KR880009934A - 피리딘-2,4-및 2,5-디카복실산 유도체, 이의 제조방법, 이의 용도 및 이들 화합물을 기본으로 하는 약제 - Google Patents
피리딘-2,4-및 2,5-디카복실산 유도체, 이의 제조방법, 이의 용도 및 이들 화합물을 기본으로 하는 약제 Download PDFInfo
- Publication number
- KR880009934A KR880009934A KR1019880001197A KR880001197A KR880009934A KR 880009934 A KR880009934 A KR 880009934A KR 1019880001197 A KR1019880001197 A KR 1019880001197A KR 880001197 A KR880001197 A KR 880001197A KR 880009934 A KR880009934 A KR 880009934A
- Authority
- KR
- South Korea
- Prior art keywords
- amino acid
- compound
- collagen
- formula
- terminus
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title claims 11
- 239000003795 chemical substances by application Substances 0.000 title 1
- 238000002360 preparation method Methods 0.000 title 1
- 235000008206 alpha-amino acids Nutrition 0.000 claims 11
- 150000001370 alpha-amino acid derivatives Chemical class 0.000 claims 8
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 102000008186 Collagen Human genes 0.000 claims 3
- 108010035532 Collagen Proteins 0.000 claims 3
- 230000015572 biosynthetic process Effects 0.000 claims 3
- 229920001436 collagen Polymers 0.000 claims 3
- 230000004060 metabolic process Effects 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 239000000126 substance Substances 0.000 claims 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- WJJMNDUMQPNECX-UHFFFAOYSA-N dipicolinic acid Chemical compound OC(=O)C1=CC=CC(C(O)=O)=N1 WJJMNDUMQPNECX-UHFFFAOYSA-N 0.000 claims 2
- 238000006460 hydrolysis reaction Methods 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 102000008490 2-Oxoglutarate 5-Dioxygenase Procollagen-Lysine Human genes 0.000 claims 1
- 108010020504 2-Oxoglutarate 5-Dioxygenase Procollagen-Lysine Proteins 0.000 claims 1
- ONIBWKKTOPOVIA-UHFFFAOYSA-N Proline Natural products OC(=O)C1CCCN1 ONIBWKKTOPOVIA-UHFFFAOYSA-N 0.000 claims 1
- 102000004079 Prolyl Hydroxylases Human genes 0.000 claims 1
- 108010043005 Prolyl Hydroxylases Proteins 0.000 claims 1
- 150000001408 amides Chemical group 0.000 claims 1
- 150000008064 anhydrides Chemical class 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 239000007795 chemical reaction product Substances 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 239000000835 fiber Substances 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 230000007062 hydrolysis Effects 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 229960003444 immunosuppressant agent Drugs 0.000 claims 1
- 230000001861 immunosuppressant effect Effects 0.000 claims 1
- 239000003018 immunosuppressive agent Substances 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/81—Amides; Imides
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- 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
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/81—Amides; Imides
- C07D213/82—Amides; Imides in position 3
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Immunology (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Bidet-Like Cleaning Device And Other Flush Toilet Accessories (AREA)
- Adhesives Or Adhesive Processes (AREA)
- Treatment And Processing Of Natural Fur Or Leather (AREA)
Abstract
내용 없음.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (11)
- 일반식(Ⅰ)의 피리딘-2, 4- 또는 -2, 5- 디카복실산 유도체 및 이의 생리학적으로 허용되는 염.상기식에서, R1은 N-말단에 결합되는 α-아미노산 또는 α아미노산 알킬 에스테르 또는 α-아미노산 아미드-또는 α-아미노산 알킬-또는 디알킬 아미드(여기서, 언급한 알킬 래디칼은 탄소수 1 내지 4이며, 페닐에 의해 임의로 일치환되고, 또는 C3- 및 C4알킬 래디칼은 측쇄일 수 있다)를 나타내거나, R1은 N-말단에 결합되는 디-또는 트리펩타이드를 나타낸다.
- 제1항에 있어서, R1이 N-말단에 결합되는 α-아미노산 또는 α-아미노산 알킬 에스테르(여기서, 알킬 래디칼은 탄소수 1 내지 3이며, 페닐에 의해 임의로 일치환되고, 또한 C3-알킬 래디칼은 측쇄일 수 있다)를 나타내는 일반식(Ⅰ)의 피리딘-2, 4- 또는 -2, 5-디카복실산 유도체 및 이의 생리학적으로 허용되는 염.
- 일반식(Ⅱ)의 화합물을 일반식(Ⅲ)의 화합물과 반응시키고, 경우에 따라, 반응 생성물을 이의 생리학적으로 허용되는 염으로 전환시킴을 특징으로 하여, 일반식(Ⅰ)의 피리딘-2, 4-또는 -2, 5-디카복실산 유도체를 제조하는 방법.상기식에서, R1은 N-말단에 결합되는 α-아미노산 또는 α-아미노산 알킬 에스테르 또는 α-아미노산 아미드, 또는 α-아미노산 알킬-또는 디알킬아미드 (여기서, 언급한 알킬 래디칼은 탄소수 1 내지 4이며, 페닐에 의해 임의로 일치환되고, 또한 C3- 및 C4-알킬 래디칼은 측쇄일 수 있다)를 나타내거나, R1은 N-말단에 결합되는 디- 또는 트리펩타이드를 나타내고, Y는 할로겐 또는 하이드록실이거나, 카보닐 그룹과 함게 활성에스테르 또는 무수물을 형성한다. (여기서, R1이 N-말단에 결합되는 디- 또는 트리펩타이드 또는 α-아미노산인 경우, 존재하는 유리 카복실 그룹(들)은 임의로 보호되며, 임의로 존재하는 이(들) 보호그룹(들)은 가수분해 또는 가수소분해 반응후에 제거되어 유리 카복실 그룹(들)을 형성한다).
- 제3항에 있어서, 디알킬 래디칼이 탄소수 1 내지 8이며, C3-C8화합물이 경우에 측쇄이거나 환상일 수 있는 디알킬카보디이미드를 동시에 첨가하여 반응를 수행하는 방법.
- 제1항 또는 2항에 있어서, 프롤린 및 라이신 하이드록실라제를 억제하기 위한 화합물.
- 제1항 또는 2항에 있어서, 섬유억제제 및 면역억제제로서 사용하기 위한 화합물.
- 일반식(Ⅰ)의 화합물로 구성된 약제.
- 약제학적으로 허용되는 부형제와 함께 일반식(Ⅰ)의 화합물을 함유하는 약제.
- 콜라겐 및 콜라겐-유사 물질의 대사와 Clg의 생합성에 영향을 미치기 위한 일반식(Ⅰ) 화합물의 용도.
- 콜라겐 및 콜라겐-유사 물질의 대사와 Clg의 생합성에 장애를 치료하기 위한 일반식(Ⅰ) 화합물의 용도.
- 일반식(Ⅰ)의 화합물을 약제에 혼입시킴을 특징으로 하여, 콜라겐 및 콜라겐-유사물질의 대사와 Clg의 생합성에 영향을 미치는 약제를 제조하는 방법.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DEP3703962.8 | 1987-02-10 | ||
| DE19873703962 DE3703962A1 (de) | 1987-02-10 | 1987-02-10 | Pyridin-2,4- und 2,5-dicarbonsaeure-derivate, verfahren zu ihrer herstellung, verwendung derselben sowie arzneimittel auf basis dieser verbindungen |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR880009934A true KR880009934A (ko) | 1988-10-05 |
| KR960004861B1 KR960004861B1 (en) | 1996-04-16 |
Family
ID=6320592
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR88001197A KR960004861B1 (en) | 1987-02-10 | 1988-02-09 | Pyridine-2,4-and 2,5-dicarboxylic-acid derivatives, a process for their preparation, their use and medicament |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US4968670A (ko) |
| EP (1) | EP0278454B1 (ko) |
| JP (1) | JPS63216871A (ko) |
| KR (1) | KR960004861B1 (ko) |
| AT (1) | ATE85048T1 (ko) |
| AU (1) | AU604293B2 (ko) |
| CA (1) | CA1315471C (ko) |
| DE (2) | DE3703962A1 (ko) |
| DK (1) | DK168008B1 (ko) |
| ES (1) | ES2046218T3 (ko) |
| FI (1) | FI90767C (ko) |
| GR (1) | GR3007607T3 (ko) |
| HU (1) | HU199801B (ko) |
| IE (1) | IE62353B1 (ko) |
| IL (1) | IL85360A0 (ko) |
| NO (1) | NO174852C (ko) |
| NZ (1) | NZ223432A (ko) |
| PH (1) | PH24512A (ko) |
| PT (1) | PT86735B (ko) |
| ZA (1) | ZA88895B (ko) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3707429A1 (de) * | 1987-03-07 | 1988-09-15 | Hoechst Ag | Substituierte pyridin-2,4-dicarbonsaeure-derivate, verfahren zu ihrer herstellung, verwendung derselben sowie arzneimittel auf basis dieser verbindungen |
| DE3924093A1 (de) * | 1989-07-20 | 1991-02-07 | Hoechst Ag | N,n'-bis(alkoxy-alkyl)-pyridin-2,4-dicarbonsaeurediamide, verfahren zu deren herstellung sowie deren verwendung |
| US5425289A (en) * | 1993-10-21 | 1995-06-20 | Snap-On Incorporated | Bung tool |
| DE3938805A1 (de) * | 1989-11-23 | 1991-05-29 | Hoechst Ag | Pyridin-2,4- und 2,5-dicarbonsaeurediamide, verfahren zu deren herstellung sowie deren verwendung |
| DE4020570A1 (de) | 1990-06-28 | 1992-01-02 | Hoechst Ag | 2,4- und 2,5-substituierte pyridin-n-oxide, verfahren zu deren herstellung sowie deren verwendung |
| DE4031000A1 (de) * | 1990-10-01 | 1992-04-09 | Hoechst Ag | 4- oder 5-substituierte pyridin-2-carbonsaeuren, verfahren zu deren herstellung sowie deren verwendung als arzneimittel |
| YU9492A (sh) * | 1991-02-05 | 1995-03-27 | Hoechst Ag. | 2,4- i 2,5-bis-tetrazolilni piridini i postupak za njihovo dobijanje |
| EP0548883A1 (de) * | 1991-12-24 | 1993-06-30 | Hoechst Aktiengesellschaft | Substituierte Pyridin-N-oxide, Verfahren zu ihrer Herstellung sowie ihre Verwendung als Arzneimittel |
| TW352384B (en) * | 1992-03-24 | 1999-02-11 | Hoechst Ag | Sulfonamido- or sulfonamidocarbonylpyridine-2-carboxamides, process for their preparation and their use as pharmaceuticals |
| DE4233124A1 (de) * | 1992-10-02 | 1994-04-07 | Hoechst Ag | Acylsulfonamido- und Sulfonamidopyridin-2-carbonsäureester sowie ihre Pyridin-N-oxide, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
| WO1999021860A1 (en) * | 1997-10-24 | 1999-05-06 | Fibrogen, Inc. | Phenanthroline derivatives |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3432094A1 (de) * | 1984-08-31 | 1986-03-06 | Hoechst Ag, 6230 Frankfurt | Ester der pyridin-2,4- und -2,5- dicarbonsaeure als arzneimittel zur inhibierung der prolin- und lysinhydroxylase |
| DE58908519D1 (de) * | 1988-08-04 | 1994-11-24 | Hoechst Ag | Verbessertes Verfahren zur Herstellung von N,N-Bis(alkoxyalkyl)-pyridin -2,4-dicarbonsäurediamiden. |
-
1987
- 1987-02-10 DE DE19873703962 patent/DE3703962A1/de not_active Withdrawn
-
1988
- 1988-02-08 ES ES198888101793T patent/ES2046218T3/es not_active Expired - Lifetime
- 1988-02-08 US US07/153,440 patent/US4968670A/en not_active Expired - Fee Related
- 1988-02-08 AT AT88101793T patent/ATE85048T1/de not_active IP Right Cessation
- 1988-02-08 FI FI880555A patent/FI90767C/fi not_active IP Right Cessation
- 1988-02-08 PH PH36468A patent/PH24512A/en unknown
- 1988-02-08 EP EP88101793A patent/EP0278454B1/de not_active Expired - Lifetime
- 1988-02-08 DE DE8888101793T patent/DE3877778D1/de not_active Expired - Fee Related
- 1988-02-08 IL IL85360A patent/IL85360A0/xx not_active IP Right Cessation
- 1988-02-08 NZ NZ223432A patent/NZ223432A/en unknown
- 1988-02-09 CA CA000558495A patent/CA1315471C/en not_active Expired - Fee Related
- 1988-02-09 NO NO880557A patent/NO174852C/no unknown
- 1988-02-09 JP JP63026722A patent/JPS63216871A/ja active Pending
- 1988-02-09 IE IE35188A patent/IE62353B1/en not_active IP Right Cessation
- 1988-02-09 PT PT86735A patent/PT86735B/pt not_active IP Right Cessation
- 1988-02-09 DK DK066188A patent/DK168008B1/da not_active IP Right Cessation
- 1988-02-09 KR KR88001197A patent/KR960004861B1/ko active IP Right Grant
- 1988-02-09 ZA ZA880895A patent/ZA88895B/xx unknown
- 1988-02-09 AU AU11451/88A patent/AU604293B2/en not_active Ceased
- 1988-02-10 HU HU88611A patent/HU199801B/hu not_active IP Right Cessation
-
1993
- 1993-04-09 GR GR930400360T patent/GR3007607T3/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US4968670A (en) | 1990-11-06 |
| KR960004861B1 (en) | 1996-04-16 |
| FI880555A0 (fi) | 1988-02-08 |
| NO880557L (no) | 1988-08-11 |
| FI90767B (fi) | 1993-12-15 |
| HU199801B (en) | 1990-03-28 |
| ATE85048T1 (de) | 1993-02-15 |
| FI880555A (fi) | 1988-08-11 |
| EP0278454B1 (de) | 1993-01-27 |
| HUT47251A (en) | 1989-02-28 |
| PT86735B (pt) | 1992-05-29 |
| AU1145188A (en) | 1988-08-11 |
| ZA88895B (en) | 1988-08-08 |
| ES2046218T3 (es) | 1994-02-01 |
| GR3007607T3 (ko) | 1993-08-31 |
| DK66188D0 (da) | 1988-02-09 |
| DE3877778D1 (de) | 1993-03-11 |
| DK168008B1 (da) | 1994-01-17 |
| NZ223432A (en) | 1990-04-26 |
| IE880351L (en) | 1988-08-10 |
| FI90767C (fi) | 1994-03-25 |
| NO880557D0 (no) | 1988-02-09 |
| CA1315471C (en) | 1993-03-30 |
| NO174852C (no) | 1994-07-20 |
| JPS63216871A (ja) | 1988-09-09 |
| PH24512A (en) | 1990-07-18 |
| IE62353B1 (en) | 1995-01-25 |
| EP0278454A2 (de) | 1988-08-17 |
| DE3703962A1 (de) | 1988-08-18 |
| NO174852B (no) | 1994-04-11 |
| AU604293B2 (en) | 1990-12-13 |
| DK66188A (da) | 1988-08-11 |
| IL85360A0 (en) | 1988-07-31 |
| PT86735A (pt) | 1988-03-01 |
| EP0278454A3 (en) | 1989-10-18 |
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