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HRP20211708T1 - Antagonisti lpa - Google Patents

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Publication number
HRP20211708T1
HRP20211708T1 HRP20211708TT HRP20211708T HRP20211708T1 HR P20211708 T1 HRP20211708 T1 HR P20211708T1 HR P20211708T T HRP20211708T T HR P20211708TT HR P20211708 T HRP20211708 T HR P20211708T HR P20211708 T1 HRP20211708 T1 HR P20211708T1
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Croatia
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independently selected
image
alkyl
pharmaceutical composition
oral pharmaceutical
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HRP20211708TT
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English (en)
Inventor
Peter Tai Wah Cheng
Robert F. Kaltenbach Iii
Jun Li
Jun Shi
Yan Shi
Shiwei Tao
Hao Zhang
Suresh Dhanusu
Kumaravel Selvakumar
Ramesh Babu Reddigunta
Steven J. Walker
Lawrence J. Kennedy
James R. Corte
Tianan Fang
Sutjano JUSUF
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Bristol-Myers Squibb Company
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Application filed by Bristol-Myers Squibb Company filed Critical Bristol-Myers Squibb Company
Publication of HRP20211708T1 publication Critical patent/HRP20211708T1/hr
Publication of HRP20211708T8 publication Critical patent/HRP20211708T8/hr

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    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/27—Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, meprobamate, carbachol, neostigmine
    • 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
    • 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
    • A61K31/4192—1,2,3-Triazoles
    • 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
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • A61P9/00—Drugs for disorders of the cardiovascular system
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C62/00—Compounds having carboxyl groups bound to carbon atoms of rings other than six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C62/08—Saturated compounds containing ether groups, groups, groups, or groups
    • C07C62/10—Saturated compounds containing ether groups, groups, groups, or groups with a six-membered ring
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • C07D249/06—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring atoms
    • C—CHEMISTRY; METALLURGY
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    • 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
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    • 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
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    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
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  • Gastroenterology & Hepatology (AREA)
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  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Dermatology (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)

Claims (14)

1. Oralna farmaceutska kompozicija koja sadrži spoj formule (III): [image] ili enantiomer, dijastereomer, stereoizomer, farmaceutski prihvatljivu sol istog, pri čemu R2 je nezavisno odabrano od CH3 i CD3; R13 je nezavisno odabrano od H i C1-4 alkila; R3 je nezavisno odabrano od H i C1-4 alkila; R4 je nezavisno odabrano od C1-6 alkila supstituiranog sa 1-3 R9, -(CR7R7)r-C3-6 cikloalkila supstituiranog sa 1-3 R8, i -(CR7R7)r-arila supstituiranog sa 1-3 R8; R5 je nezavisno odabrano od H, F, Cl, CN i C1-4 alkila; pod uvjetom da jedno od R5 je H; R6 je [image] R7 je nezavisno odabrano od H, C1-4 alkila, i C3-6 cikloalkila; ili R7 i R7, zajedno sa atomom ugljika za koji su oba vezana, formiraju C3-6 cikloalkilni prsten; R8 je nezavisno odabrano od H, C1-6 alkila supstituiranog sa 1-5 R9, C3-6 cikloalkila, F, Cl, Br, CN, =O, i COOH; R9 je nezavisno odabrano od H, F, Cl, NH2, OH, OC1-5alkila, C1-5alkila, C3-6 cikloalkila, i fenila pri čemu kada R9 je Cl, NH2 ili OH ono nije supstituirano na Ci alkila za koji je vezano; R10 je nezavisno odabrano od H, D, C1-4 alkila, i F; R11 je nezavisno odabrano od CN, -C(=O)R12, i tetrazolila; R12 je nezavisno odabrano od OH, OC1-4 alkila, NH2, i NHSO2C1-4alki; i r je nezavisno odabrano od nula, 1, 2, 3, i 4; i farmaceutski prihvatljiv nosač ili razblaživač.
2. Oralna farmaceutska kompozicija iz patentnog zahtjeva 1, pri čemu navedeni spoj ima formulu (IV): [image] ili enantiomer, dijastereomer, stereoizomer, farmaceutski prihvatljiva sol istog, pri čemu R2 je nezavisno odabrano od CH3 i CD3; R13 je nezavisno odabrano od H i C1-4 alkila; R3 je nezavisno odabrano od H i C1-4 alkila; R4 je nezavisno odabrano od C1-6 alkila, [image] [image] R5 je nezavisno odabrano od H, F, Cl, i C1-4 alkila; pod uvjetom da jedno od R5 je H; R7 je nezavisno odabrano od H, C1-4 alkila, i C3-6 cikloalkila; R8 je nezavisno odabrano od H, C1-6 alkila supstituiranog sa 1-5 R9, C3-6 cikloalkila, F, Cl, Br, CN, =O, i COOH; R9 je nezavisno odabrano od H, F, Cl, NH2, OH, OC1-5alkila, C1-5alkila, C3-6 cikloalkila, i fenila pri čemu kada R9 je Cl, NH2 ili OH ono nije supstituirano na Ci alkila za koji je vezano; R10 je nezavisno odabrano od H, D, C1-4 alkila, i F; R11 je nezavisno odabrano od CN, -C(=O)R12, i [image] i R12 je nezavisno odabrano od OH i NHSO2C1-4alki.
3. Oralna farmaceutska kompozicija iz patentnog zahtjeva 3, pri čemu R4 je nezavisno odabrano od [image] [image] [image] [image] [image] i R8 je nezavisno odabrano od H, F, Cl, Br, CN, i C1-4 alkila.
4. Oralna farmaceutska kompozicija iz patentnog zahtjeva 3, pri čemu navedeni spoj ima formulu (V): [image] ili enantiomer, dijastereomer, stereoizomer, farmaceutski prihvatljiva sol istog, pri čemu R2 je nezavisno odabrano od CH3 i CD3; R13 je nezavisno odabrano od H i CH3; R3 je nezavisno odabrano od H i CH3; R4 je nezavisno odabrano od [image] [image] [image] [image] [image] i R5 je nezavisno odabrano od H, F, i C1-4 alkila; R8 je nezavisno odabrano od H, F, Cl, Br, CN, i C1-4 alkila; R10 je nezavisno odabrano od H, D, i F; i R11 je nezavisno odabrano od -C(=O)OH, i -C(=O)NHSO2Me.
5. Oralna farmaceutska kompozicija iz patentnog zahtjeva 3, pri čemu navedeni spoj ima formulu (VI): [image] ili enantiomer, dijastereomer, stereoizomer, farmaceutski prihvatljiva sol istog, pri čemu R2 je nezavisno odabrano od CH3 i CD3; R13 je nezavisno odabrano od H i CH3; R3 je nezavisno odabrano od H i CH3; R4 je nezavisno odabrano od [image] [image] [image] R5 je nezavisno odabrano od H i CH3; i R8 je nezavisno odabrano od H, F, Cl, Br, CN, i C1-4 alkila.
6. Oralna farmaceutska kompozicija iz bilo kojeg od patentnih zahtjeva 1-4, pri čemu navedeni spoj ima formulu: [image] enantiomer, dijastereomer, stereoizomer, ili farmaceutski prihvatljiva sol istog.
7. Oralna farmaceutska kompozicija iz bilo kojeg od patentnih zahtjeva 1-4, pri čemu navedeni spoj ima formulu: [image] enantiomer, dijastereomer, stereoizomer, ili farmaceutski prihvatljiva sol istog.
8. Oralna farmaceutska kompozicija iz bilo kojeg od patentnih zahtjeva 1-4, pri čemu navedeni spoj ima formulu: [image] enantiomer, dijastereomer, stereoizomer, ili farmaceutski prihvatljiva sol istog.
9. Oralna farmaceutska kompozicija iz bilo kojeg od patentnih zahtjeva 1-4, pri čemu navedeni spoj ima formulu: [image] enantiomer, dijastereomer, stereoizomer, ili farmaceutski prihvatljiva sol istog.
10. Oralna farmaceutska kompozicija iz bilo kojeg od patentnih zahtjeva 1-4, pri čemu navedeni spoj ima formulu: [image] enantiomer, dijastereomer, stereoizomer, ili farmaceutski prihvatljiva sol istog.
11. Oralna farmaceutska kompozicija prema bilo kojem od patentnih zahtjeva 1-10 za primjenu u terapiji.
12. Oralna farmaceutska kompozicija prema bilo kojem od patentnih zahtjeva 1-10 za primjenu u liječenju ili prevenciji fibroze organa kod sisavca koji ima potrebu za istim.
13. Oralna farmaceutska kompozicija prema bilo kojem od patentnih zahtjeva 1-10 za primjenu u liječenju fibroze pluća (idiopatske fibroze pluća), astme, kronične opstruktivne bolesti pluća (HOBP), renalne fibroze, akutne povrede bubrega, kronične bubrežne bolesti, fibroze jetre (nealkoholnog steatohepatitisa), fibroze kože, fibroze crijeva, raka dojke, raka gušterače, raka jajnika, raka prostate, glioblastoma, raka kostiju, raka debelog crijeva, raka mokraćnog mjehura, raka glave i vrata, melanoma, multiplog mijeloma, kronične limfocitne leukemije, kancerogene boli, metastaze tumora, odbacivanja transplantiranih organa, skleroderme, okularne fibroze, degeneracije makule povezane sa starošću (AMD), dijabetičke retinopatije, kolagene vaskularne bolesti, ateroskleroze, Rejnoovog fenomena (Raynaud’s phenomenon) ili neuropatske boli kod sisavaca koji imaju potrebu za tim.
14. Oralna farmaceutska kompozicija prema bilo kojem od patentnih zahtjeva 1-10 za primjenu u liječenju idiopatske plućne fibroze.
HRP20211708TT 2016-06-21 2017-06-20 Antagonisti lpa HRP20211708T8 (hr)

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Application Number Priority Date Filing Date Title
US201662352792P 2016-06-21 2016-06-21
EP20154651.2A EP3666771B1 (en) 2016-06-21 2017-06-20 Lpa antagonists

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HRP20211708T1 true HRP20211708T1 (hr) 2022-02-04
HRP20211708T8 HRP20211708T8 (hr) 2022-03-04

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HRP20211708TT HRP20211708T8 (hr) 2016-06-21 2017-06-20 Antagonisti lpa
HRP20200586TT HRP20200586T1 (hr) 2016-06-21 2020-04-13 Karbamoiloksimetil triazol cikloheksilne kiseline kao antagonisti lpa

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US (8) US10071078B2 (hr)
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JP (2) JP7073281B2 (hr)
KR (2) KR102463621B1 (hr)
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AR (1) AR108838A1 (hr)
AU (2) AU2017281439B2 (hr)
BR (1) BR112018076558A2 (hr)
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EA (1) EA037585B1 (hr)
ES (2) ES2895385T3 (hr)
HR (2) HRP20211708T8 (hr)
HU (2) HUE049944T2 (hr)
IL (1) IL263767B (hr)
LT (2) LT3666771T (hr)
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MY (1) MY195782A (hr)
PE (1) PE20190211A1 (hr)
PL (2) PL3472148T3 (hr)
PT (2) PT3666771T (hr)
RS (2) RS60347B1 (hr)
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SI (2) SI3472148T1 (hr)
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TW (2) TWI757128B (hr)
UY (1) UY37302A (hr)
WO (1) WO2017223016A1 (hr)
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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR108838A1 (es) 2016-06-21 2018-10-03 Bristol Myers Squibb Co Ácidos de carbamoiloximetil triazol ciclohexilo como antagonistas de lpa
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