AU744261B2 - Use of NK-1 receptor antagonists for treating eating disorders - Google Patents
Use of NK-1 receptor antagonists for treating eating disorders Download PDFInfo
- Publication number
- AU744261B2 AU744261B2 AU70657/98A AU7065798A AU744261B2 AU 744261 B2 AU744261 B2 AU 744261B2 AU 70657/98 A AU70657/98 A AU 70657/98A AU 7065798 A AU7065798 A AU 7065798A AU 744261 B2 AU744261 B2 AU 744261B2
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- Australia
- Prior art keywords
- phenyl
- group
- hydrogen
- substituted
- optionally
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Links
- 108010040718 Neurokinin-1 Receptors Proteins 0.000 title claims description 242
- 102000002002 Neurokinin-1 Receptors Human genes 0.000 title claims description 242
- 239000002464 receptor antagonist Substances 0.000 title claims description 239
- 229940044551 receptor antagonist Drugs 0.000 title claims description 239
- 235000014632 disordered eating Nutrition 0.000 title claims description 86
- 208000030814 Eating disease Diseases 0.000 title claims description 70
- 208000019454 Feeding and Eating disease Diseases 0.000 title claims description 70
- 239000001257 hydrogen Substances 0.000 claims description 319
- 229910052739 hydrogen Inorganic materials 0.000 claims description 319
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 293
- -1 chloro, bromo, iodo Chemical group 0.000 claims description 257
- 125000000217 alkyl group Chemical group 0.000 claims description 189
- 150000001875 compounds Chemical class 0.000 claims description 172
- 125000005843 halogen group Chemical group 0.000 claims description 164
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims description 160
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 154
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 152
- 125000001424 substituent group Chemical group 0.000 claims description 146
- 239000000460 chlorine Chemical group 0.000 claims description 142
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 142
- 150000002431 hydrogen Chemical class 0.000 claims description 141
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- 125000004432 carbon atom Chemical group C* 0.000 claims description 86
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- 125000001153 fluoro group Chemical group F* 0.000 claims description 65
- 229910052760 oxygen Inorganic materials 0.000 claims description 65
- 125000000623 heterocyclic group Chemical group 0.000 claims description 63
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 63
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 61
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- 238000000034 method Methods 0.000 claims description 55
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- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 41
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- 125000006413 ring segment Chemical group 0.000 claims description 40
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- 125000002541 furyl group Chemical group 0.000 claims description 36
- DBGIVFWFUFKIQN-VIFPVBQESA-N (+)-Fenfluramine Chemical compound CCN[C@@H](C)CC1=CC=CC(C(F)(F)F)=C1 DBGIVFWFUFKIQN-VIFPVBQESA-N 0.000 claims description 35
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- ZZVUWRFHKOJYTH-UHFFFAOYSA-N diphenhydramine Chemical group C=1C=CC=CC=1C(OCCN(C)C)C1=CC=CC=C1 ZZVUWRFHKOJYTH-UHFFFAOYSA-N 0.000 claims description 32
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 32
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- DBGIVFWFUFKIQN-UHFFFAOYSA-N (+-)-Fenfluramine Chemical compound CCNC(C)CC1=CC=CC(C(F)(F)F)=C1 DBGIVFWFUFKIQN-UHFFFAOYSA-N 0.000 claims description 25
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- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims description 25
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- 125000001041 indolyl group Chemical group 0.000 claims description 25
- 125000000842 isoxazolyl group Chemical group 0.000 claims description 25
- 235000020824 obesity Nutrition 0.000 claims description 25
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims description 25
- 125000003831 tetrazolyl group Chemical group 0.000 claims description 25
- 125000001425 triazolyl group Chemical group 0.000 claims description 25
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 24
- 125000002252 acyl group Chemical group 0.000 claims description 24
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- 238000002360 preparation method Methods 0.000 claims description 24
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- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims description 18
- DHHVAGZRUROJKS-UHFFFAOYSA-N phentermine Chemical compound CC(C)(N)CC1=CC=CC=C1 DHHVAGZRUROJKS-UHFFFAOYSA-N 0.000 claims description 18
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 17
- 206010006550 Bulimia nervosa Diseases 0.000 claims description 17
- 125000002947 alkylene group Chemical group 0.000 claims description 17
- 125000001589 carboacyl group Chemical group 0.000 claims description 17
- CREMABGTGYGIQB-UHFFFAOYSA-N carbon carbon Chemical compound C.C CREMABGTGYGIQB-UHFFFAOYSA-N 0.000 claims description 17
- 239000003814 drug Substances 0.000 claims description 17
- 208000010235 Food Addiction Diseases 0.000 claims description 16
- 239000005864 Sulphur Substances 0.000 claims description 16
- 229910052801 chlorine Inorganic materials 0.000 claims description 16
- 125000000000 cycloalkoxy group Chemical group 0.000 claims description 16
- 125000005842 heteroatom Chemical group 0.000 claims description 16
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 claims description 16
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims description 16
- 125000002757 morpholinyl group Chemical group 0.000 claims description 16
- 229920006395 saturated elastomer Polymers 0.000 claims description 16
- 125000003107 substituted aryl group Chemical group 0.000 claims description 16
- 239000011593 sulfur Substances 0.000 claims description 16
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 15
- TZWKUQDQKPYNLL-UHFFFAOYSA-N cloforex Chemical compound CCOC(=O)NC(C)(C)CC1=CC=C(Cl)C=C1 TZWKUQDQKPYNLL-UHFFFAOYSA-N 0.000 claims description 15
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- PZJBWSQQDMRZHY-UHFFFAOYSA-N picilorex Chemical compound CC1NC(C2CC2)CC1C1=CC=C(Cl)C=C1 PZJBWSQQDMRZHY-UHFFFAOYSA-N 0.000 claims description 15
- 229950003624 picilorex Drugs 0.000 claims description 15
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- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 14
- ZCKAMNXUHHNZLN-UHFFFAOYSA-N Chlorphentermine Chemical compound CC(C)(N)CC1=CC=C(Cl)C=C1 ZCKAMNXUHHNZLN-UHFFFAOYSA-N 0.000 claims description 14
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- HXCXASJHZQXCKK-UHFFFAOYSA-N clortermine Chemical compound CC(C)(N)CC1=CC=CC=C1Cl HXCXASJHZQXCKK-UHFFFAOYSA-N 0.000 claims description 14
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- 238000004519 manufacturing process Methods 0.000 claims description 14
- DLNKOYKMWOXYQA-UHFFFAOYSA-N dl-pseudophenylpropanolamine Natural products CC(N)C(O)C1=CC=CC=C1 DLNKOYKMWOXYQA-UHFFFAOYSA-N 0.000 claims description 13
- DLNKOYKMWOXYQA-APPZFPTMSA-N phenylpropanolamine Chemical compound C[C@@H](N)[C@H](O)C1=CC=CC=C1 DLNKOYKMWOXYQA-APPZFPTMSA-N 0.000 claims description 13
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- 239000008194 pharmaceutical composition Substances 0.000 claims description 12
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 12
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 11
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 11
- 125000001715 oxadiazolyl group Chemical group 0.000 claims description 10
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- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims description 9
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- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims description 9
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- OOBHFESNSZDWIU-GXSJLCMTSA-N (2s,3s)-3-methyl-2-phenylmorpholine Chemical compound C[C@@H]1NCCO[C@H]1C1=CC=CC=C1 OOBHFESNSZDWIU-GXSJLCMTSA-N 0.000 claims description 8
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- 241000689227 Cora <basidiomycete fungus> Species 0.000 claims description 8
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- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 4
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- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/451—Non condensed piperidines, e.g. piperocaine having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
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- A—HUMAN NECESSITIES
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- 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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- A61K31/66—Phosphorus compounds
- A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
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- A—HUMAN NECESSITIES
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- 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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- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
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- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB9708289 | 1997-04-24 | ||
| GBGB9708289.5A GB9708289D0 (en) | 1997-04-24 | 1997-04-24 | Therapeutic use |
| GBGB9721265.8A GB9721265D0 (en) | 1997-10-07 | 1997-10-07 | Therapeutic use |
| GB9721265 | 1997-10-07 | ||
| PCT/GB1998/001161 WO1998047513A1 (fr) | 1997-04-24 | 1998-04-22 | Utilisation des antagonistes du recepteur de nk-1 dans le traitement des troubles alimentaires |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU7065798A AU7065798A (en) | 1998-11-13 |
| AU744261B2 true AU744261B2 (en) | 2002-02-21 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
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| AU70657/98A Ceased AU744261B2 (en) | 1997-04-24 | 1998-04-22 | Use of NK-1 receptor antagonists for treating eating disorders |
Country Status (5)
| Country | Link |
|---|---|
| EP (1) | EP0977572A1 (fr) |
| JP (1) | JP2001524960A (fr) |
| AU (1) | AU744261B2 (fr) |
| CA (1) | CA2287487A1 (fr) |
| WO (1) | WO1998047513A1 (fr) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE60039508D1 (de) * | 1999-03-19 | 2008-08-28 | Abbott Gmbh & Co Kg | Methoden zur behandlung der essstörungen |
| JP2003511410A (ja) * | 1999-10-13 | 2003-03-25 | グラクソ グループ リミテッド | 肥満症の治療のためのモルホリノール誘導体 |
| IL157456A0 (en) * | 2001-03-21 | 2004-03-28 | Pharmacopeia Inc Pharmacopeia | Aryl and biaryl compounds having mch modulatory activity |
| DE10311984A1 (de) * | 2003-03-12 | 2004-09-23 | Freie Universität Berlin | Verwendung von NEP-assoziierten Molekülen zur Behandlung von nichtimmunogenen-nichthypertensiven Zivilisationskrankheiten |
| CN106290894A (zh) * | 2016-07-21 | 2017-01-04 | 浙江理工大学 | 一种基于nk1r蛋白的白血病检测试剂盒 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0577394A1 (fr) * | 1992-06-29 | 1994-01-05 | Merck & Co. Inc. | Morpholine et thiomorpholine, antagonistes du récepteur de tachykinine |
| WO1996024353A1 (fr) * | 1995-02-10 | 1996-08-15 | Eli Lilly And Company | Procede de traitement ou de prevention de troubles psychiatriques |
| WO1996037207A2 (fr) * | 1995-05-25 | 1996-11-28 | Biofrontiers, Inc. | Compositions pharmaceutiques contenant du sulfate de calcium |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB8929070D0 (en) * | 1989-12-22 | 1990-02-28 | Fujisawa Pharmaceutical Co | Peptide compounds,processes for preparation thereof and pharmaceutical composition comprising the same |
| UA41251C2 (uk) * | 1990-01-04 | 2001-09-17 | Пфайзер, Інк. | Гідровані азотвмісні гетероциклічні сполуки, похідні піперидину, фармацевтична композиція та спосіб пригнічення активності речовини р в організмі |
| KR0145432B1 (ko) * | 1991-03-26 | 1998-07-15 | 알렌 제이. 스피겔 | 치환된 피페리딘의 입체선택적 제조 방법 |
| MY110227A (en) * | 1991-08-12 | 1998-03-31 | Ciba Geigy Ag | 1-acylpiperindine compounds. |
| FR2689888B1 (fr) * | 1992-04-10 | 1994-06-10 | Rhone Poulenc Rorer Sa | Nouveaux derives de perhydroisoindole, leur preparation et les compositions pharmaceutiques qui les contiennent. |
| FR2696178B1 (fr) * | 1992-09-30 | 1994-12-30 | Sanofi Elf | Amides basiques quaternaires, procédé pour leur préparation et compositions pharmaceutiques en contenant. |
| IL111002A (en) * | 1993-09-22 | 1998-09-24 | Glaxo Group Ltd | History of piperidine, their preparation and the pharmaceutical preparations containing them |
| US6403577B1 (en) * | 1993-11-17 | 2002-06-11 | Eli Lilly And Company | Hexamethyleneiminyl tachykinin receptor antagonists |
| US5612337A (en) * | 1993-12-29 | 1997-03-18 | Merck Sharp & Dohme Limited | Substituted morpholine derivatives and their use as therapeutic agents |
| TW385308B (en) * | 1994-03-04 | 2000-03-21 | Merck & Co Inc | Prodrugs of morpholine tachykinin receptor antagonists |
| US5824678A (en) * | 1994-08-15 | 1998-10-20 | Merck Sharp & Dohme Ltd. | Morpholine derivatives and their use as therapeutic agents |
| WO1997007117A1 (fr) * | 1995-08-21 | 1997-02-27 | Eli Lilly And Company | 2-acylaminopropanamines servant de secretagogues de la somatotrophine |
| WO1997038692A1 (fr) * | 1996-04-12 | 1997-10-23 | Eli Lilly And Company | Binsindoles pour traiter la douleur ou les phenomenes nociceptifs |
| EP0906315A1 (fr) * | 1996-06-21 | 1999-04-07 | MERCK SHARP & DOHME LTD. | Derives spiro-piperidine et leur utilisation comme agents therapeutiques |
| GB9613969D0 (en) * | 1996-07-03 | 1996-09-04 | Merck Sharp & Dohme | Therapeutic agents |
-
1998
- 1998-04-22 WO PCT/GB1998/001161 patent/WO1998047513A1/fr not_active Application Discontinuation
- 1998-04-22 CA CA002287487A patent/CA2287487A1/fr not_active Abandoned
- 1998-04-22 AU AU70657/98A patent/AU744261B2/en not_active Ceased
- 1998-04-22 JP JP54529098A patent/JP2001524960A/ja active Pending
- 1998-04-22 EP EP98917425A patent/EP0977572A1/fr not_active Withdrawn
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0577394A1 (fr) * | 1992-06-29 | 1994-01-05 | Merck & Co. Inc. | Morpholine et thiomorpholine, antagonistes du récepteur de tachykinine |
| WO1996024353A1 (fr) * | 1995-02-10 | 1996-08-15 | Eli Lilly And Company | Procede de traitement ou de prevention de troubles psychiatriques |
| WO1996037207A2 (fr) * | 1995-05-25 | 1996-11-28 | Biofrontiers, Inc. | Compositions pharmaceutiques contenant du sulfate de calcium |
Also Published As
| Publication number | Publication date |
|---|---|
| JP2001524960A (ja) | 2001-12-04 |
| AU7065798A (en) | 1998-11-13 |
| WO1998047513A1 (fr) | 1998-10-29 |
| CA2287487A1 (fr) | 1998-10-29 |
| EP0977572A1 (fr) | 2000-02-09 |
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| Date | Code | Title | Description |
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| FGA | Letters patent sealed or granted (standard patent) | ||
| MK14 | Patent ceased section 143(a) (annual fees not paid) or expired |