AR103170A1 - Compuestos y composiciones farmacéuticas de los mismos para el tratamiento de desordenes inflamatorios y osteoartritis - Google Patents
Compuestos y composiciones farmacéuticas de los mismos para el tratamiento de desordenes inflamatorios y osteoartritisInfo
- Publication number
- AR103170A1 AR103170A1 ARP150104189A ARP150104189A AR103170A1 AR 103170 A1 AR103170 A1 AR 103170A1 AR P150104189 A ARP150104189 A AR P150104189A AR P150104189 A ARP150104189 A AR P150104189A AR 103170 A1 AR103170 A1 AR 103170A1
- Authority
- AR
- Argentina
- Prior art keywords
- independently selected
- optionally substituted
- alkyl
- alkoxy
- halo
- Prior art date
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Classifications
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- 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
- C07D403/06—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 only aliphatic carbon atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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
- C07D233/72—Two oxygen atoms, e.g. hydantoin
- C07D233/76—Two oxygen atoms, e.g. hydantoin with substituted hydrocarbon radicals attached to the third ring carbon atom
- C07D233/78—Radicals substituted by oxygen atoms
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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
- A61K31/495—Heterocyclic 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
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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
- A61K31/535—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
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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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- 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
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- 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
- A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
-
- 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
- C07D401/04—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
-
- 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
- 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
- C07D401/14—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
-
- 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
- C07D403/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom 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
- C07D417/12—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
Abstract
Reivindicación 1: Un compuesto de acuerdo con la fórmula (1), donde: R¹ es: H, C₁₋₄ alquilo, opcionalmente sustituido con uno o más de los grupos R⁴ independientemente seleccionados; C₃₋₇ cicloalquilo monocíclico opcionalmente sustituido con grupos R⁴, independientemente seleccionados; heterocicloalquilo monocíclico de 4 - 7 miembros, que comprende de 1 a 2 heteroátomos, independientemente seleccionados de N, O, y S, opcionalmente sustituido con uno o más, C₁₋₄ alquilo, -C(=O)C₁₋₄, alquilo, o -C(=O)OC₁₋₄ alquilo, independientemente seleccionados; fenilo, opcionalmente sustituido con uno o más grupos R⁵ independientemente seleccionados; fenilo fusionado a heterocicloalquilo monocíclico de 5 - 6 miembros, comprendiendo 1, 2 ó 3 heteroátomos independientemente seleccionados de N, O, y S, cuyo heterocicloalquilo es opcionalmente sustituido con uno o más =O heteroarilo monocíclico de 5 - 6 miembros, que comprende de 1 a 2 heteroátomos, independientemente seleccionados de N, O, y S, opcionalmente sustituido con uno o más grupos R⁵ independientemente seleccionados; R² es independientemente seleccionado de: H, OH, C₁₋₄ alcoxi, y C₁₋₄ alquilo opcionalmente sustituido con uno de: OH, CN, C₁₋₄ alcoxi opcionalmente sustituido con un fenilo, o heteroarilo monocíclico de 5 - 6 miembros que comprende 1 ó 2 heteroátomos independientemente seleccionados de N, O, y S, opcionalmente sustituidos con uno o más C₁₋₄ alquilo independientemente seleccionados; cada R³ᵃ, y R³ᵇ es independientemente seleccionado de: H, y C₁₋₄ alquilo; o bien Cy es: un arilo monocíclico o bicíclico fusionado de 6 - 10 miembros, opcionalmente sustituido con uno o más grupos R⁶ independientemente seleccionados; un heteroarilo monocíclico o bicíclico fusionado de 5 - 10 miembros, que comprende 1, 2 ó 3 heteroátomos independientemente seleccionados de N, O y S, opcionalmente sustituidos con uno o más grupos R⁶, independientemente sustituidos; R⁴ es halo, OH, -CN, C₁₋₄ alquilo, C₁₋₄ alcoxi opcionalmente sustituido con C₁₋₄ alcoxi, o fenilo, C₁₋₄ tioalcoxi, heterocicloalquilo monocíclico de 4 - 7 miembros que comprende uno o más heteroátomos independientemente seleccionados de N, S, y O, opcionalmente sustituidos con uno o más de halo o -C(=O)OC₁₋₄ alquilo; fenilo, -S(=O)₂C₁₋₄ alquilo, -C(=O)OR⁷ᵃ, -C(=O)NR⁷ᵇR⁷ᶜ, NHC(=O)OR⁷ᵈ, -NHC(=O)R⁷ᵉ, -NR⁸ᵃR⁸ᵇ; cada R⁵ es halo, OH, -CN, C₁₋₄ alquilo opcionalmente sustituido con uno o más de: halo, -NR⁹ᵃR⁹ᵇ, o -C(=O)NR⁹ᶜR⁹ᵈ, independientemente sustituidos; C₁₋₄ alcoxi opcionalmente sustituido con -NR⁹ᵉR⁹ᶠ, o bien -S(=O)₂C₁₋₄ alquilo; cada R⁶ es halo, -CN, -NO₂, -CH₃, heteroarilo monocíclico o bicíclico fusionado de 5 - 10 miembros que comprende 1, 2 ó 3 heteroátomos independientemente seleccionados de N, O y S, opcionalmente sustituidos con uno o más de: halo, C₁₋₄ alquilo, C₁₋₄ alcoxi, independientemente seleccionados; -NR⁹ᵍR⁹ʰ; cada uno de R⁷ᵃ, R⁷ᵇ, R⁷ᶜ, R⁷ᵈ, o R⁷ᵉ, es: H, o bien C₁₋₄ alquilo opcionalmente sustituido con OH, C₁₋₄ alcoxi; cada uno de R⁸ᵃ, o R⁸ᵇ es independientemente seleccionado de: H, y C₁₋₄ alquilo opcionalmente sustituido con OH, C₁₋₄ alcoxi, o fenilo; cada uno de: R⁹ᵃ, R⁹ᵇ, R⁹ᶜ, R⁹ᵈ, R⁹ᵉ, R⁹ᶠ, R⁹ᵍ, y R⁹ʰ independientemente seleccionado de H, y C₁₋₄ alquilo; o una sal farmacéuticamente aceptable o un solvato o un metabolito biológicamente activo del mismo; siempre que: R¹, y R² no sean simultáneamente H; y cuando R¹ sea Me, y R² sea H, entonces Cy no sea: un resto de fórmula (2), o una sal farmacéuticamente aceptable o un solvato o la sal del solvato del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14307129 | 2014-12-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR103170A1 true AR103170A1 (es) | 2017-04-19 |
Family
ID=52345014
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP150104189A AR103170A1 (es) | 2014-12-22 | 2015-12-18 | Compuestos y composiciones farmacéuticas de los mismos para el tratamiento de desordenes inflamatorios y osteoartritis |
Country Status (50)
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JO3501B1 (ar) | 2014-12-22 | 2020-07-05 | Servier Lab | مشتقات 5-{(بيبرازين - 1-يل)-3-أوكسو - بروبيل}- إيميدازوليدين-2، 4 - دايون كمثبطات ل adamts لمعالجة هشاشة العظام) |
| GB201610056D0 (en) * | 2016-06-09 | 2016-07-27 | Galapagos Nv And Laboratoires Servier Les | Novel compounds and pharmaceutical compositions thereof for the treatment of inflammatory disorders and osteoarthritis |
| GB201610055D0 (en) | 2016-06-09 | 2016-07-27 | Galapagos Nv And Laboratoires Servier Les | Novel compounds and pharmaceutical compositions thereof for the treatment of inflammatory disorders and osteoarthritis |
| CN107540648A (zh) * | 2017-08-09 | 2018-01-05 | 江苏工程职业技术学院 | 一种达格列净的制备方法 |
| CN107652277A (zh) * | 2017-08-09 | 2018-02-02 | 江苏工程职业技术学院 | 一种依帕列净的制备方法 |
| WO2021011723A1 (en) * | 2019-07-18 | 2021-01-21 | Avidence Therapeutics, Inc. | Anti-osteoarthritis hydantoin compounds and related compositions and methods |
| KR20220137657A (ko) * | 2020-02-04 | 2022-10-12 | 지앙수 헨그루이 파마슈티컬스 컴퍼니 리미티드 | Adamts 억제제, 이의 제조 방법 및 의약적 용도 |
| WO2021204185A1 (zh) * | 2020-04-10 | 2021-10-14 | 深圳信立泰药业股份有限公司 | 一种苯并[d]氮杂卓类衍生物蛋白聚糖酶2抑制剂及其制备方法和医药用途 |
| CN113735825A (zh) * | 2020-05-27 | 2021-12-03 | 成都康弘药业集团股份有限公司 | 1,2,3,6-四氢吡啶类化合物及其制备方法和用途 |
| CN113754635A (zh) * | 2020-06-02 | 2021-12-07 | 成都康弘药业集团股份有限公司 | 稠环类化合物及其制备方法和用途 |
| CN115720578A (zh) * | 2020-07-09 | 2023-02-28 | 深圳信立泰药业股份有限公司 | 并三环类衍生物、其制备方法及其在医药上的应用 |
| JP2023552908A (ja) | 2020-12-15 | 2023-12-19 | ガラパゴス・ナムローゼ・フェンノートシャップ | （５ｓ）－シクロプロピル－５－［３－［（３ｓ）－４－（３，５－ジフルオロフェニル）－３－メチル－ピペラジン－１－イル］－３－オキソ－プロピル］イミダゾリジン－２，４－ジオンの固体形態 |
| TW202304886A (zh) * | 2021-04-02 | 2023-02-01 | 中國大陸商江蘇恒瑞醫藥股份有限公司 | Adamts抑制劑的前藥及其製備方法與醫藥用途 |
| WO2023011547A1 (zh) * | 2021-08-03 | 2023-02-09 | 江苏恒瑞医药股份有限公司 | 抑制adamts-5和/或adamts-4功能的化合物的晶型及其制备方法和应用 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4556670A (en) * | 1982-12-06 | 1985-12-03 | Pfizer Inc. | Spiro-3-hetero-azolones for treatment of diabetic complications |
| US4680306A (en) * | 1984-07-20 | 1987-07-14 | Pfizer Inc. | Sprio-imidazolones for treatment of diabetes complications |
| US5043447A (en) * | 1987-04-24 | 1991-08-27 | Syntex Pharmaceuticals, Ltd. | Substituted imidazolyl-alkyl-piperazine and -diazepine derivatives |
| SE0100902D0 (sv) | 2001-03-15 | 2001-03-15 | Astrazeneca Ab | Compounds |
| US6890915B2 (en) | 2001-05-25 | 2005-05-10 | Bristol-Myers Squibb Pharma Company | Hydantoins and related heterocycles as inhibitors of matrix metalloproteinases and/or TNF-α converting enzyme (TACE) |
| GB0405101D0 (en) | 2004-03-06 | 2004-04-07 | Astrazeneca Ab | Compounds |
| US7504424B2 (en) | 2004-07-16 | 2009-03-17 | Schering Corporation | Compounds for the treatment of inflammatory disorders |
| PT2650310T (pt) | 2012-04-13 | 2016-09-01 | Rottapharm Biotech Srl | Anticorpo anti-adamts-5, derivados e utilizações dos mesmos |
| AR092971A1 (es) * | 2012-10-26 | 2015-05-06 | Lilly Co Eli | Inhibidores de agrecanasa |
| CN104955806B (zh) | 2013-02-06 | 2018-09-14 | 默克专利股份公司 | 用于治疗骨关节炎的作为聚蛋白聚糖酶抑制剂的取代羧酸衍生物 |
| JO3501B1 (ar) | 2014-12-22 | 2020-07-05 | Servier Lab | مشتقات 5-{(بيبرازين - 1-يل)-3-أوكسو - بروبيل}- إيميدازوليدين-2، 4 - دايون كمثبطات ل adamts لمعالجة هشاشة العظام) |
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2015
- 2015-11-19 JO JOP/2015/0284A patent/JO3501B1/ar active
- 2015-12-14 TW TW104141953A patent/TWI687414B/zh active
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- 2015-12-18 PE PE2017001122A patent/PE20171099A1/es unknown
- 2015-12-18 UA UAA201707702A patent/UA122065C2/uk unknown
- 2015-12-18 PT PT15813831T patent/PT3237406T/pt unknown
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- 2015-12-22 UY UY0001036470A patent/UY36470A/es not_active Application Discontinuation
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2017
- 2017-05-24 GT GT201700107A patent/GT201700107A/es unknown
- 2017-06-07 ZA ZA2017/03905A patent/ZA201703905B/en unknown
- 2017-06-14 DO DO2017000139A patent/DOP2017000139A/es unknown
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- 2017-06-20 PH PH12017501160A patent/PH12017501160A1/en unknown
- 2017-06-21 CO CONC2017/0006174A patent/CO2017006174A2/es unknown
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- 2017-06-21 NI NI201700081A patent/NI201700081A/es unknown
- 2017-07-20 EC ECIEPI201746848A patent/ECSP17046848A/es unknown
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2018
- 2018-02-14 US US15/896,779 patent/US10487060B2/en active Active
- 2018-04-26 HK HK18105455.7A patent/HK1245793B/zh unknown
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2019
- 2019-03-15 HR HRP20190514TT patent/HRP20190514T1/hr unknown
- 2019-05-02 CY CY20191100464T patent/CY1121692T1/el unknown
- 2019-10-15 US US16/653,668 patent/US10941117B2/en active Active
- 2019-12-18 JP JP2019227801A patent/JP2020063278A/ja active Pending
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2021
- 2021-01-05 US US17/141,902 patent/US11718588B2/en active Active
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