RU2403255C2 - 6,7-ненасыщенное 7-карбамоилзамещенное производное морфинана - Google Patents
6,7-ненасыщенное 7-карбамоилзамещенное производное морфинана Download PDFInfo
- Publication number
- RU2403255C2 RU2403255C2 RU2007148412/04A RU2007148412A RU2403255C2 RU 2403255 C2 RU2403255 C2 RU 2403255C2 RU 2007148412/04 A RU2007148412/04 A RU 2007148412/04A RU 2007148412 A RU2007148412 A RU 2007148412A RU 2403255 C2 RU2403255 C2 RU 2403255C2
- Authority
- RU
- Russia
- Prior art keywords
- optionally substituted
- compound
- lower alkyl
- solvate
- pharmaceutically acceptable
- Prior art date
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- 150000001875 compounds Chemical class 0.000 claims abstract description 196
- 125000000217 alkyl group Chemical group 0.000 claims abstract description 116
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract description 68
- 239000001257 hydrogen Substances 0.000 claims abstract description 68
- 125000003545 alkoxy group Chemical group 0.000 claims abstract description 45
- 230000000694 effects Effects 0.000 claims abstract description 42
- 150000003839 salts Chemical class 0.000 claims abstract description 40
- 239000012453 solvate Substances 0.000 claims abstract description 37
- 206010047700 Vomiting Diseases 0.000 claims abstract description 36
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims abstract description 35
- 230000008673 vomiting Effects 0.000 claims abstract description 34
- 206010010774 Constipation Diseases 0.000 claims abstract description 32
- 206010028813 Nausea Diseases 0.000 claims abstract description 28
- 230000008693 nausea Effects 0.000 claims abstract description 28
- 125000003342 alkenyl group Chemical group 0.000 claims abstract description 27
- 238000011282 treatment Methods 0.000 claims abstract description 16
- 230000002265 prevention Effects 0.000 claims abstract description 11
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims abstract description 8
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims abstract description 8
- 125000003107 substituted aryl group Chemical group 0.000 claims abstract description 7
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 4
- 125000000623 heterocyclic group Chemical group 0.000 claims description 47
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- 150000002431 hydrogen Chemical class 0.000 claims description 33
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- 125000000753 cycloalkyl group Chemical group 0.000 claims description 29
- 238000000034 method Methods 0.000 claims description 28
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- 102000003840 Opioid Receptors Human genes 0.000 claims description 24
- 108090000137 Opioid Receptors Proteins 0.000 claims description 24
- 125000003118 aryl group Chemical group 0.000 claims description 20
- 125000002252 acyl group Chemical group 0.000 claims description 17
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims description 16
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- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 12
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- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 12
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 12
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- 229910052757 nitrogen Inorganic materials 0.000 claims description 11
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- 230000002829 reductive effect Effects 0.000 description 9
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- 239000008187 granular material Substances 0.000 description 7
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- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 6
- MBBZMMPHUWSWHV-BDVNFPICSA-N N-methylglucamine Chemical compound CNC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO MBBZMMPHUWSWHV-BDVNFPICSA-N 0.000 description 6
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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 description 6
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- GNWBLLYJQXKPIP-ZOGIJGBBSA-N (1s,3as,3bs,5ar,9ar,9bs,11as)-n,n-diethyl-6,9a,11a-trimethyl-7-oxo-2,3,3a,3b,4,5,5a,8,9,9b,10,11-dodecahydro-1h-indeno[5,4-f]quinoline-1-carboxamide Chemical compound CN([C@@H]1CC2)C(=O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H](C(=O)N(CC)CC)[C@@]2(C)CC1 GNWBLLYJQXKPIP-ZOGIJGBBSA-N 0.000 description 4
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- 125000002221 trityl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C([*])(C1=C(C(=C(C(=C1[H])[H])[H])[H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 description 1
- 125000003774 valeryl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
- 229920002554 vinyl polymer Polymers 0.000 description 1
- 210000001835 viscera Anatomy 0.000 description 1
- 208000030401 vitamin deficiency disease Diseases 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
- 125000001834 xanthenyl group Chemical group C1=CC=CC=2OC3=CC=CC=C3C(C12)* 0.000 description 1
- 239000000811 xylitol Substances 0.000 description 1
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 1
- 229960002675 xylitol Drugs 0.000 description 1
- 235000010447 xylitol Nutrition 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
- C07D489/06—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with a hetero atom directly attached in position 14
- C07D489/08—Oxygen atom
-
- 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
- A61K31/435—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
- A61K31/485—Morphinan derivatives, e.g. morphine, codeine
-
- 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
- A61P1/10—Laxatives
-
- 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
- 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)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Hospice & Palliative Care (AREA)
- Otolaryngology (AREA)
- Emergency Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2005151864 | 2005-05-25 | ||
| JP2005-151864 | 2005-05-25 | ||
| JP2006/065762 | 2006-03-10 | ||
| JP2006065762 | 2006-03-10 | ||
| JPPCT/JP2006/310231 | 2006-05-23 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2007148412A RU2007148412A (ru) | 2009-06-27 |
| RU2403255C2 true RU2403255C2 (ru) | 2010-11-10 |
Family
ID=37451954
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2007148412/04A RU2403255C2 (ru) | 2005-05-25 | 2006-05-25 | 6,7-ненасыщенное 7-карбамоилзамещенное производное морфинана |
Country Status (20)
| Country | Link |
|---|---|
| US (4) | USRE46365E1 (OSRAM) |
| EP (1) | EP1889848B8 (OSRAM) |
| JP (1) | JP4323547B2 (OSRAM) |
| KR (1) | KR100912782B1 (OSRAM) |
| CN (1) | CN101228172B (OSRAM) |
| AU (1) | AU2006250390B2 (OSRAM) |
| BE (1) | BE2019C533I2 (OSRAM) |
| BR (1) | BRPI0610343B8 (OSRAM) |
| CA (1) | CA2609733C (OSRAM) |
| DK (1) | DK1889848T3 (OSRAM) |
| ES (1) | ES2525215T3 (OSRAM) |
| FR (1) | FR19C1042I2 (OSRAM) |
| HU (1) | HUS1900034I1 (OSRAM) |
| MX (1) | MX2007014588A (OSRAM) |
| NL (1) | NL300996I2 (OSRAM) |
| PL (1) | PL1889848T3 (OSRAM) |
| PT (1) | PT1889848E (OSRAM) |
| RU (1) | RU2403255C2 (OSRAM) |
| TW (1) | TWI311056B (OSRAM) |
| WO (2) | WO2006126529A1 (OSRAM) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006126529A1 (ja) | 2005-05-25 | 2006-11-30 | Shionogi & Co., Ltd. | ６，７－不飽和－７－カルバモイル置換モルヒナン誘導体 |
| US10512644B2 (en) | 2007-03-12 | 2019-12-24 | Inheris Pharmaceuticals, Inc. | Oligomer-opioid agonist conjugates |
| US8173666B2 (en) | 2007-03-12 | 2012-05-08 | Nektar Therapeutics | Oligomer-opioid agonist conjugates |
| EP3090743A1 (en) * | 2008-01-09 | 2016-11-09 | Charleston Laboratories, Inc. | Pharmaceutical compositions for treating headache and eliminating nausea |
| JP5252391B2 (ja) * | 2008-02-21 | 2013-07-31 | 学校法人北里研究所 | オキサビシクロ［２．２．２］オクタンを有するモルヒナン誘導体およびその医薬用途 |
| JP5827123B2 (ja) * | 2008-09-16 | 2015-12-02 | ウェルズ ファーゴ バンク ナショナル アソシエイション | 乱用の可能性が低いｐｅｇ化オピオイド |
| MX342548B (es) * | 2009-09-18 | 2016-10-04 | Merck Sharp & Dohme Corp * | Uso del antagonista del receptor opiaceo para los trastornos del tracto gastrointestinal. |
| US20130217672A1 (en) * | 2010-05-13 | 2013-08-22 | Green Cross Corporation | (+)-3-hydroxymorphinan-based polycycle derivatives |
| AU2011327113B9 (en) * | 2010-11-12 | 2015-07-30 | Shionogi & Co., Ltd. | Crystalline 6,7-unsaturated-7-carbamoyl morphinane derivative, and method for producing same |
| PL2851075T3 (pl) | 2012-05-14 | 2022-02-21 | Shionogi & Co., Ltd. | Preparat zawierający pochodną 6,7-nienasyconego-7-karbamoilomorfinanu |
| CA3048360C (en) * | 2016-12-26 | 2021-06-29 | Shionogi & Co., Ltd. | Production method for formulation having improved content uniformity |
| JP7365358B2 (ja) | 2018-04-12 | 2023-10-19 | モーフィック セラピューティック，インコーポレイテッド | ヒトインテグリンα４β７のアンタゴニスト |
| KR102201609B1 (ko) | 2019-04-19 | 2021-01-12 | 연성정밀화학(주) | 날데메딘의 제조방법 |
| TWI857592B (zh) | 2019-10-16 | 2024-10-01 | 美商莫菲克醫療股份有限公司 | 抑制人類整合素α4β7 |
| EP4062973A4 (en) | 2019-11-20 | 2023-11-29 | Shionogi & Co., Ltd | 6,7-unsaturated-7-carbamoyl morphinan derivative-containing solid formulation |
| CN111905111B (zh) * | 2020-09-16 | 2023-03-31 | 地奥集团成都药业股份有限公司 | 一种评价复方谷氨酰胺组方对腹泻型肠易激综合征疗效的方法 |
| IT202300009864A1 (it) | 2023-05-16 | 2024-11-16 | Procos Spa | Processo per la preparazione di naldemedina |
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| SU1508960A3 (ru) * | 1984-07-05 | 1989-09-15 | Е.И.Дюпон Де Немур Энд Компани (Фирма) | Способ получени производных бензоатных эфиров 3-оксиморфинанов |
| US20010047005A1 (en) * | 1999-09-29 | 2001-11-29 | Farrar John J. | Novel methods and compositions involving opioids and antagonists thereof |
| WO2004007503A1 (ja) * | 2002-07-11 | 2004-01-22 | Toray Industries, Inc. | 悪心・嘔吐の治療または予防剤 |
| RU2004108210A (ru) * | 2001-08-23 | 2005-04-10 | Акцо Нобель Н.В. (NL) | C-14 окисление производных морфина |
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| US4272541A (en) | 1978-06-02 | 1981-06-09 | Miles Laboratories, Inc. | 7,8 and 7-8 Substituted 4,5α-epoxymorphinan-6-one compounds, and methods of treating pain and drug dependence with them |
| US4275205A (en) | 1980-05-05 | 1981-06-23 | Miles Laboratories, Inc. | 7,7-Ditosyloxymethyl-4,5α-epoxy-morphinan-6-ols |
| US4347361A (en) | 1980-12-10 | 1982-08-31 | Sisa, Incorporated | 4,5α-Epoxy-3-hydroxy or methoxy-7-(1-hydroxy-alkyl or 1-oxoalkyl)morphinan-6-one compounds |
| US4370333A (en) | 1981-06-29 | 1983-01-25 | Sisa, Incorporated | 17-Cyclopropylmethyl-3-hydroxy-14-methoxy 7α-methyl-morphinan-6-one and therapeutic method of treating pain with it |
| US4443605A (en) | 1982-07-30 | 1984-04-17 | Miles Laboratories, Inc. | 7β-Arylalkyl-6α, 7 α-oxymethylene-3-methoxy or 3-hydroxy-4, 5α-epoxy-17 methyl or 17-cycloalkyl-methyl morphinans |
| US4440932A (en) | 1982-09-09 | 1984-04-03 | Miles Laboratories, Inc. | 7β-Arylalkyl-7α-methyl-6-oxo or 6α-hydroxy-3-methoxy or 3-hydroxy-4,5α-epoxy-17-methyl or 17-cycloalkyl-methylmorphinans |
| DE69424853T2 (de) | 1993-07-23 | 2000-10-05 | Toray Industries, Inc. | Morphinan-derivate und ihre medizinische verwendung |
| US5464841A (en) | 1993-11-08 | 1995-11-07 | Univ Minnesota | Use of delta opioid receptor antagonists to treat immunoregulatory disorders |
| ES2188888T3 (es) | 1996-01-10 | 2003-07-01 | Glaxosmithkline Spa | Derivados morfinoides 8ii) con condensados con heterociclos. |
| AU5891600A (en) | 1999-07-01 | 2001-01-22 | Chemrx Advanced Technologies, Inc. | Process for synthesizing oxadiazoles |
| JP2003528819A (ja) * | 1999-11-29 | 2003-09-30 | アドラー コーポレーション | オピオイドおよびそのアンタゴニストに関する新規方法および組成物 |
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| US20040024004A1 (en) | 2001-05-04 | 2004-02-05 | Sherman Barry M. | Novel compositions and methods for enhancing potency or reducing adverse side effects of opioid agonists |
| EP1280529A2 (en) * | 2000-05-05 | 2003-02-05 | Pain Therapeutics, Inc. | Opioid antagonist containing composition for enhancing the potency or reducing adverse side effects of opioid agonists |
| DE60133584T2 (de) * | 2000-10-31 | 2009-06-04 | Rensselaer Polytechnic Institute | 4-arylpiperidine als opioidrezeptorbindende agenzien |
| AU2408602A (en) | 2000-11-22 | 2002-06-03 | Toray Industries | Indole derivatives and use thereof in medicines |
| DE10161963A1 (de) | 2001-12-17 | 2003-07-03 | Johannes Schuetz | 6-Aminomorphinanderivate, Herstellungsverfahren dafür und deren Verwendung |
| DE10229842A1 (de) * | 2002-07-03 | 2004-02-05 | Helmut Prof. Dr. Schmidhammer | Morphinanderivate und deren quartäre Ammoniumsalze substituiert in Position 14, Herstellungsverfahren und Verwendung |
| WO2004026819A2 (en) | 2002-09-18 | 2004-04-01 | The Curators Of The University Of Missouri | OPIATE ANALOGS SELECTIVE FOR THE delta-OPIOID RECEPTOR |
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| JP5266492B2 (ja) | 2004-05-28 | 2013-08-21 | ヒューマン バイオモレキュラル リサーチ インスティテュート | 代謝安定性鎮痛薬、疼痛薬物療法及び他の物質の合成 |
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-
2006
- 2006-05-23 WO PCT/JP2006/310231 patent/WO2006126529A1/ja not_active Ceased
- 2006-05-24 TW TW095118443A patent/TWI311056B/zh active
- 2006-05-25 MX MX2007014588A patent/MX2007014588A/es active IP Right Grant
- 2006-05-25 PT PT67468330T patent/PT1889848E/pt unknown
- 2006-05-25 BR BRPI0610343A patent/BRPI0610343B8/pt not_active IP Right Cessation
- 2006-05-25 WO PCT/JP2006/310454 patent/WO2006126637A1/ja not_active Ceased
- 2006-05-25 DK DK06746833.0T patent/DK1889848T3/en active
- 2006-05-25 ES ES06746833.0T patent/ES2525215T3/es active Active
- 2006-05-25 US US15/064,511 patent/USRE46365E1/en active Active
- 2006-05-25 EP EP06746833.0A patent/EP1889848B8/en active Active
- 2006-05-25 AU AU2006250390A patent/AU2006250390B2/en not_active Ceased
- 2006-05-25 US US11/920,851 patent/US8084460B2/en not_active Ceased
- 2006-05-25 CN CN2006800271187A patent/CN101228172B/zh active Active
- 2006-05-25 PL PL06746833T patent/PL1889848T3/pl unknown
- 2006-05-25 RU RU2007148412/04A patent/RU2403255C2/ru active
- 2006-05-25 JP JP2007517895A patent/JP4323547B2/ja active Active
- 2006-05-25 CA CA2609733A patent/CA2609733C/en active Active
-
2007
- 2007-11-23 KR KR1020077027287A patent/KR100912782B1/ko active Active
-
2011
- 2011-11-30 US US13/308,483 patent/US8536192B2/en not_active Ceased
-
2016
- 2016-03-08 US US15/064,538 patent/USRE46375E1/en active Active
-
2019
- 2019-06-20 FR FR19C1042C patent/FR19C1042I2/fr active Active
- 2019-06-24 BE BE2019C533C patent/BE2019C533I2/nl unknown
- 2019-06-26 NL NL300996C patent/NL300996I2/nl unknown
- 2019-07-03 HU HUS1900034C patent/HUS1900034I1/hu unknown
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
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| SU1508960A3 (ru) * | 1984-07-05 | 1989-09-15 | Е.И.Дюпон Де Немур Энд Компани (Фирма) | Способ получени производных бензоатных эфиров 3-оксиморфинанов |
| US20010047005A1 (en) * | 1999-09-29 | 2001-11-29 | Farrar John J. | Novel methods and compositions involving opioids and antagonists thereof |
| RU2004108210A (ru) * | 2001-08-23 | 2005-04-10 | Акцо Нобель Н.В. (NL) | C-14 окисление производных морфина |
| WO2004007503A1 (ja) * | 2002-07-11 | 2004-01-22 | Toray Industries, Inc. | 悪心・嘔吐の治療または予防剤 |
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