AR092354A1 - Derivados de carbamato/urea - Google Patents

Derivados de carbamato/urea

Info

Publication number
AR092354A1
AR092354A1 ARP130102583A ARP130102583A AR092354A1 AR 092354 A1 AR092354 A1 AR 092354A1 AR P130102583 A ARP130102583 A AR P130102583A AR P130102583 A ARP130102583 A AR P130102583A AR 092354 A1 AR092354 A1 AR 092354A1
Authority
AR
Argentina
Prior art keywords
alkyl
cycloalkyl
halogen
amino
once
Prior art date
Application number
ARP130102583A
Other languages
English (en)
Inventor
Jiang Haiyang
J Troxler Thomas
Wang Tielin
Curzi Marco
Wang Xiaoyang
Kay Dodd Stephanie
Gary Bock Marck
Auberson Yves
Braga Dario
Karpinski Piotr
Luca Giaffreda Stefano
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=AR092354(A1) "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 AR092354A1 publication Critical patent/AR092354A1/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/04Immunostimulants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13Dicarboxylic acids
    • C07C57/15Fumaric acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/235Saturated compounds containing more than one carboxyl group
    • C07C59/245Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
    • C07C59/265Citric acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Abstract

Reivindicación 1: Un compuesto de la fórmula (1), o una sal del mismo, en donde R¹ es alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₆, cicloalquenilo C₅₋₆ o cicloalquil C₃₋₆-alquil C₁₋₄; en donde dicho alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆ o cicloalquilo C₃₋₆-alquilo C₁₋₄ puede ser sustituido una vez o más de una vez por halógeno, y en donde dicho cicloalquilo C₃₋₆ o cicloalquenilo C₅₋₆ pueden sustituirse una vez o más de una vez por halógeno, alquilo C₁₋₄ o halógenoalquilo C₁₋₄; m es 1 ó 2; n es 0, 1, 2, 3 ó 4; cada R² es independientemente halógeno, hidroxilo, amino, ciano, nitro, alquilo C₁₋₆, halógenoalquilo C₁₋₆, hidroxialquilo C₁₋₆, alcoxi C₁₋₄-alquilo C₁₋₆, amino-alquilo C₁₋₆, alquil C₁₋₄-amino-alquilo C₁₋₆, di(alquilo C₁₋₄)-amino-alquilo C₁₋₆, alcoxilo C₁₋₆, halógeno-alcoxilo C₁₋₆, alquilamino C₁₋₆, di(alquil C₁₋₆)amino, alquenilo C₂₋₆, halógenoalquenilo C₂₋₆, alquinilo C₂₋₆ o halógenoalquilo C₂₋₆; o cicloalquilo C₃₋₆, en donde un átomo de carbono puede reemplazarse por un átomo de oxígeno, en donde el cicloalquilo C₃₋₆ puede fijarse directamente al metileno o a través de un alquileno C₁₋₂, y en donde el cicloalquilo C₃₋₆ puede sustituirse una vez o más de una vez por halógeno; o dos R² en el mismo átomo de carbono forman junto con dicho átomo de carbono un cicloalquilo C₃₋₆; X¹ es oxígeno u oxígeno -N(R⁴)-; R⁴ es hidrógeno, alquilo C₁₋₆, cicloalquilo C₃₋₆, o cicloalquil C₃₋₆-alquilo C₁₋₂; p es 1 y q es 1; p es 0 y q es 1; o p es 0 y q es 0; r es 0, 1, 2, 3 ó 4; cada R³ es independientemente halógeno, hidroxilo, amino, ciano, nitro, alquilo C₁₋₆, C₁₋₆halogenalquilo, C₁₋₆hidroxialquilo, C₁₋₄alcoxi-alquilo C₁₋₆, amino-alquilo C₁₋₆, alquil C₁₋₄-amino-alquilo C₁₋₆, di(alquilo C₁₋₄)-amino-alquilo C₁₋₆, alcoxilo C₁₋₆, halógeno-alcoxilo C₁₋₆, alquilamino C₁₋₆, di(alquil C₁₋₆)amino, alquenilo C₂₋₆, halógenoalquenilo C₂₋₆, alquinilo C₂₋₆ o halógenoalquilo C₂₋₆; o cicloalquilo C₃₋₆, en donde un átomo de carbono puede reemplazarse por un átomo de oxígeno, en donde el cicloalquilo C₃₋₆ puede fijarse directamente al metileno o a través de un alquileno C₁₋₂, y en donde el cicloalquilo C₃₋₆ puede sustituirse una vez o más de una vez por halógeno; o dos R³ en el mismo átomo de carbono forman junto con dicho átomo de carbono un cicloalquilo C₃₋₆; A es un resto de fórmula (2) en donde el enlace marcado con el asterisco se fija al átomo de nitrógeno; R⁵ es hidrógeno, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₆, cicloalquenilo C₅₋₆ o cicloalquil C₃₋₆-alquil C₁₋₄; en donde dicho alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆ o cicloalquilo C₃₋₆-alquilo C₁₋₄ puede ser sustituido una vez o más de una vez por halógeno, hidroxilo o alcoxilo C₁₋₆; y en donde dicho cicloalquilo C₃₋₆ o cicloalquenilo C₅₋₆ pueden sustituirse una vez o más de una vez por halógeno, alquilo C₁₋₄ o halógenoalquilo C₁₋₄; X² es nitrógeno o carbono; s es 0, 1, 2 ó 3; cada R⁶ es independientemente halógeno, hidroxilo, amino, ciano, nitro, alquilo C₁₋₆, C₁₋₆halogenalquilo, C₁₋₆hidroxialquilo, C₁₋₄alcoxi-alquilo C₁₋₆, amino-alquilo C₁₋₆, alquil C₁₋₄-amino-alquilo C₁₋₆, di(alquilo C₁₋₄)-amino-alquilo C₁₋₆, alcoxilo C₁₋₆, halógeno-alcoxilo C₁₋₆, alquilamino C₁₋₆, di(alquil C₁₋₆)amino, alquenilo C₂₋₆, halógenoalquenilo C₂₋₆, alquinilo C₂₋₆ o halógenoalquilo C₂₋₆; o cicloalquilo C₃₋₆, en donde un átomo de carbono puede reemplazarse por un átomo de oxígeno, en donde el cicloalquilo C₃₋₆ puede fijarse directamente al metileno o a través de un alquileno C₁₋₂, y en donde el cicloalquilo C₃₋₆ puede sustituirse una vez o más de una vez por halógeno.
ARP130102583A 2012-07-20 2013-07-22 Derivados de carbamato/urea AR092354A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN2012078933 2012-07-20
CN2013078309 2013-06-28

Publications (1)

Publication Number Publication Date
AR092354A1 true AR092354A1 (es) 2015-04-15

Family

ID=49263333

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP130102583A AR092354A1 (es) 2012-07-20 2013-07-22 Derivados de carbamato/urea

Country Status (42)

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

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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
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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

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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 (es) 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 (es) 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
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
HRP20171692T1 (hr) 2017-12-15
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

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