ATE354572T1 - Substituierte 1-piperidin-4-yl-4-azetidin-3-yl- piperazinderivate und deren verwendung als neurokininantagonisten - Google Patents
Substituierte 1-piperidin-4-yl-4-azetidin-3-yl- piperazinderivate und deren verwendung als neurokininantagonistenInfo
- Publication number
- ATE354572T1 ATE354572T1 AT03799583T AT03799583T ATE354572T1 AT E354572 T1 ATE354572 T1 AT E354572T1 AT 03799583 T AT03799583 T AT 03799583T AT 03799583 T AT03799583 T AT 03799583T AT E354572 T1 ATE354572 T1 AT E354572T1
- Authority
- AT
- Austria
- Prior art keywords
- disorders
- sub
- diseases
- neurokinin
- emesis
- Prior art date
Links
- YQHNGCCSZQYCOW-UHFFFAOYSA-N 1-(azetidin-3-yl)-4-piperidin-4-ylpiperazine Chemical class C1NCC1N1CCN(C2CCNCC2)CC1 YQHNGCCSZQYCOW-UHFFFAOYSA-N 0.000 title abstract 2
- 239000005557 antagonist Substances 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 5
- 208000035475 disorder Diseases 0.000 abstract 4
- 208000002551 irritable bowel syndrome Diseases 0.000 abstract 4
- 208000019901 Anxiety disease Diseases 0.000 abstract 2
- 208000002193 Pain Diseases 0.000 abstract 2
- 102000003141 Tachykinin Human genes 0.000 abstract 2
- 206010047700 Vomiting Diseases 0.000 abstract 2
- 230000003042 antagnostic effect Effects 0.000 abstract 2
- 230000000903 blocking effect Effects 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 239000003814 drug Substances 0.000 abstract 2
- 108060008037 tachykinin 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
- 208000027932 Collagen disease Diseases 0.000 abstract 1
- 206010012335 Dependence Diseases 0.000 abstract 1
- 208000030814 Eating disease Diseases 0.000 abstract 1
- 208000019454 Feeding and Eating disease Diseases 0.000 abstract 1
- 208000018522 Gastrointestinal disease Diseases 0.000 abstract 1
- 206010061218 Inflammation Diseases 0.000 abstract 1
- 208000021891 Micturition disease Diseases 0.000 abstract 1
- 208000019022 Mood disease Diseases 0.000 abstract 1
- 125000000815 N-oxide group Chemical group 0.000 abstract 1
- 208000007920 Neurogenic Inflammation Diseases 0.000 abstract 1
- 102000009493 Neurokinin receptors Human genes 0.000 abstract 1
- 108050000302 Neurokinin receptors Proteins 0.000 abstract 1
- 102100024304 Protachykinin-1 Human genes 0.000 abstract 1
- 208000028017 Psychotic disease Diseases 0.000 abstract 1
- 208000025747 Rheumatic disease Diseases 0.000 abstract 1
- 201000001880 Sexual dysfunction Diseases 0.000 abstract 1
- 101800003906 Substance P Proteins 0.000 abstract 1
- 206010046543 Urinary incontinence Diseases 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 230000000172 allergic effect Effects 0.000 abstract 1
- 230000036506 anxiety Effects 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 abstract 1
- 208000010668 atopic eczema Diseases 0.000 abstract 1
- 230000037396 body weight Effects 0.000 abstract 1
- 208000015114 central nervous system disease Diseases 0.000 abstract 1
- 230000027288 circadian rhythm Effects 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 235000014632 disordered eating Nutrition 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 230000004054 inflammatory process Effects 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 230000004770 neurodegeneration Effects 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- 208000022821 personality disease Diseases 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 230000000069 prophylactic effect Effects 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
- 201000000980 schizophrenia Diseases 0.000 abstract 1
- 230000020341 sensory perception of pain Effects 0.000 abstract 1
- 231100000872 sexual dysfunction Toxicity 0.000 abstract 1
- 208000017520 skin disease Diseases 0.000 abstract 1
- 208000019116 sleep disease Diseases 0.000 abstract 1
- 230000001629 suppression Effects 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
- 230000002455 vasospastic effect Effects 0.000 abstract 1
- 238000004260 weight control Methods 0.000 abstract 1
Classifications
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- 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
-
- 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
- A61P1/04—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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- 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
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- A—HUMAN NECESSITIES
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- C07D417/14—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 three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Psychiatry (AREA)
- Addiction (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Otolaryngology (AREA)
- Dermatology (AREA)
- Hospice & Palliative Care (AREA)
- Rheumatology (AREA)
- Psychology (AREA)
- Nutrition Science (AREA)
- Child & Adolescent Psychology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Urology & Nephrology (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP0214837 | 2002-12-23 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ATE354572T1 true ATE354572T1 (de) | 2007-03-15 |
Family
ID=32668703
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT03799583T ATE354572T1 (de) | 2002-12-23 | 2003-12-17 | Substituierte 1-piperidin-4-yl-4-azetidin-3-yl- piperazinderivate und deren verwendung als neurokininantagonisten |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US7435736B2 (de) |
| EP (1) | EP1581517B1 (de) |
| JP (1) | JP4660199B2 (de) |
| AT (1) | ATE354572T1 (de) |
| AU (1) | AU2003299249B2 (de) |
| CA (1) | CA2509406C (de) |
| DE (1) | DE60312042T2 (de) |
| ES (1) | ES2282731T3 (de) |
| WO (1) | WO2004056800A1 (de) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2527933C (en) | 2003-06-11 | 2009-08-11 | Merck & Co., Inc. | Substituted 3-alkyl and 3-alkenyl azetidine derivatives |
| CN103012374B (zh) | 2004-04-13 | 2015-05-20 | 因塞特公司 | 作为趋化因子受体拮抗剂的哌嗪基哌啶衍生物 |
| CA2585983C (en) * | 2004-11-10 | 2014-03-25 | Institut National De La Sante Et De La Recherche Medicale (Inserm) | Use of 1,4-bis (3-aminoalkyl) piperazine derivatives in the treatment of neurodegenerative diseases |
| GB0514017D0 (en) * | 2005-07-07 | 2005-08-17 | Ionix Pharmaceuticals Ltd | Chemical compounds |
| US7906652B2 (en) | 2005-11-28 | 2011-03-15 | Merck Sharp & Dohme Corp. | Heterocycle-substituted 3-alkyl azetidine derivatives |
| KR20120014154A (ko) * | 2009-04-22 | 2012-02-16 | 얀센 파마슈티카 엔.브이. | 모노아실글리세롤 리파제 억제제로서의 헤테로방향족 및 방향족 피페라지닐 아제티디닐 아미드 |
| US8435977B2 (en) | 2009-04-22 | 2013-05-07 | Janssen Pharmaceutica, Nv | Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitors |
| US8362001B2 (en) * | 2009-04-22 | 2013-01-29 | Janssen Pharmaceutica Nv | Azetidinyl diamides as monoacylglycerol lipase inhibitors |
| AU2011296068B2 (en) | 2010-09-03 | 2015-07-09 | Janssen Pharmaceutica Nv | Di-azetidinyl diamide as monoacylglycerol lipase inhibitors |
| EP2621918A1 (de) * | 2010-09-27 | 2013-08-07 | Janssen Pharmaceutica, N.V. | Oxopiperazin-azetidinamide und oxodiazepin-azetidinamide als monoacylglycerol-lipasehemmer |
| US8513423B2 (en) | 2010-10-22 | 2013-08-20 | Janssen Pharmaceutica, Nv | Piperidin-4-yl-azetidine diamides as monoacylglycerol lipase inhibitors |
| CN103261189B (zh) | 2010-10-22 | 2015-01-28 | 詹森药业有限公司 | 作为单酰基甘油脂肪酶抑制剂的氨基-吡咯烷-氮杂环丁烷二酰胺 |
| KR102115060B1 (ko) * | 2012-12-27 | 2020-05-25 | 알즈프로텍트 | N-(3-(4-(3-(디이소부틸아미노)프로필)피페라진-1-일)프로필)-1H-벤조[d]이미다졸-2-아민의 황산염들, 이들의 제조 방법 및 그것의 용도 |
| EP3915560A1 (de) | 2014-06-25 | 2021-12-01 | Emory University | Verfahren zur bewältigung von bedingter angst mit neurokinin-rezeptor-antagonisten |
| WO2016046130A1 (en) * | 2014-09-22 | 2016-03-31 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and pharmaceutical compositions for the treatment of fibrosis |
| US12084462B2 (en) | 2016-09-14 | 2024-09-10 | Janssen Pharmaceutica Nv | Spiro bicyclic inhibitors of menin-MLL interaction |
| HUE053907T2 (hu) | 2016-09-14 | 2021-07-28 | Janssen Pharmaceutica Nv | A menin-MLL kölcsönhatás spiro-biciklusos inhibitorai |
| MA46228A (fr) * | 2016-09-14 | 2019-07-24 | Janssen Pharmaceutica Nv | Inhibiteurs bicycliques fusionnés de l'interaction ménine-mll |
| EP3555103B1 (de) | 2016-12-15 | 2021-09-22 | Janssen Pharmaceutica NV | Azepanderivate als hemmer der menin-mll-interaktion |
| US11458129B2 (en) | 2017-11-02 | 2022-10-04 | California Institute Of Technology | Neurokinin antagonists and uses thereof |
| US11396517B1 (en) | 2017-12-20 | 2022-07-26 | Janssen Pharmaceutica Nv | Exo-aza spiro inhibitors of menin-MLL interaction |
| WO2021121327A1 (en) | 2019-12-19 | 2021-06-24 | Janssen Pharmaceutica Nv | Substituted straight chain spiro derivatives |
| EP4355729A1 (de) | 2021-06-16 | 2024-04-24 | Celgene Corporation | Azetidinylverbindungen mit einer carbonsäuregruppe zur behandlung neurodegenerativer erkrankungen |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MY110227A (en) * | 1991-08-12 | 1998-03-31 | Ciba Geigy Ag | 1-acylpiperindine compounds. |
| NZ321575A (en) | 1995-10-30 | 1999-05-28 | Janssen Pharmaceutica Nv | 1-(1,2-disubstituted piperidinyl)-4- substituted piperazine derivatives |
| GB9600235D0 (en) * | 1996-01-05 | 1996-03-06 | Pfizer Ltd | Therapeutic agents |
| GB9714129D0 (en) * | 1997-07-04 | 1997-09-10 | Pfizer Ltd | Azetidines |
| AU7788500A (en) | 1999-10-25 | 2001-05-08 | Janssen Pharmaceutica N.V. | Use of substance p antagonists for influencing the circadian timing system |
| GB0025354D0 (en) * | 2000-10-17 | 2000-11-29 | Glaxo Group Ltd | Chemical compounds |
| US6642226B2 (en) | 2001-02-06 | 2003-11-04 | Hoffman-La Roche Inc. | Substituted phenyl-piperidine methanone compounds |
| FR2820426B1 (fr) * | 2001-02-07 | 2007-05-11 | Condat Sa | Gel d'isolation thermique a reticulation controlee pour les lignes de transport d'hydrocarbures petroliers |
-
2003
- 2003-12-17 AT AT03799583T patent/ATE354572T1/de active
- 2003-12-17 WO PCT/EP2003/051042 patent/WO2004056800A1/en not_active Ceased
- 2003-12-17 US US10/540,304 patent/US7435736B2/en not_active Expired - Fee Related
- 2003-12-17 DE DE60312042T patent/DE60312042T2/de not_active Expired - Lifetime
- 2003-12-17 CA CA2509406A patent/CA2509406C/en not_active Expired - Fee Related
- 2003-12-17 JP JP2004561505A patent/JP4660199B2/ja not_active Expired - Fee Related
- 2003-12-17 ES ES03799583T patent/ES2282731T3/es not_active Expired - Lifetime
- 2003-12-17 AU AU2003299249A patent/AU2003299249B2/en not_active Ceased
- 2003-12-17 EP EP03799583A patent/EP1581517B1/de not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| DE60312042D1 (de) | 2007-04-05 |
| ES2282731T3 (es) | 2007-10-16 |
| EP1581517B1 (de) | 2007-02-21 |
| EP1581517A1 (de) | 2005-10-05 |
| JP4660199B2 (ja) | 2011-03-30 |
| JP2006512349A (ja) | 2006-04-13 |
| AU2003299249B2 (en) | 2010-05-27 |
| US7435736B2 (en) | 2008-10-14 |
| CA2509406A1 (en) | 2004-07-08 |
| US20060074069A1 (en) | 2006-04-06 |
| CA2509406C (en) | 2012-07-03 |
| DE60312042T2 (de) | 2007-10-31 |
| WO2004056800A1 (en) | 2004-07-08 |
| AU2003299249A1 (en) | 2004-07-14 |
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