ME03757B - Prolekovi jaki inhibitornih jedinjenja za lečenje gastorintestinalne inflamatorne bolesti - Google Patents
Prolekovi jaki inhibitornih jedinjenja za lečenje gastorintestinalne inflamatorne bolestiInfo
- Publication number
- ME03757B ME03757B MEP-2020-126A MEP2020126A ME03757B ME 03757 B ME03757 B ME 03757B ME P2020126 A MEP2020126 A ME P2020126A ME 03757 B ME03757 B ME 03757B
- Authority
- ME
- Montenegro
- Prior art keywords
- compound
- pharmaceutically acceptable
- acceptable salt
- formula
- iii
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title claims 28
- 239000000651 prodrug Substances 0.000 title claims 3
- 229940002612 prodrug Drugs 0.000 title claims 3
- 208000018522 Gastrointestinal disease Diseases 0.000 title 1
- 229940122245 Janus kinase inhibitor Drugs 0.000 title 1
- 208000010643 digestive system disease Diseases 0.000 title 1
- 208000018685 gastrointestinal system disease Diseases 0.000 title 1
- 230000002757 inflammatory effect Effects 0.000 title 1
- 150000003839 salts Chemical class 0.000 claims 19
- 229910052739 hydrogen Inorganic materials 0.000 claims 7
- 239000001257 hydrogen Substances 0.000 claims 7
- 238000000034 method Methods 0.000 claims 6
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- 208000017189 Gastrointestinal inflammatory disease Diseases 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 239000004012 Tofacitinib Substances 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 125000000217 alkyl group Chemical group 0.000 claims 3
- -1 cyano, hydroxy Chemical group 0.000 claims 3
- 125000005843 halogen group Chemical group 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- UJLAWZDWDVHWOW-YPMHNXCESA-N tofacitinib Chemical compound C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)C1=NC=NC2=C1C=CN2 UJLAWZDWDVHWOW-YPMHNXCESA-N 0.000 claims 3
- 229960001350 tofacitinib Drugs 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- 125000003277 amino group Chemical group 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 210000002429 large intestine Anatomy 0.000 claims 2
- 125000006239 protecting group Chemical group 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- UNILWMWFPHPYOR-KXEYIPSPSA-M 1-[6-[2-[3-[3-[3-[2-[2-[3-[[2-[2-[[(2r)-1-[[2-[[(2r)-1-[3-[2-[2-[3-[[2-(2-amino-2-oxoethoxy)acetyl]amino]propoxy]ethoxy]ethoxy]propylamino]-3-hydroxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-[(2r)-2,3-di(hexadecanoyloxy)propyl]sulfanyl-1-oxopropan-2-yl Chemical compound O=C1C(SCCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](CSC[C@@H](COC(=O)CCCCCCCCCCCCCCC)OC(=O)CCCCCCCCCCCCCCC)C(=O)NCC(=O)N[C@H](CO)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O)CC(=O)N1CCNC(=O)CCCCCN\1C2=CC=C(S([O-])(=O)=O)C=C2CC/1=C/C=C/C=C/C1=[N+](CC)C2=CC=C(S([O-])(=O)=O)C=C2C1 UNILWMWFPHPYOR-KXEYIPSPSA-M 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 102000053187 Glucuronidase Human genes 0.000 claims 1
- 108010060309 Glucuronidase Proteins 0.000 claims 1
- 229940076838 Immune checkpoint inhibitor Drugs 0.000 claims 1
- 102000037984 Inhibitory immune checkpoint proteins Human genes 0.000 claims 1
- 108091008026 Inhibitory immune checkpoint proteins Proteins 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 206010009887 colitis Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229930182480 glucuronide Natural products 0.000 claims 1
- 150000008134 glucuronides Chemical class 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 239000012274 immune-checkpoint protein inhibitor Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
- C07H15/26—Acyclic or carbocyclic radicals, substituted by 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/549—Sugars, nucleosides, nucleotides or nucleic acids
-
- 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- 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]
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H1/00—Processes for the preparation of sugar derivatives
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12P—FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
- C12P17/00—Preparation of heterocyclic carbon compounds with only O, N, S, Se or Te as ring hetero atoms
- C12P17/16—Preparation of heterocyclic carbon compounds with only O, N, S, Se or Te as ring hetero atoms containing two or more hetero rings
- C12P17/165—Heterorings having nitrogen atoms as the only ring heteroatoms
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Genetics & Genomics (AREA)
- Biotechnology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Wood Science & Technology (AREA)
- Zoology (AREA)
- Epidemiology (AREA)
- Microbiology (AREA)
- General Engineering & Computer Science (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Saccharide Compounds (AREA)
- Enzymes And Modification Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Claims (22)
1. Jedinjenje formule {I): (I) gde n je 0,1iii 2; R1 je izabran od vodonika, C 1•4 alkil, C 1.3 alkoksi, amino, nitro, halo, cijano, hidroksi triflurometil grupe;svaki R 2, kada je prisutan, nezavisno je izabran od C 1•4 alkil, C 1•3 alkoksi, amino, nitro, halo, cijano, hidroksi i triflurometil grupe;R3 je vodonik, metil iii etil; R4 je vodonik,metil iii etil;iii njegova farmaceutski prihvatljiva so.
2. Jedinjenje iz Patentnog zahteva 1,iii njegova farmaceutski prihvatljiva so, gde je R 1vodonik.
3. Jedinjenje iz Patentnog zahteva 1, iii njegova farmaceutski prihvatljiva so, gde je R 1 nitro grupa.
4. Jedinjenje iz Patentnog zahteva 1, iii njegova farmaceutski prihvatljiva so, gde je R 1 amino grupa.
5. Jedinjenje iz Pa tentnog zahteva 1,iii njegova farmaceutski prihvatljiva so, gde je n 0.1
6.Jedinjenje iz Patentnog zahteva 1,iii njegova farmaceutski prihvatljiva so,gde je n 1.
7. Jedinjenje iz Patentnog zahteva 1,formule (II):(II)gdeR1 je izabran od vodonika, C 1-4 alkil, C 1.3 alkoksi, amino, nitro, halo, cijano, hidroksi triflurometil grupe;iii njegova farmaceutski prihvatljiva so.
8. Jedinjenje iz Patentnog zahteva 7, iii njegova farmaceutski prihvatljiva so, gde je R1izabran od vodonika,metil,metoksi, amino,nitro i hloro grupe.
9. Jedinjenje iz Patentnog zahteva 7,iii njegova farmaceutski prihvatljiva so,gde je R1vodonik.
10. lO.Jedinjenje iz Patentnog zahteva 7,iii njegova farmaceutski prihvatljiva so,gde je R1amino grupa.
11. ll.Jedinjenje iz Patentnog zahteva 1,formule 1:Iiii njegova farmaceutski prihvatljiva so.
12.Jedinjenje iz Patentnog zahteva 11, pri cemu je jedinjenje
13.Farmaceutska kompozicija koja sadrzi farmaceutski prihvatljiv nosac i jedinjenje iz bilo kog odPatentnih zahteva od 1do 12.
14.Proces za pripremu jedinjenja iz Patentnog zahteva 1, iii njegove farmaceutski prihvatljive soli, proces koji obuhvata uklanjanje zastitnih grupa iz jedinja formule (1-A):3(1-A)iii njegove soli; pri cemu su R 1 R2, R3R4 in kao sto je definisano u Patentnom zahtevu 1; svaki PGa, ,je nezavisno hidroksilna zastitna grupa; i PGb je karboksilna zastitna grupa; da bi se obezbedilo jedinjenje formule (I) iii njegova farmaceutski prihvatljiva so.
15.Proces iz Patentnog zahteva 14, pri cemu je R 1 nitro; R 3 i R4 su metil; svaki PGa je acetil; PGb je metil grupa; i n je 0.
16.Proces iz Patentnog zahteva 14, za pripremu jedinjenja formule 1:1iii njegove farmaceutski prihvatljive soli, pri cemu jedinjenje formule (1-A) je jedinjenje formule14':414'iii njegova so,proces koji dodatno obuhvata:(a) reagovanje jedinjenja formule 12':ICH3OYN...............NHCH,0 N02H3c...0 oyo9,.·y· ,o-PGaPGa 0'pGa12'iii njegove soli; pri cemu je svaki PGa nezavisno hidroksilna zastitna grupa, sa jedinjenjem formule 13:13da bi se obezbedilo jedinjenje formule 14' iii njegova so.5
17.Jedinjenje formule 13:13iii njegova so.
18.Jedinjenje iz bilo kog od Patentnih zahteva od 1 do 12, za upotrebu u lecenju gastrointestinalne inflamatorne bolesti kod sisara.
19.Jedinjenje iz Patentnog zahteva 18, pri cemu je gastrointestinalna inflamatorna bolest ulcerozni kolitis.
20.Jedinjenje iz Patentnog zahteva 18, pri cemu je gastrointestinalna inflamatorna bolest Kronova bolest.
21.Jedinjenje iz Patentnog zahteva 18, pri cemu je gastrointestinalna inflamatorna bolest kolitis udruzen sa terapijom inhibitorima imunskih kontrolnih tacaka.
22.Prolek tofacitiniba koji sadrzi glukuronid, prema Patentnim zahtevima od 1do 12, za upotrebu u postupku isporuke tofacitiniba u debelo crevo sisara, pri cemu se prolek cepa dejstvom glukuronidaze u debelom crevu da bi se oslobodio tofacitinib.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562259273P | 2015-11-24 | 2015-11-24 | |
| PCT/US2016/063254 WO2017091544A1 (en) | 2015-11-24 | 2016-11-22 | Prodrugs of a jak inhibitor compound for treatment of gastrointestinal inflammatory disease |
| EP16808876.3A EP3380486B1 (en) | 2015-11-24 | 2016-11-22 | Prodrugs of a jak inhibitor compound for treatment of gastrointestinal inflammatory disease |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ME03757B true ME03757B (me) | 2021-04-20 |
Family
ID=57518004
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MEP-2020-126A ME03757B (me) | 2015-11-24 | 2016-11-22 | Prolekovi jaki inhibitornih jedinjenja za lečenje gastorintestinalne inflamatorne bolesti |
Country Status (33)
| Country | Link |
|---|---|
| US (3) | US10435428B2 (me) |
| EP (1) | EP3380486B1 (me) |
| JP (2) | JP6778747B2 (me) |
| KR (1) | KR20180080330A (me) |
| CN (1) | CN108290918B (me) |
| AU (1) | AU2016359494B2 (me) |
| BR (1) | BR112018010650A8 (me) |
| CA (1) | CA3003283A1 (me) |
| CL (1) | CL2018001345A1 (me) |
| CO (1) | CO2018005327A2 (me) |
| CY (1) | CY1122918T1 (me) |
| DK (1) | DK3380486T3 (me) |
| EA (1) | EA035816B1 (me) |
| ES (1) | ES2784523T3 (me) |
| HR (1) | HRP20200561T1 (me) |
| HU (1) | HUE049775T2 (me) |
| IL (1) | IL259076B (me) |
| LT (1) | LT3380486T (me) |
| ME (1) | ME03757B (me) |
| MX (1) | MX383107B (me) |
| MY (1) | MY189979A (me) |
| NZ (1) | NZ742574A (me) |
| PH (1) | PH12018501037A1 (me) |
| PL (1) | PL3380486T3 (me) |
| PT (1) | PT3380486T (me) |
| RS (1) | RS60237B1 (me) |
| SG (1) | SG11201803686UA (me) |
| SI (1) | SI3380486T1 (me) |
| SM (1) | SMT202000242T1 (me) |
| TW (1) | TWI703147B (me) |
| UA (1) | UA121270C2 (me) |
| WO (1) | WO2017091544A1 (me) |
| ZA (1) | ZA201802967B (me) |
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|---|---|---|---|---|
| ES2840650T3 (es) | 2015-11-03 | 2021-07-07 | Topivert Pharma Ltd | Derivados de 4,5,6,7-tetrahidro-1h-imidazo[4,5-c]piridina y 1,4,5,6,7,8-hexahidroimidazo[4,5-d]azepina como inhibidores de la quinasa janus |
| EP3371184A1 (en) | 2015-11-03 | 2018-09-12 | Topivert Pharma Limited | 4,5,6,7-tetrahydro-1h-imidazo[4,5-c]pyridine and 1,4,5,6,7,8-hexahydroimidazo[4,5-d]azepine derivatives as janus kinase inhibitors |
| AU2016359494B2 (en) | 2015-11-24 | 2021-01-07 | Theravance Biopharma R&D Ip, Llc | Prodrugs of a JAK inhibitor compound for treatment of gastrointestinal inflammatory disease |
| FR3060567B1 (fr) * | 2016-12-19 | 2019-05-24 | Ecole Normale Superieure De Lyon | Substrat de glycosidase fluorogene et procede de detection associe |
| US10472366B2 (en) | 2017-03-08 | 2019-11-12 | Theravance Biopharma R&D Ip, Llc | Glucuronide prodrugs of tofacitinib |
| BR112019024509A2 (pt) | 2017-05-23 | 2020-06-23 | Theravance Biopharma R&D Ip, Llc | Glicuronídeo de pró-fármacos dos inibidores da janus quinase |
| US10233174B2 (en) * | 2017-05-23 | 2019-03-19 | Theravance Biopharma R&D Ip, Llc | Thiocarbamate prodrugs of tofacitinib |
| WO2018226732A1 (en) * | 2017-06-05 | 2018-12-13 | Flagship Pioneering Innovations V, Inc. | Multibiotic agents and methods of using the same |
| KR20200121800A (ko) | 2018-01-05 | 2020-10-26 | 싸이브렉사 1, 인크. | 산성 또는 저산소성 질환에 걸린 조직에 관련된 질환의 치료를 위한 화합물, 조성물 및 방법 |
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| CN111094314B (zh) * | 2018-08-15 | 2022-08-12 | 江苏豪森药业集团有限公司 | 含有葡糖苷酸衍生物jak抑制剂的前药及其制备方法和应用 |
| EP3847158A1 (en) * | 2018-09-06 | 2021-07-14 | Arena Pharmaceuticals, Inc. | Compounds useful in the treatment of autoimmune and inflammatory disorders |
| CN109134564B (zh) * | 2018-09-21 | 2022-03-11 | 合肥锐思生物医药有限公司 | 乳果糖糖苷衍生物、其制备方法及其用途 |
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| PH12021551455A1 (en) * | 2018-12-19 | 2022-04-18 | Incyte Corp | Jak1 pathway inhibitors for the treatment of gastrointestinal disease |
| BR112021018168B1 (pt) | 2019-03-21 | 2023-11-28 | Onxeo | Composição farmacêutica, combinação e kit compreendendo uma molécula dbait e um inibidor de quinase para o tratamento de câncer |
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| MY209459A (en) | 2019-07-10 | 2025-07-09 | Cybrexa 3 Inc | Peptide conjugates of microtubule-targeting agents as therapeutics |
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