2-(苯基硫代)乙脒盐酸盐 - CAS号 84544-86-5

物化性质

熔点：

175 °C

计算性质

辛醇/水分配系数(LogP)：

1.03
重原子数：

12
可旋转键数：

3
环数：

1.0
sp3杂化的碳原子比例：

0.125
拓扑面积：

75.2
氢给体数：

3
氢受体数：

2

安全信息

危险品标志：

Xn
安全说明：

S26,S36/37/39
危险类别码：

R20/21/22,R36/37/38
海关编码：

2930909090

SDS

SDS：498149dd1738145aefdff64e0be52feb

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Name:	2-(Phenylthio)ethanimidamide hydrochloride 97% Material Safety Data Sheet
Synonym:	2-Phenylthioacetamidine hydrochlorid
CAS:	84544-86-5

Section 1 - Chemical Product MSDS Name:2-(Phenylthio)ethanimidamide hydrochloride 97% Material Safety Data Sheet
Synonym:2-Phenylthioacetamidine hydrochlorid

Section 2 - COMPOSITION, INFORMATION ON INGREDIENTS

CAS#	Chemical Name	content	EINECS#
84544-86-5	2-(Phenylthio)ethanimidamide hydrochlo	97%	unlisted

Hazard Symbols: XN
Risk Phrases: 20/21/22 36/37/38

Section 3 - HAZARDS IDENTIFICATION
EMERGENCY OVERVIEW
Harmful by inhalation, in contact with skin and if swallowed.
Irritating to eyes, respiratory system and skin.
Potential Health Effects
Eye:
Causes eye irritation.
Skin:
Causes skin irritation. Harmful if absorbed through the skin.
Ingestion:
Harmful if swallowed. May cause irritation of the digestive tract.
Inhalation:
Harmful if inhaled. Causes respiratory tract irritation.
Chronic:
Not available.

Section 4 - FIRST AID MEASURES
Eyes: Flush eyes with plenty of water for at least 15 minutes, occasionally lifting the upper and lower eyelids. Get medical aid.
Skin:
Get medical aid. Flush skin with plenty of water for at least 15 minutes while removing contaminated clothing and shoes.
Ingestion:
Get medical aid. Wash mouth out with water.
Inhalation:
Remove from exposure and move to fresh air immediately. If not breathing, give artificial respiration. If breathing is difficult, give oxygen. Get medical aid.
Notes to Physician:

Section 5 - FIRE FIGHTING MEASURES
General Information:
As in any fire, wear a self-contained breathing apparatus in pressure-demand, MSHA/NIOSH (approved or equivalent), and full protective gear.
Extinguishing Media:
Use water spray, dry chemical, carbon dioxide, or chemical foam.

Section 6 - ACCIDENTAL RELEASE MEASURES
General Information: Use proper personal protective equipment as indicated in Section 8.
Spills/Leaks:
Vacuum or sweep up material and place into a suitable disposal container.

Section 7 - HANDLING and STORAGE
Handling:
Avoid breathing dust, vapor, mist, or gas. Avoid contact with skin and eyes.
Storage:
Store in a cool, dry place. Store in a tightly closed container.

Section 8 - EXPOSURE CONTROLS, PERSONAL PROTECTION
Engineering Controls:
Facilities storing or utilizing this material should be equipped with an eyewash facility and a safety shower. Use adequate ventilation to keep airborne concentrations low.
Exposure Limits CAS# 84544-86-5: Personal Protective Equipment Eyes: Not available.
Skin:
Wear appropriate protective gloves to prevent skin exposure.
Clothing:
Wear appropriate protective clothing to prevent skin exposure.
Respirators:
Follow the OSHA respirator regulations found in 29 CFR 1910.134 or European Standard EN 149. Use a NIOSH/MSHA or European Standard EN 149 approved respirator if exposure limits are exceeded or if irritation or other symptoms are experienced.

Section 9 - PHYSICAL AND CHEMICAL PROPERTIES

Physical State: Solid
Color: white crystalline solid
Odor: Not available.
pH: Not available.
Vapor Pressure: Not available.
Viscosity: Not available.
Boiling Point: Not available.
Freezing/Melting Point: 175 - 177 deg C
Autoignition Temperature: Not available.
Flash Point: Not available.
Explosion Limits, lower: Not available.
Explosion Limits, upper: Not available.
Decomposition Temperature:
Solubility in water:
Specific Gravity/Density:
Molecular Formula: C8H11ClN2S
Molecular Weight: 203

Section 10 - STABILITY AND REACTIVITY
Chemical Stability:
Not available.
Conditions to Avoid:
Incompatible materials.
Incompatibilities with Other Materials:
Oxidizing agents, bases, amines.
Hazardous Decomposition Products:
Hydrogen chloride, chlorine, nitrogen oxides, carbon monoxide, oxides of sulfur, carbon dioxide.
Hazardous Polymerization: Has not been reported

Section 11 - TOXICOLOGICAL INFORMATION
RTECS#:
CAS# 84544-86-5 unlisted.
LD50/LC50:
Not available.
Carcinogenicity:
2-(Phenylthio)ethanimidamide hydrochloride - Not listed by ACGIH, IARC, or NTP.

Section 12 - ECOLOGICAL INFORMATION

Section 13 - DISPOSAL CONSIDERATIONS
Dispose of in a manner consistent with federal, state, and local regulations.

Section 14 - TRANSPORT INFORMATION

IATA
No information available.
IMO
No information available.
RID/ADR
No information available.

Section 15 - REGULATORY INFORMATION

European/International Regulations
European Labeling in Accordance with EC Directives
Hazard Symbols: XN
Risk Phrases:
R 20/21/22 Harmful by inhalation, in contact with
skin and if swallowed.
R 36/37/38 Irritating to eyes, respiratory system
and skin.
Safety Phrases:
S 26 In case of contact with eyes, rinse immediately
with plenty of water and seek medical advice.
S 36/37/39 Wear suitable protective clothing, gloves
and eye/face protection.
WGK (Water Danger/Protection)
CAS# 84544-86-5: No information available.
Canada
None of the chemicals in this product are listed on the DSL/NDSL list.
CAS# 84544-86-5 is not listed on Canada's Ingredient Disclosure List.
US FEDERAL
TSCA
CAS# 84544-86-5 is not listed on the TSCA inventory.
It is for research and development use only.

SECTION 16 - ADDITIONAL INFORMATION
N/A

反应信息

作为反应物：

描述：

2-(苯基硫代)乙脒盐酸盐、 Z 2-cyano-3-methylsulfanyl-3-(1,2,4,5-tetrahydro-benzo[d]azepin-3-yl)-acrylic acid ethyl ester 、 1,8-二氮杂双环[5.4.0]十一碳-7-烯以 N,N-二甲基甲酰胺为溶剂，生成 6-oxo-2-phenylsulfanylmethyl-4-(1,2,4,5-tetrahydro-benzo[d]azepin-3-yl)-1,6-dihydro-pyrimidine-5-carbonitrile

参考文献：

名称：

1,2,4,5-Tetrahydro-benzo[D]azepin derivatives

摘要：

本发明涉及1,2,4,5-四氢苯并[d]氮杂环己烷衍生物，以及它们的药用盐，无论是它们的外消旋形式还是光学活性形式，这些化合物是代谢型谷氨酸受体拮抗剂，因此对于治疗与这些受体相关的疾病是有用的。

公开号：

US06218385B1

点击查看最新优质反应信息

文献信息

Haloalkylguanidine compounds, pharmaceutical compositions and methods,

申请人：Imperial Chemical Industries PLC

公开号：US04447441A1

公开（公告）日：1984-05-08

The invention relates to guanidine derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. According to the invention there is provided a guanidine derivative of the formula I:- ##STR1## in which R.sup.1 and R.sup.2, same or different, are hydrogen or 1-10C alkyl, 3-8C cycloalkyl or 4-14C cycloalkylalkyl, each alkyl, cycloalkyl or cycloalkylalkyl optionally carrying one or more F, Cl or Br atoms, provided that one of R.sup.1 and R.sup.2 is halogen substituted, or R.sup.2 is hydrogen and R.sup.1 is R.sup.5 --E--W in which W is 2-6C alkylene optionally substituted by 1 or 2 1-4C alkyls, E is O,S or NR.sup.6 in which R.sup.6 is H or 1-6C alkyl, R.sup.5 is H or 1-6C alkyl optionally substituted by 1 or 2 1-4C alkyls, or R.sup.5 and R.sup.6 are joined to form a pyrrolidine, piperidine, morpholine, piperazine or N-methylpiperazine ring; ring X is a heterocyclic ring as defined in the specification; A is phenylene or 5-7C cycloalkylene, or a 1-8C alkylene into which is optionally inserted one or two groups; D is O or S; and R.sup.3 and R.sup.4 are hydrogen or a variety of radicals described in the specification: and the pharmaceutically-acceptable acid-addition salts thereof. Manufacturing processes and pharmaceutical compositions are also described.

该发明涉及胍基衍生物，它们是组胺H-2拮抗剂，能抑制胃酸分泌。根据该发明，提供了一种符合以下式I的胍基衍生物：- ##STR1## 其中R.sup.1和R.sup.2，相同或不同，是氢或1-10碳原子的烷基，3-8碳原子的环烷基或4-14碳原子的环烷基烷基，每个烷基、环烷基或环烷基烷基可选地携带一个或多个F、Cl或Br原子，前提是R.sup.1和R.sup.2中的一个是卤素取代的，或者R.sup.2是氢而R.sup.1是R.sup.5--E--W，其中W是可选地由1或2个1-4碳原子的烷基取代的2-6碳原子的亚烷基，E是O、S或NR.sup.6，其中R.sup.6是H或1-6碳原子的烷基，R.sup.5是H或1-6碳原子的烷基，可选地由1或2个1-4碳原子的烷基取代，或者R.sup.5和R.sup.6连接形成吡咯烷、哌啶、吗啉、哌嗪或N-甲基哌嗪环；环X是规范中定义的杂环；A是苯基或5-7碳原子的环烷基，或者可选地插入一到两个基团的1-8碳原子的亚烷基；D是O或S；R.sup.3和R.sup.4是氢或规范中描述的各种基团；以及其药用可接受的酸加盐。还描述了制造工艺和药物组合物。
Guanidine derivatives

申请人：IMPERIAL CHEMICAL INDUSTRIES PLC

公开号：EP0060094A2

公开（公告）日：1982-09-15

The invention relates to guanidine derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. According to the invention where is provided a guanidine derivative of the formula I:- in which R' and R2, same or different, are hydrogen or 1-10C alkyl, 3-8C cycloalkyl or 4-14C cycloalkylalkyl, each alkyl, cycloalkyl or cycloalkylalkyl optionally carrying one or more F. Cl or Br atoms, provided that one of R' and R2 is halogen substituted, or R2 is hydrogen and R' is R5-E-W in which W is 2-6C alkylene optionally substituted by 1 or 2 1-4C alkyls, E is O,S or NR5 in which R6 is H or 1-6C alkyl, R5 is H or 1-6C alkyl optionally substituted by 1 or 2 1-4C alkyls, or R5 and R6 are joined to form a pyrrolidine, piperidine, morpholine, piperazine or N-methylpiperazine ring;t ring X is a heterocyclic ring as defined in the specification; A is phenylene or 5-7C cycloalkylene, or a 1-SC alkylene into which is optionally inserted one or two groups; D is 0 or S; and R3 and R4 are hydrogen or a variety of radicals described in the specification: and the pharmaceutically-acceptable acid-addition salts thereof. Manufacturing processes and pharmaceutical compositions are also described.

本发明涉及组胺 H-2 拮抗剂和抑制胃酸分泌的胍衍生物。根据本发明提供了一种式 I 的胍衍生物其中R'和R2，相同或不同，为氢或1-10C烷基、3-8C环烷基或4-14C环烷基烷基，每个烷基、环烷基或环烷基烷基可选带一个或多个F.Cl或Br原子，条件是R'和R2中的一个被卤素取代，或R2是氢，R'是R5-E-W，其中W是任选被1或2个1-4C烷基取代的2-6C亚烷基，E是O、S或NR5，其中R6是H或1-6C烷基，R5是H或任选被1或2个1-4C烷基取代的1-6C烷基，或R5和R6连接形成吡咯烷、哌啶、吗啉、哌嗪或N-甲基哌嗪环；t 环 X 是本说明书中定义的杂环；A 是亚苯基或 5-7C 环亚烷基，或 1-SC 亚烷基，其中可选择插入一个或两个基团；D 是 0 或 S；R3 和 R4 是氢或本说明书中描述的各种基：及其药学上可接受的酸加成盐。还描述了制造工艺和药物组合物。
Tetrahydro-benzo(d)azepines and their use as antagonists at metabotropic glutamate receptors

申请人：F. HOFFMANN-LA ROCHE AG

公开号：EP1074549A2

公开（公告）日：2001-02-07

The present invention is concerned with 1,2,4,5-tetrahydro-benzo[d]azepin derivatives of the general formula wherein R1signifies hydrogen, lower alkyl, oxygen, halogen, or -OR, -O(C3-C6)cycloalkyl, -O(CHR)n-(C3-C6)cycloalkyl, -O(CHR)nCN, -O(CHR)nCF3, -O(CHR)(CHR)nNR2, -O(CHR)(CHR)nOR, -O(CHR)n-lower alkenyl, -OCF3, -OCF2-R, -OCF2-lower alkenyl, -OCHRF, -OCHF-lower alkenyl, -OCF2CRF2, -OCF2Br, -O(CHR)nCF2Br, -O(CHR)n-phenyl, wherein the phenyl group may be optionally substituted independently from each other by one to three lower alkyl, lower alkoxy, halogen, nitro or cyano groups, -O(CHR)(CHR)n-morpholino, -O(CHR)(CHR)n-pyrrolidino, -O(CHR)(CHR)n-piperidino, -O(CHR)(CHR)n-imidazolo, -O(CHR)(CHR)n-triazolo, -O(CHR)n-pyridino, -O(CHR)(CHR)n-OSi-lower alkyl, -O(CHR)(CHR)nOS(O)2-lower alkyl, -O(CH2)nCH=CF2, -O(CHR)n-2,2-dimethyl-[1.3]dioxolane, -O(CHR)n-CHOR-CH2OR, -O(CHR)n-CHOR-(CHR)n-CH2OR or -SR or -S(CHR)nCOOR, or -NR2, -N(R)(CHR)(CHR)nOR, -N(R)(CHR)nCF3, -N(R)(CHR)(CHR)n-morpholino, -N(R)(CHR)(CHR)n-imidazolo, -N(R)(CHR)(CHR)n-pyrrolidino, -N(R)(CHR)(CHR)n-pyrrolidin-2-one, -N(R)(CHR)(CHR)n-piperidino, -N(R)(CHR)(CHR)n-triazolo, -N(R)(CHR)n-pyridino, or nis 1-6; Rsignifies hydrogen, lower alkyl or lower alkenyl, independently from each other, if more than one R is present; R2signifies nitro or cyano; R3signifies hydrogen, lower alkyl, =O, =S, -SR, -S(O)2-lower alkyl, -(C3-C6)cycloalky or piperazino, optionally substituted by lower alkyl, or -CONR2, -(CHR)nCONR2, -(CHR)nOR, -(CH2)n-CF3, -CF3, -(CHR)nOC(O)CF3, -(CHR)nCOOR, -(CHR)nSC6H5, wherein the phenyl group may be optionally substituted independently from each other by one to three lower alkyl, lower alkoxy, halogen, nitro or cyano groups, -(CHR)n-1,3-dioxo-1,3-dihydro-isoindol, -(CHR)n-tetrahydro-pyran-2-yloxy or -(CHR)n-S-lower alkyl, or -NR2, -NRCO-lower alkyl, -NRCHO, -N(R)(CHR)nCN, -N(R)(CHR)nCF3, -N(R)(CHR)(CHR)n-OR, -N(R)C(O)(CHR)nO-lower alkyl, -NR(CHR)n-lower alkyl, -NR(CHR)(CHR)n-OR, -N(R)(CHR)(CHR)n-O-phenyl, wherein the phenyl group may be optionally substituted independently from each other by one to three lower alkyl, lower alkoxy, halogen, nitro or cyano groups, -N(R)(CHR)n-lower alkenyl, -N(R)(CHR)(CHR)n-O-(CHR)nOR, -N(R)(CHR)nC(O)O-lower alkyl, -N(R)(CHR)nC(O)NR-lower alkyl, -N(R)(CH2)n-2,2-dimethyl-[1.3]dioxolane, -N(R)(CHR)(CHR)nmorpholino, -N(R)(CHR)n-pyridino, -N(R)(CHR)(CHR)n-piperidino, -N(R)(CHR)(CHR)n-pyrrolidino, -N(R)(CHR)(CHR)n-O-pyridino, -N(R)(CHR)(CHR)nimidazolo, -N(R)(CHR)n-CR2-(CHR)n-OR, -N(R)(CHR)n-CR2-OR, -N(R)(CHR)n-CHOR-CH2OR, -N(R)(CHR)n-CHOR-(CHR)n-CH2OR, or -OR, -O(CHR)nCF3, -OCF3, -O(CHR)(CHR)n-O-phenyl, wherein the phenyl group may be optionally substituted independently from each other by one to three lower alkyl, lower alkoxy, halogen, nitro or cyano groups, -O(CHR)(CHR)n-O-lower alkyl, -O(CHR)n-pyridino or -O(CHR)(CHR)n-morpholino; and R4signifies hydrogen, lower alkyl, lower alkenyl or nitro, or -OR, -OCF3, -OCF2-R, -OCF2-lower alkenyl, -OCHRF, -OCHF-lower alkenyl, -O(CHR)nCF3, or -(CHR)nCHRF, -(CHR)nCF2R, -(CHR)nCF3, -(C3-C6)cycloalkyl, -(CHR)n(C3-C6)cycloalkyl, -(CHR)nCN, -(CHR)n-phenyl, wherein the phenyl group may be optionally substituted independently from each other by one to three lower alkyl, lower alkoxy, halogen, nitro or cyano groups, -(CHR)(CHR)nOR, -(CHR)nCHORCH2OR, -(CHR)(CHR)nNR2, -(CHR)nCOOR, -(CHR)(CHR)nOSi-lower alkyl, -(CHR)(CHR)n-OS(O)2-lower alkyl, -(CH2)n-CH=CF2, -CF3, -CF2-R, -CF2-lower alkenyl, -CHRF, -CHF-lower alkenyl, -(CHR)n-2,2-dimethyl-[1.3]dioxolane, -(CH2)n-2-oxo-azepan-1-yl, -(CHR)(CHR)n-morpholino, -(CHR)n-pyridino, -(CHR)(CHR)n-imidazolo, -(CHR)(CHR)n-triazolo, -(CHR)(CHR)n-pyrrolidino, optionally substituted by -(CH2)nOH, -(CHR)(CHR)n-3-hydroxy-pyrrolidino or -(CHR)(CHR)n-piperidino, or -NR2, -N(R)(CHR)n-pyridino, -N(R)C(O)O-lower alkyl, -N(CH2CF3)C(O)O-lower alkyl, -N[C(O)O-lower alkyl]2, -NR-NR-C(O)O-lower alkyl or -N(R)(CHR)nCF3, -NRCF3, -NRCF2-R, -NRCF2-lower alkenyl, -NRCHRF, -NRCHF-lower alkenyl; or is absent, if X is -N= or =N-; or R4 and R1 or R3 and R4 are interconnected to the groups -(CH2)3-5-, -(CH2)2-N=, -CH=N-N=-, -CH=CH-N=, -NH-CH=CH- or -NR-CH2-CH2- and form together with the N and C atoms to which they are attached an additional ring; R5, R6signify hydrogen, lower alkyl, lower alkoxy, amino, nitro, -SO2NH2 or halogen; or R5 and R6are interconnected to the group -O-CH2-O- and form together with the C atoms to which they are attached an additional 5-membered ring; R7, R8signify hydrogen, lower alkyl, lower alkoxy, amino, nitro or halogen; R9, R10signify hydrogen or lower alkyl; R11, R12signifies hydrogen, lower alkyl, hydroxy, lower alkoxy, lower alkoxycarbonyloxy or lower alkanoyloxy; R13, R14signify hydrogen, tritium or lower alkyl; R15, R16signifies hydrogen, tritium, lower alkyl, hydroxy, lower alkoxy, lower alkoxycarbonyloxy or lower alkanoyloxy or are together an oxo group; or Xsignifies -N=, =N-, -N<, >C= or =C<; Ysignifies -N=, =N-, -NH-, -CH= or =CH-; and the dotted line may be a bond, as well as with their pharmaceutically acceptable salts in their racemic and optically active form. It has surprisingly been found that the compounds of general formula I are antagonists at metabotropic glutamate receptors and therefore useful for the treatment of diseases related to these receptors.

本发明涉及通式如下的 1，2，4，5-四氢苯并[d]氮杂卓衍生物其中 R1表示氢、低级烷基、氧、卤素或 -OR、-O(C3-C6)环烷基、-O(CHR)n-(C3-C6)环烷基、-O(CHR)nCN、-O(CHR)nCF3、-O(CHR)(CHR)nNR2、-O(CHR)(CHR)nOR、-O(CHR)n-低级烯基、-OCF3、-OCF2-R、-OCF2-低级烯基、-OCHRF、-OCHRF、-OCHF-低级烯基、-OCF2CRF2、-OCF2Br、-O(CHR)nCF2Br、-O(CHR)n-苯基，其中苯基可任选地被一至三个低级烷基相互独立地取代、低级烷氧基、卤素、硝基或氰基、-O(CHR)(CHR)n-吗啉基、-O(CHR)(CHR)n-吡咯烷基、-O(CHR)(CHR)n-哌啶基、-O(CHR)(CHR)n-咪唑基、-O(CHR)(CHR)n-三唑、-O(CHR)n-吡啶、-O(CHR)(CHR)n-OSi-低级烷基、-O(CHR)(CHR)nOS(O)2-低级烷基、-O(CH2)nCH=CF2、-O(CHR)n-2,2-二甲基-[1.3]二氧戊环，-O(CHR)n-CHOR-CH2OR，-O(CHR)n-CHOR-(CHR)n-CH2OR 或 -SR或-S(CHR)nCOOR，或 -NR2、-N(R)(CHR)(CHR)nOR、-N(R)(CHR)nCF3、-N(R)(CHR)(CHR)n-吗啉基、-N(R)(CHR)(CHR)n-咪唑基、-N(R)(CHR)(CHR)n-吡咯烷基、-N(R)(CHR)(CHR)正-吡咯烷-2-酮，-N(R)(CHR)(CHR)正-哌啶，-N(R)(CHR)(CHR)正-三唑，-N(R)(CHR)正-吡啶，或 n 为 1-6； Rs 表示氢、低级烷基或低级烯基，彼此独立，如果存在一个以上的 R； R2 表示硝基或氰基； R3 指氢、低级烷基、=O、=S、-SR、-S(O)2-低级烷基、-(C3-C6)环烷基或哌嗪基，任选被低级烷基取代，或 -CONR2、-(CHR)nCONR2、-(CHR)nOR、-(CH2)n-CF3、-CF3、-(CHR)nOC(O)CF3、-(CHR)nCOOR、-(CHR)nSC6H5，其中苯基可任选被一至三个低级烷基相互独立地取代、低级烷氧基、卤素、硝基或氰基、-(CHR)n-1,3-二氧代-1,3-二氢-异吲哚、-(CHR)n-四氢吡喃-2-氧基或-(CHR)n-S-低级烷基，或 -NR2、-NRCO-低级烷基、-NRCHO、-N(R)(CHR)nCN、-N(R)(CHR)nCF3、-N(R)(CHR)(CHR)n-OR、-N(R)C(O)(CHR)nO-低级烷基、-NR(CHR)n-低级烷基、-NR(CHR)(CHR)n-OR、-N(R)(CHR)(CHR)n-O-苯基，其中苯基可任选被一至三个低级烷基相互独立取代、低级烷氧基、卤素、硝基或氰基、-N(R)(CHR)n-低级烯基、-N(R)(CHR)(CHR)n-O-(CHR)nOR、-N(R)(CHR)nC(O)O-低级烷基、-N(R)(CHR)nC(O)NR-低级烷基、-N(R)(CH2)n-2,2-二甲基-[1.3]二氧戊环、-N(R)(CHR)(CHR)nmorpholino、-N(R)(CHR)n-吡啶、-N(R)(CHR)(CHR)n-哌啶、-N(R)(CHR)(CHR)n-吡咯烷、-N(R)(CHR)(CHR)n-O-吡啶、-N(R)(CHR)(CHR)n-咪唑，-N(R)(CHR)n-CR2-(CHR)n-OR，-N(R)(CHR)n-CR2-OR，-N(R)(CHR)n-CHOR-CH2OR，-N(R)(CHR)n-CHOR-(CHR)n-CH2OR，或 -OR、-O(CHR)nCF3、-OCF3、-O(CHR)(CHR)n-O-苯基，其中苯基可任选被一至三个彼此独立的低级烷基、低级烷氧基、卤素、硝基或氰基、-O(CHR)(CHR)n-O-低级烷基、-O(CHR)n-吡啶基或-O(CHR)(CHR)n-吗啉基取代；以及 R4 表示氢、低级烷基、低级烯基或硝基，或 -OR、-OCF3、-OCF2-R、-OCF2-低级烯基、-OCHRF、-OCHF-低级烯基、-O(CHR)nCF3 或 -(CHR)nCHRF、-(CHR)nCF2R、-(CHR)nCF3、-(C3-C6)环烷基、-(CHR)n(C3-C6)环烷基、-(CHR)nCN、-(CHR)n-苯基，其中苯基可任选被一至三个低级烷基、低级烷氧基、卤素、硝基或氰基相互独立地取代、硝基或氰基、-(CHR)(CHR)nOR、-(CHR)nCHORCH2OR、-(CHR)(CHR)nNR2、-(CHR)nCOOR、-(CHR)(CHR)nOSi-低级烷基、-(CHR)(CHR)n-OS(O)2-低级烷基、-(CH2)n-CH=CF2、-CF3、-CF2-R、-CF2-低级烯基、-CHRF、-CHF-低级烯基、-(CHR)n-2,2-二甲基-[1.3]二氧戊环，-(CH2)n-2-氧代-氮杂卓-1-基，-(CHR)(CHR)n-吗啉基，-(CHR)n-吡啶基，-(CHR)(CHR)n-咪唑基，-(CHR)(CHR)n-三唑基、-(CHR)(CHR)n-吡咯烷，任选被-(CH2)nOH、-(CHR)(CHR)n-3-羟基吡咯烷或-(CHR)(CHR)n-哌啶取代，或 -NR2、-N(R)(CHR)n-吡啶基、-N(R)C(O)O-低级烷基、-N(CH2CF3)C(O)O-低级烷基、-N[C(O)O-低级烷基]2、-NR-NR-C(O)O-低级烷基或-N(R)(CHR)nCF3、-NRCF3、-NRCF2-R、-NRCF2-低级烯基、-NRCHRF、-NRCHF-低级烯基；如果 X 是 -N= 或 =N-，则不存在；或 R4 和 R1 或 R3 和 R4 与基团-(CH2)3-5-、-(CH2)2-N=、-CH=N-N=-、-CH=CH-N=、-NH-CH=CH-或-NR-CH2-CH2-相互连接，并与所连接的 N 原子和 C 原子一起形成一个额外的环； R5、R6 表示氢、低级烷基、低级烷氧基、氨基、硝基、-SO2NH2 或卤素；或 R5 和 R6 与基团 -O-CH2-O- 相互连接，并与所连接的 C 原子一起形成另一个 5 元环； R7、R8 表示氢、低级烷基、低级烷氧基、氨基、硝基或卤素； R9、R10 表示氢或低级烷基； R11、R12 表示氢、低级烷基、羟基、低级烷氧基、低级烷氧基羰氧基或低级烷酰氧基； R13、R14表示氢、氚或低级烷基； R15、R16 表示氢、氚、低级烷基、羟基、低级烷氧基、低级烷氧基羰氧基或低级烷酰氧基，或合在一起表示一个氧代基团；或 X表示-N=、=N-、-NC=或=C<； Y表示-N=、=N-、-NH-、-CH= 或 =CH-；以及虚线可以是键、以及外消旋和光学活性形式的药学上可接受的盐类。令人惊讶的是，通式 I 的化合物是代谢型谷氨酸受体的拮抗剂，因此可用于治疗与这些受体有关的疾病。
US4447441A

申请人：——

公开号：US4447441A

公开（公告）日：1984-05-08
US4665073A

申请人：——

公开号：US4665073A

公开（公告）日：1987-05-12

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