N-methyl-n'-nitro-n-nitrosoguanidine appears as a yellow powder. Melting point 244°F. Decomposes above 212°F. A suspected carcinogen. Extremely hazardous as a mutagen. Avoid skin contact and inhalation of of vapors. Usually stored frozen (below 32°F) in polyethylene bottles that are tightly closed and contained in a metal can. May decomposed during prolonged storage and develop sufficient pressure in a closed container to explode. Keep away from heat, sparks, and open flame.
颜色/状态：
Crystals from methanol
蒸汽压力：
1.20X10-4 mm Hg at 25 °C (est)
亨利常数：
Henry's Law constant = 1.22X10-12 atm-cu m/mol at 25 °C (est)
稳定性/保质期：
Pure compound is sensitive to light, changing to orange and green colors. Degradation products arising from prolonged or inadequate storage include N-methyl-N'-nitroguanidine, N-nitroguanidine, nitrocyanamide and guanidine. N-Methyl-N'-nitro-n-nitroso-guanidine (MNNG) is more stable than comparable alkyl-nitrosoureas and alkylnitrosourethanes. Thus, at room temp, the half life at ph 8 is about 200 hr. At ph 7.0 (phosphate buffer) and 37 °C, the half life is 170 hr. ... /It was shown that/ tap water decomposes MNNG much more rapidly than does deionized water.
分解：
Hazardous decomposition products formed under fire conditions - Carbon oxides, nitrogen oxides (NOx).
After oral administration of MNNG about 90% is excreted in the urine, mostly as N-methyl-N'-nitro-guanidine, in the first 9 hr. There is evidence that denitrosation of MNNG is effected by enzymes occurring in the stomach, liver and kidney. ...
IDENTIFICATION AND USE: N-Methyl-N'-nitro-N-nitrosoguanidine (MNNG) is a solid. It is used experimentally as a carcinogen and mutagen. It was formerly used in preparation of diazomethane. HUMAN STUDIES: MNNG can induce DNA damages and many cellular defensive events, such as DNA repair, G2/M-phase arrest and apoptosis. Noticeably, diverse cellular responses were observed to occur following MNNG treatment, including nontargeted mutations at undamaged DNA bases, endoplasmic reticulum stress induction and the activation of several signal transduction pathways. ANIMAL STUDIES: Tumors of the forestomach or glandular stomach were observed in rats exposed to MNNG in the drinking water, by stomach tube, and by ip injection; in mice exposed by stomach tube; and in male hamsters and dogs exposed via the drinking water. MNNG also caused tumors of the large intestine in rats exposed by intrarectal instillation. MNNG caused tumors of the small intestine in rats exposed via the drinking water, sc injection, or ip injection and in mice exposed by ip injection. In addition, MNNG caused tumors of the liver and peritoneum in rats exposed orally (by stomach tube or drinking water) and injection-site tumors (fibrosarcoma and rhabdomyosarcoma) in rats exposed by sc injection. In mice, MNNG administered by sc injection caused benign tumors of the liver, lung, and blood vessels (hemangoendothelioma) and by dermal application caused benign and malignant skin tumors (papilloma and carcinoma). MNNG is a potent inducer of cellular stress leading to chromosomal aberrations, point mutations, and cell killing. A high frequency of mutation was induced in O6-methylguanine-DNA methyltransferase-/- cells on exposure to a relatively low dose of MNNG.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
致癌性证据
人类致癌性证据不足。动物致癌性证据充分。总体评估：2A组：该物质很可能对人类致癌。
Inadequate evidence of carcinogenicity in humans. Sufficient evidence of carcinogenicity in animals. OVERALL EVALUATION: Group 2A: The agent is probably carcinogenic to humans.
N-Methyl-N'-nitro-N-nitrosoguanidine (MNNG) is reasonably anticipated to be a human carcinogen based on sufficient evidence of carcinogenicity from studies in experimental animals.
Following an oral dose of (14)C-labeled N-methyl-N'-nitro-N-nitrosoguanidine, most of the radioactivity was excreted in the urine within 24 hrs and less than 3 percent in the feces. Less than 3 percent of the radioactivity remained in the body as acid-insoluble materials at 24 to 48 hrs.
NOVEL GLUCOKINASE ACTIVATORS AND METHODS OF USING SAME
申请人：Ryono Denis E.
公开号：US20080009465A1
公开（公告）日：2008-01-10
Compounds are provided which are phosphonate and phosphinate activators and thus are useful in treating diabetes and related diseases and have the structure
wherein
is a heteroaryl ring;
R
4
is —(CH
2
)
n
-Z-(CH
2
)
m
—PO(OR
7
)(OR
8
), —(CH
2
)
n
Z-(CH
2
)
m
—PO(OR
7
)R
g
, —(CH
2
)
n
-Z-(CH
2
)
m
—OPO(OR
7
)R
g
, —(CH
2
)
n
Z—(CH
2
)
m
—OPO(R
9
)(R
10
), or —(CH
2
)
n
Z—(CH
2
)
m
—PO(R
9
)(R
10
);
R
5
and R
6
are independently selected from H, alkyl and halogen;
Y is R
7
(CH
2
)
s
or is absent; and
X, n, Z, m, R
4
, R
5
, R
6
, R
7
, and s are as defined herein; or a pharmaceutically acceptable salt thereof.
A method for treating diabetes and related diseases employing the above compounds is also provided.
提供了磷酸酯和磷酸酯激活剂，因此在治疗糖尿病和相关疾病方面非常有用，并具有以下结构：
其中
是杂环芳基环；
R
4
为—(CH
2
)
n
-Z-(CH
2
)
m
—PO(OR
7
)(OR
8
)、—(CH
2
)
n
Z-(CH
2
)
m
—PO(OR
7
)R
g
、—(CH
2
)
n
-Z-(CH
2
)
m
—OPO(OR
7
)R
g
、—(CH
2
)
n
Z—(CH
2
)
m
—OPO(R
9
)(R
10)
或—(CH
2
)
n
Z—(CH
2
)
m
—PO(R
9
)(R
10)
；
R
5
和R
6
分别选择自H、烷基和卤素；
Y为R
7
(CH
2
)
s
或不存在；以及
X、n、Z、m、R
4
、R
5
、R
6
、R
7
和s如本文所定义；或其药用盐。
还提供了一种利用上述化合物治疗糖尿病和相关疾病的方法。
Carbon-linked substituted piperidines and derivatives thereof useful as histamine H3 antagonists
申请人：Aslanian G. Robert
公开号：US20070010513A1
公开（公告）日：2007-01-11
Disclosed are compounds of the formula
or a pharmaceutically acceptable salt thereof, wherein:
M
1
and M
3
are CH or N;
M
2
is CH, CF or N;
Y is —C(═O)—, —C(═S)—, —(CH
2
)
q
—, —C(═NOR
7
)— or —SO
1-2
—; Z is a bond or optionally substituted alkylene or alkenylene;
R
1
is H, alkyl, alkenyl, or optionally substituted cycloalkyl, aryl, heteroaryl, heterocycloalkyl or a group of the formula:
where ring A is a monoheteroaryl ring;
R
1
is optionally substituted alkyl, alkenyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl; and the remaining variables are as defined in the specification; compositions and methods of treating allergy-induced airway responses, congestion, obesity, metabolic syndrome nonalcoholic fatty liver disease, hepatic steatosis, nonalcoholic steatohepatitis, cirrhosis, hepatacellular carcinoma or cognition deficit disorders using said compounds, alone or in combination with other agents.
Nickel-catalyzed hydrocarboxylation of ynamides with CO<sub>2</sub> and H<sub>2</sub>O: observation of unexpected regioselectivity
作者：Ryohei Doi、Iman Abdullah、Takahisa Taniguchi、Nozomi Saito、Yoshihiro Sato
DOI：10.1039/c7cc03127k
日期：——
α-amino-α,β-unsaturated esters with high regioselectivities. The selective α-carboxylation of ynamides with this catalytic protocol is unexpected in view of the electronic bias of ynamides and is in sharp contrast to our previous study in which a stoichiometric amount of Ni(0) was used to form a β-carboxylated product exclusively. We revealed that this unexpected C–C bond formation was induced by the
Compounds represented by Formula (I):
1
or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.
由化学式（I）表示的化合物及其药学上可接受的盐，可作为NMDA NR2B拮抗剂，用于缓解疼痛。
Thrombin inhibitors
申请人：Merck & Co., Inc.
公开号：US06610692B1
公开（公告）日：2003-08-26
Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure:
or a pharmaceutically acceptable salt thereof, wherein b is NY or O; c is CY2 or N;
d is CY3 or N; e is CY4 or N; f is CY5 or N; g is CY6 or N; Y4, Y5, and Y6 are independently hydrogen, C1-4 alkyl, or halogen; Y1 and Y2 are independently hydrogen, C1-4 alkyl, C3-7 cycloalkyl, halogen, NH2, OH or C1-4 alkoxy, and Y3 is hydrogen, C1-4 alkyl, C3-7 cycloalkyl, halogen, —CN, NH2, OH or C1-4 alkoxy;
A is
and W, W1, R1, R3, R4, R5, X and Z are defined in the specification.
