CY1113458T1 - Σπειρο (πιπεριδιν-4, 2'-πυρρολιδιν)-1-(3,5 τριφθορομεθυλ φαινυλ) μεθυλκαρβοξαμιδια ως ανταγωνιστες του υποδοχεα ταχυκινινης νκ1 - Google Patents
Σπειρο (πιπεριδιν-4, 2'-πυρρολιδιν)-1-(3,5 τριφθορομεθυλ φαινυλ) μεθυλκαρβοξαμιδια ως ανταγωνιστες του υποδοχεα ταχυκινινης νκ1Info
- Publication number
- CY1113458T1 CY1113458T1 CY20121101226T CY121101226T CY1113458T1 CY 1113458 T1 CY1113458 T1 CY 1113458T1 CY 20121101226 T CY20121101226 T CY 20121101226T CY 121101226 T CY121101226 T CY 121101226T CY 1113458 T1 CY1113458 T1 CY 1113458T1
- Authority
- CY
- Cyprus
- Prior art keywords
- alkyl
- halogen
- hydrogen
- methylcarboxamides
- receptor1
- Prior art date
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/10—Spiro-condensed systems
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- 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
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- 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
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
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- 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
- A61P1/10—Laxatives
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- 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
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
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- 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
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
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- 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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- 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
- A61P17/06—Antipsoriatics
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- 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
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- A—HUMAN NECESSITIES
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- 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
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- 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
- A61P25/20—Hypnotics; Sedatives
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- 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
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- 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
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- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/32—Alcohol-abuse
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- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/34—Tobacco-abuse
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- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/36—Opioid-abuse
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- 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]
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
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- 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
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- A—HUMAN NECESSITIES
- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/20—Spiro-condensed systems
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- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Immunology (AREA)
- Addiction (AREA)
- Pulmonology (AREA)
- Psychiatry (AREA)
- Dermatology (AREA)
- Pain & Pain Management (AREA)
- Urology & Nephrology (AREA)
- Otolaryngology (AREA)
- Gynecology & Obstetrics (AREA)
- Cardiology (AREA)
- Vascular Medicine (AREA)
- Anesthesiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Nutrition Science (AREA)
- Hospice & Palliative Care (AREA)
- Transplantation (AREA)
- Rheumatology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Ενώσεις του χημικού τύπου (Ι) ή ένα φαρμακευτικώς αποδεκτό άλας εξ αυτών όπου το R είναι υδρογόνο ή C1-4 αλκύλιο · το R1 είναι υδρογόνο, C1-4 αλκύλιο, C(O)OH, C(O)NH2 ή (C1-4 αλκυλένιο)R10 · τα R2 και R3 είναι ανεξαρτήτως υδρογόνο, C1-4 αλκύλιο ή το R2 από κοινού με το R3 και από κοινού με το άτομο άνθρακα στο οποίο αυτά προσαρτώνται σχηματίζουν μία C3-8 κυκλοαλκυλομάδα · το R4 είναι C1-4 αλκύλιο, C 1-4 αλκοξυομάδα ή αλογόνο · τα R5 και R7 είναι ανεξαρτήτως υδρογόνο, υδροξυομάδα, αλογόνο, C(O)NH2 , C(O)OH ή (C1-4 αλκυλένιο) R10 · τα R6 και R8 είναι ανεξαρτήτως υδρογόνο ή αλογόνο · το R9 είναι υδρογόνο, (C 1-4 αλκυλένιο)R10, C(O)NH2, C(O)OH ή το R9 από κοινού με το R σχηματίζουν έναν 6-μελή ετεροκυκλικό δακτύλιο περιέχοντας προαιρετικώς ένα περαιτέρω ετεροάτομο που επιλέγεται από οξυγόνο, θείο ή άζωτο · το R10 είναι υδρογόνο, αλογόνο, υδροξυομάδα, C(O)NH2, C(Ο)NH(C1-4 αλκύλιο), C(Ο)N(C1-4 αλκύλιο)2 ή C(Ο)OH · το n είναι 0, 1 ή 2, διεργασίες για την παρασκευή αυτών, συνθέσεις περιέχοντας αυτές και η χρήση αυτών στην αγωγή παθήσεων και καταστάσεων για τις οποίες ο ανταγωνισμός του ΝΚ1 είναι ευεργετικός.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0808030.1A GB0808030D0 (en) | 2008-05-01 | 2008-05-01 | Novel compounds |
| EP09738179A EP2300474B1 (en) | 2008-05-01 | 2009-04-29 | Spiro (piperidine-4, 2 ' -pyrrolidine) -1- (3, 5- trifluoromethyl phenyl) methylcarboxamides as nk1 tachikynin receptor antagonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CY1113458T1 true CY1113458T1 (el) | 2016-06-22 |
Family
ID=39537192
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CY20121101226T CY1113458T1 (el) | 2008-05-01 | 2012-12-17 | Σπειρο (πιπεριδιν-4, 2'-πυρρολιδιν)-1-(3,5 τριφθορομεθυλ φαινυλ) μεθυλκαρβοξαμιδια ως ανταγωνιστες του υποδοχεα ταχυκινινης νκ1 |
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US8367692B2 (el) |
| EP (1) | EP2300474B1 (el) |
| JP (1) | JP5524183B2 (el) |
| KR (1) | KR101645743B1 (el) |
| CN (1) | CN102083832B (el) |
| AU (1) | AU2009242120B2 (el) |
| BR (1) | BRPI0910530B8 (el) |
| CA (1) | CA2723062C (el) |
| CY (1) | CY1113458T1 (el) |
| DK (1) | DK2300474T3 (el) |
| EA (1) | EA017960B1 (el) |
| ES (1) | ES2395571T3 (el) |
| GB (1) | GB0808030D0 (el) |
| HR (1) | HRP20121018T1 (el) |
| IL (1) | IL208917A (el) |
| MX (1) | MX2010011985A (el) |
| PL (1) | PL2300474T3 (el) |
| PT (1) | PT2300474E (el) |
| RS (1) | RS52719B (el) |
| SI (1) | SI2300474T1 (el) |
| WO (1) | WO2009133135A1 (el) |
| ZA (1) | ZA201007519B (el) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2484674A1 (en) * | 2011-02-02 | 2012-08-08 | Rottapharm S.P.A. | Spiro aminic compounds with NK1 antagonist activity |
| CN109651368A (zh) * | 2018-12-17 | 2019-04-19 | 武汉药明康德新药开发有限公司 | 4-甲酸甲酯-2-氧-1,8-二氮杂螺[4.5]癸烷-8-甲酸叔丁酯的制备方法 |
| WO2021245512A1 (en) | 2020-06-02 | 2021-12-09 | Nerre Therapeutics Limited | Neurokinin (nk)-1 receptor antagonists for use in the treatment of pulmonary fibrosis conditions promoted by mechanical injury to the lungs |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9215706D0 (en) | 1992-07-23 | 1992-09-09 | Tollpass Limited | Parking toll collecting system |
| EP0702681A1 (en) * | 1993-06-07 | 1996-03-27 | Merck & Co. Inc. | Spiro-substituted azacycles as neurokinin antagonists |
| DE69728883T2 (de) | 1996-07-17 | 2005-04-07 | Merck & Co., Inc. | Änderung des zirkadischen rhythmus mit nicht-peptidischen neurokinin-1 rezeptor antagonisten |
| US6013652A (en) * | 1997-12-04 | 2000-01-11 | Merck & Co., Inc. | Spiro-substituted azacycles as neurokinin antagonists |
| AU7788500A (en) | 1999-10-25 | 2001-05-08 | Janssen Pharmaceutica N.V. | Use of substance p antagonists for influencing the circadian timing system |
| GB0203022D0 (en) * | 2002-02-08 | 2002-03-27 | Glaxo Group Ltd | Chemical compounds |
| WO2003066589A1 (en) * | 2002-02-08 | 2003-08-14 | Glaxo Group Limited | Piperidylcarboxamide derivatives and their use in the treatment of tachykinim-mediated diseases |
| JP4389478B2 (ja) * | 2002-05-29 | 2009-12-24 | 田辺三菱製薬株式会社 | 新規ピペリジン誘導体 |
| KR100877641B1 (ko) * | 2003-11-28 | 2009-01-09 | 미쓰비시 타나베 파마 코퍼레이션 | 피페리딘 화합물 및 그의 제조 방법 |
| JP2005154380A (ja) * | 2003-11-28 | 2005-06-16 | Tanabe Seiyaku Co Ltd | ピペリジン誘導体 |
| JP4380508B2 (ja) * | 2003-11-28 | 2009-12-09 | 田辺三菱製薬株式会社 | 医薬組成物 |
| GB0514707D0 (en) * | 2005-07-18 | 2005-08-24 | Glaxo Group Ltd | Chemical compounds |
-
2008
- 2008-05-01 GB GBGB0808030.1A patent/GB0808030D0/en not_active Ceased
-
2009
- 2009-04-29 CN CN2009801257867A patent/CN102083832B/zh active Active
- 2009-04-29 PT PT97381792T patent/PT2300474E/pt unknown
- 2009-04-29 US US12/989,699 patent/US8367692B2/en active Active
- 2009-04-29 MX MX2010011985A patent/MX2010011985A/es active IP Right Grant
- 2009-04-29 KR KR1020107026865A patent/KR101645743B1/ko active IP Right Grant
- 2009-04-29 EA EA201071259A patent/EA017960B1/ru not_active IP Right Cessation
- 2009-04-29 RS RS20120551A patent/RS52719B/en unknown
- 2009-04-29 PL PL09738179T patent/PL2300474T3/pl unknown
- 2009-04-29 WO PCT/EP2009/055190 patent/WO2009133135A1/en active Application Filing
- 2009-04-29 SI SI200930430T patent/SI2300474T1/sl unknown
- 2009-04-29 ES ES09738179T patent/ES2395571T3/es active Active
- 2009-04-29 JP JP2011506703A patent/JP5524183B2/ja active Active
- 2009-04-29 EP EP09738179A patent/EP2300474B1/en active Active
- 2009-04-29 CA CA2723062A patent/CA2723062C/en active Active
- 2009-04-29 DK DK09738179.2T patent/DK2300474T3/da active
- 2009-04-29 AU AU2009242120A patent/AU2009242120B2/en not_active Ceased
- 2009-04-29 BR BRPI0910530A patent/BRPI0910530B8/pt active IP Right Grant
-
2010
- 2010-10-21 ZA ZA2010/07519A patent/ZA201007519B/en unknown
- 2010-10-25 IL IL208917A patent/IL208917A/en active IP Right Grant
-
2012
- 2012-11-21 US US13/682,889 patent/US8633214B2/en active Active
- 2012-12-12 HR HRP20121018AT patent/HRP20121018T1/hr unknown
- 2012-12-17 CY CY20121101226T patent/CY1113458T1/el unknown
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