EA200601378A1 - Гидроизоиндолиновые антагонисты рецептора тахикинина - Google Patents
Гидроизоиндолиновые антагонисты рецептора тахикининаInfo
- Publication number
- EA200601378A1 EA200601378A1 EA200601378A EA200601378A EA200601378A1 EA 200601378 A1 EA200601378 A1 EA 200601378A1 EA 200601378 A EA200601378 A EA 200601378A EA 200601378 A EA200601378 A EA 200601378A EA 200601378 A1 EA200601378 A1 EA 200601378A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- antagonists
- receptor
- takhikinin
- isoindoline
- hydro
- Prior art date
Links
- 239000005557 antagonist Substances 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 3
- 102000002002 Neurokinin-1 Receptors Human genes 0.000 abstract 2
- 108010040718 Neurokinin-1 Receptors Proteins 0.000 abstract 2
- QDZOEBFLNHCSSF-PFFBOGFISA-N (2S)-2-[[(2R)-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-1-[(2R)-2-amino-5-carbamimidamidopentanoyl]pyrrolidine-2-carbonyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-N-[(2R)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]pentanediamide Chemical compound C([C@@H](C(=O)N[C@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)NC(=O)[C@@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CCCCN)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](N)CCCNC(N)=N)C1=CC=CC=C1 QDZOEBFLNHCSSF-PFFBOGFISA-N 0.000 abstract 1
- 208000019901 Anxiety disease Diseases 0.000 abstract 1
- 102100024304 Protachykinin-1 Human genes 0.000 abstract 1
- 101800003906 Substance P Proteins 0.000 abstract 1
- 102000003141 Tachykinin Human genes 0.000 abstract 1
- 206010046543 Urinary incontinence Diseases 0.000 abstract 1
- 206010047700 Vomiting Diseases 0.000 abstract 1
- 239000004480 active ingredient Substances 0.000 abstract 1
- 230000036506 anxiety Effects 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 108060008037 tachykinin Proteins 0.000 abstract 1
- 230000008673 vomiting Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/44—Iso-indoles; Hydrogenated iso-indoles
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/4035—Isoindoles, e.g. phthalimide
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
- A61K31/405—Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
-
- 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
- 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
- A61P13/00—Drugs for disorders of the urinary system
-
- 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
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- A61P25/22—Anxiolytics
-
- 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
- A61P25/24—Antidepressants
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Urology & Nephrology (AREA)
- Pain & Pain Management (AREA)
- Pulmonology (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Indole Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Настоящее изобретение направлено на определенные гидроизоиндолиновые соединения формулы 1, которые полезны в качестве антагонистов рецептора нейрокинина-1 (NK-1) и ингибиторов тахикинина и, в частности, вещества Р. Изобретение также имеет отношение к фармацевтическим препаратам, содержащим данные соединения в качестве активных ингредиентов, и к применению данных соединений и их препаратов для лечения определенных нарушений, включая рвоту, недержание мочи, депрессию и тревогу.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US53991304P | 2004-01-27 | 2004-01-27 | |
| US56122704P | 2004-04-09 | 2004-04-09 | |
| PCT/US2005/002149 WO2005073191A1 (en) | 2004-01-27 | 2005-01-26 | Hydroisoindoline tachykinin receptor antagonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA200601378A1 true EA200601378A1 (ru) | 2007-02-27 |
| EA010598B1 EA010598B1 (ru) | 2008-10-30 |
Family
ID=34830494
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA200601378A EA010598B1 (ru) | 2004-01-27 | 2005-01-26 | Гидроизоиндолиновые антагонисты рецептора тахикинина |
Country Status (30)
| Country | Link |
|---|---|
| US (3) | US7645790B2 (ru) |
| EP (1) | EP1711465B1 (ru) |
| JP (1) | JP3987100B2 (ru) |
| KR (1) | KR20060127927A (ru) |
| AR (1) | AR047439A1 (ru) |
| AT (1) | ATE382034T1 (ru) |
| AU (1) | AU2005207934B2 (ru) |
| BR (1) | BRPI0507050A (ru) |
| CA (1) | CA2554550C (ru) |
| CO (1) | CO5700771A2 (ru) |
| CR (1) | CR8522A (ru) |
| CY (1) | CY1107167T1 (ru) |
| DE (1) | DE602005004011T2 (ru) |
| DK (1) | DK1711465T3 (ru) |
| EA (1) | EA010598B1 (ru) |
| EC (1) | ECSP066716A (ru) |
| ES (1) | ES2297687T3 (ru) |
| GE (1) | GEP20094691B (ru) |
| HR (1) | HRP20080100T3 (ru) |
| IL (1) | IL176879A0 (ru) |
| MA (1) | MA28359A1 (ru) |
| NI (1) | NI200600164A (ru) |
| NO (1) | NO339041B1 (ru) |
| NZ (1) | NZ548415A (ru) |
| PE (1) | PE20050687A1 (ru) |
| PL (1) | PL1711465T3 (ru) |
| PT (1) | PT1711465E (ru) |
| TW (1) | TWI341198B (ru) |
| UA (1) | UA84192C2 (ru) |
| WO (1) | WO2005073191A1 (ru) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR047439A1 (es) | 2004-01-27 | 2006-01-18 | Merck & Co Inc | Antagonistas del receptor hidroisoindolina taquiquinina |
| EP1827420A4 (en) * | 2004-12-14 | 2009-03-04 | Merck & Co Inc | OCTAHYDROPYRANO [3,4-c] pyrrole tachykinin receptor Antagonist |
| WO2007002457A2 (en) * | 2005-06-27 | 2007-01-04 | Merck & Co., Inc. | Hydroisoindoline tachykinin receptor antagonists |
| AU2006269383A1 (en) | 2005-07-11 | 2007-01-18 | Merck Sharp & Dohme Corp. | Process for making hydroisoindoline tachykinin receptor antagonists |
| CA2624440A1 (en) | 2005-10-04 | 2007-04-19 | Merck & Co., Inc. | Combination therapy for the treatment of urinary frequency, urinary urgency and urinary incontinence |
| WO2007075528A2 (en) * | 2005-12-22 | 2007-07-05 | Merck & Co., Inc. | Octahydropyrano[3,4-c]pyrrole tachykinin receptor antagonists |
| EP1978965A2 (en) * | 2006-01-24 | 2008-10-15 | Merck & Co., Inc. | Hexahydro-3h-pyrrolizin-3-ones useful as tachykinin receptor antagonists |
| US20100209496A1 (en) * | 2006-09-06 | 2010-08-19 | Eleni Dokou | Liquid and semi-solid pharmaceutical formulations for oral administration of a substituted amide |
| US20090270477A1 (en) * | 2006-11-02 | 2009-10-29 | Kuethe Jeffrey T | Polymorphs of a hydroisoindoline tachykinin receptor antagonist |
| WO2008121268A1 (en) * | 2007-03-29 | 2008-10-09 | Merck & Co., Inc. | Combination therapy for the treatment-of lower urinary tract symptoms |
| US8124633B2 (en) | 2007-04-10 | 2012-02-28 | Merck Sharp & Dohme Corp. | Hydroxymethyl ether hydroisoindoline tachykinin receptor antagonists |
| JP5812500B2 (ja) | 2010-04-30 | 2015-11-17 | メルク・シャープ・エンド・ドーム・コーポレイション | 新規なβ３アドレナリン作動性受容体アゴニスト |
| US8627816B2 (en) | 2011-02-28 | 2014-01-14 | Intelliject, Inc. | Medicament delivery device for administration of opioid antagonists including formulations for naloxone |
| WO2013004766A1 (en) | 2011-07-04 | 2013-01-10 | Ferrari Giulio | Nk-1 receptor antagonists for treating corneal neovascularisation |
| US9198898B2 (en) | 2013-06-24 | 2015-12-01 | Tigercat Pharma, Inc. | Use of NK-1 receptor antagonists in pruritus |
| WO2014209962A1 (en) | 2013-06-24 | 2014-12-31 | Tigercat Pharma, Inc. | Use of nk-1 receptor antagonist serlopitant in pruritus |
| US8906951B1 (en) | 2013-06-24 | 2014-12-09 | Tigercat Pharma, Inc. | Use of NK-1 receptor antagonists in pruritus |
| IL312486B2 (en) | 2017-04-10 | 2025-05-01 | Chase Therapeutics Corp | NK1 antagonist combination and method for treating synucleinopathies |
| KR20250069704A (ko) | 2017-06-30 | 2025-05-19 | 체이스 테라퓨틱스 코포레이션 | 우울증을 치료하기 위한 nk-1 길항제 조성물 및 우울증 치료에 사용하는 방법 |
| CA3091944A1 (en) | 2018-02-26 | 2019-08-29 | Ospedale San Raffaele S.R.L. | Nk-1 antagonists for use in the treatment of ocular pain |
| WO2021180885A1 (en) | 2020-03-11 | 2021-09-16 | Ospedale San Raffaele S.R.L. | Treatment of stem cell deficiency |
| AU2021246889A1 (en) | 2020-04-03 | 2022-10-13 | Nerre Therapeutics Limited | An NK-1 receptor antagonist for treating a disease selecting from sepsis, septic shock,, acute respiratory distress syndrome (ARDS) or multiple organ dysfunction syndrome (MODS) |
| MX2022014901A (es) | 2020-06-02 | 2023-01-18 | Nerre Therapeutics Ltd | Antagonistas del receptor de neuroquinina (nk)-1 para su uso en el tratamiento de condiciones de fibrosis pulmonar promovidas por lesion mecanica a los pulmones. |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5650142A (en) * | 1995-09-27 | 1997-07-22 | Church & Dwight Co., Inc. | Bicarbonate-containing deodorant cosmetic stick compositions |
| EP0858444A4 (en) * | 1995-10-18 | 1999-12-01 | Merck & Co Inc | Cyclopentyl tachykinin receptor antagonists |
| EP1670476A4 (en) | 2003-09-30 | 2009-05-27 | Merck & Co Inc | Phenylpyrrolidine-ETHER-tachykinin receptor Antagonist |
| AR047439A1 (es) | 2004-01-27 | 2006-01-18 | Merck & Co Inc | Antagonistas del receptor hidroisoindolina taquiquinina |
-
2005
- 2005-01-20 AR ARP050100203A patent/AR047439A1/es active IP Right Grant
- 2005-01-20 TW TW094101721A patent/TWI341198B/zh not_active IP Right Cessation
- 2005-01-24 PE PE2005000090A patent/PE20050687A1/es not_active Application Discontinuation
- 2005-01-26 EA EA200601378A patent/EA010598B1/ru not_active IP Right Cessation
- 2005-01-26 PL PL05726323T patent/PL1711465T3/pl unknown
- 2005-01-26 KR KR1020067015184A patent/KR20060127927A/ko not_active Ceased
- 2005-01-26 GE GEAP20059594A patent/GEP20094691B/en unknown
- 2005-01-26 AU AU2005207934A patent/AU2005207934B2/en not_active Ceased
- 2005-01-26 CA CA2554550A patent/CA2554550C/en not_active Expired - Fee Related
- 2005-01-26 NZ NZ548415A patent/NZ548415A/en not_active IP Right Cessation
- 2005-01-26 UA UAA200609315A patent/UA84192C2/ru unknown
- 2005-01-26 DK DK05726323T patent/DK1711465T3/da active
- 2005-01-26 US US10/586,727 patent/US7645790B2/en active Active
- 2005-01-26 AT AT05726323T patent/ATE382034T1/de active
- 2005-01-26 WO PCT/US2005/002149 patent/WO2005073191A1/en not_active Ceased
- 2005-01-26 BR BRPI0507050-3A patent/BRPI0507050A/pt not_active IP Right Cessation
- 2005-01-26 EP EP05726323A patent/EP1711465B1/en not_active Expired - Lifetime
- 2005-01-26 HR HR20080100T patent/HRP20080100T3/xx unknown
- 2005-01-26 DE DE602005004011T patent/DE602005004011T2/de not_active Expired - Lifetime
- 2005-01-26 JP JP2006551356A patent/JP3987100B2/ja not_active Expired - Fee Related
- 2005-01-26 ES ES05726323T patent/ES2297687T3/es not_active Expired - Lifetime
- 2005-01-26 PT PT05726323T patent/PT1711465E/pt unknown
- 2005-01-26 US US11/043,213 patent/US7217731B2/en not_active Expired - Lifetime
-
2006
- 2006-07-16 IL IL176879A patent/IL176879A0/en unknown
- 2006-07-19 CR CR8522A patent/CR8522A/es not_active Application Discontinuation
- 2006-07-21 EC EC2006006716A patent/ECSP066716A/es unknown
- 2006-07-26 NI NI200600164A patent/NI200600164A/es unknown
- 2006-07-27 CO CO06073837A patent/CO5700771A2/es active IP Right Grant
- 2006-08-11 MA MA29265A patent/MA28359A1/fr unknown
- 2006-08-25 NO NO20063810A patent/NO339041B1/no not_active IP Right Cessation
-
2007
- 2007-03-06 US US11/714,352 patent/US7345083B2/en not_active Expired - Lifetime
-
2008
- 2008-01-31 CY CY20081100113T patent/CY1107167T1/el unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ BY KZ KG MD TJ TM |
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| PD4A | Registration of transfer of a eurasian patent in accordance with the succession in title | ||
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): RU |