AR109086A1 - Derivado de piperazina - Google Patents
Derivado de piperazinaInfo
- Publication number
- AR109086A1 AR109086A1 ARP170101999A ARP170101999A AR109086A1 AR 109086 A1 AR109086 A1 AR 109086A1 AR P170101999 A ARP170101999 A AR P170101999A AR P170101999 A ARP170101999 A AR P170101999A AR 109086 A1 AR109086 A1 AR 109086A1
- Authority
- AR
- Argentina
- Prior art keywords
- substituted
- alkyl
- bladder
- receptor
- cycloalkyl
- Prior art date
Links
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical class C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 6
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 102000008316 Type 4 Melanocortin Receptor Human genes 0.000 abstract 2
- 108010021436 Type 4 Melanocortin Receptor Proteins 0.000 abstract 2
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 150000004885 piperazines Chemical class 0.000 abstract 2
- 239000000018 receptor agonist Substances 0.000 abstract 2
- 229940044601 receptor agonist Drugs 0.000 abstract 2
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 abstract 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 206010058914 Hypotonic urinary bladder Diseases 0.000 abstract 1
- 208000000693 Neurogenic Urinary Bladder Diseases 0.000 abstract 1
- 206010029279 Neurogenic bladder Diseases 0.000 abstract 1
- 208000004403 Prostatic Hyperplasia Diseases 0.000 abstract 1
- 208000004168 Underactive Urinary Bladder Diseases 0.000 abstract 1
- 239000000556 agonist Substances 0.000 abstract 1
- 150000001721 carbon Chemical group 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000004064 dysfunction Effects 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000001183 hydrocarbyl group Chemical group 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 102000005962 receptors Human genes 0.000 abstract 1
- 108020003175 receptors Proteins 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229930195734 saturated hydrocarbon Natural products 0.000 abstract 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 abstract 1
- 210000001635 urinary tract Anatomy 0.000 abstract 1
Classifications
-
- 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
- C07D405/14—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 three or more 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
- A61K31/33—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 or sparfloxacin
-
- 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
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
-
- 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
- A61P13/10—Drugs for disorders of the urinary system of the bladder
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
- C07D207/12—Oxygen or sulfur atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
- C07D307/04—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
- C07D307/18—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no 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
- C07D307/20—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
- C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
- C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no 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
- C07D309/14—Nitrogen atoms not forming part of a nitro radical
-
- 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
- C07D403/02—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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Urology & Nephrology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
En la presente se estudiaron los agonistas del receptor MC₄, y se ha descubierto que un derivado de piperazina tiene una acción agonista del receptor MC₄, con lo cual se completa la presente solicitud. El derivado de piperazina de la presente tiene una acción agonista del receptor MC₄ y puede usarse como agente para prevenir o tratar enfermedades de vejiga y/o tracto urinario, en particular, vejiga hipoactiva, vejiga hipotónica, vejiga acontráctil, subactividad del detrusor, vejiga neurogénica, falla de la relajación uretral, disinergia de detrusor-esfínter uretral externo y disfunciones de vaciado en la hiperplasia prostática benigna. Reivindicación 1: Un compuesto de fórmula (1) o una sal de dicho compuesto, (en donde, el anillo A representa un compuesto de fórmula (2); R¹ representa alquilo C₁₋₆ que puede estar sustituido, cicloalquilo C₃₋₈ que puede estar sustituido o un heteroanillo saturado que puede estar sustituido; R²ᵃ y R²ᵇ son iguales o diferentes entre sí, y cada uno representa H o alquilo C₁₋₆ que puede estar sustituido, R²ᵃ y R²ᵇ no representan simultáneamente H, en caso de que R²ᵃ y R²ᵇ estén unidos al mismo carbono, R²ᵃ, R²ᵇ y el átomo de carbono al cual están unidos pueden formar juntos un anillo hidrocarburo saturado; R³ representa alquilo C₁₋₆ que puede estar sustituido, cicloalquilo C₃₋₈ que puede estar sustituido o fenilo que puede estar sustituido; R⁴ᵃ representa H, alquilo C₁₋₆, -C(O)R⁹ o -S(O)₂R⁹; R⁴ᵇ representa H o alquilo C₁₋₆; X representa CR⁸ o N; R⁵, R⁶, R⁷, y R⁸ son iguales o diferentes entre sí, y cada uno representa H o halógeno; R⁹ representa alquilo C₁₋₆ que puede estar sustituido o cicloalquilo C₃₋₈ que puede estar sustituido; y n representa 0 ó 1).
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2016141542 | 2016-07-19 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR109086A1 true AR109086A1 (es) | 2018-10-24 |
Family
ID=60992481
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP170101999A AR109086A1 (es) | 2016-07-19 | 2017-07-18 | Derivado de piperazina |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US10710988B2 (es) |
| EP (1) | EP3489231B1 (es) |
| JP (1) | JP6908041B2 (es) |
| CN (1) | CN109563074B (es) |
| AR (1) | AR109086A1 (es) |
| ES (1) | ES2880174T3 (es) |
| PL (1) | PL3489231T3 (es) |
| PT (1) | PT3489231T (es) |
| TW (1) | TW201811769A (es) |
| WO (1) | WO2018016458A1 (es) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113929598A (zh) * | 2021-11-24 | 2022-01-14 | 上海吉奉生物科技有限公司 | 一种（s）-2-叔丁氧羰基氨基-3-（4,4-二氟环己基）丙酸的合成方法 |
| CN114478346A (zh) * | 2021-12-31 | 2022-05-13 | 和鼎（南京）医药技术有限公司 | 一种制备乌帕替尼中间体的方法 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7115607B2 (en) * | 2001-07-25 | 2006-10-03 | Amgen Inc. | Substituted piperazinyl amides and methods of use |
| ATE342057T1 (de) * | 2002-01-23 | 2006-11-15 | Lilly Co Eli | Melanocortinrezeptoragonisten |
| WO2004078716A1 (en) | 2003-03-03 | 2004-09-16 | Merck & Co. Inc. | Acylated piperazine derivatives as melanocortin-4 receptor agonists |
| WO2005040109A1 (en) * | 2003-10-22 | 2005-05-06 | Neurocrine Biosciences, Inc. | Ligands of melanocortin receptors and compositions and methods related thereto |
| CN1988906A (zh) | 2004-07-19 | 2007-06-27 | 默克公司 | 用作黑皮质素－4受体激动剂的酰基化哌啶衍生物 |
| EP1928460A2 (en) * | 2005-08-01 | 2008-06-11 | Pfizer Limited | Mc4r-agonists for the treatment of urinary tract dysfunction |
| RU2731913C2 (ru) | 2015-08-04 | 2020-09-09 | Астеллас Фарма Инк. | Пиперазиновое производное |
-
2017
- 2017-07-18 US US16/314,730 patent/US10710988B2/en active Active
- 2017-07-18 JP JP2018528537A patent/JP6908041B2/ja active Active
- 2017-07-18 WO PCT/JP2017/025842 patent/WO2018016458A1/ja unknown
- 2017-07-18 PL PL17830975T patent/PL3489231T3/pl unknown
- 2017-07-18 AR ARP170101999A patent/AR109086A1/es unknown
- 2017-07-18 CN CN201780044430.5A patent/CN109563074B/zh active Active
- 2017-07-18 EP EP17830975.3A patent/EP3489231B1/en active Active
- 2017-07-18 ES ES17830975T patent/ES2880174T3/es active Active
- 2017-07-18 TW TW106123979A patent/TW201811769A/zh unknown
- 2017-07-18 PT PT178309753T patent/PT3489231T/pt unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP3489231A4 (en) | 2020-03-04 |
| ES2880174T3 (es) | 2021-11-23 |
| CN109563074B (zh) | 2021-09-28 |
| PL3489231T3 (pl) | 2021-10-25 |
| TW201811769A (zh) | 2018-04-01 |
| WO2018016458A1 (ja) | 2018-01-25 |
| PT3489231T (pt) | 2021-07-14 |
| EP3489231B1 (en) | 2021-06-09 |
| JPWO2018016458A1 (ja) | 2019-05-09 |
| US10710988B2 (en) | 2020-07-14 |
| CN109563074A (zh) | 2019-04-02 |
| EP3489231A1 (en) | 2019-05-29 |
| US20190202815A1 (en) | 2019-07-04 |
| JP6908041B2 (ja) | 2021-07-21 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |