BR112013031121A2 - composto de acordo com a fórmula i a v, ou um sal farmaceuticamente aceitável, solvato, polimorfo, ou pró-droga do mesmo; composto; polimorfo de sal cloridrato de 2-morfolino-n-(3-(4-(5-(pirrolidina-1-carbonil)-1h-pirrol-3-il)tiazol-2-il)acetamida (fórmula i); ingrediente ativo constituído do mesmo; composição farmacêutica; polimorfo de 2-morfolino-n-(3-(4-(5-(pirrolidina-1-carbonil)1h-pirrol-3-il)tiazol-2-il)fenil)acetamida (fórmula i); ingrediente ativo constituído do mesmo; uso de um composto ou sal farmaceuticamente aceitável, solvato, polimorfo ou pró-droga do mesmo e uso de um polimorfo ou ingrediente ativo de sal cloridrato de 2-morfolino-n-(3-(4-(5-(pirrolidina-1-carbonil)-1h-pirrol-3-il)tiazol-2il)tiazol-2-il)fenil)acetamida (fórmula i) e uso de um polimorfo ou ingrediente ativo de 2-morfolino-n-(3-(4-(5-(pirrolidina-1-carbonil)-1h1pirrol-3-il)tiazol-2-il)fenil)acetamida(fórmula i) na fabricação de um medicamento - Google Patents

composto de acordo com a fórmula i a v, ou um sal farmaceuticamente aceitável, solvato, polimorfo, ou pró-droga do mesmo; composto; polimorfo de sal cloridrato de 2-morfolino-n-(3-(4-(5-(pirrolidina-1-carbonil)-1h-pirrol-3-il)tiazol-2-il)acetamida (fórmula i); ingrediente ativo constituído do mesmo; composição farmacêutica; polimorfo de 2-morfolino-n-(3-(4-(5-(pirrolidina-1-carbonil)1h-pirrol-3-il)tiazol-2-il)fenil)acetamida (fórmula i); ingrediente ativo constituído do mesmo; uso de um composto ou sal farmaceuticamente aceitável, solvato, polimorfo ou pró-droga do mesmo e uso de um polimorfo ou ingrediente ativo de sal cloridrato de 2-morfolino-n-(3-(4-(5-(pirrolidina-1-carbonil)-1h-pirrol-3-il)tiazol-2il)tiazol-2-il)fenil)acetamida (fórmula i) e uso de um polimorfo ou ingrediente ativo de 2-morfolino-n-(3-(4-(5-(pirrolidina-1-carbonil)-1h1pirrol-3-il)tiazol-2-il)fenil)acetamida(fórmula i) na fabricação de um medicamento

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Publication number
BR112013031121A2
BR112013031121A2 BR112013031121-5A BR112013031121A BR112013031121A2 BR 112013031121 A2 BR112013031121 A2 BR 112013031121A2 BR 112013031121 A BR112013031121 A BR 112013031121A BR 112013031121 A2 BR112013031121 A2 BR 112013031121A2
Authority
BR
Brazil
Prior art keywords
polymorph
formula
thiazol
pyrrol
carbonyl
Prior art date
Application number
BR112013031121-5A
Other languages
English (en)
Other versions
BR112013031121B1 (pt
Inventor
M. Becker Oren
Bloch Itai
Ben-Zeev Efrat
Shitrit Alina
Yacovan Avihai
Gazal Sharon
Behar Vered
Konson Alexander
Schutz Nili
Mirilashvili Sima
Golan Gali
Original Assignee
Clevexel Pharma
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 Clevexel Pharma filed Critical Clevexel Pharma
Publication of BR112013031121A2 publication Critical patent/BR112013031121A2/pt
Publication of BR112013031121B1 publication Critical patent/BR112013031121B1/pt

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    • C—CHEMISTRY; METALLURGY
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    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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    • A61P25/00—Drugs for disorders of the nervous system
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    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/04—Artificial tears; Irrigation solutions
    • 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]
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or 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
    • C07D277/38—Nitrogen atoms
    • C07D277/40—Unsubstituted amino or imino radicals
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    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/113—Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
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    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/14—Ortho-condensed systems
    • C07D491/147—Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
    • C—CHEMISTRY; METALLURGY
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    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/22—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains four or more hetero rings
    • C—CHEMISTRY; METALLURGY
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    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D495/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F15/00—Compounds containing elements of Groups 8, 9, 10 or 18 of the Periodic System
    • C07F15/06—Cobalt compounds
    • C07F15/065—Cobalt compounds without a metal-carbon linkage

Abstract

composto de acordo com a fórmula i a v, ou um sal farmaceuticamente aceitável, solvato, polimorfo, ou pródroga do mesmo; composto; polimorfo de sal cloridrato de 2- morfolino-n-(3-(4-(5-(pirrolidina-1-carbonil)-1 h-pirrol-3- il)tiazol-2-il)fenil)acetamida (fórmula i); ingrediente ativo constituído do mesmo; composição farmacêutica; polimorfo de 2-morfolino-n-(3-(4-(5-(pirrolidina-1-carbonil)-1 h-pirrol-3- il)tiazol-2-il)fenil)acetamida (fórmula i); ingrediente ativo constituído do mesmo; uso de um composto ou sal farmaceuticamente aceitável, solvato, polimorfo ou pródroga do mesmo e uso de um polimorfo ou ingrediente ativo de sal cloridrato de 2-morfolino-n-(3-(4-(5-pirrolidina-1-carbonil)-1 h-pirrol-3-il)tiazol-2-il)fenil)acetamida (fórmula i) e uso de um polimorfo ou ingrediente ativo de 2-morfolino-n-(3- (4-(5-(pirrolidina-1-carbonil)-1 h-pirrol-3-il)tiazol-2- il)fenil)acetamida(fórmula i) na abricação de um medicamento a invenção refere-se aos compostos e métodos para modular componentes de uma cascata de sinalização de quinase.
BR112013031121-5A 2011-06-07 2012-06-07 Composto para modulação de uma quinase BR112013031121B1 (pt)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201161520256P 2011-06-07 2011-06-07
US61/520,256 2011-06-07
US201161562700P 2011-11-22 2011-11-22
US61/562,700 2011-11-22
US201261640139P 2012-04-30 2012-04-30
US61/640,139 2012-04-30
PCT/IB2012/001987 WO2012172438A2 (en) 2011-06-07 2012-06-07 Compositions and methods for modulating a kinase

Publications (2)

Publication Number Publication Date
BR112013031121A2 true BR112013031121A2 (pt) 2019-04-09
BR112013031121B1 BR112013031121B1 (pt) 2022-03-29

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BR112013031121-5A BR112013031121B1 (pt) 2011-06-07 2012-06-07 Composto para modulação de uma quinase

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US (1) US8937065B2 (pt)
EP (1) EP2718290B1 (pt)
JP (1) JP6054379B2 (pt)
CN (1) CN103717593B (pt)
AU (1) AU2012270029B2 (pt)
BR (1) BR112013031121B1 (pt)
CA (1) CA2837268C (pt)
DK (1) DK2718290T3 (pt)
ES (1) ES2585244T3 (pt)
HK (1) HK1191324A1 (pt)
HR (1) HRP20160879T1 (pt)
HU (1) HUE028097T2 (pt)
IL (1) IL229692A (pt)
MX (1) MX355415B (pt)
PL (1) PL2718290T3 (pt)
PT (1) PT2718290T (pt)
WO (1) WO2012172438A2 (pt)
ZA (1) ZA201309042B (pt)

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BR112015001690A2 (pt) 2012-07-24 2017-11-07 Pharmacyclics Inc mutações associadas com a resistência a inibidores da tirosina quinase de bruton (btk)
CN107056754B (zh) * 2015-12-07 2020-12-04 苏州信诺维医药科技有限公司 内嵌脲类结构的wnt通路抑制剂
US10821104B2 (en) 2015-12-07 2020-11-03 Suzhou Sinovent Pharmaceuticals Co., Ltd. Five-membered heterocyclic amides WNT pathway inhibitor
WO2021146903A1 (zh) * 2020-01-21 2021-07-29 苏州信诺维医药科技股份有限公司 一种含氮化合物的晶型
AU2022280871A1 (en) * 2021-05-26 2023-12-07 Emory University Jak inhibitors for managing conditions in patients with down's syndrome or other trisomy
CA3233636A1 (en) * 2021-09-29 2023-04-06 Repare Therapeutics Inc. N-(5-substituted-[(1,3,4-thiadiazolyl) or (thiazolyl)])(substituted)carboxamide compounds and use thereof for inhibiting human polymerase theta

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JP6054379B2 (ja) 2016-12-27
HK1191324A1 (zh) 2014-07-25
IL229692A (en) 2017-04-30
CA2837268C (en) 2020-05-12
CN103717593B (zh) 2016-07-06
ZA201309042B (en) 2014-08-27
IL229692A0 (en) 2014-01-30
WO2012172438A9 (en) 2013-02-07
JP2014520108A (ja) 2014-08-21
WO2012172438A2 (en) 2012-12-20
WO2012172438A3 (en) 2013-03-28
US20120316148A1 (en) 2012-12-13
EP2718290B1 (en) 2016-05-04
PL2718290T3 (pl) 2016-11-30
MX2013014433A (es) 2014-02-27
CN103717593A (zh) 2014-04-09
HRP20160879T1 (hr) 2016-09-23
CA2837268A1 (en) 2012-12-20
MX355415B (es) 2018-04-18
AU2012270029A8 (en) 2014-01-30
AU2012270029A1 (en) 2012-12-20
ES2585244T3 (es) 2016-10-04
BR112013031121B1 (pt) 2022-03-29
US8937065B2 (en) 2015-01-20
PT2718290T (pt) 2016-07-14

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