HUP0301228A2 - 3-azabicyclo(3.1.0)hexane derivatives having opioid receptor affinity, process for their preparation and pharmaceutical compositions containing them - Google Patents
3-azabicyclo(3.1.0)hexane derivatives having opioid receptor affinity, process for their preparation and pharmaceutical compositions containing themInfo
- Publication number
- HUP0301228A2 HUP0301228A2 HU0301228A HUP0301228A HUP0301228A2 HU P0301228 A2 HUP0301228 A2 HU P0301228A2 HU 0301228 A HU0301228 A HU 0301228A HU P0301228 A HUP0301228 A HU P0301228A HU P0301228 A2 HUP0301228 A2 HU P0301228A2
- Authority
- HU
- Hungary
- Prior art keywords
- alkyl
- group
- carbon atoms
- ring
- halogen
- Prior art date
Links
- 108090000137 Opioid Receptors Proteins 0.000 title abstract 3
- 102000003840 Opioid Receptors Human genes 0.000 title abstract 3
- 150000005228 3‐azabicyclo[3.1.0]hexanes Chemical class 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 125000004432 carbon atom Chemical group C* 0.000 abstract 5
- 125000003342 alkenyl group Chemical group 0.000 abstract 3
- 125000000304 alkynyl group Chemical group 0.000 abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 208000003251 Pruritus Diseases 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000001188 haloalkyl group Chemical group 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 1
- 208000007848 Alcoholism Diseases 0.000 abstract 1
- 206010010774 Constipation Diseases 0.000 abstract 1
- 208000030814 Eating disease Diseases 0.000 abstract 1
- 208000019454 Feeding and Eating disease Diseases 0.000 abstract 1
- 206010019196 Head injury Diseases 0.000 abstract 1
- 206010028813 Nausea Diseases 0.000 abstract 1
- 208000012488 Opiate Overdose Diseases 0.000 abstract 1
- 101100244562 Pseudomonas aeruginosa (strain ATCC 15692 / DSM 22644 / CIP 104116 / JCM 14847 / LMG 12228 / 1C / PRS 101 / PAO1) oprD gene Proteins 0.000 abstract 1
- 201000001880 Sexual dysfunction Diseases 0.000 abstract 1
- 125000004423 acyloxy group Chemical group 0.000 abstract 1
- 201000007930 alcohol dependence Diseases 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000004104 aryloxy group Chemical group 0.000 abstract 1
- 125000001589 carboacyl group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000000000 cycloalkoxy group Chemical group 0.000 abstract 1
- 108700023159 delta Opioid Receptors Proteins 0.000 abstract 1
- 102000048124 delta Opioid Receptors Human genes 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 235000014632 disordered eating Nutrition 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 208000002551 irritable bowel syndrome Diseases 0.000 abstract 1
- 230000007803 itching Effects 0.000 abstract 1
- 102000048260 kappa Opioid Receptors Human genes 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 102000051367 mu Opioid Receptors Human genes 0.000 abstract 1
- 230000008693 nausea Effects 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 231100000872 sexual dysfunction Toxicity 0.000 abstract 1
- 230000035939 shock Effects 0.000 abstract 1
- 230000000391 smoking effect Effects 0.000 abstract 1
- 208000020431 spinal cord injury Diseases 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 208000024891 symptom Diseases 0.000 abstract 1
- 210000004916 vomit Anatomy 0.000 abstract 1
- 230000008673 vomiting Effects 0.000 abstract 1
- 108020001588 κ-opioid receptors Proteins 0.000 abstract 1
- 108020001612 μ-opioid receptors Proteins 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
-
- 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
- C07D209/52—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 condensed with a ring other than six-membered
-
- 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
- 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
- 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
-
- 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
-
- 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
-
- 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
-
- 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
- A61P17/04—Antipruritics
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
-
- 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
-
- 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
-
- 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
-
- 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
-
- 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
- C07D403/12—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 chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Addiction (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Dermatology (AREA)
- Reproductive Health (AREA)
- Endocrinology (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Nutrition Science (AREA)
- Otolaryngology (AREA)
- Gynecology & Obstetrics (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Indole Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Az (I) általános képletű vegyületek - ahol az Ar-gyűrű adott esetbenbenzolgyűrűvel kondenzált fenilgyűrűt vagy 5- vagy 6-tagúheteroarilgyűrűt jelent; R1 jelentése önmagában H, halogénatom, NO2,NH2, NY2WY1, Hetl, AD, CO2R7, C(O)R8, C(=NOH)R8 vagy OE; R2 jelentéseönmagában H vagy halogénatom; vagy R1 és R2 abban az esetben, ha aszomszédos szénatomokhoz kapcsolódnak, azokkal a szénatomokkal együtt,amelyekhez kapcsolódnak egy Het1a csoportot jelentenek; R3 jelentéseH, CN, halogénatom, alkoxi-, alkoxikarbonil-, alkanoil-, alkanoiloxi-,cikloalkil-, cikloalkiloxi-, cikloalkanoil-, aril-, ariloxi-,heteroaril-, telített heterociklusos csoport, NR12R13, CONR12R13,NY2WY1, alkil-, alkenil-, alkinilcsoport (ahol az alkil-, alkenil- ésalkinilcsoportok bármelyike adott esetben szubsztituáltak); R4jelentése alkil-, alkenil- vagy alkinilcsoport, amely csoportokmindegyike a nitrogénatomhoz egy sp3 szénatomon keresztül kapcsolódik,és amely csoport egy vagy több szubsztituenssel szubsztituált; R5 ésR8 jelentése egymástól függetlenül H vagy alkilcsoport; vagy R5 és R8azokkal a szénatomokkal együtt, amelyekhez kapcsolódnak,cikloalkilgyűrűt alkotnak; R6, R7, R9 és R10 jelentése külön-külön H;vagy R5 és R6 vagy R7 azokkal a szénatomokkal együtt, amelyekhezkapcsolódnak, cikloalkilgyűrűt alkotnak; X jelentése halogénatom,alkil-, alkoxi-, halogénalkil-, vagy halogénalkoxicsoport; n értéke 0,1 vagy 2; q értéke 0 vagy 1 - és gyógyászatilag elfogadhatószármazékaik vagy prodrogjaik opiát-receptorokhoz, például mü-, kappa-és delta-receptorokhoz kötődnek. Fenti tulajdonságuk következtébenopiátreceptorok által mediált betegségek vagy állapotok, előnyösenirritábilis bél szindróma; székrekedés; émelygés; hányás; pruritus;táplálkozási rendellenességek; opiát túladagolások; depresszió;dohányzás és alkoholizmus; szexuális diszfunkció; sokk; gutaütés;gerincsérülés és/vagy fejtrauma; valamint a viszketéssel mint tünetteljellemzett állapotok kezelésére alkalmazhatók. A találmány kiterjed avegyületek előállítására és ezeket tartalmazó gyógyszerkészítményekreis. ÓThe compounds of general formula (I) - where the Ar-ring means a phenyl ring condensed with a benzene ring or a 5- or 6-membered heteroaryl ring; R 1 alone is H, halogen, NO 2 , NH 2 , NY 2 WY 1 , Hetl, AD, CO 2 R 7 , C(O)R 8 , C(=NOH)R 8 or OE; R2 alone is H or halogen; or R1 and R2 in the event that they are attached to adjacent carbon atoms, together with the carbon atoms to which they are attached represent a Het1a group; R3 is H, CN, halogen, alkoxy-, alkoxycarbonyl-, alkanoyl-, alkanoyloxy-, cycloalkyl-, cycloalkyloxy-, cycloalkanoyl-, aryl-, aryloxy-, heteroaryl-, saturated heterocyclic group, NR12R13, CONR12R13, NY2WY1, alkyl-, alkenyl, alkynyl (where any of the alkyl, alkenyl and alkynyl groups are optionally substituted); R4 is an alkyl, alkenyl or alkynyl group, each of which groups is connected to the nitrogen atom through an sp3 carbon atom, and which group is substituted with one or more substituents; R 5 and R 8 are independently H or alkyl; or R5 and R8, together with the carbon atoms to which they are attached, form a cycloalkyl ring; R 6 , R 7 , R 9 and R 10 are individually H; or R 5 and R 6 or R 7 together with the carbon atoms to which they are attached form a cycloalkyl ring; X is a halogen atom, an alkyl-, an alkoxy-, a haloalkyl-, or a haloalkyl group; n is 0, 1 or 2; q is 0 or 1 - and their pharmaceutically acceptable derivatives or prodrugs bind to opiate receptors such as mu, kappa and delta receptors. Due to their above properties, diseases or conditions mediated by opiate receptors, preferably irritable bowel syndrome; constipation; nausea; vomit; pruritus; eating disorders; opiate overdoses; depression; smoking and alcoholism; sexual dysfunction; shock; stroke; spinal cord injury and/or head trauma; and can be used to treat conditions characterized by itching as a symptom. The invention covers the production of compounds and pharmaceutical preparations containing them. HE
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0015562.2A GB0015562D0 (en) | 2000-06-23 | 2000-06-23 | Heterocycles |
| PCT/IB2001/001035 WO2001098267A1 (en) | 2000-06-23 | 2001-06-07 | 3-azabicyclo (3.1.0) hexane derivatives having opioid receptor affinity |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP0301228A2 true HUP0301228A2 (en) | 2003-08-28 |
| HUP0301228A3 HUP0301228A3 (en) | 2005-08-29 |
Family
ID=9894368
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0301228A HUP0301228A3 (en) | 2000-06-23 | 2001-06-07 | 3-azabicyclo(3.1.0)hexane derivatives having opioid receptor affinity, process for their preparation and pharmaceutical compositions containing them |
Country Status (34)
| Country | Link |
|---|---|
| EP (1) | EP1292574A1 (en) |
| JP (1) | JP2004512263A (en) |
| KR (1) | KR20040002386A (en) |
| CN (1) | CN1639121A (en) |
| AP (1) | AP2002002698A0 (en) |
| AR (1) | AR028969A1 (en) |
| AU (1) | AU781837B2 (en) |
| BG (1) | BG107329A (en) |
| BR (1) | BR0111867A (en) |
| CA (1) | CA2412188A1 (en) |
| CZ (1) | CZ20023967A3 (en) |
| DO (1) | DOP2001000187A (en) |
| DZ (1) | DZ3368A1 (en) |
| EA (1) | EA005117B1 (en) |
| GB (1) | GB0015562D0 (en) |
| HR (1) | HRP20020998A2 (en) |
| HU (1) | HUP0301228A3 (en) |
| IL (1) | IL153427A0 (en) |
| IS (1) | IS6637A (en) |
| MA (1) | MA26915A1 (en) |
| MX (1) | MXPA02012878A (en) |
| NO (1) | NO20026168L (en) |
| NZ (1) | NZ523141A (en) |
| OA (1) | OA12293A (en) |
| PA (1) | PA8519401A1 (en) |
| PE (1) | PE20020253A1 (en) |
| PL (1) | PL365956A1 (en) |
| SK (1) | SK17172002A3 (en) |
| TN (1) | TNSN01094A1 (en) |
| UA (1) | UA73176C2 (en) |
| UY (1) | UY26787A1 (en) |
| WO (1) | WO2001098267A1 (en) |
| YU (1) | YU91802A (en) |
| ZA (1) | ZA200210278B (en) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL368919A1 (en) | 2001-10-22 | 2005-04-04 | Pfizer Products Inc. | 3-azabicyclo (3.1.0) hexane derivatives as opioid receptor antagonists |
| JP2005531557A (en) * | 2002-05-17 | 2005-10-20 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフトング | Use of effective compounds as selective opiate receptor modulators |
| DE10259245A1 (en) | 2002-12-17 | 2004-07-01 | Merck Patent Gmbh | Derivatives of asimadolin with covalently bound acids |
| EP2070922B1 (en) | 2004-02-23 | 2011-08-17 | Glaxo Group Limited | Azabicyclo(3.1.0) hexane derivatives useful as modulators of dopamine D3 receptors |
| GB0507680D0 (en) * | 2005-04-15 | 2005-05-25 | Glaxo Group Ltd | Compounds |
| WO2006133945A1 (en) * | 2005-06-14 | 2006-12-21 | Glaxo Group Limited | Novel compounds |
| WO2007113258A1 (en) * | 2006-04-03 | 2007-10-11 | Glaxo Group Limited | Azabicyclo [3. 1. o] hexane derivatives as modulators of dopamine d3 receptors |
| EP2636407A3 (en) | 2007-03-30 | 2013-11-06 | Tioga Pharmaceuticals, Inc. | Kappa-opiate agonists for the treatment of diarrhea-predominant and alternating irritable bowel syndrome |
| TWI423801B (en) * | 2007-08-27 | 2014-01-21 | Theravance Inc | 8-azabicyclo[3.2.1]octyl-2-hydroxybenzamide compounds as mu opioid receptor antagonists |
| CA2936749C (en) | 2010-06-11 | 2019-07-09 | Joshua R. Giguere | Transition metal-catalyzed processes for the preparation of n-allyl compounds and use thereof |
| EP2621902B1 (en) | 2010-09-28 | 2017-04-12 | Panacea Biotec Ltd | 3-azabicyclo[3.1.0]hexane compounds useful for the treatment of cns disorders |
| CN105764888B (en) * | 2013-11-20 | 2018-04-06 | 株式会社三和化学研究所 | A kind of new 3 azabicyclos [3.1.0] hexame derivatives and its medical usage |
| CN113307760A (en) | 2015-05-20 | 2021-08-27 | 宇部兴产株式会社 | Novel crystal of salt of 3-azabicyclo [3.1.0] hexane derivative and medical application thereof |
| EP3582779B1 (en) * | 2017-02-17 | 2024-04-17 | Trevena, Inc. | 5-membered aza-heterocyclic containing delta-opioid receptor modulating compounds, methods of using and making the same |
| BR112019016775A2 (en) | 2017-02-17 | 2020-03-31 | Trevena, Inc. | DELTA-OPIOIDE MODULATING RECEIVER COMPOUNDS CONTAINING 7-MEMBER AZA-HETEROCYCLIC, METHODS OF USE AND PRODUCTION OF THE SAME |
| JPWO2018159716A1 (en) | 2017-03-02 | 2019-12-26 | 株式会社三和化学研究所 | Drugs for alcohol use disorders |
| CN108250088B (en) * | 2018-01-04 | 2020-10-30 | 四川之江高新材料股份有限公司 | Preparation method of N, N, N '-trimethyl-N' -hydroxyethyl bisaminoethylether |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3065230A (en) * | 1959-03-16 | 1962-11-20 | Burroughs Wellcome Co | Azabicyclohexanes and method of preparing them |
| IL86061A (en) * | 1987-04-16 | 1992-07-15 | Lilly Co Eli | Derivatives of trans-3,4-isomer of 4-methyl-4-phenyl-piperidines,process for their preparation and pharmaceutical compositions containing them |
| US5159081A (en) * | 1991-03-29 | 1992-10-27 | Eli Lilly And Company | Intermediates of peripherally selective n-carbonyl-3,4,4-trisubstituted piperidine opioid antagonists |
| DE4341403A1 (en) * | 1993-12-04 | 1995-06-08 | Basf Ag | N-substituted 3-azabicycloalkane derivatives, their preparation and use |
| TWI244481B (en) * | 1998-12-23 | 2005-12-01 | Pfizer | 3-azabicyclo[3.1.0]hexane derivatives useful in therapy |
| PE20001420A1 (en) * | 1998-12-23 | 2000-12-18 | Pfizer | CCR5 MODULATORS |
-
2000
- 2000-06-23 GB GBGB0015562.2A patent/GB0015562D0/en not_active Ceased
-
2001
- 2001-06-06 DO DO2001000187A patent/DOP2001000187A/en unknown
- 2001-06-07 IL IL15342701A patent/IL153427A0/en unknown
- 2001-06-07 AU AU62591/01A patent/AU781837B2/en not_active Ceased
- 2001-06-07 OA OA1200200386A patent/OA12293A/en unknown
- 2001-06-07 EA EA200201269A patent/EA005117B1/en not_active IP Right Cessation
- 2001-06-07 JP JP2002504223A patent/JP2004512263A/en not_active Withdrawn
- 2001-06-07 WO PCT/IB2001/001035 patent/WO2001098267A1/en not_active Application Discontinuation
- 2001-06-07 EP EP01936728A patent/EP1292574A1/en not_active Withdrawn
- 2001-06-07 AP APAP/P/2002/002698A patent/AP2002002698A0/en unknown
- 2001-06-07 PL PL01365956A patent/PL365956A1/en not_active Application Discontinuation
- 2001-06-07 CN CNA018116086A patent/CN1639121A/en active Pending
- 2001-06-07 HU HU0301228A patent/HUP0301228A3/en unknown
- 2001-06-07 CZ CZ20023967A patent/CZ20023967A3/en unknown
- 2001-06-07 MX MXPA02012878A patent/MXPA02012878A/en unknown
- 2001-06-07 CA CA002412188A patent/CA2412188A1/en not_active Abandoned
- 2001-06-07 KR KR1020027017503A patent/KR20040002386A/en not_active Application Discontinuation
- 2001-06-07 DZ DZ013368A patent/DZ3368A1/en active
- 2001-06-07 YU YU91802A patent/YU91802A/en unknown
- 2001-06-07 SK SK1717-2002A patent/SK17172002A3/en unknown
- 2001-06-07 BR BR0111867-6A patent/BR0111867A/en not_active IP Right Cessation
- 2001-06-07 NZ NZ523141A patent/NZ523141A/en unknown
- 2001-06-12 PA PA20018519401A patent/PA8519401A1/en unknown
- 2001-06-21 UY UY26787A patent/UY26787A1/en not_active Application Discontinuation
- 2001-06-21 PE PE2001000604A patent/PE20020253A1/en not_active Application Discontinuation
- 2001-06-21 AR ARP010102957A patent/AR028969A1/en unknown
- 2001-06-22 TN TNTNSN01094A patent/TNSN01094A1/en unknown
- 2001-07-06 UA UA20021210406A patent/UA73176C2/en unknown
-
2002
- 2002-11-28 BG BG107329A patent/BG107329A/en unknown
- 2002-11-28 IS IS6637A patent/IS6637A/en unknown
- 2002-12-12 HR HR20020998A patent/HRP20020998A2/en not_active Application Discontinuation
- 2002-12-16 MA MA26955A patent/MA26915A1/en unknown
- 2002-12-19 ZA ZA200210278A patent/ZA200210278B/en unknown
- 2002-12-20 NO NO20026168A patent/NO20026168L/en not_active Application Discontinuation
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| FD9A | Lapse of provisional protection due to non-payment of fees |