

Publications (1)

Publication Number Publication Date
HRP20171692T1 true HRP20171692T1 (hr) 2017-12-15

Family

ID=49263333

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20171692TT HRP20171692T1 (hr) 2012-07-20 2017-11-06 Derivati karbamat/uree

Country Status (42)

Country Link
US (4) US9034874B2 (hr)
EP (1) EP2875016B1 (hr)
JP (1) JP6203841B2 (hr)
KR (1) KR102150739B1 (hr)
CN (1) CN104470911B (hr)
AP (1) AP3710A (hr)
AR (1) AR092354A1 (hr)
AU (1) AU2013291617B2 (hr)
BR (1) BR112015001207B1 (hr)
CA (1) CA2878006C (hr)
CL (1) CL2015000056A1 (hr)
CO (1) CO7170173A2 (hr)
CR (1) CR20150019A (hr)
CU (1) CU24248B1 (hr)
CY (1) CY1119492T1 (hr)
DK (1) DK2875016T3 (hr)
EA (1) EA026091B1 (hr)
ES (1) ES2648512T3 (hr)
GT (1) GT201500012A (hr)
HK (1) HK1204609A1 (hr)
HR (1) HRP20171692T1 (hr)
HU (1) HUE035592T2 (hr)
IL (1) IL236656A (hr)
IN (1) IN2014DN10449A (hr)
JO (1) JO3439B1 (hr)
LT (1) LT2875016T (hr)
MX (1) MX362059B (hr)
MY (1) MY168752A (hr)
NO (1) NO2875016T3 (hr)
NZ (1) NZ702346A (hr)
PE (1) PE20151155A1 (hr)
PH (1) PH12014502743B1 (hr)
PL (1) PL2875016T3 (hr)
PT (1) PT2875016T (hr)
RS (1) RS56479B1 (hr)
SG (2) SG10201700188PA (hr)
SI (1) SI2875016T1 (hr)
TN (1) TN2014000497A1 (hr)
TW (1) TWI597276B (hr)
UY (1) UY34921A (hr)
WO (1) WO2014013469A1 (hr)
ZA (1) ZA201408805B (hr)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR088256A1 (es) 2011-10-08 2014-05-21 Novartis Ag Derivados de carbamato / urea como antagonistas del receptor h3
US9034874B2 (en) 2012-07-20 2015-05-19 Novartis Ag Carbamate/urea derivatives
EP3391886A1 (en) * 2017-04-19 2018-10-24 Novartis AG The use of a h3r inverse agonist for the treatment of shift work disorder
US20190381056A1 (en) 2018-06-17 2019-12-19 Axsome Therapeutics, Inc. Compositions for delivery of reboxetine
AU2019359549A1 (en) 2018-10-11 2021-03-25 Novartis Ag The use of a H3R inverse agonist for the treatment of excessive daytime sleepiness associated with parkinson's disease (PD)
US11020402B2 (en) 2018-10-15 2021-06-01 Axsome Therapeutics, Inc. Use of reboxetine to treat narcolepsy
US20200147093A1 (en) 2018-10-15 2020-05-14 Axsome Therapeutics, Inc. Use of esreboxetine to treat nervous system disorders such as fibromyalgia
WO2022113008A1 (en) 2020-11-27 2022-06-02 Richter Gedeon Nyrt. Histamine h3 receptor antagonists/inverse agonists for the treatment of autism spectrum disorder

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2567518B1 (fr) 1984-07-11 1987-11-13 Sanofi Sa Nouveaux composes a noyau heterocyclique azote, leur preparation et les medicaments qui en contiennent
TW301607B (hr) 1993-03-09 1997-04-01 Takeda Pharm Industry Co Ltd
HUP0204496A3 (en) 2000-01-20 2004-07-28 Eisai Co Ltd Novel piperidine compounds and pharmaceutical compositions containing the same and process for preparation the same
US6849621B2 (en) 2001-03-13 2005-02-01 Schering Corporation Piperidine compounds
WO2004078163A2 (en) 2003-02-28 2004-09-16 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
EP1615909B1 (en) 2003-04-23 2008-07-23 Glaxo Group Limited Piperazine derivatives and their use for the treatment of neurological and psychiatric diseases
EP1717230B1 (en) 2004-02-13 2014-08-06 Msd K.K. Fused-ring 4-oxopyrimidine derivative
SE0401971D0 (sv) * 2004-08-02 2004-08-02 Astrazeneca Ab Piperidne derivatives
CN1976926A (zh) 2004-09-02 2007-06-06 特瓦制药工业有限公司 奥美沙坦酯的制备
CA2575177A1 (en) 2004-09-02 2006-03-16 Teva Pharmaceutical Industries Ltd. Purification of olmesartan medoxomil
EP1909797A4 (en) 2005-08-02 2013-02-27 Neurogen Corp DIPIPERAZINYL KETONE AND RELATED ANALOG
JP2009514846A (ja) 2005-11-04 2009-04-09 ファイザー・リミテッド テトラヒドロナフチリジン誘導体
US20090182140A1 (en) 2005-12-02 2009-07-16 Mitsubishi Tanabe Pharma Corporation Alicyclic Heterocyclic Compound
ATE546441T1 (de) * 2007-12-05 2012-03-15 Astrazeneca Ab Piperazinderivate und ihre verwendung als modulatoren des leptinrezeptors
TWI498115B (zh) * 2007-12-27 2015-09-01 Daiichi Sankyo Co Ltd 咪唑羰基化合物
EP2328586A2 (en) 2008-05-20 2011-06-08 Cephalon, Inc. Substituted pyridazinone derivatives as histamine-3 (h3) receptor ligands
ES2601007T3 (es) 2010-01-22 2017-02-13 Taiho Pharmaceutical Co., Ltd. Compuesto de piperazina que presenta un efecto inhibidor de PGDS
TW201217312A (en) * 2010-09-22 2012-05-01 Gruenenthal Gmbh Substituted benzamide compounds
AR088256A1 (es) * 2011-10-08 2014-05-21 Novartis Ag Derivados de carbamato / urea como antagonistas del receptor h3
US9034874B2 (en) 2012-07-20 2015-05-19 Novartis Ag Carbamate/urea derivatives

Also Published As

Publication number Publication date
NZ702346A (en) 2017-06-30
EA026091B1 (ru) 2017-02-28
HK1204609A1 (en) 2015-11-27
CU24248B1 (es) 2017-02-02
US9034874B2 (en) 2015-05-19
ZA201408805B (en) 2016-08-31
WO2014013469A1 (en) 2014-01-23
CU20150006A7 (es) 2016-02-29
CL2015000056A1 (es) 2015-03-20
US20140163036A1 (en) 2014-06-12
EP2875016B1 (en) 2017-08-23
MX362059B (es) 2019-01-07
KR20150036081A (ko) 2015-04-07
AU2013291617B2 (en) 2015-10-01
CO7170173A2 (es) 2015-01-28
US9273026B2 (en) 2016-03-01
PH12014502743A1 (en) 2015-02-02
TW201408656A (zh) 2014-03-01
CN104470911A (zh) 2015-03-25
MX2015000903A (es) 2015-04-10
JP2015522606A (ja) 2015-08-06
US20150218127A1 (en) 2015-08-06
IL236656A (en) 2017-12-31
CA2878006A1 (en) 2014-01-23
PH12014502743B1 (en) 2015-02-02
DK2875016T3 (da) 2017-11-27
IN2014DN10449A (hr) 2015-08-21
AU2013291617A1 (en) 2015-01-15
CR20150019A (es) 2015-05-04
TN2014000497A1 (en) 2016-03-30
US9624192B2 (en) 2017-04-18
SG11201408020RA (en) 2015-03-30
BR112015001207A8 (pt) 2018-01-16
CA2878006C (en) 2020-10-27
NO2875016T3 (hr) 2018-01-20
BR112015001207A2 (pt) 2017-08-01
PE20151155A1 (es) 2015-08-05
PT2875016T (pt) 2017-11-30
GT201500012A (es) 2017-11-09
RS56479B1 (sr) 2018-01-31
JO3439B1 (ar) 2019-10-20
AR092354A1 (es) 2015-04-15
EA201590250A1 (ru) 2015-05-29
UY34921A (es) 2014-02-28
HUE035592T2 (en) 2018-05-28
EP2875016A1 (en) 2015-05-27
SG10201700188PA (en) 2017-02-27
AP3710A (en) 2016-05-31
TWI597276B (zh) 2017-09-01
JP6203841B2 (ja) 2017-09-27
BR112015001207B1 (pt) 2022-08-09
US20170275264A1 (en) 2017-09-28
LT2875016T (lt) 2017-11-10
KR102150739B1 (ko) 2020-09-02
ES2648512T3 (es) 2018-01-03
PL2875016T3 (pl) 2018-01-31
AP2014008109A0 (en) 2014-12-31
MY168752A (en) 2018-11-30
CN104470911B (zh) 2018-04-06
SI2875016T1 (sl) 2017-11-30
CY1119492T1 (el) 2018-03-07
IL236656A0 (en) 2015-02-26
US20160244426A1 (en) 2016-08-25

Similar Documents

Publication Publication Date Title
HRP20171692T1 (hr) Derivati karbamat/uree
HRP20180916T1 (hr) Inhibitori demetilaze od lsd1 na bazi arilciklopropilamina i njihova medicinska uporaba
HRP20130738T1 (hr) Postupak lijeäśenja ili profilakse
HRP20170638T1 (hr) MODULATORI RETINOIDNIMA SRODNOG SIROČETA RECEPTORA γ (ROR-γ), NAMIJENJENI UPOTREBI U LIJEČENJU AUTOIMUNIH I PROTUUPALNIH BOLESTI
HRP20211041T1 (hr) Anthelmintski depsipeptidni spojevi
HRP20170787T1 (hr) Piridon amidi kao modulatori natrijevih kanala
HRP20140011T1 (hr) Derivati oksazina i njihova uporaba u lijeäśenju neuroloških poremeä†aja
HRP20161103T1 (hr) Kemijski spojevi
JP2014514286A5 (hr)
MA30231B1 (fr) Derives de benzamides et d'heteroarenes
JP2015522606A5 (hr)
BRPI0820112B8 (pt) derivados de isoxazol-piridina, seu uso e processos de preparação e medicamento
RU2013138717A (ru) Конденсированные производные аминодигидротиазина, пригодные в качестве ингибиторов васе
HRP20090593T1 (hr) Derivati benzimidazola i njihova uporaba kao antagonista aii receptora
MX2010006182A (es) Derivados de isoxazolo-piridazina.
EA201070145A1 (ru) Новые антимикробные соединения, их синтез и применение для лечения инфекций у млекопитающих
RU2017116197A (ru) 2-амино-3,5-дифтор-3,6-диметил-6-фенил-3,4,5,6-тетрагидропиридины как ингибиторы васе1 для лечения болезни альцгеймера
RU2018104868A (ru) 2-амино-3-фтор-3-(фторметил)-6-метил-6-фенил-3,4,5,6-тетрагидропиридины в качестве ингибиторов bace1
RS50661B (sr) Beta kristalni oblik ivabradin hidrohlorida, postupak njegove izrade i farmaceutske smeše koje ga sadrže
PT2420491E (pt) Compostos de piperidina 3,5-substituída como inibidores de renina
SI2935307T1 (en) Non-reactive 19-alkoxy-17-substituted steroids useful in therapeutic procedures
HRP20171515T1 (hr) Spojevi fenoksietilpiperidina
NZ588121A (en) Novel estrogen receptor ligands
MX2010005753A (es) Derivados de isoxazolo-pirazina.
HRP20140884T1 (hr) Derivati fenoksipiridinilamida i njihova primjena u lijeäśenju bolesnih stanja posredovanih inhibitorima pde4