MX2019010096A - Derivados de 1, 4, 6-trisustituidos-2-alquil-1h-benzo[d]imidazol como inhibidores de dihidroorotato oxigenasa. - Google Patents

Derivados de 1, 4, 6-trisustituidos-2-alquil-1h-benzo[d]imidazol como inhibidores de dihidroorotato oxigenasa.

Info

Publication number
MX2019010096A
MX2019010096A MX2019010096A MX2019010096A MX2019010096A MX 2019010096 A MX2019010096 A MX 2019010096A MX 2019010096 A MX2019010096 A MX 2019010096A MX 2019010096 A MX2019010096 A MX 2019010096A MX 2019010096 A MX2019010096 A MX 2019010096A
Authority
MX
Mexico
Prior art keywords
trisubstituted
benzo
alkyl
imidazole derivatives
formula
Prior art date
Application number
MX2019010096A
Other languages
English (en)
Inventor
Sanjeeva Rao Thunuguntla Siva
Kumar Panigrahi Sunil
Hosahalli Subramanya
Schwarz Matthias
Arlt Michael
Original Assignee
Merck Patent Gmbh
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 Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of MX2019010096A publication Critical patent/MX2019010096A/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/08—Radicals containing only hydrogen and carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
    • 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/5355—Non-condensed oxazines 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
    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • 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
    • C07D401/10—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 carbon chain containing aromatic rings
    • 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
    • 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
    • C07D403/10—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 linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D417/10—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 carbon chain containing aromatic rings

Abstract

La presente invencion provee derivados de 1, 4, 6-trisustituidos-2-alquil-1Hbenzo[d]imidazol como compuestos inhibidores de dihidroorotato oxigenasa de formula (I), los cuales pueden ser terapeuticamente utiles como inhibidores de DHODH; en los cuales R1 a R3 y 'm' tienen significados dados en la especificacion y sales farmacéuticamente aceptables o estereoisomeros de los mismos que son utiles en el tratamiento y prevencion en enfermedades o trastornos, en particular su uso en enfermedades o trastornos donde existe una ventaja en la inhibicion de DHODH; la presente invencion tambien provee metodos para sintetizar derivados de 1,4,6-trisustituidos-2-alquil-1H-benz o[d]imidazol de formula (I); la presente invención tambien provee formulaciones farmaceuticas que comprenden al menos uno del compuesto inhibidor DHODH de formula (I) junto con un portador farmaceuticamente aceptable, diluyente o excipiente.
MX2019010096A 2017-02-24 2018-02-23 Derivados de 1, 4, 6-trisustituidos-2-alquil-1h-benzo[d]imidazol como inhibidores de dihidroorotato oxigenasa. MX2019010096A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN201741006586 2017-02-24
PCT/EP2018/054602 WO2018154088A1 (en) 2017-02-24 2018-02-23 1, 4, 6-trisubstituted-2-alkyl-1h-benzo[d]imidazole derivatives as dihydroorotate oxygenase inhibitors

Publications (1)

Publication Number Publication Date
MX2019010096A true MX2019010096A (es) 2020-01-09

Family

ID=61563366

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2019010096A MX2019010096A (es) 2017-02-24 2018-02-23 Derivados de 1, 4, 6-trisustituidos-2-alquil-1h-benzo[d]imidazol como inhibidores de dihidroorotato oxigenasa.

Country Status (13)

Country Link
US (1) US11028054B2 (es)
EP (1) EP3585772B1 (es)
JP (1) JP7146785B2 (es)
KR (1) KR20190120786A (es)
CN (1) CN110325514B (es)
AU (1) AU2018223982B2 (es)
BR (1) BR112019017567A2 (es)
CA (1) CA3053068A1 (es)
EA (1) EA201991916A1 (es)
IL (1) IL268843B (es)
MA (1) MA47593A (es)
MX (1) MX2019010096A (es)
WO (1) WO2018154088A1 (es)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW202104207A (zh) 2019-04-17 2021-02-01 美商健生生物科技公司 二氫乳清酸脫氫酶抑制劑
EP4136074A1 (en) * 2020-04-16 2023-02-22 F. Hoffmann-La Roche AG Indazole derivatives
JP2023522327A (ja) * 2020-04-16 2023-05-30 エフ． ホフマン－ラ ロシュ アーゲー ベンズイミダゾール誘導体
EP4136076A1 (en) * 2020-04-16 2023-02-22 F. Hoffmann-La Roche AG Biphenyl derivatives
JP2023521437A (ja) * 2020-04-16 2023-05-24 エフ． ホフマン－ラ ロシュ アーゲー ベンズイミダゾール誘導体
WO2021209475A1 (en) * 2020-04-16 2021-10-21 F. Hoffmann-La Roche Ag Sulfamoylamide derivatives

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4172896A (en) 1978-06-05 1979-10-30 Dainippon Pharmaceutical Co., Ltd. Methane-sulfonamide derivatives, the preparation thereof and composition comprising the same
DE59010701D1 (de) 1990-05-18 1997-05-22 Hoechst Ag Isoxazol-4-carbonsäureamide und hydroxyalkyliden-cyanessigsäureamide, diese verbindungen enthaltende arzneimittel und deren verwendung
GB9217295D0 (en) 1992-08-14 1992-09-30 Wellcome Found Controlled released tablets
US5358970A (en) 1993-08-12 1994-10-25 Burroughs Wellcome Co. Pharmaceutical composition containing bupropion hydrochloride and a stabilizer
GB9315856D0 (en) 1993-07-30 1993-09-15 Wellcome Found Stabilized pharmaceutical
US5541231A (en) 1993-07-30 1996-07-30 Glaxo Wellcome Inc. Stabilized Pharmaceutical
JP3979783B2 (ja) 1997-07-29 2007-09-19 アルコン ラボラトリーズ インコーポレイテッド ガラクトマンナンポリマー及びホウ酸塩を含む眼科組成物
US5904937A (en) 1997-10-03 1999-05-18 Fmc Corporation Taste masked pharmaceutical compositions
AU2483599A (en) 1998-01-29 1999-08-16 Sepracor, Inc. Pharmaceutical uses of optically pure (-)-bupropion
US8889112B2 (en) 1999-09-16 2014-11-18 Ocularis Pharma, Llc Ophthalmic formulations including selective alpha 1 antagonists
AU7622000A (en) * 1999-10-01 2001-05-10 Institute Of Molecular And Cell Biology Compounds for the treatment of viral-mediated diseases
US6841561B1 (en) 1999-10-01 2005-01-11 Institute Of Molecular And Cell Biology Dihydroorotate dehydrogenase inhibitors for the treatment of viral-mediated diseases
US6933289B2 (en) 2003-07-01 2005-08-23 Allergan, Inc. Inhibition of irritating side effects associated with use of a topical ophthalmic medication
EP1654002B2 (en) 2003-08-07 2014-01-29 Allergan, Inc. Compositions for delivery of therapeutics into the eyes
US20050059744A1 (en) 2003-09-12 2005-03-17 Allergan, Inc. Methods and compositions for the treatment of pain and other alpha 2 adrenergic-mediated conditions
ES2882797T3 (es) 2009-04-02 2021-12-02 Merck Serono Sa Inhibidores de dihidroorotato deshidrogenasa
EP3019482B1 (en) * 2013-02-25 2018-08-15 Aurigene Discovery Technologies Limited Trisubstituted benzotriazole derivatives as dihydroorotate oxygenase inhibitors

Also Published As

Publication number Publication date
MA47593A (fr) 2020-01-01
EP3585772B1 (en) 2023-10-11
IL268843B (en) 2022-03-01
JP7146785B2 (ja) 2022-10-04
EA201991916A1 (ru) 2020-01-21
KR20190120786A (ko) 2019-10-24
WO2018154088A1 (en) 2018-08-30
US11028054B2 (en) 2021-06-08
CA3053068A1 (en) 2018-08-30
IL268843A (en) 2019-10-31
AU2018223982A1 (en) 2019-08-29
AU2018223982B2 (en) 2022-02-03
EP3585772A1 (en) 2020-01-01
BR112019017567A2 (pt) 2020-03-24
JP2020508327A (ja) 2020-03-19
CN110325514A (zh) 2019-10-11
CN110325514B (zh) 2023-06-13
US20200140395A1 (en) 2020-05-07

Similar Documents

Publication Publication Date Title
MX2019010096A (es) Derivados de 1, 4, 6-trisustituidos-2-alquil-1h-benzo[d]imidazol como inhibidores de dihidroorotato oxigenasa.
WO2014128669A3 (en) Trisubstituted benzotriazole derivatives as dihydroorotate oxygenase inhibitors
PH12016501338A1 (en) Indazole compounds as irak4 inhibitors
PH12020500529A1 (en) Bicyclic heterocyclyl derivatives as irak4 inhibitors
PH12018502227A1 (en) Macrocyclic mcl1 inhibitors for treating cancer
WO2014106800A3 (en) Substituted 2-amino pyrimidine derivatives as kinase inhibitors
MX2023007192A (es) Inhibidores de prmt5.
WO2014125408A3 (en) Substituted 1h-pyrrolopyridinone derivatives as kinase inhibitors
MX2022010011A (es) Inhibidores de prmt5 novedosos.
MX2020005363A (es) Compuestos heterociclicos como inhibidores de prmt5.
EA033689B9 (ru) Ингибиторы g12c kras
EP3693369A3 (en) Bromodomain inhibitors
MX2013012776A (es) Inhibidores de la tirosina cinasa de bazo que contienen aminopiridina.
PH12021550825A1 (en) Quinoline derivatives as alpha4beta7 integrin inhibitors
MY165902A (en) Substituted pyridine derivatives as fabi inhibitors
CR20230286A (es) Inhibidores de prmt5 novedosos
PH12019500036A1 (en) Heterocyclic compound used as fgfr inhibitor
MX2020001531A (es) Nuevos compuestos hetorociclicos como inhibidores de cdk8/19.
SA519410865B1 (ar) مركب حلقي شبيه بكُومارين بوصفه مثبط mek واستخدامه
NZ631388A (en) Phenyl-urea and phenyl-carbamate derivatives as inhibitors of protein aggregation
WO2014072930A3 (en) Fused pyridine derivatives as antibacterial agents
AU2018279669A8 (en) Carboxylic acid derivative as at AT2R receptor antagonist
MX2019012640A (es) Metodos de uso de derivados de benzotriazoles trisustituidos como inhibidores de dihidroorotato-oxigenasa.
ZA202201499B (en) Dual atm and dna-pk inhibitors for use in anti-tumor therapy
IN2014MN02433A (es)